ANTIANGINAL DRUGS

DR.FOUZIA
ANGINA
Angina pectoris denotes chest pain caused by accumulation of
metabolites resulting from myocardial ischemia
Pathological aspect of angina
Imbalance b/w oxygen
demand of heart and
oxygen supplied to it
(coronary vessels)
ANGINA
Treatment objectives:
1-↓ oxygen demand
2-↑ delivery (by↑ coronary flow)
TYPES OF ANGINA
1-Stable angina, Effort induced, Classic or Typical angina
2-Unstable angina
3-Variant angina, Vasospastic angina, Prinzemetal angina, Rest angina
4-Acute coronary syndrome
ANTI-ANGINAL DRUGS
1-Organic nitrates
Isosorbide dinitrate, Glyceryl Trinitrate, Nitroglycerine
2-β- blockers
Atenolol Metoprolol
3-Ca channel blockers
Verapamil Diltiazem
4-K channel opener
Nicorandil
5- Na channel blokers
Ranolazine
6-Pfox inhibitors
Trimetazidine
NITRATES
Nitroglycerin(NG) prototype of group
Routes of administration of nitrates:
Oral-- Isosorbide Mononitrate
S/L-- Nitroglycerin, Isosorbide dinitrate
Transdermal-- Nitroglycerin
Inhalational -- Amyl nitrite - obsolete
NITRATES--PHARMACODYNAMICS
Mechanism of action:
Vasodilation
1-Intracellular conversion to nitric acid(NO)
2- ↑ NO ↑Guanylyl cyclase ↑ c GMP
3-Relaxation of vascular smooth muscles:
Dilation of large veins↓Preload
Dilation of coronary vessels ↑ blood flow to cardiac muscles
DENITRATION OF NITRATES WITHIN SMOOTH MUSCLE CELLS RELEASES
NITRIC OXIDE

STIMULATES GUANYLYL CYCLASE

VENODILATION ARTERIOLAR DILATATION

VENOUS POOLING

DECREASED PRELOAD DECREASED AFTER LOAD

DECREASED FLOW TO HEART

DECREASED STRETCHING AND MYOCARDIAL FIBRE TENSION

DECREASED FORCE OF CONTRACTION

DECREASED O2 REQUIREMENT

RELIEF OF ANGINA
NITRATES
Adverse effects:
Headache
Postural hypotension
Tachycardia
Facial flushing
Tolerance (Nitrate-free-interval)
Skin rashes (Transdermal patch)
CALCIUM CHANNEL BLOCKERS (CCBs)
Verapamil & Diltiazem : More effect on heart
Amlodipine : More effect on blood vessels
Mechanism of action:
1-Block L type Ca channels in cardiac muscles &blood vessels
Beneficial effects of CCBs in Angina
1-↓ in contractility of the heart
2-↓HR
3-↓TPR
4-Reversal of vasospasm ( Prophylaxis of vasospastic angina)
CCBs
Adverse effects:
Bradycardia
Atrioventricular block
Cardiac arrest
Heart failure
Flushing
Dizziness
Nausea
Constipation
Peripheral edema (Salt & Water retention)
β-BLOCKERS
β-blockers are first-line drugs in chronic effort angina
Beneficial effects in angina
1-↓ HR
2-↓ Contractility
3-↓ Cardiac output
4- ↓ BP
1,2,3, 4 lead to ↓ myocardial oxygen consumption Relief of angina
and improved exercise tolerance.
β-BLOCKERS
Adverse effects:
1- Bradycardia
2- ↑ in ejection time
3-Fatigue
4-Erectile dysfunction
6-Insomnia
7-Unpleasant dreams
β-BLOCKERS
Contraindications:
1-Asthma
2- Severe bradycardia
3- Artioventricular blockade
4-Bradycardia-tachycardia syndrome
5-Severe unstable left ventricular failure.
MANGAEMENT OF ANGINA
Stable Angina
Nitrates, CCBs, β blockers
Vasospastic Angina
Nitrates , CCBs
β blockers are contraindicated
Unstable Angina & Acute Coronary syndrome:
Combination of Aspirin and Clopidogril (Antiplatelet drugs)
I/V Heparin (Anticoagulant)
Nitrates, β blockers, CCBs(resistant cases)
Lipid lowering drugs + ACEI should also be started