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44 Cards in this Set
- Front
- Back
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S-phase of mitosis
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DNA synthesis
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G2 phase of mitosis
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synthesis of components needed for mitosis
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M phase of mitosis
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PMAT (mitosis as we know it!)
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G1 phase of mitosis
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synthesis of components needed for DNA synthesis
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What type of kinetics do cytotoxic drugs have?
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first-order kinetics; given doses kill a constant proportion of the cell population rather than a constant number of cells
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How many cells of a population will a 4-Log-Kill dose kill?
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by a magnitude of 4 logs less (if the population was 10 to the X-th power, then number of remaining cells would be 10 to the (X-4 power)
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What is the MOA of the alkylating agents?
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CCNS drugs (all cell cycle phases killed); form alkylate nucleophile groups on DNA bases; leads to cross-linking of bases, abnormal base pairing, and DNA strand breaks
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How does resistance to alkylating agents form?
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increased DNA repair, decreased drug permeability, production of trapping agents like thiols
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What are some common alkylating agent drugs used?
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chlorambucil, cyclophosphamide, mechlorethamine; carmustine, lomustine, busulfan; cisplatin, dacarbazine, procarbazine
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What is cyclophosphamide used for clinically?
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non-hodgkin's lymphoma, breast cancer, ovarian cancer, neuroblastoma
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What is mechlorethamine used for clincally?
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hodgkin's lymphoma
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What are the platinum analog drugs?
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cisplatin, carboplatin, oxaliplatin
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How is cisplatin cleared from the body?
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kidneys…unchanged
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What is the clinical use of cisplatin?
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testicular carcinoma; cancers of the bladder, lung and ovaries
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What is a clinical use of oxaliplatin?
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advanced colon cancer
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How can the nephrotoxicity be reduced with cisplatin?
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administration of mannitol with forced hydration
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What is the MOA of procarbazine?
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forms hydrogen peroxide, generating free radicals that damage DNA
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How is procarbazine eliminated from the body?
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hepatic elimination
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What is procarbazine used for clinically?
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Part of a regimen for hodgkin's lymphoma
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What is busulfan used for clinically?
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chronic myelogenous leukemia
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What are two akkylating agents that are used to treat brain tumors?
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carmustine and lomustine
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What is the MOA of methotrexate?
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inhibitor of dihydrofolate reductase; decreases levels of thymidylate, purine nucleotides, and amino acids; forms polyglutamate derivative which is for cytotoxic actions
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How is methotrexate metabolized and excreted?
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haha trick question! It is NOT metabolized.. But it is eliminated by the kidney
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what are some clinical uses of methotrexate?
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choriocarcinoma, acute leukemia, non-hodgkin's and cutaneous t-cell lymphoma, breast cancer; also for RA and ectopic pregnancy (aborticant)
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How can the toxicity of methotrexate be reduced?
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administration of leucovorin aka folinic acid
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What is the MOA of mercaptopurine and thioguanine?
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purine antimetabolites; activated to toxic nucleotides by HGPRTases
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What can inhibit the metabolism of mercaptopurine?
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allopurinol
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What is the MOA of fluorouracil (5-FU)?
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converted to 5-FdUMP which inhibits thymidylate synthase
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What are the clinical uses of 5-FU?
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bladder, breast, colon, head/neck, liver, ovarian cancers
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What are the vinca alkaloids?
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vinblastine, vincristine, vinorelbine
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what are the podophyllotoxins?
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etoposide, and teniposide
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what are the taxanes?
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paclitaxel and docetaxel
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What is the MOA of the vinca alkaloids?
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block formation of the mitotic spindle; prevents the assembly of tubulin dimers into microtubles; M-phase action
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What is the MOA of etoposide?
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increases DNA degradation; inhibits mitochondrial electron transport; most active during late S and early G2 phases
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What are 2 drugs that inhibit topoisomerase 1?
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topotecan and irinotecan
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What is a clinical use of topotecan?
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second line therapy for ovarian cancer and small cell lung cancer
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What is the MOA of paclitaxel and docetaxel?
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interfere with dissasembly of the mitotic spindle
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What is a clinical use of paclitexel and docetaxel?
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advanced ovarian and breast cancers
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What is the MOA of bleomycin?
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generates free radicals which cause strand breaks in DNA and inhibit DNA synthesis; CCS drug active in G2 phase
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What is the MOA of dactinomycin?
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CCNS drug that binds to dsDNA and inhibits DNA-dep-RNA synthesis; parenterally only
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What can be used in estrogen sensitive breast cancer?
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tamoxifen; selective estrogen receptor modulator
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What is the MOA of imatinib?
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inhibits tyrosine kinase activity of the Bcr-abl oncogene commonly seen in CML
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What drug causes hemorrhagic cystitis? How can it be prevented?
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cyclophosphamide's toxic metabolite Acrolein causes hemorrhagic cystitis; Mensa can prevent it
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Cancer drug with most pulmonary toxicity is...
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bleomycin
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