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Ketoconazole (systemic): Pediatric drug information

Ketoconazole (systemic): Pediatric drug information
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For additional information see "Ketoconazole (systemic): Drug information" and "Ketoconazole (systemic): Patient drug information"

For abbreviations, symbols, and age group definitions show table
ALERT: US Boxed Warning
Appropriate use:

Because ketoconazole tablets have been associated with serious adverse effects, ketoconazole tablets are not indicated for the treatment of onychomycosis, cutaneous dermatophyte infections, or Candida infections. Use ketoconazole only when other effective antifungal therapy is not available or tolerated and the potential benefits are considered to outweigh the potential risks.

Hepatotoxicity:

Serious hepatotoxicity, including cases with a fatal outcome or requiring liver transplantation, has occurred with the use of oral ketoconazole. Some patients had no obvious risk factors for liver disease. Inform patients receiving this drug of the risk and closely monitor.

QT prolongation and drug interactions leading to QT prolongation:

Coadministration of the following drugs with ketoconazole is contraindicated: dofetilide, quinidine, pimozide, lurasidone, cisapride, methadone, disopyramide, dronedarone, and ranolazine. Ketoconazole can cause elevated plasma concentrations of these drugs and may prolong QT intervals, sometimes resulting in life-threatening ventricular dysrhythmias, such as torsades de pointes.

Brand Names: Canada
  • APO-Ketoconazole;
  • Ketoconazole-200;
  • TEVA-Ketoconazole
Therapeutic Category
  • Antifungal Agent, Imidazole Derivative;
  • Antifungal Agent, Oral;
  • Cortisol Synthesis Inhibitor
Dosing: Pediatric
Fungal infection

Fungal infection (systemic): Children ≥2 years and Adolescents: Oral: 3.3 to 6.6 mg/kg/day once daily; maximum daily dose: 400 mg/day; duration of therapy variable based on pathogen, patient, and disease-specific factors. Note: Usual adult dose: 200 mg/day; systemic ketoconazole should only be used when other effective antifungal therapy is not available or tolerated due to potential for serious adverse reactions.

Peripheral precocious puberty

Peripheral precocious puberty (gonadotropin-independent): Very limited data available, optimal dose not defined: Children ≥2 years and Adolescents: Oral: 10 to 20 mg/kg/day in 3 divided doses (Ref). Reported doses in patients with familial male-limited precocious puberty or McCune-Albright syndrome vary widely; however, all describe response with decreased testosterone levels and cessation of puberty; some authors report flat doses of 400 to 600 mg/day divided 2 to 3 times daily (Ref); others describe weight-based doses as high as 30 mg/kg/day in 3 divided doses (Ref).

Cushing syndrome, second-line therapy

Cushing syndrome, second-line therapy: Very limited data available: Children ≥12 years and Adolescents: Oral: Initial: 400 to 600 mg/day in 2 or 3 divided doses; doses can be increased by 200 mg/day every 7 to 28 days based on patient response (urinary or plasma cortisol) and tolerability to 800 to 1,200 mg/day in 2 or 3 divided doses (Ref). In one compassionate use trial of adult and pediatric patients with Cushing syndrome (n=108; mean age: 51.3 years; range: 11 to 86 years), median final dose of ketoconazole was 600 mg/day (range: 200 to 1,200 mg/day) in divided doses (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

Altered kidney function: Children ≥2 years and Adolescents: Oral:

Mild to severe impairment: No dosage adjustment necessary.

Hemodialysis: Minimally dialyzable: There are no dosage adjustments provided in the manufacturer's labeling; ketoconazole pharmacokinetics are not significantly altered in patients on hemodialysis, and, as a result, no dosage adjustments are necessary (Ref).

Dosing: Liver Impairment: Pediatric

Children ≥2 years and Adolescents:

Baseline hepatic impairment: There are no dosage adjustments provided in manufacturer's labeling; use with extreme caution due to risks of hepatotoxicity; use is contraindicated with acute or chronic liver disease.

Hepatotoxicity during treatment: If ALT > ULN or 30% above baseline (or if patient is symptomatic), interrupt therapy and obtain full hepatic function panel. Upon normalization of liver function, may consider resuming therapy if benefit outweighs risk (hepatotoxicity has been reported on rechallenge).

Dosing: Adult

(For additional information see "Ketoconazole (systemic): Drug information")

Cushing syndrome

Cushing syndrome (off-label use): Oral: Initial: 400 to 600 mg/day in 2 or 3 divided doses; may increase dose by 200 mg/day every 7 to 28 days up to a maximum of 1.2 g/day in 2 or 3 divided doses. Dosage range: 200 mg to 1.2 g per day; mean effective dose in most studies: 600 to 800 mg/day in 2 divided doses (Ref).

Fungal infection

Fungal infection (systemic):

Note: Reserve for when other effective antifungal therapy is not available or tolerated and the potential benefits outweigh the potential risks.

Oral: 200 mg once daily; may increase to 400 mg once daily if response is insufficient. Continue until active fungal infection is resolved; some infections may require a treatment duration of up to 6 months.

Prostate cancer, advanced

Prostate cancer, advanced (off-label use): Oral: 400 mg 3 times daily, in combination with oral hydrocortisone, until disease progression (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.

Mild to severe impairment: No dosage adjustment necessary because ketoconazole pharmacokinetics are not significantly altered in patients with kidney impairment (Ref).

Hemodialysis: Minimally dialyzable: No dosage adjustment necessary because ketoconazole pharmacokinetics are not significantly altered in patients on hemodialysis (Ref).

Dosing: Liver Impairment: Adult

Use is contraindicated in acute or chronic liver disease.

Hepatotoxicity during treatment:

US labeling: If ALT >ULN or 30% above baseline or if patient is symptomatic, interrupt therapy and obtain full hepatic function panel. Upon normalization of liver function, may consider resuming therapy if benefit outweighs risk (hepatotoxicity has been reported on rechallenge).

Canadian labeling: Discontinue therapy for liver function tests >3 times ULN or if abnormalities persist, worsen, or are associated with hepatotoxicity symptoms.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequency not always defined.

Cardiovascular: Orthostatic hypotension, peripheral edema

Central nervous system: Fatigue, insomnia, malaise, nervousness, paresthesia

Dermatologic: Pruritus (2%), alopecia, dermatitis, erythema, erythema multiforme, skin rash, urticaria, xeroderma

Endocrine & metabolic: Hot flash, hyperlipidemia, menstrual disease

Gastrointestinal: Nausea (3%), vomiting (3%), abdominal pain (1%), anorexia, constipation, dysgeusia, dyspepsia, flatulence, increased appetite, tongue discoloration, upper abdominal pain, xerostomia

Hematologic & oncologic: Decreased platelet count

Hepatic: Jaundice

Hypersensitivity: Anaphylactoid reaction

Neuromuscular & skeletal: Myalgia, weakness

Respiratory: Epistaxis

Miscellaneous: Alcohol intolerance

<1%, postmarketing, and/or case reports: Acute generalized exanthematous pustulosis, adrenocortical insufficiency (≥400 mg/day), anaphylactic shock, anaphylaxis, angioedema, arthralgia, azoospermia, bulging fontanel (infants), chills, cholestatic hepatitis, cirrhosis, decreased plasma testosterone (impaired at 800 mg/day), depression, diarrhea, dizziness, drowsiness, erectile dysfunction (doses >200-400 mg/day), fever, gynecomastia, headache, hemolytic anemia, hepatic failure, hepatic necrosis, hepatitis, hepatotoxicity, hypertriglyceridemia, hypersensitivity reaction, impotence, increased intracranial pressure (reversible), leukopenia, myopathy, papilledema, photophobia, prolonged QT interval on ECG, skin photosensitivity, suicidal tendencies, thrombocytopenia

Contraindications

Hypersensitivity to ketoconazole or any component of the formulation; acute or chronic liver disease; coadministration with alprazolam, cisapride, colchicine, disopyramide, dofetilide, dronedarone, eplerenone, ergot alkaloids (eg, dihydroergotamine, ergometrine, ergotamine, methylergometrine), felodipine, irinotecan, lovastatin, lurasidone, methadone, oral midazolam, nisoldipine, pimozide, quinidine, ranolazine, simvastatin, tolvaptan, triazolam.

Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Canadian labeling: Additional contraindications (not in US labeling): Women of childbearing potential unless effective forms of contraception are used; coadministration with astemizole or terfenadine.

Warnings/Precautions

Concerns related to adverse effects:

• Adrenal suppression: High doses of ketoconazole may depress adrenocortical function; returns to baseline upon discontinuation of therapy. Do not exceed recommended maximum dosing.

• Bone fragility: In animal studies, increased long bone fragility with cases of fracture has been observed with high-dose ketoconazole. Careful dose selection may be advisable for patients susceptible to bone fragility (eg, patients who are postmenopausal, older adults).

• Hypersensitivity reactions: Hypersensitivity reactions, including anaphylaxis and urticaria, have been reported; some reactions occurred after the initial dose.

Disease-related concerns:

• Achlorhydria: Absorption is reduced in patients with achlorhydria.

• CNS infections: Ketoconazole has poor penetration into cerebral-spinal fluid and should not be used to treat fungal meningitis.

• Hepatic impairment: Ketoconazole has been associated with hepatotoxicity, including fatal cases and cases requiring liver transplantation; some patients had no apparent risk factors for hepatic disease. Toxicity was observed after a median duration of therapy of ~4 weeks, but has also been noted after as little as 3 days; may occur when patients receive high doses for short durations or low doses for long durations. Cases have been reported in patients treated with ketoconazole for onychomycosis, cutaneous dermatophyte infections, or Candida infections. Use with caution in patients with preexisting hepatic impairment, those on prolonged therapy and/or taking other hepatotoxic drugs concurrently. Hepatic dysfunction is typically (but not always) reversible upon discontinuation.

• Prostate cancer: In European clinical trials of men with metastatic prostate cancer, fatalities were reported in a small number of study participants within 14 days of initiating high-dose ketoconazole (1,200 mg daily); a causal effect has not been established.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Generic: 200 mg

Generic Equivalent Available: US

Yes

Pricing: US

Tablets (Ketoconazole Oral)

200 mg (per each): $3.16 - $3.79

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Generic: 200 mg

Extemporaneous Preparations

20 mg/mL Oral Suspension

A 20 mg/mL oral suspension may be made with tablets and one of three different vehicles (a 1:1 mixture of Ora-Sweet® and Ora-Plus®, a 1:1 mixture of Ora-Sweet® SF and Ora-Plus®, or a 1:4 mixture of cherry syrup and Simple Syrup, NF). Crush twelve 200 mg tablets in a mortar and reduce to a fine powder. Add 20 mL of chosen vehicle and mix to a uniform paste; mix while adding the vehicle in incremental proportions to almost 120 mL; transfer to a calibrated bottle, rinse mortar with vehicle, and add quantity of vehicle sufficient to make 120 mL. Label "shake well" and "refrigerate". Stable for 60 days.

Nahata MC, Pai VB, and Hipple TF, Pediatric Drug Formulations, 5th ed, Cincinnati, OH: Harvey Whitney Books Co, 2004.
Administration: Pediatric

Oral: Administer oral tablets 2 hours prior to antacids to prevent decreased absorption due to the high pH of gastric contents. Patients with achlorhydria should administer with acidic liquid (eg, nondiet cola or orange juice).

Administration: Adult

Administer oral tablets 2 hours prior to antacids to prevent decreased absorption due to the high pH of gastric contents. Patients with achlorhydria should administer with acidic liquid (eg, soda pop).

Storage/Stability

Store at 20°C to 25°C (68°F to 77°F).

Medication Guide and/or Vaccine Information Statement (VIS)

An FDA-approved patient medication guide, which is available with the product information and at http://www.fda.gov/downloads/Drugs/DrugSafety/UCM362592.pdf, must be dispensed with this medication.

Use

Treatment of susceptible fungal infections, including blastomycosis, coccidioidomycosis, histoplasmosis, paracoccidioidomycosis, and chromomycosis in patients who have failed or who are intolerant to other antifungal therapies (FDA approved in ages ≥2 years and adults). Note: Systemic ketoconazole should only be used when other effective antifungal therapy is not available or tolerated due to potential for serious adverse reactions.

Medication Safety Issues
Sound-alike/look-alike issues:

Nizoral may be confused with Nasarel, Neoral, Nitrol

Metabolism/Transport Effects

Substrate of CYP3A4 (Major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits CYP2C19 (Weak), CYP2C8 (Weak), CYP3A4 (Strong), P-glycoprotein;

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program

Abemaciclib: Ketoconazole (Systemic) may increase serum concentration of Abemaciclib. Risk X: Avoid

Acalabrutinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Acalabrutinib. Risk X: Avoid

Acrivastine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Acrivastine. Risk C: Monitor

Adagrasib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Adagrasib. Management: Avoid use of adagrasib and strong CYP3A4 inhibitors until adagrasib concentrations have reached steady state (ie, after approximately 8 days of therapy). Risk D: Consider Therapy Modification

Ado-Trastuzumab Emtansine: CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Ado-Trastuzumab Emtansine. Specifically, strong CYP3A4 inhibitors may increase concentrations of the cytotoxic DM1 component. Management: Avoid concomitant use of ado-trastuzumab emtansine and strong CYP3A4 inhibitors when possible. Consider alternatives that do not inhibit CYP3A4 or consider administering after CYP3A4 inhibitor discontinuation. Monitor for toxicities if combined. Risk D: Consider Therapy Modification

Afatinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Afatinib. Management: If combined, administer the P-gp inhibitor simultaneously with, or after, the dose of afatinib. Monitor closely for signs and symptoms of afatinib toxicity and if the combination is not tolerated, reduce the afatinib dose by 10 mg. Risk D: Consider Therapy Modification

Alcohol (Ethyl): Ketoconazole (Systemic) may increase adverse/toxic effects of Alcohol (Ethyl). Specifically, a disulfiram-like reaction to alcohol may occur. Alcohol (Ethyl) may increase hepatotoxic effects of Ketoconazole (Systemic). Risk X: Avoid

ALfentanil: CYP3A4 Inhibitors (Strong) may increase serum concentration of ALfentanil. Management: If use of alfentanil and strong CYP3A4 inhibitors is necessary, consider dosage reduction of alfentanil until stable drug effects are achieved. Frequently monitor patients for respiratory depression and sedation when these agents are combined. Risk D: Consider Therapy Modification

Alfuzosin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Alfuzosin. Risk X: Avoid

Aliskiren: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Aliskiren. Risk C: Monitor

Alitretinoin (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Alitretinoin (Systemic). Management: Consider reducing the alitretinoin dose to 10 mg when used together with strong CYP3A4 inhibitors. Monitor for increased alitretinoin effects/toxicities if combined with a strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Almotriptan: CYP3A4 Inhibitors (Strong) may increase serum concentration of Almotriptan. Management: Limit initial almotriptan dose to 6.25 mg and maximum dose to 12.5 mg in any 24-period when used with a strong CYP3A4 inhibitor. Avoid concurrent use in patients with impaired hepatic or renal function. Risk D: Consider Therapy Modification

