Effect of dosage and route of administration of trazodone on cerebral concentration of 1-m-chlorophenylpiperazine in rats. Kinetics of trazodone biotransformation in rats.
The levels of trazodone (TRZ) and its metabolite, 1-m-chlorophenylpiperazine (CPP) in the rat brain were tested after single and multiple administration of TRZ ip or po. After a single oral dose and after multiple ip or po administration of TRZ, the brain level of CPP exceeded markedly that of the parent compound. Some of pharmacokinetic parameters of TRZ and CPP were significantly changed after chronic treatment. As the biological effect of CPP is opposite to that of its parent compound, the high level of metabolite in the central nervous system may affect strongly the pharmacological activity of TRZ.
D000818:Animals; D001711:Biotransformation; D001921:Brain / Q000378:metabolism*; D007700:Kinetics; D008297:Male; D010879:Piperazines / Q000032:analysis* / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D014196:Trazodone / Q000008:administration & dosage / Q000378:metabolism*
D010879:Piperazines; C015068:1-(3-chlorophenyl)piperazine; D014196:Trazodone