Pharmacokinetics of tranylcypromine in patients who are depressed: relationship to cardiovascular effects

Clinical Pharmacology and Therapeutics
A G MallingerJ Ehler

Abstract

We investigated the pharmacokinetics of tranylcypromine, as well as the relationship between plasma levels of this agent and its effects on blood pressure and pulse rate. Tranylcypromine was absorbed rapidly after oral dosing, with the peak level being attained within 0.67 to 3.50 hours. Absorption was biphasic in seven of nine subjects. Elimination of tranylcypromine also was rapid, with a t 1/2 between 1.54 and 3.15 hours. From 2 to 7 hours after dosing, standing systolic and diastolic blood pressures were lowered and standing pulse was raised, compared with baseline. Onset of the effect on standing systolic blood pressure was correlated with the time of peak plasma tranylcypromine concentration. Maximum orthostatic drop of blood pressure and rise of pulse rate occurred 2 hours after dosing. Mean plasma tranylcypromine concentrations were correlated with mean orthostatic drop of systolic blood pressure and rise of pulse rate. Patients who have clinically significant hypotensive reactions to this agent may benefit from changes in their dose regimen aimed at minimizing peak tranylcypromine levels.

Citations

Apr 17, 2004·Clinical Pharmacokinetics·Catherine C Crone, Geoffrey M Gabriel
Aug 24, 2006·European Archives of Psychiatry and Clinical Neuroscience·Helge Frieling, Stefan Bleich
Apr 24, 1992·Pharmaceutisch Weekblad. Scientific Edition·P G Krugers DagneauxT S Van der Veer
Jul 16, 2008·Proceedings of the National Academy of Sciences of the United States of America·Natalia MastIrina A Pikuleva
Sep 1, 1987·Cellular and Molecular Neurobiology·R T CouttsT W Hall
May 13, 1999·Cellular and Molecular Neurobiology·G B BakerS H Kennedy

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