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Probenecid inhibits the glucuronidation of indomethacin andO-desmethylindomethacin in humans
- Source :
- Pharmacy World & Science. 16:22-26
- Publication Year :
- 1994
- Publisher :
- Springer Science and Business Media LLC, 1994.
-
Abstract
- Indomethacin is metabolized in humans by O-demethylation, and by acyl glucuronidation to the 1-O-glucuronide. Indomethacin, its metabolite, and their conjugates can be measured directly by gradient high-pressure liquid chromatographic analysis without enzymic deglucuronidation. The pharmacokinetic profile of indomethacin and some preliminary pharmacokinetic parameters of indomethacin obtained from one human volunteer are given. In plasma only the parent drug indomethacin is present, while in urine the acyl and ether glucuronides are present in high concentrations. This confirms other reports that indomethacin and O-desmethylindomethacin may be glucuronidated in the kidney. Probenecid is a known substrate for renal glucuronidation. If indomethacin is glucuronidated in the human kidney like probenecid, then this glucuronidation might be reduced or inhibited under probenecid co-medication. This pilot experiment shows that probenecid reduced the acyl glucuronidation of indomethacin by 50% and completely inhibited the formation of O-desmethylindomethacin acyl and ether glucuronide.
- Subjects :
- Male
Metabolite
Indomethacin
Acyl glucuronidation
Glucuronidation
Pharmaceutical Science
Glucuronates
Pilot Projects
Pharmacy
Pharmacology
Kidney
Toxicology
Deglucuronidation
chemistry.chemical_compound
Pharmacokinetics
medicine
Humans
Pharmacology (medical)
Chromatography, High Pressure Liquid
Probenecid
Chemistry
Kidney metabolism
General Medicine
Middle Aged
Glucuronide
medicine.drug
Subjects
Details
- ISSN :
- 1573739X and 09281231
- Volume :
- 16
- Database :
- OpenAIRE
- Journal :
- Pharmacy World & Science
- Accession number :
- edsair.doi.dedup.....5d590e4fa2ea1dd30352ba4599121a41