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Istradefylline: Drug information

Istradefylline: Drug information
(For additional information see "Istradefylline: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Nourianz
Pharmacologic Category
  • Anti-Parkinson Agent, Adenosine Receptor Antagonist
Dosing: Adult
Parkinson disease, "off" episode

Parkinson disease, "off" episode: Oral: 20 mg once daily; may further increase dose based on response and tolerability to a maximum dose of 40 mg once daily.

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

Dosage adjustment for concomitant tobacco smoking (≥20 cigarettes/day or the equivalent amount of another tobacco product): 40 mg once daily.

Dosing: Kidney Impairment: Adult

CrCl ≥15 mL/minute: No dosage adjustment necessary.

CrCl <15 mL/minute: Has not been studied.

End-stage renal disease requiring hemodialysis: Has not been studied.

Dosing: Hepatic Impairment: Adult

Mild hepatic impairment (Child-Pugh class A): No dosage adjustment necessary.

Moderate hepatic impairment (Child-Pugh class B): 20 mg once daily (maximum dose: 20 mg/day).

Severe hepatic impairment (Child-Pugh class C): Avoid use; has not been studied.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequencies noted refer to experience with combination therapy.

>10%: Neuromuscular & skeletal: Dyskinesia (15% to 17%)

1% to 10%:

Central nervous system: Insomnia (6%), dizziness (3% to 6%), auditory hallucination (≤6%), hallucination (≤6%), visual hallucination (≤6%), abnormal behavior (≤2%), abnormality in thinking (≤2%), aggressive behavior (≤2%), agitation (≤2%), confusion (≤2%), delirium (≤2%), delusion (≤2%), disorientation (≤2%), mania (≤2%), paranoid ideation (≤2%)

Dermatologic: Skin rash (2%)

Endocrine & metabolic: Increased serum glucose (1% to 2%)

Gastrointestinal: Nausea (6%), constipation (5% to 6%), decreased appetite (3%), diarrhea (2%)

Hepatic: Increased serum alkaline phosphatase (2%)

Renal: Increased blood urea nitrogen (1% to 2%)

Respiratory: Upper respiratory tract inflammation (1% to 2%)

<1%: Impulse control disorder

Postmarketing: Increased libido

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Warnings/Precautions

Concerns related to adverse effects:

• Dyskinesias: May cause or exacerbate dyskinesias. Use with caution in patients with preexisting dyskinesias.

• Impulse control disorders: Has been associated with compulsive behaviors and/or loss of impulse control, which has manifested as pathological gambling, compulsive buying, libido increases (hypersexuality), binge eating, and/or other intense urges. Dose reduction or discontinuation of therapy has been reported to reverse these behaviors.

• Psychotic effects: May cause or exacerbate mental status and behavioral changes, which may be severe, including psychotic-like behavior during treatment or after starting or increasing the dose; manifestations may include paranoid ideation, delusions, hallucinations, confusion, psychotic-like behavior, disorientation, aggressive behavior, agitation, and delirium. Avoid use in patients with a major psychotic disorder.

Disease-related concerns:

• Hepatic impairment: Use with caution in patients with hepatic impairment; moderate impairment (Child-Pugh class B) requires lower maximum dose. Use is not recommended in severe hepatic impairment (Child-Pugh class C); has not been studied.

Special populations:

• Tobacco smoker: Tobacco smokers have been shown to have a decreased systemic exposure to istradefylline; a higher dose is recommended with use of ≥20 cigarettes/day or the tobacco equivalent.

Dosage Forms: US

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

Tablet, Oral:

Nourianz: 20 mg, 40 mg

Generic Equivalent Available: US

No

Pricing: US

Tablets (Nourianz Oral)

20 mg (per each): $75.71

40 mg (per each): $75.71

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.

Administration: Adult

Oral: May be taken with or without food.

Use: Labeled Indications

Parkinson disease, "off" episode: Treatment of Parkinson disease, in combination with levodopa/carbidopa, in adult patients experiencing "off" episodes.

Metabolism/Transport Effects

Substrate of CYP1A2 (minor), CYP2B6 (minor), CYP2C8 (minor), CYP2C9 (minor), CYP2D6 (minor), CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits CYP3A4 (weak)

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 Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

ALPRAZolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of ALPRAZolam. Risk C: Monitor therapy

Atorvastatin: Istradefylline may increase the serum concentration of Atorvastatin. Risk C: Monitor therapy

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

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 Istradefylline. Risk C: Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of Istradefylline. Risk X: Avoid combination

CYP3A4 Inhibitors (Strong): May increase the 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

Digoxin: Istradefylline may increase the serum concentration of Digoxin. Risk C: Monitor therapy

Dofetilide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide. Risk C: Monitor therapy

Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). 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

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). 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: Istradefylline may increase the serum concentration of Lomitapide. Management: Decrease the initial dose of lomitapide by half in patients taking lomitapide 10 mg daily or more when used in combination with weak CYP3A4 inhibitors, including istradefylline (dose of 40 mg daily or more). The maximum dose of lomitapide is 30 mg daily. 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

Midazolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Midazolam. Risk C: Monitor therapy

NiMODipine: CYP3A4 Inhibitors (Weak) may increase the serum concentration of NiMODipine. Risk C: Monitor therapy

Pimozide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide. 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 Istradefylline. Risk X: Avoid combination

Tacrolimus (Systemic): CYP3A4 Inhibitors (Weak) may increase the serum concentration of Tacrolimus (Systemic). Risk C: Monitor therapy

Tobacco (Smoked): May decrease the serum concentration of Istradefylline. Management: The recommended dosage of istradefylline in patients who use tobacco in amounts of 20 or more cigarettes per day (or the equivalent of another tobacco product) is 40 mg once daily. Risk D: Consider therapy modification

Triazolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Triazolam. Risk C: Monitor therapy

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

Reproductive Considerations

Females of reproductive potential should use effective contraception during therapy.

Pregnancy Considerations

Based on data from animal reproduction studies, in utero exposure to istradefylline may cause fetal harm.

Breastfeeding Considerations

It is not known if istradefylline is present in breast milk.

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.

Monitoring Parameters

Mental status and behavioral changes; dyskinesias.

Mechanism of Action

The mechanism of action of istradefylline is unknown. In in vitro studies and in in vivo animal studies, istradefylline was demonstrated to be an adenosine A2A receptor antagonist.

Pharmacokinetics (Adult Data Unless Noted)

Distribution: Vd/F: ~557 L

Protein binding: ~98%

Metabolism: Primarily via CYP1A1 and CYP3A4, with minor contribution from CYP1A2, 2B6, 2C8, CYP2C9, CYP2C18, and 2D6

Half-life elimination: ~83 hours

Time to peak: Median: 3 to 4 hours

Excretion: Feces: ~48%; urine: 39%

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Hepatic function impairment: Moderate hepatic impairment (Child-Pugh class B): AUC0-24 steady state exposure is predicted to be increased 3.3-fold based on estimated mean terminal half-life.

Smoking: Smoking (ie, tobacco) ≥20 cigarettes a day decreased steady-state systemic exposure by 38% to 54%.

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

  • (BD) Bangladesh: Aric;
  • (JP) Japan: Nouriast;
  • (PR) Puerto Rico: Nourianz
  1. Nourianz (istradefylline) [prescribing information]. Bedminster, NJ: Kyowa Kirin Inc; May 2020.
Topic 122395 Version 56.0

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