Repro drugs

Question 1

Leuprolide

Answer 1

GnRH analog with agonist properties when used in pulsatile fashion. Antagonist when used continuously. Downregulates GnRH receptor in pituitary and decreases FSH and LH.

Used for prostate cancer, uterine fibroids, precocious puberty

Question 2

Leuprolide toxicity

Answer 2

Antiandrogen, N/V

Question 3

Estrogens

Answer 3

ethinyl estradiol, DES, mestranol.

Bind estrogen receptors. Used for hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women.

Question 4

Estrogen toxicity

Answer 4

Increased risk of endometrial cancer. Can cause clear cell carcinoma in babies exposed to DES. Increased risk of thrombi.

Don’t use in ER+ breast cancer or with history of DVT

Question 5

Clomiphene

Answer 5

A SERM. Antagonist at estrogen receptors in hypothalamus, so prevents normal feedback, increasing LH and FSH from pituitary which stimulates ovulation. Used to treat infertility due to PCOS and other anovulatory conditions.

Question 6

Clomiphene Toxicity

Answer 6

Hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances

Question 7

Tamoxifen

Answer 7

A SERM. Antagonist of estrogen at breast tissue. Agonist at uterus and bone.

Question 8

Tamoxifen Toxicity

Answer 8

Can increase risk of endometrial cancer and thromboembolism

Question 9

Raloxifene

Answer 9

A serm, agonist on bone, antagonist at uterus.

Question 10

Anastrozole/exemestane

Answer 10

Aromatase inhibitor used in postmenopausal women with breast cancer.

Question 11

Progestins

Answer 11

Bind progesterone receptors, decrease growth and increase vascularization of endometrium. Used as oral contraceptives and in the treatment of endometrial cancer and AUB.

Question 12

Mifepristone

Answer 12

An inhibitor of progestins at progesterone receptors. Used to terminate pregnancy, adminstered with misoprostol

Question 13

How does oral contraception work?

Answer 13

Estrogen and progestins inhibit LH and FH and therefore decrease estrogen surve. No LH surge and no ovulation.

Progestins cause thickening of cervial mucus and limit access of sperm.

Question 14

Contraindications for oral contraception

Answer 14

Smokers >35 years old – can cause cardiovascular events

patients with history of stroke

Question 15

Tertabuline

Answer 15

B2 agonist that is used to relax the uterus. Used to reduce contraction frequency in women during labot

Question 16

Danazol

Answer 16

Synthetic androgen that act as a partial agonist at androgen receptors. used for endometriosis and angioedema.

Question 17

Danazol toxicity

Answer 17

Weight gain, edema, acne, hirsuitism, masculinization, decreased HDL.

Question 18

Finasteride

Answer 18

5 alpha reductase inhibitor. used in BPH, also promotes hair growth. To prevent male pattern hair loss, give a drug that will encourage female breast growth

Question 19

Flutamide

Answer 19

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

Question 20

Ketoconazole/spironolactone

Answer 20

Inhibits testosterone synthesis. Given in PCOS to prevent hirsuitism. Can cause gynecomastia and amenorrhea

Question 21

Tamulosin

Answer 21

A1 agonist used to treat BPH by inhibiting smooth muscle contraction. Doesn’t affect vasculature.

Question 22

Sildenafil side effects

Answer 22

Headache, flushing, dyspepsia, impaired blue-green color vision. Risk of life threatening hypotension in patients wth nitrites.