DIT Immunosuppressants MEchanism and side effects for each

Question 1

Cyclosporine?

Answer 1

Binds cyclophilin and inhibits calcineurin and IL-2 produciton stopped so no T cell activation

NEPHROTOXIC
HTN

Question 2

Tacrolimus?

Answer 2

Binds FK binding proteins and inhibits calcineurin to inhibit IL-2 (similar to cyclosporine)

Nephrotoxic
HTN
Neurotixicity

Question 3

Sirolimus

Answer 3

Binds FKBP-12 with blocks MTOR and IL-2 response is blocked (no downstream effects)

Dont stress side effects

Question 4

Aziothioprine?

Answer 4

Precursor of 6-MP (prodrug_

Interfere with nucleic acid synthesis

Side effects:
Bone marrow suppression.

METABOLIZED BY XANTHINE OXIDASE so allopurionl makes it worse (6MP broken down by it too)

Question 5

Mycophenolate

Answer 5

Inhibits IMP-dehydrogenase so no guanine is made

Prevents B and T cell proliferation

Risk of lymphoma, miscariage

Question 6

Muromonab?

Answer 6

Binds CD3 on T cells to prevent acute transplant rejection.

T cell can’t do signal transduction

Question 7

Daclizumab?

Answer 7

Binds CD25: IL-2 receptor on activated T cells

No IL-2 signalling (similar as sarolimus)

Question 8

Thalidomide?

Answer 8

Blocks TNFalpha.

Inhibits new vessel formation

Question 9

Anti TNFalpha drugs?

Answer 9

Inlfiximab, adalimumab, ETANERCEPT (decoy receptor)

PAIR diseases (B27)!
Psoriasitic arthritis
Ankylosing spondylitis
IBD
Reactive arthritis
Rheumatoid arthritis

Question 10

Abciximab?

Answer 10

Anti GpIIbIIIa

Question 11

Trastuzumab?

Answer 11

Anti Her2

Question 12

Omalizumab?

Answer 12

Anti IgE for severe asthma (but expensive so rarely used)