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pt > L 12 and 13 estrogens > Flashcards

L 12 and 13 estrogens Flashcards

1
Q

estrogens

A

-Development and maintenance of female
reproductive tissues (ovaries, uterus, breast, vagina)
-Regulation in CNS (temperature, mood)
-Effects in peripheral tissues (bone, cardiovascular, liver)

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2
Q

progesterone

A

-Development and maintenance of female
reproductive tissues (uterus and breast)
-Maintenance of pregnancy
-Effects in other tissues (brain

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3
Q

17 beta estradiol

A

-Most potent estrogen in human
-Binds to the estrogen receptor and alters rate of transcription
-Produced mostly in the ovaries in premenopausal women.
-Synthesized most in the placenta during pregnancy.
-Plasma levels: 5 – 85 ng/dL
-Cyclically varies during the menstrual cycle.
-Mostly bound to sex hormone-binding globulin (SHBG) and albumin and only 2% free in circulation.

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4
Q

gransulosa cells produce

A

estrogen

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5
Q

corpus letum produces both

A

estrogen and progesterone

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6
Q

menstrual cycle

A

early follicular phase, late follicular phase, luteal phase

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7
Q

early follicular phase

A

Estrogen suppresses the production of
FSH.

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8
Q

late follicular phase

A

Estrogen stimulates the surge of LH and FSH –> ovulation and formation of corpus luteum

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9
Q

luteal phase

A

Estrogen and progesterone suppresses
the production of LH and FSH

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10
Q

if pregnancy does not occur

A

-corpus luteum degenerates.
-Production of estrogen and progesterone by corpus luteum declines. –> menstruation

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11
Q

if pregnancy occurs

A

-Fertilized egg/embryo secrets human chorionic gonadotropin (hCG).
-hCG acts like LH to stimulate corpus luteum to produce progesterone during the first trimester.
-Higher progesterone levels support maintenance of endometrium.
-Chromatographic immunoassays of hCG in the urine are used as pregnancy tests.

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12
Q

estrone and estriol are synthesized in the

A

liver and peripheral tissues

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13
Q

types of estrogens

A

-estrogenic activity is shared by large number of chemical substances
-natural estrogen
-synthetic estrogens
-phytoestrogens
-environmental estrogens

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14
Q

natural estrogens

A

-17β‐Estradiol – Most potent
-Estrone – Less potent
-Estriol – Less potent. Dominant form during pregnancy (synthesized in the placenta)

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15
Q

synthetic estrogens

A

drugs with estrogenic activities (steroidal and non-steroidal)

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16
Q

phytoestrogens

A

estrogen-mimetic compounds in plants (flavonoids)

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17
Q

environmental estrogens

A

compounds used in the manufacture of plastics (bisphenol, alkyl-phenols, phthalate products)

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18
Q

metabolism and excretion of estrogens

A

-Metabolized in the liver mostly and excreted to the bile and to the urine.
-Conjugated estrogens in the bile can be hydrolyzed in the intestine and reabsorbed (enterohepatic circulation).
-Orally administered estrogens have a high ratio of hepatic to peripheral effects; can be avoided by using a routes that avoid first-pass liver exposure

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19
Q

physical effects of estrogen on female maturation

A

-Development of the vagina, uterus, and uterine tubes
-Stromal development and ductal growth in the breast
-Accelerated growth phase and the epiphyseal closure
-Growth of axillary and pubic hair
-Alteration in the distribution of body fat to produce female body contours
-Pigmentation in the skin (nipples, areolae, and genital region)

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20
Q

physical effects of estrogen on endometrial effects

A

-Development of endometrial lining during menstrual cycles
-Prolonged exposure leads to hyperplasia of the endometrium and abnormal bleeding.

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21
Q

physiological effects of estrogen on metabolic and cardiovascular effects

A

-Decrease in the rate of resorption of bone
 Estrogen deficiency can lead to osteoporosis.
-Stimulation of synthesis of transcortin and SHBG
-Alteration in the composition of plasma lipids
 Increase in HDL
 Decrease in LDL

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22
Q

physiological effects of estrogen on blood coagulation

A

enhancement of the coagulability of blood

23
Q

physiologial effects of estrogen on CNS

A

mood

24
Q

clinical uses of estrogen

A

-hormone replacement therapy in postmenopausal women
-osteoporosis
-hormonal contraception
-replacement therapy in patients with hypogonadism

25
Q

hormone replacement therapy in postmenopausal women

A

-Relief of CNS disturbances – hot flashes, sweating, flushing
-Relief of symptoms resulting from urogenital atrophy - vaginal dryness, increased risk of infections
-Relief of psychological effects – mood swings, insomnia, depression, nervousness

26
Q

osteoporosis

A

-For post-menopausal osteoporosis only
-Estrogens decrease the rate of bone resorption

27
Q

replacement therapy in patients with primary hypogonadism

A

-Failure of development of the ovaries
-Chromosomal disorders
 Turner syndrome – absence of one or all sex chromosomes
-Castration (oophorectomy)

28
Q

adverse effects of estrogens

A

uterine bleeding
endometrial carcinoma
breast cancer
nausea, headaches, fluid retention, weight gain

29
Q

uterine bleeding

A

-estrogen therapy is a major cause of postmenopausal uterine bleeding.
-Endometrial hyperplasia
-Estrogen should be given cyclically.
-Can be prevented by administration of a progestin in each cycle

30
Q

endometrial carcinoma

A

concomitant use of progestin reduces risk

31
Q

breast cancer

A

-Particularly for a long-term use
-Addition of a progestin does not have a protective effect.

