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20 Cards in this Set
- Front
- Back
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IMMUNOSUPPRESSANTS:
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Calcineurin inhibitors:
- Cyclosporine - Tacrolimus |
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Metabolite of the fungus B. Nivea
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Cyclosporine (SANDIMMUNE, NEORAL)
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MOA of Cyclosporine:
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Inhibits antigen-triggered signal transduction in T-lymphocytes.
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CYCLOPHILIN:
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Cytoplasmic receptor protein
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Indication for cyclosporin
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1. organ transplant
2. RA 3. PSORIASIS |
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Cyclosporin used in combo with:
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1. glucocorticoids
2. AZA 3. Mycophenolate mofetil 4. sirolimus |
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MOST COMMON SIDE EFFECT OF CYCLOSPORIN:
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1. Nephrotoxicity
2. HTN - 50% of renal transplant and almost all cardiac transplant |
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Drugs that DECREASE cyclo.
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1. Rifampin
2. Phenobarbital 3. Phenytoin. |
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Increase cyclo:
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1. Verapamil, nicardipine
2. Fluconazole, Keto 3. Erythromycin 4. Indinavir 5. Grape fruit juice |
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Cyclo reduces CL
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1. digoxin
2. lovastatin 3. prednisolone |
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TACROLIMUS same pathway except binds to:
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FKBP-12 an immunophilin structually related to cyclophilin.
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Therapeutic Dosage
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Prophylaxis of solid organ rejection.
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Toxicity of Tacrolimus:
if switching b/w cyclo wait for 24 hrs. |
Nephrotoxicity
Neurotoxicity GI complaint Hypertension Hyperkalemia Hyperglycemia |
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Nephrotoxicity of Tacrolimus:
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Negative effect of pancreatic islet beta cells:
1. glucose intolerance 2. diabetes mellitus 3. increased risk of secondary tumors and opportunistic infections. |
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RAPAMUNE (Sirolimus/Rapamycin)
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Macrocyclic lactone produced by STREPTOMYCES HYGROSCOPICUS
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RAPAMUNE
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inhibits the mammalian kinase, target of rapamycin (mTOR)
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rapamune used in conjunction with:
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calcineurin inhibitor and glucocorticoids for PROPHYLAXIS of organ transplant rejection
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Use of Sirolimus:
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dose-dependent increase in serum cholesterol and TG that may require tx.
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Mycophenolate Mofetil (cellcept)
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- ester prodrug
- mycophenolic drug (active drug) INHIBITS INOSINE MONOPHOSPHATE DEHYDROGENASE |
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CELLCEPT is decreased absorption when:
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CO-ADM with Al/Mg hydroxide
cholestyramine |
