Term
cancers where response to hormones agonists/antagonsits
ex:-3 |
|
Definition
hormone responsive tissue
breast, prostate, elukemi/lymph |
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Term
|
Definition
breast/ovarain proliferation
cytoskel orgnaization
signal transduction |
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Term
| what is primary target axis for reproductive hormones- |
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Definition
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Term
| look at slide 6 to look at target issues (cant understand what of) |
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Definition
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Term
|
Definition
ovrian follicles
corpus luetum
placenta |
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Term
|
Definition
| testosterone (some aromatase enzyme tissues) |
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|
Term
what enzyme converts androgens to estrogen
(testoterone->estradiol and androstendione->estrone) |
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Definition
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|
Term
hgihest estrogen acitvity-
least- |
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Definition
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|
Term
estradiol->estrone->estriol *
which form is excreted in urine? |
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Definition
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|
Term
| premenaoupsal women get estrogne production from? |
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Definition
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|
Term
| post-menopausal women only get estrogen produced where? |
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Definition
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|
Term
| the target of estrogen in premenopausla women- |
|
Definition
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|
Term
| the target of estrogen meds in post-menopausal women-2 |
|
Definition
androstenedion in the peripheral
aromatase in breast adipose |
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Term
|
Definition
|
|
Term
| slide 12 for overall way to go at delpeting estrogen |
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Definition
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|
Term
| a complete estrogen blockade in pre-menopause women is accomplished thru what combo tx- |
|
Definition
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|
Term
| Af1 is what domain on the ER (estrogen recpt) |
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Definition
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|
Term
| AF2 is what domain on ER? |
|
Definition
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|
Term
ER is kept inactive by?
binding to _displaces these and Afs are activated |
|
Definition
heat shock proteins
estradoil |
|
|
Term
| which AF is estradoil activation depednent? |
|
Definition
|
|
Term
| the estrogen recpt (ERs) alpha and beta have diff-2 |
|
Definition
distribution
affinty
activations of genes |
|
|
Term
| estrogen mode of action- 4 steps |
|
Definition
1-bind to cytosol recpt
2- dissoc and dimerize
3go to nucelus and get coactivators
4-fully activate tnrascription |
|
|
Term
selective estrogen recpt modulators (SERMS)-4
which is a competitive inhibitor? |
|
Definition
raloxifene (Evista)
phytoestrogens
tamoxifen
climiphene;
tamox |
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|
Term
tamoxifene blocks-
this results in- |
|
Definition
AF2 on ER
paritally active trnascirption |
|
|
Term
| estrogen target -diethylstilbestol- is for what drug |
|
Definition
|
|
Term
| what is the pure anti-estrogen |
|
Definition
|
|
Term
| what are the aromatase inhibitors=3 |
|
Definition
anastrazole
letrozole
exemestane |
|
|
Term
tamoxifen is complete antag -
partial in - |
|
Definition
|
|
Term
|
Definition
|
|
Term
| which drug has to be hepaticlly metab for ER activity? |
|
Definition
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|
Term
| 4-hydroxy(name of drug) is the active species of |
|
Definition
|
|
Term
|
Definition
metastatic breast
pallatative advd breast |
|
|
Term
what drug is a chemopreventative agent for women with hgih risk for breast cancer?
how much for how long?
what's the reeduction in risk? |
|
Definition
tamoxifen
20 mg x 5 yrs
50% |
|
|
Term
| dosing and freq for tamoxifen |
|
Definition
|
|
Term
|
Definition
hot flash
decrease libido
vaginal bleed |
|
|
Term
| 10% more survival when tamox used combo with chemo |
|
Definition
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|
Term
| tho tamoxifen has anti estrogen effect on breast, where cna it have pro-estrogen effects?-3 |
|
Definition
|
|
Term
| emetic potential of tamoxifen or toremifene |
|
Definition
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|
Term
|
Definition
|
|
Term
|
Definition
| hot flash,THROMBOSIS , tumor flare |
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|
Term
| if cells resistant to tamofixen, they are also resit to? |
|
Definition
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|
Term
| effect on bone is les sin tamox or torem? |
|
Definition
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|
Term
| benefits from Tamox/torem-4 |
|
Definition
less recurrance metastasis
reduced local reoccurance
reduced second new breast cancer
reduce osteoporsis |
|
|
Term
| negatives of tamx/torem-4 |
|
Definition
increase cataracts
increased blood clots
increased endometiral cancer
hot flashes/vag dryness |
|
|
Term
| the NSABP study showed that tamox only icnrease endometiral cancer by about 1% |
|
Definition
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|
Term
| fulvestrant is indicated for _ cancer, for psot/pre-menopause following _ therapy |
|
Definition
ER psotive metastatic breast cancer
post-men
anti-estrogen |
|
|
Term
| whcih drug cna be used if tamoxifen resistant |
|
Definition
|
|
Term
|
Definition
| ER antag equal binding to estradoiu-> ER depednt trnascription is abolished in breast cancer |
|
|
Term
admin of fulvestrant
freq? |
|
Definition
|
|
Term
|
Definition
|
|
Term
| fulvestrant is contraindicated in which ppl |
|
Definition
|
|
Term
|
Definition
|
|
Term
raloxifine doesnt have estrogen effect where?
does do? |
|
Definition
breast, uterine
increases bone density |
|
|
Term
| raloxifine has what metab? |
|
Definition
| 1st pass( veyr hgi prot bound) |
|
|
Term
| contraidnciaiton for rlaoxifene-2 |
|
Definition
preggo
blood clot disorders |
|
|
Term
| D/C use of raloxifine for _ hrs when -2 |
|
Definition
72
surgery, immobilization |
|
|
Term
| raloxifene is not useful for tx- |
|
Definition
|
|
Term
| diff btwn tamox and fulvestrant- |
|
Definition
tamox= partial transcp (reduced tumor cell division)
fulvestrant= no trnascp |
|
|
Term
| ER and PgRs are recpotrs. if both are neg what is the repsonse to hromone tx? |
|
Definition
| low, no recpot for drugs to bind to |
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