Alosetron: CYP3A4 Inhibitors (Strong) may increase serum concentration of Alosetron. Risk C: Monitor

ALPRAZolam: CYP3A4 Inhibitors (Strong) may increase serum concentration of ALPRAZolam. Risk X: Avoid

Amiodarone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Amiodarone. Management: Consider alternatives to use of amiodarone and strong CYP3A4 inhibitors. If combined, monitor for increased amiodarone concentrations and toxicities. Risk D: Consider Therapy Modification

AmLODIPine: CYP3A4 Inhibitors (Strong) may increase serum concentration of AmLODIPine. Risk C: Monitor

Antacids: May decrease serum concentration of Ketoconazole (Systemic). Management: Administer antacids at least 1 hour prior to, or 2 hours after, ketoconazole. Additionally, administer ketoconazole with an acidic beverage (eg, non-diet cola) and monitor patients closely for signs of inadequate clinical response to ketoconazole. Risk D: Consider Therapy Modification

Antihepaciviral Combination Products: May increase serum concentration of Ketoconazole (Systemic). Ketoconazole (Systemic) may increase serum concentration of Antihepaciviral Combination Products. Specifically, ketoconazole may increase serum concentrations of paritaprevir. Management: Limit the dose of ketoconazole to 200 mg per day in patients taking antihepaciviral combination products. Additionally, monitor for increased ketoconazole effects/toxicities and for increased paritaprevir effects/toxicities. Risk D: Consider Therapy Modification

Apixaban: Inhibitors of CYP3A4 (Strong) and P-glycoprotein may increase serum concentration of Apixaban. Management: US labeling recommends a 50% apixaban dose reduction in patients who would otherwise receive 5 or 10 mg twice daily, and avoiding in patients who would otherwise receive 2.5 mg twice daily. Canadian labeling lists any combined use as contraindicated. Risk D: Consider Therapy Modification

Aprepitant: CYP3A4 Inhibitors (Strong) may increase serum concentration of Aprepitant. Risk X: Avoid

ARIPiprazole Lauroxil: CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of ARIPiprazole Lauroxil. Management: Decrease aripiprazole lauroxil dose to next lower strength if used with strong CYP3A4 inhibitors for over 14 days. No dose adjustment needed if using the lowest dose (441 mg). Max dose is 441 mg in CYP2D6 PMs or if also taking strong CYP2D6 inhibitors. Risk D: Consider Therapy Modification

ARIPiprazole: CYP3A4 Inhibitors (Strong) may increase serum concentration of ARIPiprazole. Management: Aripiprazole dose reductions are required for indications other than major depressive disorder. Dose reductions vary based on formulation, initial starting dose, CYP2D6 genotype, and use of CYP2D6 inhibitors. See full interaction monograph for details. Risk D: Consider Therapy Modification

Artemether and Lumefantrine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Artemether and Lumefantrine. CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Artemether and Lumefantrine. Specifically, concentrations of dihydroartemisinin (DHA), the active metabolite of artemether may be increased. Risk C: Monitor

Asciminib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Asciminib. Risk C: Monitor

Atazanavir: CYP3A4 Inhibitors (Strong) may increase serum concentration of Atazanavir. Risk C: Monitor

Atogepant: CYP3A4 Inhibitors (Strong) may increase serum concentration of Atogepant. Management: For treatment of episodic migraine, the recommended atogepant dose is 10 mg once daily with a concurrent strong CYP3A4 inhibitor. If used for treatment of chronic migraine, concurrent use of atogepant with strong CYP3A4 inhibitors should be avoided. Risk D: Consider Therapy Modification

Atorvastatin: May increase adverse/toxic effects of Ketoconazole (Systemic). Specifically, there is a theoretical potential for additive effects on reducing endogenous steroid concentrations. Ketoconazole (Systemic) may increase serum concentration of Atorvastatin. Risk C: Monitor

Atovaquone: Ketoconazole (Systemic) may increase serum concentration of Atovaquone. Risk C: Monitor

Avacopan: CYP3A4 Inhibitors (Strong) may increase serum concentration of Avacopan. Management: Decrease the avacopan dose to 30 mg once daily during coadministration with strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Avanafil: CYP3A4 Inhibitors (Strong) may increase serum concentration of Avanafil. Risk X: Avoid

Avapritinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Avapritinib. Risk X: Avoid

Axitinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Axitinib. Management: Avoid concurrent use of axitinib with any strong CYP3A inhibitor whenever possible. If a strong CYP3A inhibitor must be used with axitinib, a 50% axitinib dose reduction is recommended. Risk D: Consider Therapy Modification

Barnidipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Barnidipine. Risk X: Avoid

Beclomethasone (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Beclomethasone (Systemic). Risk C: Monitor

Bedaquiline: CYP3A4 Inhibitors (Strong) may increase serum concentration of Bedaquiline. CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Bedaquiline. Risk C: Monitor

Benidipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Benidipine. Risk C: Monitor

Benperidol: CYP3A4 Inhibitors (Strong) may increase serum concentration of Benperidol. Risk C: Monitor

Benzhydrocodone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Benzhydrocodone. Specifically, the concentration of hydrocodone may be increased. Risk C: Monitor

Beta-Acetyldigoxin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Beta-Acetyldigoxin. Risk C: Monitor

Betamethasone (Nasal): CYP3A4 Inhibitors (Strong) may increase serum concentration of Betamethasone (Nasal). Risk C: Monitor

Betamethasone (Ophthalmic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Betamethasone (Ophthalmic). Risk C: Monitor

Betamethasone (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Betamethasone (Systemic). Risk C: Monitor

Betamethasone (Topical): CYP3A4 Inhibitors (Strong) may increase serum concentration of Betamethasone (Topical). Risk C: Monitor

Bilastine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Bilastine. Risk X: Avoid

Blonanserin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Blonanserin. Risk X: Avoid

Bortezomib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Bortezomib. Risk C: Monitor

Bosentan: CYP3A4 Inhibitors (Strong) may increase serum concentration of Bosentan. Risk C: Monitor

Bosutinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Bosutinib. Risk X: Avoid

Brentuximab Vedotin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Brentuximab Vedotin. Specifically, concentrations of the active monomethyl auristatin E (MMAE) component may be increased. Risk C: Monitor

Brexpiprazole: CYP3A4 Inhibitors (Strong) may increase serum concentration of Brexpiprazole. Management: Reduce brexpiprazole dose 50% with strong CYP3A4 inhibitors; reduce to 25% of usual if used with both a strong CYP3A4 inhibitor and a CYP2D6 inhibitor in patients not being treated for MDD, or strong CYP3A4 inhibitor used in a CYP2D6 poor metabolizer. Risk D: Consider Therapy Modification

Brigatinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Brigatinib. Management: Avoid concurrent use of brigatinib with strong CYP3A4 inhibitors when possible. If combination cannot be avoided, reduce the brigatinib dose by approximately 50%, rounding to the nearest tablet strength (ie, from 180 mg to 90 mg, or from 90 mg to 60 mg). Risk D: Consider Therapy Modification

Bromocriptine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Bromocriptine. Management: Consider alternatives to the use of bromocriptine with strong CYP3A4 inhibitors. If combined, monitor closely for increased bromocriptine toxicities and consider bromocriptine dose reductions. Risk D: Consider Therapy Modification

Bromperidol: CYP3A4 Inhibitors (Strong) may increase serum concentration of Bromperidol. Risk C: Monitor

Brotizolam: CYP3A4 Inhibitors (Strong) may increase serum concentration of Brotizolam. Risk C: Monitor

Budesonide (Nasal): CYP3A4 Inhibitors (Strong) may increase serum concentration of Budesonide (Nasal). Risk C: Monitor

Budesonide (Oral Inhalation): CYP3A4 Inhibitors (Strong) may increase serum concentration of Budesonide (Oral Inhalation). Management: Consider alternatives to this combination when possible. If combined, monitor for increased corticosteroid adverse effects during coadministration of inhaled budesonide and strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Budesonide (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Budesonide (Systemic). Management: Avoid the concomitant use of CYP3A4 inhibitors and oral budesonide. If patients receive both budesonide and a strong CYP3A4 inhibitor, they should be closely monitored for signs and symptoms of corticosteroid excess. Risk D: Consider Therapy Modification

Budesonide (Topical): CYP3A4 Inhibitors (Strong) may increase serum concentration of Budesonide (Topical). Risk X: Avoid

Buprenorphine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Buprenorphine. Risk C: Monitor

BusPIRone: CYP3A4 Inhibitors (Strong) may increase serum concentration of BusPIRone. Management: Limit the buspirone dose to 2.5 mg daily and monitor patients for increased buspirone effects/toxicities if combined with strong CYP3A4 inhibitors. Dose adjustments of buspirone or a strong CYP3A4 inhibitor should be based on clinical assessment. Risk D: Consider Therapy Modification

Butorphanol: CYP3A4 Inhibitors (Strong) may increase serum concentration of Butorphanol. Risk C: Monitor

Cabazitaxel: CYP3A4 Inhibitors (Strong) may increase serum concentration of Cabazitaxel. Management: Concurrent use of cabazitaxel with strong inhibitors of CYP3A4 should be avoided when possible. If such a combination must be used, consider a 25% reduction in the cabazitaxel dose. Risk D: Consider Therapy Modification

Cabozantinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Cabozantinib. Management: Avoid use of a strong CYP3A4 inhibitor with cabozantinib if possible. If combined, decrease cabozantinib capsules (Cometriq) by 40 mg from previous dose or decrease cabozantinib tablets (Cabometyx) by 20 mg from previous dose. Risk D: Consider Therapy Modification

Calcifediol: CYP3A4 Inhibitors (Strong) may increase serum concentration of Calcifediol. Risk C: Monitor

Calcitriol (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Calcitriol (Systemic). Risk C: Monitor

Cannabidiol: CYP3A4 Inhibitors (Strong) may increase serum concentration of Cannabidiol. Risk C: Monitor

Cannabis: CYP3A4 Inhibitors (Strong) may increase serum concentration of Cannabis. More specifically, tetrahydrocannabinol and cannabidiol serum concentrations may be increased. Risk C: Monitor

Capivasertib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Capivasertib. Management: Avoid concomitant use of capivasertib with strong CYP3A4 inhibitors when possible. If combined, reduce the capivasertib dose to 320 mg twice daily for 4 days, followed by 3 days off. Monitor patients closely for adverse reactions. Risk D: Consider Therapy Modification

Capmatinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Capmatinib. Risk C: Monitor

Cariprazine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Cariprazine. CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Cariprazine. Specifically, concentrations of didesmethylcariprazine (DDCAR), the primary active metabolite of cariprazine, may increase. Management: Cariprazine dose adjustments are recommended and depend upon whether a patient is initiating a strong CYP3A4 inhibitor or cariprazine, as well as cariprazine indication. See full mono for details. Some non-US labels contraindicate this combination. Risk D: Consider Therapy Modification

Celiprolol: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Celiprolol. Risk C: Monitor

Ceritinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ceritinib. Management: Avoid this combination whenever possible. If combined, the ceritinib dose should be reduced by approximately one-third (to the nearest 150 mg). Resume the prior ceritinib dose after cessation of the strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

ChlordiazePOXIDE: CYP3A4 Inhibitors (Strong) may increase serum concentration of ChlordiazePOXIDE. Risk C: Monitor

Choline C 11: Antiandrogens may decrease therapeutic effects of Choline C 11. Risk C: Monitor

Ciclesonide (Oral Inhalation): CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Ciclesonide (Oral Inhalation). Risk C: Monitor

Cilnidipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Cilnidipine. Risk C: Monitor

Cilostazol: CYP3A4 Inhibitors (Strong) may increase serum concentration of Cilostazol. Management: Decrease the dose of cilostazol to 50 mg twice daily when combined with strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Cinacalcet: CYP3A4 Inhibitors (Strong) may increase serum concentration of Cinacalcet. Risk C: Monitor

Cisapride: CYP3A4 Inhibitors (Strong) may increase serum concentration of Cisapride. Risk X: Avoid

Clarithromycin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Clarithromycin. CYP3A4 Inhibitors (Strong) may decrease active metabolite exposure of Clarithromycin. Risk C: Monitor

Clindamycin (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Clindamycin (Systemic). Risk C: Monitor

CloBAZam: CYP2C19 Inhibitors (Weak) may increase serum concentration of CloBAZam. CYP2C19 Inhibitors (Weak) may increase active metabolite exposure of CloBAZam. Risk C: Monitor

Clofazimine: May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor

ClonazePAM: CYP3A4 Inhibitors (Strong) may increase serum concentration of ClonazePAM. Risk C: Monitor

CloZAPine: CYP3A4 Inhibitors (Strong) may increase serum concentration of CloZAPine. Risk C: Monitor

Cobicistat: Ketoconazole (Systemic) may increase serum concentration of Cobicistat. Cobicistat may increase serum concentration of Ketoconazole (Systemic). Management: Limit ketoconazole to a maximum adult dose of 200 mg/day in patients being treated with the elvitegravir/cobicistat/emtricitabine/tenofovir combination product. Dosing recommendations for other cobicistat-containing products are not available. Risk D: Consider Therapy Modification

Cobimetinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Cobimetinib. Risk X: Avoid

Codeine: CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Codeine. Risk C: Monitor

Colchicine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Colchicine. Management: This combination is often contraindicated, but combined use may be permitted with dose adjustment and monitoring. Recommendations vary based on brand, indication, use of P-gp inhibitors, and hepatic/renal function. See interaction monograph for details. Risk D: Consider Therapy Modification

Colchicine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Colchicine. Colchicine distribution into certain tissues (e.g., brain) may also be increased. Management: This combination is often contraindicated, but combined use may be permitted with dose adjustment and monitoring. Recommendations vary based on brand, indication, use of CYP3A4 inhibitors, and hepatic/renal function. See interaction monograph for details. Risk D: Consider Therapy Modification

Conivaptan: CYP3A4 Inhibitors (Strong) may increase serum concentration of Conivaptan. Risk X: Avoid

Copanlisib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Copanlisib. Management: If concomitant use of copanlisib and strong CYP3A4 inhibitors cannot be avoided, reduce the copanlisib dose to 45 mg. Monitor patients for increased copanlisib effects/toxicities. Risk D: Consider Therapy Modification

Cortisone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Cortisone. Risk C: Monitor

Crizotinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Crizotinib. Management: Avoid concomitant use of crizotinib and strong CYP3A4 inhibitors whenever possible. If combined use cannot be avoided, crizotinib dose reductions are required, which vary according to indication. See full interaction monograph for details. Risk D: Consider Therapy Modification

CycloPHOSphamide: Ketoconazole (Systemic) may increase serum concentration of CycloPHOSphamide. Risk C: Monitor

