RT Journal Article
SR Electronic
T1 PHYSIOLOGICAL DISPOSITION AND URINARY METABOLITES OF CYPROHEPTADINE IN THE DOG, RAT, AND CAT
JF Drug Metabolism and Disposition
JO Drug Metab Dispos
FD American Society for Pharmacology and Experimental Therapeutics
SP 406
OP 415
VO 2
IS 5
A1 HUCKER, H. B.
A1 BALLETTO, A. J.
A1 STAUFFER, S. C.
A1 ZACCHEI, A. G.
A1 ARISON, B. H.
YR 1974
UL http://dmd.aspetjournals.org/content/2/5/406.abstract
AB 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. Copyright © 1974 by The American Society for Pharmacology and Experimental Therapeutics