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33 Cards in this Set
- Front
- Back
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The gene is often involved in the translocation with the retinoic acid receptor alpha gene associated with acute promyelocytic leukemia (APL).
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PML
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Receptor that is critical for differentiation?
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retinoic acid receptor (RAR)
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One of the hallmarks of cancer?
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A block in the process of differentiation
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Critical for proliferation inhibition and myeloid differentiation?
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PML
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When these two genes fuse, they both lose their effects?
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PML and RAR-alpha
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MOA of All-trans retinoic acid?
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-displaces a repressor of differentiation
-promotes the degradation of the PML-RAR-a fusion protein |
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MOA of Arsenic trioxide?
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-promotes degradation of PML-RARa fusion protein
-generates free radicals and inhibits angiogenesis |
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Clinical toxicities of arsenic trioxide?
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leukocyte maturation syndrome and
cardiotoxicity |
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Effect of Arsenic trixide on PML-RARa?
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post translational modification of protein
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Effect of all-transe retinoic acid (ATRA) on PML-RARa?
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replaces repressor and induces degradation -no post translational modification
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Tamoxifen MOA?
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Competitively binds to estrogen receptors on tumors and other tissue targets, producing a nuclear complex that decreases DNA synthesis and inhibits estrogen effects
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Tamoxifen in breast cells?
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Antiestrogenic
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Tamoxifen in uterus and endometric cells?
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estrogenic
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Tamoxifen uses?
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Breast cancer treatment and prevention:
-Oral: 20-40 mg/day; daily doses -DCIS (females): Oral: 20 mg once daily for 5 years -Breast cancer risk reduction (pre- and postmenopausal high-risk females): Oral: 20 mg/day for 5 year |
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Raloxifine MOA?
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Same as all SERMs: agonism or antagonism of estrogen receptors. Acts like estrogen to prevent bone loss and has the potential to block some estrogen effects in the breast and uterine tissues.
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Pure anti-estrogen selective estrogen receptor downregulator?
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Faslodex
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Faslodex MOA?
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Steroidal compound which competitively binds to estrogen receptors on tumors and other tissue targets, producing a nuclear complex that decreases DNA synthesis and inhibits estrogen effects. Fulvestrant has no estrogen-receptor agonist activity. Causes down-regulation of estrogen receptors and inhibits tumor growth
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Faslodex uses?
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Treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following antiestrogen therapy
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Faslodex dosing?
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I.M.: 250 mg at 1-month intervals
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MOA of aromatase inhibitors (AIs)?
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inhibit production of estrogen
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3 Aromatase inhibitors?
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-Exemestane
-Anastrazole -Letrozole |
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MOA of aromatase inhibitors?
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Irreversible, steroidal aromatase inactivators prevent conversion of androgens to estrogens by tying up the enzyme aromatase. In breast cancers where growth is estrogen-dependent, this medicine will lower circulating estrogens.
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Exemesatane dosing?
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25 mg once daily; continue until tumor progression is evident
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Anastrazole dosing?
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Oral: 1 mg once daily
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Anastrazole metabolisma and excretion?
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-Metabolism: Extensively hepatic
-Excretion: Urine (10% as unchanged drug; 60% as metabolites) |
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Letrozole dosing?
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Breast cancer: Females: Oral: 2.5 mg once daily
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Letrozole metabolism?
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Hepatic via CYP3A4 and 2A6 to an inactive carbinol metabolite
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Megestrol MOA?
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A synthetic progestin with antiestrogenic properties which disrupt the estrogen receptor cycle. Megestrol interferes with the normal estrogen cycle and results in a lower LH titer
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Megestrol uses?
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Palliative treatment of breast and endometrial carcinoma; treatment of anorexia, cachexia, or unexplained significant weight loss in patients with AIDS
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Megestrol doses?
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Oral: Tablet: 40 mg 4 times/day
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Leuprolide uses?
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Palliative treatment of advanced prostate cancer; management of endometriosis; treatment of anemia caused by uterine leiomyomata (fibroids); central precocious puberty
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Leuprolide MOA?
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Leuprolide, is an agonist of luteinizing hormone-releasing hormone (LHRH). Acting as a potent inhibitor of gonadotropin secretion; continuous administration results in suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH with subsequent decrease in testosterone (male) and estrogen (female) levels.
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Leuprolide Doses?
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SubQ: 1 mg/day
IM:Lupron Depot®: 7.5 mg/dose given monthly (every 28-33 days) OR Lupron Depot®-3: 22.5 mg every 3 months OR Lupron Depot®-4: 30 mg every 4 month |
