Istradefylline
Parkinson Disease
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Drug Status
Government Approvals
US(FDA)
WHO Essential Medicine
NO
Known Teratogen
No
Pharmaceutical Class
NA
Controlled Drug Substance
No
Istradefylline
Summary
Istradefylline is used for treating adults with Parkinson's disease who experience 'off episodes'. These are periods when symptoms like difficulty moving, walking, and speaking become worse as the effect of medication wears off or happens randomly.
Istradefylline is an adenosine receptor antagonist. It works by altering the activity of certain natural substances in the brain. This helps improve movement, muscle control, and balance in patients with Parkinson's disease, reducing off episodes.
The usual daily dose of Istradefylline for adults is 20 mg, taken orally once daily. This may be increased to a maximum of 40 mg once daily based on individual need and tolerability.
Common side effects of Istradefylline include dyskinesia, dizziness, constipation, nausea, and insomnia. Serious adverse effects include hallucinations and psychotic behavior.
Istradefylline may cause dyskinesia, hallucinations, and impulse control disorders. It should not be used by patients with major psychotic disorders. Smoking may decrease its effectiveness, and it should be used cautiously in patients with moderate hepatic impairment.
Indications and Purpose
How does Istradefylline work?
Istradefylline works as an adenosine A2A receptor antagonist. By blocking these receptors, it helps to modulate neurotransmitter activity in the brain, which can improve movement and reduce "off" episodes in patients with Parkinson's disease.
Is Istradefylline effective?
Istradefylline has been shown to be effective in reducing "off" time in patients with Parkinson's disease when used as an adjunct to levodopa/carbidopa. Clinical trials demonstrated a statistically significant decrease in "off" time and an increase in "on" time without troublesome dyskinesia compared to placebo.
What is Istradefylline?
Istradefylline is used to treat "off" episodes in Parkinson's disease patients taking levodopa/carbidopa. It belongs to a class of medications called adenosine receptor antagonists, which work by altering the activity of certain natural substances in the brain to improve movement and muscle control.
Directions for Use
How do I take Istradefylline?
Istradefylline should be taken once daily, with or without food, at the same time each day. There are no specific food restrictions, but it is important to follow your doctor's instructions and discuss any dietary concerns with them.
How should I store Istradefylline?
Store Istradefylline at room temperature between 68°F to 77°F (20°C to 25°C). Keep it in its original container, tightly closed, and out of reach of children. Avoid storing it in the bathroom to prevent exposure to moisture.
What is the usual dose of Istradefylline?
The usual daily dose of Istradefylline for adults is 20 mg, which can be increased to a maximum of 40 mg once daily based on individual need and tolerability. There is no established dose for children as the safety and effectiveness of Istradefylline in pediatric patients have not been established.
Warnings and Precautions
Can Istradefylline be taken safely while breastfeeding?
There is no data on the presence of Istradefylline in human milk or its effects on the breastfed infant. It is present in the milk of lactating rats. The decision to use Istradefylline while breastfeeding should consider the benefits of breastfeeding and the mother's need for the medication.
Can Istradefylline be taken safely while pregnant?
There are no adequate data on the use of Istradefylline in pregnant women. Animal studies have shown teratogenic effects, especially when combined with levodopa/carbidopa. Women of childbearing potential should use contraception during treatment, and it is not recommended during pregnancy.
Can I take Istradefylline with other prescription drugs?
Istradefylline interacts with strong CYP3A4 inhibitors, which can increase its levels, and strong CYP3A4 inducers, which can decrease its effectiveness. Avoid using it with strong CYP3A4 inducers like rifampin and St. John's wort. Consult your doctor about all medications you are taking.
Is Istradefylline safe for the elderly?
No specific dosage adjustment is recommended for elderly patients taking Istradefylline. However, since a significant portion of clinical trial participants were aged 65 and older, it is important to monitor for side effects and effectiveness. Always consult a healthcare provider for personalized advice.
Who should avoid taking Istradefylline?
Important warnings for Istradefylline include the risk of dyskinesia, hallucinations, and impulse control disorders. Patients with major psychotic disorders should not use it. Smoking may decrease its effectiveness, and it should be used cautiously in patients with moderate hepatic impairment.
