Menotropins
human menopausal gonadotropin, or hMG
Follicle stimulating hormone (3)
Follitropin alfa (rFSH alfa), Follitropin beta (rFSH beta), Urofollitropin (uFSH)
Leuteinizing hormone
Lutropin alfa
Human choriogonadotropin hormone
Choriogonadotropin alfa (rhCG)
Gonadotropin-releasing hormone analogs (6)
- Leuprolide
* You have to grow up to ride loop-rollercoasters - Goserelin, Histrelin, Nafarelin, Triptorelin, Gonadorelin (synthetic human GnRH)
* Ellen was always very little
Gonadotropin-releasing hormone antagonists (3)
Cetrorelix, Degarelix, Ganirelix
Estrogens (4)
Conjugated estrogens (Premarin), Estradiol valerate, Ethinyl estradiol, Mestranol
Progestins (6)
Desogestrel/Etonogestrel, Drospinenone, Medroxyprogesterone, Norethindrone, Norgestimate, Norgestrel
Estrogen and Progesterone inhibitors and antagonists (4 classes)
- Mifepristone
- Selective estrogen receptor modulators (Raloxifene, Tamoxifen Toremifene)
- Aromatase inhibitors (Anastrazole, Exemestane, Letrozole)
Which estrogen is commonly found in oral and implantable contraceptives?
Ethinyl estradiol
Which has more variation in oral and implantable contraceptives, estrogen or progesterone?
Progesterone
Why is Ethinyl estradiol so common?
Very potent; resistant to hepatic metabolism –> can give very low dose
Estrogen adverse effects
Nausea, breast tenderness, hyperpigmentation, increased migraines, cholestasis, gallbladder disease, HTN, Breast/Endometrial cancer(?)
Estrogen contraindications
Estrogen-dependent neoplasm, genital bleeding, liver disease, blood disorder, heavy smoker, CV disease, migraine with aura
Progesterone adverse effects
Breakthrough bleeding, Breast cancer, androgenic effects (weight gain, acne, hirsutism, low HDL)
When to give progestin-only contraceptive
Migraines, 35yo+ and smoker or obese, blood disorder, CV disease, HTN, SLE, high cholesterol
Which progesterone is not androgenic?
Desogestrel, Norgestimate
Dropsirenone
Dees No Drops (your voice)
Acne treatment
Desogestrel, Norgestimate, Dropsirenone
Combination oral contraceptives MOA
Prevent ovulation (feedback inhibition)
- suppressed GnRH/LH/FSH
- absent LH surge
- low endogenous steroids
Progestin-only pills
Highly effective - thick cervical mucus, impaired implantation; only blocks 60% ovulations
Benefits of Combination oral contraceptives
Estrogen - osteoporosis prevention, reduced cholesterol
Combination - reduce ovarian & colon cancer, ectopic pregnancy, breast disease, dysfunctional uterine bleeding/dysmenorrhea; improve PMS, hirsutism, acne
Benefit of LARC
e. g. Mirena (Levonorgestrel)
- Rapid return to fertility after removal
Implantable contraceptive
Etonogestrel (progestin)
Depo-provera
Medroxyprogesterone acetate
- IM or SQ every 3 mos
- can take 6-12 mos for fertility to return
Transdermal preparatoin
Ethinyl estradiol & Norelgestromin
Vaginal contraceptive ring
Ethinyl estradiol & Etonogestrel
(NuvaRing)
- rapid return to fertility after removal
Failure rate with typical and perfect use
- COC
- Progestin-only
- Transdermal
- Vaginal
Typical use: 9%
Perfect use: 0.3%
Failure rate with typical and perfect use
- IUD
- Implant
- Sterilization (female)
Typical use
- IUD: 0.15-0.4%
- Implant: 0.05%
- Sterilization: 0.5%
Perfect use
- IUD: 0.2-0.4%
- Implant: 0.05%
- Sterilization: 0.5%
DDIs
Cytochrome P450 inducers
- Phenytoin
- Rifampin
Antibiotics (interfere with GI flora’s ability to increase bioavailability of estrogens)
Pregnancy termination
Mifepristone
*“But I want my life to be pristine… wahh.”
- progesterone receptor antagonist
- used with Misoprostol (prostaglandin E1)
- 95% effective within 7 weeks
ADR: prolonged bleeding
Morning after
Levonorgestrel
- progesterone receptor antagonist
- DOES NOT reverse pregnancy
- No rx
Ulipristal acetate
- progesterone receptor antagonist
- may interfere with pregnancy
- Rx required
Time frame for most postcoital contraceptives
72 hours (for 99% effectiveness)
Absolute contraindications of estrogen therapy
- Thromboembolic disease
- Undiagnosed abnormal genital bleeding
- Potential for estrogen-dependent neoplasia
- Impaired liver function
- Possible pregnancy
Selective Estrogen Receptor Modulators (SERMs)
Tamoxifen, Toremifene
- competitive partial agonist inhibitors of estradiol
- antagonist on breast; agonist at other tissues
- Tx of ER+ breast cancer
Raloxifene
- antagonist on endometrium and breast; agonist on lipids and bone
- Prevent osteoporosis and breast cancer
Aromatase inhibitors
Anastrazole, Letrozole, Exemestane
- inhibit aromatase function (can’t produce estrone or estradiole)
- Tx of breast cancer in postmenopausal women
- DO NOT GIVE TO FERTILE WOMEN
What do you NOT give to a fertile woman who has breast cancer?
Aromatase inhibitors (Anastrazole, Letrozole, Exemestane)
