Pharm 3 Estrogen/Progestin Flashcards Preview

Test 9 > Pharm 3 Estrogen/Progestin > Flashcards

Flashcards in Pharm 3 Estrogen/Progestin Deck (47):
1

Ovarian-pituitary cycle

-Elevated FSH during 1st half stimulates follicle
-Midcycle estradiol exerts positive feedback, triggers LH surge
-LH surge induces ovulation, stimulates corpus luteum and progesterone production

2

Pregnancy hormone

hCG (chorionic gonadotorpin) identical to LH, maintains estrogen and progesterone production by maintaining corpus luteum

3

Hormones interacting with endometrium

-Estrogen mediates proliferation
-Progesterone maintains secretory state

4

Base molecule for estrodiol/testosterone synthesis

Cholesterol

5

Hormone replacement therapy

Estradiol undergoes extensive first-pass metabolism, so use conjugated estrogens (estrone sulfate)

6

-Estrone sulfate-
indication

Conjugated estrogen absorbed in lower gut
-Hormone replacement therapy

7

-Ethinyl estradiol-
indication

Ethinyl substitution reduces first-pass metabolism, greater oral potency than conjugated estrogens
-Oral contraceptives

8

-Estradiol cypionate-

Insoluble in water
-Once monthly IM for HRT

9

-Medroxyprogesterone-

Breast and endometrial cancer
-Oral or IM

10

-Megestrol-

Endometrial cancer

11

-Norethindrone-

19-nortestosterone derivative Progestin
-Oral contraceptives

12

-Desogestrel-

Progesterone for oral contraceptive
-Lowest degree of androgenic activity

13

Estradiol/Progesterone transport

-Estradiol bound to SHBG (sex hormone binding globulin) high affinity
-Progesterone bound to CBG (corticosteroid binding globulin) with high affinity
-Both bound to albumin with low affinity

14

Estradiol/Progesterone Metabolism

Hepatic conjugation
-Estradiol -> estrone -> bile -> reabsorbed
-Progesterone -> pregnanediol

15

Estrogen MOA

Binds to nuclear receptor (homodimer), regulates trasncription

16

Progestin MOA

Binds to response element similar to that of corticosteroids

17

Estrogen effects on bone

-Prepubertal growth of long bones
-Pubertal closure of epiphyses
-Post pubertal decreased bone resorption

18

Estrogen effects on clotting

-Increase clotting factors
-Decrease antithrombin
-Increase platelet adhesiveness

19

Estrogen effects on lipids

Increase HDL, triglycerides
Decrease LDL

20

Estrogen effect of sex behavior

-Mediates testosterone's effect on libido

21

Estrogen other effects

-Maintain skin and blood vessel integrity
-Increase CBG, TBG, SHBG
-Increase cortisol
-Increase Na and water retention

22

Progesterone v Estrogen

Antagonize estrogen
-Decrease Na retention
-Decrease HDL
-Increase metabolism
-Downregulate receptors

23

Progesterone other effects

-Stimulate respiratory center
-Increase insulin, reduce glucose tolerance
-Acne
-Weight gain

24

Primary hypogonadic impaired development Tx

-Start estrogen at 11-13, add progestin when growht is completed

25

Hysterectomy HRT

Unopposed estrogen (don't worry about progesterone)

26

Other clinical uses for Estrogen

-Ovarian suppression for hyperandrogenism
-Ovulation suppression in dysmenorrhea
-Androgen-dependent prostate cancer (suppress gonadotropin secretion)

27

Estradiol levels postmenopausal

1/4 that of males

28

Postmenopausal HRT alleviates (5)

Sleep disturbances
Hot flashes
Urogenital changes
Osteoporosis
High cholesterol

29

HRT contraindications

Liver disease
Breast or other estrogen-dependent cancer

30

Low dose combination OC

-All use ethinyl estradiol
-Norgestrel for monophasic
-Norethindrone for bi/triphasic

31

Monophasic v Triphasic

-Triphasic eliminates period for 90 days
-Triphasic reduces total dose of progestin (reduced SE)

32

OC MOA

Inhibit gonadotropin secretion, suppress ovulation (progestin only blocks ovulation 60-80%)
-Thicken cervical mucus
-Reduce tubal secretion/motility
-Change uterine endometrium

33

OC mild AE

Breakthrough bleeding
-Tx with higher dose estrogen or different progestin

34

OC moderate AE

Acne with higher progestin doses
-Nausea, mastalgia, weight gain, headache

35

OC severe AE

-Thromboembolism (estrogen dependent)
-Myocardial infarction
-Cholestatic jaundice

36

OC neoplasm risk

Hepatic adenoma

37

OC contraindications

Impaired liver function, h/o thromboembolic disease, CAD, hyperlipidemia

38

OC caution with

Migraine, HTN, DM, gallbladder disease

39

OC drug interactions

-Decreased efficacy with antibiotics that affect GI absorption
-Insulin efficacy reduced by OC

40

Tx for endometriosis

Medroxyprogesterone Acetate (IM injection every 3 months)
-Amenorrhea side effect

41

-Clomiphene-

Antiestrogen (competitive) reduces negative feedback
-Induces ovulation

42

-Fulvestrant-

Pure estrogen receptor antagonist
-For treating hormone-responsive metastatic breast cancer in postmenopausal women

43

-Tamoxifen-

Anti-estrogen on breast
-Pro-estrogen on lipids, bones, endometrium
-Tx perimenopausal symptoms

44

-Raloxifene-

Anti-estrogen on breast, pro (1/2 strength) on bones
-Tx post-menopausal osteoporosis, BRCA
-No effect on perimenopausal symptoms

45

-Mifepristone (RU 486)-
MOA
Parent molecule
Effect

Progesterone-R antagonist, glucocorticoid-R antagonist, prostaglandin dehydrogenase inhibitor
-Norethindrone derivative
-Stimulate uterine SM contractility

46

-Mifepristone-
other use

Glucocorticoid receptor antagonist
-Tx Cushing's secondary to ectopic ACTH secretion

47

Abortion regimen

Mifepristone in first 49 days
-Misoprostol (prostaglandin analog) 48 hours later to expel blastocyst