L14 Progestins

Question 1

List the general physiological effects of progesterone

Answer 1

menstruation cycle
metabolic effects
interference with aldosterone
depressant & hypnotic effects on the brain

Question 2

What are physiological effects on the menstrual cycle caused by progesterone?

Answer 2

Causes the maturation and secretory changes in the endometrium following ovulation

Question 3

What are physiological effects on metabolism caused by progesterone?

Answer 3

• Increases basal insulin levels and the insulin response to glucose
• Promotes glycogen storage in the liver

Question 4

What are physiological effects caused by progesterone’s interference with aldosterone?

Answer 4

• 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

List the clinical uses of progestins

Answer 5

• hormonal contraception
• HRT in combination with estrogens
• endometriosis
• dysmenorrhea
• bleeding disorders

Question 6

What is the clinical role of progestins when used as part of HRT with estrogens?

Answer 6

They can prevent some adverse effects of estrogens (uterine bleeding and endometrial carcinoma)

Question 7

What is the clinical role of progestins when used to treat endometriosis?

Answer 7

Progestins suppress the growth of endometrial cells, preventing them from growing outside of the uterine cavity

Question 8

What is the role of a 17a-ethynyl moiety on a progestin?

Answer 8

oral activity

Question 9

What is the role of a C-18 methyl or ethyl group on progestins?

Answer 9

it is required for activity

Question 10

What is the role of the ketone at the 3 position on progestins?

Answer 10

it is essential for activity & can be introduced by in vivo oxidation

Question 11

What is the role of a 6-Me group on progestins?

Answer 11

it enhances activity

Question 12

What are the pharmacological effects of Oral Contraceptives?

Answer 12

• inhibition of ovulation (estrogen & progestin)
• suppression of ovarian function
• change in the cervical mucus & in the uterine endometrium, which decreases in the likelihood of conception & implantation
• breast enlargement & suppression of lactation for combo products

Question 13

List the types of hormonal contraceptives

Answer 13

• combinations of estrogens & progestins
• continuous progestin therapy w/o estrogen
• Oral, implantable, IUD, or depot injection

Question 14

List the mild adverse effects of OCs

Answer 14

• caused by estrogens: nausea, HTN, edema, breast fullness
• caused by progestins: increased appetite, fatigue, breast regression

Question 15

List the moderate effects of OCs

Answer 15

• common in progestin-only: irregular menstruation / breakthrough bleeding
• common for combo products: weight gain, acne, hirsutism
• amenorrhea

Question 16

List the severe effects of OCs

Answer 16

• can be dangerous in women > 35 who smoke
• venous thromboembolic disease (estrogens)
• MI (androgenic activity of progestins)