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Cardenolides= 5 ring unsaturated
Bufadienolides= 6 ring conjugated |
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All glycoside contain these two portions |
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Sugar (glycoside)
aglycone (steroid) |
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Cis part of glycosides
Trans part of glycosides
[image] |
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Cis part of glycosides= A-B, C-D
Trans part of glycosides= B-C |
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This group on glycosides has a major impact on partitioning and pharmacokinetoics |
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Glycoside C-3 aglycone portion connected to mono or polysach by |
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Beta-1,4-glycosidic linkages |
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Definition
Inhibition of NA/K atpase in myocardium
(5 membered ring interacts w/ Mg2+) |
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Definition
provide critical hydrophobic and hydrophilic intrxn in the Na/K atpase pump
(cardiac glycoside activity) |
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Digoxin half life
Digoxin metab by..... |
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Definition
1.5 to 2 days in pt w/ normal renal func
Metab by PgP pump....Rx intrxns cause toxicity |
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Definition
-INHIBIT HYDROLYSIS OF cAMP
Milrinone (Primacor) **DOC due to selectivity & shorter 1/2 life
Inamrinone (Inocor) |
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MOLSIDOMINE (corvaton)
ORAL NO DONOR VASODILATOR TX OF HF
MOLECULAR O2 IS REQUIRED TO RELEASE NO FROM SIN-1A |
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Spironolactone (Aldactone) |
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Most potent minaralocoticoid |
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In spironolactone the ______constituent is important sterically for binding MR rec |
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Definition
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90% of SPironolcatone is metab to its active form __________ |
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Definition
CANRENONE----more potent than spironolactone |
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Eplerenone has the C7 substituent, lactone ring, and _______ |
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Definition
9alpha,11alpha-epoxy group |
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DUe to this group eplerenone has a 20 to 40 fold lower affinity for MR receptor than spironolactone |
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Be careful with ______ and eplerenone |
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Serious potentially fatal side effect of MR antagnists |
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EPLERENONE is more selective Aldosterone antagonist bc |
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Definition
no inhib effects on androgen receptor, glucocorticoid receptor, and progesterone receptor |
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eplerenone has _______side effects compared to ________ |
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Definition
less side effects than spironolactone |
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Spironolactone competitively inhibits |
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Definition
Aldosterone from binding MR |
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Term
cAMP is the main second messenger of the _____ |
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Definition
cAMP is the main second messenger of the β-adrenergic receptor (β-AR) pathway producing positive chronotropic, inotropic, and lusitropic effects during sympathetic stimulation. |
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