Reproductive Drugs

Front 1

Anti-androgens: drugs?

Back 1

Finasteride, flutamide, ketoconazole, spironolactone

Front 2

Finasteride: mechanism, use

Back 2

M: 5-alpha reductase inhibitor --> inhibits conversion of testosterone to DHT (which is more potent)

U: BPH, male pattern baldness

Front 3

Flutamide: mechanism, use

Back 3

M: non-steroidal competitive inhibitor of androgens at the testosterone receptor

U: prostate carcinoma

Front 4

Ketoconazole: mechanism, use, toxicity

Back 4

M: inhibits steroid synthesis

U: prevent hirsutism in polycystic ovarian syndrome

T: gynecomastia, amenorrhea

Front 5

Spironolactone: mechanism, use toxicity

Back 5

M: inhibits steroid binding

U: prevent hirsutism in polycystic ovarian syndrome

T: gynecomastia, amenorrhea

Front 6

Leuprolide: mechanism, use, toxicity

Back 6

M: GnRH analog - agonist properties (pulsatile dosing), antagonist properties (continuous dosing)

U: infertility (pulsatile), prostate cancer (continuous - use with flutamide), uterine fibrosis

T: anti-androgen, nausea, vomiting

Front 7

Sildenafil, vardenafil: mechanism, use, toxicity

Back 7

M: inhibit cGMP phosphodiesterase --> increases cGMP --> smooth muscle relaxation, increased blood flow, penile erection

U: erectile dysfunction

T: headache, flushing, dyspepsia, impaired blue-green color vision, life-threatening hypotension (when used with nitrates)

Front 8

Mifepristone (RU-486): mechanism, use, toxicity

Back 8

M: competitive inhibitor of progestins at progesterone receptors

U: termination of pregnancy (given with misoprostol)

T: heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain

Front 9

Oral contraception (synthetic progestins, estrogen): mechanism, advantages, disadvantages

Back 9

M: prevent estrogen surge and LH surge --> ovulation does not occur

A: reliable (<1% failure), decrease risk of endometrial + ovarian cancer, decrease incidence of ectopic pregnancy, decrease pelvic infection, regulation of menses

D: taken daily, no protection against STDs, increased TG, depression, weight gain, nausea, HTN, hypercoagulable states

Front 10

Hormone replacement therapy: mechanism, use, toxicity

Back 10

M: increase estrogen levels

U: relief or prevention of menopausal symptoms and osteoporosis

T: increased risk of endometrial cancer (progesterone can be added), increased CV risk

Front 11

Dinoprostone: mechanism, use

Back 11

M: PGE2 analog --> cervical dilation + uterine contraction

U: induce labor

Front 12

Ritodrine, terbutaline: mechanism, use

Back 12

M: beta-2 agonists --> relax uterus

U: reduce premature uterine contractions

Front 13

Anastrozole, exemestane: mechanism, use

Back 13

M: aromatase inhibitors

U: used in postmenopausal women with breast cancer

Front 14

Testosterone (methyltestosterone): mechanism, use, toxicity

Back 14

M: agonist at androgen receptors, stimulation anabolism

U: hypogonadism, promote secondary sex characteristics, promote recovery after burn or injury, ER-positive breast cancer (exemestane)

T: masculinization in females, reduces intratesticular testosterone in males by inhibiting Leydig cells, gonadal atrophy, premature closing of epiphyseal plates; increases LDL, decreases HDL

Front 15

Estrogens (ethinyl estradiol, DES, mestranol): mechanism, use, toxicity, contraindications

Back 15

M: bind estrogen receptors

U: hypogonadism, ovarian failure, menstrual abnormalities, HRT in post-menopausal women, men with androgen-dependent prostate cancer

T: increased risk of endometrial cancer, bleeding in post-menopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, increase risk of thrombi

Contraindications: ER-positive breast cancer

Front 16

Progestins: mechanism, use

Back 16

M: bind progesterone receptors, reduce growth, increase vascularization of endometrium

U: used in oral contraceptives, endometrial cancer, abnormal uterine bleeding

Front 17

Clomiphene: mechanism, use, toxicity

Back 17

M: partial agonist at estrogen receptors in hypothalamus; prevents normal feedback inhibition; increases release of LH and FSH from pituitary --> stimulates ovulation
U: infertility, polycystic ovarian syndrome
T: hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances

Front 18

Tamoxifen: mechanism, use

Back 18

M: partial estrogen agonist; antagonist on breast tissue

T: prevent recurrence of ER-positive breast cancer

Front 19

Raloxifene: mechanism, use

Back 19

M: partial estrogen agonist in bone --> reduces resorption of bone

U: osteoporosis