Immunosuppressants

Question 1

MOA of cyclosporine?

Answer 1

Inhibits calcineurin and blocks the activation of T cells.

No T cells = no IL-2

Question 2

What are the major immunosuppressant drugs?

Answer 2

Cyclosporine
Tacrolimus
Sirolimus
Azathioprine
Muromonab-CD3

Question 3

When is cyclosporine used?

Answer 3

Suppresses organ rejection and some AI diseases.

Question 4

MOA of tacrolimus?

Answer 4

Binds FK-binding protein and inhibits calcineurin –> decreased T cell activation

No T cells = no IL-2

Question 5

MOA of Sirolimus?

Answer 5

Inhibits mTOR and thus T cell proliferation (no IL-2 is made)

Question 6

MOA of Azathioprine?

Answer 6

Metabolized to 6-MP and interferes with cell maturation.

Question 7

MOA of Muromonab-CD3?

Answer 7

MAbto CD3 that blocks T cell interactions and activation.

Question 8

Immunosupressant that causes gingival hyperplasia?

Answer 8

Cyclosporine

Question 9

What immunosuppressant has interactions with allopurinol? Why?

Answer 9

Azathioprine, because it is metabolized by Xanthine Oxidase (which allopurinol inhibits).