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)
Progestin drugs with the most Androgenic effect
Only progestin drugs with NO androgen effect
Levonorgestel (++++), Desogestrel (+++), Norgestrel (+++)
Drospirenone (Spironolactone-analog), Dienogest
Non-Oral Progestins (w/ administration type)
Norelgestromin (patch WITH ESTROGEN) Etonogestrel (vaginal ring WITH ESTROGEN) Etonogestrel (implantable rod) Medroxyprogesterone (injection) Levonorgestrel (IUD)
Non-contraceptive benefits of combination HCs include reduction in what cancers?
Ovary, Endometrium, Colon/Rectum
Non-contraceptive benefits of combination HCs include improvements in what other symptoms?
Irregular cycles, dysmenorrhea, menorrhagia, function ovarian cysts, acne, anemia, PMDD
Non-contraceptive benefits of combination HCs include the prevention of what things?
Bone loss, fibrocystic/benign breast disease, PID, ectopic pregnancy
Non-contraceptive benefits of combination HCs include the treatment of what other symptoms?
Acne, hirsutism, peri-menopausal symptoms
***Estrogens have been shown to DECREASE what lab values/physiologic activities?
Cholesterol (TC, LDL)
Anti-thrombin 3
Osteoclastic activity (bone turnover)
Bile acid levels
***Estrogens have been shown to INCREASE what lab values/physiologic activities?
TGs and HDL Clotting factors Platelet aggregation RAAS activity (Na/fluid retention) Hormone-binding globulins Iron/TIBC Prolactin
Adverse effects of HCs
Irregular bleeding, breast tenderness, fluid retention (weight gain), mood changes, headaches and GI distress, hyperkalemia (Drospirenone), acne/hirsutism/wt gain (androgenic effects)
SERIOUS adverse effects of HCs
MI/Stroke/DVT/PE/intestinal ischemia
HTN
Gallbladder disease
**CONTRAINDICATIONS to using HCs
Hx of vascular-related disease Pregnancy Breast/endometrial/hepatic neoplasms Undiagnosed vaginal bleeding Uncontrolled HTN SMOKER (>35 y/o)
Emergency contraception - drug
MoA
Levonorgestrel
Inhibition of ovulation
Emergency contraception must be administered before what?
Implantation
What is Ella?
MoA
Ulipristal acetate – emergency contraception
Progesterone-receptor modulator – inhibits ovulation
