PT  - JOURNAL ARTICLE
AU  - Zampaglione, N
AU  - Hilbert, J M
AU  - Ning, J
AU  - Chung, M
AU  - Gural, R
AU  - Symchowicz, S
TI  - Disposition and metabolic fate of 14C-quazepam in man.
DP  - 1985 Jan 01
TA  - Drug Metabolism and Disposition
PG  - 25--29
VI  - 13
IP  - 1
4099  - http://dmd.aspetjournals.org/content/13/1/25.short
4100  - http://dmd.aspetjournals.org/content/13/1/25.full
SO  - Drug Metab Dispos1985 Jan 01; 13
AB  - The absorption, metabolism, and excretion of quazepam, a new benzodiazepine hypnotic, was investigated in six normal male volunteers after oral administration of 25 mg 14C-quazepam in solution. Quazepam was well absorbed. Plasma radioactivity peaked (324.6 ng quazepam eq/ml) 1.75 hr postdose. Unchanged quazepam reached its maximum plasma level (148 ng/ml) at 1.5 hr with an apparent absorption half-life of 0.4 hr. Major plasma metabolites of quazepam were 2-oxoquazepam (OQ), obtained by replacement of S by O,N-desalkyl-2-oxoquazepam (DOQ), and 3-hydroxy-2-oxoquazepam (HOQ) glucuronide. Both OQ and DOQ are pharmacologically active. Plasma elimination half-lives for quazepam, OQ, DOQ, and radioactivity were 39, 40, 69, and 76 hr, respectively. The respective AUC (120 hr) values were 715, 438, 3323, and 11402 hr X ng/ml. Approximately 54% of the radioactive dose was excreted in the urine (31.3%) and feces (22.7%) over a 5-day period. HOQ glucuronide was the major urinary metabolite of quazepam. Other metabolites present in the urine in relatively large amounts were glucuronides of DOQ and HDOQ.