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Anti-Anginal Agents

Anti-Anginal Agents. Angina Disease, symptoms Types of Anti-anginal Agents Nitrovasodilators, calcium channel blockers and b -blockers Nitrovasodilators Structure, physical properties, biochemical mechanism of action, metabolism and pharmacokinetics Calcium channel blockers

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Anti-Anginal Agents

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  1. Anti-Anginal Agents • Angina Disease, symptoms • Types of Anti-anginal Agents Nitrovasodilators, calcium channel blockers and b-blockers • Nitrovasodilators Structure, physical properties, biochemical mechanism of action, metabolism and pharmacokinetics • Calcium channel blockers Types, structure, physical properties, biochemical mechanism of action MEDC 604 Anti-anginals

  2. Angina MEDC 604 Anti-anginals

  3. Nitrovasodilators MEDC 604 Anti-anginals

  4. Structure Nitrate Esters MEDC 604 Anti-anginals

  5. Onset (min) Duration of Action (min) Metabolites Amyl nitrite 0.25 1 Nitroglycerin 2 30 3 60 Active Isosorbide dinitrate Erythrityl tetranitrate 15 180 Pentaerythritol tetranitrate 20 330 Pharmacokinetics of Nitrate Esters MEDC 604 Anti-anginals

  6. Nitrate Ester NO Guanylate Cyclase Biochemical Mechanism of Action MEDC 604 Anti-anginals

  7. Calcium channel blockers MEDC 604 Anti-anginals

  8. Structure of Ca+2 channel blockers MEDC 604 Anti-anginals

  9. Protein Binding Duration of Action Metabolites Amlodipine >95% 24 h phenyl hydroxylations, inactive Nicardipine 95% 3 h phenyl hydroxylations, 1 active <1% Diltiazem ~80% 6 h iv desacetyl derivative, ~ 50 % active Bepridil Extensive inactive metabolites >90% 24 h Verapamil 90% 8 h N-demethyl derivative, ~ 20 % active Protein Binding of Calcium Channels Blockers MEDC 604 Anti-anginals

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