CycloSPORINE (Systemic): Antifungal Agents (Azole Derivatives, Systemic) may increase serum concentration of CycloSPORINE (Systemic). Management: Consider reducing cyclosporine doses by 50% to 80% during coadministration with ketoconazole, 50% with voriconazole or itraconazole, and 25% with posaconazole. Cyclosporine dose reductions may be required with other azoles. Risk D: Consider Therapy Modification

CYP3A4 Inducers (Moderate): May decrease serum concentration of Ketoconazole (Systemic). Risk C: Monitor

CYP3A4 Inducers (Strong): May decrease serum concentration of Ketoconazole (Systemic). Management: The use of ketoconazole concurrently with or within 2 weeks of a strong CYP3A4 inducer is not recommended. If such a combination cannot be avoided, monitor patients closely for evidence of diminished clinical response to ketoconazole. Risk D: Consider Therapy Modification

CYP3A4 Inhibitors (Strong): May increase serum concentration of Ketoconazole (Systemic). Risk C: Monitor

Cyproterone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Cyproterone. Risk C: Monitor

Dabigatran Etexilate: Ketoconazole (Systemic) may increase serum concentration of Dabigatran Etexilate. Management: Dose reductions and/or avoidance of this combination may be necessary. Specific recommendations vary by renal function and indication for dabigatran. Refer to full interaction monograph for details. Risk D: Consider Therapy Modification

Dabrafenib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Dabrafenib. Management: Consider alternatives to any strong CYP3A4 inhibitor for patients being treated with dabrafenib. If such a combination cannot be avoided, monitor closely for evidence of dabrafenib-related adverse effects. Risk D: Consider Therapy Modification

Daclatasvir: CYP3A4 Inhibitors (Strong) may increase serum concentration of Daclatasvir. Management: Decrease the daclatasvir dose to 30 mg once daily if combined with a strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Dapoxetine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Dapoxetine. Risk X: Avoid

Daprodustat: CYP2C8 Inhibitors (Weak) may increase serum concentration of Daprodustat. Risk C: Monitor

Daridorexant: CYP3A4 Inhibitors (Strong) may increase serum concentration of Daridorexant. Risk X: Avoid

Darifenacin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Darifenacin. Management: Limit the darifenacin dose to no more than 7.5 mg daily if combined with strong CYP3A4 inhibitors. Monitor patients for increased darifenacin toxicities (eg, dry mouth, constipation, headache, CNS effects) when these agents are combined. Risk D: Consider Therapy Modification

Darolutamide: Inhibitors of CYP3A4 (Strong) and P-glycoprotein may increase serum concentration of Darolutamide. Risk C: Monitor

Darunavir: May increase serum concentration of Ketoconazole (Systemic). Ketoconazole (Systemic) may increase serum concentration of Darunavir. Management: Limit the adult maximum ketoconazole dose to 200 mg/day in patients receiving darunavir/ritonavir and monitor closely for ketoconazole adverse effects. Risk D: Consider Therapy Modification

Dasatinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Dasatinib. Management: This combination should be avoided if possible. If combined, decrease dasatinib dose from 140 mg to 40 mg, 100 mg to 20 mg, or 70 mg to 20 mg. For patients taking 60 mg or 40 mg daily, stop dasatinib until the CYP3A4 inhibitor is discontinued. Risk D: Consider Therapy Modification

Deflazacort: CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Deflazacort. Management: Administer one third of the recommended deflazacort dose when used together with a strong or moderate CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Delamanid: CYP3A4 Inhibitors (Strong) may increase serum concentration of Delamanid. Management: Increase ECG monitoring frequency if delamanid is combined with strong CYP3A4 inhibitors due to the risk for QTc interval prolongation. Continue frequent ECG assessments throughout full delamanid treatment period. Risk D: Consider Therapy Modification

DexAMETHasone (Ophthalmic): CYP3A4 Inhibitors (Strong) may increase serum concentration of DexAMETHasone (Ophthalmic). Risk C: Monitor

DexAMETHasone (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of DexAMETHasone (Systemic). Risk C: Monitor

DiazePAM: CYP3A4 Inhibitors (Strong) may increase serum concentration of DiazePAM. Risk C: Monitor

Diazoxide Choline: CYP3A4 Inhibitors (Strong) may increase serum concentration of Diazoxide Choline. Risk C: Monitor

Dichlorphenamide: Antifungal Agents (Azole Derivatives, Systemic) may increase hypokalemic effects of Dichlorphenamide. Risk C: Monitor

Didanosine: May decrease serum concentration of Ketoconazole (Systemic). Management: Administer oral ketoconazole at least 2 hours prior to buffered didanosine. This interaction is not expected with enteric-coated didanosine capsules since they do not contain buffering agents. Risk D: Consider Therapy Modification

Dienogest: CYP3A4 Inhibitors (Strong) may increase serum concentration of Dienogest. Risk C: Monitor

Digitoxin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Digitoxin. Risk C: Monitor

Digitoxin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Digitoxin. Risk C: Monitor

Digoxin: Ketoconazole (Systemic) may increase serum concentration of Digoxin. Risk C: Monitor

DilTIAZem: CYP3A4 Inhibitors (Strong) may increase serum concentration of DilTIAZem. Risk C: Monitor

Disopyramide: Ketoconazole (Systemic) may increase serum concentration of Disopyramide. Risk X: Avoid

DOCEtaxel: CYP3A4 Inhibitors (Strong) may increase serum concentration of DOCEtaxel. Management: Avoid the concomitant use of docetaxel and strong CYP3A4 inhibitors when possible. If combined use is unavoidable, consider a 50% docetaxel dose reduction and monitor for increased docetaxel toxicities. Risk D: Consider Therapy Modification

Dofetilide: Ketoconazole (Systemic) may increase serum concentration of Dofetilide. Risk X: Avoid

Domperidone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Domperidone. Risk X: Avoid

Doxazosin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Doxazosin. Risk C: Monitor

Doxercalciferol: CYP3A4 Inhibitors (Strong) may decrease active metabolite exposure of Doxercalciferol. Risk C: Monitor

DOXOrubicin (Conventional): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of DOXOrubicin (Conventional). Risk X: Avoid

DOXOrubicin (Liposomal): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of DOXOrubicin (Liposomal). Risk C: Monitor

DroNABinol: CYP3A4 Inhibitors (Strong) may increase serum concentration of DroNABinol. Risk C: Monitor

Dronedarone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Dronedarone. Risk X: Avoid

Dutasteride: CYP3A4 Inhibitors (Strong) may increase serum concentration of Dutasteride. Risk C: Monitor

Duvelisib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Duvelisib. Management: Reduce the dose of duvelisib to 15 mg twice a day when used together with a strong CYP3A4 inhibitor. Monitor closely for evidence of altered response to treatment. Risk D: Consider Therapy Modification

Dydrogesterone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Dydrogesterone. Risk C: Monitor

Ebastine: CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Ebastine. CYP3A4 Inhibitors (Strong) may increase serum concentration of Ebastine. Risk C: Monitor

Edoxaban: Ketoconazole (Systemic) may increase serum concentration of Edoxaban. Management: In patients treated for DVT/PE, reduce the edoxaban dose to 30 mg daily when combined with oral ketoconazole. No dose adjustment is recommended for patients treated for atrial fibrillation. Monitor for increased edoxaban toxicities (ie, bleeding). Risk D: Consider Therapy Modification

Efavirenz: May decrease serum concentration of Ketoconazole (Systemic). Management: The use of ketoconazole concurrently with or within 2 weeks of efavirenz is not recommended. If such a combination cannot be avoided, monitor patients closely for evidence of diminished clinical response to ketoconazole. Risk D: Consider Therapy Modification

Efonidipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Efonidipine. Risk C: Monitor

Elacestrant: CYP3A4 Inhibitors (Strong) may increase serum concentration of Elacestrant. Risk X: Avoid

Elagolix, Estradiol, and Norethindrone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Elagolix, Estradiol, and Norethindrone. Elagolix, Estradiol, and Norethindrone may decrease serum concentration of CYP3A4 Inhibitors (Strong). Specifically, concentrations of strong CYP3A4 inhibitors that are also CYP3A4 substrates may be decreased. Risk X: Avoid

Elagolix: CYP3A4 Inhibitors (Strong) may increase serum concentration of Elagolix. Management: Use of the elagolix 200 mg twice daily dose with a strong CYP3A4 inhibitor for longer than 1 month is not recommended. Limit combined use of the elagolix 150 mg once daily dose with a strong CYP3A4 inhibitor to a maximum of 6 months. Risk D: Consider Therapy Modification

Elbasvir and Grazoprevir: Ketoconazole (Systemic) may increase serum concentration of Elbasvir and Grazoprevir. Risk X: Avoid

Eletriptan: CYP3A4 Inhibitors (Strong) may increase serum concentration of Eletriptan. Risk X: Avoid

Elexacaftor, Tezacaftor, and Ivacaftor: CYP3A4 Inhibitors (Strong) may increase serum concentration of Elexacaftor, Tezacaftor, and Ivacaftor. Management: Administer elexacaftor/tezacaftor/ivacaftor in the morning, twice a week, 3 to 4 days apart, with no evening doses of ivacaftor alone. Specific dosing varies by age and weight. See full monograph for details. Risk D: Consider Therapy Modification

Eliglustat: CYP3A4 Inhibitors (Strong) may increase serum concentration of Eliglustat. Management: Reduce eliglustat dose to 84 mg daily in CYP2D6 EMs when used with strong CYP3A4 inhibitors. Use of strong CYP3A4 inhibitors is contraindicated in CYP2D6 IMs, PMs, or in CYP2D6 EMs who are also taking strong or moderate CYP2D6 inhibitors. Risk D: Consider Therapy Modification

Emedastine (Systemic): Ketoconazole (Systemic) may increase serum concentration of Emedastine (Systemic). Risk C: Monitor

Enasidenib: May decrease serum concentration of Antifungal Agents (Azole Derivatives, Systemic). Risk X: Avoid

Encorafenib: Ketoconazole (Systemic) may increase serum concentration of Encorafenib. Encorafenib may decrease serum concentration of Ketoconazole (Systemic). Management: Avoid use of ketoconazole with encorafenib, and for 2 weeks after encorafenib discontinuation. If combined, decrease encorafenib from 450 mg to 150 mg; or from 300 mg, 225 mg, or 150 mg to 75 mg. Additionally, monitor for reduced ketoconazole efficacy. Risk D: Consider Therapy Modification

Enfortumab Vedotin: Inhibitors of CYP3A4 (Strong) and P-glycoprotein may increase serum concentration of Enfortumab Vedotin. Specifically, concentrations of the active monomethyl auristatin E (MMAE) component may be increased. Risk C: Monitor

Ensartinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ensartinib. Risk X: Avoid

Ensartinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Ensartinib. Risk X: Avoid

Entrectinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Entrectinib. Management: Avoid strong CYP3A4 inhibitors if possible. If needed, reduce entrectinib dose to 50 mg on alternating days if starting dose 200 mg; to 50 mg/day if starting dose 300 mg or 400 mg; to 100 mg/day if starting dose 600 mg. Risk D: Consider Therapy Modification

Eplerenone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Eplerenone. Risk X: Avoid

Erdafitinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Erdafitinib. Management: Avoid concomitant use of erdafitinib and strong CYP3A4 inhibitors when possible. If combined, monitor closely for erdafitinib adverse reactions and consider dose modifications accordingly. Risk D: Consider Therapy Modification

Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): CYP3A4 Inhibitors (Strong) may increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid

Erlotinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Erlotinib. Management: Avoid use of this combination when possible. When the combination must be used, monitor the patient closely for the development of erlotinib-associated adverse reactions, and if such severe reactions occur, reduce the erlotinib dose (in 50 mg decrements). Risk D: Consider Therapy Modification

Erythromycin (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Erythromycin (Systemic). Management: Consider alternatives to this combination when possible. If combined, monitor for increased erythromycin effects and toxicities, including QTc interval prolongation. Risk D: Consider Therapy Modification

Esketamine (Injection): CYP3A4 Inhibitors (Strong) may increase serum concentration of Esketamine (Injection). Risk C: Monitor

Estazolam: Ketoconazole (Systemic) may increase serum concentration of Estazolam. Risk X: Avoid

Estrogen Derivatives: CYP3A4 Inhibitors (Strong) may increase serum concentration of Estrogen Derivatives. Risk C: Monitor

Eszopiclone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Eszopiclone. Management: Limit the eszopiclone dose to 2 mg daily when combined with strong CYP3A4 inhibitors and monitor for increased eszopiclone effects and toxicities (eg, somnolence, drowsiness, CNS depression). Risk D: Consider Therapy Modification

Etizolam: CYP3A4 Inhibitors (Strong) may increase serum concentration of Etizolam. Risk C: Monitor

Etoposide Phosphate: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Etoposide Phosphate. Risk C: Monitor

Etoposide: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Etoposide. Risk C: Monitor

Etravirine: Ketoconazole (Systemic) may increase serum concentration of Etravirine. Etravirine may decrease serum concentration of Ketoconazole (Systemic). Risk C: Monitor

Everolimus: Inhibitors of CYP3A4 (Strong) and P-glycoprotein may increase serum concentration of Everolimus. Risk X: Avoid

Evogliptin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Evogliptin. Risk C: Monitor

Fedratinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Fedratinib. Management: Consider alternatives when possible. If used together, decrease fedratinib dose to 200 mg/day. After the inhibitor is stopped, increase fedratinib to 300 mg/day for the first 2 weeks and then to 400 mg/day as tolerated. Risk D: Consider Therapy Modification

Felodipine: Ketoconazole (Systemic) may increase serum concentration of Felodipine. Risk X: Avoid

FentaNYL: CYP3A4 Inhibitors (Strong) may increase serum concentration of FentaNYL. Management: Consider fentanyl dose reductions when combined with a strong CYP3A4 inhibitor. Monitor for respiratory depression and sedation. Upon discontinuation of a CYP3A4 inhibitor, consider a fentanyl dose increase; monitor for signs and symptoms of withdrawal. Risk D: Consider Therapy Modification

Fesoterodine: CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Fesoterodine. Management: Limit fesoterodine doses to 4 mg daily in patients who are also receiving strong CYP3A4 inhibitors. This combination is not recommended in pediatric patients weighing 25 kg up to 35 kg. Risk D: Consider Therapy Modification

Fexinidazole: CYP3A4 Inhibitors (Strong) may decrease active metabolite exposure of Fexinidazole. Management: Avoid use of fexinidazole and strong CYP3A4 inhibitors when possible. If combined, monitor for reduced fexinidazole efficacy. Risk D: Consider Therapy Modification

Fimasartan: Ketoconazole (Systemic) may increase serum concentration of Fimasartan. Risk C: Monitor

Finerenone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Finerenone. Risk X: Avoid

