PK

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What is the MOA of methotrexate

blocks dihydrofolate reductase which blocks actions of folic acid
Describe the pharmacokinetics of methotrexate
- A: 100% bioavailable; saturable
- D: multi-compartmental
- M: minimal
- E: predominately renal
What are the uses of methotrexate?
- 1. oncology related: leukemias, lymphomas, etc.
- 2. non-oncologic uses: RA, servere psoriasis, etc.
What are the methotrexate rescue therapy options?
- Leucovorin (folinic acid)
- Glucarpidse (Voraxaze)
What is leucovorin and how does it work?
- Methotrexate rescue therapy
- Restores folate stores needed for purine/pyrimidine sythesis
- Given with high-dose methotrexate regimens to help prevent toxicities
What is Glucarpidase and how does is work?
- Methotrexate rescue therapy
- Converts methotrexate to inactive metabolites
- Indicated when methotrexate concentration is in toxic range, specifically for patients w/ impaired renal function
If administered together, how far apart should Leucovorin and Glucarpidase be separated?

Leucovorin should not be administered within 2 hours of Glucarpidase.

Glucarpidase will break down leucovorin b/c it is structurally similar
What is the goal of therapeutic drug monitoring (TDM) for methotrexate?

To prevent methotrexate toxicity
What is the MOA of busulfan?

An alkylating agent that binds to DNA and prevents it from replicating and moving forward
What are the uses of busulfan?
- leukemia
- conditioning regimen for hematopoietic stem cell transplant
What is the goal of TDM for bsulfan?

to maintain therapeutic concentration
What is the risk associated with supratherapeutic concentrations of busulfan?

liver injury = sinusoidal obstruction syndrome (veno-occlusive disease)

Author

ch.tyrrell

150787

Card Set

Description

Chemotherapy (7)

Updated

2012-04-29T00:47:29Z

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