Womens Health Med Chem Flashcards

0
Q

ER signaling

A

1) Bind to estrogen receptor
2) ER Transciption factor tether
3) growth factor phosphorylate ER
4) non genomic actions: cytoplasm proteins

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1
Q

Estrogen

A
Female maturation
Endometrial effects
Metabolic bone resorption 
Adipose leptin
Blood coagulability 2,7,9,10
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2
Q

Tamoxifen

Raloxifene, clomiphene

A

Blocks ER

Selective estrogen receptor modulator

SERM-ifen, iphene
Partial agonist antagonist

For breast cancer

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3
Q

Major estrogens

A

Estriol, estrone, estradiol

Estradiol is major secretory product of the ovary

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4
Q

Precursor for estrogen synthesis

A

Pregnenolone -> androstenedione ->

Aromatase to produce estrone and estradiol

Estrone is precursor for estriol

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5
Q

Pulsatile GnRH

A

Endogenous

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6
Q

Fertility

A

GnRH agonist (less multiple gestations)

Clomiphene: competitive inhibitor of endogenous estrogen and blocks negative feedback, stimulate ovulation

DC clomiphene if visual AE

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7
Q

Contraception

A

Oral contraceptive: consistent high estrogen & progestin levels inhibit GnRH, inhibit FSH, LH (release and egg maturation), insufficient endometrial thickening, thick cervical mucus

Danazol: inhibits LH/FSH surge

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8
Q

Endometriosis

A

Ketoconazole

Danazol: suppress ovarian function and midcycle LH/FSH surge

Synthetic androgen

Androgens cause atrophy

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9
Q

Breast cancer

A

Fulvestrant - pure ER antagonist (if resistant to tamoxifen)
SERM

Anatrozole, letrozole Aromatase inhibitors (decrease estrogen production)
Exemestane: irreversible Aromatase inhibitor

Most breast cancer cells are ER+ and proliferate by estrogen

Block androgen conversion to estrogen

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10
Q

GnRH

A

Stimulates release of FSH/LH

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11
Q

FSH

A

Develops follicles, estrogen secretion, and induces expression of LH receptors

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12
Q

LH

A

Regulates Aromatase ( production of 17B-estradiol from testosterone)

Surge LH= ovulation

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13
Q

HPA negative feedback

A

Estrogen and progesterone on GnRH

Inhibin on FSH release

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14
Q

GnRH neurons

A

Stimulated by NE neurons

Inhibited by opioid, dopamine, GABA

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15
Q

Anterior pituitary

A

Stimulate production of hormones by peripheral endocrine/ liver

16
Q

Secretion of GnRH

A

Depends on gene KiSS and kisspeptin

High estrogen inhibits secretion of kisspeptin

17
Q

Estrogen metabolism

A

CYP 3A4

Rifampin, SJW

18
Q

Progesterone

A

Most important natural progestin produced by corpus luteum

Builds endometrium

Precursor to androgen and estrogen, adrenocorticoids

Elevate during pregnancy and peak in 3rd trimester, mimic pregnancy

Metabolized by liver

19
Q

Progestins

A

Most are 19-nortestosterone derivatives

Estrane 1st gen norethindrone

Drosperinone 4th gen derived from 17a-spironolactone
Minimize androgenic properties

Long term ovarian suppression
Thick cervical mucus

20
Q

Mifepristone

A

Binds to progesterone receptor and inhibits progesterone

Degrades corpus luteum

21
Q

Osphena

A

Treat painful interfourse

Estrogen agonist

Increases risk of endometrial cancer in women who use unopposed estrogen

22
Q

Aromatase inhibitor

A

Inhibit production of estrogen from testosterone

And block androstenedione to estrone