Fingolimod: Ketoconazole (Systemic) may increase serum concentration of Fingolimod. Ketoconazole (Systemic) may increase active metabolite exposure of Fingolimod. Risk C: Monitor

Flibanserin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Flibanserin. Management: Use of flibanserin with strong CYP3A4 inhibitors is contraindicated. If starting flibanserin, start 2 weeks after the last dose of the CYP3A4 inhibitor. If starting a CYP3A4 inhibitor, start 2 days after the last dose of flibanserin. Risk X: Avoid

Flotufolastat F18: Coadministration of Antiandrogens and Flotufolastat F18 may alter diagnostic results. Management: Therapies targeting the androgen pathway may result in changes in the uptake of flotufolastat F18 in prostate cancer. The impact of these therapies on the performance of flotufolastat F18 is unknown; consider use of alternative agents. Risk D: Consider Therapy Modification

Flunitrazepam: CYP3A4 Inhibitors (Strong) may increase serum concentration of Flunitrazepam. Risk C: Monitor

Fluticasone (Nasal): CYP3A4 Inhibitors (Strong) may increase serum concentration of Fluticasone (Nasal). Risk X: Avoid

Fluticasone (Oral Inhalation): CYP3A4 Inhibitors (Strong) may increase serum concentration of Fluticasone (Oral Inhalation). Management: Consider alternatives to this combination if possible. Coadministration of fluticasone propionate and strong CYP3A4 inhibitors is not recommended. If combined, monitor patients for systemic corticosteroid adverse effects (eg, adrenal suppression). Risk D: Consider Therapy Modification

Fluticasone (Topical): CYP3A4 Inhibitors (Strong) may increase serum concentration of Fluticasone (Topical). Risk C: Monitor

Fosamprenavir: May increase serum concentration of Ketoconazole (Systemic). Ketoconazole (Systemic) may increase active metabolite exposure of Fosamprenavir. Specifically, amprenavir concentrations may be increased. Management: Limit the adult maximum ketoconazole dose to 200 mg/day with fosamprenavir/ritonavir. In patients receiving fosamprenavir without ritonavir, patients receiving greater than 400 mg/day ketoconazole may also require dose reduction. Risk D: Consider Therapy Modification

Fosaprepitant: CYP3A4 Inhibitors (Strong) may increase serum concentration of Fosaprepitant. Risk X: Avoid

Fostamatinib: CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Fostamatinib. Risk C: Monitor

Fusidic Acid (Systemic): May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider Therapy Modification

Futibatinib: Inhibitors of CYP3A4 (Strong) and P-glycoprotein may increase serum concentration of Futibatinib. Risk X: Avoid

Gallium Ga 68 PSMA-11: Antiandrogens may decrease therapeutic effects of Gallium Ga 68 PSMA-11. Management: Therapies targeting the androgen pathway may result in changes in the uptake of gallium Ga 68 PSMA-11 (gozetotide) in prostate cancer. The impact on the performance of gallium Ga 68 PSMA-11 (gozetotide) is unknown; consider use of alternative agents. Risk D: Consider Therapy Modification

Gefitinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Gefitinib. Risk C: Monitor

Gepirone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Gepirone. Risk X: Avoid

Gepotidacin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Gepotidacin. Management: Avoid coadministration of gepotidacin and strong CYP3A4 inhibitors if possible. If coadministration cannot be avoided, conduct a baseline ECG, monitor closely for altered electrolytes, and correct electrolyte abnormalities as needed. Risk D: Consider Therapy Modification

Gilteritinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Gilteritinib. Management: Consider alternatives to the use of a strong CYP3A4 inhibitor with gilteritinib. If the combination cannot be avoided, monitor more closely for evidence of gilteritinib toxicities. Risk D: Consider Therapy Modification

Glasdegib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Glasdegib. Management: Consider alternatives to this combination when possible. If the combination must be used, monitor closely for evidence of QT interval prolongation and other adverse reactions to glasdegib. Risk D: Consider Therapy Modification

Glecaprevir and Pibrentasvir: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Glecaprevir and Pibrentasvir. Risk C: Monitor

GuanFACINE: CYP3A4 Inhibitors (Strong) may increase serum concentration of GuanFACINE. Management: Reduce the extended-release guanfacine dose 50% when combined with a strong CYP3A4 inhibitor. Monitor for increased guanfacine toxicities when these agents are combined. Risk D: Consider Therapy Modification

Halofantrine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Halofantrine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for halofantrine toxicities, including QTc interval prolongation. Risk D: Consider Therapy Modification

Haloperidol: CYP3A4 Inhibitors (Strong) may increase serum concentration of Haloperidol. Risk C: Monitor

Haloperidol: QT-prolonging Agents (Indeterminate Risk - Caution) may increase QTc-prolonging effects of Haloperidol. Risk C: Monitor

Histamine H2 Receptor Antagonists: May decrease serum concentration of Ketoconazole (Systemic). Management: Administer ketoconazole with an acidic beverage (eg, non-diet cola) and monitor for reduced efficacy if concomitant use with a H2RA is required. Increases in ketoconazole dose may be required. Risk D: Consider Therapy Modification

Hormonal Contraceptives: CYP3A4 Inhibitors (Strong) may increase serum concentration of Hormonal Contraceptives. Risk C: Monitor

HYDROcodone: CYP3A4 Inhibitors (Strong) may increase serum concentration of HYDROcodone. Risk C: Monitor

Hydrocortisone (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Hydrocortisone (Systemic). Risk C: Monitor

Hyoscyamine: May decrease serum concentration of Ketoconazole (Systemic). Management: Take hyoscyamine at least 2 hours after ingestion of ketoconazole. Monitor for decreased therapeutic effects of ketoconazole if used together with hyoscyamine. Risk D: Consider Therapy Modification

Ibrexafungerp: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ibrexafungerp. Management: Decrease the ibrexafungerp dose to 150 mg every 12 hours for 2 doses in patients receiving strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Ibrutinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ibrutinib. Management: Avoid concomitant use of ibrutinib and strong CYP3A4 inhibitors. If a strong CYP3A4 inhibitor must be used short-term (eg, anti-infectives for 7 days or less), interrupt ibrutinib therapy until the strong CYP3A4 inhibitor is discontinued. Risk X: Avoid

Idelalisib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Idelalisib. Management: Use alternative therapies that are not strong CYP3A4 inhibitors whenever possible. If unable to use alternative drugs, monitor patients more frequently for idelalisib toxicities. Risk D: Consider Therapy Modification

Ifosfamide: CYP3A4 Inhibitors (Strong) may increase adverse/toxic effects of Ifosfamide. CYP3A4 Inhibitors (Strong) may decrease active metabolite exposure of Ifosfamide. Risk C: Monitor

Iloperidone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Iloperidone. CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Iloperidone. Specifically, concentrations of the metabolites P88 and P95 may be increased. Management: Reduce iloperidone dose by half when administered with a strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Imatinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Imatinib. Risk C: Monitor

Imidafenacin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Imidafenacin. Risk C: Monitor

Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies): May increase hepatotoxic effects of Ketoconazole (Systemic). Risk C: Monitor

Indinavir: Ketoconazole (Systemic) may increase serum concentration of Indinavir. Indinavir may increase serum concentration of Ketoconazole (Systemic). Management: Reduce the indinavir dose to 600 mg every 8 hours when given with ketoconazole. Monitor for increased systemic effects (including adverse/toxic effects) of ketoconazole. Risk D: Consider Therapy Modification

Indium 111 Capromab Pendetide: Coadministration of Antiandrogens and Indium 111 Capromab Pendetide may alter diagnostic results. Risk X: Avoid

Inhibitors of the Proton Pump (PPIs and PCABs): Ketoconazole (Systemic) may increase serum concentration of Inhibitors of the Proton Pump (PPIs and PCABs). Inhibitors of the Proton Pump (PPIs and PCABs) may decrease absorption of Ketoconazole (Systemic). Management: Administer ketoconazole with an acidic beverage, such as non-diet cola, to increase gastric acidity and improve absorption if concomitant use with proton pump inhibitors or potassium-competitive acid blockers is necessary. Risk D: Consider Therapy Modification

Irinotecan Products: Ketoconazole (Systemic) may increase active metabolite exposure of Irinotecan Products. Specifically, serum concentrations of SN-38 may be increased. Risk X: Avoid

Isavuconazonium Sulfate: CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Isavuconazonium Sulfate. Specifically, CYP3A4 Inhibitors (Strong) may increase isavuconazole serum concentrations. Risk X: Avoid

Isoniazid: May decrease serum concentration of Ketoconazole (Systemic). Management: Avoid use of isoniazid from 2 weeks before and during treatment with ketoconazole when possible. If potential benefits outweigh the risks, monitor closely for reduced clinical response to ketoconazole and adjust the ketoconazole dose as needed. Risk D: Consider Therapy Modification

Isradipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Isradipine. Risk C: Monitor

Istradefylline: CYP3A4 Inhibitors (Strong) may increase serum concentration of Istradefylline. Management: Limit the maximum istradefylline dose to 20 mg daily when combined with strong CYP3A4 inhibitors and monitor for increased istradefylline effects/toxicities. Risk D: Consider Therapy Modification

Itraconazole: CYP3A4 Inhibitors (Strong) may increase serum concentration of Itraconazole. Risk C: Monitor

Ivabradine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ivabradine. Risk X: Avoid

Ivacaftor: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ivacaftor. Management: Ivacaftor dose reductions are required; consult full drug interaction monograph content for age- and weight-specific recommendations. Risk D: Consider Therapy Modification

Ivosidenib: Ketoconazole (Systemic) may increase serum concentration of Ivosidenib. Ivosidenib may decrease serum concentration of Ketoconazole (Systemic). Risk X: Avoid

Ixabepilone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ixabepilone. Management: Avoid use of ixabepilone and strong CYP3A4 inhibitors when possible. If combined, reduce the ixabepilone dose to 20 mg/m2. The previous ixabepilone dose can be resumed 1 week after discontinuation of the strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Ketamine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ketamine. Risk C: Monitor

Lacidipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Lacidipine. Risk C: Monitor

Lapatinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Lapatinib. Management: Avoid use of lapatinib and strong CYP3A4 inhibitors when possible. If combined, a reduced lapatinib dose of 500 mg daily should be considered. The previous lapatinib dose can be resumed 1 week after discontinuation of the strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Larotrectinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Larotrectinib. Management: Avoid use of strong CYP3A4 inhibitors with larotrectinib. If this combination cannot be avoided, reduce the larotrectinib dose by 50%. Increase to previous dose after stopping the inhibitor after a period of 3 to 5 times the inhibitor's half-life. Risk D: Consider Therapy Modification

Lefamulin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Lefamulin. Management: Avoid concomitant use of lefamulin tablets and strong inhibitors of CYP3A4. Risk X: Avoid

Lemborexant: CYP3A4 Inhibitors (Strong) may increase serum concentration of Lemborexant. Risk X: Avoid

Leniolisib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Leniolisib. Risk X: Avoid

Lenvatinib: Ketoconazole (Systemic) may increase QTc-prolonging effects of Lenvatinib. Ketoconazole (Systemic) may increase serum concentration of Lenvatinib. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor

Lercanidipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Lercanidipine. Risk X: Avoid

Leuprolide and Norethindrone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Leuprolide and Norethindrone. Specifically, concentrations of norethindrone may increase. Risk C: Monitor

Levamlodipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Levamlodipine. Risk C: Monitor

Levobupivacaine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Levobupivacaine. Risk C: Monitor

Levoketoconazole: CYP3A4 Inhibitors (Strong) may increase serum concentration of Levoketoconazole. Risk X: Avoid

Levomethadone: Ketoconazole (Systemic) may increase serum concentration of Levomethadone. Risk C: Monitor

Levomilnacipran: CYP3A4 Inhibitors (Strong) may increase serum concentration of Levomilnacipran. Management: The dose of levomilnacipran should not exceed 80 mg once daily when used with strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Lidocaine (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Lidocaine (Systemic). Risk C: Monitor

Lomitapide: CYP3A4 Inhibitors (Strong) may increase serum concentration of Lomitapide. Risk X: Avoid

Lonafarnib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Lonafarnib. Risk X: Avoid

Lopinavir: Ketoconazole (Systemic) may increase serum concentration of Lopinavir. Lopinavir may increase serum concentration of Ketoconazole (Systemic). Management: Ketoconazole doses greater than 200 mg/day are not recommended in combination with lopinavir/ritonavir. Risk D: Consider Therapy Modification

Loratadine: Ketoconazole (Systemic) may increase serum concentration of Loratadine. Risk C: Monitor

Lorlatinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Lorlatinib. Management: Avoid use of lorlatinib with strong CYP3A4 inhibitors. If the combination cannot be avoided, reduce the lorlatinib dose from 100 mg once daily to 75 mg once daily, or from 75 mg once daily to 50 mg once daily. Risk D: Consider Therapy Modification

Lovastatin: CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Lovastatin. CYP3A4 Inhibitors (Strong) may increase serum concentration of Lovastatin. Risk X: Avoid

Lumacaftor and Ivacaftor: Ketoconazole (Systemic) may increase serum concentration of Lumacaftor and Ivacaftor. Lumacaftor and Ivacaftor may decrease serum concentration of Ketoconazole (Systemic). Management: Consider alternatives to this combination. If combined, monitor for reduced ketoconazole serum concentrations and efficacy. If lumacaftor/ivacaftor is initiated in patients taking ketoconazole, lumacaftor/ivacaftor dose reductions are needed. Risk D: Consider Therapy Modification

Lumateperone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Lumateperone. Management: Limit the lumateperone dose to 10.5 mg once daily when used with a strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Lurasidone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Lurasidone. Risk X: Avoid

Lurbinectedin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Lurbinectedin. Management: Avoid concomitant use of lurbinectedin and strong CYP3A4 inhibitors. If coadministration with a strong CYP3A4 inhibitor cannot be avoided, reduce the lurbinectedin dose by 50%. Risk D: Consider Therapy Modification

Macitentan: CYP3A4 Inhibitors (Strong) may increase serum concentration of Macitentan. Risk X: Avoid

Manidipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Manidipine. Management: Consider avoiding concomitant use of manidipine and strong CYP3A4 inhibitors. If combined, monitor closely for increased manidipine effects and toxicities. Manidipine dose reductions may be required. Risk D: Consider Therapy Modification

Maraviroc: CYP3A4 Inhibitors (Strong) may increase serum concentration of Maraviroc. Management: Reduce maraviroc to 150mg twice/day in adult and pediatrics weighing 40kg or more. See full interaction monograph for dose adjustments in pediatrics weighing 10 to less than 40kg. Do not use if CrCl less than 30mL/min or in those weighing less than 10 kg. Risk D: Consider Therapy Modification

Mavacamten: CYP2C19 Inhibitors (Weak) may increase serum concentration of Mavacamten. Management: Start mavacamten at 5 mg/day if stable on a weak CYP2C19 inhibitor, and reduce the mavacamten dose by one dose level if initiating a weak CYP2C19 inhibitor. Avoid initiating weak CYP2C19 inhibitors in patients on mavacamten 2.5 mg/day. Risk D: Consider Therapy Modification

