Reproductive Pharmacology

Question 1

GnRH analog with agonist properties when used in a pulsatile fashion; antagonist properties when used in continuous fashion (downregulates GnRH receptor in pituitary, leading to decreased FSH, LH)

Answer 1

Leuprolide

Question 2

Give __________ in pulsatile doses for infertility

Answer 2

Leuprolide

Question 3

Give __________ in continuous dose for prostate cancer or precocious puberty

Answer 3

Leuprolide

Question 4

Toxicity - Antiandrogen, nausea, vomiting

Answer 4

Leuprolide

Question 5

Agonist at androgen receptors

Answer 5

Testosterone, Methyltestosterone

Question 6

Use this to treat hypogonadism and promote development of secondary sex characteristics in males; stimulation of anabolism to promote recovery after burn or injury

Answer 6

Testosterone, Methyltestosterone

Question 7

Toxicity - Can cause masculinization in females, reduces intratesticular testosterone in males by inhibiting the release of LH (via negative feedback), leading to gonadal atrophy; premature fusion of epiphyseal plates, increased LDL, decreased HDL

Answer 7

Testosterone, Methyltestosterone

Question 8

A 5-alpha-reductase inhibitor. Useful in BPH. Also promotes hair growth - used to treat male pattern baldness

Answer 8

Finasteride

Note that 5-alpha-reductase converts testosterone into DHT (more potent)

Question 9

A nonsteroidal competitive inhibitor of androgens at the testosterone receptor. Used in prostate carcinoma.

Answer 9

Flutamide

Question 10

Inhibits steroid synthesis (inhibits 17, 20 desmolase)

Answer 10

Ketoconazole

Question 11

Inhibits steroid binding

Answer 11

Spirnolactone

Question 12

Can be used in PCOS to prevent hirsutism

Answer 12

Spirnolactone, Ketoconazole

Question 13

Side effects of gynecomastia and amenorrhea

Answer 13

Spirnolactone, Ketoconazole

Question 14

Bind estrogen receptors

Answer 14

Ethinyl estradiol, DES, mestranol

Question 15

Use this for hypogonadism in females or ovarian failure, menstrual abnormalities, HRT in postemenopausal women, use in men with androgen-dependent prostate cancer.

Answer 15

Ethinyl estradiol, DES, mestranol

Question 16

Toxicity - Increased risk for endometrial cancer, bleeding in postmenopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, increased risk of thrombi

Answer 16

Ethinyl estradiol, DES, mestranol

Question 17

Toxicity - Contraindicated for ER positive breast cancer, history of DVTs

Answer 17

Ethinyl estradiol, DES, mestranol

Question 18

Partial agonist (inhibits) at estrogen receptors in the hypothalamus. Prevents normal feedback inhibition and increases release of LH and FSH from the pituitary, which stimulates ovulation. Used to treat infertility and PCOS. May cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, and visual disturbances

Answer 18

Clomiphene

Question 19

Do NOT use this for hypothalamic amenorrhea

Answer 19

Clomiphene (there is already low estrogen in the system)

Question 20

Antagonist on breast tissue, used to treat and prevent recurrence of ER-positive breast cancer

Agonist on endometrium

Answer 20

Tamoxifen

Question 21

Give this medication for lobular carcinoma in situ

Answer 21

Tamoxifen

Question 22

Agonist at bone, reduces resorption of bone, used to treat osteoporosis

Answer 22

Raloxifene

Question 23

Unopposed estrogen replacement therapy increases the risk of endometrial cancer, so __________ is added.

Answer 23

Progesterone

Question 24

Aromatase inhibitors used in postmenopausal women with breast cancer

Answer 24

Anastrozole, exemestane

Question 25

Bind progesterone receptors, reduce growth and increase vascularization of endometrium. Used in the treatment of endometrial cancer and abnormal uterine bleeding.

Answer 25

Progestins

Question 26

Competitive inhibitor of progestins at the progesterone receptor in uterus. Used for termination of pregnancy. Administered with misoprostol (PGE)

Answer 26

RU-486, Mifepristone TX - Heavy bleeding, GI effects, abdominal pain

Question 27

Contraindications for OCP

Answer 27

Smokers > 35 years of age, migraines, pregnancy, uncontrolled HTN, history of thromboembolism/stroke or estrogen-dependent tumor

Question 28

Alpha-1 antagonist used to treat BPH by inhibiting smooth muscle contraction in the prostate. Selective for alpha1A,D receptors (found on prostate) vs. vascular alpha1B receptors

Answer 28

Tamsulosin

Question 29

Inhibit PDE5, causing increase in cGMP, smooth muscle relaxation in the corpus cavernosum, increase blood flow and penile erection

Answer 29

Sildenafil, vardenafil

Question 30

Toxicity - headache, flushing, dyspepsia, impaired blue-green color vision. Risk of life-threatening hypotension in patients taking nitrates.

Answer 30

Sildenafil, vardenafil

Question 31

Synthetic androgen that acts as a partial agonist at androgen receptors. Used for endometriosis and hereditary angioedema.

Answer 31

Danazol interesting...male sex hormones (androgens), which increase production of C1-INH in the liver through an as yet unknown mechanism. Danazol is the most commonly used

Question 32

Toxicity - weight fain, edema, acne, hirsutism, masculinization, decreased HDL, hepatotoxic

Answer 32

Danazol