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Effect of cianopramine, a tricyclic antidepressant, on platelet serotonin uptake and peripheral adrenergic function
Author(s) -
Eichler Hans G,
Gasic Slobodan,
Korn Adrienne
Publication year - 1984
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1984.216
Subject(s) - tricyclic , serotonin , pharmacology , chemistry , norepinephrine , phenylephrine , medicine , platelet , antidepressant , endocrinology , tyramine , blood pressure , catecholamine , imipramine , tricyclic antidepressant , adrenergic , reuptake , receptor , dopamine , alternative medicine , pathology , hippocampus
Cianopramine, a new tricyclic antidepressant, is a potent inhibitor of neuronal serotonin (5‐HT) uptake in animals. We studied the effect of cianopramine on 5‐HT uptake (ex vivo) in platelets and on peripheral neuronal adrenergic function in catecholamine pressure response tests in normal subjects. The inhibition of 14 C‐labeled 5‐HT uptake into platelets was 57% ± 12% 2 hr after 0.5 mg (after 24 hr: 27% ± 13%), 59% ± 10% 2 hr after 1 mg (24 hr: 41% ± 13%), and 80% ± 2% 2 hr after 2 mg cianopramine (24 hr: 52% ± 10%). Systolic blood pressure response to intravenous tyramine and norepinephrine was unchanged after 2 mg cianopramine. The phenylephrine dose required for an increase of 40 mm Hg in systolic blood pressure was 67 ± 25 μg/min before cianopramine and 86 ± 32 μg/min 2 hr after 2 mg cianopramine, which suggests weak α‐receptor antagonism of cianopramine. Our results in man are consistent with potent, specific 5‐HT uptake inhibition by cianopramine without a clinically relevant effect on peripheral neuronal norepinephrine reuptake. Clinical Pharmacology and Therapeutics (1984) 36, 542–545; doi: 10.1038/clpt.1984.216