Istradefylline

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Istradefylline is an Adenosine A₂A Receptor Antagonist that is FDA approved for the treatment of adult patients with Parkinson’s disease (PD) experiencing “off” episodes along with treatment to levodopa/carbidopa. Common adverse reactions include Dyskinesia (involuntary muscle movements), Hallucinations Insomnia, Nausea, and Constipation..

There is limited information regarding Istradefylline FDA-Labeled Indications and Dosage (Adult) in the drug label.

There is limited information regarding Off-Label Guideline-Supported Use of Istradefylline in adult patients.

There is limited information regarding Off-Label Non–Guideline-Supported Use of Istradefylline in adult patients.

Gastrointestinal Disorders: Nausea, constipation.​

Nervous System Disorders: Dyskinesia, dizziness.​ nourianz.com +4

Psychiatric Disorders: Hallucinations, insomnia.​

General Disorders: Increased blood creatine phosphokinase.

There is limited information regarding Off-Label Guideline-Supported Use of Istradefylline in pediatric patients.

There is limited information regarding Off-Label Non–Guideline-Supported Use of Istradefylline in pediatric patients.

There is limited information regarding Istradefylline Contraindications in the drug label.

There is limited information regarding Istradefylline Warnings’ in the drug label.

Gastrointestinal Disorders: Nausea, constipation.​

Nervous System Disorders: Dyskinesia, dizziness.​

Psychiatric Disorders: Hallucinations, insomnia.​

General Disorders: Increased blood creatine phosphokinase.

There is limited information regarding Istradefylline Postmarketing Experience in the drug label.

Strong CYP3A4 Inhibitors: Co-administration increases istradefylline exposure. The maximum recommended dosage is 20 mg once daily when used with strong CYP3A4 inhibitors.​

Strong CYP3A4 Inducers: Avoid use with strong CYP3A4 inducers as they may decrease istradefylline effectiveness.​

Pregnancy Category (FDA): Istradefylline may cause fetal harm. Advise pregnant women of the potential risk to a fetus.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Istradefylline in women who are pregnant.

There is no FDA guidance on use of Istradefylline during labor and delivery.

There is no FDA guidance on the use of Istradefylline in women who are nursing.

There is no FDA guidance on the use of Istradefylline in pediatric settings.

There is no FDA guidance on the use of Istradefylline in geriatric settings.

There is no FDA guidance on the use of Istradefylline with respect to specific gender populations.

There is no FDA guidance on the use of Istradefylline with respect to specific racial populations.

There is no FDA guidance on the use of Istradefylline in patients with renal impairment.

For patients with moderate hepatic impairment (Child-Pugh Class B), the maximum recommended dosage is 20 mg once daily. Avoid use in patients with severe hepatic impairment (Child-Pugh Class C).​

There is no FDA guidance on the use of Istradefylline in women of reproductive potentials and males.

There is no FDA guidance one the use of Istradefylline in patients who are immunocompromised.

Dosage: The recommended starting dosage is 20 mg once daily, which may be increased to a maximum of 40 mg once daily based on individual patient needs and tolerability.

Dyskinesia: Monitor for the onset or worsening of dyskinesia.​ Psychiatric Symptoms: Observe for hallucinations, psychotic behavior, or impulse control disorders.

Istradefylline is administered orally.

In case of overdose, provide symptomatic and supportive treatment. There is no known antidote for istradefylline overdose.​

There is limited information regarding Istradefylline Pharmacology in the drug label.

Istradefylline is an adenosine A₂A receptor antagonist. The precise mechanism by which it exerts its therapeutic effect in Parkinson’s disease is unknown.

There is limited information regarding Istradefylline Structure in the drug label.

Istradefylline’s antagonism of the adenosine A₂A receptor is thought to play a role in its effects on motor activity in Parkinson’s disease.

Absorption: Peak plasma concentrations are reached approximately 4 hours after oral administration.​

Distribution: The volume of distribution is approximately 557 liters, with 98% protein binding.​

Metabolism: Metabolized primarily by CYP1A1, CYP3A4, and CYP3A5 enzymes.​

Elimination: The elimination half-life is approximately 64-69 hours. Excretion occurs via feces (68%) and urine (18%).

There is limited information regarding Istradefylline Nonclinical Toxicology in the drug label.

There is limited information regarding Istradefylline Clinical Studies in the drug label.

Dosage Forms and Strengths: Istradefylline is supplied as film-coated tablets in the following strengths:​

20 mg tablets: Light pink, round, debossed with “20” on one side.​ 40 mg tablets: Light pink, oval-shaped, debossed with “40” on one side

Storage Conditions: Store at room temperature between 68°F to 77°F (20°C to 25°C). ​ Keep the medication in its original container, tightly closed, and away from excess heat and moisture. ​ Keep out of the reach of children.​

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There is limited information regarding Istradefylline Patient Counseling Information in the drug label.

Alcohol-Istradefylline interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Istradefylline is marketed under the brand name NOURIANZ.

There is limited information regarding Istradefylline Look-Alike Drug Names in the drug label.

The contents of this FDA label are provided by the National Library of Medicine.