The pharmacokinetics of risperidone in humans: a summary.
Risperidone is rapidly and completely absorbed after oral administration; less than 1% is excreted unchanged in the feces. The principal metabolite was found to be 9-hydroxyrisperidone. Hydroxylation of risperidone is subject to the same genetic polymorphism as debrisoquine and dextromethorphan. In poor metabolizers the half-life of risperidone was about 19 hours compared with about 3 hours in extensive metabolizers. However, becuase the pharmacology of 9-hydroxyrisperidone is very similar to that of risperidone, the half-life for the "active fraction" (risperidone +9-hydroxyrisperidone) was found to be approximately 20 hours in extensive and poor metabolizers. We found that risperidone exhibited linear elimination kinetics and that steady state was reached within 1 day for risperidone and within 5 days for the active fraction.
Heykants
J
J
Department of Drug Metabolism and Pharmacokinetics, Janssen Research Foundation, Beerse, Belgium.
Huang
M L
ML
Mannens
G
G
Meuldermans
W
W
Snoeck
E
E
Van Beijsterveldt
L
L
Van Peer
A
A
Woestenborghs
R
R
D000368:Aged; D000818:Animals; D014150:Antipsychotic Agents / Q000493:pharmacokinetics*; D001711:Biotransformation; D004285:Dogs; D006207:Half-Life; D006801:Humans; D007555:Isoxazoles / Q000493:pharmacokinetics*; D008103:Liver Cirrhosis / Q000378:metabolism; D008297:Male; D000068882:Paliperidone Palmitate; D010880:Piperidines / Q000493:pharmacokinetics*; D011743:Pyrimidines / Q000493:pharmacokinetics; D051381:Rats; D012016:Reference Values; D051437:Renal Insufficiency / Q000378:metabolism; D018967:Risperidone; D012559:Schizophrenia / Q000097:blood
D014150:Antipsychotic Agents; D007555:Isoxazoles; D010880:Piperidines; D011743:Pyrimidines; D018967:Risperidone; D000068882:Paliperidone Palmitate