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Estrogenic Drugs Flashcards

1
Q

Tamoxifen

  • MOA
  • IND
  • SE
A
  • MOA
    • SERM
    • estrogen receptor antagonist
  • IND
    • ER positive breast cancer
  • SE
    • Endometrial hyperplasia and cancer
    • Venous thromboembolism
    • Pulmonary embolism
    • Cataracts
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2
Q

Raloxifene

  • MOA
  • IND
  • SE
A
  • MOA
    • SERM
    • Antagonizes estrogen
  • IND
    • Post-menopausal osteoporosis
    • Invasive breast cancer
  • SE
    • fewer side effects than tamoxifen
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3
Q

Toremifene

  • MOA
  • IND
  • SE
A
  • MOA
    • SERM
    • ER antagonist
  • IND
    • Metastatic breat cancer
  • SE
    • Fewer side effects than tamoxifen
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4
Q

Clomiphene

  • MOA
  • IND
  • SE
A
  • MOA
    • SERM
    • Estrogen and E2 antagonist
    • Blocks negative feedback at hypothalamus and pituitary
      • (increased gonadotropins)
  • IND
    • Used to induce ovulation
  • SE
    • Thromboembolism
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5
Q

Mifepristone

  • MOA
  • IND
  • SE
A
  • MOA
    • Progesterone receptor antagonist
      • breaks down endometrium in pregnancy
    • Given with Prostaglandin
      • stimulates uterine contractions
  • IND
    • Abortifacent (through 49 days)
  • SE
    • Heavy uterine bleeding
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6
Q

Exemestane

  • MOA
  • IND
  • SE
A
  • MOA
    • Aromatase inhibitor
  • IND
    • Alternate therapy for tamoxifen
      • ER positive breast cancer
  • SE
    • Osteoporatic fractures
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7
Q

Anastrazole

  • MOA
  • IND
  • SE
A
  • MOA
    • Aromatase inhibitor (converts androgens to estrogen)
    • Decreased estradiol
  • IND
    • ER+ breast cancer
  • SE
    • Osteoporosis

Used over tamoxifen due to fewer thromboembolic events

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8
Q

Letrozole

  • MOA
  • IND
  • SE
A
  • MOA
    • Aromatase inhibitor
  • IND
    • ER positive breast cancer
    • Induce ovulation
  • SE
    • Osteoporotic fractures
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9
Q

What side effect is common in aromatase inhibiting drugs?

A

Osteoporotic fractures

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10
Q

What are legitimate uses for androgenic steroids?

A
  1. Hypogonadism
  2. Breast cancer
  3. Stimulation of erythropoiesis
    • Danazol used in anemias
  4. Hereditary angioedema
    • testosterone increases C1 inhibitor
  5. AIDS-related muscle wasting
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11
Q

Danazol

  • MOA
  • IND
  • SE
A
  • MOA
    • anti-estrogen
      • feedback suppression of gonadotropins
      • suppresses ovulation
    • weak androgen activity
  • IND
    • Heavy menstrual bleeding
    • Endometriosis
    • Fibrocystic breast disease
    • Hereditary angioedema
    • Anemia
      • Stimulation of erythropoiesis
  • SE
    • Hepatocellular damage
    • Teratogen
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12
Q

Cyproterone acetate

  • MOA
  • IND
  • SE
A
  • MOA
    • weak partial agonist for androgen receptor
      • anti-androgen
  • IND
    • Hirsutism
  • SE
    • (-) spermatogenesis
    • excessive sex drive
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13
Q

Megestrol acetate

  • MOA
  • IND
  • SE
A
  • MOA
    • weak partial agonist for androgen receptor
  • IND
    • Hirsutism
  • SE
    • (-) spermatogenesis
    • Excessive sex drive
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14
Q

Flutamide

  • MOA
  • IND
  • SE
A
  • MOA
    • Antiandrogen
  • IND
    • Prostate cancer
  • SE
    • Hepatotoxicity
    • If used alone:
      • Gynecomastia
      • Impotence
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15
Q

Bicalutamide

  • MOA
  • IND
  • SE
A
  • MOA
    • Antiandrogen
  • IND
    • Prostate cancer
  • SE
    • Less hepatotoxicity than flutamide
    • If used alone:
      • Gynecomastia
      • Impotence
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16
Q

Why is Bicalutamide preferred over Flutamide in the treatment of prostate cancer?

A

Less hepatotoxicity

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17
Q

Spironolactone

  • MOA
  • IND
  • SE
A
  • MOA
    • (-) aldosterone
      • K-sparing diuretic
    • (-) androgen receptor
    • (-) testosterone synthesis
  • IND
    • Heart failure
    • Hypertension
    • Hirsutism and acne in women
  • SE
    • Gynecomastia in men
18
Q

Finasteride

  • MOA
  • IND
A
  • MOA
    • Inhibits 5-alpha-reductase
      • decreased dihydrotestosterone
  • IND
    • Benighn prostatic hyperplasia
    • Male pattern baldness
19
Q

What are the side effects of “megadose” anabolic steroids to enhance athletic performance?

