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25 Cards in this Set
- Front
- Back
Estrogen Antagonists categories (4) and are useful in treating what?
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1)impeded estrogens
2)triphenyletyhylene antiestrogens 3)pure antiestrogens 4)SERMs estrogen-dependent breast cancer |
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Impeded estrogen ex
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estriol
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Triphenylethylene antiestrogens ex
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tamoxifen
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Pure antiestrogens characterisits
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NO estrogenic properties, just pure antagonists
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SERMs def and ex
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Activate the estrogen receptor and also have tissue-specific estrogen agonist or antagonist activity
Raloxifene (evista) |
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2 types of Aromatase inhibitors and their fxn
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1)steroidal
2)nonsteroidal block conversion of androgens to estrogens, treat estrogen-dependent breast cancer |
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Steroidal Aromatase inhibitors desc.
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will be steroids themselves and try to imitate testosterone (the endogenous Aromatase substrate)
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Nonsteroidal aromatase inhibitors desc. (4)
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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 |
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Nonsteroidal aromatoase inhibitors ex (3)
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1)Aminoglutethimide
2)Anastrozole 3)Letrozole |
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Aromatoase is considered a...
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cytochrome P450 enzyme
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Progesterone maintains...
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pregnancy
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Pregnancy is detected (in urine) via...
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the progestin 5beta-pregnandiol glucuronide
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Why are synthetic progestins needed
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b/c progestins are very unstable
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Synthetic progestin groups (3)
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1)androgen series
2)17alpha-progesterone derivatives 3)Antiprogestins |
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Mechanism of Antiprogestins?
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has large group @ C11
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Synthetic Anabolic agents desc. (3)
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1)NO sex hormone properties via...
2)alpha methyl @ C17 & 3)slight A ring changes |
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Androgen drug categories (2)
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1)synthetic androgens
2)19-norandrogens |
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Testosterone has 2 fxns
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1)sex hormone
2)androgen |
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Synthetic androgens are made that way via...
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F @ C9 and OH @ C11; destroys anabolic activity and highly increases androgenic activity
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Antiandrogens (2 classes)
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1)androgen antagonists
2)inhibitors of androgen biosynthesis |
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Androgen antagonists desc
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antagonize the axn of dihydrotestosterone @ androgen receptor
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Inhibitors of Androgen biosynthesis target...(3)
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1)5alpha reductase
2)17alpha hydroxylase 3)17,20 lyase |
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Uses of androgen antagonists (4)
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1)acne
2)virilization in women 3)hyperplasia of prostate 4)neoplasia of prostate |
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2 5alpha reducatse inhibitors
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1)medrogesterone
2)finasteride |
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Major therapeutic/structural classifications of sex hormones (6)
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1)estrogens
2)progestins 3)aromatase inhibitors 4)estrogen antagonists 5)androgens 6)antiandrogens |