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98 Cards in this Set

  • Front
  • Back
Microtubule inhibitors
Vincristine
MOA of alkylation and free radical formation
Damage DNA
MOA of antimetabolites and Topoisomerase inhibitors
Inhibit synthesis or functions
Drug resistance mechanisms of cancer cells
Increased DNA repair, formation of trapping agents, Change in target enzymes, Decreased activation of prodrugs, Inactivation of anticancer drugs, decreased drug accumulation
Alkylating agents - nitrogen mustards
Chorambucil, cyclophosphamide, mechlorethamine
Alkylating agents - nitrosureas
carmustine, lomustine
Alkylating agents - alkylsulfonates
Busulfan
Tumor cell resistance to alkylating agents involves
increased DNA repair, decreased drug permeability, and the production of trapping agents
Alkylating agent used in treatmet of non-hodgkin's lymphoma, breast and ovarian cancers and neuroblastoma
Cyclophosphamide
Cyclophosphamide toxicity
GI distress, myelosuppression, and alopecia
Acrolein is a byproduct of cyclophosphamide and may result in
Hemorrhagic cystitis - treated with vigorous hydration and mesna
Alkylating agent used in Hodgkin Lymphoma
Mechlorethamine
Toxicity of Mechlorethamine
GI distress, myelosuppresion, alopecia, and sterility.
Has marked VESICANT actions
Alkylating agent used in Testicular Ca, bladder, lung and ovary
Cisplatin and Carboplatin
Tozicity of cisplatin
Neuro and nephrotoxic
Antagonist of folic acid
methotrexate
MOA of methotrexate
interferes with nucleic acid and protein metabolism
Methotrexate is effective in
choriocarcinoma, acute leukemias, non-Hodgkin's lymphoma, cutaneous T cell lymphoma
An abortifacient used in ectopic pregnancy
Methotrexate
Toxic effects of methotrexate may be reduced with
administration of folinic acid - leucovorin

leucovorin rescue therapy
Drugs that enhance the toxicity of methotrexate
Salicylates, NSAIDS, sulfonamides, sulfonylureas
Purine antimetabolites activated by HGPRT
Mercaptopurine and thioguanine
Metabolism of 6-MP is inhibited by
Allopurinol
Used in the treatment of ALL and CML
Purine antimetabolites
Toxicity of 6-MP and 6-TG
Bone marrow suppression and hepatic dysfunction
Pyrimidine anti-metabolite
Cytarabine (Ara-C)
Toxicity of Ara-C
GI and myelosuppression
Neurotoxic in high doses
Thymineless death
Fluorouracil (5-FU)
Act primarily during the M phase of the cell cycle
Vinblastine and Vincristine
Used for lymphomas, neuroblastomma, testicular carcinoma and Kaposi's sarcoma
Vinblastine
May cause neurotoxic actions - areflexia, peripheral neuritis, and paralytic ileus
Vincristine
Inhibits mitochondrial electron transport
Etoposide and teniposide
Prevent microtubule disassembly into tubulin monomers
Paclitaxel and Docetaxel
Primary agent used in the treatment of estrogen receptor-positive breast cancer
Tamoxifen - estrogen receptor partial agonist, which may increase the risk of endometrial carcinoma
Monoclonal antibody used for the treatment of metastatic breast cancer
Trastuzumab - Binds to the receptor tyrosine kinase Erb-B2 [HER-2], overexpressed on some breast cancers
Vinca alkaloid used as part of the MOPP regimen for lymphomas, wilms tumor, and choriocarcinomas
Vincristine - M phase inhibitor
Inhibits the enzyme aromatase and is used for the treatment of estrogen-dependent breast cancer
Anastrozole - Inhibitor of steroid synthesis

Aminoglutethimide is a similar drug that inhibits the conversion of cholesterol to pregnenolone
This antineoplastic agent is used for the treatment of testicular carcinoma and squamous cell carcinoma; it can cause life-threatening pulmonary fibrosis
Bleomycin - G2 phase inhibitor
Highly lipophilic nitrosureas that readily cross the blood-brain barrier and are used for the treatment of many brain tumors
Carmustine and Lomustine - alkylating agents result in DNA cross-linking and strand breaks
Platinum-containing compound used in the treatment of testicular and lung carcinomas
Cisplatin - nephrotoxicity and acoustic nerve damage

Carboplatin has less toxicity but greater myelosuppression
Alkylating agent used for the treatment of non-Hodgkin lymphoma and breast and ovarian carcinomas
Cyclophosphamide - Major SE = hemorrhagic cystitis

May be decreased by vigorous hydration and mesna
Part of the AVBD regimen, an antibiotic-type compound used in the treatment of myelomas, sarcomas, and lymphomas
Adriamycin (Doxorubicin) - associated with significant cardiotoxicity and dilated cardiomyopathy
Inhibitor of topoisomerase II used for the treatment of small cell carcinoma of the lung and prostate, and testicular cancers
Etoposide - G2 phase-specific inhibition - resulting in DNA breaks and degradation
Inhibits thymidylate synthase, resulting in thymineless death, and is used for the treatment of colon cancer and superficial tumors, such as basal cell carcinoma
Fluorouracil (5-FU) - S-phase antimetabolite

causes myelosuppression
Androgen receptor antagonist, used for the treatment of carcinoma of the prostate
Flutamide - SE of gynecomastia and libido changes
Recombinantly produced cytokine, used for the treatment of hairy cell leukemia
Interferon Alpha
Gonadotropin-releasing hormone (GnRH) agonists, used for the treatment of metastatic carcinoma of the prostate
Leuprolide, Goserelin, Nafarelin

