Immuno drugs

Question 1

Hydroxycholoroquine

Answer 1

Antimalarial drug that is also used for RA, SLE, Sjogren’s, porphyria cutanea tarda

Toxicity: GI distress, retinopathy, can exacerbate G6PD deficiency anemia

Question 2

What drugs can cause drug-induced lupus?

Answer 2

Sulfonamides, hydralazine, INH, procainamide and phenytoin (SHIPP)

Question 3

Cyclosporine - what is the mechanism, use and toxicity?

Answer 3

Mechanism: Calcineurin inhibitor; binds cyclophilin. Blocks T-cell activation by preventing IL-2 transcription

Use: Transplant rejection prophylaxis, psoriasis, RA

Toxicity: **Nephrotoxicity, HTN, hyperlipidemia, neurotoxicity, gingival hyperplasia, hirsutism

Question 4

Tacrolimus (FK506) - what is the mechanism, use and toxicity?

Answer 4

Mechanism: Calcineurin inhibitor; binds FK506 binding protein (FKBP). Blocks T-cell activation by preventing IL-2 transcription

Use: Transplant rejection prophylaxis

Toxicity: **Nephrotoxicity, increase risk of diabetes and neurotoxicity (no gingival hyperplasia or hirsutism like cyclosporine)

Question 5

Sirolimus (rapamycin) - what is the mechanism, use and toxicity?

Answer 5

Mechanism: mTOR inhibitor (MAPK cascade); binds FKBP. Prevents response by IL-2 -> blocks T-cell activation and B-cell differentiation

Use: Kidney transplant rejection prophylaxis

Toxicity: Anemia, thrombocytopenia, leukopenia, insulin resistance, hyperlipidemia; NOT nephrotoxic

Question 6

Daclizumab, basiliximab - what is the mechanism, use and toxicity?

Answer 6

Mechanism: Monoclonal ab, block IL-2R

Use: Kidney transplant rejection prophylaxis

Toxicity: Edema, HTN, tremor

Question 7

Azathioprine - what is the mechanism, use and toxicity?

Answer 7

Mechanism: Antimetabolite precursor of 6MP. Inhibits lymphocyte proliferation by blocking nucleotide synthesis

Use: Transplant rejection prophylaxis, RA, Crohn’s disease, glomerulonephritis and other autoimmune disease

Toxicity: Leukopenia, anemia, thrombocytopenia [Note: 6MP degraded by xanthine oxidase –> toxicity increases with allopurinol]

Question 8

Glucocorticoids - what is the mechanism, use and toxicity?

Answer 8

Mechanism: Inhibit NF-kB -> decreases transcription of many cytokines -> suppresses B and T-cell function

Use: Transplant rejection prophylaxis, many autoimmune disorders, inflammation

Toxicity: Can cause Cushing syndrome, hyperglycemia, osteoporosis, central obesity, muscle breakdown, psychosis, acne, HTN, cataracts, avascular necrosis