PT  - JOURNAL ARTICLE
AU  - T L Ding
AU  - L Z Benet
TI  - Comparative bioavailability and pharmacokinetic studies of azathioprine and 6-mercaptopurine in the rhesus monkey.
DP  - 1979 Nov 01
TA  - Drug Metabolism and Disposition
PG  - 373--377
VI  - 7
IP  - 6
4099  - http://dmd.aspetjournals.org/content/7/6/373.short
4100  - http://dmd.aspetjournals.org/content/7/6/373.full
SO  - Drug Metab Dispos1979 Nov 01; 7
AB  - 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.