Hormonal Contraceptives - Segars Flashcards
**5 MoAs of HCs
- Modify mid-cycle surges of LH and FSH
- Inhibit ovulation by suppressing HPO axis
- Diminish ovarian hormone production
- Produce unfavorable endometrial changes
- Thicken cervical mucus to impede sperm transit
3 types of oral tablets
- Combo
- Progestin only
- Extended cycle
5 types of non-daily methods
- Injectable
- Implantable
- Patch
- Vaginal ring
- IUD
3 estrogens in oral HCs
- Ethinyl estradiol
- Estradiol valerate
- Mestranol
How is ethinyl estradiol different from normal estradiol?
Ethinyl group slows hepatic/enzymatic degradation (much longer half life)
What is estradiol valerate?
Synthetic pro-drug of 17-beta estradiol, metabolized to estradiol
What is Mestranol?
Metabolized to ethinyl estradiol
Progestin groups in HCs
Which group has more masculinizing effects?
- 19-Nortestosterone-analogs
- Spironolactone-analog
19-NT
Groups of 19-Nortestosterone-analogs
Which group has more estrogenic effects and issues?
Estranes
Gonanes
Estranes
A patient is having an estrogen-related side effect of her HC. Which progestin drug group is a better substitute: Estranes or Gonanes?
Gonanes
3 Estrane drugs
Norethindrone
Norethindrone acetate
Ethynodiol diacetate
5 Gonane drugs
Desogestrel Dienogest Levonorgestrel Norgestrel Norgestimate
Spironolactone-analog drug
Drospirenone
Progestin drugs with the most Progestin effect
What class are those? Are ALL gonanes like them?
Desogestrel (++++), Levonorgestrel (++++), Norgestrel (+++)
Gonanes (19-NT); NO, only these 3
Progestin drugs with any Estrogen effect
What drug class are they?
Ethynodiol diacetate (+++), Norethindrone (++), Norethindrone acetate (++)
Estranes (19-NT)