Mavacamten: CYP3A4 Inhibitors (Strong) may increase serum concentration of Mavacamten. Management: For patients on stable therapy with a strong CYP3A4 inhibitor initiate mavacamten at 2.5 mg daily. For patients initiating a strong CYP3A4 inhibitor during mavacamten therapy, dose reductions are recommended. See full mono for details. Risk D: Consider Therapy Modification

Mavorixafor: CYP3A4 Inhibitors (Strong) may increase serum concentration of Mavorixafor. Management: Decrease the mavorixafor dose to 200 mg daily if combined with strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Mefloquine: Ketoconazole (Systemic) may increase serum concentration of Mefloquine. Risk X: Avoid

Meperidine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Meperidine. Risk C: Monitor

Methadone: Ketoconazole (Systemic) may increase serum concentration of Methadone. Risk X: Avoid

MethylPREDNISolone: CYP3A4 Inhibitors (Strong) may increase serum concentration of MethylPREDNISolone. Risk C: Monitor

Midazolam: Ketoconazole (Systemic) may increase serum concentration of Midazolam. Management: Oral midazolam is contraindicated with ketoconazole. Avoid use with nasal midazolam. Consider alternatives to use with other routes of midazolam (IV, IM) when possible. Consider use of lower midazolam doses if combined. Risk X: Avoid

Midostaurin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Midostaurin. Management: Seek alternatives to the concomitant use of midostaurin and strong CYP3A4 inhibitors if possible. If concomitant use cannot be avoided, monitor patients for increased risk of adverse reactions. Risk D: Consider Therapy Modification

MiFEPRIStone: CYP3A4 Inhibitors (Strong) may increase serum concentration of MiFEPRIStone. Management: For treatment of hyperglycemia in Cushing's syndrome, start mifepristone at 300 mg/day, may titrate to a maximum of 900 mg/day. If starting a strong CYP3A4 inhibitor and taking > 300 mg/day mifepristone, decrease the mifepristone dose by 300 mg/day. Risk D: Consider Therapy Modification

Mirodenafil: CYP3A4 Inhibitors (Strong) may increase serum concentration of Mirodenafil. Management: Consider using a lower dose of mirodenafil when used with strong CYP3A4 inhibitors. Monitor for increased mirodenafil effects/toxicities with the use of this combination. Risk D: Consider Therapy Modification

Mirtazapine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Mirtazapine. Risk C: Monitor

Mirvetuximab Soravtansine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Mirvetuximab Soravtansine. Risk C: Monitor

Mitapivat: CYP3A4 Inhibitors (Strong) may increase serum concentration of Mitapivat. Risk X: Avoid

Mizolastine: Antifungal Agents (Azole Derivatives, Systemic) may increase serum concentration of Mizolastine. Risk X: Avoid

Mobocertinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Mobocertinib. CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Mobocertinib. Risk X: Avoid

Mometasone (Nasal): CYP3A4 Inhibitors (Strong) may increase serum concentration of Mometasone (Nasal). Risk C: Monitor

Mometasone (Oral Inhalation): CYP3A4 Inhibitors (Strong) may increase serum concentration of Mometasone (Oral Inhalation). Risk C: Monitor

Mometasone (Topical): CYP3A4 Inhibitors (Strong) may increase serum concentration of Mometasone (Topical). Risk C: Monitor

Morphine (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Morphine (Systemic). Risk C: Monitor

Nadolol: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Nadolol. Risk C: Monitor

Naldemedine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Naldemedine. Risk C: Monitor

Nalfurafine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Nalfurafine. Risk C: Monitor

Naloxegol: CYP3A4 Inhibitors (Strong) may increase serum concentration of Naloxegol. Risk X: Avoid

Nelfinavir: CYP3A4 Inhibitors (Strong) may increase serum concentration of Nelfinavir. Risk C: Monitor

Neratinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Neratinib. Risk X: Avoid

Nevirapine: May decrease serum concentration of Ketoconazole (Systemic). Management: Avoid use of nevirapine in the 2 weeks prior to and during ketoconazole therapy unless benefits outweigh the risk of diminished ketoconazole efficacy. Monitor ketoconazole efficacy and consider dose increases if combined. Risk D: Consider Therapy Modification

NiCARdipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of NiCARdipine. Risk C: Monitor

NIFEdipine (Topical): CYP3A4 Inhibitors (Strong) may increase serum concentration of NIFEdipine (Topical). Risk X: Avoid

NIFEdipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of NIFEdipine. Management: Consider alternatives to this combination when possible. If combined, initiate nifedipine at the lowest dose available and monitor patients closely for increased nifedipine effects and toxicities (eg, hypotension, edema). Risk D: Consider Therapy Modification

Nilotinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Nilotinib. Management: Avoid if possible. If coadministration cannot be avoided, nilotinib dose adjustments are recommended and depend on the dosage form of nilotinib used and indication treated. See full monograph for details. Risk D: Consider Therapy Modification

Nilvadipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Nilvadipine. Risk C: Monitor

NiMODipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of NiMODipine. Risk X: Avoid

Nintedanib: Inhibitors of CYP3A4 (Strong) and P-glycoprotein may increase serum concentration of Nintedanib. Risk C: Monitor

Nirmatrelvir and Ritonavir: Ketoconazole (Systemic) may increase serum concentration of Nirmatrelvir and Ritonavir. Nirmatrelvir and Ritonavir may increase serum concentration of Ketoconazole (Systemic). Risk C: Monitor

Nirogacestat: CYP3A4 Inhibitors (Strong) may increase serum concentration of Nirogacestat. Risk X: Avoid

Nisoldipine: Ketoconazole (Systemic) may increase serum concentration of Nisoldipine. Risk X: Avoid

Nitrendipine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Nitrendipine. Risk C: Monitor

Olaparib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Olaparib. Management: Avoid use of strong CYP3A4 inhibitors with olaparib, if possible. If such concurrent use cannot be avoided, the dose of olaparib tablets should be reduced to 100 mg twice daily and the dose of olaparib capsules should be reduced to 150 mg twice daily. Risk D: Consider Therapy Modification

Oliceridine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Oliceridine. Risk C: Monitor

Olmutinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Olmutinib. Risk C: Monitor

Omaveloxolone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Omaveloxolone. Management: Avoid this combination if possible. If coadministration is required, decrease the omaveloxolone dose to 50 mg daily and monitor closely for adverse reactions. Discontinue coadministration if adverse reactions occur. Risk D: Consider Therapy Modification

Ornidazole: Ketoconazole (Systemic) may increase serum concentration of Ornidazole. Risk C: Monitor

Osilodrostat: CYP3A4 Inhibitors (Strong) may increase serum concentration of Osilodrostat. Management: Reduce osilodrostat dose by 50% during coadministration with a strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Ospemifene: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ospemifene. Risk C: Monitor

OxyBUTYnin: CYP3A4 Inhibitors (Strong) may increase serum concentration of OxyBUTYnin. Risk C: Monitor

OxyCODONE: CYP3A4 Inhibitors (Strong) may increase adverse/toxic effects of OxyCODONE. CYP3A4 Inhibitors (Strong) may increase serum concentration of OxyCODONE. Serum concentrations of the active metabolite oxymorphone may also be increased. Risk C: Monitor

PACLitaxel (Conventional): CYP3A4 Inhibitors (Strong) may increase serum concentration of PACLitaxel (Conventional). Risk C: Monitor

PACLitaxel (Protein Bound): CYP3A4 Inhibitors (Strong) may increase serum concentration of PACLitaxel (Protein Bound). Risk C: Monitor

Pacritinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Pacritinib. Risk X: Avoid

Palbociclib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Palbociclib. Management: Avoid concurrent use of strong CYP3A4 inhibitors with palbociclib when possible. If the use of a strong CYP3A4 inhibitor cannot be avoided, decrease the palbociclib dose to 75 mg/day. Risk D: Consider Therapy Modification

Palovarotene: CYP3A4 Inhibitors (Strong) may increase serum concentration of Palovarotene. Risk X: Avoid

Panobinostat: CYP3A4 Inhibitors (Strong) may increase serum concentration of Panobinostat. Management: Reduce the panobinostat dose to 10 mg when it must be used with a strong CYP3A4 inhibitor. Monitor patient response to therapy closely for evidence of more severe adverse effects related to panobinostat therapy. Risk D: Consider Therapy Modification

Parecoxib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Parecoxib. Specifically, serum concentrations of the active moiety valdecoxib may be increased. Risk C: Monitor

Paricalcitol: CYP3A4 Inhibitors (Strong) may increase serum concentration of Paricalcitol. Risk C: Monitor

PAZOPanib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of PAZOPanib. Risk X: Avoid

Pemigatinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Pemigatinib. Management: If combined use cannot be avoided, reduce the pemigatinib dose from 13.5 mg daily to 9 mg daily, or from 9 mg daily to 4.5 mg daily. Resume prior pemigatinib dose after stopping the strong inhibitor once 3 half-lives of the inhibitor has passed. Risk D: Consider Therapy Modification

Pexidartinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Pexidartinib. Management: If combined use cannot be avoided, pexidartinib dose should be reduced as follows: reduce pexidartinib doses of 500 mg or 375 mg daily to 125 mg twice daily; reduce pexidartinib 250 mg daily to 125 mg once daily. Risk D: Consider Therapy Modification

Piflufolastat F18: Coadministration of Antiandrogens and Piflufolastat F18 may alter diagnostic results. Management: Therapies targeting the androgen pathway may result in changes in the uptake of piflufolastat F18 in prostate cancer. The impact of these therapies on the performance of piflufolastat F18 is unknown; consider use of alternative agents. Risk D: Consider Therapy Modification

Pimavanserin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Pimavanserin. Management: Decrease the pimavanserin dose to 10 mg daily when combined with strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Pimecrolimus: CYP3A4 Inhibitors (Strong) may decrease metabolism of Pimecrolimus. Risk C: Monitor

Pimozide: CYP3A4 Inhibitors (Strong) may increase serum concentration of Pimozide. Risk X: Avoid

Piperaquine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Piperaquine. Risk C: Monitor

Pirtobrutinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Pirtobrutinib. Management: Avoid concomitant use when possible. If combined, reduce the pirtobrutinib dose by 50 mg. If current dose is 50 mg, interrupt pirtobrutinib treatment during strong CYP3A4 inhibitor use. Risk D: Consider Therapy Modification

Polatuzumab Vedotin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Polatuzumab Vedotin. Exposure to unconjugated MMAE, the cytotoxic small molecule component of polatuzumab vedotin, may be increased. Risk C: Monitor

PONATinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of PONATinib. Management: Avoid concomitant use if possible. If combined, reduce ponatinib dose as follows: If taking 45 mg, reduce to 30 mg; if taking 30 mg, reduce to 15 mg; if taking 15 mg, reduce to 10 mg. If taking 10 mg, avoid concomitant use with strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Pralsetinib: Inhibitors of CYP3A4 (Strong) and P-glycoprotein may increase serum concentration of Pralsetinib. Management: Avoid concomitant use if possible. If combined, reduce the pralsetinib dose. If taking 400 mg or 300 mg once daily, reduce to 200 mg once daily. If taking 200 mg once daily, reduce to 100 mg once daily. Risk D: Consider Therapy Modification

Prazepam: CYP3A4 Inhibitors (Strong) may increase serum concentration of Prazepam. Risk C: Monitor

Praziquantel: CYP3A4 Inhibitors (Strong) may increase serum concentration of Praziquantel. Risk C: Monitor

PrednisoLONE (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of PrednisoLONE (Systemic). Risk C: Monitor

PredniSONE: CYP3A4 Inhibitors (Strong) may increase serum concentration of PredniSONE. Risk C: Monitor

Propafenone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Propafenone. Risk C: Monitor

QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor

QUEtiapine: CYP3A4 Inhibitors (Strong) may increase serum concentration of QUEtiapine. Management: In quetiapine treated patients, reduce quetiapine to one-sixth of original dose after starting a strong CYP3A4 inhibitor. In those on strong CYP3A4 inhibitors, start quetiapine at lowest dose and up-titrate as needed. Risk D: Consider Therapy Modification

Quinidine (Non-Therapeutic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Quinidine (Non-Therapeutic). Risk C: Monitor

QuiNIDine: Ketoconazole (Systemic) may increase QTc-prolonging effects of QuiNIDine. Ketoconazole (Systemic) may increase serum concentration of QuiNIDine. Risk X: Avoid

QuiNINE: CYP3A4 Inhibitors (Strong) may increase serum concentration of QuiNINE. Risk C: Monitor

Quizartinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Quizartinib. Management: If combination is necessary, reduce quizartinib dose as follows: from 53 mg daily to 26.5 mg daily; from 35.4 mg daily to 17.7 mg daily; from 26.5 mg daily to 17.7 mg daily. If taking 17.7 mg daily avoid quizartinib while on the strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Radotinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Radotinib. Risk X: Avoid

Ramelteon: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ramelteon. Risk C: Monitor

Ranolazine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ranolazine. Risk X: Avoid

Reboxetine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Reboxetine. Risk C: Monitor

Red Yeast Rice: CYP3A4 Inhibitors (Strong) may increase serum concentration of Red Yeast Rice. Specifically, concentrations of lovastatin and related compounds found in Red Yeast Rice may be increased. Risk X: Avoid

Regorafenib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Regorafenib. CYP3A4 Inhibitors (Strong) may decrease active metabolite exposure of Regorafenib. Risk X: Avoid

Relugolix, Estradiol, and Norethindrone: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Relugolix, Estradiol, and Norethindrone. Management: Avoid use of relugolix/estradiol/norethindrone with P-glycoprotein (P-gp) inhibitors. If concomitant use is unavoidable, relugolix/estradiol/norethindrone should be administered at least 6 hours before the P-gp inhibitor. Risk D: Consider Therapy Modification

Relugolix: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Relugolix. Management: Avoid coadministration of relugolix with oral P-gp inhibitors whenever possible. If combined, take relugolix at least 6 hours prior to the P-gp inhibitor and monitor patients more frequently for adverse reactions. Risk D: Consider Therapy Modification

Repaglinide: CYP3A4 Inhibitors (Strong) may increase serum concentration of Repaglinide. Risk C: Monitor

Repotrectinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Repotrectinib. Risk X: Avoid

Retapamulin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Retapamulin. Management: The use of retapamulin with strong CYP3A4 inhibitors is not recommended in patients less than 2 years old. No action is required in other populations. Risk C: Monitor

Revumenib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Revumenib. Management: If combined use is required, decrease revumenib dose for patients weighing 40 kg or more to 160 mg orally twice/day; for patients weighing less than 40 kg to 95 mg/m2 twice daily. Risk D: Consider Therapy Modification

