Term
Cyclosporine
MOA
Metabolism
Side effects
Use |
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Definition
MOA: Binds to cyclophilin--> inhibition of calcineurin phosphatase--> decreased activation of NF-AT--> decreased production of IL-2
Metabolism: CYP3A (need therapeutic drug monitoring)
Side effects: HTN, hyperglycemia, hyperkalemia, neurotoxicity, renal dysfunction, hirsutism, gingival hyperplasia, hepatotoxicity, increased risk of infections and malignancies.
Renal transplant |
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Term
Drugs that increase the concentration of cyclosporine |
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Definition
Ca channel blockers
Antifungals (Ketoconazole)
Antibiotics (Erythromycin)
Methyprednisolone |
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Term
Drugs that decrease the concentration of cyclosporine |
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Definition
Phenobarbital
Phenytoin
Carbamazepine
Rifampin
St. Johns Wort |
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Term
Tacrolimus
MOA:
Metabolism:
Side Effects: |
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Definition
MOA: Binds to FK binding protein--> inhibition of calcineurin phosphatase--> decreased activation of NF-AT--> decreased IL-2 synthesis
Metabolism: CYP 3A
Side effects: Renal, HTN, neurotoxicity, hyperglycemia, hyperkalemia, GI problems, increased risk of infections and malignancy |
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Term
Sirolimus
MOA
Metabolism
Side effects |
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Definition
MOA: Binds to FK binding protein 12--> inhibition of mammalian target of rapamycin--> inhibition of interleukin-driven T cell proliferation
Metabolism: CYP 3A
Side Effects: Hyperlipidemia, myelosuppression, pneumonitis, increased risk of malignancy and infections |
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Term
Mycophenolate mofetil
MOA:
Side Effects:
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Definition
MOA: converted to mycophenolic acid which inhibits inosine monophosphate dehydrogenase which leads to inhibition of de novo synthesis of inosine monophosphate dehydrogenase. This is selective for lymphocytes.
Side Effects: GI (Vomiting, diarrhea), neutropenia, Increased risk of infections and malignancies, teratogenic |
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Term
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Definition
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Term
Thalidomide
Side effects
Use |
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Definition
Side Effects: Teratogenicity which causes birth defects and death in even a single dose. Required to use System for Thalidomide Education and Prescribing Safety (STEPS)
Other side effects: peripheral neuropathy, increased risk of venous thromboembolic events (DVT, PE)
Use: Multiple myeloma, erythema nodosum leprosum |
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Term
Muromonab-CD3
Binds to
Use |
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Definition
CD3
Renal transplant rejection |
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Term
Basiliximab, Daclizumab
Binds to
Example of use |
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Definition
Binds to: IL-2 receptor
Renal transplantation |
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Term
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Definition
TNF
Rheumatoid arthritis and IBD |
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Term
Etanercept
Binds to
Example of Use |
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Definition
TNF receptor
Rheumatoid Arthritis |
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Term
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Definition
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Term
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Definition
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