Progestins

Question 1

Functions as a hormone and precursor to the estrogens, androgens and corticosteroids

Answer 1

Progesterone

Question 2

Inactive form of progesterone

Answer 2

Pregnanediol

Question 3

SAR Progesterone

Answer 3

Question 4

2nd gen progestin; high oral bioavailability
Used in intrauterine devices (IUDs)
What is its active form?

Answer 4

Levonorgestrel
Active form- levo

Question 5

Prodrug
Converted to levonorgestrel oxime and then to levonogestrel in vivo

Answer 5

Norgestimate

Question 6

3rd generation progestin; prodrug
Rapidly metabolized to etonogestrel
High oral bioavailability

Answer 6

Desogestrel

Question 7

The active form of desogestrel
Structurally analogous to levonorgestrel
Used in the subdermal implant (Nexplanon) or the vaginal ring (Nuvaring)

Answer 7

Etonogestrel

Question 8

4th gen progestin
Relatively weak progestogenic activity
Antimineralocorticoid activity
Negates side effects of ethynyl estradiol in combination therapy

Answer 8

Drospirenone

Question 9

1st gen progestin
Used for depot injection (Depo-Provera) as a long-acting progesterone-only contraceptive

Answer 9

Medroxyprogesterone acetate (MPA)

Question 10

SPRM; Used as an emergency contraceptive
Can be effective up to 5 days after unprotected sex
SE: nausea, abdominal pain

Answer 10

Ulipristal acetate (Ella)

Question 11

Progesterone antagonist
Abortifacient (combo with misoprostol) up to 70 days
SE: Nausea, vomiting, bleeding

Answer 11

Mifepristone (RU-486)

Question 12

Weak androgen, weak progestin and antiestrogen
Effective for endometriosis by inhibiting surges of LH and FSG and suppress ovarian function (atrophy of endometrium)
Adverse effects: weak androgenic activity; weight gain, decreased breast size, acne, oily skin, hirsutism
Contra: hepatic dysfunction, pregnancy and breast feeding

Answer 12

Danazol