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Anti-metabolites
Lecture 2
11
Pharmacology
Professional
04/10/2013

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Cards

Term
What are the different classes of anti-metabolites?
Definition
- Folic acid analogs
- Pyrimidine analogs
- Purine analogs
**All are S phase specific
Term
How is dTMP/thymidylate made?
Definition
dUMP converted to thymidine, phosphorylated using THF. Thymidylate synthase + THF transfers the methyl group.
**Methotrexate blocks DHFR, needed to convert DHF to THF
Term
What is polyglutamated-Methotrexate?
Definition
A form used by the body that inhibits DHFR, thymidylate synthase, and purine synthesis.
Term
How is methotrexate dosed?
Definition
- IV
- Myelosuppression, GI, NEPHROtoxic
**Rescue - leucovorin, but decreases efficacy
Term
How does pemextred compare to methotrexate?
Definition
More potent inhibitor of purines
Better transport into tumor cells
**Also IV, nephrotoxic
Term
What are purines and pyrimidines?
Definition
- Purines: Adenosine and Guanine
- Pyrimidines: Cytosine and thymine
Term
What drugs are pyrimidine (C/T) antagonists?
Definition
- 5-FU - blocks thymidylate synthesis. Fluorine stabilizes complex inactivating enzyme. Give w/ leucovorin. IV
- Capecitabine - prodrug of 5-FU. Can give PO, more diarrhea
- Cytarabine - Cytosine, competes for chain termination. IV/IT infusion
- Gemcitabine - fluorine, prevents elongation. IV
**Hand-foot
Term
How is leucovorin used?
Definition
- Rescue for MTX
- Increases efficacy of 5-FU
Term
How does Azacitidine work?
Definition
incorporates into DNA and inhibits methyltransferase, causing demethylation in DNA - does not block synthesis
- IV
Term
What drugs are purine analogs?
Definition
- 6-mercaptopurine - PO, guanine analog. HYPERURICEMIA, can use allopurinol but must decr dose 75% due to xanthine oxidase
- Fludarabine - Adenosine analog. Resistant to deamination = long half life. IV, HEMOLYTIC ANEMIA
- Clofarabine - IV, capillary leak/SIRS
- Nelarabine - IV, neurotoxic
- Pentostatin - guanine, 7 member ring. IV
Term
How does hydroxyurea work?
Definition
inhibits ribonucleotide reductase to block DNA synthesis
PO
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