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52 Cards in this Set
- Front
- Back
What are the two types of adrenal corticoids?
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Glucocorticoids, & Mineralcorticoids
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What are the steroid hormones made from?
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Cholesterol
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What do the mineralocorticoids do?
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Control cellular electrolytes (Na, K) and water balance
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What do glucocorticoids do? (3)
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1) regulate carbohydrates, fat, and protein metabolism
2) regulate the inflammatory response 3) involved in reaction to stress, allergic response |
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What are the therapeutic uses of estrogens? (3)
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1) birth control, 2) HRT, & 3) Treatment of estrogen deficiency from ovarian failure
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Where are estrogens and progestins synthesized?
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ovaries and placenta
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What are the three functions of estrogen?
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1) reproduction and development of female sex organs
2) role in ovulation and pregnancy 3) increase bone density |
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Function of progestins (3)
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1) maintains pregnancy, 2) inhibits follicular maturation and ovulation, & 3) prevents spontaneous uterine contraction
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Therapeutic uses of progestins (3)
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1) birth control, 2) reduction of risk of endometrial cancer, & 3) breast or endometrial carcinoma
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Therapuetic uses of androgens (3)
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1) androgen replacement therapy (anabolic use), 2) osteoporosis treatment- relieve bone pain, & 3) metastatic breast carcinoma
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Where are androgens synthesized?
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Testes and andrenal cortex
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What are the two androgenic activities of androgens?
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1) growth and development of male sex organs & 2) development of secondary sexual characteristics
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Two anabolic activities of androgens
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1) development of muscle mass
2) reverse catabolic or tissue-depleting processes |
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Beta stereochemistry
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point OUT towards the reader
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Alpha stereochemistry
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point AWAY from the reader
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Number of carbons in cholestanes?
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27
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Number of carbons in cholanes?
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24
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Number of carbons in pregnanes?
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21
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Number of carbons in androstanes?
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19
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Number of carbons in estranges?
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18
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hydroxysteroid dehydrogenase
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oxides alcohol to ketone
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3-oxosteroid-4,5-isomerase
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isomerizes the double bond from the 5-6 to the 4-5 position
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When are aromatase inhibitors used?
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For the treatment of estrogen-dependent cancers
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dehydrogenase
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depends on the environment (NADP+ or NADPH)
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Lyase
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cleaves c-c bonds
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What is another name for reductant dehydrogenase?
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oxioreductase
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What is the effect of glucocorticoids?
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Greatly turns down immune activity
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What is one of the key differences in mineralocorticoid activity?
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It is NOT anti-inflammatory
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Luteinizing hormone
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Heterodimeric glycoprotein hormone that stimulates the synthesis of testosterone and progesterone
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Mechanism of action of LH
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LH binds to its cell surface receptor and increase the intracellular cAMP level via activation of a G-protein, then cAMP activates cholesterol esterase's, which generates free cholesterol.
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G:M of cortisone
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0.8:0.8
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G:M of hydrocortisone
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1:1
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G:M of prednisone
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3.5:0.6
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G:M of prednisolone
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4:0.6
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G:M of methyprednisone
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5:0
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G:M of dexamethasone
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30:0
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Effect of the 1-2 double bond
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increases the G activity
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Effect of 6-Me
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Abolishes the M activity
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Effect of a 9-F
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No M activity and very high G
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Effect of 16-Me
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No M activity and very high G
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Estradiol
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the most potent endogenous estrogen
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Estradiol dehydrogenase reaction
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Interconvertible by estrone and estradiol
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What is the most active anti-inflammatory steroid with NO minerocorticoid activity?
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Dexmethasone
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How do you block the oxidation of estradiol?
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Block C-17 alkyne- makes it more potent than estradiol
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What are the structural requirements for non-steroidal estrogens?
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rigid structure, fixed distance between the -OH's or -OMe's
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How is estrogen metabolized?
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hydroxylated at the ortho position to the 3-OH group (2/4-hydroxylase) to produce catechol estrogens
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Is the C-19 group necessary for pro gestational activity?
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NO
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Does the 17alpha group maintain progestin activity?
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YES
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Requirements for anabolic activity (2)
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1) steroid skeleton, & 2) alkyl group at 17 alpha
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Requirements for adrogenic activity? (2)
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1) steroid skeleton, 2) ketone on 17 position
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19-norandrogens structural activity
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removal of the 19-CH3 group reduces androgenic properties and maintains anabolic activity
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19-norandrogens (2 examples)
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Ethylestrenol & Norethandrolone
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