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

Raloxifene MOA IND SE

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

Toremifene MOA IND SE

MOA SERM ER antagonist IND Metastatic breat cancer SE Fewer side effects than tamoxifen

Clomiphene MOA IND SE

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

Mifepristone MOA IND SE

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

Exemestane MOA IND SE

MOA Aromatase inhibitor IND Alternate therapy for tamoxifen ER positive breast cancer SE Osteoporatic fractures

Anastrazole MOA IND SE

MOA Aromatase inhibitor (converts androgens to estrogen) Decreased estradiol IND ER+ breast cancer SE Osteoporosis Used over tamoxifen due to fewer thromboembolic events

MOA Aromatase inhibitor IND ER positive breast cancer Induce ovulation SE Osteoporotic fractures

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

Cyproterone acetate MOA IND SE

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

Megestrol acetate MOA IND SE

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

MOA Antiandrogen IND Prostate cancer SE Hepatotoxicity If used alone: Gynecomastia Impotence

Bicalutamide MOA IND SE

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

Spironolactone MOA IND SE

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

Estrogenic Drugs Flashcards by Brittany Byerley

Tamoxifen

MOA
- SERM
- estrogen receptor antagonist
IND
- ER positive breast cancer
SE
- Endometrial hyperplasia and cancer
- Venous thromboembolism
- Pulmonary embolism
- Cataracts

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Raloxifene

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

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Toremifene

MOA
- SERM
- ER antagonist
IND
- Metastatic breat cancer
SE
- Fewer side effects than tamoxifen

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Clomiphene

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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Mifepristone

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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Exemestane

MOA
- Aromatase inhibitor
IND
- Alternate therapy for tamoxifen
  - ER positive breast cancer
SE
- Osteoporatic fractures

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Anastrazole

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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Letrozole

MOA
- Aromatase inhibitor
IND
- ER positive breast cancer
- Induce ovulation
SE
- Osteoporotic fractures

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What side effect is common in aromatase inhibiting drugs?

Osteoporotic fractures

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What are legitimate uses for androgenic steroids?

Hypogonadism
Breast cancer
Stimulation of erythropoiesis
- Danazol used in anemias
Hereditary angioedema
- testosterone increases C1 inhibitor
AIDS-related muscle wasting

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Danazol

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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Cyproterone acetate

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

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Megestrol acetate

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

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Flutamide

MOA
- Antiandrogen
IND
- Prostate cancer
SE
- Hepatotoxicity
- If used alone:
  - Gynecomastia
  - Impotence

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Bicalutamide

MOA
- Antiandrogen
IND
- Prostate cancer
SE
- Less hepatotoxicity than flutamide
- If used alone:
  - Gynecomastia
  - Impotence

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

Less hepatotoxicity

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Spironolactone

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

Finasteride

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MOA
- Inhibits 5-alpha-reductase
  - decreased dihydrotestosterone
IND
- Benighn prostatic hyperplasia
- Male pattern baldness

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

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(-) spermatogenesis
Testicular atrophy
Atherosclerosis
Edema and weight gain
Hepatic cancer

What is the clinical use of Gossypol?

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Male contraceptive

Permanent in 20%

Nefidipine

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MOA
- alters lipid metabolism of sperm so not able to fertilize an egg
IND
- Male contraception
  - reversible

What is the therapeutic use of RISUG / VasalGel?

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Male contraceptive

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

Sermorelin

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MOA
- analog of GHRH
IND
- Test if growth hormone deficiency is primary (pituitary insufficiency) or secondary (hypothalamic insufficiency)

What are the indications for IGF-1 Mecasermin?

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Those that lack functional GH receptors in liver
Those that have anti-GH abs

Octreotide * MOA * IND

* MOA * Somatastatic analog * (-) GH * (-) pancreas insulin * IND * Acromegaly * Carcinoid syndrome * Pituitary adenomas secreting TSH

Pegvisomant * MOA * IND * SE

* MOA * GH analog * Binds GH receptors in liver * Lowers IGF levels * IND * Acromegaly * SE * Swelling of limbs * Hypoglycemia * Hepatitis

Bromocriptine * MOA * IND

* MOA * ergot alkaloid * DA agonist * IND * Prolactin secreting adenomas

Cabergoline * MOA * IND

* MOA * ergot alkyloid * DA agonist * IND * prolactin secreting adenomas

Pitocin * MOA * IND

* MOA * Oxytocin analog * IND * Induction of labor * Reduce postpartum hemorrhage * Stimulate milk let down response

Dinoprost * MOA * IND

* MOA * Prostaglandin F2 * IND * Abortifacient * induces labor

Dinoprostone * MOA * IND

* MOA * Prostaglandin E2 * IND * Abortifacient * Cervial dilation

Misoprostol * MOA * IND

* IND * Prostaglandin E1 * IND * Abortifacient

What is the clinical use of Ergonovine?

Facilitate placental delivery

Miferpristone * MOA * IND

* MOA * blocks progesterone receptor * IND * Abortifacient

Atosiban * MOA * IND

* MOA * Oxytocin receptor antagonist * IND * Prevent uterine contractions

Nefedipine * MOA * IND

* MOA * Ca channel blocker * IND * Prevent uterine contractions

Terbutaline * MOA * IND

* MOA * ß2 agonist * IND * (-) uterine contractions

Indomethacin * MOA * IND

* MOA * COX inhibitor * IND * (-) uterine contractions

Magnesium sulfate IV * MOA * IND

* MOA * Myosin light chain inhibitor * IND * Prevent uterine contractions

Desmopressin * MOA * IND

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

Conivaptan * MOA * IND

* MOA * Vasopressing antagonist * binds V1 and V2 * IND * Hypovolemic hyponatremia * HF * Cirrhosis * Syndrome of inappropriate ADH

Tolvaptan * MOA * IND

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

Estrogenic Drugs Flashcards

(42 cards)