Estrogens, Progestins, And Hormone Replacement Flashcards
List 4 progestins
Progesterone
Medroxyprogesterone
Norethindrone
Norgestimate
List 3 estrogens
Estradiol
Conjugated Estrogens
Ethinyl estradiol
SERMS
- Tamoxifen
- Raloxifene
Bisphosphates
Alendronate
Ibandronate
1) Estrogens do what to the endometrium?
2) Progesterone does what to endometrium?
1) Stimulate growth
2) Inhibits endometrial growth, maintains vascular supply and secretory capacity, an its withdrawal leads to menstruation.
Metabolic effects of estrogen includes:
- Decreased bone resorption
- Decreased total and LDL cholesterol, increased HDL and Trigs
- Increased synthesis of blood clotting factors and angiotensinogen
- Increased levels of binding globulins for thyroxine, cortisol, sex steroids
What has rapid first pass metabolism in the liver when given orally and is mainly used in hormone replacement therapy (HRT) and hypogonadism?
Estradiol- Can be in slow-release depot forms for IM injection, Topical preps, micronized oral prep.
Most common of several natural estrogen preparations, containing ester conjugates and salts of estrone and estriol. Major use is in HRT. What is it?
Conjugated Estrogens
What is a synthetic estradiol analog?
Ethinyl estradiol
What does the Ethinyl group do in ethinyl estradiol?
Slows metabolism, increases potency and oral effectiveness.
What is a prodrug of ethinyl estradiol?
Mestranol
Therapeutic uses of estrogens include:
-Hypogonadism, hypopituitarism.
A) Replacement therapy to promote normal growth and development of secondary sexual characteristics.
B) Low dose for growth stimulation, higher doses for epiphysial closure and sexual development. Gonadotropins (LH and FSH) required for fertility.
- Post-menopausal replacement therapy
- In oral contraceptives
SE of estrogens
- Nausea, edema, breast tenderness, hyperpigmentation
- Migraine, cholestasis, insulin resistance, liver and gallbladder disease
- Thromboembolic complications
- Endometrial hyperplasia- increase risk of cancer
- Gynecomastia, feminization in men
- Teratogenesis occurred with long-ago use of DES early in pregnancy
- Metabolic changes in cholesterol, bone, clotting factors, esp. high dose oral preps.
What progestins are available?
- Progesterone
- Medoxyprogesterone
- Norethindrone
- Norethindrone
- Norgeastimate
What may be safer for long-term HRT for progesterone? Available in IM, creams, suppositories, slow release IUD.
Progesterone (generic)
What is the prototype of synthetic progestins structurally related to progesterone (21 carbons)? Used as the acetate ester.
Medoxyprogesterone
T/F: Medoxyprogesterone has mainly progesterone-like effects, with little or no concern about androgen or estrogen activity?
True
What is the prototype of synthetic progestins structurally related to testosterone (18 carbons)?
Norethindrone
T/F: Norethindrone retains some androgenic activity, causing beneficial effects?
False- causing unwanted side effects.
How is Norethindrone administered and how are the used?
Oral- used in oral contraceptives, some now for HRT.
What is a new derivative of northindrone with essentially no androgenic effect and are used only in combo oral contraceptives?
Norgestimate
Adverse effects of androgenic progestins are…
-SE for all progestins include…
Acne, wt. gain, masculinization, altered libido, decreased HDl and increased LDL.
-All progestins: Menstrual changes, nausea, bloating, teratogenesis, others
The women’s health initiative (WHI) found that HRT for long term use does what?
-Increase risk of coronary heart disease, strokes, and pulmonary embolisms.Reduced osteoporosis and colorectal cancer. Both estrogen and progestin increase risk of breast CA.
If a patient has no uterus, what would you use for HRT?
Just estrogen
