I

Immunosuppressive Agents

USES

Improvement of both short- and long-term allograft survivals.

ACTION

Basiliximab: An interleukin-2 (IL-2) receptor antagonist inhibiting IL-2 binding. This prevents activation of lymphocytes, and the response of the immune system to antigens is impaired.

Cyclosporine: Inhibits production and release of IL-2.

Daclizumab: An IL-2 receptor antagonist inhibiting IL-2 binding.

Mycophenolate: A prodrug that reversibly binds and inhibits inosine monophosphate dehydrogenase (IMPD), resulting in inhibition of purine nucleotide synthesis, inhibiting DNA and RNA synthesis and subsequent synthesis of T and B cells.

Sirolimus: Inhibits IL-2–stimulated T-lymphocyte activation and proliferation, which may occur through formation of a complex.

Tacrolimus: Inhibits IL-2–stimulated T-lymphocyte activation and proliferation, which may occur through formation of a complex.

IMMUNOSUPPRESSIVE AGENTS

Name	Availability	Dosage	Side Effects
Basiliximab (Simulect)	I: 10 mg, 20 mg	20 mg for 2 doses (on day of transplant, then 4 days after transplantation)	Abdominal pain, asthenia, cough, dizziness, dyspnea, dysuria, edema, hypertension, infection, tremors
Cyclosporine (Neoral, Sandimmune)	C: 25 mg, 50 mg, 100 mg S: 100 mg/ml I: 50 mg/ml	Dose dependent on type of transplant and formulation	Hypertension, hyperkalemia, nephrotoxicity, coarsening of facial features, hirsutism, gingival hyperplasia, nausea, vomiting, diarrhea, hepatotoxicity, hyperuricemia, hypertriglyceridemia, hypercholesterolemia, tremors, paresthesia, seizures, risk of infection/malignancy
Mycophenolate (CellCept, Myfortic)	Cellcept: C: 250 mg I: 500 mg S: 200 mg/ml T: 500 mg Myfortic: T(DR): 180 mg, 320 mg	Cellcept: 1–1.5 g 2 times/day based on type of transplant Myfortic: Renal: 720 mg 2 times/day	Diarrhea, vomiting, leukopenia, neutropenia, infections
Sirolimus (Rapamune)	S: 1 mg/ml T: 0.5 mg, 1 mg, 2 mg	2–6 mg/day	Dyspnea, leukopenia, thrombocytopenia, hyperlipidemia, abdominal pain, acne, arthralgia, fever, diarrhea, constipation, headaches, vomiting, weight gain
Tacrolimus (Prograf)	C: 0.5 mg, 1 mg, 5 mg I: 5 mg/ml C(ER): 0.5 mg, 1 mg, 5 mg T(ER): 0.75 mg, 1 mg, 4 mg	Heart: 0.075 mg/kg/day in 2 divided doses q12h Kidney: 0.1–0.2 mg/kg/day in 2 divided doses q12h Liver: 0.1–0.15 mg/kg/day in 2 divided doses q12h	Nephrotoxicity, neurotoxicity, hyperglycemia, nausea, vomiting, photophobia, infections, hypertension, hyperlipidemia

C, Capsules; DR, Delayed release; ER, extended release; I, injection; S, oral solution or suspension; T, tablets.