1. What is the MOA of methotrexate?
    • anti-folate
    • blocks the actions of folic acid by blocking dihydrofolate reductase
    • blocks the synthesis of purines and DNA
  2. What is the absorption of methotrexate?
    100% for doses below 30 mg/m2
  3. What is the percentage of methotrexate bound to proteins?
  4. What is the Vd of methotrexate? What type of compartment model does methotrexate follow?
    • 0.2-0.5 L/kg
    • Multicompartmental
  5. What is the distribution 1/2 life of methotrexate? elimination 1/2 life?
    • 2-3 hrs
    • 10 hrs
  6. With an increase or decrease in urine pH will you see methotrexate precipitate and cause nephrotoxicity?
  7. What is leucovorin?
    • Folinic acid
    • Restores folate stores needed for purine/pyrimidine synthesis
  8. What is glucarpidase?
    • Drug that converts methotrexate to inactive metabolites
    • Used mainly in emergency situations when methotrexate is in toxic ranges--specifically for patients with impaired renal function
    • Must be separated from leucovorin by 2 hours
  9. What are some side effects of methotrexate?
    • stomatitis
    • Inflammation of the GI tract
    • immunosuppression
  10. What is the goal methotrexate concentration?
    < 0.1 micromolar by 48 hours following initiation
  11. What is the percentage of absorption for busulfan?
  12. What percentage of busulfan binds to plasma proteins? RBCs?
    • 32%
    • 47%
  13. What type of metabolism do busulfan undergo?
    • Hepatic
    • Glutathione conjugation
    • Oxidation
  14. What is sinusoidal obstructionsyndrome?
    • AKA veno-occlusive disease
    • Primary injury to liver due to supratherapeutic concentrations of Busulfan
    • Significant post-transplant complication leading to mortality
  15. What is the target range of busulfan?
    5-7 mcg/ml/hr
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