Istradefylline
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Omid Afkhami-Ardakani
Disclaimer
WikiDoc MAKES NO GUARANTEE OF VALIDITY. WikiDoc is not a professional health care provider, nor is it a suitable replacement for a licensed healthcare provider. WikiDoc is intended to be an educational tool, not a tool for any form of healthcare delivery. The educational content on WikiDoc drug pages is based upon the FDA package insert, National Library of Medicine content and practice guidelines / consensus statements. WikiDoc does not promote the administration of any medication or device that is not consistent with its labeling. Please read our full disclaimer here.
Overview
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..
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
There is limited information regarding Istradefylline FDA-Labeled Indications and Dosage (Adult) in the drug label.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Istradefylline in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Istradefylline in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
Gastrointestinal Disorders: Nausea, constipation.
Nervous System Disorders: Dyskinesia, dizziness. nourianz.com +4
Psychiatric Disorders:
Hallucinations, insomnia.
General Disorders: Increased blood creatine phosphokinase.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Istradefylline in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Istradefylline in pediatric patients.
Contraindications
There is limited information regarding Istradefylline Contraindications in the drug label.
Warnings
There is limited information regarding Istradefylline Warnings' in the drug label.
Adverse Reactions
Clinical Trials Experience
Gastrointestinal Disorders: Nausea, constipation.
Nervous System Disorders: Dyskinesia, dizziness.
Psychiatric Disorders: Hallucinations, insomnia.
General Disorders: Increased blood creatine phosphokinase.
Postmarketing Experience
There is limited information regarding Istradefylline Postmarketing Experience in the drug label.
Drug Interactions
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.
Use in Specific Populations
Pregnancy
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.
Labor and Delivery
There is no FDA guidance on use of Istradefylline during labor and delivery.
Nursing Mothers
There is no FDA guidance on the use of Istradefylline in women who are nursing.
Pediatric Use
There is no FDA guidance on the use of Istradefylline in pediatric settings.
Geriatic Use
There is no FDA guidance on the use of Istradefylline in geriatric settings.
Gender
There is no FDA guidance on the use of Istradefylline with respect to specific gender populations.
Race
There is no FDA guidance on the use of Istradefylline with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Istradefylline in patients with renal impairment.
Hepatic 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).
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Istradefylline in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Istradefylline in patients who are immunocompromised.
Administration and Monitoring
Administration
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.
Monitoring
Dyskinesia: Monitor for the onset or worsening of dyskinesia. Psychiatric Symptoms: Observe for hallucinations, psychotic behavior, or impulse control disorders.
IV Compatibility
Istradefylline is administered orally.
Overdosage
In case of overdose, provide symptomatic and supportive treatment. There is no known antidote for istradefylline overdose.
Pharmacology
There is limited information regarding Istradefylline Pharmacology in the drug label.
Mechanism of Action
Istradefylline is an adenosine A₂A receptor antagonist. The precise mechanism by which it exerts its therapeutic effect in Parkinson's disease is unknown.
Structure
There is limited information regarding Istradefylline Structure in the drug label.
Pharmacodynamics
Istradefylline's antagonism of the adenosine A₂A receptor is thought to play a role in its effects on motor activity in Parkinson's disease.
Pharmacokinetics
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%).
Nonclinical Toxicology
There is limited information regarding Istradefylline Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Istradefylline Clinical Studies in the drug label.
How Supplied
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
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.
Images
Drug Images
{{#ask: Page Name::Istradefylline |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}
Package and Label Display Panel
{{#ask: Label Page::Istradefylline |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}
Patient Counseling Information
There is limited information regarding Istradefylline Patient Counseling Information in the drug label.
Precautions with Alcohol
Alcohol-Istradefylline interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
Istradefylline is marketed under the brand name NOURIANZ.
Look-Alike Drug Names
There is limited information regarding Istradefylline Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.