Version May 2024
Note: Rescriptor has been discontinued in the United States for >1 year.
HIV-1 infection (part of combination): Oral: 400 mg 3 times/day. Note: Delavirdine is no longer recommended for use in the treatment of HIV (Ref).
No dosage adjustment provided in manufacturer’s labeling (has not been studied). Guidelines state that no dosage adjustment is necessary in renal impairment (Ref).
No dosage adjustment provided in manufacturer’s labeling (has not been studied). However, delavirdine is primarily metabolized by the liver, use with caution.
Refer to adult dosing.
HIV-1 infection (part of combination): Adolescents ≥16 years: Refer to adult dosing.
Adolescents ≥16 years: There are no dosage adjustments provided in manufacturer’s labeling; guidelines state that no dosage adjustment is necessary in renal impairment (Ref).
Adolescents ≥16 years: There are no dosage adjustments provided in manufacturer’s labeling (has not been studied). However, delavirdine is primarily metabolized by the liver, use with caution.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
Frequency not always defined. Frequency of adverse reactions reported from occurrence in clinical trials with delavirdine when used as part of combination antiretroviral therapy.
Cardiovascular: Cardiac arrhythmia, cardiac insufficiency, cardiac rate disturbance, cardiomyopathy, hypersensitivity angiitis, hypertension, orthostatic hypotension, peripheral vascular disease
Central nervous system: Headache (19% to 20%), depression (10% to 15%), anxiety (6% to 8%), cognitive dysfunction, confusion, emotional lability, hallucination, paralysis, vertigo
Dermatologic: Skin rash (16% to 32%), desquamation, erythema multiforme, fungal dermatitis, Stevens-Johnson syndrome
Endocrine & metabolic: Increased serum transaminases (2% to 5%), increased amylase (3%), increased serum bilirubin (2%), hyperglycemia, hyperkalemia, hypertriglyceridemia, hyperuricemia, hypocalcemia, hyponatremia, hypophosphatemia, increased gamma-glutamyl transferase, menstrual disease, redistribution of body fat
Gastrointestinal: Nausea (20% to 25%), vomiting (3% to 11%), abdominal pain (4% to 6%), anorexia, bloody stools, colitis, diarrhea, diverticulitis, fecal incontinence, gastroenteritis, gastrointestinal hemorrhage, gingival hemorrhage, increased serum lipase, pancreatitis, vomiting
Genitourinary: Hematuria, urinary tract infection
Hematologic & oncologic: Decreased hemoglobin (1% to 3%), prolonged prothrombin time (2%), adenopathy, bruise, eosinophilia, granulocytosis, leukopenia, pancytopenia, purpura, spleen disease, thrombocytopenia
Hepatic: Hepatomegaly, increased serum alkaline phosphatase, jaundice
Hypersensitivity: Angioedema, hypersensitivity reaction
Infection: Abscess, candidiasis (oral/vaginal), infection
Neuromuscular & skeletal: Ostealgia, tetany
Ophthalmic: Conjunctivitis
Renal: Increased serum creatinine, nephrolithiasis, renal pain
Respiratory: Bronchitis (6% to 8%), chest congestion, dyspnea, pneumonia
Miscellaneous: Fever (4% to 12%)
<1%, postmarketing and/or case reports: Acute renal failure, hemolytic anemia, hepatic failure, immune reconstitution syndrome, rhabdomyolysis
Hypersensitivity to delavirdine or any component of the formulation; concurrent use of alprazolam, astemizole, cisapride, ergot alkaloids, midazolam, pimozide, rifampin, terfenadine, or triazolam
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Concerns related to adverse effects:
• Fat redistribution: May cause redistribution of fat (eg, buffalo hump, peripheral wasting with increased abdominal girth, cushingoid appearance).
• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) later in therapy; further evaluation and treatment may be required.
• Rash: Occurs frequently, may require discontinuation of therapy; usually occurs within 1-3 weeks and lasts <2 weeks. Most patients may resume therapy following a treatment interruption.
Disease-related concerns:
• Hepatic impairment: Use with caution in patients with hepatic impairment.
• HIV: Appropriate use: Due to rapid emergence of resistance, delavirdine should not be used as monotherapy or as a component of an initial antiretroviral regimen; cross-resistance may be conferred to other non-nucleoside reverse transcriptase inhibitors, although potential for cross-resistance with protease inhibitors is low.
• Renal impairment: Use with caution in patients with renal impairment.
Concurrent drug therapy issues:
• High potential for interactions: Use with caution in patients taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates (see Drug Interactions); consider alternative agents that avoid or lessen the potential for CYP-mediated interactions.
Special populations:
• Pediatric: Safety and efficacy have not been established in children.
Other warnings/precautions:
• Long-term effects: The long-term effects of delavirdine are not known.
