Immunosuppressants

Question 1

Cyclosporine (MOA, use, SE)

Answer 1

MOA - Binds cyclophilin -> inhibits calcineurin -> prevents IL-2 transcription
Use - Psoriasis, RA, Lupus nephritis
SE - nephrotoxicity

Question 2

Tacrolimus (MOA, use, SE)

Answer 2

Binds FK506 -> inhibits calcineurin -> prevents IL-2 transcription
Use - topical for eczema
SE - nephrotoxicity & neurotoxicity

Question 3

Sirolimus (Rapamycin) (MOA)

Answer 3

binds FKBP-12 -> inhibits mTOR -> prevents response to IL-2

Question 4

Azathioprine (MOA, use, SE)

Answer 4

MOA - antimetabolite precursor of 6-mercaptopurine -> inhibits lymphocyte proliferation by blocking nucleotide synthesis
Use - RA, Crohn’s, glomerulonephritis, lupus nephritis, kidney transplants
SE - 6-MP is degraded by xanthine oxidase; increased toxicity with allopurinol

Question 5

Mycophenolate mofetil (MOA, use, SE)

Answer 5

MOA - reversibly inhibits IMP dehydrogenase -> prevents purine synthesis of B and T cells
Use - lupus nephritis
SE - HTN, hyperglycemia, hypercholesterolemia

Question 6

Thalidomide (MOA, use, SE)

Answer 6

MOA - suppresses TNF-alpha production, increases NK cells and IL-2
Use - Hansen disease, multiple myeloma
SE - phocomelia (limb defects in pregnancy)

Question 7

Antibody that binds Il-2 receptor on activated T cells

Answer 7

Daclizumab