Abstract
Cyproheptadine was well absorbed and excreted almost equally in the urine and feces of the dog, rat, and cat. Plasma levels of radioactivity were considerably higher in the dog than in the rat. About 17% of the dose was excreted in dog bile in 6 hr. The N-oxide, trans-10,11-dihydroxy and 10,11-epoxide analogs were major metabolites of the drug in dog urine. Minor amounts of 10-ketodesmethylcyproheptadine, desmethylcyproheptadine, and cis-10,11-dihydroxycypro-heptadine, were also present. Major metabolites in cat urine were cis- and trans-10,11-dihydroxycyproheptadine along with minor amounts of cis- and trans-10,11-dihydroxydesmethyl-cyproheptadine, cyproheptadine-N-oxide, desmethylcyproheptadine, and 10-hydroxycyproheptadine. Rats excreted the drug almost entirely as 10,11-epoxydesmethylcyproheptadine. Placental transfer and excretion of the drug in milk occurred only to a limited extent.
Footnotes
- Received February 21, 1974.
- Copyright © 1974 by The American Society for Pharmacology and Experimental Therapeutics
DMD articles become freely available 12 months after publication, and remain freely available for 5 years.Non-open access articles that fall outside this five year window are available only to institutional subscribers and current ASPET members, or through the article purchase feature at the bottom of the page.
|