Ribociclib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ribociclib. Management: Avoid use of ribociclib with strong CYP3A4 inhibitors when possible; if combined use cannot be avoided, reduce ribociclib dose to 400 mg once daily in advanced or metastatic breast cancer; reduce ribociclib dose to 200 mg daily in early breast cancer. Risk D: Consider Therapy Modification

Rifabutin: May decrease serum concentration of Ketoconazole (Systemic). Ketoconazole (Systemic) may increase serum concentration of Rifabutin. Management: The use of ketoconazole concurrently with or within 2 weeks of rifabutin is not recommended. If combined, monitor patients closely for evidence of diminished clinical response to ketoconazole and for increased rifabutin toxicities. Risk D: Consider Therapy Modification

RifAXIMin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of RifAXIMin. Risk C: Monitor

Rilpivirine: Ketoconazole (Systemic) may increase serum concentration of Rilpivirine. Rilpivirine may decrease serum concentration of Ketoconazole (Systemic). Risk C: Monitor

Rimegepant: CYP3A4 Inhibitors (Strong) may increase serum concentration of Rimegepant. Risk X: Avoid

Riociguat: Inhibitors of CYP3A4 (Strong) and P-glycoprotein may increase serum concentration of Riociguat. Management: Consider a riociguat starting dose of 0.5 mg 3 times a day when initiating riociguat in patients receiving strong CYP3A4 and P-gp inhibitors. Monitor for hypotension when these agents are combined and reduce the riociguat dose as needed. Risk D: Consider Therapy Modification

Ripretinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ripretinib. CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Ripretinib. Risk C: Monitor

RisperiDONE: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of RisperiDONE. Risk C: Monitor

Ritonavir: May increase serum concentration of Ketoconazole (Systemic). Management: Limit the adult maximum ketoconazole dose to 200 mg/day in patients receiving ritonavir. Risk D: Consider Therapy Modification

Rivaroxaban: Inhibitors of CYP3A4 (Strong) and P-glycoprotein may increase serum concentration of Rivaroxaban. Risk X: Avoid

Roflumilast-Containing Products: CYP3A4 Inhibitors (Strong) may increase serum concentration of Roflumilast-Containing Products. Risk C: Monitor

RomiDEPsin: CYP3A4 Inhibitors (Strong) may increase serum concentration of RomiDEPsin. Risk C: Monitor

Rupatadine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Rupatadine. Risk X: Avoid

Ruxolitinib (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Ruxolitinib (Systemic). Management: This combination should be avoided under some circumstances; dose adjustments may be required in some circumstances and depend on the indication for ruxolitinib. See monograph for details. Risk D: Consider Therapy Modification

Ruxolitinib (Topical): CYP3A4 Inhibitors (Strong) may increase serum concentration of Ruxolitinib (Topical). Risk X: Avoid

Saccharomyces boulardii: Antifungal Agents (Systemic and Oral [Non-Absorbable]) may decrease therapeutic effects of Saccharomyces boulardii. Risk X: Avoid

Salmeterol: CYP3A4 Inhibitors (Strong) may increase serum concentration of Salmeterol. Risk X: Avoid

Saquinavir: May increase serum concentration of Ketoconazole (Systemic). Ketoconazole (Systemic) may increase serum concentration of Saquinavir. Management: Limit the adult maximum ketoconazole dose to 200 mg/day in patients receiving saquinavir/ritonavir. Risk D: Consider Therapy Modification

SAXagliptin: CYP3A4 Inhibitors (Strong) may increase serum concentration of SAXagliptin. Management: Limit the saxagliptin dose to 2.5 mg daily when combined with strong CYP3A4 inhibitors. When using the saxagliptin combination products saxagliptin/dapagliflozin or saxagliptin/dapagliflozin/metformin, avoid use with strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Selpercatinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Selpercatinib. Management: Avoid combination if possible. If use is necessary, reduce selpercatinib dose as follows: from 120 mg twice/day to 40 mg twice/day, or from 160 mg twice/day to 80 mg twice/day. Risk D: Consider Therapy Modification

Selumetinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Selumetinib. Management: Avoid concomitant use when possible. If combined, selumetinib dose reductions are recommended and vary based on body surface area and selumetinib dose. For details, see the full drug interaction monograph or selumetinib prescribing information. Risk D: Consider Therapy Modification

Sertindole: CYP3A4 Inhibitors (Strong) may increase serum concentration of Sertindole. Risk X: Avoid

Sildenafil: CYP3A4 Inhibitors (Strong) may increase serum concentration of Sildenafil. Management: Use of sildenafil for pulmonary arterial hypertension (PAH) should be avoided with strong CYP3A4 inhibitors. When used for erectile dysfunction, consider using a lower starting dose of 25 mg and monitor patients for sildenafil toxicities. Risk D: Consider Therapy Modification

Silodosin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Silodosin. Risk X: Avoid

Simeprevir: CYP3A4 Inhibitors (Strong) may increase serum concentration of Simeprevir. Risk X: Avoid

Simvastatin: CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Simvastatin. CYP3A4 Inhibitors (Strong) may increase serum concentration of Simvastatin. Risk X: Avoid

Sirolimus (Conventional): CYP3A4 Inhibitors (Strong) may increase serum concentration of Sirolimus (Conventional). Management: Avoid concurrent use of sirolimus with strong CYP3A4 inhibitors when possible and alternative agents with lesser interaction potential with sirolimus should be considered. Concomitant use of sirolimus and voriconazole or posaconazole is contraindicated. Risk D: Consider Therapy Modification

Sirolimus (Conventional): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Sirolimus (Conventional). Management: Avoid concurrent use of sirolimus with P-glycoprotein (P-gp) inhibitors when possible and alternative agents with lesser interaction potential with sirolimus should be considered. Monitor for increased sirolimus concentrations/toxicity if combined. Risk D: Consider Therapy Modification

Sirolimus (Protein Bound): CYP3A4 Inhibitors (Strong) may increase serum concentration of Sirolimus (Protein Bound). Risk X: Avoid

Sirolimus (Topical): CYP3A4 Inhibitors (Strong) may increase serum concentration of Sirolimus (Topical). Risk C: Monitor

Solifenacin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Solifenacin. Management: Limit adult solifenacin doses to 5 mg daily and limit doses in pediatric patients to the recommended weight-based starting dose (and do not increase the dose) when combined with strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Sonidegib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Sonidegib. Risk X: Avoid

Sparsentan: CYP3A4 Inhibitors (Strong) may increase serum concentration of Sparsentan. Risk X: Avoid

Sucralfate: May decrease serum concentration of Ketoconazole (Systemic). Risk C: Monitor

SUFentanil: CYP3A4 Inhibitors (Strong) may increase serum concentration of SUFentanil. Management: If a strong CYP3A4 inhibitor is initiated in a patient on sufentanil, consider a sufentanil dose reduction and monitor for increased sufentanil effects and toxicities (eg, respiratory depression). Risk D: Consider Therapy Modification

SUNItinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of SUNItinib. Management: Avoid when possible. If combined, decrease sunitinib dose to a minimum of 37.5 mg daily when treating GIST or RCC. Decrease sunitinib dose to a minimum of 25 mg daily when treating PNET. Monitor patients for both reduced efficacy and increased toxicities. Risk D: Consider Therapy Modification

Suvorexant: CYP3A4 Inhibitors (Strong) may increase serum concentration of Suvorexant. Risk X: Avoid

Suzetrigine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Suzetrigine. Risk X: Avoid

Tacrolimus (Systemic): Ketoconazole (Systemic) may increase serum concentration of Tacrolimus (Systemic). Management: Tacrolimus dose adjustment may be required; empiric dose reductions of 50% have been recommended. Monitor tacrolimus concentrations and clinical response closely. Risk D: Consider Therapy Modification

Tacrolimus (Topical): CYP3A4 Inhibitors (Strong) may increase serum concentration of Tacrolimus (Topical). Risk C: Monitor

Tadalafil: CYP3A4 Inhibitors (Strong) may increase serum concentration of Tadalafil. Management: Avoid this combination in patients taking tadalafil for pulmonary arterial hypertension. In patients taking tadalafil for ED or BPH, max tadalafil dose is 2.5 mg if taking daily or 10 mg no more frequently than every 72 hours if used as needed. Risk D: Consider Therapy Modification

Talazoparib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Talazoparib. Risk C: Monitor

Tamsulosin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Tamsulosin. Risk X: Avoid

Tasimelteon: CYP3A4 Inhibitors (Strong) may increase serum concentration of Tasimelteon. Risk C: Monitor

Tazemetostat: CYP3A4 Inhibitors (Strong) may increase serum concentration of Tazemetostat. Risk X: Avoid

Temsirolimus: CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Temsirolimus. Specifically, concentrations of sirolimus may be increased. Management: Avoid concomitant use of temsirolimus and strong CYP3A4 inhibitors. If coadministration is unavoidable, decrease temsirolimus dose to 12.5 mg per week. Resume previous temsirolimus dose 1 week after discontinuation of the strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Teneligliptin: Ketoconazole (Systemic) may increase serum concentration of Teneligliptin. Risk C: Monitor

Teniposide: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Teniposide. Risk C: Monitor

Tenofovir Disoproxil Fumarate: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Tenofovir Disoproxil Fumarate. Risk C: Monitor

Tetrahydrocannabinol and Cannabidiol: CYP3A4 Inhibitors (Strong) may increase serum concentration of Tetrahydrocannabinol and Cannabidiol. Risk C: Monitor

Tetrahydrocannabinol: CYP3A4 Inhibitors (Strong) may increase serum concentration of Tetrahydrocannabinol. Risk C: Monitor

Tezacaftor and Ivacaftor: CYP3A4 Inhibitors (Strong) may increase serum concentration of Tezacaftor and Ivacaftor. Management: If combined with strong CYP3A4 inhibitors, tezacaftor/ivacaftor should be administered in the morning, twice a week, approximately 3 to 4 days apart. Tezacaftor/ivacaftor dose depends on age and weight; see full Lexi-Interact monograph for details. Risk D: Consider Therapy Modification

Thiotepa: CYP3A4 Inhibitors (Strong) may decrease active metabolite exposure of Thiotepa. CYP3A4 Inhibitors (Strong) may increase serum concentration of Thiotepa. Management: Avoid coadministration of thiotepa and strong CYP3A4 inhibitors. If concomitant use cannot be avoided, monitor for thiotepa adverse effects and decreased efficacy. Risk D: Consider Therapy Modification

Ticagrelor: CYP3A4 Inhibitors (Strong) may decrease active metabolite exposure of Ticagrelor. CYP3A4 Inhibitors (Strong) may increase serum concentration of Ticagrelor. Risk X: Avoid

Tilidine: CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Tilidine. CYP3A4 Inhibitors (Strong) may increase serum concentration of Tilidine. Risk C: Monitor

Tipranavir: May increase serum concentration of Ketoconazole (Systemic). Management: Adult ketoconazole doses greater than 200 mg/day are not recommended in patients treated with tipranavir. Risk D: Consider Therapy Modification

Tisotumab Vedotin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Tisotumab Vedotin. Specifically, concentrations of the active monomethyl auristatin E (MMAE) component may be increased. Risk C: Monitor

Tofacitinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Tofacitinib. Management: Tofacitinib dose reductions are recommended when combined with strong CYP3A4 inhibitors. Recommended dose adjustments vary by tofacitinib formulation and therapeutic indication. See full Lexi Interact monograph for details. Risk D: Consider Therapy Modification

Tolterodine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Tolterodine. Management: The maximum recommended dose of tolterodine is 2 mg per day (1 mg twice daily for immediate-release tablets or 2 mg daily for extended-release capsules) when used together with a strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Tolvaptan: CYP3A4 Inhibitors (Strong) may increase serum concentration of Tolvaptan. Risk X: Avoid

Topotecan: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Topotecan. Risk X: Avoid

Toremifene: CYP3A4 Inhibitors (Strong) may increase serum concentration of Toremifene. Management: Use of toremifene with strong CYP3A4 inhibitors should be avoided if possible. If coadministration is necessary, monitor for increased toremifene toxicities, including QTc interval prolongation. Risk D: Consider Therapy Modification

Trabectedin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Trabectedin. Risk X: Avoid

TraMADol: CYP3A4 Inhibitors (Strong) may increase serum concentration of TraMADol. CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of TraMADol. Risk C: Monitor

TraZODone: CYP3A4 Inhibitors (Strong) may increase serum concentration of TraZODone. Management: Consider the use of a lower trazodone dose and monitor for increased trazodone effects (eg, sedation, QTc prolongation) if combined with strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Tretinoin (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Tretinoin (Systemic). Management: Avoid use of tretinoin and strong CYP3A4 inhibitors when possible. If combined, monitor for increased tretinoin concentrations and toxicities (eg, pseudotumor cerebri, hypercalcemia). Risk D: Consider Therapy Modification

Triamcinolone (Nasal): CYP3A4 Inhibitors (Strong) may increase serum concentration of Triamcinolone (Nasal). Risk C: Monitor

Triamcinolone (Ophthalmic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Triamcinolone (Ophthalmic). Risk C: Monitor

Triamcinolone (Systemic): CYP3A4 Inhibitors (Strong) may increase serum concentration of Triamcinolone (Systemic). Management: Consider alternatives to this combination when possible. If combined, monitor for increased corticosteroid adverse effects during coadministration of triamcinolone and strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Triamcinolone (Topical): CYP3A4 Inhibitors (Strong) may increase serum concentration of Triamcinolone (Topical). Risk C: Monitor

Triazolam: CYP3A4 Inhibitors (Strong) may increase serum concentration of Triazolam. Risk X: Avoid

Ubrogepant: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ubrogepant. Risk X: Avoid

Udenafil: CYP3A4 Inhibitors (Strong) may increase serum concentration of Udenafil. Risk X: Avoid

Ulipristal: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ulipristal. Risk C: Monitor

Upadacitinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Upadacitinib. Management: Upadacitinib dose adjustments are often needed when combined with strong CYP3A4 inhibitors. Specific adjustments vary based on upadacitinib indication. See full interact monograph for details. Risk D: Consider Therapy Modification

Valbenazine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Valbenazine. CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Valbenazine. Management: Reduce the valbenazine dose to 40 mg daily when combined with strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Vamorolone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Vamorolone. Management: Reduce the vamorolone dose to 4 mg/kg daily, with a maximum dose of 200 mg daily for patients weighing over 50 kg, when combined with strong CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Vanzacaftor, Tezacaftor, and Deutivacaftor: CYP3A4 Inhibitors (Strong) may increase serum concentration of Vanzacaftor, Tezacaftor, and Deutivacaftor. Management: Age- and weight-specific dose reductions of vanzacaftor, tezacaftor, and deutivacaftor are recommended. Please see full Interact monograph or labeling for details. Risk D: Consider Therapy Modification

