Repro Drugs Flashcards
Leuprolide
-GnRH analog with agonist properties when used in pulsatile fashion / antagonist when used continuously
Use: uterine fibroids, endometriosis, precocious puberty, prostate cx,infertility, breast cancer/androgen excess
Adverse: hypogonadism, decreased libido, ED, nausea vomiting, edema, depression, decreased bone density when >6 months
Ethinyl estradiol, DES, mestranol
-bind estrogen receptors
-hypogonadism or ovarian failure, menstrual abnormalities, hormone replacement therapy
Adverse: increase risk of endometrial cx, bleeding in postmenopausal, clear cell adenocarcinoma in vagina, increased clot risk, lipid effects (increase TG, cholesterol)
Clomiphene
Selective estrogen receptor modulator
- antagonist at estrogen receptor in hypothalamus
- prevents LH and FSH from pituitary, stimulates ovulation
- used to treat infertility due to anovulation
- may cause hot flashes, ovarian enlargement, visual disturbances, pituitary tumor
Tamoxifen
Selective estrogen receptor modulator
- antagonist at breast, agonist at bone
- increase risk of thromboembolic events and endometrial cancer
- used to treat and prevent recurrence of ER/PR positive breast cancer
Raloxifene
Selective estrogen receptor modulators
- antagonist at breast, uterus, agonist at bone
- increased risk of thromboembolic event but NOT cancer
- used to treat osteoporosis
Anastrozole, letrozole, exemestane
Aromatase inhibitors
- inhibit peripheral conversion of androgens to estrogen
- use: ER positive breast cancer in postmenopausal women
Hormone replacement therapy
- use: relief of menopausal symptoms, osteoporosis
- unopposed estrogen therapy increases risk for endometrial cancer, progesterone/progestin is added.
- possible increased CV risk
Levonorgestrel, medroxyprogesterone, etonogestrel, norethindrone, megestrol
Progestins
- bind progesterone receptors, decrease growth and increase vascularization of endometrium, thicken cervical mucus
- use: contraception, endometrial cancer, abnormal uterine bleeding,
Mifepristone, ulipristal
Anti progestins
- competitive inhibitors of progestins at progesterone receptors
- use: termination of pregnancy (mifepristone with misoprostal), emergency contraceptive (ulipristal)
Combined contraceptives
- progestin and ethinyl estradiol
- estrogen and progestin inhibit FSH/LH and prevent estrogen surge, no ovulation
- progestin=thickening of cervical mucus, limit access of sperm to uterus and endometrial proliferation is inhibited, thinner and less viable
- contraindications: smokers, pts with CV disease, migraines, breast cancer and liver disease
Copper IUD
- produces local inflammation rxn toxic to sperm and ova, preventing fertilization and implantation, no hormones
- use: long acting reversible contraception, most effective emergency contraception
- adverse: heavier, longer menses, dysmenorrhea, risk of PID with insertion
Tocolytics
Meds that relax the uterus
Terbutaline
-B2 agonist
Used to slow contraction frequency in labor and prolong time to delivery
Adverse: dizziness, drowsiness, breathing probs, irregular heartbeat, maternal hyperglycemia, pulmonary edema, hypotension, tachycardia
-Not for use for longer than 48-72 hours
Nifedipine
-Ca2+ channel blocker
-used to decrease contraction in preterm labor, peripheral vasodilator
Contraindicated: women with hypotension, caution with CHF, left sided failure
Indomethacin
NSAID
-used to slow contractions in preterm labor
Danazol
-synthetic androgen that acts as partial agonist at androgen receptors
Use: endometriosis, hereditary angioedema
Adverse: weight gain, edema, acne, hirsutism, masculinization, lower HDL levels, hepatotoxic, pseudotumor cerebri
Testosterone, methyltestosterone
-agonists at androgen receptors
Use: treat hypogonadism, promote development of 2ndary sex characteristics, stimulate anabolism to promote recovery after burn/injury, stimulate RBC production in anemias, promote weight gain in wasting pts (AIDS)
Adverse: masculization of females, decrease intratesticular T in males by inhibiting LH release, high LDL, low HDL, cholestatic jaundice, elevated liver enzymes, hepatocellular carcinoma
Finasteride
5alpha reductase inhibitor
-decreases conversion of testosterone to DHT
Use: BPH and male pattern baldness, female hirsutism
Adverse: orthostatic hypotension, dizziness, decreased libido, fatigue, jaundice
-caution with liver pts, should be avoided in pregnancy (RF X)
Flutamide
Nonsteroidal competitive inhibitor at androgen receptors
Use: prostate carcinoma, androgen excess
Adverse: hot flashes, decreased libido, diarrhea, vomiting
-liver function should be monitored
Ketoconazole
-inhibits steroid synthesis (inhibits 17,20 desmolase/17alpha hydroxylase)
Use: PCOS to reduce androgenic symptoms, steroid responsive metastatic prostate cancer
Adverse: gynecomastia and amenorrhea, orthostatic hypotension, dizziness, fatigue, jaundice, vomiting
-rarely causes reversible hepatotoxicity, may cause prolong QT interval, inhibits cortisol synthesis
Spironolactone
Inhibits steroid binding, 17,20 desmolase/17alpha hydroxylase
Use: PCOS to reduce androgenic symptoms
Adverse: gynecomastia and amenorrhea, rarely polyuria, gastritis, fatigue, potential to cause hyperkalemia
Tamsulosin
Alpha-1antagonist
Use: treat BPH by inhibiting smooth muscle contraction
-selective for alpha 1A/d vs vascular alpha 1B
Sildenafil, vardenafil, tadalafil
Inhibit phophodiesterase type 5
-increase cGMP, prolong smooth muscle relaxation in response to NO, increase blood flow in corpus cavernosum of penis, decrease pulmonary vascular resistance
Use: ED, pulmonary hypertension, BPH
Adverse: headache, flushing, dyspepsia, cyanopia, hypotension in pts taking nitrates
Minoxidil
-direct arteriolar vasodilator
Use: androgenetic alopecia, severe refractory hypertension
