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Pharmacology Test #5 > Estrogens > Flashcards

Estrogens Flashcards

1
Q

What does estrogen do in the body?

A

development and maintenance of female reproductive tissues; regulation in CNs; effects in peripheral tissues

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2
Q

What does progesterone do in the body?

A

Development and maintenance of female reproductive tissues; maintenance of pregnancy; effects in other tissues (brain)

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3
Q

Most potent estrogen in humans

A

17beta-estradiol

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4
Q

Where is 17b-estradiol produced?

A

mostly in the ovaries in premenopausal women; synthesized most in the placenta during pregnancy

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5
Q

Estrogen and progesterone are produced by

A

granulosa cells and the corpus luteum

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6
Q

Early follicular phase

A

estrogen suppresses the production of FSH

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7
Q

Late follicular phase

A

Estrogen and progesterone stimulate the surge of LH and FSH -> ovulation and formation of the corpus luteum

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8
Q

Luteal phase

A

Estrogen and progesterone suppresses the production of LH and FSH

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9
Q

What happens if pregnancy does not occur?

A

corpus luteum degenerates; production of estrogen and progesterone by corpus luteum declines

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10
Q

What happens if pregnancy occurs?

A

fertilized egg/embryo secretes hCG; hCG acts like LH to stimulate corpus luteum to produce progesterone during the first trimester; higher progesterone levels support maintenance of the endometrium

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11
Q

Estron and estriol are synthesized

A

in the liver and in peripheral tissues

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12
Q

Natural estrogens

A

17beta-estradiol
Estrone
Estriol

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13
Q

Synthetic estrogens

A

Drugs with estrogenic activities

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14
Q

Phytoestrogens

A

Estrogen-mimetic compounds in plants (flavonoids)

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15
Q

Environmental estrogens

A

Compounds used in the manufacture of plastics (bisphenols, alkyphenols, phthalate phenols)

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16
Q

Metabolism and excretion of estrogen

A

Metabolized in the liver mostly and excreted to the bile and to the urine

17
Q

Physiologic effects of estrogen

A

Female maturation, endometrial effects, metabolic and CV effects, blood coagulation, CNS/mood

18
Q

Clinical uses of estrogens

A

Postmenopausal hormone therapy in post-menopausal women, osteoporosis

19
Q

Adverse effects of estrogens

A

Uterine bleeding, endometrial carcinoma, breast cancer, thromboembolism, nausea, headache, fluid retention, weight gain

20
Q

17alpha-alkylated estrogens

A

Mestranol;
Quinestrol;
Ethinyl estradiol

21
Q

17alpha-alkylation prevents

A

conversion to estron -> enhances oral bioavailability and increases the half life

22
Q

Estrogenic esters

A

Estradiol valerate

Estradiol cypionate

23
Q

Esterification decreases

A

solubility and slows the absorption -> prolongs the action

24
Q

Conjugated estrogens

A

Estrone sulfate

Equilin sulfate

25
Q

Where do you get conjugated estrogens from

A

collected from pregnant mare urine

26
Q

Non-steroidal estrogens

A

Diethyl stilbestrol

Chlorotrianisene

27
Q

Diethyl stilbestrol

A

used in advanced prostate cancer

28
Q

Chlorotrianisene

A

postpartum breast engorgement; menopause symptoms; prostate cancer

29
Q

Selective estrogen receptor modulators (SERM)

A

Tamoxifen
Toremifene
Raloxifene
Clomiphene

30
Q

Tamoxifen

A

partial estrogen agonist; antiestrogen and estrogenic actions; treatment of breast cancer; prevents breast cancer in high risk women

31
Q

Raloxifene

A

SERM; partial estrogen agonist; prevents osteoporosis; decreases LDL levels; increases risk for blood clots; does not stimulate endometrial cells; may cause hot flashes

32
Q

Clomiphene

A

SERM; partial estrogen agonist; increases secretion of FSH and LH by inhibiting negative estradiol feedback; used to sitmulate ovulation in women with oligomenorhea or amenorrhea and ovulatory dysfunction; polycystic ovary syndrome

33
Q

Fulvestrant

A

selective estrogen receptor downregulator; pure estrogen receptor antagonist

34
Q

Aromatase inhibitors

A

Anastrozole, Letrozole, Exemestane

Pharmacology Test #5 (11 decks)

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