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Flashcards in Repro Drugs Deck (45):
1

Leuprolide: Mechanism

GnRH analog with agonist properties when used in a pulsatile fashion.
ANTAGONIST when used in a continuous fashion (downregulates GnRH receptor in pituitary --> decreased FSH/LH)

2

Leuprolide: Clinical Use

Pulsatile -- infertility
Continuous -- Prostate cancer, Uterine fibriouds, Precocious puberty

3

For prostate cancer, use continuous or pulsatile leuprolide? Also, with what other drug

Treat prostate cancer with continuous leuprolide and co-administer with flutamide (competitive inhibitor of androgens)

4

Leuprolide: Toxicity

Antiandrogen, nausea, vomiting

5

Testosterone, Methyltestosterone: Mechanism

Agonist at androgen receptors

6

Testosterone: Clinical Use

Treats hypogonaidism and promotes development of secondary sex characteristics; stimulation of anabolism to promote recovery after burn or injury

7

Testosterone: Toxicity

Causes masculinization in females; reduces intratesticular testosterones in males by inhibiting release of LH (via negative feedback), leading to gonadal atrophy. Premature closure of epiphyseal plates.

8

Testosterone effect on cholesterol

Increased LDL; Decreased HDL

9

Enzyme for conversion of testosterone to DHT

5-alpha reductase. DHT is more potent than testosterone

10

Finasteride

5-alpha reductase inhibitor (decreases conversion of testosterone to DHT).

11

Finasteride Uses

Useful for BPH (as DHT is primary mediator that causes hyperplasia in prostate). Also promotes hair growth - used to treat male pattern baldness

12

Flutamide

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

13

Ketoconazole

Inhibits steroid synthesis (inhibits 17, 20 desmolase).

14

Spironolactone

Inhibits steroid binding.

15

Rx for polycystic ovarian syndrome to prevent hirsuitism

Spironolactone and Ketoconazole. Can cause gynecomastia and amenorrhea

16

Estrogens - name them

Ethinyl, Estradiol, DES, mestranol

17

Estrogen: Mechanism

Bind estrogen receptors

18

Estrogen: Clinical Use

Hypogonadism or ovarian failure.
Menstrual abnormalities,
HRT in postmenopausal women;
use in men with androgen dependent prostate cancer

19

Estrogen: Toxicity

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

20

Contraindications of Estrogen use

- ER-positive breast cancer
- history of DVTs

21

Selective Estrogen Receptor Modulators (SERMs)

Clomiphene, Tamoxifen, Raloxifene

22

Clomiphine

SERM - partial agonist at estrogen receptors in hypothalamus.
Prevents normal feedback inhibition and increases release of LH and FSH from pituitary which stimulates ovulation

23

Clomiphine: Use

Treat infertitility and polycystic ovarian syndrome. May cause hot flashes, ovarian enlargement. Multiple simultaneous pregancies, and visual disturbances

24

Raloxifene

SERM. Agonist on bone; Reduces resorption of bone; Used to treat osteoporosis.

25

Tamoxifen

Antagonist at breast tissue; Used to treat and prevent recurrence of ER-positive breast cancer.

26

Hormone replacement therapy

Used for relief or prevention of menopausal symptoms (e.g. hot flashes, vaginal atrophy) and osteoporosis (increases estrogen, decreases osteoclast activity)

27

Discuss risks of HRT of cancer, CV dises

Unopposed estrogen replacement therapy (ERT increases risk of endometrial cancer, so progesterone is added. Possible INCREASED CV risk

28

Anastrozole/ Exemestane

Aromatase inhibitors used in postmenopausal women with breast cancer

29

Progestins : Mechanism

Bind progesterone receptors, reduce growth and increase vascularization of endometrium.

30

Progestin: Clinical Use

Used in oral contraceptive and in the treatment of endometrial cancer and abnormal uterine bleeding

31

Mifepristone (RU-486): Mechanism

Competitive inhibitor of progestins at progesterone receptors

32

Mifepristone (RU-486): Clinical Use

Termination of pregnancy. Administered with misprostol (PGE1)

33

Mifepristone (RU-486): Toxicity

Heavy bleeding, GI effects (nausea, vomiting, abdominal pain)

34

Oral contraception (synthetic progestins, estrogen)

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

35

Discuss progestins and pregnancy prevention

Progestins cause thickening of cervical mucus, thus limiting access of sperm to uterus. Also inhibit endometrial proliferation, thus making endometrium less suitable for implantation of an embryo.

36

Contraindications of OCP

Smokers > 35 y.o
Increased risk of CV events
Patients with a hx of thromboembolism and stroke or hx of estrogen dependent tumor

37

Terbutaline

B2 agonist that relaxes the uterus; reduces premature uterine contractions

38

Tamsulosin

Alpha 1 antagonist used to treat BPH by inhibiting smooth muscle contraction. Selective alpha 1AD receptors (found on prostate) vs. vascular alpha 1 B receptors `

39

Sildenafil, vardenafil

Phosphodiesterase inhibitors

40

Sildenafil, Vardenafil: Mechanism

Inhibit phosphodiesterase 5, causing increase in cGMP smooth muscle relaxation in the corpus canvernosum, increased blood flow and penile erection

41

Sildenafil, Vardenafil: Clinical Use

Treatment of erectile dysfunction

42

Sildenafil, Vardenafil: Toxicity

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

"Hot and sweaty", but then "Headache", "Heartburn, "Hypotension"

43

Danazol: Mechanism

Synthentic androgen that acts as partial agonist at androgen receptors.

44

Danazol: Clinical Use

Endometriosis and hereditary angiodema

45

Danazol: Toxicity

Weight fain, edema, acne, hirsuitism, masculinization. Decreased HDL levels, hepatotoxicity