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98 Cards in this Set
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- Back
Microtubule inhibitors
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Vincristine
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MOA of alkylation and free radical formation
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Damage DNA
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MOA of antimetabolites and Topoisomerase inhibitors
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Inhibit synthesis or functions
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Drug resistance mechanisms of cancer cells
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Increased DNA repair, formation of trapping agents, Change in target enzymes, Decreased activation of prodrugs, Inactivation of anticancer drugs, decreased drug accumulation
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Alkylating agents - nitrogen mustards
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Chorambucil, cyclophosphamide, mechlorethamine
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Alkylating agents - nitrosureas
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carmustine, lomustine
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Alkylating agents - alkylsulfonates
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Busulfan
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Tumor cell resistance to alkylating agents involves
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increased DNA repair, decreased drug permeability, and the production of trapping agents
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Alkylating agent used in treatmet of non-hodgkin's lymphoma, breast and ovarian cancers and neuroblastoma
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Cyclophosphamide
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Cyclophosphamide toxicity
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GI distress, myelosuppression, and alopecia
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Acrolein is a byproduct of cyclophosphamide and may result in
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Hemorrhagic cystitis - treated with vigorous hydration and mesna
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Alkylating agent used in Hodgkin Lymphoma
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Mechlorethamine
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Toxicity of Mechlorethamine
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GI distress, myelosuppresion, alopecia, and sterility.
Has marked VESICANT actions |
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Alkylating agent used in Testicular Ca, bladder, lung and ovary
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Cisplatin and Carboplatin
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Tozicity of cisplatin
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Neuro and nephrotoxic
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Antagonist of folic acid
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methotrexate
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MOA of methotrexate
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interferes with nucleic acid and protein metabolism
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Methotrexate is effective in
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choriocarcinoma, acute leukemias, non-Hodgkin's lymphoma, cutaneous T cell lymphoma
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An abortifacient used in ectopic pregnancy
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Methotrexate
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Toxic effects of methotrexate may be reduced with
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administration of folinic acid - leucovorin
leucovorin rescue therapy |
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Drugs that enhance the toxicity of methotrexate
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Salicylates, NSAIDS, sulfonamides, sulfonylureas
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Purine antimetabolites activated by HGPRT
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Mercaptopurine and thioguanine
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Metabolism of 6-MP is inhibited by
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Allopurinol
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Used in the treatment of ALL and CML
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Purine antimetabolites
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Toxicity of 6-MP and 6-TG
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Bone marrow suppression and hepatic dysfunction
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Pyrimidine anti-metabolite
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Cytarabine (Ara-C)
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Toxicity of Ara-C
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GI and myelosuppression
Neurotoxic in high doses |
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Thymineless death
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Fluorouracil (5-FU)
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Act primarily during the M phase of the cell cycle
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Vinblastine and Vincristine
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Used for lymphomas, neuroblastomma, testicular carcinoma and Kaposi's sarcoma
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Vinblastine
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May cause neurotoxic actions - areflexia, peripheral neuritis, and paralytic ileus
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Vincristine
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Inhibits mitochondrial electron transport
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Etoposide and teniposide
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Prevent microtubule disassembly into tubulin monomers
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Paclitaxel and Docetaxel
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Primary agent used in the treatment of estrogen receptor-positive breast cancer
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Tamoxifen - estrogen receptor partial agonist, which may increase the risk of endometrial carcinoma
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Monoclonal antibody used for the treatment of metastatic breast cancer
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Trastuzumab - Binds to the receptor tyrosine kinase Erb-B2 [HER-2], overexpressed on some breast cancers
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Vinca alkaloid used as part of the MOPP regimen for lymphomas, wilms tumor, and choriocarcinomas
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Vincristine - M phase inhibitor
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Inhibits the enzyme aromatase and is used for the treatment of estrogen-dependent breast cancer
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Anastrozole - Inhibitor of steroid synthesis
Aminoglutethimide is a similar drug that inhibits the conversion of cholesterol to pregnenolone |
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This antineoplastic agent is used for the treatment of testicular carcinoma and squamous cell carcinoma; it can cause life-threatening pulmonary fibrosis
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Bleomycin - G2 phase inhibitor
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Highly lipophilic nitrosureas that readily cross the blood-brain barrier and are used for the treatment of many brain tumors
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Carmustine and Lomustine - alkylating agents result in DNA cross-linking and strand breaks
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Platinum-containing compound used in the treatment of testicular and lung carcinomas
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Cisplatin - nephrotoxicity and acoustic nerve damage
Carboplatin has less toxicity but greater myelosuppression |
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Alkylating agent used for the treatment of non-Hodgkin lymphoma and breast and ovarian carcinomas
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Cyclophosphamide - Major SE = hemorrhagic cystitis
May be decreased by vigorous hydration and mesna |
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Part of the AVBD regimen, an antibiotic-type compound used in the treatment of myelomas, sarcomas, and lymphomas
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Adriamycin (Doxorubicin) - associated with significant cardiotoxicity and dilated cardiomyopathy
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Inhibitor of topoisomerase II used for the treatment of small cell carcinoma of the lung and prostate, and testicular cancers
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Etoposide - G2 phase-specific inhibition - resulting in DNA breaks and degradation
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Inhibits thymidylate synthase, resulting in thymineless death, and is used for the treatment of colon cancer and superficial tumors, such as basal cell carcinoma
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Fluorouracil (5-FU) - S-phase antimetabolite
causes myelosuppression |
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Androgen receptor antagonist, used for the treatment of carcinoma of the prostate
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Flutamide - SE of gynecomastia and libido changes
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Recombinantly produced cytokine, used for the treatment of hairy cell leukemia
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Interferon Alpha
