PK

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Author:
ch.tyrrell
ID:
150732
Filename:
PK
Updated:
2012-04-28 17:45:45
Tags:
Immunosuppressants Lec
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Description:
Immunosuppressants
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  1. When is therapeutic drug monitoring (TDM) implemented?
    • 1. critically-dosed agents
    • 2. critically-dosed immunosuppressants
  2. What is the dosing conversion from IV to PO for cyclosporine?
    IV is 1/3 of PO dose

    (3:1 conversion ration PO: IV)
  3. What kind of Vd does Cyclosporine have?
    Large Vd = 3-7 L/kg
  4. What is the intial dose of cyclosporine?
    2.5 mg/kg PO q 12h
  5. What is the target therapeutic range (Co level) of cyclosporine?
    200-300 ng/ml during the first 6 months post-transplant in kidney and liver transplant patients

    300-400 ng/ml during the first 6 months post-transplant in heart/lung transplant patients
  6. When should cyclosporine steady state Co levels be monitored?
    • 3x per week x 1st month
    • 2x per week x next 2 months
    • weekly x 3 months
    • monthly thereafter or after any dose change
  7. What is the dose adjustment for cyclosporine?
    adjust doses by 25-50 mg PO q 12h to achieve therapeutic levels
  8. What is the dosing for Tacrolimus?
    0.075 mg/kg PO q 12h then titrated based on steady state trough (Co) blood levels
  9. What is the target therapeutic range (Co level) for Tacrolimus?
    5-15 ng/ml, depending on transplant type and time post-transplant
  10. What is the monitoring of steady state Co levels for Tacrolimus?
    • 3x per week x 1st month
    • 2x per week x next 2 months
    • weekly x 3 months
    • monthly thereafter or after any dose change
  11. What is the dose adjustment for Tacrolimus?
    Adjust dose by 1-2mg PO q 12h to achieve therapeutic levels
  12. Sirolimus is available is what formulation?
    oral tablets, oral solution and coated arterial stents
  13. What is the half-life of Sirolimus?
    57-63 hours
  14. What are the loading and maintenance doses of Sirolimus?
    Loading: should be 3x the maintenance dose


    • Kidney/liver: LD = 6mg MD = 2mg daily
    • Heart/lungs: LD = 15mg MD = 5mg daily
  15. What is the target therapeutic range (Co level) of Sirolimus?
    5-15 ng/ml (similar to tacrolimus), depending on transplant type, concurrent immunosuppressants, and time post-transplant
  16. Which CYP3A4/P-gp inhibitors increase the concentration of immunosuppressive agents by interferring with their metabolism?
    • macrolide antibiotics (except azithromycin)
    • non-DHP CCB (verapamil & diltiazem)
    • azoles
    • protease inhibitors
  17. Which CYP3A4/P-gp inducers decrease the concentration of immunosuppressive agents by interfering with their metabolism?
    • phenytoin
    • phenobarbital
    • rifampin/rifabutin
    • carbamazepine
  18. What kind of interaction do statins have with immunosuppressants?
    They are CYP3A4 substrates
  19. What kind of interaction can occur with statins and immunosuppressants?
    Potential to increase statin concentrations with concomitant use
  20. Describe statin-induced myositis.
    • dose-dependent reduction of vascular smooth-muscle cell proliferation
    • statins cause release of myoglobin from breakdown of muscle cells
    • myoglobin causes renal injury or failure

    myalgia-->myopathy-->rhabdomyolysis
  21. What effect does grapefruit juice have on CSA/TAC/SRL drug concentrations?
    increase
  22. What effect does St. John's Wort have on CSA/TAC/SRL drug concentrations?
    decrease
  23. What are the consequences of supratherapeutic levels of CSA/TAC concentrations?
    • nephrotoxicity
    • over-immunosuppression (inc risk of infections)
    • hypertension
    • tremors (specifically TAC)
    • electrolyte abnormalities
  24. What are the consequences of subtherapeutic levels of CSA/TAC concentrations?
    transplant rejection
  25. What are the consequences of supratherapeutic levels of SRL concentrations?
    • over-immunosuppression (inc risk of infections)
    • anemia
    • leukopenia
    • thrombocytopenia
  26. What are the consequences of subtherapeutic levels of SRL concentrations?
    transplant rejection
  27. What is the ceiling statin dose?
    One-half of normal dose (maximum)
  28. When should CSA and TAC levels be checked?
    at least 2-3 days after any dosage change depending on interacting drug
  29. When should SRL levels be checked?
    one week after dose changes depending on interacting drug
  30. What is the guideline for dosage changes for CSA?
    CSA doses may be increased or decreased by 25-50 mg PO q 12h depending on toxicity or efficacy issues
  31. What is the guideline for dosage changes for TAC?
    TAC doses may increased or decreased by 1-2 mg PO q 12h
  32. What is the guideline for dosage changes for SRL?
    SRL doses may increased or decreased by 1-2 mg PO daily

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