drugs

Question 1

leuprolide

Answer 1

GnRH analog –> antagonist with continuous use, agonist with pulsatile uses

uses: clinical fibroids, endometriosis, precocious puberty, prostate cancer, infertility

Question 2

estrogens

Answer 2

Drugs: ethinyl estradiol, DES, mestranol

MAO: bind to estrogen receptors

Uses: hypogonadism or ovarian failure, menstrual abnormalities, hormone replacement therapy, men with androgen-dependent prostate cancer

can increase HDL

effects: increased risk of endometrial cancer, bleeding in postmenopausal, clear cell adenocarcinoma in DES, increased risk of thrombi
contraindications: ER positive breast cancer, history of DVTs

Question 3

clomiphene

Answer 3

selective estrogen receptor modulator

antagonist of estrogen receptor in hypothalamus

prevents normal feedback inhibition and increased release of LH and FSH from pituitary

uses: treating infertility due to anovulation

may cause hot flashes, ovarian enlargement, multiple gestations, visual disturbances

Question 4

tamoxifen

Answer 4

selective estrogen receptor modulator

antagonist at breast

agonist at bone, uterues

increased risk of thrombus and endometrial cancer

used to treat and prevent recurrence of ER/PR positive breast cancer

Question 5

raloxifene

Answer 5

antagonist of estrogen at breast and uterus

agonist at bone

increased risk of thrombus

no increased risk of endometrial cancer

used to treat osteoporosis

Question 6

aromatase inhibitors

Answer 6

Drugs: anastrozole, letrozole, exemestane

inhibit peripheral conversion of androgens to estrogens

used in ER positive breast cancer in postmenopausal women

Question 7

hormone replacement therapy

Answer 7

used for relief or prevention of menopausal symptoms and osteoporosis

increased risk of endometrial cancer if unopposed

possible increased CV risk

Question 8

fulvestrant

Answer 8

full estrogen antagonist used in breast cancer that is refractory to tamoxifen

Question 9

progestins

Answer 9

drugs: levonorgestrel, medroxyprogesterone, etonogestrel, norethindrone, megestrol,

can lower HDL, and have androgenic activity

binds progesterone receptors, decreased growth and increased vascularization of endometrium

thickened cervical mucus

used as contraception, in endometrial cancer, AUB

progestin challenge used to diagnose anovulation and Asherman syndrome

Question 10

antiprogestins

Answer 10

drugs: mifepristone, ulipristal

MOA: competitive inhibitors at progesterone receptors

uses: termination of pregnancy and emergency contraception

Question 11

terbutaline and ritodrine

Answer 11

beta 2 agonists that relax uterus to decrease contraction frequency in women during labor

Question 12

danazol

Answer 12

GnRH agonist

acts as partial agonist at androgen receptor

used in endometriosis, hereditary angioedema

adverse effects: weight gain, edema, acne, hirsutism, masculinization, lowered HDL, hepatotoxicity, pseudotumor cerebri

Question 13

finasteride

Answer 13

5 alpha reductase inhibitor

prevents conversion of testosterone to DHT

used for BPH and male pattern baldness

Question 14

flutamide

Answer 14

nonsteroidal competitive inhibitor at androgen receptors

used for prostate carcinoma

can cause liver damage

Question 15

ketoconazole

Answer 15

inhibits steroid synthesis

inhibits 17,20 desmolase/17 alpha hydroxylase

used in PCOS

can cause gynecomastia and amenorrhea

Question 16

spironolactone

Answer 16

inhibits steroid binding

treats hirsuitism in women

used in PCOS

can cause gynecomastia and amenorrhea

Question 17

Tamsulosin

Answer 17

alpha 1 antagonist use to treat BPH by inhibiting smooth muscle contraction

selective for alpha 1 receptors

Question 18

PDE5 inhibitors

Answer 18

sildenafil, vardenafil, tadalafil

increase cGMP to cause smooth muscle relaxation

increase blood flow to penis and decrease pulmonary vascular resistance

used in ED, pulmonary HTN, BPH

can cause headache, flushing, dyspepsia, cyanopia

risk of life threatening hypotension in patients taking nitrates