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Human Reproduction > Week 4: Reproductive Pharmacology: Antiestrogens > Flashcards

Week 4: Reproductive Pharmacology: Antiestrogens Flashcards

1
Q

Fluvestrant MOA

A

Estrogen receptor antagonist

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2
Q

Fluvestrant clinical uses

A

Treatment of Tamoxifen-resistant breast cancer

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3
Q

Fluvestrant side effects

A
  • Hot flushes
  • injection site pain
  • live enzyme abnormalities
  • joint disorders
  • Hypersensitivity reactions have been reported (including urticaria and angioedema)
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4
Q

Fluvestrant contraidnications

A
  • Hypersensitivity reactions have been reported (including urticaria and angioedema)
  • use with caution in patients with a history of bleeding disorders (including thrombocytopenia) and/or patients on anticoagulant therapy
    • bleeding/hematoma may occur from IM administration
  • Use with caution in patients with hepatic impairment
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5
Q

Tamoxifen MOA

A

Selective Estrogen Receptor Modulator (SERM)

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6
Q

SERM AKA

A

Selective Estrogen Receptor Modulator

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7
Q

Tamoxifen clinical uses

A

Hormone-responsive breast cancer

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8
Q

Tamoxifen side effects

A
  • Cardiovascular effects (eg vasodilation, hypertension, peripheral edema)
  • CNS effects (eg mood changes)
  • Dermatologic effects (hot flashesm fluid retention, altered menses, amenorrhea)
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9
Q

Tamoxifen contraindications

A
  • concurrent warfarin therapy or history of DVT or PE
  • Tamoxifen use for breast cancer risk reduction in women at high-risk for breast cancer and in women with ductal carcinoma in situ (DCIS) is associated with an increased incidence of uterine or endometrial cancers and thromboembolic events
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10
Q

DCIS AKA

A

Ductal carcinoma in situ (DCIS)

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11
Q

Tamoxifen notes

A

Off-label use in females with precocious puberty secondary to McCune-Albright Syndrome

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12
Q

Anastrozole MOA

A

Aromatase inhibitor

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13
Q

Anastrozole clinical use

A

Breast cancer; First-line treatment of locally advanced or metastatic breast cancer (hormone receptor-positive or unknown) in postmenopausal women

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14
Q

Anastrozole side effects

A
  • Vasodilation
  • ischemic heart disease (17% of patients with pre-existing ischemic heart disease)
  • edema
  • CNS effects (eg fatigue, mood disorder, headache)
  • hot flashes
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15
Q

Anastrozole contrainidications

A

Concerns:

Associated with a reduction in bone mineral density; use with caution in patients with hyperlipidemias

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16
Q

Anastrozole notes

A

Anastrozole offers no clinical benefit in premenopausal women with breast cancer

17
Q

Danazol MOA

A

Inhibits several cytochrome P450 enzymes involved in gonadal steroid synthesis and is a weak partial agonist of progestin, androgen and glucocorticoid receptors

18
Q

Danazol clinical use

A

Treatment of:

  • endometriosis
  • fibrocystic breast disease
  • hereditary angioedema
19
Q

Danazol side effects

A
  • Edema
  • Flushing
  • Hypertension
  • Amenorrhea (which may continue post-therapy)
  • various CNS effects
20
Q

Danazol contraindications

A
  • Breast-feeding
  • porphyria
  • markedly impaired hepatic, renal or cardiac function
  • androgen-dependent tumor
  • active or history of thrombosis or thromboembolic disease
  • Danazol administration has been associated with several cases benign intracranial hypertension also known as pseudotumor cerebri
21
Q

Danazol notes

A

May cause nonreversible androgenic effects

22
Q

Clomiphene MOA

A
  • Selective Estrogen receptor modulator (SERM) acting as an estrogen receptor antagonist
  • Increases FSH and LH release by anterior pituitary
23
Q

Clomiphene clinical uses

A
  • Infertility
  • Ovulation induction
24
Q

Clomiphene side effects

A
  • Multiple gestations
  • Ovarian hyperstimulation
  • Ovarian cysts
  • Headache
  • Dizziness
  • Blurred vision
  • Abnormal vaginal bleeding
25
Q

Clomiphene contraindications

A
  • Ovarian cyst
  • Pituitary tumor
26
Q

Leuprolide MOA

A
  • GnRH analog: acts as an agonist at the GnRH
  • Pulsatile administration mimicking endogenous release induces ovulation in anovulatory conditions
  • Chronic administration leads to receptor GnRH downregulation: can be used to downregulate FSH and LH release, allowing for administration of exogenous FSH and LH (or hCG) to induce ovulation
  • Can also be used to trigger FSH and LH release
27
Q

Leuprolide clinical uses

A
  • Infertility
  • precocious puberty
28
Q

Leuprolide side effects

A
  • Hot flashes
  • headache
  • breakthrough bleeding
29
Q

Leuprolide contraindications

A

Known allergic reactions to leuprolide

30
Q

Leuprolide notes

A

Also used in treating prostate cancer and endometriosis

Human Reproduction (40 decks)

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