Pharmacokinetics of the antidepressant rolipram in healthy volunteers

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.