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14 Cards in this Set
- Front
- Back
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Folate antagonist Purine / Pyrinidine synthesis inhibitor Inhibits dihydrofolate reductase Kidney excretion Toxicity = Myelosuppression and GI toxicity, acute chemicalarachnoiditis, subacute neuropathy, chronic demyelinating encephalopathy |
Methotrexate |
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Antidote for MTX-Induced toxicity Large amounts of substrate can bypass inhibited enzyme |
Leucovorin |
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Pyrimidine Antagonist Interferes with conversion of deoxyuridylic acid to thymidylic acid. Depriving the cell of precursors for DNA synthesis
Max cytotoxic effect in s-phase Toxicity= Myelosuppression and GI toxicity For colon CA , breast CA, neck CA |
5-Fluorouracil & 5-fluorodeoxyuridine |
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Pyrimidine Antagonist Inhibition of DNA Polymerase DOC for AML Nausea, vomiting and diarrhea, neurotoxic after intrathecal admin, hepatotoxicity cycle specific S phase |
Cytosine arabinoside (cytarabine) |
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Pyrimidine Antagonist MOA: DNA synthesis inhibitor by incorporation into the DNA Impairs Dna repair Inhibition of ribonucleoside reductase Cycle specific s phase
Myelosuppression Increase in transaminases, flu like syndrome |
Gemcitabine |
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Purine Antagonist
Inhibition of de novo purine synthesis by thiol group substitution in hypoxanthine and xanthine
S phase Myelosuppression, GI Toxicity For AML ALL |
6-Mercaptopurine and 6-Thioguanine |
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Purine Antagonist Inhibition of DNA synthesis by incorporation as a false nucleotide Inhibition of DNA Polymerase, ligase and primase DNA chain termination
Myelosuppression Nausea vomiting diarrhea For CLL |
Fludarabine |
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Ribonucleoside reductase inhibitor Inhibition of DNA synthesis, regulation of gene expression Cycle specific S Phase Bone marrow suppression leucopenia
For: myeloproliferative disease CML Blast Crisis in AMLto lower blast count |
Hydroxyurea |
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Cell cycle specific M phase Tubulin and microtubules
MOA: binding to tubulin -> inhibition of microtubule assembly and dissolution of mitotic spindle -> arrest of cells in metaphase
CYP450-3A |
Vincristine - ALL, lymphoma, Wilm's tumor Vinblastine - testicular CA, bladder CA, Hodgkin's dx Vinorelbine - non small cell lung CA, breast CA |
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Vincristine adverse effects |
Parasthesias of distal fingers and lower extremeties loss of DTR's
Cranial nerve palsy, jaw pain
SIADH leading to hyponatremia |
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Vinorelbine adverse effects |
Constipation nausea vomiting diarrhea stomatitis Less neurotoxic: mild sensory neuropathy |
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Microtubulin Inhibitor M phase cycle specific MOA: Binding to Microtubuke associated proteins causing dissociation of MAP from tubulin and inhibition of microtubule assembly and disassembly For metastatic prostatic CA |
Estramustine |
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Taxanes Microtubulin inhibitors MOA: binding to beta tubulin sub unit leading to stabilization of microtubule causing cell death M phase specific CYP450 Neutropenia, peripheral neuropathy Ovarian CA, breast CA, head and neck CA, esophageal CA, non small cell lung CA |
Paclitaxel more hypersensitive reactions (Cremophor El) Docetaxel less hypersensitivity reactions |
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Topoisomerase 1 inhibitor Inhibits TOP1 DNA repair enzyme will cause accumulation of cleavable complexes and unstable DNA causing subsequent death of the cell Cell cycle non specific |
Topotecan Irinotecan |
