Effect of cianopramine, a tricyclic antidepressant, on platelet serotonin uptake and peripheral adrenergic function.
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 14C-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 micrograms/min before cianopramine and 86 +/- 32 micrograms/min 2 hr after 2 mg cianopramine, which suggests weak alpha-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.
D000284:Administration, Oral; D000328:Adult; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism*; D001794:Blood Pressure / Q000187:drug effects; D002250:Carbon Radioisotopes; D004311:Double-Blind Method; D005260:Female; D006801:Humans; D007099:Imipramine / Q000031:analogs & derivatives* / Q000494:pharmacology; D007263:Infusions, Parenteral; D008297:Male; D009638:Norepinephrine / Q000494:pharmacology; D010656:Phenylephrine / Q000494:pharmacology; D011897:Random Allocation; D012701:Serotonin / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000097:blood*; D014439:Tyramine / Q000494:pharmacology
D002250:Carbon Radioisotopes; D012702:Serotonin Antagonists; C024316:cianopramine; D010656:Phenylephrine; D012701:Serotonin; D007099:Imipramine; D009638:Norepinephrine; D014439:Tyramine