Reproductive- Pharmacology Flashcards
Control of reproductive hormones
Pag. 636
Leuprolide
- Mechanism
- Clinical use
- Adverse effects
GnRH analog
- agonist when pulsatile fashion;
- antagonist when used in continuous
Uterine fibroids, endometriosis, precocious puberty, prostate cancer, infertility
Hypogonadism, decrease libido, erectile dysfunction,
nausea, vomiting.
Estrogens
- Names
- Clinical use
Ethinyl estradiol, DES, mestranol.
Hypogonadism or ovarian failure, menstrual abnormalities (combined OCPs), hormone
replacement therapy in postmenopausal women
Estrogens
- Adverse effects
- Contraindications
risk of endometrial cancer (when given without progesterone), bleeding in postmenopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, risk of thrombi
ER ⊕ breast cancer, history of DVTs, tobacco use in women > 35 years old.
Selective estrogen receptor modulators (SERMs)
Clomiphene, Tamoxifen, Raloxifen
Clomiphene
- Mechanism
- Clinical use
- Adverse effects
Antagonist at estrogen receptors in hypothalamus.
Used to treat infertility due to anovulation (eg, PCOS).
SERMs may cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visua disturbances.
Tamoxifen
- Mechanism
- Clinical use
- Adverse effects
Antagonist at breast; agonist at bone, uterus;
Used to treat and prevent recurrence of ER/PR ⊕ breast cancer.
Risk of thromboembolic events and endometrial
cancer.
Raloxifen
- Mechanism
- Clinical use
- Adverse effects
Antagonist at breast, uterus; agonist at bone;
Used primarily to treat osteoporosis.
Risk of thromboembolic events but no increased risk
of endometrial cancer (vs tamoxifen)
Aromatase inhibitors
- Names
- Mechanism
- Clinical use
Anastrozole, letrozole, exemestane
Inhibit peripheral conversion of androgens to estrogen
ER ⊕ breast cancer in postmenopausal women.
Hormone replacement therapy
Used for relief or prevention of menopausal symptoms,
osteoporosis.
Unopposed estrogen replacement therapy risk of endometrial cancer, progesterone/progestin is added. Possible increased cardiovascular risk.
Progestins
- Names
- Mechanism
Levonorgestrel, medroxyprogesterone, etonogestrel, norethindrone, megestrol
Bind progesterone receptors, decrease growth and increase vascularization of endometrium, thicken cervical mucus
Progestins
- Clinical use
Contraception, endometrial cancer, abnormal uterine bleeding.
Progestin challenge: presence of withdrawal bleeding
excludes anatomic defects (eg, Asherman syndrome) and chronic anovulation without estrogen
Antiprogestins
- Names
- Mechanism
- Clinical use
Mifepristone, ulipristal.
Competitive inhibitors of progestins at progesterone receptors.
Termination of pregnancy (mifepristone with misoprostol); emergency contraception (ulipristal).
Combined contraception
- Combination
- Mechanism
- Contraindications
Progestins and ethinyl estradiol
Inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge no LH surge no ovulation.
smokers > 35 years old, risk of cardiovascular disease, migraine, breast cancer, liver disease
Copper intrauterine device
- Mechanism
- Clinical use
- Adverse effects
Produces local inflammatory reaction toxic to sperm and ova
Long-acting reversible contraception. Most effective emergency contraception
Heavier or longer menses, dysmenorrhea. Risk of PID with insertion