Estrogens Flashcards
Three main examples of 17 alpha alkylated estrogens
Ethinyl Estradiol
Mestranol
Quinestrol
Significance of 17alpha alkylation
3 alkylation?
17- prevents conversion of estrone, enhanced bioavailability
3 - quickly removed in vivo
Significance of estrogenic esters
Examples
Esterification decreases solubility, slows absorption
Estradiol valerate, estradiol cypionate
Structural detail about conjugated estrogens that matters. Name it
Has Sulfur group added on
Premarin (Estrone+Equilin sulfate)
functional difference betwen SERMS and estrogens
SERMS block helix 12 from cofactor activating
Two man non-steroidal estrogens + their use
Diethyl stilbestrol (advanced prostate cancer) Chlorotrianisene (menopause, prostate cancer)
Tamoxifen is used for…
Structural detail..
Antiestrogen actions in breast cancer
No OH group, but added by the body
Use of Reloxifene
Prevents osteoporosis in postmenopausal
Decreases LDL
Increases clot risk
Decreases breast cancer risk
Important details on the SERM Clomiphene
Increases FSH and LH (stops negative feedback)
Stimulates sovulation
Details on Fulvestrant
SERD
More effective thean SERM in tamoxifen resistant patients
Three important aromatase inhibitors
Anastrozole
Letrozole
Exemestane
2nd generation progestins
Levonorgestrel
Norgestimate (prodrug of levonorogestrel)
3rd generation progestins
etonogestrel
Desogestrel (prodrug of etonogestrel)
These are the ones used in subdermal implants
Significance of Drospirenone
Weak progestin, but negates the side effects of ethynyl estradiol in combination therapy
Significance of Medroxyprogesterone acetate
1st gen progestin
Used for depot injection as long acting progesterone only contraceptive
