Istradefylline

Istradefylline tablet is an adenosine receptor antagonist indicated as adjunctive treatment to levodopa/carbidopa in adult patients with Parkinson's disease experiencing "off" episodes.

Istradefylline is a selective adenosine A_2A receptor inhibitor. These receptors are found in the basal ganglia, a region of the brain that suffers degeneration in Parkinson's disease, and is also significantly involved in motor control. A_2A receptors are also expressed on GABAergic medium spiny neurons within the indirect striato-pallidal pathway. The GABAergic action of this pathway is thereby reduced. Istradefylline has 56 times the affinity for A_2A receptors than A₁ receptors.

The recommended dosage of Istradefylline is 20 mg administered orally once daily. The dosage may be increased to a maximum of 40 mg once daily, based on individual need and tolerability. Patients who smoke 20 or more cigarettes per day (or the equivalent of another tobacco product) the recommended dosage is 40 mg once daily.

Patients with Hepatic Impairment: Maximum recommended dosage with moderate hepatic impairment is 20 mg once daily, use of Istradefylline in patients with severe hepatic impairment should be avoided.

Use in Children: Safety and effectiveness of Istradefylline in pediatric patients have not been established.

The recommended maximum dosage of Istradefylline with concomitant use of strong CYP 3A4 inhibitors (Ketoconazole) is 20 mg once daily and avoid use with strong CYP 3A4 inducers (Rifampicin).

Istradefylline is contraindicated in patients with known hypersensitivity to any component of this drug, and in patients with severe hepatic impairment.

The most common adverse reactions of Istradefylline are dyskinesia, dizziness, constipation, nausea, hallucination, and insomnia.

Use of Istradefylline during pregnancy is not recommended. Based on studies it may cause fetal harm. There are no data on the presence of Istradefylline in human milk, the effects of Istradefylline on the breastfed infant, or on milk production. Caution should be exercised when administered to a nursing woman.

Monitor patients for dyskinesia or exacerbation of existing dyskinesia. If hallucinations / psychotic behavior / impulse control / compulsive behaviors occurs then consider dosage reduction or stop Istradefylline.

There is limited clinical experience regarding human overdose with Istradefylline. If an overdose occurs, Istradefylline treatment should be discontinued and supportive treatment should be administered as clinically indicated.

Antiparkinson drugs

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.