Antimetabolites for Immunosuppression

Azathioprine and mycophenolate both function as antimetabolites and are used to prevent transplant rejection. 

Azathioprine is a nucleotide analog that decreases proliferation of lymphocytes. Azathioprine is initially converted to 6-mercaptopurine, which is then converted to an active metabolite. The active metabolites inhibit purine synthesis and can also be inserted into DNA/RNA rendering the DNA/RNA non-functional.

Mycophenolate inhibits IMP (inosine monophosphate dehydrogenase), which is used to produce GMP, which is used for nucleic acid synthesis. Lack of GMP reduces production of rapidly dividing lymphocytes.

Class Drugs

• Azathioprine

• Mycophenolate

Class Mechanism of Action

See individual drugs

Class Applications

See individual drugs

Class Adverse Effects

See individual drugs

Drug Table

Drug Name	Application	Comments	Image
Azathioprine	Prevention of transplant rejection	Mechanism; -Nucleotide analog that decreases proliferation of lymphocytes; -Initially converted to 6-mercaptopurine, which is then converted to active metabolites; -Inhibits purine synthesis; -Metabolites can also be inserted into DNA/RNA rendering the DNA/RNA non-functional; Adverse Effects; Bone marrow suppression	"Arizona" "Thigh" "Pine Tree"
Mycophenolate	Liver, kidney, and heart transplants	Mechanism; -Inhibits IMP dehydrogenase (inosine monophosphate dehydrogenase), which is used to produce GMP.; -GMP is used for nucleic acid synthesis.; -Lack of GMP reduces production of rapidly dividing lymphocytes; Adverse Effects; GI Effects	"Mycotic Fence" "Latte"