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Gonadotropin-releasing hormone (GnRH) agonists, used for the treatment of metastatic carcinoma of the prostate
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Leuprolide, Goserelin, Nafarelin
In a pulsatile administration, can be used for infertility |
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Purine metabolites, used for the treatment of leukemias and lymphomas
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Mercaptopurine (6-MP)
Thioguanine (6-TG) Requires activation by HGPRT |
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Folic acid analog, used for the treatment of leukemias, non-hodgkin lymphoma, RA and therapeutic abortions
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Methotrexate - S phase inhibitor of dihydrofolate reductase
Myelosuppression can be treated with leucovorin |
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Microtubule stabilizing agent, used for the treatment of ovarian and breast carcinomas
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Paclitaxel - M phase agent prevents mitotic spindle from breaking down. Inhibits completion of anaphase
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Glucocorticoid used for the treatment of leukemias and lymphomas, as well as for RA and asthma
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Prednisone - triggers apoptosis
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Monoclonal antibody used for the treatment of low-grade non-hodgkin lymphoma
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Rituximab - binds to CD 20 antigen on B cells
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Inhibits the de novo synthesis of purine ring
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6-mercaptopurine
Thioguanine |
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Inhibition of dihydrofolate reductase leads to an inhibition of purine ring and dTMP synthesis
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Methotrexate
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Inhibits dTMP synthesis
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5-fluorouracil
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Terminates DNA chain elongation
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Cytarabine
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Scission of DNA by an oxidative process
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Bleomycin peptide antibiotics
Doxorubicin Daunorubicin |
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Intercalate with DNA, disrupting DNA functions
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Dactinomycin, Doxorubicin, Daunorubicin
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Alter structure and function of DNA by cross-linking and/or fragmenting of DNA strands
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Alkylating agents
Nitrosureas and Cisplatin |
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Cell cycle specific drugs
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Antimetabolites
Bleomycin peptides Vinca alkaloids Etoposide |
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Cell-cycle non-specific drugs
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Alkylating agents
Antibiotics Cisplatin Nitrosoureas |
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Regimen for treating ALL
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POMP
Prednisone Oncovin (vincristine) Methotrexate Purinethol (mercaptopurine) |
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MOA for multi-drug resistance
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P-glycoprotein
ATP drug pumping efflux |
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Treatment induced neoplasms as a result of treatment with
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Alkylating agents
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Antimetabolites primarily target which phase of the cell cycle
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S phase
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Low dose methotrexate is effective in tx of
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Psoriasis, RA and Crohn's
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Methotrexate is effective for the tx of
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ALL, choriocarcinoma, Burkitt lymphoma, breast CA, and head/neck carcinomas
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Effective for treatment of superficial basal cell carcinoma
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5-fluorouracil
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5-FU must be administered with what coenzyme to be effective
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Leucovorin
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Breast cancer tx that is used after resistance to first line drugs
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Capecitabine
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MOA of Capecitabine
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Same as 5-FU - thymidylate synthase inhibition
Capecitabine is metabolized to 5-FU |
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Tx of Wilm's tumor
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Surgery
Dactinomycin and vincristine |
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Anthracycline antibiotics
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Doxorubicin
Daunorubicin |
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Anthracyclines are maximally effective in what cell cycles?
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S and G2
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MOA of Gemcitabine
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Incorporated into sites in the growing strand that would ordinarily contain cytosine
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SE of anthracyclines
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Cardiotoxicity
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Drugs produce red urine
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Anthracyclines
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Bleomycin is unusual in that
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myelosuppression is rare
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Extravasation of mechloroethamine is treated with
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infiltration with sodium thiosulfite to inactivate the drug
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Cytotoxic drug produced by hydroxylation by cytochrome P450
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Cyclophosphamide and ifosfamide
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Venoocclusive disease of the liver in 25% of patients
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Cyclophosphamide
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Resistance to Nitrosoureas as a result of
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Increased DNA repair
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Treatment of astrocytomas and treatment resistant gliomas
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temozolomide
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Dose limiting toxicity of paclitaxel and docetaxel
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Neutropenia
Alleviated with G-CSF filgrastim |
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Tumors that are hormone sensitive may be
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Hormone responsive
or Hormone dependent |
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May result in hypercalcemia, requiring cessation of the drug
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Tamoxifen
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Aromatase inhibitors
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Aminoglutetimide, Anastrozole, Letrozole, Exemestane
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Aromatase rxns are responsible for
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extra-adrenal synthesis of estrogen from androstenedione
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SE of flutamide
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Liver failure
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Monoclonal antibodies
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Trastuzumab, rituximab, bevacizumab, cetuximab
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Specifically targets the extracellular domain of HER2
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Trastuzumab
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Serious toxicity associated with Trastuzumab
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CHF
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Chimeric monoclonal antibody directed against CD 20
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Rituximab
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Adverse rxn to rituximab
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hypotension, bronchospasm and angioedema
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Tumor lysis syndrome
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within 24 hours of first dose of rituximab
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antiangiogenesis
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Bevacizumab
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Topoisomerase I inhibitors
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Irinotecan and Topotecan
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Used in the treatment of CML, advantage over interferon alpha
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Imantinib - can be given orally
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