Estrogens and Progestins

Question 1

What are the estrogen derivatives used clinically?

Answer 1

Conj. Equine estrogens 
Diethylstilbestrol
estradiol
ethinyl estradiol
mestranol

Question 2

What are the clinically used progestins? (progesterone derived)

Answer 2

Medroxyprogesterone acetate (MPA)

Question 3

What are the clinically used progestins? (19-nor compounds)

Answer 3

.

Question 4

When does positive feedback occur in the ovarian cycle?

Answer 4

Mid cycle (day 14) induces ovulation

Question 5

What hormones are involvedin the follicular phase

Answer 5

High F low Amp LH

Question 6

What steps are involved in the follicular phase

Answer 6

HF/LA LH secretion
Estrogen rises
Endometrial Proliferation

Question 7

What causes the ovulation phase?

Answer 7

Estrogen induced gonadotropin surge

Question 8

What steps are involved in the Luteal Phase?

Answer 8

Rise in Estrogen and Progesterone

Endometrial diff under control of progesterone

Question 9

What is the MOA of Steroids?

Answer 9

Steroids bind to intracellular receptors and mod. transcriptional activity
Ag/Ant compete for steroidbinding sites

Alternative pathways too

Question 10

What are the metabolic effects of Estrogen?

Answer 10

Dec LDL, Inc HDL, Inc TRGs
Keeps bone from being resorbed
Inc. coagulation factors
dec. antithrombin
Increases Plasma Proteins

Question 11

What are the Metabolic effects of Progesterone?

Answer 11

Inc. LDL, Inc Fat Deposition

Inc. Fasting Glucose

Question 12

What are the endometrial effects of Estrogen?

Answer 12

Endo. Proliferation

Question 13

What are the endometrial effects of Progesterone?

Answer 13

Endo Differentiation, prep for implantation, decrease uterine contractions

Question 14

What are the effects of Estro/Progesterone onthe menstrual cycle?

Answer 14

Estrogen- Reg Follicular Phase

Progesterone- Reg Luteal phase

Question 15

What are the effects of Progesterone on Uterus smooth muscle?

Answer 15

Decrease uterine contraction
DecProstaglandin
Maintain relaxin secretion

Question 16

What are the effects of Progesterone on Cervical glands?

Answer 16

Increase cervical mucous Viscosity

Question 17

What is the reason for chemical modification of estrogen?

Answer 17

Increase the half life by putting ethinyl group on it.

HL = from minutes to 13-27 hrs

Question 18

What is different about the conjugated equine estrogens? (naturally derived)

Answer 18

Need to give much more bc it is much more readily metabolized

Question 19

What are the pharmacological uses of estrogens? Hypogonadism

Answer 19

Hypogonadism (promotes dev. of female sex organs)

Development of Ovaries, fallopian tubes, uterus, vagina and breasts

Question 20

What are the pharmacological uses of estrogens? Hormone Replacement therapy

Answer 20

Maint boneDensity
Supress hot flahes
Supress Urogenitl atrophy
HPG axis 
Endometrium- 
Bone- antiresorptive
Development- Ov, Fall tubes, Ut, vag, br

Question 21

What are the Pathophysiology effects of Estrogens?

Answer 21

Inc Risk of: CHD
Stroke
PE
Breast Cancer
Dec risk of: Colorectal cancer
Hip Fracture

Question 22

What are the pharmacological uses of estrogens? Contraception

Answer 22

HPG axis: negative feedback activation of axis

Decreased ovulation

Question 23

What are the pharmacological uses of estrogens? Acne Tx

Answer 23

Supress steroidogenensis
Increase SHBG production by liver and dec. free T conc.
HPG Axis
Liver- increase plasma proteins

Question 24

What are the adverse effects of Estrogen?

Answer 24

Br Tenderness
Endometrial Hyperplasia
Inc Blood Coagulation

Nausea
Cholestasis- Change in cholesterol secretion, bile canaliculi function
Migraine
Cancer 
Bloating- loss ofintravascular fluid

Question 25

What are the cancer risks associated with Hormone Replacement Therpy?

Answer 25

HRT combo: Breast cancer (due to progestin not estrogen) HRT just estrogen: Endometrial Cancer Contraceptive: Red risk of ovarian and endometrial Cancer Cancer Mech: Trophic effects of hormones Reactive oxy species prod. from met. of drug

Question 26

What two drugs are often combined for HRT?

Answer 26

Estrogen and Medroxy-Progesterone

Question 27

What are the clinical uses of Progestins? Contraceptive

Answer 27

Alone or in combination with estrogen (more effetive) HPG Axis Cervical Glands

Question 28

What are the clinical uses of Progestins? HRT

Answer 28

Dec Risk of endometrial hyperplasia

Question 29

What are the clinical uses of Progestins? Dysmenhorrea

Answer 29

Dec. Endometrial Mass | and dec prostaglandin prod

Question 30

What are the clinical uses of Progestins? Endometriosis

Answer 30

Dec endometrial proliferation by regulating ER expression and stimulating differentiation of endometrial cells