Sertraline: a new antidepressant.
The authors review preclinical data; clinical pharmacology data; and efficacy data of sertraline, a novel serotonin uptake inhibitor. Both in vitro and in vivo, sertraline is a potent and specific serotonin uptake inhibitor (possessing up to 10 times the activity of similar agents). Chronic dosing produces down-regulation of beta-adrenergic receptors. In man, sertraline inhibits platelet serotonin uptake and is devoid of obvious cardiac effects. The plasma half-life of sertraline is 25 hours. Studies on psychomotor performance show little or no effect at doses up to 100 mg, whereas 200 and 400 mg appear to possess some sedating action. Sertraline exhibits acute antidepressant effects in the dose range 50 to 200 mg/day; in addition, in the same dose range it prevents recurrence of depression. Its side-effect profile is similar to that of drugs of the same class (dry mouth, nausea, and diarrhea being the most prominent); it lacks the obvious anticholinergic and sedating effects of amitriptyline.
Doogan
D P
DP
Department of Clinical Research, Pfizer Limited, Sandwich, Kent, U.K.
Caillard
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V
D015057:1-Naphthylamine / Q000009:adverse effects / Q000031:analogs & derivatives / Q000494:pharmacology* / Q000627:therapeutic use; D000639:Amitriptyline / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000928:Antidepressive Agents; D002986:Clinical Trials as Topic; D003866:Depressive Disorder / Q000188:drug therapy; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008297:Male; D051379:Mice; D009281:Naphthalenes / Q000494:pharmacology*; D051381:Rats; D011943:Receptors, Adrenergic, beta / Q000187:drug effects; D017981:Receptors, Neurotransmitter / Q000187:drug effects; D012702:Serotonin Antagonists / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D020280:Sertraline
D000928:Antidepressive Agents; D009281:Naphthalenes; D011943:Receptors, Adrenergic, beta; D017981:Receptors, Neurotransmitter; D012702:Serotonin Antagonists; D000639:Amitriptyline; D015057:1-Naphthylamine; D020280:Sertraline