Gonadal hormones Flashcards
How many carbons for each gonadal hormones.
Estrogen 18C
Progesterone C-21 steroid
Testosterone C-19 steroid
Full estrogen antagonist.
Partial estrogen antagonist and agonist.
Clomiphene and Tamoxifen
Raloxifine (Selective E receptor modulator SERM)
How does Clomiphene stimulate ovulation?
Interferes with negative feedback of E on hypothalamus and pituitary thus inc. secretion of gonadotropin releasing hormone (GnRH)
Raloxifine agonist and antagonist effect?
Agonist: reduced bone resorption thereby decreases bone turnover and on lipid metabolism
Antagonist: Effect on uterine and breast tissues
Antiestrogen drugs’ side effects.
Tamoxifen: hot flashes, vag bleeding, mens irreg, risk of endometrial cancer, n & v (least nauseating anticancer drug)
Clomiphene: ovarian enlargement, vasomotor flushes, visual disturbances
Raloxifine: hot flushes
Basic nucleus of Progesterone.
Pregnane
Two types of Progesterone.
17-alpha hydroxyprogesterone such as medroxyprogesterone acetate and megestrol acetate.
17-alpha ethinylandrogens (more potent) Norethindrone and Norethynodrel
Norethindrone and Norethynodrel are commonly used as what?
oral contraceptives due to potent oral activity, more lipid soluble and less first pass metabolism
Progesterone is used alone for the treatment of what?
Amenorrhea, abnormal uterine bleeding and endometriosis
Injection used for amenorrhea and abnormal uterine bleeding, and dosing.
Medroxyprogesterone acetate (Depo-Provera injection) 150mg injected every 3 months
Progesterone SE
Unexpected or increased lactation, depression, loss or changes in speech, coordination, stomach pain, swelling of face ankles feet, moods fatigue
OCP used when progesterone levels are high and as abortifacient MOA.
Mifepristone (RU 486) - partial ago and anta progesterone. Interferes with progesterone and decreases hCG production
Estrogen SEs
Feminization, nausea, stomach upset, depression, weight gain, inc blood clotting, edema, HTN, stroke MI, late bleeding
Anastrozole and Finasteride are what type of inhibitors?
Anatrozole- Aromatase inhibitors
Finasteride- 5-alphase reductase inhibitors
Depo-provera can be used postabortal state when? And during lactation?
postabortal state - 5 days postpartum
during lactation - 6wk postpartum