Term
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Definition
| Calcineurin Inhibitor 2. Blocks calcineurin activity à Blocks IL-2 txn 3. Renal toxicity (70% of patients); hypertension in DM patients; tremors, hirsutism; increased risk of malignancy and infection 4. Interacts with drugs that affect P450 enzymes (NO grapefruit); **RENAL TOXICITY is enhanced by SIROLIMUS via reduced drug metab |
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Term
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Definition
| Calcineurin Inhibitor Blocks calcineurin activity à blocks IL-2 txn (100x more potent than cyclosporine) 3.Renal toxicity (70% of patients); hypertension in DM patients; tremors, hirsutism; increased risk of malignancy and infection 4.Interacts with drugs that affect P450 enzymes (NO grapefruit); **RENAL TOXICITY is enhanced by SIROLIMUS via reduced drug metab. |
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Term
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Definition
| mTOR inhibitor 2. Blocks mTOR (serine/thr kinase) activity in signaling pathways that affect cell growth/metab 3. Dose-dependent increased in TAGs and cholesterol; enhances calcineurin inhibitors’ NEPHROTOXICITY (extending half-life); anemia; leukopenia; infections 4. Drugs that affect CYP3A4 and P glycoprotein; **Use enhances RENAL TOXICITY of calcineurin inhibitors |
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Term
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Definition
| mTOR inhibitor 2.Blocks mTOR (serine/thr kinase) activity in signaling pathways that affect cell growth/metab 3. Dose-dependent increased in TAGs and cholesterol; enhances calcineurin inhibitors’ NEPHROTOXICITY (extending half-life); anemia; leukopenia; infections 4. Drugs that affect CYP3A4 and P glycoprotein; **Use enhances RENAL TOXICITY of calcineurin inhibitors |
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Term
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Definition
| Cytotoxic agent, DMARD 2. Metabolized into 6-thioguanine, which then can block (1) de novo purine synthesis and (2) DNA replication (via 6-thio-dGTP) 3. Bone marrow suppression, GI disturbances, increased risk of infections and neoplasias 4. Mainly metabolized by **xanthine oxidase; longer half-life of azathioprine if using Allopurinol |
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Term
| Mycophenolate mofetil (MMF) |
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Definition
| Cytotoxic agent, DMARD 2. Inhibits IMP dehydrogenase (blocks de novo purine synthesis) 3. GI disturbances, myelosuppression, headache, hypertension 4. Approved by FDA to use WITH calcineurin inhibitors and corticosteroids . |
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Term
| Anti-lymphocyte/thymocyte globulin (ATG) |
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Definition
| Immunosuppressive polyclonal antibodies (often from rabbit serum) 2. Binds circulating lymphocytes, depletes thymus-dependent lymphocytes (T-cells) 3. Potential for serum sickness (antibodies made from rabbit serum); increased risk of infections/neoplasias, leukopenia, thromocytopenia 3. no sighnicant drug interactions |
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Term
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Definition
| Immunosuppressive human monoclonal Ab 2. Monoclonal antibody to alpha subunit of IL-2R on activated T-cell 3. Immunosuppression (used against acute rejection in transplant recipients) 4. Less toxicity due to specificity; increase risk of infections/neoplasias 4. No significant drug interactions |
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Term
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Definition
| Immunosuppressive mouse monoclonal Ab 2. Monoclonal antibody to CD3 subunit of TCRs on T-cells 3. Serum sickness to murine protein; increase risk of infections/neoplasias |
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