azathioprine

Question 1

What is azathioprine?

Answer 1

Immunosuppressive antimetabolite pro-drug.

Converted to 6-mercaptopurine in the body to block purine metabolism and DNA synthesis

Question 2

What is azathioprine indicated for?

Answer 2

RA
preventing renal transplant rejection
crohn’s disease
ulcerative colitis

Question 3

What is the role of azathioprine in IBD therapy?

Answer 3

-

Question 4

What are the relevant PK or PD parameters with azathioprine use?

Answer 4

well absorbed following oral administration
moderate (30%) binding to plasma proteins

activation occurs via hypoxanthine-guanine phosphoribosyltransferase

Question 5

What is the mechanism of action of azathioprine?

Answer 5

antagonises purine metabolism
may inhibit synthesis of DNA, RNA and proteins
May also interfere with cellular metabolism and inhibit mitosis

terminates dna chain and causes cytotoxicity