Pharmacokinetics of the Antidepressant Rolipram in Healthy Volunteers

Abstract

1. The pharmacokinetics of rolipram were studied in healthy male volunteers using ³H-rolipram and a radioimmunoassay for measurement of unchanged drug.

2. Rolipram was rapidly and completely absorbed after an oral dose of 1 mg. Bioavailability was 73%.

3. Plasma levels of the unchanged drug declined with a terminal half-life of 2 h. The total clearance of rolipram was 2 ml/min per kg.

4. Labelled rolipram was excreted rapidly and completely. The main route of elimination was via the urine.