Flashcards in Estrogens and Progesterones and Androgens Deck (40)
What are the indications for exogenous estrogens?
HRT- postmenopausal women
Primary ovarian insufficiency
Estrogens must be given with progestins in which women? Why?
Women with a uterus- to prevent endometrial hyperplasia/cancer
High risk/Prior history Breast Cancer
History endometrial cancer
History thromboembolic disease
History of genital bleeding
Effect of tamoxifen in endometrium?
Effect of tamoxifen in the bone?
Primary prevention of high risk breast cancer
Treatment of advanced breast cancer
Treatment of male gynecomastia
Tamoxifen: adverse effects?
Increased risk of thromboemoblic events
INCREASED RISK OF ENDOMETRIAL CANCER
Effect of ralxoifene in the bone?
Effect of raloxifene in the endometrium?
Treatment of osteoporosis in postmenopausal women
Alternative to tamoxifen in prevention of breast cancer primary prevention
Effect of clomiphene in the hypothalamus/pituitary?
Antagonist- inhibits negative feedback from E2 and promotes release of LH/FSH
Effect of clomiphene in the ovary?
Treatment of anovulation in PCOS
Treatment of advanced ER+ metastatic breast cancer- typically following failure of tamoxifen therapy
Name three aromatase inhibitors?
Aromatase inhibitors: indications?
Adjuvant therapy of ER+ breast cancers in postmenopausal women
Name 6 progestins
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
Bleeding due to fibroids
Decrease risk of endometrial and ovarian cancer
Combined oral contraception: contraindications
Age > 35 y & smoking
Coronary artery disease
History venous thrombosis
History of stroke
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
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?
What are contraindications for testosterone use?
Prostate cancer or high levels of PSA
Untreated sleep apnea (can worsen sleep apnea)
Name 4 AR antagonists
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
Inhibition of CYP17A1: Inhibits synthesis of testosterone (also affects cortisol ,but not aldosterone)
Hormone-resistant prostate cancer not responding to
androgen deprivation therapy
Antagonist/weak partial agonist of AR
-Also binds MR as a K+ sparing diuretic
Tx of women with hirsutism, acne, or androgenic alopecia
Name 2 5-alpha reductase inhibitors
Inhibits testosterone--> DHT conversion