Reproductive Pharm Flashcards
How does minoxidil work and what 2 conditions can it be used for?
Minoxidil is a direct arteriolar vasodilator (decreases afterload)
Used in:
1) androgenetic alopecia
2) severe refractory hypertension
Sildenafil, vardenafil, tadalafil are used in? What is their mechanism of action. List side effects and if their contraindications.
Sildenafil, vardenafil, tadalafil are used in erectile dysfunction. They inhibit PDE-5 which normally breaks down cCMP leading to more cCMP, smooth muscle relaxation in corpus cavernosum, increase blood flow, penile erection.
Side effects: headache, flushing, dyspepsia, cyanopsia (blue-tinted vision). Risk of life-threatening hypotension in patients taking nitrates (venodilators)
Contraindicated in ppl on nitrates b/c both can cause severe hypotension.
Tamsulosin can be used to treat BPH. What is its mech of action?
a1-antagonist that can inhibit smooth muscle contraction. It’s selective for a1A,D receptors (found on prostate) vs. vascular a1B receptors.
What is the mech of action of mifepristone (RU-486). What is it used for? What about side effects?
Mifepristone is a competitive inhibitor of progrestin at progesterone receptors that can be used to terminate early pregnancy. Used with misoprostol (PGE1 analog).
Side effects: Heavy bleeding, GI (N/V, anorexia), abdominal pain.
What do terbutaline and ritodrine do?
They’re b2-agonists that can relax the uterus; used to decrease contraction frequency in women during labor.
What is the mechanism of danazol? clinical use? toxicity?
Danazol is a synthetic androgen that acts as a partial agonist at androgen receptors. Danazol is used for endometriosis, hereditary angioedema (C1 esterase inhibitor deficiency)
Side effects: weight gain, edema, acne, hirsutism, masculinization decrease HDL levels, hepatotoxicity
Testosterone and methyltestosterone are androgen receptor agonists that can be used to treat hypogonadism, and promote development of 2nd sex characteristics, can stimulate anabolism to promote recovery after burn or injury. What are some toxicities associated with its use?
- masculinization in females
- decrease intratesticular testosterone in males by inhibiting release of LH (via negative feedback) –> gonadal atropy
- premature closing of epiphyseal plates by promoting Ca2+ deposition in bones
- increase LDL, decrease HDL
- leukopenia
- decrease spermatogenesis, male pattern baldness
What is the mech of action of finasteride?
Finasteride is an anti-androgen that inhibits 5a-reductase. 5a-reductase normally stimulates testosterone into DHT, which is more potent. Decrease DHT is useful in BPH (takes 6-12 months for improvement; but decrease prostate size/volume to improve bladder obstruction) and male pattern baldness.
What is the mech of action of flutamide?
Flutamide is an anti-androgen; it is a non-steroidal competitive inhibitor at androgen receptors. Used for prostate carcinoma (often used with leuprolide, a GnRH agonist).
Ketoconazole is an anti-fungal that can inhibit steroid synthesis (inhibits 17,20-desmolase) and spironolactone is a K+ sparring diuretic that can also inhibit steroid binding (inhibits 17a-hydroxylase and 17,20-desmolase). They are both used to treat? Both have symptoms of?
Ketoconazole and spironolactone are used to treat polycystic ovarian syndrome to reduce androgenic symptoms. Both have side effects of gynecomastia and amenorrhea.
What is leuprolide/goserelin? What is it used for? Toxicity?
Leuprolide is a GnRH analog that has agonist properties when given pulsatile fashion and antagonist properties when given continuous (downregulates GnRH receptors in pituitary –> decrease LH and FSH).
Clinical uses:
pulsatile: infertility
continuous: prostate cancer (+flutamide -a competitive inhibitor at androgen receptors), uterine fibroids, precocious puberty.
Side effects: anti-androgen, N/V
Estrogens (ethinyl estradiol, DES, mestranol) bind estrogen receptors that can be used in hypogonadism or ovarian failure, menstural abnormalities, hormone replacement therapy in post-menopausal women, use in men w/ androgen-dependent prostate cancer. What are some toxicities associated with estrogen use?
- increase risk of endometrial cancer
- bleeding in postmenopausal women
- clear cell adenocarcinoma of vagina in females exposed to DES in utero
- increase risk of thrombi
contraindicated in ER + breast cancer, history of DVTs
Clomiphene is a selective estrogen modulator that works as an antagonist at estrogen receptors in hypothalamus. What does it do? side effects?
Clomiphene is an antagonist at estrogen receptors in hypothalamus and will prevent normal feedback inhibition and increase release of LH and FSH from pituitary to stimulate ovulation.
Clomiphene is used to treat infertility due to anovulation (e.g. PCOS).
side effects: hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances.
Tamoxifen is a SERM that is antagonist at ______, agonists at ______ and ________ with increased risk of __________ and _______. used to treat and prevent recurrence of ER/PR + breast cancer.
Tamoxifen is antagonist at breasts; and agonists at bones and uterus. Increase risk of thromboembolic events and endometrial carcinoma.
Raloxifene is a SERM that is antagonists at ______ and ______, and agonist at _______ with increased risk of _______, but not _________. Used primarily to treat osteoporosis.
Raloxifene is a SERM that is antagonist at breasts and uterus, and agonist at bones with increased risk of thromboembolic events but not endometrial carcinoma.
