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Article
Title	Identification of the UDP-Glueuronosyltransferase (UGT) Isoforms involved in Buprenorphine Glucuronidation and Evaluation of the Inhibitory Potential of this Drug on UGTs
Author	Rouguieg K, Sauvage F L, Comte J H, Marquet P, Picard N
Article Information		Abstract
Publication	Ther-Drug-Monit	This study evaluated the specific contribution of individual UDP-glucuronosyltransferase (UGT) isoforms to the hepatic glucuronidation (HG) of buprenorphine (BUP) and the inhibitory capacity of BUP on the different UGT in human liver microsomes (HLM). UGT 1A1, 1A3 and 2B7 produced BUP-glucuronide at detectable levels. UGT 2B7 showed high affinity towards BUP. BUP inhibited the activities of UGT 2B7, UGT 1A3, UGT 1A4 and UGT 1A1. Thus, UGT2B7 is the main isoform involved in BUP HG and showed an inhibitory effect on several hepatic UGT. The IC50 observed are much higher than usual therapeutic levels suggesting that drug-drug interactions might not be clinically relevant. (conference abstract: 11th International Congress of Therapeutic Drug Monitoring & Clinical Toxicology, Montreal, Quebec, Canada, 03/10/2009-08/10/2009).
Reference	BUPP10056
Year	2009
Logged	02/02/2010
Volume	31
Part	5
Pages	abs 222
ISSN	0163-4356
Keywords
Comparison Drug
Language	English