Professional Documents
Culture Documents
By: Dr Meherunisa
Associate professor
CIMS
Angina
• Atherosclerotic disease, also known as coronary artery disease
(CAD) or ischemic heart disease (IHD), is the most common
cause of mortality worldwide.
• Atherosclerotic lesions in coronary arteries can obstruct blood
flow, leading to an imbalance in myocardial oxygen supply and
demand that presents as
– stable angina (ischaemic chest pain)
– an acute coronary syndrome
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Angina
• unstable angina.
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Angina
• Transient, self-limited episodes (15 seconds to 15 minutes)
of myocardial ischemia (stable angina) do not result in cellular
death; such as occurs in myocardial infarction (MI).
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Types of Angina
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Stable Angina
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Unstable angina (Acute coronary syndrome)
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Prinzmetal's or variant or vasospastic angina
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Prinzmetal's or variant or vasospastic angina
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Determinants of the volume of oxygen required by the heart.
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Angina-precipitating factors:
Ischemia
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Therapeutic strategies
1. Increase blood flow to ischemic heart muscle and/or
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Nicorandil, Potassium channel activators,
Treatment algorithm for improving symptoms in patients with
stable angina.
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Organic nitrates
Nitroglyserine, Isosorbid dinitrate, Isosorbid mononitrate
• They are effective in all types of angina pectoris.
at therapeutic doses :has 2 major effects
a)Dilation of the large veins resulting in pooling of blood
in the veins which diminish the preload and reduces the
work of the heart
b)Dilates the coronary vasculature providing increased
blood supply to the heart muscle
↓ Preload
↓ Afterload
Relieving vasospasm
Redistribution blood flow
• The total effect is a decrease in myocardial oxygen consumption
because of decreased cardiac work
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A. Mechanism of action
• relax vascular smooth muscle
by their intracellular
conversion to nitrite ions, to
nitric oxide,
• activates guanylate cyclase
(GC) and increases the cGMP.
• dephosphorylation of the
myosin light chain, vascular
smooth muscle relaxation.
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Pharmacokinetics of Nitroglycerine
• Prototype: nitrate
• significant first-pass effect metabolism of nitroglycerin occurs
in the liver with PO forms
• Therefore, it is common to take the drug either sublingually or
via a transdermal patch,
• The time to onset of action varies from 1 minute for
nitroglycerin to more than 1 hour for isosorbide mononitrate.
• Isosorbide mononitrate owes its improved bioavailability and
long duration of action to its stability against hepatic
breakdown.
• Oral isosorbide dinitrate undergoes denitration to two
mononitrates, both of which possess antianginal activity.
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Time to peak effect and duration of action
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Common nitrate preparations
Glyceryl trinitrate can be taken by sublingual tablet or
spray
The effects start within minutes and last ~30 min
Transdermal patches and I.V preparations are also
available
Isosorbide mononitrate is a longer acting preparation
which is given orally (half-life 4hrs), and slow release
preparations are available.
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Beta Blockers
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Beta Blockers
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Mechanism of Action
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Reasons for Using Nitrates and β-Blockers in
Combination in Angina
Blockers.
by β-Blockers .
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Calcium Channel Blockers (CCBs)
ex : amlodipine, diltiazem, felodipine, nicardipine, nifedipine, verapamil
Mechanism of Action
• Calcium is essential for muscular contraction.
• The CCBs protect the tissue by inhibiting the entrance of Ca+2
into cardiac and smooth muscle cells of the coronary and
systemic arterial beds.
• All CCBs are therefore arteriodilators that cause a decrease in
vascular resistance. Cause peripheral arterial vasodilation
• Reduce myocardial contractility (-ve inotropic action)
• Result: decreased myocardial oxygen demand
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Mechanism of Action
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Calcium-channel blockers
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Calcium Channel Blockers
a dihydropyridine derivative
A- Nifedipine
• a dihydropyridine derivative.
• functions mainly as an arteriolar vasodilator.
• This drug has minimal effect on cardiac conduction or heart
rate.
• Used in variant angina caused by spontaneous coronary
spasm
• Other members of this class, amlodipine, nicardipine, and
felodipine, have similar cardiovascular characteristics except
for amlodipine, which does not affect heart rate or cardiac
output.
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Calcium Channel Blockers
B- nondihydropyridine derivative/ Verpamil
• The diphenylalkylamine
• slows cardiac atrioventricular (AV) conduction directly,
• and decreases HR, contractility, BP, and oxygen demand.
• causes greater -ve inotropic effects than nifedipine, but it is
a weaker vasodilator.
• is extensively metabolized by the liver.
• is contraindicated in patients with preexisting depressed
cardiac function or AV conduction abnormalities.
• Drug Interaction: verapamil increases digoxin levels.
• It also causes constipation.
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Calcium Channel Blockers
C- nondihydropyridine derivative/ Deltiazem
• Its cardiovascular effects similar to verpamil
• Reduce the HR but lesser than verpamil
• Reduce BP
• Relieve coronary artery spasm so used in variant angina
• Can be used in angina in patients with concomitant diseases
I. First-line agents for treatment of:
1. angina,
2. hypertension,
3. supraventricular tachycardia
II. Short-term management of atrial fibrillation and flutter
Very acceptable side effect and safety profile, May cause:
• hypotension, palpitations, tachycardia or bradycardia, constipation,
nausea, dyspnea
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Newer Antianginal Drugs
Sodium Channel Blocker, Ranolazine
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Thank you
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