Reproductive Flashcards
Leuprolide
GnRH analog.
Agonist properties (pulsatile) or antagonist properties (continuous) - downregulates GnRH receptor in pituitary, decreases FSH/LH release.
Infertility (agonist), prostate cancer (continuous, use w/ flutamide), uterine fibroids (continuous), precocious puberty (continuous).
Anti-androgen side effects, nausea, vomiting.
Ethinyl estradiol
Estrogen.
Binds estrogen receptors.
Hypogonadism/ovarian failure, menstrual abnormalities, HRT in post-menopausal women women, men with androgen-dependent prostate cancer.
Increased risk of endometrial cancer, bleeding (post-menopausal women), increased risk of thrombi.
Do not use in ER+ breast cancer or in patients with history of DVTs.
Diethylstilbestrol (DES)
Estrogen.
Binds estrogen receptors.
Hypogonadism/ovarian failure, menstrual abnormalities, HRT in post-menopausal women women, men with androgen-dependent prostate cancer.
Vaginal clear cell carcinoma in females exposed in utero, increased risk of endometrial cancer, bleeding (post-menopausal women), increased risk of thrombi.
Do not use in ER+ breast cancer or in patients with history of DVTs.
Mestranol
Estrogen.
Binds estrogen receptors.
Hypogonadism/ovarian failure, menstrual abnormalities, HRT in post-menopausal women women, men with androgen-dependent prostate cancer.
Increased risk of endometrial cancer, bleeding (post-menopausal women), increased risk of thrombi.
Do not use in ER+ breast cancer or in patients with history of DVTs.
Clomiphene
Selective estrogen receptor modulator (SERM)
Antagonist at estrogen receptors in hypothalamus. Prevents normal feedback inhibition and increases release of LH and FSH from pituitary, which stimulates ovulation.
Infertility due to involution (e.g. PCOS)
Hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances.
Tamoxifen
Selective estrogen receptor modulator (SERM)
Antagonist on breast tissue. Agonist at uterus, bone.
Treatment and prevention of recurrence of ER+ breast cancer.
Associated with endometrial cancer, thromboembolic events.
Raloxifene
Agonist on bone, antagonist at uterus.
Osteoporosis.
Increased risk of thromboembolic events, decreased resorption of bone.
Hormone replacement therapy
Relief or prevention of menopausal symptoms (hot flashes, vaginal atrophy) and osteoporosis (increase estrogen, decrease osteoclast activity).
Unopposed estrogen replacement therapy (ERT) increases risk of endometrial cancer (must add progesterone). Increased cardiovascular risk.
Anastrozole
Aromatase inhibitor.
Post-menopausal women with breast cancer.
Exemestane
Aromatase inhibitor.
Post-menopausal women with breast cancer.
Progestin
Bind progesterone receptors, decrease growth and increase vascularization of endometrium.
Oral contraceptives, treatment of endometrial cancer and abnormal uterine bleeding.
Mifepristone (RU-486)
Competitive inhibitor of progestins at progesterone receptors.
Termination of pregnancy. Administered with misoprostol (PGE1).
Heavy bleeding, GI side effects (nausea, vomiting, anorexia), abdominal pain.
Oral contraception (synthetic progestins, estrogen)
Estrogens and progestin inhibit LH/FSH, preventing estrogen surge. No estrogen surge, no LH surge, no ovulation.
Progestins: Thickening of cervical mucus (limiting access of sperm to uterus), inhibit endometrial proliferation (less suitable for implantation).
Contraindicated in smokers >35 years old (increased risk of CV events), patients with history of thromboembolism, stroke, or history of estrogen-dependent tumor.
Terbutaline
β2 agonist
Relaxes uterus
Decreases contraction frequency in women during labor.
Danazol
Synthetic androgen.
Partial agonist at androgen receptors.
Endometriosis, hereditary angioedema.
Weight gain, edema, acne, hirsutism, masculinization, decreased HDL levels, hepatotoxicity.
Testosterone
Androgen.
Agonist at androgen receptors.
Hypogonadism, promotes development of secondary sex characteristics, stimulation of anabolism to promote recovery after burn or injury.
Masculinization in females, decreased intratesticular testosterone in males (inhibits LH release) leading to gonadal atrophy, premature closure of epiphyseal plates, increased LDL, decreased HDL.
Methyltestosterone
Androgen.
Agonist at androgen receptors.
Hypogonadism, promotes development of secondary sex characteristics, stimulation of anabolism to promote recovery after burn or injury.
Masculinization in females, decreased intratesticular testosterone in males (inhibits LH release) leading to gonadal atrophy, premature closure of epiphyseal plates, increased LDL, decreased HDL.
Finasteride
Anti-androgen.
5α-reductase inhibitor. Decreases conversion of testosterone to DHT.
BPH, male-pattern baldness (promotes hair growth).
Flutamide
Anti-androgen.
Non-steroidal competitive inhibitor of androgens at testosterone receptor.
Prostate carcinoma.
Ketoconazole
Anti-androgen.
Inhibits steroid synthesis via inhibition of 17,20-desmolase.
PCOS (with spironolactone).
Gynecomastia, amenorrhea.
Spironolactone
Anti-androgen.
Inhibits steroid binding, 17α-hydroxylase, and 17,20-desmolase.
PCOS (with ketoconazole).
Gynecomastia, amenorrhea.
Tamsulosin
α-1 agonist
Inhibits smooth muscle contraction. Selective for α-1A,D receptors (prostate) vs α-1B receptors (vasculature).
BPH
Sildenafil
Inhibits phosphodiesterase 5, increasing cGMP, smooth muscle relaxation in corpus cavernous, increased blood flow, and penile erection.
Erectile dysfunction
Headache, flushing, dyspepsia, impaired blue-green color vision. Risk of life-threatening hypotension in patients taking nitrates.
Vardenafil
Inhibits phosphodiesterase 5, increasing cGMP, smooth muscle relaxation in corpus cavernous, increased blood flow, and penile erection.
Erectile dysfunction
Headache, flushing, dyspepsia, impaired blue-green color vision. Risk of life-threatening hypotension in patients taking nitrates.