Vardenafil: Ketoconazole (Systemic) may increase serum concentration of Vardenafil. Management: Limit Levitra (vardenafil) dose to 5 mg per 24 hours with ketoconazole 200 mg/day and 2.5 mg per 24 hours with ketoconazole 400 mg/day. Avoid concomitant use of Staxyn (vardenafil) and ketoconazole. Combined use is contraindicated outside of the US. Risk D: Consider Therapy Modification

Vemurafenib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Vemurafenib. Management: Avoid concurrent use of vemurafenib with strong CYP3A4 inhibitors when possible. If concomitant use is unavoidable, consider a vemurafenib dose reduction if clinically indicated. Risk D: Consider Therapy Modification

Venetoclax: CYP3A4 Inhibitors (Strong) may increase serum concentration of Venetoclax. Management: Coadministration is contraindicated during venetoclax initiation and ramp-up in CLL/SLL patients. Reduced venetoclax doses are required during ramp-up for patients with AML, and all maintenance therapy. See full Lexi Interact monograph for details. Risk D: Consider Therapy Modification

Verapamil: CYP3A4 Inhibitors (Strong) may increase serum concentration of Verapamil. Risk C: Monitor

Vilanterol: CYP3A4 Inhibitors (Strong) may increase serum concentration of Vilanterol. Risk C: Monitor

Vilazodone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Vilazodone. Management: Limit the maximum vilazodone dose to 20 mg daily in patients receiving strong CYP3A4 inhibitors. The original vilazodone dose can be resumed following discontinuation of the strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

VinBLAStine: CYP3A4 Inhibitors (Strong) may increase serum concentration of VinBLAStine. Risk C: Monitor

VinCRIStine: CYP3A4 Inhibitors (Strong) may increase serum concentration of VinCRIStine. Risk X: Avoid

Vindesine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Vindesine. Risk C: Monitor

Vinflunine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Vinflunine. CYP3A4 Inhibitors (Strong) may increase active metabolite exposure of Vinflunine. Risk X: Avoid

Vinorelbine: CYP3A4 Inhibitors (Strong) may increase serum concentration of Vinorelbine. Risk C: Monitor

Vitamin K Antagonists: Ketoconazole (Systemic) may increase serum concentration of Vitamin K Antagonists. Risk C: Monitor

Voclosporin: CYP3A4 Inhibitors (Strong) may increase serum concentration of Voclosporin. Risk X: Avoid

Vorapaxar: CYP3A4 Inhibitors (Strong) may increase serum concentration of Vorapaxar. Risk X: Avoid

Voriconazole: CYP3A4 Inhibitors (Strong) may increase serum concentration of Voriconazole. Risk C: Monitor

Zanubrutinib: CYP3A4 Inhibitors (Strong) may increase serum concentration of Zanubrutinib. Management: Decrease the zanubrutinib dose to 80 mg once daily during coadministration with a strong CYP3A4 inhibitor. Further dose adjustments may be required for zanubrutinib toxicities, refer to prescribing information for details. Risk D: Consider Therapy Modification

Ziprasidone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Ziprasidone. Risk C: Monitor

Zolpidem: CYP3A4 Inhibitors (Strong) may increase serum concentration of Zolpidem. Risk C: Monitor

Zopiclone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Zopiclone. Management: If coadministered with strong CYP3A4 inhibitors, initiate zopiclone at 3.75 mg in adults, with a maximum dose of 5 mg. Monitor for zopiclone toxicity (eg, drowsiness, confusion, lethargy, ataxia, respiratory depression). Risk D: Consider Therapy Modification

Zuranolone: CYP3A4 Inhibitors (Strong) may increase serum concentration of Zuranolone. Management: Reduce the zuranolone dose to 30 mg once daily when used concomitantly with a strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Reproductive Considerations

Patients with Cushing syndrome often experience oligomenorrhea or amenorrhea due to the pathological cortisol excess associated with this disease. Patients treated with ketoconazole may experience a decrease in ovulatory disturbances and should be informed of the potential return of fertility (Berwaerts 1999; Bronstein 2015; Brue 2018).

The use of ketoconazole in male patients has been associated with decreased testosterone concentrations. Effects are dose related and reversible when ketoconazole is discontinued. Testosterone levels become impaired with doses of 800 mg/day. Adverse effects have included reversible gynecomastia, oligospermia, and impotence.

Pregnancy Considerations

Based on the mechanism of action, in utero ketoconazole exposure may theoretically cause adverse events in the fetus (Pilmis 2015).

Agents other than ketoconazole are recommended for the treatment of systemic fungal infections in pregnant patients (Pilmis 2015).

Untreated Cushing syndrome during pregnancy may cause adverse events in the mother and fetus. Data related to ketoconazole for the treatment of Cushing disease (off-label use) during pregnancy are limited. Medication may be considered for patients when surgery is not an option or for symptomatic control at initial diagnosis (ESE [Luger 2021]).

Monitoring Parameters

Hepatic function tests (baseline and frequently during therapy), including weekly ALT for the duration of treatment, adrenal function (as clinically appropriate).

Mechanism of Action

Alters the permeability of the cell wall by blocking fungal cytochrome P450; inhibits biosynthesis of triglycerides and phospholipids by fungi; inhibits several fungal enzymes that results in a build-up of toxic concentrations of hydrogen peroxide; also inhibits several adrenal enzymes (CYP11A1 [cholesterol side chain cleavage enzyme], CYP17 [17 alpha-hydroxylase], CYP11B1 [11 beta-hydroxylase], CYP11B2 [aldosterone synthase]) responsible for androgen and cortisol synthesis (Castinetti 2021).

Pharmacokinetics (Adult Data Unless Noted)

Distribution: Well into inflamed joint fluid, saliva, bile, urine, sebum, cerumen, feces, tendons, skin and soft tissue, and testes; crosses blood-brain barrier poorly; only negligible amounts reach CSF.

Protein binding: ~99% (mainly albumin).

Metabolism: Partially hepatic via CYP3A4 to inactive metabolites.

Bioavailability: Decreases as gastric pH increases.

Half-life elimination: Biphasic: Initial: 2 hours; Terminal: 8 hours.

Time to peak, serum: 1 to 2 hours.

Excretion: Feces (57%); urine (13% [2% to 4% unchanged]).

