Estrogens and Progestins Flashcards

1
Q

What are the estrogen derivatives used clinically?

A
Conj. Equine estrogens 
Diethylstilbestrol
estradiol
ethinyl estradiol
mestranol
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2
Q

What are the clinically used progestins? (progesterone derived)

A

Medroxyprogesterone acetate (MPA)

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3
Q

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

A

.

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4
Q

When does positive feedback occur in the ovarian cycle?

A

Mid cycle (day 14) induces ovulation

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5
Q

What hormones are involvedin the follicular phase

A

High F low Amp LH

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6
Q

What steps are involved in the follicular phase

A

HF/LA LH secretion
Estrogen rises
Endometrial Proliferation

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7
Q

What causes the ovulation phase?

A

Estrogen induced gonadotropin surge

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8
Q

What steps are involved in the Luteal Phase?

A

Rise in Estrogen and Progesterone

Endometrial diff under control of progesterone

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9
Q

What is the MOA of Steroids?

A

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

Alternative pathways too

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10
Q

What are the metabolic effects of Estrogen?

A
Dec LDL, Inc HDL, Inc TRGs
Keeps bone from being resorbed
Inc. coagulation factors
dec. antithrombin
Increases Plasma Proteins
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11
Q

What are the Metabolic effects of Progesterone?

A

Inc. LDL, Inc Fat Deposition

Inc. Fasting Glucose

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12
Q

What are the endometrial effects of Estrogen?

A

Endo. Proliferation

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13
Q

What are the endometrial effects of Progesterone?

A

Endo Differentiation, prep for implantation, decrease uterine contractions

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14
Q

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

A

Estrogen- Reg Follicular Phase

Progesterone- Reg Luteal phase

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15
Q

What are the effects of Progesterone on Uterus smooth muscle?

A

Decrease uterine contraction
DecProstaglandin
Maintain relaxin secretion

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16
Q

What are the effects of Progesterone on Cervical glands?

A

Increase cervical mucous Viscosity

17
Q

What is the reason for chemical modification of estrogen?

A

Increase the half life by putting ethinyl group on it.

HL = from minutes to 13-27 hrs

18
Q

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

A

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

19
Q

What are the pharmacological uses of estrogens? Hypogonadism

A

Hypogonadism (promotes dev. of female sex organs)

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

20
Q

What are the pharmacological uses of estrogens? Hormone Replacement therapy

A
Maint boneDensity
Supress hot flahes
Supress Urogenitl atrophy
HPG axis 
Endometrium- 
Bone- antiresorptive
Development- Ov, Fall tubes, Ut, vag, br
21
Q

What are the Pathophysiology effects of Estrogens?

A
Inc Risk of: CHD
Stroke
PE
Breast Cancer
Dec risk of: Colorectal cancer
Hip Fracture
22
Q

What are the pharmacological uses of estrogens? Contraception

A

HPG axis: negative feedback activation of axis

Decreased ovulation

23
Q

What are the pharmacological uses of estrogens? Acne Tx

A

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

24
Q

What are the adverse effects of Estrogen?

A

Br Tenderness
Endometrial Hyperplasia
Inc Blood Coagulation

Nausea
Cholestasis- Change in cholesterol secretion, bile canaliculi function
Migraine
Cancer 
Bloating- loss ofintravascular fluid
25
Q

What are the cancer risks associated with Hormone Replacement Therpy?

A

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

26
Q

What two drugs are often combined for HRT?

A

Estrogen and Medroxy-Progesterone

27
Q

What are the clinical uses of Progestins? Contraceptive

A

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

28
Q

What are the clinical uses of Progestins? HRT

A

Dec Risk of endometrial hyperplasia

29
Q

What are the clinical uses of Progestins? Dysmenhorrea

A

Dec. Endometrial Mass

and dec prostaglandin prod

30
Q

What are the clinical uses of Progestins? Endometriosis

A

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