Estrogenic Compounds

Question 1

What are the characteristics of Natural Estrogens - Estradiol

Answer 1

● Usually administered IM
● High 1st pass metabolism
● Micronized estradiol (Estrace®) is oral and has
higher absorption

Question 2

What are the characteristics of Conjugated Estrogens

Answer 2

● Conjugated estrogenic steroids from mare urine (sulfate conjugate)
● Most common use Hormone Replacement Therapy
● Premarin®

Question 3

What are the characteristics of Synthetic Estradiol Derivatives

Answer 3

● Has ethinyl group (C = C) at C-17 which delays hepatic metabolism

● Major use = estrogen component of contraceptive agents
Examples: Ethinyl estradiol (in contraceptives), mestranol, quinestrol

Question 4

What are the characteristics of Nonsteroidal Estrogens

Answer 4

● Synthetic
● Oral
● Estrogen agonists
● Examples: diethylstilbestrol (DES) – ↑ incidence of
vaginal & cervical cancer in daughters of women
who used it during pregnancy;
● chlortrianesene = (TACE)

Question 5

What are the characteristics of Raloxifene: a Selective Estrogen Receptor Modulator (SERM)

Answer 5

● Synthetic, nonsteroidal estrogen
● SERMs are agents with tissue-selective actions
● Raloxifene (Evista®) is a SERM – acts as a partial
agonist of estrogen receptors in the bone
● Does not have a proliferative effect on the
endometrium
● Has an anti- proliferative effect on estrogen
receptor-positive breast cell cancer lines
● Does not alleviate the vasomotor symptoms
associated with menopause
● Used to treat osteoporosis in post-menopausal
women
● Less risk of breast/endometrial cancer
● Reduces total cholesterol and LDL, but does not
increase HDL
● Adverse effects include hot flashes and leg cramps
and a 3-fold increase in deep vein thrombosis and pulmonary embolism

Question 6

Which are the Estrogenic Compounds?

Answer 6

● Natural Estrogens - Estradiol
● Conjugated Estrogens
● Synthetic Estradiol Derivatives
● Non steroidal Estrogens
● Raloxifene: a  Selective Estrogen Receptor Modulator (SERM)