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Immunosupressants: What is the MOA of cyclosprine?
cyclosporine (Sandimmune or Neoral) belongs to calcineurin inhibitors, which means it inhibits calcineurin-dependent translocation of cytosolic subunit of nuclear factor of activated T-cells
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cyclosporine interacts with what diseases?
- DM (worsens glycemic control)
- (tacrolimus also interacts with DM)
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What are some SE of cyclosporine?
CNS(seizure,hallucination, insomnia), gingivial hyperplasia, HTN, hepatotoxic, nephrotoxic, DM, hyperlipidemia, hyperkalemia, hypomagnesemia, hirsutism
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What are some drug interactions with cyclosporine? (metabolized by CYP450, 3A)
- CYP3A4 inducers: phenytoin, phenobarbital, carbamazepine, nevaripine, efavirenz, st.john wort, rifampin
- CYP3A4 inhibitors: grape juice, non-dihydropyridines (CCB), azoles, most protease inhibitors
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Coadministration of statin (lova, simva,atrovastatin) with cyclosporine does what?
increase HMG-CoA, increased risk of rhabdomyolysis
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What is the MOA tacrolimus?
tacrolimus (Prograf) belongs to calcineurin inhibitors; it inhibits translocation of cytosolic subunit of nuclear factor of activated t-cells
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What are drug interactions with tacrolimus?
metabolized by CYP450; 3A isoenzymes.. same drug interactions as with cyclosporine
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What are some SE of tacrolimus?
CNS(seizure, hallucincations,insomnia),alopecia, HTN, hepatotoxic, DM, nephrotoxic, hyperlipidemia, hyperkalemia, hypomagnesemia, anemia
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What is the MOA of sirolimus?
sirolimus (Rapamune) belongs to mTOR inhibitors; it binds to FKBP-12 to form a complex that binds and inhibits activation of its target protein mTOR (mammalian target of rapamycin)
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What are the drug interactions with sirolimus?
- metabolized by CYP450;3A isoenzymes.
- same as with cyclosporine and tacrolimus
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What are the disease and sirolimus interactions?
liver transplant(increase mortality), lung transplant(fatal bronchical...)
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What are the SE of sirolimus?
anorexia, oral ulcers, GI, hyperlipidemia, HTN, hyperkalemia, leukopenia, thrombocytopenia
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What drugs belong to calcineurin inhibitors?
cyclosprine and tacrolimus
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What drugs belong to antiproliferative agents?
azathioprine, mycophenolate mofetil/sodium
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What is the MOA of azathioprine?
azathioprine(Imuran) is a purine analogue prodrug cleaved to mecaptopurine and inhibit synthesis of DNA,RNA, and protein
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What are drug interactions with azathioprine?
concominant use with allopurinol will increase effect of azathioprine (when used together decrease dose by 65-75%)
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What are disease interactions with azathioprine?
renal insufficiency
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What are SE of azathioprine?
retinopathy, GI, neutropenia, thrombocytopenia
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What is the MOA of mycophenolate mofetil?
brand name Cellcept belongs to antiproliferative agents, is metabolized to mycophenolic acid which cause noncompetitive reverse inhibition of inosine monophosphate dehydrogenase (critical enzyme in denovo pathway of purine synthesis) which is crucial during lymphocyte activations and proleferation
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What are the drug interactions of mycophenolate mofetil?
cyclosporine, cholestyramine, colestipol and colesevelam, antacids, efficacy of brith control may be decreased
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What are disease and mycophenolate mofetil interactions?
severe renal impairment
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What are the SE of mycophenolate mofetil?
GI, leukopenia, thrombocytopenia, anemia
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What is the MOA of mycophenolate sodium?
brand name is Myfortic, MOA is same as mycophenolate mofetil except it comes in delayed relase tabs. and that delivers the mycophenolic acid
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What are drug interactions with mycophenolate sodium?
cholestyramine, antacids, efficacy of birth control may be decreased?
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What are the disease and mycophenolate sodium interactions and SE of drug?
same as with mycophenolate mofetil
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What IV corticosteroids are used with transplant drugs?
methylprednisolone and dexamethasone
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What are oral corticosteroids that are used with transplant drugs?
prednisone, prednisolone, dexamethasone
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What are the drug interactions with corticosteroids?
- metabolized by CYP450;3A isoenzymes
- same as with cyclosprine and tacrolimus
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What are disease and corticosteroids interactions?
DM, osteopenia, osteoporosis
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What are some SE with corticosteroids?
CNS(ex.insomnia), HTN, edema, DM, hyperlipidemia, growth supression, hirsutism, myopathy, and osteoporosis
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What drugs belong to monoclonal antibodies class?
muromonab-CD3, basiliximab, daclizumab
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What premedications need to be given before IV bolus orthoclone (muromonab-CD3)?
IV steroids, tylenol, antihistamines 1hr. prior to dose
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What needs to be assessed prior to dose of orthoclone?
volume status (pt. with volume overload or uncompensated CHF (coronary heart failure) should not get this drug)
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What are the SE of orthoclone?
dizzy, HA, photophobia, tachycardia, tremor, pulmonary edema
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What are the SE of basiliximab(Simulect)-(Ig6) or daclizumab(Zenapax)?
hypersensitivity, including anaphylaxis
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What drugs belong to polyclonal antibodies?
- antithymocyte globulin(equine) (Agam)
- antithymocyte globulin(rabbit) (hymoglobulin)
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What drugs need to be given before polyclonal antibodies?
IV steroids,tylenol, antihistamine 1hr prior to dose
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What are SE and monitoring of polyclonal antibodies?
- infusion related reactions(fever,chills,dypnea), leukopenia, thrombocytopenia
- Monitoring: goal for tx. of acute rejection is supression of CD3 lineage to <50cells/mm3
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