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Istradefylline is a selective adenosine A2A 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. A2A 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 A2A receptors than A1 receptors.
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).
The most common adverse reactions of Istradefylline are dyskinesia, dizziness, constipation, nausea, hallucination, and insomnia.
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.
Antiparkinson drugs
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.