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antineoplastics II
cmbm exam V
32
Chemistry
Graduate
02/16/2010

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Term
what does vincristine do? what is it good for? ADRs? is there a similar agent?
Definition
vincristine prevents microtubule formation, which is needed for daughter cell formation; M phase is inhibited. they are good for rapidly growing tumors. ADRs include local irritation w/injection, *neurotoxicity* vinblastine is similar; both are plant derivatives
Term
what drugs inhibit topoisomerase I (which breaks and reseals single-strand DNA)?
Definition
campothecin analogues: irinotecan and topotecan, which are S-phase specific drugs
Term
what drugs inhibit topoisomerase II (which breaks and reseals double-strand DNA)?
Definition
podophyllotoxins: etoposide (*broad spectrum, can lead to 2ndary leukemia) and teniposide, which act on both S and G2 phases
Term
what is FOLFIRI?
Definition
a drug complex 5 flourouracil and leucovorin used with irinotecan for colorectal cancer or cisplatin for lung CA
Term
what is paclitaxel? what is it used for? ADRs?
Definition
paclitaxel is a plant-derived agent which acts in M phase is good against ovarian and breast CA as well as use in stents after coronary angioplasty, b/c it causes such severe neutropenia. it can cause peripheral neuropathy so it needs to be monitored, but it is an important drug that is commonly used.
Term
what does L-asparaginase do? what are side effects?
Definition
this enzyme breaks down asparganine; normal cells have asparagnine synthetase so they are able to make their own - but cancer cells do not have this enzyme, therefore, if L-asparaginase is administered, cancer cells cannot carry out proper protein synthesis. this is good for rapidly-growing tumors in blood/lymph (lymphoma/leukemia). ADRs include hyperglycemia, bleeding and hepatoxicity. it is derived from e. coli.
Term
when are hormonal agents indicated for CA?
Definition
prostate, breast CA; sex hormomone antagonists block receptors for each corresponding sex and sex-specific CA
Term
what is tamoxifen? ADRs?
Definition
a selective anti-estrogen receptor, (estrogen -> estrogen receptor -> growth factor -> cyclin dependent kinases -> cell division), it is lipid soluble which crosses cell membranes and binds to nuclear receptors where it reduces the expression of ALL growth factor receptors (tyrosine kinase receptors). it is usually complexed with anastrozole (aromatase inhibitor). ADRs include: menstrual irregularities and endometrial CA over time
Term
ALL growth factor receptors are ____?
Definition
tyrosine kinase receptors
Term
how many cancers is p53 involved in?
Definition
50%
Term
how do most cancer drugs work?
Definition
most drugs work by binding to DNA, disrupting DNA synthesis etc - if DNA is screwed up enough, p53 tells cells to die
Term
how many cancers is p53 involved in?
Definition
50%
Term
how do most cancer drugs work?
Definition
most drugs work by binding to DNA, disrupting DNA synthesis etc - DNA gets too “screwed up” p53 tells cells to die, however cancer cells do develop ways to not die
Term
what drugs target problems with ErbB2 amplification
Definition
herceptins
Term
what are 2 aromatase inhibitors we should know about? what does aromatase do? what are they indicated for?
Definition
aromatase is responsible for conversion of androstenedione and testosterone to estrone and estradiol respectively. anostrazole and letrozole (non-steroidal) both inhibit estrogen synthesis from androestendione and testosterone. they are indicated for breast CA and are usually combined with tamoxifen
Term
what does flutamide do? ADR?
Definition
this non-steroidal androgen receptor agonist is indicated in prostate CA and interrupts negative feedback of testosterone through the pituitary-hypothalamic axis). it may attenuate impotency
Term
what is leuprolide? what is it used for?
Definition
a gonadotropin-releasing hormone that increases estrogen/testosterone production but chronically inhibits FSH and LH production. it is used for prostate CA
Term
what are procarbazine and dacarbazine? what are they effective against?
Definition
procarbazine and dacarbazine are effective against lymphomas. they are monofunctional alkylating agents that methylate DNA, leading to miscoding and misreading (therefore efficacious in rapidly dividing CA)
Term
what is trastuzumab/herceptin? ADRs?
Definition
this monoclonal antibody is effective in breast cancers that overexpress HER-2 receptors (growth factors). pulm rxns are possible, but for the most part it is very selective and efficacious in breast cancer treatment
Term
what is bevacizumab/avastin?
Definition
monoclonal antibody for colorectal and lung cancers that works by binding to VEGF receptors
Term
can monoclonal antibodies cure cancer alone?
Definition
no, not yet, other cytotoxic drugs are still necessary
Term
what drug can cause acute hemorrhagic cystitis?
Definition
cyclophosphamide
Term
what is the M/A for 5-FU?
Definition
cytotoxicity resulting from a metabolite that interferes with the production of dTMP
Term
what is a cell cycle specific anticancer drug that acts mainly in the M phase of the cell cycle?
Definition
paclitaxel
Term
it is important to monitor serum MTX level during the initial course of drug treatment because?
Definition
high MTX levels in the blood require additional leucovorin rescue
Term
maintenance of a high urinary pH is important during methotrexate treatment in this patient because?
Definition
methotrexate is a weak acid; making a salt - the ionized form of the drug will not readily penetrate cell membranes
Term
a cancer cell that is resistant to the effects of both vincristine and methotrexate probably has developed that resistance as a result of?
Definition
increase in expression of a P-glycoprotein transporter
Term
does trastuzumab have specific activity in a subset of female breast cancers?
Definition
yes
Term
are plant alkaloids cell cycle specific (CCS) and is used in both the MOPP and ABVD regimens?
Definition
yes
Term
what antibx CA rx is commonly associated with pulmonary infiltration?
Definition
bleomycin
Term
what adverse effect would be likely for a patient to experience with FOLFOX?
Definition
myelosuppression
Term
would vincristine be highly effective w/hodgkin's?
Definition
yes
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