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41 Cards in this Set

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Indication for Tamoxifen
Estrogen-dependent breast cancer
MOA of Tamoxifen
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
Tamoxifen Side Effects
Hot flashes, N/V, myelosuppression, DVT, pulmonary embolism

Linked to endometrial cancer and blood clots

(+) estrogenic effects on bone and cholesterol
Indication for Toremifene
Estrogen-dependent breast cancer

Possible: prostate cancer prophylaxis
MOA of Toremifene
Tamoxifen analog – increases TNF-beta, decreases cell proliferation and cell growth
Toremifene Side Effects
Hot flashes, N/V, myelosuppression, DVT, pulmonary embolism

Linked to endometrial cancer and blood clots

(+) estrogenic effects on bone and cholesterol
Indication for Raloxifene
Osteoporosis

FDA (2007) – reduce breast cancer risk in postmenopausal women with osteoporosis and postmenopausal at high risk for breast cancer
MOA of Raloxifene
SERM
• Estrogen effects in bone and CV
• Antagonist in breast and uterine tissue
Raloxifene Side Effects
Increased incidence of thromboembolism, hot flashes, muscle cramps, teratogenic in animals
Indications for Fulvestrant
Postmenopausal hormone sensitive metastatic breast cancer (monthly IM injections)
MOA of Fulvestrant
SERD
• Pure anti-estrogen, down regulates estrogen receptor
Fulvestrant Side Effects
Nausea
Asthenia
Pain
Vasodilation
Headache
f you use this in pre-menopausal women, you shift that woman to post-menopausal
Fulvestrant
Indications for Anastrozole, Letrozole
All women with postmenopausal estrogen sensitive breast cancer
MOA of Anastrozole, Letrozole
Nonsteroidal competitive aromatase inhibitors, decreases estrogen
Anastrozole, Letrozole Side Effects
Nausea, hot flashes, hair thinning, muscle pain

Less CV events than tomaxifen
In postmenopausal women, estrogen is produced by ________ rather than by ovaries
aromatase
Exemestane Side Effects
Nausea, hot flashes, edema, fatigue, less frequent gynecological symptoms, more common visual disturbances and bone fractures
Indications for Exemestane
Postmenopausal ER (+) breast cancer in women after 2-3 years of Tamoxifen or for 5 years by itself
MOA of Exemestane
Irreversible steroidal aromatase suicide inhibitor, decreases estrogen
Flutamide, Nilutamide, Bicalutamide MOA
Synthetic nonsteroidal anti-androgens

Binds androgen receptor to block testosterone stimulation of cancer cells
Side Effects of Flutamide, Nilutamide, Bicalutamide
Gynecomastia, GI distress

Decreases libido, vasomotor flushing
Indications for Flutamide, Nilutamide, Bicalutamide
Prostate cancer
Usually given with leuprolidae or goserelin
Flutamide, Nilutamide or Bicalutamide
Leuprolife, Goserelin, Histrelin, Triptorelin MOA
Analogs of GnRH
• Occupy LHRH receptor in pituitary continuously, desensitize and inhibit release of FSH and LH
FSH and LH responsible for testosterone release
Side Effects of Leuprolife, Goserelin, Histrelin, Triptorelin
Impotence, hot flashes, gynecomastia, N/V
Indications for Leuprolife, Goserelin, Histrelin, Triptorelin
Daily SQ or monthly depot for Prostate Cancer
LHRH Antagonist Nasal Spray
Nafarelin
Frequencies of
IFN Alpha-2A
IFN Alpha-2B
SQ, multiple times weekly up to 12 months
Human recombinant form made in E.coli
IFN Alpha-2A
IFN Alpha-2B
Indications for IFN Alpha-2A
IFN Alpha-2B
Hairy cell leukemia
Kaposi’s sarcoma
CML
Chronic hepatitis C
Chronic hepatitis B
Malignant melanoma
MS
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
Immunostimulant that is passed to Fetus
IFN Alpha-2A
IFN Alpha-2B
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
Aldesleukin (IL-2) Indication
Metastatic renal cell carcinoma, metastatic melanoma, colorectal, malignant lymphoma
Aldesleukin (IL-2) Side Effects
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
Aldesleukin (IL-2) MOA
???
Aldesleukin (IL-2) Frequency
IV or infusion for 5-day cycles with 5-9 days between cycles
Recombinant human IL-2 made in E.coli (immune response reaction)
Aldesleukin (IL-2)
Extreme caution in patients with cardiac, pulmonary, renal, or hepatic disease or seizure disorders
Aldesleukin (IL-2)
Immunostim that you should avoid in both pregnancy and breastfeeding
Aldesleukin (IL-2)