Chemotherapy

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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
What is the absorption of methotrexate?

100% for doses below 30 mg/m²
What is the percentage of methotrexate bound to proteins?

50%
What is the Vd of methotrexate? What type of compartment model does methotrexate follow?
- 0.2-0.5 L/kg
- Multicompartmental
What is the distribution 1/2 life of methotrexate? elimination 1/2 life?
- 2-3 hrs
- 10 hrs
With an increase or decrease in urine pH will you see methotrexate precipitate and cause nephrotoxicity?

Decrease
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?
- stomatitis
- Inflammation of the GI tract
- immunosuppression
What is the goal methotrexate concentration?

< 0.1 micromolar by 48 hours following initiation
What is the percentage of absorption for busulfan?

70-100%
What percentage of busulfan binds to plasma proteins? RBCs?
- 32%
- 47%
What type of metabolism do busulfan undergo?
- Hepatic
- Glutathione conjugation
- Oxidation
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?

5-7 mcg/ml/hr

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rclee06

144706

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Chemotherapy

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Updated

3/30/2012, 2:36:45 AM

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