Progestins

Question 1

Progesterone is the most important progestin and precursor to __________

Answer 1

Estrogens
Androgens
Corticosteroids

Question 2

Progesterone is synthesized in the________

Answer 2

Ovary (corpus luteum), Testis and adrenal glands

Question 3

Progesterone are metabolized in the liver by ________ into __________ and excreted into Urine

Answer 3

Glucoranidation

Pregnanediol (inactive)

Question 4

Progesterone functions to:

Answer 4

Cause maturation and secretory changes in the endometrium following ovulation
Increases basal insulin levels and the insulin response to glucose.
Promotes glycogen storage in the liver.
Competes with aldosterone for the mineralocorticoid receptor.
Causes a decrease in Na+ reabsorption.Increase in aldosterone secretion by the adrenal cortex (in pregnancy)

Question 5

Progesterone is used clinically for_____

Answer 5

Hormonal contraceptive
Hormone replacement therapy
Endometriosis (Suppress growth of endometrial tissue)
Dysmenorrhea

Question 6

Progestins structure, 17-ethynyl group increases_______

Answer 6

Biovailability

Question 7

Name two Progestins

Answer 7

Norgestimate (prodrug for Levonorgestrel)
Levonor(gestrel)
Deso(gestrel) (prodrug for etonogestrel)
Etono(gestrel) (Used in subdermal implant/Vaginal ring)

Question 8

Drospirenenon (4th Gen) is used to negate the side effects of _______ in combination therapy

Answer 8

Ethynyl estradiol.

Question 9

Medroxyprogesterone acetate (1st Gen) is a

Answer 9

Long acting progestetone-only contaceptive. (depot injection)

Question 10

________ is the only progestin with antiandrogenic activity

Answer 10

Drospirenone

Question 11

Hoemonal contraception normally inclucombines______ and _______

Answer 11

Estrogens and progestins

Question 12

Etonogestrel is used in_________

Answer 12

Implantable contaceptives

Question 13

Pharmacological effects of oral contaceptives

Answer 13

Inhibition of ovulation (progestins and extrogens selectively inhibit pituitary function)
Change cervical mucus (thicker to inhibit sperm motility)
Supression of lactation
Stimulation of breast enlargement
Supression of ovarian function

Question 14

What are the severe side effects of oral contaceptive use?

Answer 14

Venous thromboembolic disease (due to estrogens)
MI- Due to androgenic activity of progestins
Can be dangerous in women over 35 who smoke

Question 15

Rifampin’s and Phenytoin’s effect on oral contraceptives

Answer 15

Increases drug metabolizing enzymes in liver and increases rate of metabolism of many drugs including oral contraceptives.

Question 16

Plan B uses _________ at a high dose.

Answer 16

Levonorgestrel

Question 17

Mifepristone (RU-486)

Answer 17

Is used a s a postcoital contaceptive (progesterone antagonist) and for abortions when combined with Misoprostol (PGE1 derivative)

Question 18

Danazol is used to treat ________ by inhibiting______ and _________ therefore suppressing ovarian function

Answer 18

Endometriosis
LH
FSH

Question 19

Danazol is contraindicated in_______

Answer 19

Hepatic dysfunction

Pregnancy and breast feeding