Rescriptor has been discontinued in the United States for >1 year.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Tablet, Oral, as mesylate:
Rescriptor: 200 mg [DSC]
No
Tablets (Rescriptor Oral)
200 mg (per each): $2.97
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.
Patients with achlorhydria should take the drug with an acidic beverage; antacids and delavirdine should be separated by 1 hour. A dispersion of delavirdine may be prepared by adding four 100 mg tablets to at least 3 oz of water. Allow to stand for a few minutes and stir until uniform dispersion. Drink immediately. Rinse glass and mouth, then swallow the rinse to ensure total dose administered. The 200 mg tablets should be taken intact.
Oral: Administer without regard to meals. Patients with achlorhydria should take the drug with an acidic beverage. Antacids and delavirdine should be separated by 1 hour.
100 mg tablets: May be dispersed in water prior to consumption. A dispersion may be prepared by adding four 100 mg tablets to at least 3 oz (90 mL) of water. Allow to stand for a few minutes and stir until uniform dispersion. Drink immediately. Rinse glass and mouth, then swallow the rinse to ensure total dose administered.
200 mg tablets: Administer as intact tablets; not dispersible in water.
HIV-1 infection: Treatment of HIV-1 infection in combination with at least two additional antiretroviral agents. Note: Delavirdine is no longer recommended for use in the treatment of HIV (HHS [adult] 2019).
Delavirdine may be confused with dalfampridine
Substrate of CYP2D6 (minor), CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits CYP3A4 (weak)
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 Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
ALPRAZolam: Delavirdine may increase the serum concentration of ALPRAZolam. Risk X: Avoid combination
Antacids: May decrease the serum concentration of Delavirdine. Management: Separate doses of delavirdine and antacids by at least 1 hour. Monitor for decreased delavirdine therapeutic effects with this combination. Risk D: Consider therapy modification
Astemizole: Delavirdine may increase the serum concentration of Astemizole. Risk X: Avoid combination
Atorvastatin: Delavirdine may increase the serum concentration of Atorvastatin. Risk C: Monitor therapy
CarBAMazepine: May decrease the serum concentration of Delavirdine. Risk X: Avoid combination
Cisapride: Delavirdine may increase the serum concentration of Cisapride. Risk X: Avoid combination
CycloSPORINE (Systemic): CYP3A4 Inhibitors (Weak) may increase the serum concentration of CycloSPORINE (Systemic). Risk C: Monitor therapy
CYP3A4 Inducers (Moderate): May decrease the serum concentration of Delavirdine. Risk C: Monitor therapy
CYP3A4 Inducers (Strong): May decrease the serum concentration of Delavirdine. Management: Consider avoiding this combination if possible. If concomitant use is necessary, monitor for decreased delavirdine concentrations and effects if coadministered with strong CYP3A4 inducers. Risk D: Consider therapy modification
DexAMETHasone (Systemic): May decrease the serum concentration of Delavirdine. Risk C: Monitor therapy
Dofetilide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide. Risk C: Monitor therapy
Ergonovine: Reverse Transcriptase Inhibitors (Non-Nucleoside) may increase the serum concentration of Ergonovine. Specifically, this would be most likely with delavrdine, while other Non-Nucleoside Reverse Transcriptase Inhibitors may be more likely to decrease the concentration of Ergonovine. Risk X: Avoid combination
Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): Delavirdine may increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Finerenone: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Finerenone. Risk C: Monitor therapy
Flibanserin: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Flibanserin. Risk C: Monitor therapy
Fosamprenavir: May decrease the serum concentration of Delavirdine. The active metabolite amprenavir is likely responsible for this effect. Delavirdine may increase the serum concentration of Fosamprenavir. Specifically, delavirdine may increase concentrations of the active metabolite amprenavir. Risk X: Avoid combination
Fosphenytoin: May decrease the serum concentration of Delavirdine. Risk X: Avoid combination
Histamine H2 Receptor Antagonists: May decrease the serum concentration of Delavirdine. Risk X: Avoid combination
Indinavir: Delavirdine may increase the serum concentration of Indinavir. Management: Consider reducing the indinavir dose to 600 mg every 8 hours if coadministered with delavirdine. Risk D: Consider therapy modification
Inhibitors of the Proton Pump (PPIs and PCABs): May decrease the serum concentration of Delavirdine. Management: Chronic therapy with PPIs or PCABs should be avoided in patients treated with delavirdine. The clinical significance of short-term PPI or PCAB therapy with delavirdine is uncertain, but such therapy should be undertaken with caution. Risk X: Avoid combination
Ixabepilone: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Ixabepilone. Risk C: Monitor therapy
Lemborexant: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lemborexant. Management: The maximum recommended dosage of lemborexant is 5 mg, no more than once per night, when coadministered with weak CYP3A4 inhibitors. Risk D: Consider therapy modification
