Immunosuppressants

Question 1

Calcineurin Inhibitors

Answer 1

• prevents organ transplant rejection

- meds differ in structure but share the same mechanism

Question 2

Cyclosporine (Sandimmune)

Answer 2

• suppresses the production of interleukin-2, interferon gamma, and other cytokines
• DOC for organ rejection of an allogenic transplant
• absorption unpredictable
• serum blood levels checked

Question 3

Cyclosporine (Sandimmune) - AE

Answer 3

• nephrotoxicity
• infection
• hepatotoxicity
• leukopenia
• anaphylactic rxn
• hirsutism

Question 4

Cyclosporine (Sandimmune) - drug interactions that decrease levels

Answer 4

• phenytoin
• phenobarbital
• carbamazepine
• rifampin

Question 5

Cyclosporine (Sandimmune) - drug interactions that increase levels

Answer 5

• azole antifungals
• amphotericin B
• macrolide antibiotics

Question 6

CS - more interactions

Answer 6

• nephrotoxic drugs
• grapefruit juice
• repaglinide (Prandin) - oral hypoglycemic drug

Question 7

Tacrolimus (Prograf)

Answer 7

• alternate to cyclosporine
• more toxic
• concurrent use with glucocorticoids
• prophylaxis of organ rejection
• AE: NEPHROTOXICITY, neurotoxicity, GI, hypertension, hyperkalemia, hyperglycemia, hirsutism, gum hyperplasia, anaphylaxis (IV)

Question 8

TP - interactions

Answer 8

• agents that inhibit CYP3A
• grapefruit juice
• NSAIDS

Question 9

mTOR

Answer 9

• structurally similar to tacrolimus
• suppresses B cell and T cell proliferation
• mammalina target of rapamycin (mTOR)

Question 10

Sirolimus (Rapamune) - mTOR inh.

Answer 10

• renal transplant rejection
• used with glucocorticoids and cyclosporine
• AE: increased risk for infection, increases cholesterol and triglycerides, rick of renal injury, rash, acne, anemia, thrombocytopenia, joint pain, diarrhea, and hypokalemia
• DI: drugs that inhibit/induce CYP3A4, high-fat foods, and grapefruit juice

Question 11

Cytotoxic drugs

Answer 11

• suppresses by killing B and T lymphocytes undergoing proliferation
• toxic to all proliferating cells
• AE: bone marrow suppression, GI, reduced fertility, alopecia (hair loss)

Question 12

Azathioprine (Imuran)

Answer 12

• cytotoxic drug
• used for autoimmune diseases and transplants
• AE: bone marrow suppression, mutagenic and teratogenic, neoplasms

Question 13

Cyclophosphamide (Cytoxan, Neosar)

Answer 13

• anticancer drug

Question 14

Methotrexate (Rheumatrex, Trexall)

Answer 14

• anticancer agent
• autoimmune disorders
• suppression of B and T lymphocytes

Question 15

Mitoxantrone (Novantrone)

Answer 15

• anticancer agent
• reductions of neurologic disability and clinical relapse for MS patients
• dangerous drug reserved for pts who are not responsive to safer drugs

Question 16

Muromonab-CD3 (Orthoclone OKT3)

Answer 16

• monoclonal antibody
• blocks T cell fx, prevents acute rejection of transplants, depletes T cells before bone marrow transplant
• AE: fever, chills, dyspnea, chest pain, N/V

Question 17

Basiliximab

Answer 17

• monoclonal antibodies
• blocks activation of T cells by IL-2
• prophylaxis of acute organ rejection