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41 Cards in this Set
- Front
- Back
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Indication for Tamoxifen
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Estrogen-dependent breast cancer
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MOA of Tamoxifen
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SERM – competes with estrogen for receptor binding
agonist - in some tissues antag - on receptor so any estrogen that binds won’t have activity so you remove that portion of the tumor due to the estrogen that binds but you have cancer growth from other mechanisms |
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Tamoxifen Side Effects
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Hot flashes, N/V, myelosuppression, DVT, pulmonary embolism
Linked to endometrial cancer and blood clots (+) estrogenic effects on bone and cholesterol |
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Indication for Toremifene
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Estrogen-dependent breast cancer
Possible: prostate cancer prophylaxis |
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MOA of Toremifene
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Tamoxifen analog – increases TNF-beta, decreases cell proliferation and cell growth
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Toremifene Side Effects
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Hot flashes, N/V, myelosuppression, DVT, pulmonary embolism
Linked to endometrial cancer and blood clots (+) estrogenic effects on bone and cholesterol |
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Indication for Raloxifene
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Osteoporosis
FDA (2007) – reduce breast cancer risk in postmenopausal women with osteoporosis and postmenopausal at high risk for breast cancer |
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MOA of Raloxifene
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SERM
• Estrogen effects in bone and CV • Antagonist in breast and uterine tissue |
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Raloxifene Side Effects
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Increased incidence of thromboembolism, hot flashes, muscle cramps, teratogenic in animals
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Indications for Fulvestrant
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Postmenopausal hormone sensitive metastatic breast cancer (monthly IM injections)
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MOA of Fulvestrant
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SERD
• Pure anti-estrogen, down regulates estrogen receptor |
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Fulvestrant Side Effects
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Nausea
Asthenia Pain Vasodilation Headache |
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f you use this in pre-menopausal women, you shift that woman to post-menopausal
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Fulvestrant
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Indications for Anastrozole, Letrozole
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All women with postmenopausal estrogen sensitive breast cancer
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MOA of Anastrozole, Letrozole
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Nonsteroidal competitive aromatase inhibitors, decreases estrogen
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Anastrozole, Letrozole Side Effects
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Nausea, hot flashes, hair thinning, muscle pain
Less CV events than tomaxifen |
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In postmenopausal women, estrogen is produced by ________ rather than by ovaries
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aromatase
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Exemestane Side Effects
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Nausea, hot flashes, edema, fatigue, less frequent gynecological symptoms, more common visual disturbances and bone fractures
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Indications for Exemestane
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Postmenopausal ER (+) breast cancer in women after 2-3 years of Tamoxifen or for 5 years by itself
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MOA of Exemestane
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Irreversible steroidal aromatase suicide inhibitor, decreases estrogen
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Flutamide, Nilutamide, Bicalutamide MOA
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Synthetic nonsteroidal anti-androgens
Binds androgen receptor to block testosterone stimulation of cancer cells |
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Side Effects of Flutamide, Nilutamide, Bicalutamide
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Gynecomastia, GI distress
Decreases libido, vasomotor flushing |
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Indications for Flutamide, Nilutamide, Bicalutamide
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Prostate cancer
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Usually given with leuprolidae or goserelin
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Flutamide, Nilutamide or Bicalutamide
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Leuprolife, Goserelin, Histrelin, Triptorelin MOA
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Analogs of GnRH
• Occupy LHRH receptor in pituitary continuously, desensitize and inhibit release of FSH and LH FSH and LH responsible for testosterone release |
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Side Effects of Leuprolife, Goserelin, Histrelin, Triptorelin
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Impotence, hot flashes, gynecomastia, N/V
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Indications for Leuprolife, Goserelin, Histrelin, Triptorelin
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Daily SQ or monthly depot for Prostate Cancer
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LHRH Antagonist Nasal Spray
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Nafarelin
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Frequencies of
IFN Alpha-2A IFN Alpha-2B |
SQ, multiple times weekly up to 12 months
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Human recombinant form made in E.coli
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IFN Alpha-2A
IFN Alpha-2B |
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Indications for IFN Alpha-2A
IFN Alpha-2B |
Hairy cell leukemia
Kaposi’s sarcoma CML Chronic hepatitis C Chronic hepatitis B Malignant melanoma MS |
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MOA of IFN Alpha-2A
IFN Alpha-2B |
• Increases cytotoxicity of NKC
• Increases phagocytic ability of macrophages • Increases ability of macrophage to present “processed antigen” to T-helpher cells |
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Immunostimulant that is passed to Fetus
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IFN Alpha-2A
IFN Alpha-2B |
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Side Effects of IFN Alpha-2A
IFN Alpha-2B |
Flu-flike symptoms, hair loss, diminish with time with daily administration
Dizziness, confusion, depression, aggressive behavior, decreased mental status, visual problems, coma CI in pregnancy, no breastfeeding |
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Aldesleukin (IL-2) Indication
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Metastatic renal cell carcinoma, metastatic melanoma, colorectal, malignant lymphoma
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Aldesleukin (IL-2) Side Effects
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Fever, chills, myalgia, N/V
Capillary leak syndrome • Hypotension (70% require pressor therapy such as fluids or alpha agonists) Arrhythmias, MI, heart failure Pulmonary edema, failure CNS – headaches, dizziness, mental changes, seizures, coma, (~70% CNS edema) Hepatotoxicity Myelosuppression |
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Aldesleukin (IL-2) MOA
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???
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Aldesleukin (IL-2) Frequency
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IV or infusion for 5-day cycles with 5-9 days between cycles
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Recombinant human IL-2 made in E.coli (immune response reaction)
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Aldesleukin (IL-2)
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Extreme caution in patients with cardiac, pulmonary, renal, or hepatic disease or seizure disorders
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Aldesleukin (IL-2)
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Immunostim that you should avoid in both pregnancy and breastfeeding
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Aldesleukin (IL-2)
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