Zomepirac glucuronide

Involvement of tissue esterases is documented for zomepirac glucuronide, which undergoes rapid hydrolysis in vivo in the guinea pig and rabbit [30], Co-administration of (phenylmethyl)sulfonyl fluoride (an inhibitor of esterases) dramatically decreased the apparent plasma clearance of zomepirac glucuronide, and, in other experiments, strongly increased the apparent plasma clearance of zomepirac administered as such. 

Probenecid Zomepirac Zomepirac CL declined by 64%, zomepirac glucuronide CL formation decreased by 71%, urinary excretion of zomepirac glucuronide decreased from 72% to 58% 121... 

High Pressure Liquid Chromatography. In serum or plasma sensitivity 50 ng/ml, UV detection—C. L. Welch et al, Clin. Chem., 1982, 28, 481-484. In urine zomepirac and zomepirac glucuronide, detection limit about 100 ng/ml, UV detection—P. Pietta and A. Calatroni, J. Chromat., 1983, 275 Biomed. AppL, 26, 217-222. 

Following a single oral dose of 200 mg to 5 subjects, peak plasma concentrations of 4.5 to 11.3 pg/ml (mean 9) were attained in about 1 hour mean peak plasma concentrations of zomepirac glucuronide and hydroxyzomepiracof 3.9 ig/ml and 0.2 pg/ml, respectively, were attained in 0.5 to 3 hours (P. J. O Neill et ai, J. din. Pharmac., 1982,22,470-476). 

Smith PC, Langendijk PN, Boss JA, et al. Effect of probenecid on the formation and elimination of acyl glucuronides studies with zomepirac. Clin Pharmacol Ther 1985 38(2) 121-127. 

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