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


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

Xanthine Oxidase
Glutathione Measurement
Cleaved Cell
Azathioprine Sulfate
High Pressure Liquid Chromatography Procedure

Trending Feeds


Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Sexual Dimorphism in Neurodegeneration

There exist sex differences in neurodevelopmental and neurodegenerative disorders. For instance, multiple sclerosis is more common in women, whereas Parkinson’s disease is more common in men. Here is the latest research on sexual dimorphism in neurodegeneration

HLA Genetic Variation

HLA genetic variation has been found to confer risk for a wide variety of diseases. Identifying these associations and understanding their molecular mechanisms is ongoing and holds promise for the development of therapeutics. Find the latest research on HLA genetic variation here.

Super-resolution Microscopy

Super-resolution microscopy is the term commonly given to fluorescence microscopy techniques with resolutions that are not limited by the diffraction of light. Here are the latest discoveries pertaining to super-resolution microscopy.

Genetic Screens in iPSC-derived Brain Cells

Genetic screening is a critical tool that can be employed to define and understand gene function and interaction. This feed focuses on genetic screens conducted using induced pluripotent stem cell (iPSC)-derived brain cells.

Brain Lower Grade Glioma

Low grade gliomas in the brain form from oligodendrocytes and astrocytes and are the slowest-growing glioma in adults. Discover the latest research on these brain tumors here.

CD4/CD8 Signaling

Cluster of differentiation 4 and 8 (CD8 and CD8) are glycoproteins founds on the surface of immune cells. Here is the latest research on their role in cell signaling pathways.

Alignment-free Sequence Analysis Tools

Alignment-free sequence analyses have been applied to problems ranging from whole-genome phylogeny to the classification of protein families, identification of horizontally transferred genes, and detection of recombined sequences. Here is the latest research.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.