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18 Cards in this Set
- Front
- Back
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What are the 3 main types of drugs used to treat heart failure?
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Positive inotropes
Vasodilators Miscellaneous drugs for chronic failure |
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What are the 2 portions of a cardiac glycoside?
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The sugar moiety (glycone) and the steroid moiety (aglycone) also known as genin
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What are cardiac glycosides used for clinically?
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They are positive inotropes used in heart failure
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A major structural feature of cardiac glycosides is this.
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C-17 Lactone ring
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What are plant derived cardiac glycosides called? Animal derived cardiac glycosides?
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Cardenilides
Bufadinolide |
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What is the structural difference between them?
Draw these structures |
Cardenilides contain a 5 membered lactone ring with 1 double bond.
Bufadinolides contain a 6 membered lactone ring with 2 double bonds. |
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In cardiac glycosides, how are all the sugars linked to each other?
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By the Beta - 3 position
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What is Lanatoside A composed of?
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Digitoxigenin + 4 linked sugars
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What is Lanatoside B composed of?
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Lanatoside B is identical to Lanatoside A except, instead of containing Digitoxigenin, it contains Ditoxigenin which has an extra OH at the C-16 position.
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What is Lanatoside C composed of?
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Lanatoside C is identical to Lanatoside A, except it contains Digoxigenin instead of Digitoxigenin which has an extra OH at the C-12 position.
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If you cleave LA and LC you get these two drugs respectively.
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Digitoxin
Digoxin |
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What is the mechanism of action for cardiac glycosides?
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They inhibit the Na/K pump thereby increasing Na which increases Ca in the sarcoplasmic reticulum. This increases contractility.
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The steroid nucleus of cardiac glycosides contribute the most pharmacologically. What is the importance of the sugar chain?
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They are important for how the drug gets to its target. They increase solubility of the molecule.
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Which part of the cardiac glycoside is important for active site binding?
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The 17-lactone ring. Double bond is important also.
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What are the 3 types of drugs used in treatment of angina?
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Beta Blockers
Ca channel blockers Nitrates |
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What 4 classes of drugs are used to treat arrhythmia?
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Na channel blockers
K channel blockers Ca channel blockers Beta blockers |
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What is the mechanism of action for class 1a antiarrythmics?
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They block Na channels and inhibit phase 0 of the action potential.
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What is the protypical class 1a antiarrythmic? Draw this molecule.
Point out the more basic nitrogen. |
Quinidine
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