Estrogens and Progesterones and Androgens Flashcards by Allison Zarnke

What are the indications for exogenous estrogens?

HRT- postmenopausal women
Oral contraceptives
Primary hypogonadism
Primary ovarian insufficiency

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Estrogens must be given with progestins in which women? Why?

Women with a uterus- to prevent endometrial hyperplasia/cancer

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Estrogens: contraindications?

High risk/Prior history Breast Cancer
History endometrial cancer
History thromboembolic disease
History of genital bleeding
Liver disease
Heavy smoking

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Effect of tamoxifen in endometrium?

Partial agonist

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Effect of tamoxifen in the bone?

partial agonist

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Tamoxifen: indication?

Primary prevention of high risk breast cancer
Treatment of advanced breast cancer
Treatment of male gynecomastia

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Tamoxifen: adverse effects?

Hot flashes
Increased risk of thromboemoblic events
INCREASED RISK OF ENDOMETRIAL CANCER

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Effect of ralxoifene in the bone?

Partial agonist

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Effect of raloxifene in the endometrium?

antagonist

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Raloxifene: indications

Treatment of osteoporosis in postmenopausal women

Alternative to tamoxifen in prevention of breast cancer primary prevention

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Effect of clomiphene in the hypothalamus/pituitary?

Antagonist- inhibits negative feedback from E2 and promotes release of LH/FSH

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Effect of clomiphene in the ovary?

Partial agonist

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Clomiphene: indication?

Treatment of anovulation in PCOS

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Fulvestrant: indications?

Treatment of advanced ER+ metastatic breast cancer- typically following failure of tamoxifen therapy

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Name three aromatase inhibitors?

Anastrazole
Letrozole
Exemestane

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Aromatase inhibitors: indications?

Adjuvant therapy of ER+ breast cancers in postmenopausal women

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Name 6 progestins

Norgestrel
Levongestrel
Norethindrone
Desogestrel
Gestodene
Norgestimate

Progestins: indications?

Hormone replacement

Hormonal contraception

How do progestins work as contraceptives?

Decrease GnRH frequency –> decrease gonadotropin release and ovulation
Thickens cervical mucus

Other than contraception, what are combined oral contraceptives used for?

Menstrual cycle disorders
Hyperandrogenism (acne)
Bleeding due to fibroids
Endometriosis
Decrease risk of endometrial and ovarian cancer

Combined oral contraception: contraindications

Age > 35 y &amp; smoking
Coronary artery disease
History venous thrombosis
History of stroke
Systemic lupus
History breast cancer
History liver disease

What the MOA of high dose levonorgestrel?

Activates PR –> inhibits/delays ovulation by inhibiting the LH surge

When is high dose levonorgestrel effective?

Only effective if given 1-2d prior to LH surge. Must be given within 72h of intercourse
- Taken once daily for 5 d

Ulipristal: MOA?

Partial agonist of PR: antagonist in the presence of progesterone

Effective at delaying/inhibiting ovulation even if given during LH surge

Other than use as "plan B" - what is another indication for ulipristal?

Tx of uterine fibroids

When is ulipristal effective at preventing unwanted pregnancy?

Effective if given up to 5 days after sex

Mifepristone + misprostal: indication

abortifactant (<70 days gestation)

What are the MOAs of Mifepristone and misprostal?

Mifepristone: PR antagonist- promotes menses (also GR and AR antagonist) Misprostal: promotes uterine contraction to expel the fetus

What are contraindications of mifepristone/misprostal?

Chronic adrenal insufficiency can precipitate and adrenal crisis (through GR receptor antagonism) Bleeding disorders or people on anticoagulants

What is the only indication for giving exogenous testosterone?

Male hypogonadism

What are contraindications for testosterone use?

Prostate cancer or high levels of PSA | Untreated sleep apnea (can worsen sleep apnea)

Name 4 AR antagonists

Flutamide Bicalutamide Nilutamide Enzalutamide

What are the indications for the AR antagonists?

Treatment of advanced prostate cancer - used in combo with androgen deprivation therapy (GnRH agonists/antagonists) Flutamide is also used in treatment of hyperandrogenism in women

Abiraterone: MOA?

Inhibition of CYP17A1: Inhibits synthesis of testosterone (also affects cortisol ,but not aldosterone)

Abiraterone: indications?

Hormone-resistant prostate cancer not responding to | androgen deprivation therapy

Spironolactone: MOA?

Antagonist/weak partial agonist of AR -Also binds MR as a K+ sparing diuretic

Spironolactone: indication?

Tx of women with hirsutism, acne, or androgenic alopecia

Name 2 5-alpha reductase inhibitors

Finasteride | Dutasteride

Finasteride/Dutasteride: MOA?

Inhibits testosterone--> DHT conversion

Finasteride/Dutasteride: indications?

BPH, male pattern baldness, female hirsutism