title: The metabolism of methazolamide - identification of metabolites in guinea pig urine.
abstract: The in vivo metabolism of methazolamide, a carbonic anhydrase inhibitor, was studied using guinea pigs as the animals. (14)C-Labeled methazolamide was synthesized. Eighty percent of intraperitoneally injected radioactivity was recovered from urine and feces within 24 hours. HPLC analysis on a C(18) 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 C(18) column. Their chemical structure was revealed by UV-absorbance spect a and LC/MS, and confirmed by comparing it with that of chemically synthesized compound. They were a glucuronide, (2-acetylimino-3-methyl-Δ(4)-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.
authors.affiliation: School of Nursing and School of Comprehensive Rehabilitation, Osaka Prefecture University, Habikino, Osaka 583- 8555, Japan.
authors.forename: Kenichi
authors.initials: K
authors.lastname: Kishida
authors.forename: Norihiro
authors.initials: N
authors.lastname: Yamamura
authors.forename: Yoshiaki
authors.initials: Y
authors.lastname: Iwai
authors.forename: Yoshiteru
authors.initials: Y
authors.lastname: Sakamoto
authors.forename: Makihiko
authors.initials: M
authors.lastname: Kuhara
authors.forename: Tetsuo
authors.initials: T
authors.lastname: Sasabe
mesh_terms: D000818:Animals; D001711:Biotransformation; D002250:Carbon Radioisotopes; D002257:Carbonic Anhydrase Inhibitors / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics* / Q000652:urine*; D002851:Chromatography, High Pressure Liquid / Q000592:standards; D005243:Feces / Q000737:chemistry; D020719:Glucuronides / Q000652:urine; D006168:Guinea Pigs; D007274:Injections, Intraperitoneal; D008297:Male; D008704:Methazolamide / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics* / Q000652:urine*; D015394:Molecular Structure; D012015:Reference Standards; D013056:Spectrophotometry, Ultraviolet / Q000592:standards; D013451:Sulfonic Acids / Q000652:urine; D053719:Tandem Mass Spectrometry / Q000592:standards
chemical_list: D002250:Carbon Radioisotopes; D002257:Carbonic Anhydrase Inhibitors; D020719:Glucuronides; D013451:Sulfonic Acids; D008704:Methazolamide