[Pharmacokinetic characteristics of 14C-peritol based on data on its distribution in rat tissue]

Peritol (cyproheptadine) is chemically 1-methyl-4-(5-dibenzo-cyclohepta-trenilidin)-piperidine hydrochloride. It has a pronounced antihistamine and antiserotonin action. When injected intravenously to rats 14C-peritol is rapidly excreted from blood (T 1/2 = 2 h). The concentration of 14C-peritol as judged from the absorption ratio (AR), varies within the first 15 minutes. The magnitude of the AR ranged within 0.44 (muscles) to 17.1 (kidneys) on intravenous injection, and within 0.1 (skin) to 5.5 (liver) when administered into the stomach. Excretion of the label from the body (intravenous administration) occurred from T 1/2 = 44 h, and from T 1/2 = 40 h (intragastric administration). The total amount of radioactivity resorbed from the gastrointestinal tract was equal to 46.3% at the height of accumulation by organs and tissues (one hour after administration). Radiochromatography made it possible to disclose that 14C-peritol was retained in the rat body for 6 hours whereupon underwent metabolism.