Park lecture 3 Flashcards
Most important progestin in humans
Progesterone
What is an effect of progesterone being so featureless
All other hormones can be synthesized from progesterone, but due to this there will be some cross reactivity.
Where is progesterone produced
ovary, testes, adrenal gland
during follicular phase only_________ is produced. During Luteal phase, _________&__________ is produced
Estrogen
Estrogen & progesterone
When are the two times progesterone is synthesized in large quantity
Large quantities of progesterone is synthesized by corpus luteum in luteal phase and placenta during pregnancy
Why are synthetic progesterone’s used over progesterone?
Half life of progesterone is 5 minutes (that is why synthetic progestins are used)
How is progesterone inactivated inside the body?
Inactivated by hydrolysis of ketone
When progesterone is excreted in urine, it is converted into______ and conjugated with______
Pregnanediol, glucuronic acid
physiological effect of progesterone on menstruation cycle
Causes maturation of endometrium following ovulation
Metabolic effect of progesterone
Increase basal insulin levels and insulin response to glucose
effect of progesterone on glycogen storage
Increases glycogen storage in liver
Why do women gain weight during pregnancy
Because progesterone promotes storage of progesterone in liver
What does aldosterone do in the body
Increases the amount of Na+ reuptake, increasing the amount of water retained.
Relationship between progesterone and aldosterone
Progesterone binds to aldosterone receptor and antagonizes its function
Effect of progesterone on Na+ levels
Since progesterone antagonizes aldosterone, Na+ levels will decrease in the body.
Name 5 uses of Progesterone
-Hormonal contraception
-HRT in combination with estrogen
-Endometriosis prevention
-Dysmenorrhea
-bleeding disorders
Why is progesterone used in HRT in combination with estrogens
Progesterone decreases some adverse effects of estrogens
which hormone promotes endometrial growth, which hormone suppresses it
Estrogen promotes
progesterone suppresses
What addition to the structure of progestins would add oral activity
C17-a ethynyl moiety
What addition of structure is required for activity
C-18 Methyl or Ethyl are required for activity
Which substitution in progestins has the highest activity but poor oral availability
C-17 B acetyl
Which substituents in progestins are used for oral preparations
17-b OH or esters
What substituent is essential for activity
Ketone at C3
_______ alone is necessary for the growth of endometrium
Estrogen
Introducing which hormone will not allow endometrium to grow fully.
Progesterone
giving which hormone will stop menstrual cycle completely
progesterone
1st generation progestin drug names
Norethindrone
Ethynodiol diacetate
17 ethinyl group use?
Increases bioavailability
replacement f 17-acetyl with OH use?
Increases bioavailability
2nd gen drug names
Lenonorgestrel
Norgestimate
Active isomer of norgestrel
Levonorgestrel
What drug is a pro drug that is converted into levonorgestrel invivo
Norgestimate
3rd gen progestin drug names
Desogestrel
Etonogestrel
Which 3rd gen drug is a prodrug
Desogestrel
Desogestrel is rapidly metabolized to
Etonogestrel
4th gen drug names
Drosperinone
Which drug has weak progesterone activity
Progesterone
which drug has antimineralcorticoid activity
drosperinone
What drug negates side effects of ethynyl estradiol in combination therapy
drosperinone
Which drug has antiandrogenic activities
Drosperinone
Why do progestins frequently have androgenic effect?
They bind to androgen receptor due to dimilar structure as testosterone
why do progestins frequently have hormonal activities other than progesteronic effects
Due to i/a with steroid receptors
which progestin drug has powerful androgen effects
Lenonorgestrel
Most commonly used combination of estrogen drugs
ethynyl estradiol and progestins
Difference between monophasic vs diphasic & triphasic
Monophasic indicates progesterone levels are constant throughout all 21 days, while biphasic and triphasic increases weekly
How is ovulation inhibited
By production of estrogens and progestins
effect of oral contraceptive on uterus
Change in cervical mucus and in uterine endometrium
How does oral contraception affect cervical mucus and uterine endometrium
Decrease in likelihood of conception and implantation
effect of oral contraceptive on breast (combination only)
Stimulation of breasts and supression of lactation
mild adverse effects of oral contraceptive (estrogenic)
HTN, nausea, edema, breast fullness
mild adverse effects of oral contraceptives (progesterone)
increase in appetite, fatigue, breast regression
What is a moderate adverse effect of oral contraception more common in progesterone only contraceptive
Irregularity in menstruation
What are some other moderate adverse effects of oral contraceptives
Amenorrhea
weight gain, acne, hirsutism
severe adverse effects of oral contraceptive due to estrogen?
Venous thromboembolic disease
severe adverse effects of oral contraceptives due to progestin
Myocardial infraction