Lomitapide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lomitapide. Management: Patients on lomitapide 5 mg/day may continue that dose. Patients taking lomitapide 10 mg/day or more should decrease the lomitapide dose by half. The lomitapide dose may then be titrated up to a max adult dose of 30 mg/day. Risk D: Consider therapy modification
Lonafarnib: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lonafarnib. Management: Avoid concurrent use of lonafarnib with weak CYP3A4 inhibitors. If concurrent use is unavoidable, reduce the lonafarnib dose to or continue at a dose of 115 mg/square meter. Monitor for evidence of arrhythmia, syncope, palpitations, or similar effects. Risk D: Consider therapy modification
Lopinavir: Delavirdine may increase the serum concentration of Lopinavir. Management: Consider alternatives to this combination. Safe and effective doses for coadministration have not been determined according to lopinavir/ritonavir prescribing information. Risk D: Consider therapy modification
Midazolam: Delavirdine may increase the serum concentration of Midazolam. Risk X: Avoid combination
Nelfinavir: May decrease the serum concentration of Delavirdine. Delavirdine may increase the serum concentration of Nelfinavir. Management: Consider alternatives to this combination. Safe and effective doses for coadministration have not been determined according to the nelfinavir and delavirdine prescribing information. Risk D: Consider therapy modification
NiMODipine: CYP3A4 Inhibitors (Weak) may increase the serum concentration of NiMODipine. Risk C: Monitor therapy
Nirmatrelvir and Ritonavir: Delavirdine may increase the serum concentration of Nirmatrelvir and Ritonavir. Specifically, concentrations of ritonavir may be increased. Risk C: Monitor therapy
Orlistat: May decrease the serum concentration of Antiretroviral Agents. Risk C: Monitor therapy
PHENobarbital: May decrease the serum concentration of Delavirdine. Risk X: Avoid combination
Phenytoin: May decrease the serum concentration of Delavirdine. Risk X: Avoid combination
Pimozide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide. Risk X: Avoid combination
Primidone: May decrease the serum concentration of Delavirdine. Risk X: Avoid combination
Reverse Transcriptase Inhibitors (Non-Nucleoside): May enhance the adverse/toxic effect of other Reverse Transcriptase Inhibitors (Non-Nucleoside). Reverse Transcriptase Inhibitors (Non-Nucleoside) may decrease the serum concentration of other Reverse Transcriptase Inhibitors (Non-Nucleoside). Specifically, efavirenz and nevirapine may decrease the serum concentrations of other non-nucleoside reverse transcriptase inhibitors. Reverse Transcriptase Inhibitors (Non-Nucleoside) may increase the serum concentration of other Reverse Transcriptase Inhibitors (Non-Nucleoside). Specifically, delavirdine may increase the serum concentration of etravirine. Risk X: Avoid combination
Rifabutin: May decrease the serum concentration of Delavirdine. Delavirdine may increase the serum concentration of Rifabutin. Risk X: Avoid combination
RifAMPin: May decrease the serum concentration of Delavirdine. Risk X: Avoid combination
Ritonavir: Delavirdine may increase the serum concentration of Ritonavir. Management: Consider alternatives to this combination. Safe and effective doses for coadministration have not been determined according to ritonavir prescribing information. Risk D: Consider therapy modification
Saquinavir: Delavirdine may increase the serum concentration of Saquinavir. Management: Coadministratin of saquinavir and delavirdine is not recommended. If concomitant use cannot be avoided, monitor hepatic function frequently. Risk D: Consider therapy modification
Simeprevir: Delavirdine may increase the serum concentration of Simeprevir. Risk X: Avoid combination
Simvastatin: CYP3A4 Inhibitors (Weak) may increase serum concentrations of the active metabolite(s) of Simvastatin. CYP3A4 Inhibitors (Weak) may increase the serum concentration of Simvastatin. Risk C: Monitor therapy
Sirolimus (Conventional): CYP3A4 Inhibitors (Weak) may increase the serum concentration of Sirolimus (Conventional). Risk C: Monitor therapy
Sirolimus (Protein Bound): CYP3A4 Inhibitors (Weak) may increase the serum concentration of Sirolimus (Protein Bound). Management: Reduce the dose of protein bound sirolimus to 56 mg/m2 when used concomitantly with a weak CYP3A4 inhibitor. Risk D: Consider therapy modification
St John's Wort: May decrease the serum concentration of Delavirdine. Risk X: Avoid combination
Tacrolimus (Systemic): CYP3A4 Inhibitors (Weak) may increase the serum concentration of Tacrolimus (Systemic). Risk C: Monitor therapy
Terfenadine: Delavirdine may increase the serum concentration of Terfenadine. Risk X: Avoid combination
Triazolam: Delavirdine may increase the serum concentration of Triazolam. Risk X: Avoid combination
Ubrogepant: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Ubrogepant. Management: In patients taking weak CYP3A4 inhibitors, the initial and second dose (given at least 2 hours later if needed) of ubrogepant should be limited to 50 mg. Risk D: Consider therapy modification
Contraception is not required to initiate or continue antiretroviral therapy.
