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kyleannkelsey
on FreezingBlue Flashcards.
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Is Tacrolimus (FK506) or Cyclosporine (CsA) more likely to cause HYPERlipidemia?
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Is Tacrolimus (FK506) or Cyclosporine (CsA) more likely to cause Myocardial Hypertrophy?
- Same risk
- May be due to HTN
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Is Tacrolimus (FK506) or Cyclosporine (CsA) more likely to cause Hirsutism?
CsA
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Is Tacrolimus (FK506) or Cyclosporine (CsA) more likely to cause Alopecia?
FK
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Is Tacrolimus (FK506) or Cyclosporine (CsA) more likely to cause electrolyte imbalances?
Same risk
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What types of electrolyte imbalances are common with Calcineurin inhibitors?
Increased K and decreased Mg
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What drugs cause increased Calcineurin inhibitor levels?
- Azoles
- Dilt/Verap
- Macrolides (Azith, Clarith, Eryth, Telith)
- PIs
- Grapefruit juice
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What drugs cause decreased Calcineurin Inhibitor levels?
- Phenytoin, Phenobarbital, Carbamazepine
- Rifampin
- St. John’s Wart
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What is the MOA of Sirolimus (Rapamune)?
- Macrolide immunosuppressant
- Binds to FK, which binds to mTOR
- Inhibits T cell proliferation by inhibiting cellular response to IL-2
- Prevents B cell differentiation/antibody production
- Also has antifungal and antitumor properties
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When is Sirolimus (Rapamune) used/not used?
- Renal transplants (low-high risk)
- Higher risk of hepatic artery thrombosis = so not best for liver transplant
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What are the dosing/admin considerations for Sirolimus (Rapamune)?
- No body weight dosing
- Load: 6 mg PO ASAP postop
- Maintenance: 2 mg PO QD
- 1 & 2 mg tablets
- Avoid light
- Refrigerate
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What monitoring should be done for Sirolimus (Rapamune)?
- 1st year Trough: 16-24 ng/mL
- > 1 year postop Trough: 12-20 ng/mL
- Concurrently w/ CsA: 10-15 ng/mL
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What are the AE for Sirolimus (Rapamune)?
- Leukopenia
- Thrombocytopenia
- Hyperlipidemia
- CYP3A4 and pgp substrate and inhibitor
- Vori and Keto CI (increases conc 10x)
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When is Everolimus (Zortress) used/not used?
- Only for Kidney Transplant LOW-MOD
- Not used in severe risk patients
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What are the dosing/admin concerns for Everolimus (Zortress)?
- No loading dose
- Take w/ or w/o food, but be consistent
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What is the MOA for corticosteroids?
- Inhibition of Cytokines (IL-1,2,3,6 & TNFa)
- Interfere w/ cell migration and recognition
- Inhibition IL-1 secretion from macrophages
- Decreased IL-2 secretion from T cells
- Inhibit generation of CD8+ T cells
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What is a normal dose of Corticosteroids during induction?
IV methylpred 3 mg/kg
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What is a normal dose of Corticosteroids during maintenance therapy?
- IV Methylpred Postop day 1: 0.5-2 mg/kg
- Transition to PO
- Taper over next months to 5-20 mg QD
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What drugs are considered Calcineurin Inhibitor sparing?
Corticosteroids
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What are the AE of Corticosteroids?
- CNS
- HTN
- Infection
- Increased appetite/weight
- OP
- Cataracts
- Glucose intolerance
- HLD
- Cushing’s
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What is the MOA of Mycophenolate (MMF)?
- Selective, reversible inhibitor or inosine monophosphate dehydrogenase (IMPDH) needed for purine synthesis
- Specific for T cells and B cells (more so than Azathioprine)
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When is Mycophenolate (MMF) used/not used?
- Common for both liver and kidney disease
- In combo with a Calcineurin inhibitor
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What are the pharmacokinetics of Mycophenolate (MMF)?
- Absorption of 75% or more
- Increased AUC may occur after chronic use due to enterohepatic recirculation – dose adjust as needed
- Hepatic metabolism
- Renal tubular secretion
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What DDIs does Mycophenolate have?
- Increases Acyclovir and probenecid – competes for renal tubular secretion
- Bile acid resins (cholestyramine, etc.) and Al or Mg based antacids – decrease MMF by 40%
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What Antacids are AL or Mg containing?
- Mg: Equate, Maalox lq, Milk of Magnesia, Rennie, Mylanta, Rolaids and Gelusil
- Al: Equate, Malox lq and Tabs, Mylanta and Gelusil
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What are the dosing/admin concerns for Mycophenolate (MMF)?
- 100 mg Cellcept: 720 mg Myfortic
- Cellcept: 1-1.5g BID, 250 caps and 500 mg tabs
- Myfortic: 720 BID PO, 180 mg and 360mg tabs – better if GI issues occur with Cellcept
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