Study your flashcards anywhere!

Download the official Cram app for free >

  • Shuffle
    Toggle On
    Toggle Off
  • Alphabetize
    Toggle On
    Toggle Off
  • Front First
    Toggle On
    Toggle Off
  • Both Sides
    Toggle On
    Toggle Off
  • Read
    Toggle On
    Toggle Off
Reading...
Front

How to study your flashcards.

Right/Left arrow keys: Navigate between flashcards.right arrow keyleft arrow key

Up/Down arrow keys: Flip the card between the front and back.down keyup key

H key: Show hint (3rd side).h key

A key: Read text to speech.a key

image

Play button

image

Play button

image

Progress

1/53

Click to flip

53 Cards in this Set

  • Front
  • Back
cyclophosphamide
alkylating agent: bischloroethyl amine (nitrogen mustard) prodrug: requires metabolic activation in liver. Oral administration possible. less highly reactive than mechloroethamine prototype
mechlorethamine
alkylating agent: bischloroethyl amine (nitrogen mustard). Prototype. Administered IV
carmustine
alkylating agent: nitrosourea. Has 2nd chloroethyl group.
lomustine
alkylating agent: nitrosourea.
procarbazine
metabolized to alkylating agent and free radical. Used against hodgkin's disease as part of MOPP regimen. No cross resistance w. other antineoplastic agents. Risk of developing leukemia bcuz of mutagenicity
carboplatin
platinum coordinating complex. DNA cross-linking. May inhibit DNA biosynthesis , but cell cycle nonspecific. Useful in combo regimens. Adverse: nephrotoxicity, acoustic nerve dysfxn
cisplatin
platinum coordinating complex. DNA cross-linking. May inhibit DNA biosynthesis , but cell cycle nonspecific. Useful in combo regimens. Adverse: nephrotoxicity, acoustic nerve dysfxn
5-fluorouracil (5-FU)
antimetabolite: pyrimidine antagonist. Metabolites inhibits thymidylate synthetase, and are incorporated into newly synthesized DNA and RNA
6-mercaptopurine
antimetabolite: purine antagonist. Fraudulent base incorporation, activated by conversion to NMPs, NTPs by hypoxanthine-guanine phosphoribosyl transferase (HGPRT). Resistance if enyzme levels downregulated. Eliminated by xanthine oxidase. Active form of azothioprine.
6-thioguanine
antimetabolite: purine antagonist. Fraudulent base incorporation, activated by conversion to NMPs, NTPs by hypoxanthine-guanine phosphoribosyl transferase (HGPRT). Resistance if enyzme levels downregulated
capecitabine
antimetabolite: pyrimidine antagonist. Oral prodrug of fluorouracil, requires thymidine phosphorylase, higher expression and thus activation in tumor tissues. Used for colon cancer and refractory breast cancer
cytosine arabinoside (cytarabine, ara C)
antimetabolite. Pyrimidine antagonist. After conversions -->araCTP is inhibitor of DNA synthesis, also incorporated into DNA causing mutations and breaks. Requires deoxycitidine kinase (lost in resistant cells). "chain blocking nucleotide analog"
methotrexate
antimetabolite. Folic acid analog. Inhibits dihydrofolate reductase, blocking synthesis of DNA, RNA. Accumulates in cell as a polyglutamate derivative (enhanced toxicity)
leucovorin
folinic acid rescue from methotrexate (source of tetrahydrofolate)
actinomycin D (Dactinomycin)
anti-tumor antibiotic. Or anthracycline. Highly potent, DNA intercalating. (-) DNA transcription via RNA polymerase. NOT cell cycle specific
bleomycin
anti-tumor antibiotic. Complex natural product, may cause anaphylaxis (small text doses to start). Mechanism for killing: DNA strand breakage. Effects broad spectrum of tumors. Risk of pulmonary fibrosis at large doses. No significant myelosuppression - used in ABVD
daunorubicin
anthracycline anti-tumor antibiotic, topoisomerase inhibitor.
doxorubicin (Adriamycin)
anthracycline anti-tumor antibiotic, topoisomerase inhibitor.
paclitaxel (Taxol)
mitotic spindle poison. Plant alkaloid. Blocks microtubule Depolymerization. Used for ovarian and advanced breast cancers
vinblastine
mitotic spindle poison: vinca alkaloid. M-phase specific. Inhibits microtubule polymerization. SIDE EFFECTS: nausea, vomiting, bonemarrow depression (dose limiting). Used against lymphomas, Hodgkins. Part of ABVD. Resistance by tubulin gene mutations
vincristine (Oncovorin)
mitotic spindle poison: vinca alkaloid. M-phase specific. Inhibits microtubule polymerization. SIDE EFFECTS: none acutely, milder (not dose limiting) bone marrow depression. significant neurotoxicity (muscle weakness). Used against acute childhood leukemia, lymphomas, Hodgkins. Part of M[O]PP. Resistance by tubulin gene mutations
irinotecan
