Repro Pharm from FA Flashcards
(27 cards)
Leuprolide
Mechanism?
GnRH analog with agonist properties when used in pulsatile fashion
Antagonist properties when used in continuous fashion (downregs GnRH receptor in pituitary -> decrease in FSH/LH)
Leuprolide
Clinical Use? (4)
Infertility (pulsatile)
Prostate cancer (continuous - use with flutamide*)
Uterine fibroids (continuous)
Precocious puberty (continuous)
“Leuprolide can be used in LIEU of GnRH”
*flutamide = anti-androgen, competes with Test and DHT for receptors, used w prostate cancer
Leuprolide
Tox?
Antiandrogen, nausea, vomiting
Estrogens (ethinyl estradiol, DES, mestranol)
Mechanism?
Bind estrogen receptors
Estrogens (ethinyl estradiol, DES, mestranol)
Clinical Use? (for women and men)
Women: hypogonadism or ovarian failure, menstrual abnormalities, HRT in post-menopausal women
Men: androgen-dependent prostate cancer
Estrogens (ethinyl estradiol, DES, mestranol)
Tox? Contraindications?
- Incr risk of endometrial cancer, bleeding in post-menopausal women, incr risk of thrombi.
- Females exposed to DES in utero: clear cell adenocarcinoma of vagina
- Contra: ER+ breast cancer, history of DVTs
Selective Estrogen Receptor Modulators (SERMs)
name three?
Clomiphene
Tamoxifen
Raloxifene
Clomiphene
Class? Mech? Clinical use? Tox?
Class: SERM
Mech: antagonist at estrogen receptor in hypothalamus. Prevents normal feedback inhibition -> increases release of LH and FSH from pituitary -> stimulates ovulation.
Use: infertility treatment due to anovulation (ie PCOS).
Tox: hot flashes, ovarian enlargement, mult simultaneous pregnancies, visual disturbances
Tamoxifen
Class? Mech? Clinical use? Tox?
Class: SERM
Mech: antagonist on breast tissue; agonist at uterus and bone
Use: treatment (and recurrence prevention) of ER+ breast cancer
Tox: Associated with endometrial cancer and thromboembolisms
Raloxifene
Class? Mech? Clinical use? Tox?
Class: SERM
Use: osteoporosis treatment
Mech: decreases resorption of bone. Agonist at bone, antagonist at uterus.
Tox: increased risk of thromboembolic events
Hormone Replacement Therapy
Use (2)? Tox? Mech?
Use: –relief/prevention of menopausal symptoms (hot flashes, vaginal atrophy)
-Prev/treatment of osteoporosis
Mech (specific to osteoporosis? FA sucks): increases estrogen, decr osteoclast activity
Tox: unopposed estrogen replacement therapy increases the risk of endometrial cancer: progesterone therefore added. Possible increased CV risk
Anastrozole/Exemestane
Mech? Use?
Use: used in postmenopausal women with breast cancer
Mech: Aromatase inhibitors
Progestins
Use? Mech?
Use: in oral contraceptives, treatment of endometrial cancer and abnormal uterine bleeding
Mech: bind progesterone receptors, decrease growth and increase vascularization of endometrium
Mifepristone (RU-486)
Use? Mech? Tox?
Use: pregnancy termination. Used with misoprostol (PGE1)
Mech: Competes with progestins at progesterone receptors
Tox: Heavy bleeding, GI effects (N/V/anorexia), abd pain
Oral contraceptives (synthetic progestins, estrogens)
Mech? Contra?
Estrogens and progestins inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge -> no LH surge -> no ovulation
Contraindication: smokers > 35y (increased risk of CV events), pts with hx of thromboembolism and stroke, pts with hx of estrogen-dependent tumor
Oral contraceptives – qualities of the progestin component
Progestins cause thickening of the cervical mucus, thereby limiting access of sperm to uterus. Progestins also inhibit endometrial proliferation -> endometrium less suitable for the implantation of an embryo.
Terbutaline
Use? Mech?
Decrease the frequency of contractions during labor
Mech: B2 agonist -> relaxes the uterus
Danazol
Use? Mech? Tox?
Use: for endometriosis and hereditary angioedema
Mech: synthetic androgen; acts as partial agonist at androgen receptors
Tox: Wt gain, edema, acna, hirsutism, masculinazation, decr HDL levels, hepatotoxic.
Testosterone, methyltestosterone
Mech? Use? Tox?
Mech: Agonist at androgen receptors
Use: treats hypogonadism; promotes development of secondary sex characteristics; stimulates anabolism to promote recovery after burn or injury
Tox: Females -> masculinization
Males: decreases intratesticular testosterone by inhibiting release of LH (via neg feedback) -> gonadal atrophy. Premature closure of epiphyseal plates. Increases LDL, decreases HDL.
Antiandrogens
name 4?
relevant mechanism?
- Finasteride
- Flutamide
- Ketoconazole
- Spironolactone
Remember that 5a-reductase converts testosterone to DHT (more potent).
Finasteride
Mech? Use?
Inhibits 5a-reductase.
Use: BPH, also promotes hair growth (used in male-pattern baldness)
Flutamide
Mech? Use?
Nonsteroidal competitive inhibitor of androgens at the testosterone receptor
Use: prostate carcinoma
Ketoconazole
Use? Mech? Tox?
Treats hirsutism of PCOS
Inhibits steroid synthesis (inhibits 17,20 desmolase)
Tox: amenorrhea, gynecomastia
“To prevent male pattern hair loss, give a drug that will encourage female breast growth”
Spironolactone
Use? Mech?
Treats hirsutism of PCOS
Inhibits steroid binding, 17a-hydroxylase, and 17,20 desmolase
Tox: amenorrhea, gynecomastia
“To prevent male pattern hair loss, give a drug that will encourage female breast growth”
