Estrogenic Compound s

Question 1

Which are the Estrogenic Compounds?

Answer 1

● Natural Estrogens - Estradiol
● Conjugated Estrogens
● Synthetic Estradiol Derivatives
● Nonsteroidal Estrogens
● Raloxifene

Question 2

What are the main characteristics of Natural Estrogens - Estradiol?

Answer 2

● High 1 st pass metabolism

Question 3

What are the main characteristics of Conjugated Estrogens?

Answer 3

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

Question 4

What are the main characteristics of Synthetic Estradiol Derivatives?

Answer 4

● 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 5

What are the main characteristics of Nonsteroidal Estrogens?

Answer 5

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

Question 6

What are the main characteristics of Raloxifene?

Answer 6

● 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
● Adverse effects include hot flashes and leg cramps
and a 3-fold increase in deep vein thrombosis and pulmonary embolism

Question 7

What are SERMS?

Answer 7

SERMs are agents with tissue-selective actions