Progestins

Question 1

Most important progestin in humans

Answer 1

Progesterone

Question 2

Function of progesterone

Answer 2

functions as a hormone and also a precursor to the estrogens, androgens and corticosteroids

Question 3

Where is progesterone synthesized?

Answer 3

in the ovary, testis, and the adrenal glands

by the corpus luteum in the ovary in the luteal phase and by the placenta during pregnancy

Question 4

Metabolism/excretion of progesterone

Answer 4

almost completely metabolized in one passage through the liver; converted to pregnanediol and conjugated with glucuronic acid; excreted into the urine

Question 5

Physiologic effects of progesterone

Answer 5

Menstruation cycle; increases basal insulin levels and insulin response to glucose; promotes glycogen storagein the liver; interferes with aldosterone; depressant and hypnotic effects on the brain

Question 6

Clinical uses of progesterone

Answer 6

Hormonal contraception; hormone replacement therapy in combination with estrogens; endometriosis; dysmenorrhea; bleeding disorders

Question 7

Progestins

Answer 7

Levonorgestrel
Norgestimate
Desogestrel
Etonogestrel
Drospirenone
Medroxyprogesterone acetate

Question 8

Levonorgestrel

Answer 8

2nd generation progestin; high oral bioavailability

Question 9

Norgestimate

Answer 9

prodrug; converted to levonorgestrel oxime then to levonogestrel in vivo

Question 10

Desogestrel

Answer 10

3rd generation progestin; prodrug

Question 11

Etonogestrel

Answer 11

used in the subdermal implant or the vaginal ring

Question 12

Drospirenone

Answer 12

4th generation progestin; antimineralocorticoid activity

Question 13

Medroxyprogesterone acetate

Answer 13

1st generation progestin; used for depot injection as a long acting progesterone-only contraceptive

Question 14

Types of hormonal contraception

Answer 14

Monophasic, biphasic, triphasic, continuous progestin therapy without estrogen

Question 15

Pharmacological effects of oral contraceptives

Answer 15

inhibition of ovulation; suppression of ovarian function; change in the cervical mucus and in uterine endometrium; stimulation of breasts

Question 16

Mild effects of oral contraceptives

Answer 16

nausea, hypertension, edema, breast fullness (estrogens)

increased appetitie, fatigue, breast regression (progestins)

Question 17

Moderate effects of oral contraceptives

Answer 17

Irregularities in menstruation; weight gain, acne, hirsuitism, amenorrhea

Question 18

Severe effects of oral contracepives

Answer 18

VTs, MIs

Question 19

Drug interactions with oral contraceptives

Answer 19

increase blood levels of other steroids; anticonvulsants; antibiotics

Question 20

Mifepristone

Answer 20

progesterone antagonist; postcoital contraceptive; abortifacient in combination with misoprostol

Question 21

Danazol

Answer 21

inhibits the surges of LH and Fsh and suppresses ovarian function