Estrogens and antiestrogens Flashcards

1
Q

Natural estrogens

A

Estradiol > Estrone > Estriol

Estradiol, most potent, formed by ovaries

Estrone and Estriol are formed in the liver and adipose from androstenedione. androstenedione and DHEA made by adrenal cortex.

PreMarin- Pregnant Horse Estrogen
Pregnant Marin (Mare)
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2
Q

Synthetic estrogens

A

Steroids:

  • EthinylEstradiol
  • Mestranol
  • Quinestrol

Non-steroidal

  • Dienestrol
  • Methestrol

Conjugated, depot estyrogens
- Estradiol valerate

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3
Q

Steroidal estrogens

A

Ethinylestradiol
Mestranol
Quinestrol

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4
Q

What carrier is estrogen bound to in blood?

A

Sex hormone binding globulin

AND

Albumin

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5
Q

Clinical use for estrogen

A

Primary hypogonadism, hormone replacement; Turner syndrome

Postmenopausal hormone therapy along with progestins

Hormonal contraceptions

Ovarian suppression, dysmenorrhea, excessive bleeding, severe PMS

Hirsutism, Amenorrhea

Last line treatment for prostate cancer, a form of palliative chemical castration

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6
Q

Estrogen SEs

A

Increased risk for endometrial and breast cancers, hyperplasias.

Hypercoagulability

Nausea

Breast tenderness

Hyperpigmentation

Migraines

Cholestasis and gall stones

Hepatic adenomas

Postmenopausal uterine bleeding

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7
Q

What is Diethylstilbestrol?

A

A non-steroidal estrogen that is no longer used.
Was used in the 70’s

Daughters of mom’s who used DES have increased risk for infertility, ectopic pregnancies, and vaginal adenocarcinomas.

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8
Q

Estrogen contraindications

A

Endometrial or breast cancers

Endometriosis

Patients with undiagnosed genital bleeding (endometrial cancer?)

Severe liver disease (unable to process)

Thromboembolism history

Heavy smokers.

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9
Q

What are the SERMs

A
Clomifen
Tamoxifen
Toremifen
Raloxifen
Bazedoxifen
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10
Q

What are the aromatase inhibitors

A

Steroidal:
- Exemestane, Formestane
the steroidal aromatase inhibitors have androgenic effects in women.

Non-steroidal:

  • Anastrozole
  • Letrozole
  • Fadrozole
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