Based on the Health and Humans Services (HHS) perinatal HIV guidelines, delavirdine is not one of the recommended antiretroviral agents for use in patients who are trying to conceive.
Maximum viral suppression sustained below the limits of detection prior to conception is recommended for all persons with HIV who are planning a pregnancy. Optimization of the health of the person who will become pregnant is recommended. Selection of or changes to a specific antiretroviral regimen prior to pregnancy should be done as part of a shared decision-making process. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth.
Health care providers caring for couples planning a pregnancy when 1 or both partners are diagnosed with HIV may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2023).
Outcome information specific to delavirdine use in pregnancy is no longer being reviewed and updated in the Health and Humans Services (HHS) perinatal guidelines. The HHS perinatal HIV guidelines do not recommend delavirdine as one of the antiretroviral agents for use during pregnancy.
Maternal antiretroviral therapy (ART) may be associated with adverse pregnancy outcomes including preterm birth, low birth weight, and small for gestational age infants. Actual risks may be influenced by maternal factors such as disease severity, gestational age at initiation of therapy, and specific ART regimen, therefore close fetal monitoring is recommended. Because there is clear benefit to appropriate treatment, maternal ART should not be withheld due to concerns for adverse neonatal outcomes. Long-term follow-up is recommended for all infants exposed to antiretroviral medications; children not diagnosed with HIV but who were exposed to ART in utero or as a neonate and develop significant organ system abnormalities of unknown etiology (particularly of the CNS or heart) should be evaluated for potential metabolic dysfunction.
ART is recommended for all pregnant people with HIV to maximize their health, maintain the viral load below the limit of detection, and reduce the risk of perinatal transmission. Selection of or changes to a specific antiretroviral regimen during pregnancy should be done as part of a shared decision-making process. Patients on fully suppressive regimens prior to pregnancy generally may continue the same regimen considering known pregnancy outcomes and pharmacokinetic data. Monitoring of patients who are pregnant is more frequent than in patients who are not pregnant. ART initiated during pregnancy can be modified after delivery. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth.
Data collection to monitor pregnancy and infant outcomes following exposure to ART is ongoing. Health care providers should enroll all patients exposed to antiretroviral medications during pregnancy in the Antiretroviral Pregnancy Registry (1-800-258-4263). Enrollment should be done as early in pregnancy as possible.
Health care providers caring for pregnant patients with HIV and their infants may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2023).
It is not known if delavirdine is present in breast milk.
Maintaining maximum viral suppression during pregnancy and postpartum decreases but does not eliminate the risk of HIV transmission via breast milk. In addition, multiclass-resistant virus has been detected in breastfeeding infants who acquire HIV despite maternal therapy. In the United States, where formula is usually accessible, affordable, safe, and sustainable, and the risk of infant mortality due to diarrhea and respiratory infections is low, the Health and Human Services perinatal HIV guidelines do not recommend breastfeeding for patients with HIV when safer infant feeding options are available. Persons with HIV who maintain an undetectable viral load while taking antiretroviral therapy (ART) should evaluate infant feeding options (formula, banked donor milk, or breastfeeding) as part of a shared decision-making process (if breastfeeding is being considered, see guidelines for measures to reduce the risk of HIV transmission). When the HIV status at delivery is not known, breast milk may be expressed and stored until a negative test is available. If HIV infection is diagnosed after breastfeeding has been initiated, breastfeeding should be discontinued immediately. Breastfeeding is not recommended for persons with HIV who are not taking ART and/or who do not have sustained viral suppression.
Information is available for counseling and managing patients with HIV who are considering breastfeeding (1-888-448-8765). In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth (HHS [perinatal] 2023).
May be taken without regard to meals.
Liver function tests if administered with saquinavir
Delavirdine binds directly to reverse transcriptase, blocking RNA-dependent and DNA-dependent DNA polymerase activities
Absorption: Rapid
Distribution: Low concentration in saliva and semen; CSF 0.4% concurrent plasma concentration
Protein binding: ~98%, primarily albumin
Metabolism: Hepatic via CYP3A4 and 2D6 (Note: May reduce CYP3A activity and inhibit its own metabolism.)
Bioavailability: Tablet: 85% as tablet; ~100% as oral slurry
Half-life elimination: 5.8 hours (range: 2 to 11 hours)
Time to peak, plasma: 1 hour
Excretion: Urine (51%, <5% as unchanged drug); feces (44%); nonlinear kinetics exhibited
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