CLASSIFICATION OF IMMUNOSUPPRESSIVE AGENTS
Immunosuppressive agents (IMS) are prescribed for early-stage immunosuppression, the management of late-stage immunosuppression, or the maintenance of organ rejection. In general, they are classified as induction therapies, maintenance therapies, and antirejection therapies.
Induction therapies: Therapies given immediately after transplant to prevent acute rejection. Maintenance therapies: Consist of all immunosuppressive medications prescribed before, during, or after transplant and with the purpose of long-term use. Antire-jection immunosuppression: Involves all immuno-suppressive medications prescribed for dealing with an episode of acute rejection in the initial post-transplant period or during a specific follow-up period, typically up to 30 days after the diagnosis of acute rejection.
The major IMS agents include a combination of agents, including calcineurin inhibitors (tacrolimus and cyclosporine), antimetabolites (mycophenolate mofetil and azathioprine), mammalian target of rapamycin inhibitors (everolimus and sirolimus), and corticosteroids(IV methyl-prednisolone and oral prednisone).
The primary goal in post-transplant pts is to individualize therapy to include the optimal combination of IMS, which can improve pt survival by preventing acute rejection, while also preventing or decreasing the incidence of adverse effects.
IMMUNOSUPPRESSIVE AGENTS
| Name | Class | Action | Indication | Adverse effects |
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| Azathioprine (Imuran) | Antimetabolite | Inhibition of purine synthesis and B and T cells | Prevent rejection renal transplantation | Myelosuppression, hepatitis | | Basiliximab (Simulect) | IL-2 receptor antagonist | Inhibits IL-2 mediated activation of lymphocytes | Renal transplant (prophylaxis of acute rejection) | Constipation, nausea, vomiting, diarrhea, dyspepsia | | Belatacept (Nulojix) | Selective T-cell co-stimulation blocker | Fusion protein blocks interaction to actiivate T lymphocytes | Renal transplant (prophylaxis of acute rejection) | Anemia, diarrhea, peripheral edema, UTI, constipation, cough, nausea, vomiting, leukopenia | | Cyclosporine (Neoral, Gengraf) | Calcineurin inhibition | Blocks T-cell transcription | Prophylaxis of organ rejection in kidney, liver and heart transplants | Nephrotoxicity, neurotoxicity, hy-perlipidemia, diabetes, hepatotoxicity, refractory hypertension | | Everolimus (Zortress) | mTOR kinase inhibitor | Inhibits lymphocyte response to cytokine stimulation | Prophylaxis of organ rejection in kidney (low to moderate risk), liver transplants | Peripheral edema, hypertension, hyperlipidemia, anemia, leukope-nia | | Mycophenlate (Cellcept, Myfortic) | Antimetabolite | Exhibits cytostatic and reversible effect on B and T lymphocytes | Prophylaxis of organ rejection in kidney, liver and heart transplants | Diarrhea, leukopenia, infection, vomiting | | Sirolimus (Rapamune) | mTOR kinase inhibitor | Inhibits lymphocyte response to cytokine stimulation | Prevent rejection renal transplantation | Peripheral edema, hypertriglyceridemia, hypertension, hyperlipidemia, abdominal pair, diarrhea, fever, UTI, anemia, thrombocytopenia | | Tacrolimus (Prograf) | Calcineurin inhibition | Blocks T-cell transcription | Prophylaxis of organ rejection in kidney, liver, lung and heart transplants | Hypertension, diabetes, fever, leukopenia, UTI, headache, abdominal pain, peripheral edema, hyperkalemia, hyperlipidemia |
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