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Nizoral;
  • (AR) Argentina: Fitonal | Fungicil | Grenfung | Ketoconazol | Ketoconazol fabra | Ketonazol | Micoral | Orifungal | Orifungal m | Prurisedan antimicotico m | Socosep;
  • (AT) Austria: Ketoconazole hra | Nizoral;
  • (AU) Australia: Nizoral;
  • (BD) Bangladesh: Ketocon | Ketofun | Ketoral | Ketotab | Kezona;
  • (BE) Belgium: Nizoral;
  • (BF) Burkina Faso: Knz 200;
  • (BG) Bulgaria: Nizoral;
  • (BR) Brazil: Aciderm | Candoral | Cetaconal | Cetocol | Cetoconalab | Cetoconazol | Cetoderm | Cetohexal | Cetomed | Cetomicoss | Cetomizol | Cetonax | Cetoneo | Cetonil | Cetonin | Cetozan | Cetozaz | Cetozol | Conazol | Dermitrat | Fungonazol | Fungoral | Izonax | Ketacon | Ketocon | Ketomicol | Ketonan | Ketonazol | Lozan | Meradizol | Miconan | Micoral | Micotrat | Nizonazol | Nizoral | Noriderm | Noronal | Sifnazol | Sioconazol | Tonazox | Zanoc | Zolmicol;
  • (CH) Switzerland: Nizoral;
  • (CL) Chile: Eprofil | Fungarest | Fungium | Ketoconazol | Ketonil | Tructum;
  • (CN) China: Fu kang wang | Nizoral;
  • (CO) Colombia: Betascan | Ciclofung | Fazol | Fungisterol | Fungivac | Hongosil | Kectogal | Kestofungil | Ketanalin | Ketimic | Ketoconazol | Ketoconazol mk | Ketofar | Ketomed | Ketomicol | Ketoprol | Ketovac | Ketozol | Micocidin | Micotek | Mikor | Nizoral | Ovale | Unidox;
  • (CZ) Czech Republic: Nizoral | Oronazol;
  • (DE) Germany: Nizoral | Nizoral j-c;
  • (DO) Dominican Republic: Conazol | Dermoket | Fraconazol | Inaket | Ketoconazol | Ketolam | Ketonizol | Ketoprol | Ketoral | Ketozol | Ketzole | Liondox | Mikozin | Mizox | Nacozol | Nizoral | Nor-Nizal | Rapamic | Sudermal;
  • (EC) Ecuador: Chemicom | Chemicon | Fungium | Ketoconazol | Ketoconazol ariston | Ketoconazol mk | Ketoconazol R | Ketonizol | Liondox | Micosin | Nizoral | Soridermal | Tructum;
  • (EE) Estonia: Apo ketoconazole | Ketoconazole usp | Nizoral | Oronazol;
  • (EG) Egypt: Fungizol | Ketozole | Kizol | Nizoral;
  • (ES) Spain: Fungarest | Fungo | Fungo hubber | Ketoconazol ratiopharm | Ketoisdin | Micoticum | Panfungol;
  • (ET) Ethiopia: Dermazol | Ketoconazole usp;
  • (FI) Finland: Ketoconazole hra | Nizoral | Nizoral orion;
  • (FR) France: Nizoral;
  • (GB) United Kingdom: Ketoconazole hra | Nizoral;
  • (GR) Greece: Aquarius | Botaderm | Cezolin | Ebersept | Fungoral | Ilgem | Mycofebrin | Sostatin | Vafluson;
  • (HK) Hong Kong: Antanazol | Antigal | Apo ketoconazole | Diazon | Ebersept | Fungazol | Funginox | Ketocin | Ketocon | Ketozol | Kezole | Mycoral | Nizoral | Qualiketol | Scholz | Ziconal;
  • (HR) Croatia: Ketoconazole hra;
  • (HU) Hungary: Ketoconazole hra | Nizoral;
  • (ID) Indonesia: Anfuhex | Cidaral | Dexazol | Fexazol | Formyco | Funet | Fungasol | Fungoral | Grazol | Interzol | Ketoconazole 200 | Lusanoc | Micoticum | Muzoral | Mycoderm | Mycoral | Mycozid | Nizol | Nizoral | Omegzole | Picamic | Profungal | Solinfec | Thicazol | Tokasid | Wizol | Zoloral | Zoralin | Zumazol;
  • (IE) Ireland: Ketoconazole hra | Nizoral;
  • (IL) Israel: Nizoral;
  • (IN) India: Alketop | Atiket | Conkit | Ecoket | Emcon | Exket | Fungicide | Hyphoral | Kenz | Ketafung | Ketmith | Keto | Ketodac | Ketodust | Ketol | Ketostal | Ketovate | Ketovib | Ketoza | Ketozole | Ketzol | Kevon | Konaz | Nizoclin | Nizol | Nizral | Nozal | Phytoral;
  • (IT) Italy: Ketoconazole hra | Ketoconazolo | Nizoral;
  • (JO) Jordan: Kenazol | Nizoral;
  • (KE) Kenya: Carenazol | Conazole | Dermizol | Etocon | Fungicide | Hitoral | Kecozole | Kenazole | Ketarin | Ketocos | Ketomac | Ketoziral | Kezole | Kior | Konazol | Nazole | Phytoral;
  • (KR) Korea, Republic of: Antanazole | Caszol | Comozol | Dermasol | Funkil | Jr ketoconazole | Kaszol | Katonal | Kenasol | Kepazol | Ketocel | Ketonal | Ketonazole | Kezonal | Kitonal | Myzole | Nizoral | Poconazol | Smazole | Spike;
  • (KW) Kuwait: Nizoral;
  • (LB) Lebanon: Ketonaz | Nizoral;
  • (LT) Lithuania: Ketoconazol HRA | Ketozol | Nizoral | Oronazol | Sostatin;
  • (LU) Luxembourg: Nizoral;
  • (LV) Latvia: Ketoconazole hra | Ketokonazols | Ketozol | Nizoral | Oronazol | Sostatin;
  • (MA) Morocco: Nizoral;
  • (MX) Mexico: Akorazol | Conazol | Etacon | Eurolat | Fumas K | Fungocin | Fungoral | Fungosine | Honzil | Keplozol | Keprobiozol | Ketoconazol | Ketoconazol Collins | Ketoconazol gi bru | Ketoconazol gi ser | Ketoconazol Landsteiner | Ketone | Ketoril | Ketowest | Konaturil | Lizkol | Lizovag | Messelzol | Mi-Ke-Son'S-V | Micoser | Micozol | Mycocil | Mycodib | Nastil | Nizoral | Onofin-k | Prenalon | Termizol | Tiniazol | Tocomizol | Tomiko;
  • (MY) Malaysia: Antanazol | Axcel Ketoconazole | Dha-Ketozole | Diazon | Fungazol | Funginox | Keta | Ketazon | Ketobid | Ketofly | Ketosil | Ketozol | Ketozotan | Kezol | Kezoral | Nizoral | Pristinex | Sunazol | Yucomy | Zorinax;
  • (NG) Nigeria: Axoral | Dermoral | Divasoral | Fungizole | Fungral | Jvi ketoconazole | Ketoconazole marcolivia | Medcef | Truzoral;
  • (NL) Netherlands: Nizoral;
  • (NO) Norway: Fungoral;
  • (NZ) New Zealand: Nizoral;
  • (PE) Peru: Fungosin | Ketocon | Ketoconazol | Ketoconazol 200 mg | Ketomicin | Ketomicol | Konazol | Liondox | Nizoral | Oxonazol | Termizol;
  • (PH) Philippines: Donaxene | Ketovid | Konazole | Nizoral;
  • (PK) Pakistan: Alfung | Conaz | Funginil | Kare | Kenazol | Ketacon | Keto | Ketomark | Ketor | Ketorex | Ketoval | Konazole | Kz | Mycolock | Nizoral | Sostatin | Spike | Tocozole;
  • (PL) Poland: Fungores | Ketokonazol | Ketokonazole Hasco | Ketozol | Nizoral;
  • (PR) Puerto Rico: Nizoral;
  • (PT) Portugal: Cetoconazol | Frisolac | Ketoconazole hra | Nizale | Nizoral | Rapamic | Tedol;
  • (PY) Paraguay: Cetonil | Fungal | Fungium | Hongosan ket | Ketoconazol dutriec | Ketoconazol genfar | Ketoconazol millet | Ketoral | Micoplus | Nizoral;
  • (RO) Romania: Kefungin | Ketoconazol arena | Ketoconazol fabiol | Ketoconazol farmex | Ketoconazol ozone | Ketoconazole hra | Ketostin | Sostatin;
  • (RU) Russian Federation: Brizoral | Fungavis | Funginok | Fungistab | Ketoconazol | Ketoconazol ds | Ketoconazol-fpo | Mycozoral | Nizoral | Oronazol;
  • (SA) Saudi Arabia: Nizoral;
  • (SE) Sweden: Fungoral | Ketoconazole hra;
  • (SG) Singapore: Antanazol | Dha-Ketozole | Ketozole | Kezoral | Konazole | Mycoral | Nizoral | Profungal | Sunazol | Yucomy;
  • (SI) Slovenia: Oronazol;
  • (SK) Slovakia: Ketoconazole hra | Nizoral | Oronazol;
  • (SR) Suriname: Apo ketoconazole | Interzol | Ketoral | Kezole | Nizoral | Sostatin;
  • (TH) Thailand: Chintaral | Chintoral | Conazol | Dermed | Diazon | Fungasin | Fungazol | Fungiderm-k | Fungimed | Funginox | Fungiral | Fungizin | Funora | J.v. nazole | Katsin | Kazinal | Kenazol | Kenazole | Keneral | Kenoral | Ketazon | Ketocine | Ketocox | Ketolan | Ketomed | Keton | Ketonazole | Ketopac | Ketoral | Ketosil | Ketotab | Ketotop | Ketozal | Kezole | Kezomex | Kezora | Kino | Konazol | Manoketo | Masarol | Matiget | Mizoco | Mizoron | Myco-Kenazol | Mycoral | Natoral | Nazery | Nazole | Nicozone | Ninazol | Nizoral | Nora | P-Kezole | Pasalen | Pinnarol | Pipketo | Seatozol | Sporoxyl;
  • (TN) Tunisia: Ketozol | Nizoral;
  • (TR) Turkey: Fungoral | Ketoral | Nizoral;
  • (TW) Taiwan: Clear | Cotrizine | Ketazole | Ketona | Ketozol | Mecozol | Nicogus | Nizoral | Rich | Sugen | Tinuvin | Yucomy;
  • (UA) Ukraine: Dermazol | Ketozoral Darnitsa | Nizoral | Oronazol;
  • (UG) Uganda: Dermizol | Ketoren | Ketos | Ketrozol | Nazol;
  • (UY) Uruguay: Cetonil | Etrux | Fitonal | Ketoconazol Lazar | Liondox | Micoralex | Nizoral | Tructum;
  • (VE) Venezuela, Bolivarian Republic of: Kenazol | Ketazol | Ketoconazol | Ketoconazol mf | Ketocoval | Micosept | Nizoral | Noractin;
  • (VN) Viet Nam: Celtonal | Etoral;
  • (ZA) South Africa: Ketazol | Nizoral;
  • (ZM) Zambia: Dermiral | Fungicide | Ketazol | Keto 200 | Ketomex | Ketos;
  • (ZW) Zimbabwe: Knz 200 | Phytoral
  1. Almeida MQ, Brito VN, Lins TS, et al. Long-term treatment of familial male-limited precocious puberty (testotoxicosis) with cyproterone acetate or ketoconazole. Clin Endocrinol (Oxf). 2008;69(1):93-98. [PubMed 18088394]
  2. Amado JA, Pesquera C, Gonzalez EM, Otero M, Freijanes J, Alvarez A. Successful treatment with ketoconazole of Cushing's syndrome in pregnancy. Postgrad Med J. 1990;66(773):221-223. [PubMed 2362890]
  3. APO-Ketoconazole [product monograph]. Weston, Ontario: Apotex Inc; November 2021.
  4. Aronoff GR, Bennett WM, Berns JS, et al. Drug Prescribing in Renal Failure: Dosing Guidelines for Adults and Children. 5th ed. Philadelphia, PA: American College of Physicians; 2007, p 71.
  5. Basch E, Loblaw DA, Oliver TK, et al. Systemic therapy in men with metastatic castration-resistant prostate cancer: American Society of Clinical Oncology and Cancer Care Ontario clinical practice guideline. J Clin Oncol. 2014;32(30):3436-3448. [PubMed 25199761]
  6. Berwaerts J, Verhelst J, Mahler C, Abs R. Cushing's syndrome in pregnancy treated by ketoconazole: case report and review of the literature. Gynecol Endocrinol. 1999;13(3):175-182. [PubMed 10451809]
  7. Brass C, Galgiani JN, Blaschke TF, Defelice R, O'Reilly RA, Stevens DA. Disposition of ketoconazole, an oral antifungal, in humans. Antimicrob Agents Chemother. 1982;21(1):151-158. [PubMed 6282204]
  8. Bronstein MD, Machado MC, Fragoso MC. Management of endocrine disease: management of pregnant patients with Cushing's syndrome. Eur J Endocrinol. 2015;173(2):R85-R91. [PubMed 25872515]
  9. Brue T, Amodru V, Castinetti F. Management of endocrine disease: management of Cushing's syndrome during pregnancy: solved and unsolved questions. Eur J Endocrinol. 2018;178(6):R259-R266. [PubMed 29523633]
  10. Carter TC, Druschel CM, Romitti PA, et al. Antifungal drugs and the risk of selected birth defects. Am J Obstet Gynecol. 2008;198(2):191. [PubMed 18226621]
  11. Castinetti F, Guignat L, Giraud P, et al. Ketoconazole in Cushing's disease: is it worth a try? J Clin Endocrinol Metab. 2014;99(5):1623-1630. doi:10.1210/jc.2013-3628 [PubMed 24471573]
  12. Castinetti F, Nieman LK, Reincke M, Newell-Price J. Approach to the patient treated with steroidogenesis inhibitors. J Clin Endocrinol Metab. 2021;106(7):2114-2123. doi:10.1210/clinem/dgab122 [PubMed 33675650]
  13. Daneshmend TK, Warnock DW. Clinical pharmacokinetics of ketoconazole. Clin Pharmacokinet. 1988;14(1):13-34. doi:10.2165/00003088-198814010-00002 [PubMed 3280211]
  14. DeFelice R, Johnson DG, Galgiani JN. Gynecomastia with ketoconazole. Antimicrob Agents Chemother. 1981;19(6):1073-1074. [PubMed 6267997]
  15. De Pedrini P, Rapisarda R, Spanò G. The effect of ketoconazole on sebum secretion in patients suffering from acne and seborrhoea. Int J Tissue React. 1988;10(2):111-113. [PubMed 2972661]
  16. Fleseriu M, Auchus R, Bancos I, et al. Consensus on diagnosis and management of Cushing's disease: a guideline update. Lancet Diabetes Endocrinol. 2021;9(12):847-875. doi:10.1016/S2213-8587(21)00235-7 [PubMed 34687601]
  17. Galgiani JN, Ampel NM, Blair JE, et al. 2016 Infectious Diseases Society of America (IDSA) clinical practice guideline for the treatment of coccidioidomycosis. Clin Infect Dis. 2016;63(6):e112-e146. [PubMed 27470238]
  18. Ghetti P, Patrone P, Tosti A. Ketoconazole in the treatment of acne in women. Arch Dermatol. 1986;122(6):629. [PubMed 2940977]
  19. HHS Panel on Opportunistic Infections in HIV-Infected Adults and Adolescents. Guidelines for the prevention and treatment of opportunistic infections in HIV-infected adults and adolescents: recommendations from the Centers for Disease Control and Prevention, the National Institutes of Health, and the HIV Medicine Association of the Infectious Diseases Society of America. http://aidsinfo.nih.gov/contentfiles/lvguidelines/adult_oi.pdf.
  20. Holland FJ, Kirsch SE, Selby R. Gonadotropin-independent precocious puberty ("testotoxicosis"): influence of maturational status on response to ketoconazole. J Clin Endocrinol Metab. 1987;64(2):328-333. [PubMed 3539979]
  21. Janssen PA, Symoens JE. Hepatic Reactions During Ketoconazole Treatment. Am J Med. 1983;74(1B):80-85. [PubMed 6129799]
  22. Kazy Z, Puhó E, Czeizel AE. Population-based case-control study of oral ketoconazole treatment for birth outcomes. Congenit Anom (Kyoto). 2005;45(1):5-8. [PubMed 15737124]
  23. Ketoconazole [prescribing information]. Morgantown, WV: Mylan Pharmaceuticals Inc; March 2018.
  24. Ketoconazole [prescribing information]. East Brunswick, NJ: Strides Pharma Inc; May 2023.
  25. Ketoconazole [product monograph]. Weston, Ontario, Canada: Apotex Inc; April 2021.
  26. Ketoconazole [summary of product characteristics]. Chatillon, France: HRA Pharma Rare Diseases; January 2020.
  27. Kliegman RM and St. Geme J, eds. Nelson Textbook of Pediatrics. 21st ed. Philadelphia, PA: Saunders Elsevier; 2020.
  28. Lind J. Limb malformations in a case of hydrops fetalis with ketoconazole use during pregnancy. Abstracts of the 11th World Congress of Gynecology and Obstetrics (Berlin). Arch GynecoI. 1985;237(Suppl):398.
  29. Lindsay JR, Jonklaas J, Oldfield EH, Nieman LK. Cushing's syndrome during pregnancy: personal experience and review of the literature. J Clin Endocrinol Metab. 2005;90(5):3077-3083. [PubMed 15705919]
  30. Luger A, Broersen LHA, Biermasz NR, et al. ESE clinical practice guideline on functioning and nonfunctioning pituitary adenomas in pregnancy. Eur J Endocrinol. 2021;185(3):G1-G33. doi:10.1530/EJE-21-0462 [PubMed 34425558]
  31. Messina MF, Arrigo T, Wasniewska M, et al. Combined treatment with ketoconazole and cyproterone acetate in a boy with McCune-Albright syndrome and peripheral precocious puberty. J Endocrinol Invest. 2008;31(9):839-840. [PubMed 18997496]
  32. Miller JW, Crapo L. The medical treatment of Cushing's syndrome. Endocr Rev. 1993;14(4):443-458. doi:10.1210/edrv-14-4-443 [PubMed 7693447]
  33. Mølgaard-Nielsen D, Pasternak B, Hviid A. Use of oral fluconazole during pregnancy and the risk of birth defects. N Engl J Med. 2013;369(9):830-839. [PubMed 23984730]
  34. Moncet D, Morando DJ, Pitoia F, Katz SB, Rossi MA, Bruno OD. Ketoconazole therapy: an efficacious alternative to achieve eucortisolism in patients with Cushing's syndrome. Medicina (B Aires). 2007;67(1):26-31. [PubMed 17408017]
  35. Moretti ME, Ito S, Koren G. Disposition of Maternal Ketoconazole in Breast Milk. Am J Obstet Gynecol. 1995;173(5):1625-1626. [PubMed 7503214]
  36. Nizoral (ketoconazole) [prescribing information]. Titusville, NJ: Janssen Pharmaceuticals; 2014.
  37. Nieman LK, Biller BM, Findling JW, et al; Endocrine Society. Treatment of Cushing's syndrome: an Endocrine Society clinical practice guideline. J Clin Endocrinol Metab. 2015;100(8):2807-2831. doi:10.1210/jc.2015-1818 [PubMed 26222757]
  38. Norris JF, Cunliffe WJ. Effect of ketoconazole on sebum excretion rate. Arch Dermatol. 1987;123(3):301. [PubMed 2949711]
  39. Pilmis B, Jullien V, Sobel J, Lecuit M, Lortholary O, Charlier C. Antifungal drugs during pregnancy: an updated review. J Antimicrob Chemother. 2015;70(1):14-22. [PubMed 25204341]
  40. Pont A, Graybill JR, Craven PC, et al. High-dose ketoconazole therapy and adrenal and testicular function in humans. Arch Intern Med. 1984;144(11):2150-2153. [PubMed 6093722]
  41. Prebtani AP, Donat D, Ezzat S. Worrisome striae in pregnancy. Lancet. 2000;355(9216):1692. [PubMed 10905246]
  42. Ryan CJ, Halabi S, Ou SS, et al. Adrenal Androgen Levels as Predictors of Outcome in Prostate Cancer Patients Treated With Ketoconazole Plus Antiandrogen Withdrawal: Results from a Cancer and Leukemia Group B Study. Clin Cancer Res. 2007;13(7):2030-2037. [PubMed 17404083]
  43. Santen RJ, Van den Bossche H, Symoens J, Brugmans J, DeCoster R. Site of action of low dose ketoconazole on androgen biosynthesis in men. J Clin Endocrinol Metab. 1983;57(4):732-736. [PubMed 6309882]
  44. Schoelwer M, Eugster EA. Treatment of peripheral precocious puberty. Endocr Dev. 2016;29:230-239. [PubMed 26680582]
  45. Schürmeyer T, Nieschlag E. Effect of ketoconazole and other imidazole fungicides on testosterone biosynthesis. Acta Endocrinol (Copenh).1984;105(2):275-280. [PubMed 6320571]
  46. Sedlak T, Shufelt C, Iribarren C, et al. Oral Contraceptive Use and the ECG: Evidence of an Adverse QT Effect on Corrected QT Interval. Ann Noninvasive Electrocardiol. 2013;18(4):389-398. [PubMed 23879279]
  47. Small EJ, Halabi S, Dawson NA, et al. Antiandrogen Withdrawal Alone or in Combination With Ketoconazole in Androgen-Independent Prostate Cancer Patients: A Phase III Trial (CALGB 9583). J Clin Oncol. 2004;22(6):1025-1033. [PubMed 15020604]
  48. Soriano-Guillén L, Lahlou N, Chauvet G, Roger M, Chaussain JL, Carel JC. Adult height after ketoconazole treatment in patients with familial male-limited precocious puberty. J Clin Endocrinol Metab. 2005;90(1):147-151. [PubMed 15522928]
  49. Strauss JS, Krowchuk DP, Leyden JJ, et al; American Academy of Dermatology/American Academy of Dermatology Association. Guidelines of care for acne vulgaris management. J Am Acad Dermatol. 2007;56(4):651-663. [PubMed 17276540]
  50. Sugita T, Miyamoto M, Tsuboi R, Takatori K, Ikeda R, Nishikawa A. In vitro activities of azole antifungal agents against Propionibacterium acnes isolated from patients with acne vulgaris. Biol Pharm Bull. 2010;33(1):125-127. [PubMed 20045949]
  51. Syed FA, Chalew SA. Ketoconazole treatment of gonadotropin independent precocious puberty in girls with McCune-Albright syndrome: a preliminary report. J Pediatr Endocrinol Metab. 1999;12(1):81-83. [PubMed 10392352]
  52. Young J, Bertherat J, Vantyghem MC, et al. Hepatic safety of ketoconazole in Cushing's syndrome: results of a compassionate use programme in France. Eur J Endocrinol. 2018;178(5):447-458. [PubMed 29472378]
  53. Venturoli S, Fabbri R, Dal Prato L, et al. Ketoconazole therapy for women with acne and/or hirsutism. J Clin Endocrinol Metab. 1990;71(2):335-339. [PubMed 2166069]
  54. Zaenglein AL, Pathy AL, Schlosser BJ, et al. Guidelines of care for the management of acne vulgaris. J Am Acad Dermatol. 2016;74(5):945-973.e33. [PubMed 26897386]
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