Progestins

Question 1

Medroxyprogesterone acetate

Answer 1

contains the 21 carbon skeleton of progesterone
Agents are highly selective and have a spectrum of activity similar to progesterone
Also a long lasting progesterone for long term contraceptive action

Question 2

Norethindrone, Norgestrel

Answer 2

derived from 19-nortestosterone
Compounds with “nor” lack the C 19, 20, 21 carbons found in progesterone and resemble testosterone
Have protestation activity, but also have androgenic effects
Also used as progestin ONLY contraceptives and preventing the LH surge, and other contraceptive effects on cervical mucus and endometrial lining

Question 3

Norgestimate

Answer 3

Third generation drug
no estrogenic effects
Drosperidone- aldosterone antagonist & progestin
can cause blood clots

Question 4

MOA of progesterone action

Answer 4

progesterone receptor is expressed in the female reproductive, mammary gland, CNS, an the pituitary

Question 5

Therapeutic uses of progestins

Answer 5

1. contraception
2. w/ estrogen for hormonal replacement therapy in postmenopausal women
   Also can be used in ovarian suppression- dysmenorrhea, endometriosis, uterine bleeding

Question 6

Mifepristone

Answer 6

derivative of 19-nor progestins
COMPETITIVE INHIBITOR of progesterone and glucocorticoid binding to their respective receptors
MOA: causes abortion by blockade of progesterone receptors, leading to detachment of the blastocyst

Question 7

Ulipristal

Answer 7

selective progesterone receptor modulator acts as partial agonist

Question 8

Where does negative feedback from progesterone go?

Answer 8

hypothalamus and pituitary

Question 9

where does negative feedback from estrogen go?

Answer 9

primarily on the pituitary

Question 10

Monophonic Oral Contraceptives

Answer 10

same amount of estrogen and progestin are in each tablet, which is taken for 21 days. Last 7 tablets are inert, may contain iron

Question 11

Biphasic Oral Contraceptives

Answer 11

2 different tablets containing varying amounts of active ingredients taken at different times in 21 day cycle

Question 12

Triphasic Oral Contraceptives

Answer 12

3 different tablets containing varying amounts of active ingredients to be taken at different times in 21 day cycle

Question 13

MOA of combination Oral Contraceptives

Answer 13

estrogens suppress FSH and thus, prevent development of the dominant follicle. Estrogen also potentiates the action of the progestin component, suppressing the LH surge
Ovulation is blocked by progestin
Estrogen stabilizes the endometrial lining

Question 14

Side effects of OC, estrogen component

Answer 14

nausea & vomiting
cramping
fluid retention
dizziness and headache

Question 15

Side effects of OC, progestin component

Answer 15

spotting and breakthrough bleeding
weight gain
Acne
Hirsutism

Question 16

Risk of OC in smokers

Answer 16

increase risk of cardiovascular disease, particularly MI

risk of venous thromboembolism