EFFECT OF DOSAGE AND ROUTE OF ADMINISTRATION OF TRAZODONE ON CEREBRAL CONCENTRATION OF 1-M-CHLOROPHENYLPIPERAZINE IN RATS - KINETICS OF TRAZODONE BIOTRANSFORMATION IN RATS

  • 1 January 1983
    • journal article
    • research article
    • Vol. 35  (3) , 241-247
Abstract
The levels of trazodone (TRZ) [an antidepressant which antagonizes the central serotonin system] and its metabolite, 1-m-chlorophenylpiperzine (CPP) [a central serotonin agonist] in the rat brain were tested after single and multiple administration of TRZ i.p. or p.o. [orally]. After a single p.o. dose and after multiple i.p. or p.o. 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 CNS may strongly affect the pharmacological activity of TRZ.

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