TY - JOUR T1 - Physiological disposition and metabolism of cyclobenzaprine in the rat, dog, rhesus monkey, and man. JF - Drug Metabolism and Disposition JO - Drug Metab Dispos SP - 659 LP - 672 VL - 6 IS - 6 AU - H B Hucker AU - S C Stauffer AU - A J Balletto AU - S D White AU - A G Zacchei AU - B H Arison Y1 - 1978/11/01 UR - http://dmd.aspetjournals.org/content/6/6/659.abstract N2 - The absorption, distribution, excretion, and metabolism of 3-(5 H-dibenzo[a,d]cyclohepten-5-ylidene)-N,N-dimethyl-1-propanamine (cyclobenzaprine) were investigated in the rat, dog, rhesus monkey, and man. The drug was well absorbed in all species after oral administration. The rat eliminated the drug primarily in the feces, but urinary excretion was predominant in the dog, monkey, and man. The drug was rapidly and widely distributed into rat tissues, highest concentrations being found in the small intestine, lung, kidney, and liver. The drug was highly bound in human plasma. Extensive biliary excretion of the labeled compound was observed in the rat. Major metabolites in the rat were phenolic derivatives but in man the major metabolites were 10,11-dihydroxynortriptyline and cyclobenzaprine glucuronide. Only minor amounts of unchanged drug were present in the urine. ER -