Progestins

Question 1

Progesterone is a precursor for _______, _______, and ________.

Answer 1

estrogen, androgens, and corticosteroids

Question 2

Where are progestins extensively metabolized?

Answer 2

in the liver

Question 3

What are the metabolic effects of progestins?

Answer 3

(1) maturation/maintenance of uterine wall after ovulation
(2) increases insulin levels/insulin response to glucose
(3) competes for MC receptor with aldosterone - increases aldosterone synthesis as compensatory response
(4) depressant/hypnotic effects on brain

Question 4

What are the clinical uses of progestins?

Answer 4

(1) hormonal contraception
(2) hormone replacement therapy
(3) endometriosis (suppresses growth of endometrial cells)
(4) dysmenorrhea
(5) bleeding disorders

Question 5

Which structural modification is essential for oral activity of progestins?

Answer 5

17-ethynyl moiety

Question 6

What structural moieties are necessary for progestin activity?

Answer 6

3 ketone, C18 methyl group

Question 7

Which progestin is used in NuvaRing and in subdermal implants?

Answer 7

etonogestrel

Question 8

Describe the clinically significant properties of the 4th-gen progestin drospirenone.

Answer 8

weak progestin activity, but blocks MC activity leading to less water retention with OC use

Question 9

Which progestin is used as a depot injection?

Answer 9

medroxyprogesterone acetate

Question 10

Which progestin has the highest androgenic activity?

Answer 10

levonorgestrel

Question 11

Describe the pharmacological effects of progestins.

Answer 11

They inhibit ovulation by selective inhibition of the pituitary. They decrease the likelihood of implantation by changing the properties of uterine mucus. They also suppress ovarian function (reversible with discontinuation).

Question 12

What are the side effects associated with oral contraceptives?

Answer 12

N/V, HA, weight gain, VTE, MI, menstrual irregularity, hirsutism (if androgenic progestin), acne, amenorrhea

Question 13

Name some common drug classes that a pharmacist should watch for when a patient is taking an OC.

Answer 13

antibiotics (rifampin, tetracyclines)
phenytoin
glucocorticoids/other steroids

Question 14

What post-coital contraceptive can be effective up to 5 days after unprotected sex? What drug class does it belong to?

Answer 14

Ulipristal acetate (ella) - selective progesterone receptor modulator

Question 15

Mifeprostone

Answer 15

a progesterone antagonist used as a post-coital contraceptive, usually in combination with misoprostol to induce abortion up to 7 weeks post-coitus

Question 16

Danazole

Answer 16

a progestin used for endometriosis

inhibits LH/FSH surge and causes endometrial shedding

side effects result from weak androgenic activity (weight gain, acne, hirsutism, oily skin, decreased breast size)

contraindicated in pregnancy/lactation, hepatic dysfunction