AntiAnginal Agents Angina Disease symptoms Types of Antianginal

Anti-Anginal Agents Ö Angina Disease, symptoms Ö Types of Anti-anginal Agents Nitrovasodilators, calcium channel blockers and bblockers Ö Nitrovasodilators Structure, physical properties, biochemical mechanism of action, metabolism and pharmacokinetics Ö Calcium channel blockers Types, structure, physical properties, biochemical mechanism of action 10/16/2021 MEDC 604 Anti-anginals 1

Angina 10/16/2021 MEDC 604 Anti-anginals 2

Nitrovasodilators 10/16/2021 MEDC 604 Anti-anginals 3

Structure Nitrate Esters 10/16/2021 MEDC 604 Anti-anginals 4

Pharmacokinetics of Nitrate Esters Amyl nitrite Onset (min) 0. 25 Nitroglycerin 2 30 Isosorbide dinitrate 3 60 Erythrityl tetranitrate 15 180 Pentaerythritol tetranitrate 20 330 10/16/2021 Duration of Action Metabolites (min) MEDC 604 Anti-anginals 1 Active 5

Biochemical Mechanism of Action Nitrate Ester 10/16/2021 NO Guanylate Cyclase MEDC 604 Anti-anginals 6

Calcium channel blockers 10/16/2021 MEDC 604 Anti-anginals 7

Structure of Ca+2 channel blockers 10/16/2021 MEDC 604 Anti-anginals 8

Protein Binding of Calcium Channels Blockers Protein Duration of Binding 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 >90% 24 h Extensive inactive metabolites Verapamil 90% 8 h N-demethyl derivative, ~ 20 % active 10/16/2021 MEDC 604 Anti-anginals 9