Home
Resources
Publications
Probenecid Inhibits the Glucuronidation of Indomethacin and O-desmethylindomethacin in Humans. A Pilot Experiment

Probenecid Inhibits the Glucuronidation of Indomethacin and O-desmethylindomethacin in Humans. A Pilot Experiment

T B Vree, M van den Biggelaar-Martea, C P Verwey-van Wissen, E W van Ewijk-Beneken Kolmer

Pharm World Sci. 1994 Feb 18;16(1):22-6.

PMID: 8156046

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP2504327	O-Desmethylindomethacin		2504-32-7	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: