Drugs Flashcards
Drug: Azathioprine
“Mechanism: Antimetabolite precursor of 6-mercaptopurine; inhibits lymphocyte proliferation by blocking nucleotide synthesis.”
Azathioprine - Indications
“Rheumatoid arthritis
Azathioprine - Toxicity
“Pancytopenia.”
Azathioprine - Notes
“6-MP degraded by xanthine oxidase; toxicity is increased by allopurinol. Pronounce ‘azaTHIOpurine’.”
Drug: Mycophenolate mofetil
“Mechanism: Reversibly inhibits IMP dehydrogenase
Mycophenolate mofetil - Indications
“Glucocorticoid-sparing agent in rheumatic disease.”
Mycophenolate mofetil - Toxicity
“GI upset
Mycophenolate mofetil - Notes
“Associated with invasive CMV infection; less nephrotoxic and neurotoxic.”
Drug: Glucocorticoids
“Mechanism: Inhibit NF-κB; suppress B- and T-cell function by decreasing transcription of many cytokines; induce T-cell apoptosis.”
Glucocorticoids - Indications
“Many autoimmune and inflammatory disorders
Glucocorticoids - Toxicity
“Cushing syndrome
Glucocorticoids - Notes
“Abrupt discontinuation may cause adrenal insufficiency due to suppressed endogenous production.”
Drug: Cyclosporine
“Mechanism: Calcineurin inhibitor; binds cyclophilin. Blocks T-cell activation by preventing IL-2 transcription.”
Cyclosporine - Indications
“Psoriasis
Cyclosporine - Toxicity
“Nephrotoxicity
Cyclosporine - Notes
“Highly nephrotoxic
Drug: Tacrolimus (FK506)
“Mechanism: Calcineurin inhibitor; binds FKBP. Blocks T-cell activation by preventing IL-2 transcription.”
Tacrolimus - Indications
“Immunosuppression after solid organ transplant.”
Tacrolimus - Toxicity
“Increased risk of diabetes and neurotoxicity; no gingival hyperplasia or hirsutism.”
Drug: Sirolimus (Rapamycin)
“Mechanism: mTOR inhibitor; binds FKBP. Blocks T-cell activation and B-cell differentiation by preventing response to IL-2.”
Sirolimus - Indications
“Kidney transplant rejection prophylaxis.”
Sirolimus - Toxicity
“Pancytopenia
Sirolimus - Notes
“Synergistic with cyclosporine; also used in drug-eluting stents.”
Drug: Basiliximab
“Mechanism: Monoclonal antibody; blocks IL-2R.”
Basiliximab - Indications
“Edema
Bone marrow stimulation: Erythropoietin
“Agent: Epoetin alfa (EPO analog). Clinical Uses: Anemias (especially in renal failure). Associated with increased risk of hypertension and thromboembolic events.”
Colony-stimulating factors
“Agent: Filgrastim (G-CSF)
Thrombopoietin
“Agent: Romiplostim (TPO analog)
Immunotherapy: Interleukin-2
“Agent: Aldesleukin. Clinical Uses: Renal cell carcinoma
Immunotherapy: Interferons
“IFN-α: Chronic hepatitis B and C
