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25 Cards in this Set

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Estrogen Antagonists categories (4) and are useful in treating what?
1)impeded estrogens
2)triphenyletyhylene antiestrogens
3)pure antiestrogens
4)SERMs

estrogen-dependent breast cancer
Impeded estrogen ex
estriol
Triphenylethylene antiestrogens ex
tamoxifen
Pure antiestrogens characterisits
NO estrogenic properties, just pure antagonists
SERMs def and ex
Activate the estrogen receptor and also have tissue-specific estrogen agonist or antagonist activity

Raloxifene (evista)
2 types of Aromatase inhibitors and their fxn
1)steroidal
2)nonsteroidal

block conversion of androgens to estrogens, treat estrogen-dependent breast cancer
Steroidal Aromatase inhibitors desc.
will be steroids themselves and try to imitate testosterone (the endogenous Aromatase substrate)
Nonsteroidal aromatase inhibitors desc. (4)
1)contain heterocyclic rings
2)inhibit adrenal steroidogenesis
3)produce inhibition by binding of the N atom in heterocyclic ring w/ heme iron of aromatase
4)contain highly N substituted rings
Nonsteroidal aromatoase inhibitors ex (3)
1)Aminoglutethimide
2)Anastrozole
3)Letrozole
Aromatoase is considered a...
cytochrome P450 enzyme
Progesterone maintains...
pregnancy
Pregnancy is detected (in urine) via...
the progestin 5beta-pregnandiol glucuronide
Why are synthetic progestins needed
b/c progestins are very unstable
Synthetic progestin groups (3)
1)androgen series
2)17alpha-progesterone derivatives
3)Antiprogestins
Mechanism of Antiprogestins?
has large group @ C11
Synthetic Anabolic agents desc. (3)
1)NO sex hormone properties via...
2)alpha methyl @ C17 &
3)slight A ring changes
Androgen drug categories (2)
1)synthetic androgens
2)19-norandrogens
Testosterone has 2 fxns
1)sex hormone
2)androgen
Synthetic androgens are made that way via...
F @ C9 and OH @ C11; destroys anabolic activity and highly increases androgenic activity
Antiandrogens (2 classes)
1)androgen antagonists
2)inhibitors of androgen biosynthesis
Androgen antagonists desc
antagonize the axn of dihydrotestosterone @ androgen receptor
Inhibitors of Androgen biosynthesis target...(3)
1)5alpha reductase
2)17alpha hydroxylase
3)17,20 lyase
Uses of androgen antagonists (4)
1)acne
2)virilization in women
3)hyperplasia of prostate
4)neoplasia of prostate
2 5alpha reducatse inhibitors
1)medrogesterone
2)finasteride
Major therapeutic/structural classifications of sex hormones (6)
1)estrogens
2)progestins
3)aromatase inhibitors
4)estrogen antagonists
5)androgens
6)antiandrogens