PMID: 43222Nov 1, 1979

Comparative bioavailability and pharmacokinetic studies of azathioprine and 6-mercaptopurine in the rhesus monkey

Drug Metabolism and Disposition : the Biological Fate of Chemicals
T L Ding, L Z Benet

Abstract

Azathioprine (AZA) is cleaved in vivo by glutathione to 6-mercpatopurine (6-MP). 6-MP plasma levels were measured by HPLC in four male rhesus monkeys following oral and iv doses of the two drugs. Following iv 6-MP administration, 6-MP levels were described by a two-compartment body model; mean terminal half-life; plasma clearance (CLp), and volume of distribution (Vdss) were 41.6 +/- 12.1 min, 48.4 +/- 15.4 ml/min/kg, and 1.76 +/- 0.64 liters/kg, respectively. 8-Hydroxymercpatopurine (8-OHMP) was identified as a metabolites of AZA. 8-OHMP had a CLp twice that for 6-MP, while its Vdss was similar to that for 6-MP. After an iv dose, AZA is converted to 6-MP to the extent of 15%. The conversion of AZA to 6-MP and 8-OHMP was independent of the route of administration. Differences in AZA and 6-MP kinetics among the monkeys were attributed to differences in individual aldehyde oxidase and xanthine oxidase levels.

Related Concepts

Mercaptopurine
Xanthine Oxidase
Cercopithecidae
Glutathione Measurement
Platyrrhini
Azathioprine
Cleaved Cell
Azathioprine Sulfate
High Pressure Liquid Chromatography Procedure
Monkeys

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