A
  1. (-) spermatogenesis
  2. Testicular atrophy
  3. Atherosclerosis
  4. Edema and weight gain
  5. Hepatic cancer
20
Q

What is the clinical use of Gossypol?

A

Male contraceptive

Permanent in 20%

21
Q

Nefidipine

  • MOA
  • IND
A
  • MOA
    • alters lipid metabolism of sperm so not able to fertilize an egg
  • IND
    • Male contraception
      • reversible
22
Q

What is the therapeutic use of RISUG / VasalGel?

A

Male contraceptive

Positive-charged polymer damages negatively charged sperm as they pass thru the vas deferens

23
Q

Sermorelin

  • MOA
  • IND
  • SE
A
  • MOA
    • analog of GHRH
  • IND
    • Test if growth hormone deficiency is primary (pituitary insufficiency) or secondary (hypothalamic insufficiency)
24
Q

What are the indications for IGF-1 Mecasermin?

A
  • Those that lack functional GH receptors in liver
  • Those that have anti-GH abs
25
Q

Octreotide

  • MOA
  • IND
A
  • MOA
    • Somatastatic analog
      • (-) GH
      • (-) pancreas insulin
  • IND
    • Acromegaly
    • Carcinoid syndrome
    • Pituitary adenomas secreting TSH
26
Q

Pegvisomant

  • MOA
  • IND
  • SE
A
  • MOA
    • GH analog
    • Binds GH receptors in liver
    • Lowers IGF levels
  • IND
    • Acromegaly
  • SE
    • Swelling of limbs
    • Hypoglycemia
    • Hepatitis
27
Q

Bromocriptine

  • MOA
  • IND
A
  • MOA
    • ergot alkaloid
    • DA agonist
  • IND
    • Prolactin secreting adenomas
28
Q

Cabergoline

  • MOA
  • IND
A
  • MOA
    • ergot alkyloid
    • DA agonist
  • IND
    • prolactin secreting adenomas
29
Q

Pitocin

  • MOA
  • IND
A
  • MOA
    • Oxytocin analog
  • IND
    • Induction of labor
    • Reduce postpartum hemorrhage
    • Stimulate milk let down response
30
Q

Dinoprost

  • MOA
  • IND
A
  • MOA
    • Prostaglandin F2
  • IND
    • Abortifacient
      • induces labor
31
Q

Dinoprostone

  • MOA
  • IND
A
  • MOA
    • Prostaglandin E2
  • IND
    • Abortifacient
      • Cervial dilation
32
Q

Misoprostol

  • MOA
  • IND
A
  • IND
    • Prostaglandin E1
  • IND
    • Abortifacient
33
Q

What is the clinical use of Ergonovine?

A

Facilitate placental delivery

34
Q

Miferpristone

  • MOA
  • IND
A
  • MOA
    • blocks progesterone receptor
  • IND
    • Abortifacient
35
Q

Atosiban

  • MOA
  • IND
A
  • MOA
    • Oxytocin receptor antagonist
  • IND
    • Prevent uterine contractions
36
Q

Nefedipine

  • MOA
  • IND
A
  • MOA
    • Ca channel blocker
  • IND
    • Prevent uterine contractions
37
Q

Terbutaline

  • MOA
  • IND
A
  • MOA
    • ß2 agonist
  • IND
    • (-) uterine contractions
38
Q

Indomethacin

  • MOA
  • IND
A
  • MOA
    • COX inhibitor
  • IND
    • (-) uterine contractions
39
Q

Magnesium sulfate IV

  • MOA
  • IND
A
  • MOA
    • Myosin light chain inhibitor
  • IND
    • Prevent uterine contractions
40
Q

Desmopressin

  • MOA
  • IND
A
  • MOA
    • analog of vasopressin
  • IND
    • Neurogenic diabetes insipidis
      • lacks post. pituitary ADH secretion
    • Nocturnal enuresis
    • Bleeding disorders
      • smooth muscle contraction
    • Esophageal varicies
41
Q

Conivaptan

  • MOA
  • IND
A
  • MOA
    • Vasopressing antagonist
    • binds V1 and V2
  • IND
    • Hypovolemic hyponatremia
      • HF
      • Cirrhosis
      • Syndrome of inappropriate ADH
42
Q

Tolvaptan

  • MOA
  • IND
A
  • MOA
    • Vasopressing antagonist
    • binds V2 only
  • IND
    • Hypovolemic hyponatremia
      • HF
      • Cirrhosis
      • Syndrome of inappropriate ADH

Pharmacology (12 decks)

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