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Therapeutics > Estrogens Drugs > Flashcards

Estrogens Drugs Flashcards

1
Q

17a-alkylated estrogens

A

Ethinyl estradiol
Mestranol
Quinestrol

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2
Q

Ethinyl estradiol

A

17a-alkylated estrogen

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3
Q

Mestranol

A

17a-alkylated estrogen

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4
Q

Quinestrol

A

17a-alkylated estrogen

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5
Q

17a-alkylated estrogen MOA

A

17a-alkylation prevents conversion to estrone -> enhances bioavailability and half life
3-alkylated ether is quickly dealkylated in vivo

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6
Q

Estrogenic esters

A

Estradiol valerate
Estradiol cypionate

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7
Q

Estradiol valerate

A

Estrogenic ester

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8
Q

Estradiol cypionate

A

Estrogenic ester

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9
Q

Estrogenic esters MOA

A

Esterification decreases solubility and slows the absorption
Slow absorption from the injection site (depot) prolongs the action -> less frequent injections
Prodrugs

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10
Q

Conjugated estrogens

A

Estrone sulfate
Equilin sulfate

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11
Q

Estrone sulfate

A

Conjugated estrogen

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12
Q

Equilin sulfate

A

Conjugated estrogen

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13
Q

Conjugated estrogens MOA

A

Usually collected from pregnant mares’ urine
Mix of estrogens
50-60% estrone sulfate
20-30% equilin sulfate
Other estrogenic substances

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14
Q

Non-steroidal estrogens:

A

Diethylstilbestrol
Chlorotrianisene

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15
Q

Diethylstilbestrol

A

Non steroidal estrogen
Used in 1940-1970 to prevent miscarriages
Increased risk of vaginal adenocarcinoma in women exposed in utero
Used in advanced prostate cancer

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16
Q

Chlorotrianisene

A

Non-steroidal estrogen
Postpartum breast engorgement
Menopause symptoms
Prostate cancer

17
Q

SERMS

A

Selective estrogen receptor modulators
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

18
Q

SERM types

A

Tamoxifen
Toremifene
Ospemifene
Raloxifene
Bazedoxifene
Clomiphene

19
Q

Tamoxifen

A

SERM
Prodrug: Oxidized in vivo
Partial estrogen agonist
Antiestrogen actions:
Tx breast cancer; prevents breast cancer in high risk women
Estrogenic actions:
Weak estrogen agonist at endometrial cells
Increases the risk for thromboembolic events
Prevents osteoporosis

20
Q

Toremifene

A

SERM
Structurally similar to tamoxifen
Used to treat advanced breast cancer

21
Q

Ospemifene

A

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

22
Q

Raloxifene

A

SERM; partial estrogen agonist
Tissue-specific activities
Estrogen actions:
Prevents osteoporosis in postmenopausal women (Approved)
Does not stimulate endometrial cells
May cause hot flashes

23
Q

Bazedoxifiene

A

SERM
Recently approved analog of Raloxifene with similar activities

24
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 PCOS)
PCOS:
7% of women of reproductive age
Gonadotropin-dependent ovarian hyperandrogenism
Anovulation and infertility

25
Q

Fulvestrant

A

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

26
Q

Aromatase inhibitors

A

Anastrozole
Letrozole
Exemestane

27
Q

Anastrozole

A

Aromatase inhibitor

28
Q

Letrozole

A

Aromatase inhibitor

29
Q

Exemestane

A

Aromatase inhibitor

30
Q

Aromatase inhibitors MOA

A

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

31
Q

Clinical uses of estrogens

A

Hormone replacement therapy in postmenopausal women (Relief of CNS disturbances, relief of urogenital atrophy symptoms, relief of psychological effects)
Osteoporosis
Hormonal contraception
Replacement therapy in patients with primary hypogonadism
Castration

Therapeutics (61 decks)

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