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Istradefylline

Medically reviewed by Drugs.com. Last updated on Jan 28, 2019.

Pronunciation

(IS tra DEF i lin)

Index Terms

  • Nourianz

Dosage Forms

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

Tablet, Oral:

Nourianz: 20 mg, 40 mg

Brand Names: U.S.

  • Nourianz

Pharmacologic Category

  • Anti-Parkinson Agent, Adenosine Receptor Antagonist

Use: Labeled Indications

Parkinson disease: Treatment of Parkinson disease, in combination with levodopa/carbidopa, in adult patients experiencing “off” episodes

Contraindications

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

Drug Interactions

ARIPiprazole: CYP3A4 Inhibitors (Weak) may increase the serum concentration of ARIPiprazole. Management: Monitor for increased aripiprazole pharmacologic effects. Aripiprazole dose adjustments may or may not be required based on concomitant therapy and/or indication. Consult full interaction monograph for specific recommendations. Monitor therapy

AtorvaSTATin: Istradefylline may increase the serum concentration of AtorvaSTATin. Monitor therapy

Bosentan: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

CYP3A4 Inducers (Moderate): May decrease the serum concentration of Istradefylline. Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of Istradefylline. 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. Consider therapy modification

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

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

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

Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Flibanserin: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Flibanserin. Monitor therapy

Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

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. Consider therapy modification

Lorlatinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences. Consider therapy modification

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

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

Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

St John's Wort: May decrease the serum concentration of Istradefylline. Avoid combination

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. Consider therapy modification

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Adverse Reactions

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

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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Other brands: Nourianz

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