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Cyproheptadine is a serotonin and histamine antagonist with anticholinergic and sedative effects. Antiserotonin and antihistamine drugs appear to compete with serotonin and histamine, respectively, for receptor sites.
Pharmacokinetics And Metabolism
After a single 4mg oral dose of 14C-labelled Cyproheptadine HCl in normal subjects, given as tablets, 2-20% of the radioactivity was excreted in the stools. Only about 34% of the stool radioactivity was unchanged drug, corresponding to less than 5.7% of the dose. At least 40% of the administered radioactivity was excreted in the urine. No detectable amount of unchanged drug were present in the urine of patients on chronic 12-20 mg daily doses. The principle metabolite found in human urine has been identified as a quaternary ammonium glucuronide conjugate of cyproheptadine. Elimination is diminished in renal insufficiency.
Last reviewed on RxList: 10/10/2016
This monograph has been modified to include the generic and brand name in many instances.
Additional Cyproheptadine Information
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