ANTI-ANGINAL DRUGS

PHCL-L3-Cardiopharm-lecture10

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introduction
Angina pectoris
The types of angina
Stable angina Unstable angina Variant angina

The pathologic physiological mechanism of angina:

an imbalance between the myocardial

oxygen supply and demand

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major determinants of myocardial oxygen consumption: myocardial basic metabolism heart rate contractility ventricular volume wall tension ventricular pressure ejection time blood pressure (peripheral resistance)

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The mechanism of antianginal drugs Decrease myocardial oxygen consumption Increase myocardial blood and oxygen supply antiplatelet & antithrombosis

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Classification of Anti-Angina Drugs

Organic nitrates -adrenoceptor blocking drugs calcium antagonists other antiagina drugs

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Organic nitrates
Nitroglycerin, isosorbide dinitrate isosorbide mononitrate

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2.Pharmacological mechanism Organic nitrates

NO
guanylyl cyclase

cGMP
cGMP dependent protein kinase

intracellular Ca2+
vascular smooth muscle relaxation
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Pharmacological action of Organic Nitrates 1. decrease myocardiac oxygen consumption

dilate venousdecrease blood returning to heartdecrease ventricular end-diastolic volume and pressure (large dose) dilate arterialdecrease peripheral resistancedecrease afterload

2. 3. 4.

increase blood supply to ischemia area redistribution of coronary blood flow Inhibit of platelet aggregation, increase the release of PGI2 and CGRP
CGRP: (calcitonin gene-related peptide ) The neuropeptide is widely distributed in neural tissue of the brain, gut, perivascular nerves, and other tissue. It is a potent endogenous vasodilator

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-adrenoceptor blocking drugs

The mechanism of antiangina
1. decrease myocardial oxygen consumption
block -adrenoceptor inhibit myocardial contractility and heart

rate

2. improve blood and oxygen supply to ischamia area 3. lower heart rateprolong diastolic perfusion timeincrease endocardium flow 4. promote oxygen to dissociate from HbO2

cilinical uses
stable and unstable angina; myocardia infarction

contraindication
variant angina, bronchial asthma, bradycardia, The

combined use with nitroglycerin

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calcium antagonists
mechanism of antiangina
1. dilate coronary arterial 2. reduction in peripheral vascular resistance 3. negative chronotropic and inotropic, decrease myocardiac oxygen consumpation 4. protect cardiac myocytes 5. Anti-atherosclerosis

clinical used

Variant angina, Stable angina, Unstable angina

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other anti-agina drugs

carvedilol Nicorandil
Activateurs des canaux potassique

molsidomine sodium tanshinon

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