Estrogens and Progestins

Question 1

Estrogens

Answer 1

Sexual development, maintain reproductive tissue
Stimulate long-bone growth, closure of epiphyses
Decreased bone resorption
Improves lipid profiles, decreased LDL, increased HDL, decreased CV dz risk
Increased risk blood clotting, thrombotic dz

Question 2

Estradiol

Answer 2

Oral, rapid first pass metabolism
Slow-release depot forms (fatty acid esters) (IM)
Topical (vaginal creams, ring, transdermal patches, transdermal spray, micronized oral prep)
Use: HRT, hypogonadism

Question 3

Conjugated estrogens

Answer 3

Ester conjugates and salts of estrone + estriol
Premarin: pregnant mare urine
Oral, IV, IM, vaginal
Use: HRT

Question 4

Ethinyl estradiol

Answer 4

Synthetic estradiol analog 
Ethinyl group: slows metabolism 
Increased potency, oral effectiveness, duration of action 
Mestranol: prodrug 
Use: OC, HRT

Question 5

Progesterone

Answer 5

IM, cream, suppository, IUD
Retain 19-Me group, C20-21 structure (21C)
No concern about androgen/estrogen activity

Question 6

Medoxyprogesterone acetate

Answer 6

Oral, IM

Injection as long-acting contraceptive

Question 7

Synthetic progestins

Answer 7

Structurally related to testosterone
Lack C20-21 structure
Lack 19-Me group
“19-nor” testosterone derivative
Chemically altered: orally effective, progesterone-like activity, decrease androgenic activity, “impeded androgens”
Some retain residual androgenic activity (unwanted side effects)
Orally effective, OC, HRT

Question 8

Norethindrone acetate

Answer 8

synthetic progestin

Significant androgenic action

Question 9

Progestins

Answer 9

Use: contraception, HRT (with E), dysfxnl uterine bleeding (endometrial hyperplasia), endometriosis, metastatic endometrial/breast cancer
Adverse: acne, menstrual changes, nausea, bloating, teratogenesis?
Androgenic progestins: severe acne, wt gain, masculinization, altered libido, worsened serum lipid profiles