32
Q

17 alpha alkylated estrogens

A

-Ethinyl estradiol, Mestranol, Quinestrol
-17α-alkylation prevents conversion to estrone. –> enhances oral bioavailability and increases the half life.
-3-alkylated ether is quickly dealkylated in vivo.

33
Q

estrogenic esters

A

-Esterification decreases solubility and slows the absorption.
-Slow absorption from the injection site (depot) prolongs the action.–> less frequent injections.
-Estradiol valerate, Estradiol cypionate

34
Q

conjugated estrogens

A

-Usually collected from pregnant mares’ urine (Premarin ®).
-Mixture of estrogens
 50-60% estrone sulfate
 20-30% equilin sulfate
 Other estrogenic substances

35
Q

diethylstilbestrol

A

-Used in 1940 – 1970 to prevent miscarriage.
-increased risk of vaginal adenocarcinoma in women exposed in utero.
-Used in advanced prostate cancer.

36
Q

chlorotrianisene

A

-Postpartum breast engorgement
-Menopause symptoms
-Prostate cancer

37
Q

selective estrogen receptor modulators

A

-SERM
-“Designer estrogens”
-Partial estrogen agonists
 Block the action of stronger estrogens.
-Estrogenic in some tissues and antiestrogenic in others
-Mostly nonsteroidal estrogens
-Hold promise as the alternative for estrogen replacement therapy.

38
Q

structural basis of SERM actvity

A

-Ligand binding domain with an agonist (diethyl stilbestrol) bound
-Helix 12 conformation allows for coactivator binding.
-Ligand binding domain with a selective estrogen receptor modulator (tamoxifen) bound
-Helix 12 conformation blocks coactivator binding.

39
Q

tamoxifen

A

-Prodrug; oxidized in vivo.
-Partial estrogen agonist
-Antiestrogen actions
 Treatment of breast cancer
 Prevents breast cancer in high risk women.
-Estrogenic actions
 Weak estrogen agonist at endometrial cells
 increase the risk for thromboembolic events.
 Prevents osteoporosis.

40
Q

toremifene

A

-Structurally similar to tamoxifen
-SERM
-Used to treat advanced breast cancer

41
Q

ospemifene

A

-Structurally similar to toremifene
-SERM
-Estrogenic effects on the vaginal epithelium
-Used to treat dyspareunia in post-menopausal
women

42
Q

raloxifene

A

-SERM; partial estrogen agonist
-Tissue-specific activities
-Bazedoxifene is a recently approved analog with similar
activities

43
Q

raloxifene estrogen actions

A

-Estrogen actions
-Prevents osteoporosis in postmenopausal women
(approved).
- Decreases LDL levels in blood.
-increases the risk for blood clots.

44
Q

raloxifene antiestrogen actions

A

 Decreases the risk for breast cancer (approved).
 Does not stimulate endometrial cells.
 May cause hot flashes.

45
Q

clomiphene

A

-SERM; partial estrogen agonist
-Increases secretion of FSH and LH by inhibiting negative estradiol feedback.
-Used to stimulate ovulation in women with oligomenorrhea or amenorrhea and ovulatory dysfunction (frequently from polycystic ovary syndrome).
-Polycystic ovary syndrome (PCOS)
-7% of women of reproductive age
-Gonadotropin-dependent ovarian hyperandrogenism
-Anovulation and infertility

46
Q

fulvestrant

A

-Selective estrogen receptor downregulator (SERD)
-Pure estrogen receptor antagonist for the treatment of breast cancer
-Somewhat more effective than SERM in patients who have become resistant to tamoxifen

47
Q

aromatase inhibitors

A

-Block the biosynthesis of estrogens.
-Effective in some patients whose breast cancer has become resistant to tamoxifen.
-Ovulation induction (off-label use)
-Gynecomastia

48
Q

17α‐alkylated estrogens (too many brand
names)

A

-Ethinyl estradiol
-Mestranol
-Quinestrol

49
Q

estrogenic esters

A

-Estradiol valerate (Progynova® )
-Estradiol cypionate (Depo-Estradiol® )

50
Q

conjugates estrogens

A

Estrone sulfate/equilin sulfate (Premarin ® )

51
Q

nonsteroidal estrogen agonist

A

-Diethylstilbestrol (Stilphostrol ® )
-Chlorotrianisene (Tace ® )

52
Q

selective estrogen receptor modulators (SERMs)

A

-Tamoxifen (Nolvadex® , Soltamox ® )
-Toremifene (Fareston ® )
-Ospemifene (Osphena® , Senshio® )
-Raloxifene (Evista® )
-Bazedoxifene (Conbriza® ,Viviant ® )
-Clomiphene (Clomid® )

53
Q

selective estrogen receptor downregulator (SERD)

A

Fulvestrant (Faslodex®)

54
Q

aromatase inhibitor

A

-Anastrazole (Arimidex ®)
-Letrozole (Femara® )
-Exemestane (Aromasin® )

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