Pharmacokinetics and Pharmacodynamics of procyclidine in man.
The pharmacokinetics and pharmacodynamics of procyclidine (10 mg) after oral and intravenous administration were studied in six healthy volunteers. Treatment order was randomised and the study was placebo-controlled and conducted blind. After oral dosing the mean peak plasma concentration was 116 ng/ml and mean bioavailability was 75%. After both oral and intravenous dosing the mean values for the volume of distribution, total body clearance and plasma elimination half-life of procyclidine were in the order of 1 l/kg, 68 ml/min and 12 h respectively. Autonomic effects were maximal within 0.5 h of intravenous administration and at about 1-2 h after oral dosing. Significant effects on pupil diameter, visual near point, salivary secretion and heart rate occurred after intravenous treatment and similar but less marked effects occurred after the oral dose. Significant autonomic effects were still detectable 12 h after both forms of treatment.
D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D004311:Double-Blind Method; D005260:Female; D006207:Half-Life; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007275:Injections, Intravenous; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D011352:Procyclidine / Q000009:adverse effects / Q000378:metabolism* / Q000494:pharmacology; D011680:Pupil / Q000187:drug effects; D011759:Pyrrolidines / Q000378:metabolism*; D011897:Random Allocation; D012463:Saliva / Q000032:analysis; D012737:Sex Factors
D011759:Pyrrolidines; D011352:Procyclidine