Repro

Question 1

Leuprolide

MOA

Answer 1

GnRH analog
Pulsatile - agonist
Continuous - antagonist

Question 2

Leuprolide

Clinical use

Answer 2

Infertility (pulsatile)
Prostate cancer, uterine fibroids (continuous)
Precocious puberty (continuous)

Question 3

Estrogens (Ethinyl estradiol, DES, mestranol)

Clinical use

Answer 3

Binds estrogen receptors.

For hypogonadism, ovarial failure, menses abnormalities, HRT.

Question 4

Estrogens

Toxicity

Answer 4

Inc. risk Endometrial cancer.
Bleeding in postmenopause.
CI in ER-positive breast cancer, hx of DVT.

Question 5

Clomiphene

[MOA, clinical use]

Answer 5

SERM – Estrogen receptor antagonist at hypothalamus.
Prevents feedback inhibition – inc. LH/FSH – ovulation.
For infertility (anovulation).

Question 6

Tamoxifen

[MOA, clinical use, toxicity]

Answer 6

SERM: Antagonist at breast; agonist at bone, uterus.
Treat and prevent recurrence of ER/PR-positive breast cancer.
Tox: inc. risk of thromboembolism, endometrial cancer.

Question 7

Raloxifene

[MOA, clinical use]

Answer 7

SERM: Antagonist at breast, uterus; agonist at bone.
Treat osteoporosis.
Inc. risk of thromboembolism.

Question 8

Hormone replacement therapy.
For what?
Estrogen? Progesterone?

Answer 8

For menopausal sx, osteoporosis.

Unopposed estrogen inc. risk of endometrial cancer – add progesterone (estrogen + progesterone).

Question 9

Progestins

[MOA, clinical use]

Answer 9

Bind progesterone receptors. Used in OCPs.
Dec. growth and inc. endometrial vascularization.
For endometrial cancer, abnormal uterine bleeding.

Question 10

Oral contraception

MOA

Answer 10

Estrogen + progestin.
Inhibit LH/FSH – no estrogen surge – no LH surge – no ovulation.
> Progestins: thick cervical mucus, limits sperm access to uterus; inhibit endometrial proliferation, so harder to implant.

Question 11

Oral contraception

Contraindications

Answer 11

Smokers > 35 y.o
Hx of thromboembolism, stoke
Hx. of estrogen-dependent tumor

Question 12

Terbutaline, Ritodrine

Clinical use

Answer 12

B2-agonists
Relax the uterus.
To dec. contraction frequency in labor.

Question 13

Testosterone

Clinical use

Answer 13

Androgen receptor agonist.

For hypogonadism; to develop secondary sex chars.

Question 14

Testosterone

Toxicity

Answer 14

Masculinization in females.
Gonadal atrophy in males (inhibits LH release) – dec. intratesticular testosterone.
Premature closure of epiphyseal plates.

Question 15

Finasteride

[MOA, use]

Answer 15

Antiandrogen; 5a-reductase inhibitor (testosterone –> DHT).

For BPH, male-pattern baldness.

Question 16

Flutamide

[MOA, use]

Answer 16

Antiandrogen; Nonsteroidal competitive androgen receptor inhibitor.
For prostate CA.

Question 17

Ketoconazole

[MOA, use, SE]

Answer 17

Antiandrogen.
Inhibits 17,20-desmolase (cholesterol – androgen) – Inhibits steroid synthesis.
For polycystic ovarian syndrome – reduce androgenic sx.
SE: gynecomastia, amenorrhea

Question 18

Spironolactone

[MOA, use, SE]

Answer 18

Antiandrogen.
Inhibits steroid binding, 17a-hydroxylase, 17,20-desmolase.
For polycystic ovarian syndrome.
SE: gynecomastia, amenorrhea

Question 19

Tamsulosin

[MOA, use]

Answer 19

a1-antagonist (alpha1A,D receptors in prostate).
Inhibit smooth muscle contraction, for BPH.
Treat BPH

Question 20

Sildenafil, Vardenafil, Tadalafil

[MOA, clinical use]

Answer 20

Inhibit PDE-5 – inc. cGMP – smooth muscle relaxation in corpus cavernosum, inc. blood flow – penile erection.
For erectile dysfunction.

Question 21

Sildenafil, Vardenafil, Tadalafil

Toxicity

Answer 21

Life-threatening Hypotension in pts taking nitrates.

Headache, heartburn

Question 22

Anastrozole/Exemestane

[MOA, use]

Answer 22

Aromatase inhibitors.
Used in postmenopausal women w/ ER-positive breast cancer.
*Source of estrogen after menopause becomes peripheral conversion of androgens.

Question 23

Danazol

[MOA, use]

Answer 23

> Partial agonist at androgen receptors – induces a state of pseudomenopause by suppressing ovarian fxn and inhibits FSH/LH secretion, causing endometrial atrophy.
For endometriosis, hereditary angioedema.

Question 24

Mifepristone (RU-486)

[MOA, use]

Answer 24

Competitive inhibitor of pregestins at progesterone receptor.
Termination of pregnancy.
*Administer w/ misoprostol (PGE1)