Reference

Identification of cyclobenzaprine-10,11-epoxides in rat urine and after incubation with rat liver microsomes

Identification of cyclobenzaprine-10,11-epoxides in rat urine and after incubation with rat liver microsomes. Belvedere, G.; Frigerio, A.; Pantarotto, C.; Rovei, V. (Ist. Ric. Farmacol. "Mario Negri", Milan, Italy). Adv. Mass Spectrom. Biochem. Med., 2, 101-18 (English) 1977. 6682-26-4 and 303-50-4 are also in the experiment. CODEN: AMSMDB. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Section cross-reference(s): 26 After injection of cyclobenzaprine-HCl (I) [6202-23-9] (200 gm, i.p.) to rats, the following metabolites were isolated in the urine: cyclobenzaprine-10,11-epoxide [58256-08-9], cyclobenzaprine N-oxide [6682-26-4], demethylcyclobenzaprine [303-50-4], hydroxycyclobenzaprine [59920-63-7], demethylhydroxycyclobenzaprine [59920-64-8], and hydroxycyclobenzaprine N-oxide [59920-65-9]. After incubation of I with the rat liver microsomal fraction, the metabolites were: cyclobenzaprine-10,11-epoxide, cyclobenzaprine N-oxide, demethylcyclobenzaprine, and 10,11-epoxycyclobenzaprine N-oxide [58728-71-5]. .

Plasma levels and bioavailability of cyclobenzaprine in human subjects

Plasma levels and bioavailability of cyclobenzaprine in human subjects. Hucker, H. B.; Stauffer, S. C.; Albert, K. S.; Lei, B. W. (Merck Inst. Ther. Res., West Point, Pa., USA). J. Clin. Pharmacol., 17(11-12), 719-27 (English) 1977. CODEN: JCPCBR. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Cyclobenzaprine-HCl (I-HCl) [6202-23-9] was extensively metabolized in healthy volunteers, less than 1% of the dose being excreted unchanged in the urine. Comparison of areas under plasma level curves (AUC) after oral and i.v. doses suggested that I may be partly metabolized in the lumen or during its 1st passage through the gut wall and/or liver. Av. plasma levels of drug increased with increasing dosage, but the AUC increased less rapidly with increasing dose, possibly because of dose-dependent absorption.