Drugs for Reproductive Health Flashcards
how do leuprolide, goserelin, histrelin, nafarelin, and triptorelin work?
synthetic GnRH agonists that provide sustained/ non-pulsatile administration to inhibit pituitary release of FSH and LH
[recall pulsatile GnRH from the hypothalamus stimulates FSH and LH from anterior pituitary]
what are the clinical indications of leuprolide? (3)
synthetic GnRH agonist (inhibits FSH/LH release via continuous/non-pulsatile administration) used to treat:
- endometriosis
- uterine leiomyomata (fibroids)
- prostate cancer (1st line)
what adverse side effects are associated with GnRH agonists such as leuprolide, goserelin, histrelin, nafarelin, and triptorelin?
symptoms related to low estrogen —> hot flashes, decreased libido, reduced bone density, vaginal dryness (women), gynecomastia (men)
what are the clinical indications of follitropin and lutropin?
recombinant FSH and LH, respectively, used in combination to treat infertility in men and women
stimulate spermatogenesis in men and ovulation in women (who fail to respond to other treatments)
most commonly used for controlled ovarian hyperstimulation (COH) in assisted reproductive procedures like IVF
what drugs cause ovarian hyperstimulation syndrome (OHSS) and how does this present?
serious complication of therapy with follitropin and lutropin (recombinant FSH, LH) used to treat infertility
characterized by ovarian enlargement, ascites, hydrothorax, and hypovolemia
ethinyl estradiol vs levonorgestrel
both are components of oral contraceptives that suppress GnRH and subsequent FSH/LH release to prevent ovulation
ethinyl estradiol: estrogen used in combination estrogen-progestin contraceptives
levonorgestrel: progestin used in estrogen-progestin contraceptives
what are 4 serious adverse effects associated with oral contraceptives?
- venous thromboembolic disease (3x higher risk)
- myocardial infarction
- cerebrovascular disease (women over 35)
- depression
contrast the effects of tamoxifen and raloxifene
both are SERMs (selective estrogen receptor modulators)
tamoxifen: estrogen antagonist in breast, agonist in endometrium and bone
raloxifene: estrogen antagonist in breast and endometrium, agonist in bone
what are the clinical indications of tamoxifen vs raloxifene?
both are SERMs (selective estrogen receptor modulators)
tamoxifen: ER antagonist in breast tissue, used in advanced ER-positive breast cancer or chemoprevention of breast cancer in high-risk women
raloxifene: partial ER agonist in bone, used to prevent/treat osteoporosis in post-menopausal women
clomiphene vs fulvestrant
clomiphene: weak partial estrogen receptor agonist that acts as competitive inhibitor of endogenous estrogens —> relieves negative feedback in hypothalamus to increase release of GnRH, FSH, LH and stimulate follicle growth/ovulation
fulvestrant: pure estrogen receptor antagonist —> treats ER-positive breast cancer
what is the clinical indication for clomiphene?
weak partial estrogen receptor agonist that acts as competitive inhibitor of endogenous estrogens —> relieves negative feedback in hypothalamus to increase release of GnRH, FSH, LH and stimulate follicle growth/ovulation
used to treat anovulation in women with oligomenorrhea or amenorrhea and ovulatory dysfunction (must be treated repeatedly until pregnancy is achieved)
mechanism of anastrozole and letrozole vs exemestane
anastrozole and letrozole: non-steroidal competitive inhibitors of aromatase
exemestane: steroid molecule that covalently/irreversibly binds aromatase
[recall aromatase converts testosterone to estradiol]
what is the clinical indication of anastrozole, letrozole, and exemestane
aromatase inhibitor: prevent conversion of testosterone to estradiol
used to treat advanced ER-positive breast cancer in post-menopausal women
what kind of drugs are finasteride and dutasteride?
5-alpha reductase inhibitors: prevent conversion of testosterone to DHT (dihydrotestosterone)
used to treat benign prostatic hyperplasia (BPH)
continuous treatment with which of these agents can be used to treat endometriosis?
a. ethinyl estradiol
b. leuprolide
c. lutropin
d. clomiphene
e. letrozole
b. leuprolide: GnRH agonist —> reduces LH/FSH secretion (with continuous administration)
a. ethinyl estradiol: oral contraceptive
c. lutropin: recombinant LH
d. clomiphene: antiestrogen
e. letrozole: aromatase inhibitor