topoisomerase inhibitor: camptothecin. Bind "cleaveable complex" of topo I and DNA, block religation of single-strand break. Use: colorectal cancer. Dose-limiting toxicity: diarrhea
topotecan
topoisomerase inhibitor: camptothecin. Bind "cleaveable complex" of topo I and DNA, block religation of single-strand break. Uses: ovarian and lung cancers. Dose-limiting toxicity: myelosuppresion
etoposide
topoisomerase inhibitor: topo II blocker. Forms ternary complex with it and DNA, interferes with religation.
prednisone
adrenocorticosteroid. Suppresses mitosis of lymphocytes, used in combo regimens for leukemia, lymphoma, and myeloma. Palliative agent in other cancers (decrease swelling, pain)
idoxifene
antagonist of hormone action. SERM.
raloxifene
antagonist of hormone action. SERM. Approved for Tx of breast cancer. Lower associated risk of endo cancer and thrombotic events than tamoxifen.
tamoxifen
antagonist of hormone action. SERM. Binds estrogen receptor, competes with estrogen. Partial agonist of receptor, efficacy varies on tissue. Adverse: hot flashes. Use: estrogen-responsive tissue cancers: breast (male and female) and uterine endometrium
anastrozole
antagonist of hormone action. Aromatase inhibitor, blocks conversion of androgens ot estrogen. Tx breast cancer
letrozole
antagonist of hormone action. Aromatase inhibitor, blocks conversion of androgens ot estrogen. Tx breast cancer
leuprolide
antagonist of hormone action. Anti-androgen - analog of GnRH. Pulsatile delivery elevates levels of andro/estrogens. Continuous, high dose Tx lowers andro/estrogen. Chemical castration, ablation. Tx of prostatic cancer
flutamide
antagonist of hormone action. Androgen receoptor antagonist. Ineffective alone due to rapid receptor mutation. Used w/ leuprolide to block initial pulse of high androgen levels and potential "flare" of prostate cancer when therapy starts
erlotinib
EGFR kinase inhibitor. Tx: non-small cell lung cancer
gefitinib (Iressa)
EGFR kinase inhibitor. Tx: non-small cell lung cancer
lapatinib
EGFR kinase inhibitor AND HER2 kinase inhibitor. In breast cancer trials
imatinib (Gleevac)
PDGFR, bcr/abl, kit(stem cell factor receptor) inhibitor. Tx: chronic myelogenous leukemia (bcr/abl mutation). GI stromal tumors (kit mutations), chronic myelomonocytic leukemia (ETV6-PDGFR fusion)
cetuximab (Erbitux)
chimeric/humanized antibody, anti EGFR. Tx: colon cancer
rituximab (Rituxan)
chimeric/humanized antibody, anti CD20 (on Bcells) expressed in 90% of non-hodgkin's lymphomas. Ab binds and kills B cells effectively using complement and Ab dependent cell-mediated cytotoxicity
trastuzumab (Herceptin)
chimeric/humanized antibody, anti-HER2. "humanized" Tx for refractory metastatic breast cancer (HER2 elevated in 30% of breast tumors) Direct tumor cell, immune mediated effects.
alkylating agents: bischloroethyl amines
alkylates w/ DNA. Cl- electrophiles search out neutrophiles. 2 branches w/ Cl- so can crosslink 2 bases.
alkylating agents: nitrosoureas
hydrophobic, crosses BBB (useful against brain tumors). Little cross-resistancw with other alkylating agents. 1 chloroethyl group (2 in bischloroethyl amines)
MOPP
mechloroethamine, vincristine (Oncovin), procarbazine, prednisone
antimetabolites
drugs that target cells in S phase, inhibit metabolic actions needed in S-phase
mechanisms for methotrexate resistance
amplification of DHFR gene, DHFR mutation, decreased uptake of methotrexate, increased efflux of methotrexate
allopurinol
intereferes w. purine metabolism to reduce uric acid accumulation associated with tumor cell death. Inhibits xanthine oxidase, which metabolizes 6-mercaptopurine)
anthracyclines
DNA intercalation (put themselvesin the gap w/ anthracyclin ring). DNA topoisomerase II binding. NOT cell cycle specific. Irreversible cardiac toxicity at high doses. Severe or total alopecia at standard doses.
alopecia
hair loss
ABVD
combo regimen consisting of doxorubicin [A]driamycin] (anthracycline), bleomycin (antibiotic cuts DNA), vinblastine (microtubule poison), decarbazinel (alkylating agent)
SERM
selective estrogen response modulators
STAR
study of tamoxifen and raloxifene (as cancer preventitive agents)
bcr/abl protein tyrosine kinase
arises from gene rearrangment/fusion in chronic myelogenous leukemia
drug resistance mechanisms (5-6)
alterations in drug uptake/transport. Increased concentration of target enzyme or decreased affinity of inhibitor for target enzyme. Decreased rate of metabolic drug activation. Increased rate of drug metabolism/inactivation. Increased rate of drug efflux.
MDR1
nonspecific drug efflux pump