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Flashcards in Reproductive Drugs Deck (42)
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1
Q

Leuprolide mechanism

A

-GnRH analog with agonist properties when used in a pulsatile fashion; antagonist properties when used continuously (downregulates GnRH receptor in the pituitary leading to decreased FSH/LH)

2
Q

Clinical use of Leuprolide

A

infertility prostate cancer uterine fibroids precocious puberty

3
Q

Clinical use of estrogens (ethinyl estradiol, DES, mestranol)

A

-hypogonadism or ovarian failure -mesntrual abnormalities -HRT in postmenopausal women -used in men with androgen dependent prostate cancer

4
Q

Toxicity of estrogens

A

-increased risk of endometrial cancer -bleeding -clear cell adenocarcionma of vagina (DES) -increased risk of thrombi

5
Q

Estrogens are contraindicated in...

A

ER + breast cancer and those with a hx of DVTs

6
Q

Selective Estrogen Receptor Modulators (SERMs)

A

-Clomiphene -Tamoxifen -Raloxifene

7
Q

Clomiphene is an...

A

antagonist at estrogen receptors in the hypothalamus that prevents normal feedback inhibition leading to increaed release of LH and FSH from the pituitary which stimulates ovulation.

8
Q

CLompihene is used to treat...

A

infertility due to anovulation (PCOS).

9
Q

Clomiphene may cause...

A

hot flashes, ovarian enlargement, multiple simultaneous pregnancies and visual disturbances.

10
Q

Tamoxifen is an...

A

antagonist on breat tissue and agonist in bone and the uterus.

11
Q

Tamoxifen is associated with...

A

endometrial cancer and thromboembolic events.

12
Q

Tamoxifen is primarily used to treat and prevent recurrence of...

A

ER + breast cancer.

13
Q

Raloxifene is an...

A

agonist on bone and antagonist at the uterus.

14
Q

Raloxifene increases risk of...

A

thromboemblic events.

15
Q

Raloxifene is used to treat...

A

osteoporosis bc it decreases resorption of bone.

16
Q

HRT is used for...

A

relief of menopausal symptoms and osteoporosis.

17
Q

Unopposed estrogen replacement therapy increases risk of...

A

endometrial cancer so progesterone is added.

18
Q

Anastrozole/Exemestane are...

A

aromatase inhibitors used in postmenopausal women with breast cancer

19
Q

Progestins MOA

A

bind progesterone receptors to decrease growth and increase vascularization of the endometrium

20
Q

Progestins Use

A

used in oral contraceptives and in treatment of endometrial cancer and abnormal uterine bleeding

21
Q

Mifepristone MOA

A

competitive inhibitor of progestins

22
Q

Clinical use of mifepristone

A

termination of pregnancy (administered with misoprostol (PGE1))

23
Q

In OCPs, estrogen and progestins inhibit...

A

LH/FSH and thus prevent the estrogen surge. No estrogen surge means no LH sruge means no ovulation.

24
Q

In OCPs, progestins cause...

A

thickening of the cervical mucus (limiting access to sperm) and they inhibit endometrial proliferation making it less suitable for implantation.

25
Q

Contraindications for OCPs

A

smokers > 35 hx of thromboembolism, stroke or estrogen-dependent tumors

26
Q

Terbutaline is a...

A

beta2-agonist that relaxes the uterus; usted to decrease contraction frequency in women during labor.

27
Q

Danazol MOA

A

synthetic androgen that acts as a partial agonist

28
Q

Use of Danazol

A

endometriosis and angioedema

29
Q

Toxicity of Danazol

A

-weight gain -edema -acne -hirsutism -masculinization -decreased HDL -hepatotoxicity

30
Q

MOA of Testosterone and Methyltestosterone

A

agonist at androgen receptors

31
Q

Use of Testosterone and Mehtyltestosterone

A

-hypogonadism -promotes development of secondary sex characteristics -stimulation of anabolism to promote recovery after burn or injury

32
Q

Toxicity of testosterone

A

-masculinization -decrease intratesticular testosterone (gonadal atrophy due to decreased LH) -premature closure of epiphyseal plates -increased LDL, decreased HDL

33
Q

Finasteride is a...

A

5alpha-reductase inhibitor that decreases the conversion of testosterone to DHT

34
Q

Finasteride uses

A

-BPH -male pattern baldness

35
Q

Flutamide is a...

A

nonsteroidal competitive inhibitor of androgens at teh testoterone receptor.

36
Q

Flutamide is used in...

A

prostate carcinoma.

37
Q

Ketoconazole inhibits...

A

steroid synthesis (inhibits 17,20-desmolase).

38
Q

Spironolactone inhibits...

A

steroid binding, 17alpha-hydroxylase and 17,20-desmolase.

39
Q

Ketoconazole and spironolactone are used in the treatment of...

A

PCOS to prevent hirsutism. Both have side effects of gynecomastia and amenorrhea.

40
Q

Tamsulosin is an...

A

alpha1-antagonist used to treat BPH by inhibiting smooth muscle contraction. Selective for alpha1A,D receptor found on prostate.

41
Q

Sildenafil and Vardenafil MOA

A

inhibit phosphodiesterase-5 causing increased cGMP, smooth muscle relaxation, increased blood flow and penile erection

42
Q

Toxicity of Sildenafil and Vardenafil

A

-dyspepsia -impaired blue-green color vision -risk of life-threatening hypotension in pts taking nitrates (since they block teh breakdown of NO)