PICAMILON
GABA-niacin prodrug developed in the USSR that crosses the BBB and releases GABA to produce anxiolytic and cerebrovascular effects.
Picamilon was developed in the Soviet Union and is registered as a medication in Russia for cerebrovascular disorders. Recent Russian clinical trials (n=50 and n=44) in patients with chronic cerebral ischemia showed significant improvements in cognitive function (MoCA scale), sleep quality, neurological deficits, and cerebral hemodynamics over 60-70 day treatment courses, with favorable safety profiles (>92% good tolerability). A combination product with ginkgo biloba (n=278) showed superior cognitive improvement versus ginkgo monotherapy. However, an FDA screening study found picamilon inactive against 50 biological targets in vitro, raising questions about its direct pharmacological activity. In the US, picamilon has never been FDA-approved but is sold as a dietary supplement, with a study finding highly variable quantities (2.7-721.5 mg per serving) across 31 supplements. Evidence is largely limited to Russian-language studies; independent Western clinical trials are lacking.