In a pulsatile administration, can be used for infertility
Purine metabolites, used for the treatment of leukemias and lymphomas
Mercaptopurine (6-MP)
Thioguanine (6-TG)

Requires activation by HGPRT
Folic acid analog, used for the treatment of leukemias, non-hodgkin lymphoma, RA and therapeutic abortions
Methotrexate - S phase inhibitor of dihydrofolate reductase

Myelosuppression can be treated with leucovorin
Microtubule stabilizing agent, used for the treatment of ovarian and breast carcinomas
Paclitaxel - M phase agent prevents mitotic spindle from breaking down. Inhibits completion of anaphase
Glucocorticoid used for the treatment of leukemias and lymphomas, as well as for RA and asthma
Prednisone - triggers apoptosis
Monoclonal antibody used for the treatment of low-grade non-hodgkin lymphoma
Rituximab - binds to CD 20 antigen on B cells
Inhibits the de novo synthesis of purine ring
6-mercaptopurine

Thioguanine
Inhibition of dihydrofolate reductase leads to an inhibition of purine ring and dTMP synthesis
Methotrexate
Inhibits dTMP synthesis
5-fluorouracil
Terminates DNA chain elongation
Cytarabine
Scission of DNA by an oxidative process
Bleomycin peptide antibiotics

Doxorubicin Daunorubicin
Intercalate with DNA, disrupting DNA functions
Dactinomycin, Doxorubicin, Daunorubicin
Alter structure and function of DNA by cross-linking and/or fragmenting of DNA strands
Alkylating agents

Nitrosureas and Cisplatin
Cell cycle specific drugs
Antimetabolites
Bleomycin peptides
Vinca alkaloids
Etoposide
Cell-cycle non-specific drugs
Alkylating agents
Antibiotics
Cisplatin
Nitrosoureas
Regimen for treating ALL
POMP
Prednisone
Oncovin (vincristine)
Methotrexate
Purinethol (mercaptopurine)
MOA for multi-drug resistance
P-glycoprotein

ATP drug pumping efflux
Treatment induced neoplasms as a result of treatment with
Alkylating agents
Antimetabolites primarily target which phase of the cell cycle
S phase
Low dose methotrexate is effective in tx of
Psoriasis, RA and Crohn's
Methotrexate is effective for the tx of
ALL, choriocarcinoma, Burkitt lymphoma, breast CA, and head/neck carcinomas
Effective for treatment of superficial basal cell carcinoma
5-fluorouracil
5-FU must be administered with what coenzyme to be effective
Leucovorin
Breast cancer tx that is used after resistance to first line drugs
Capecitabine
MOA of Capecitabine
Same as 5-FU - thymidylate synthase inhibition

Capecitabine is metabolized to 5-FU
Tx of Wilm's tumor
Surgery

Dactinomycin and vincristine
Anthracycline antibiotics
Doxorubicin
Daunorubicin
Anthracyclines are maximally effective in what cell cycles?
S and G2
MOA of Gemcitabine
Incorporated into sites in the growing strand that would ordinarily contain cytosine
SE of anthracyclines
Cardiotoxicity
Drugs produce red urine
Anthracyclines
Bleomycin is unusual in that
myelosuppression is rare
Extravasation of mechloroethamine is treated with
infiltration with sodium thiosulfite to inactivate the drug
Cytotoxic drug produced by hydroxylation by cytochrome P450
Cyclophosphamide and ifosfamide
Venoocclusive disease of the liver in 25% of patients
Cyclophosphamide
Resistance to Nitrosoureas as a result of
Increased DNA repair
Treatment of astrocytomas and treatment resistant gliomas
temozolomide
Dose limiting toxicity of paclitaxel and docetaxel
Neutropenia

Alleviated with G-CSF filgrastim
Tumors that are hormone sensitive may be
Hormone responsive
or
Hormone dependent
May result in hypercalcemia, requiring cessation of the drug
Tamoxifen
Aromatase inhibitors
Aminoglutetimide, Anastrozole, Letrozole, Exemestane
Aromatase rxns are responsible for
extra-adrenal synthesis of estrogen from androstenedione
SE of flutamide
Liver failure
Monoclonal antibodies
Trastuzumab, rituximab, bevacizumab, cetuximab
Specifically targets the extracellular domain of HER2
Trastuzumab
Serious toxicity associated with Trastuzumab
CHF
Chimeric monoclonal antibody directed against CD 20
Rituximab
Adverse rxn to rituximab
hypotension, bronchospasm and angioedema
Tumor lysis syndrome
within 24 hours of first dose of rituximab
antiangiogenesis
Bevacizumab
Topoisomerase I inhibitors
Irinotecan and Topotecan
Used in the treatment of CML, advantage over interferon alpha
Imantinib - can be given orally