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Flashcards in Repro Pharm from FA Deck (27):
1

Leuprolide

Mechanism?

GnRH analog with agonist properties when used in pulsatile fashion

Antagonist properties when used in continuous fashion (downregs GnRH receptor in pituitary -> decrease in FSH/LH)

2

Leuprolide

Clinical Use? (4)

Infertility (pulsatile)

Prostate cancer (continuous - use with flutamide*)

Uterine fibroids (continuous)

Precocious puberty (continuous)

"Leuprolide can be used in LIEU of GnRH"

*flutamide = anti-androgen, competes with Test and DHT for receptors, used w prostate cancer

3

Leuprolide

Tox?

Antiandrogen, nausea, vomiting

4

Estrogens (ethinyl estradiol, DES, mestranol)

Mechanism?

Bind estrogen receptors

5

Estrogens (ethinyl estradiol, DES, mestranol)

Clinical Use? (for women and men)

Women: hypogonadism or ovarian failure, menstrual abnormalities, HRT in post-menopausal women

Men: androgen-dependent prostate cancer

6

Estrogens (ethinyl estradiol, DES, mestranol)

Tox? Contraindications?

-Incr risk of endometrial cancer, bleeding in post-menopausal women, incr risk of thrombi.

-Females exposed to DES in utero: clear cell adenocarcinoma of vagina

-Contra: ER+ breast cancer, history of DVTs

7

Selective Estrogen Receptor Modulators (SERMs)

name three?

Clomiphene

Tamoxifen

Raloxifene

8

Clomiphene

Class? Mech? Clinical use? Tox?

Class: SERM

Mech: antagonist at estrogen receptor in hypothalamus. Prevents normal feedback inhibition -> increases release of LH and FSH from pituitary -> stimulates ovulation.

Use: infertility treatment due to anovulation (ie PCOS).

Tox: hot flashes, ovarian enlargement, mult simultaneous pregnancies, visual disturbances

9

Tamoxifen

Class? Mech? Clinical use? Tox?

Class: SERM

Mech: antagonist on breast tissue; agonist at uterus and bone

Use: treatment (and recurrence prevention) of ER+ breast cancer

Tox: Associated with endometrial cancer and thromboembolisms

10

Raloxifene

Class? Mech? Clinical use? Tox?

Class: SERM

Use: osteoporosis treatment

Mech: decreases resorption of bone. Agonist at bone, antagonist at uterus. 

Tox: increased risk of thromboembolic events

 

11

Hormone Replacement Therapy

Use (2)? Tox? Mech?

Use: --relief/prevention of menopausal symptoms (hot flashes, vaginal atrophy)

-Prev/treatment of osteoporosis

Mech (specific to osteoporosis? FA sucks): increases estrogen, decr osteoclast activity

Tox: unopposed estrogen replacement therapy increases the risk of endometrial cancer: progesterone therefore added. Possible increased CV risk

12

Anastrozole/Exemestane

Mech? Use?

Use: used in postmenopausal women with breast cancer

Mech: Aromatase inhibitors

13

Progestins

Use? Mech?

Use: in oral contraceptives, treatment of endometrial cancer and abnormal uterine bleeding

Mech: bind progesterone receptors, decrease growth and increase vascularization of endometrium

14

Mifepristone (RU-486)

Use? Mech? Tox?

Use: pregnancy termination. Used with misoprostol (PGE1)

Mech: Competes with progestins at progesterone receptors

Tox: Heavy bleeding, GI effects (N/V/anorexia), abd pain

15

Oral contraceptives (synthetic progestins, estrogens)

Mech? Contra?

Estrogens and progestins inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge -> no LH surge -> no ovulation

Contraindication: smokers > 35y (increased risk of CV events), pts with hx of thromboembolism and stroke, pts with hx of estrogen-dependent tumor

16

Oral contraceptives -- qualities of the progestin component

Progestins cause thickening of the cervical mucus, thereby limiting access of sperm to uterus. Progestins also inhibit endometrial proliferation -> endometrium less suitable for the implantation of an embryo.

17

Terbutaline

Use? Mech?

Decrease the frequency of contractions during labor

Mech: B2 agonist -> relaxes the uterus

18

Danazol

Use? Mech? Tox?

Use: for endometriosis and hereditary angioedema

Mech: synthetic androgen; acts as partial agonist at androgen receptors

Tox: Wt gain, edema, acna, hirsutism, masculinazation, decr HDL levels, hepatotoxic.

19

Testosterone, methyltestosterone

Mech? Use? Tox?

Mech: Agonist at androgen receptors

Use: treats hypogonadism; promotes development of secondary sex characteristics; stimulates anabolism to promote recovery after burn or injury

Tox: Females -> masculinization

Males: decreases intratesticular testosterone by inhibiting release of LH (via neg feedback) -> gonadal atrophy. Premature closure of epiphyseal plates. Increases LDL, decreases HDL.

20

Antiandrogens

name 4?

relevant mechanism?

-Finasteride

-Flutamide

-Ketoconazole

-Spironolactone

Remember that 5a-reductase converts testosterone to DHT (more potent).

21

Finasteride

Mech? Use?

Inhibits 5a-reductase. 

Use: BPH, also promotes hair growth (used in male-pattern baldness)

22

Flutamide

Mech? Use?

Nonsteroidal competitive inhibitor of androgens at the testosterone receptor

Use: prostate carcinoma

23

Ketoconazole

Use? Mech? Tox?

Treats hirsutism of PCOS

Inhibits steroid synthesis (inhibits 17,20 desmolase)

Tox: amenorrhea, gynecomastia

"To prevent male pattern hair loss, give a drug that will encourage female breast growth"

24

Spironolactone

Use? Mech?

Treats hirsutism of PCOS

Inhibits steroid binding, 17a-hydroxylase, and 17,20 desmolase

Tox: amenorrhea, gynecomastia

"To prevent male pattern hair loss, give a drug that will encourage female breast growth"

25

Tamsulosin

Use? Mech?

Used to treat BPH by inhibiting smooth muscle contraction.

alpha1-antagonist. Selective for alpha1A,D receptors (on prostate) rather than alpha1B receptors (vascular)

26

Sildenafil, Vardenafil

Mech? Use? Tox?

Use: erectile dysfunction

Mech: inhibits phosphodiesterase 5, causing incr cGMP, smooth muscle relaxation in the corpus cavernosum, increased blood flow, penile erection

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

"Sildenafil and Vardenafil FILL the penis. Hot and sweaty -> Headache, Heartburn, Hypotension"

27

(Uworld question)

2 types of meds for BPH?

- alpha-adrenergic inhibitors (e: doxazosin) to relax VSM at bladder neck

-5a reductase inhibitors (prevent conversion of Test to DHT)