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Flashcards in Female repro pharm Deck (28):
1

general adverse effects of progestins

Headache

breakthrough bleeding

androgenic actions, acne hirsuitism

2

decreases estrogen driven endometrial proliferation and leads to development of secondary endometrium

progesterone

2

contraindications estrogens

pregnancy

estrogen dependent cancers

undiagnosed uterine bleeding

thromboembolic disorders

2

spironolactone analogue

indications and side effects

Drospirenone

indications: pregnancy prevention, PMDD, moderate acne vulgaris

 

side effects - antimineralcorticoid activity

K should be monitored for hyperkalemia

2

therapuetic uses for progestins

Hormonal contraceptives

Post menopause hormone replacement (only with estrogen)

diagnosis of secondary amenorrhea

endometrial hyperplasia

3

progesterone analog, (injected+oral)

medroxprogesterone

4

natural estrogens

17b estradiol

estrone

estriol

6

progesterone binds what in plasma

corticosteroid binding globulin

albumin

some progestins bind SHBG

7

anti estrogen that inhibits action of strong estrogens via inhibition of feedback (pituitary hypothalamus) thus increasing pulsitile gonadotropin release amplitude

Clomiphene

7

mechanism and indication  Raloxifene

 

side effects

SERM estrogen agonist in bone

Use: reudce rate of bone loss (osteopororsis prophylaxis) risk reduction for invasive breast cancer

 

side effects: (estrogenic) reduces total cholesterol, hot flashes, increases thrombosis, leg cramps (does NOT cause endometrial thickening as Tamoxifene)

8

therapeutic approaches for postmenopausal replacement

estrogen/progetin combo (intact uterus)

estrogen only (post hysterectomy)

9

Clomiphene mechanism

inhibits action of strong estrogens via inhibition of feedback at pituitary and hypothalamus 

causes increase in GnRH pulse amplitude

11

phsyiological effects of estrogen on endometrium

enhance cervical mucus and increases water content

promotes endometrial proliferation

increases tubule contractility favoring rhythmic contractions of myometrium

12

indication, mechanism, side effects ulipristal

Emergency contraception 

 

selective progesterone receptor mdoulator > inhibits LH release > inhibits LH induced folliculr rupture in ovary when taken 5 days after intercourse (inhibits ovulation)

 

side effects - headache, abd pain 

13

synthetic estrogens

ehtinyl estradiol

mestranol

14

decreases the frequency of GnRH pulses, critical for suppressing gonadotropin release

progesterone

16

estrogen skeletal effects

skeletal maturation

epiphyseal plate closure

postive effects on bone mass

17

adverse effects estrogens

Gall bladder disease (due to increase cholesterol content in bile)

oral estrogens increase risk of thromboembolic disease

nausea and vomiting on initial use

breast swelling 

migrane headaches

18

SERMS

Tamoxifen 

Raloxifene

18

Alternatives to estrogen for the treatment of osteoporosis

raloxifene

alendronate (bisphosphonate)

20

progesterone derivative, etyinyl substituent at C17 slows hepatic metabolism to reduce firsts pass

 

progesterone derivative, racemic mixture, 13 ethyl subtituent results in potent progestin with less androgenic activity

norethindrone

 

Norgestrel

22

therapeutic uses of estrogens

combination oral contraceptives

post-menopause hormone replacement therapy

failure of pituitary function and and ovarian development

23

half life progesterone

minutes

24

relative strength of natural estrogens

estradiol > estrone > estriol

25

Tamoxifen mechanism and idication

 

side effects

SERM: mixed estrogenic and anti estrogenic effects (esp breast)

 

use: treatment and preventionof breast cancer (ER positive)

 

side effects (estrogenic) hot flashes, endometrial poliferation (risk of endometrial cancer)

increased thromboembolic disease

antiresoptive effect on bone

 

26

emergency contraceptive regimens

Levonorgeestrel + ethinyl estradiol (2 doses)

Levonorgesrel alone (2 doses)

Ulipristal 

27

Aromatase inhibitors, specific mechanism, indication and side effects

Letrozole+Anastrozole: non steroidal reversible inhibitors of aromatase (reduce T>estradiol, Androstenedion>Estrone)

Exemestane: suicide inhibitor

 

use: treat breast cancer, ovulation induction (off-label)

side effects: hot flashes

28

inidcation, mechanism Mfepristone (Ru-486)

 

 

side effects

abortifacient

competitive progesterone receptor modulator (mainly antagonist)

competitively binds receptor, causing decidual breakdown leading to placental detachment.

snetizies myometrium to contractile actions of prostaglandins for expulsion

 

vaginal bleeding