Gonadal hormones & inhibitors

Question 1

Ethinyl estradiol

Answer 1

• MOA
• activation of estrogen receptors
• Clinical
• hypogonadism in females, hormone replacement therapy, contraceptives, osteoporosis in postmenopausal women
• Kinetics
• oral, parenteral, transdermal
• CYP dependent metabolism
• enterohepatic recirculation occurs
• Tox, int.
• lots, check book

Question 2

Progesterone

Answer 2

• MOA
• activates progesterone receptors
• Clinical
• hormone replacement therapy, contraceptives
• Kinetics
• oral, parenteral, transdermal
• CYP dependent metabolism
• enterohepatic recirculation occurs
• Tox, int.
• weight gain, reversible decrease in bone mineral density (high doses)

Question 3

SERMs

Answer 3

• Tamoxifen
• estrogen antagonist in breast tissue and CNS
• estrogen agonist in liver and bone
• prevention and adjuvant treatment of hormone-responsive breast cancer
• oral
• tox: hot flushes, thromboembolism, endometrial hyperplasia
• Raloxifene
• antagonist effects in breast, CNS, endometrium
• agonist effects in liver
• osteoporosis and prevention of breast cancer
• Clomiphene
• antagonist effect in pituitary increases gonadotropin secretion
• used for ovulation induction

Question 4

Anastrazole, exemestane

Answer 4

• MOA
• reduces estrogen synthesis by inhibiting aromatase enzyme
• Clinical
• adjuvant treatment of hormone-responsive breast cancer
• Kinetics
• oral
• Tox, int.
• flushes, reduced bone mineral density, joint symptoms
• Exemestane
• irreversible aromatase inhibitor

Question 5

Mifepristone

Answer 5

*

Question 6

UNFINISHED!