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19 Cards in this Set
- Front
- Back
Methotrexate (MTX)
- mechanism - non-neoplastic uses - toxicities? Reversible? |
folic acid analog inhibits DHFR --> \\dTMP --> \\DNA synth and \\protein synth
Abortion, ectopic pregnancy, RA, psoriasis Myelosuppression reversible by leucovorin (folinic acid). Macrovesicular fatty change i/liver; mucositis; teratogenic. |
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5-FU
- mech - synergy with what? - Toxicities? Rescue? |
Pyrimidine analog bioactv to 5F-dUMP which covalently complexes folic acid. this inhibits thymidylate synthase --> \\dTMP
Synergy w/MTX BMS, rescue w/ thymidine Photosensitivity |
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6-MP
- mech - toxicities - metabolized by what? added toxicity with what? |
actv by HGPRTase --> Purine analog --> \\denovo purine synth.
BMS, GI, Liver. xanthine oxidase; thus trouble to give with allopurinol. |
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6-TG (thioguanine)
- mech - one clinical use - toxicities? added tox with allopurinol? |
actv by HGPRTase --> purine analog that inhibits denovo purine synth
ALL BMS. Is OK to give w/allopurinol. |
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Cytarabine (ara-C)
- mech - toxicities? |
Pyrimidine antagonist --> inhibition of DNA polymerase.
Leukopenia, thrombocytopenia, megaloblastic anemia. |
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What are the 4 antitumor antiBx types?
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- Dactinomyin (Actinomycin D)
- Doxorubicin, Adriamycin, danunorubicin - Bleomycin - Etoposide (VP-16), teniposide |
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Dactinomycin
- mechanism - used in which group of tumors? - toxicity? |
intercalates DNA
childhood tumors (Ewing's, rhabdomyosarcoma, wilm's tumors, etc) BMS |
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Doxorubicin
- mechanism - part of which regimen - toxicity |
- generates free radicals --> noncovalently intercalate i/DNA --> breaks DNA --> \\replication
ABVD (Adriamycin) for Hodgkin's Cardiotoxicity, BMS, marked alopecia. Toxic to tissues w/extravasation. |
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Bleomycin
- mechanism (stage specific?) - part of which regimen - toxicity |
Induces free radical formation which causes breaks in DNA strands. G2 specific.
ABVD for Hodgkin's Pulmonary fibrosis, skin changes. MINIMAL BMS. |
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Etoposide (VP-16), teniposide
- mechanism (stage specific?) - tx what? - toxicity |
Inhibits topo II --> ^^DNA degradation. Late S to G2.
Small cell carcinoma of lung (oat cell) BMS, GI irritation, alopecia. |
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Cyclophosphamide, ifosfamide
- mechanism? Require actv by what? - toxicity? can partially prevent w/ what? |
Covalently X-link DNA. Req actv by liver.
hemorrhagic cystitis partially preventable with mesna. Also BMS. |
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Nitrosoureas
- name some - mechanism - clincal use - toxicities |
carmustine, lomustine, semustine, streptozocin
Cross BBB --> CNS. Requires bioactivation. Brain tumors. CNS toxicity (dizziness, ataxia) |
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Busulfan
- mech - tx's what? - non neoplastic use? - toxicity? |
alkylates DNA.
CML. Ablating BM for SCT. Pulmonary fibrosis & hyperpigmentation. |
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Vincristine, vinblastine
- mech? active phase? - part of which regimen? - vincristine tox? - vinblastine tox? |
b/tubulin in M-phase blocking polymerization of mt's.
MOPP (Onvocin) for Hodgkin's neurotoxicity, paralytic ileus BMS |
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Paclitaxel, Taxols
- mech - use? - tox? |
hyperstabilizes polymerized mt's i/M phase.
Ovarian and breast carcinomas. BMS and hypersensitivity. |
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Cisplatin, carboplatin
- mechanism - tox |
cross link DNA
nephrotox & acoustic nerve damage |
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Hydroxyurea
- mech - skin cancer use? - leukemia use? - other dz use? - tox? |
inhibits Ribonucleotide Reductase (S-phase)
melanoma CML SSD BMS, GI upset |
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Trastuzumab (Herceptin)
- mech - clincal use - tox |
monoclonal Ab against Her-2 (erb-B2).
metastatic breast cancer Cardiotoxicity |
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Imatinib (Gleevec)
- mech - clinical use - tox |
bcr-abl tyrosine kinase inhibitor
CML, GI stromal tumors Fluid retention |