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- ISSN: 1872-3128
- E-ISSN: 1874-0758
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The Metabolism of Methazolamide - Identification of Metabolites in Guinea Pig Urine
- Source: Drug Metabolism Letters, Volume 5, Issue 1, Jan 2011, p. 45 - 54
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- 01 Jan 2011
Abstract
The in vivo metabolism of methazolamide, a carbonic anhydrase inhibitor, was studied using guinea pigs as the animals. 14C-Labeled methazolamide was synthesized. Eighty percent of intraperitoneally injected radioactivity was recovered from urine and feces within 24 hours. HPLC analysis on a C18 column detected 2 radioactive metabolites (Peaks A and B). The Peaks A and B were isolated from the urine of the animals dosed with non-radioactive methazolamide. They were purified on the C18 column. Their chemical structure was revealed by UV-absorbance spectra and LC/MS, and confirmed by comparing it with that of chemically synthesized compound. They were a glucuronide, (2-acetylimino-3- methyl-Δ4-1,3,4-thiadiazol-5-yl)-1-thio-β-D-glucopyranosiduronic acid, and a sulfonic acid, N-[3-methyl-5-sulfo-1,3,4- thiadiazol-2(3H)-ylidene]acetamide.
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