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What is the MOA of methotrexate?
- blocks the actions of folic acid by blocking dihydrofolate reductase
- blocks the synthesis of purines and DNA
What is the absorption of methotrexate?
100% for doses below 30 mg/m2
What is the percentage of methotrexate bound to proteins?
What is the Vd of methotrexate? What type of compartment model does methotrexate follow?
- 0.2-0.5 L/kg
What is the distribution 1/2 life of methotrexate? elimination 1/2 life?
With an increase or decrease in urine pH will you see methotrexate precipitate and cause nephrotoxicity?
What is leucovorin?
- Folinic acid
- Restores folate stores needed for purine/pyrimidine synthesis
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
What are some side effects of methotrexate?
- Inflammation of the GI tract
What is the goal methotrexate concentration?
< 0.1 micromolar by 48 hours following initiation
What is the percentage of absorption for busulfan?
What percentage of busulfan binds to plasma proteins? RBCs?
What type of metabolism do busulfan undergo?
- Glutathione conjugation
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
What is the target range of busulfan?
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