Immunosuppressants

Question 1

Cyclosporine

Answer 1

MOA: inhibits T cell activation by calcineurin inhibition
Uses: organ transplantation, autoimmune disorders
SE: nephrotoxicity, hypertension
Kinetics: metabolized by CYP450 enzymes, excreted in bile

Question 2

Tacrolimus

Answer 2

MOA: inhibits T cell activation by calcineurin inhibition
Uses: organ transplantation, topical use for atopic dermatitis/psoriasis
SE: neurotoxicity, nephrotoxicity, hyperglycemia/diabetes
Kinetics: metabolized by CYP450

Question 3

Sirolimus

Answer 3

MOA: inhibits mTOR (blocks G1-S transition)
Uses: combination therapy for organ transplant
SE: hyperlipemia, bone marrow suppression
Kinetics: oral administration, metabolized by CYP450, long half-life

Question 4

Mycophenolate Mofetil

Answer 4

MOA: inhibits inosine monophosphate dehydrogenase, inhibits cell cycle
Uses: oral or IV for organ transplant
SE: bone marrow suppression, GI (diarrhea, vomiting)

Question 5

Azathioprine

Answer 5

MOA: metabolized into fraudulent nucleotide (6-Thio-IMP)
Uses: organ transplant, autoimmune diseases
SE: bone marrow suppression, hepatic toxicity
Kinetics: orally, interferes with xanthine oxidase function (Allopurinol)

Question 6

Methotrexate

Answer 6

MOA: metabolized into fraudulent nucleotide (6-Thio-IMP)
Uses: organ transplant, autoimmune diseases
SE: bone marrow suppression, hepatic toxicity
Kinetics: orally, interferes with xanthine oxidase function (Allopurinol)

Question 7

Cyclophosphamide

Answer 7

MOA: alkylating agent leading to cytotoxicity of lymphoid cells
Uses: chemotherapy, organ transplant, autoimmune disorders
SE: toxicity to rapidly growing tissue, nausea, vomiting

Question 8

Anti-thymocyte/Anti-lymphocyte Ab

Answer 8

MOA: activates cytotoxicity (complement, Cell mediated), block lymphocyte function
Uses: immunosuppression, treat acute renal transplant rejection
SE: fever/chill, leukopenia, thrombocytopenia, develop Ab against Ab host

Question 9

Rho(D) Immunoglobulin

Answer 9

MOA: binds Rho antigen and prevents sensitization of Rh-negative woman to Rh-positive fetus
Uses: IM to mother to prevent hemolytic disease of newborn
SE: low grade fever

Question 10

Muromonab-CD3

Answer 10

MOA: inactivate T cell function, depletes T cells
Uses: organ transplant and steroid resistant rejection
SE: cytokine release syndrome, HAMA reaction (patient produces anti-mouse Ab)

Question 11

Alefacept

Answer 11

MOA: inhibits T cell activation by binding CD2
Uses: plaque psoriasis
SE: dose-dependent reduction of T cells

Question 12

Etanercept

Answer 12

MOA: humanized IgG fused to TNF receptor binds TNFalpha and beta
Uses: rheumatoid arthritis, can be used with methotrexate
SE: infusion reaction (fever, urticaria, hypotension, dyspnea), serious infections, lymphoma

Question 13

Adalimumab and Golimumab

Answer 13

Adalimumab and Golimumab
MOA: human Ab that blocks TNFalpha from binding receptor, suppresses inflammatory cytokines
Uses: rheumatoid arthritis
SE: infusion reaction (fever, urticaria, hypotension, dyspnea), serious infections, lymphoma

Question 14

Infliximab and Certolizumab

Answer 14

MOA: humanized Ab that blocks TNFalpha from binding receptor, suppress inflammatory cytokines
Uses: rheumatoid arthritis, Crohn’s disease
SE: infusion reaction (fever, urticaria, hypotension, dyspnea), serious infections, lymphoma