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Anti-Anginal Agents: Submitted By

The document discusses anti-anginal drugs, which are medications used to treat angina pectoris, or chest pain caused by reduced blood flow to the heart. It classifies anti-anginal drugs into three main categories: organic nitrates, calcium channel blockers, and beta blockers. Organic nitrates work to relax and widen blood vessels, calcium channel blockers block calcium ions from entering muscle cells and dilate blood vessels, and beta blockers slow the heart rate to reduce its workload. The document provides examples of common drugs that fall into each category.

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Arvi Khan
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0% found this document useful (0 votes)
66 views34 pages

Anti-Anginal Agents: Submitted By

The document discusses anti-anginal drugs, which are medications used to treat angina pectoris, or chest pain caused by reduced blood flow to the heart. It classifies anti-anginal drugs into three main categories: organic nitrates, calcium channel blockers, and beta blockers. Organic nitrates work to relax and widen blood vessels, calcium channel blockers block calcium ions from entering muscle cells and dilate blood vessels, and beta blockers slow the heart rate to reduce its workload. The document provides examples of common drugs that fall into each category.

Uploaded by

Arvi Khan
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PPTX, PDF, TXT or read online on Scribd
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Anti-anginal

agents
Submitted by,
Group – 9
Shanjida Islam – BPH 067 07410
Tabiku Sultana Orpa – BPH 067 07411
Sumaya Akter – BPH 067 07412
Content

Introduction
▪ Definition
▪ Symptoms
▪ Causes
▪ Types
▪ Risk factors & complications
▪ Diagnosis & treatment strategy.
Classification of Anti-anginal drugs
▪ Organic Nitrates
▪ Calcium Channel Blockers (CCB)
▪ Beta Blockers
Conclusion
Introduction

Coronary artery disease is the narrowing or blockage of the coronary arteries. This condition is usually
caused by atherosclerosis. Atherosclerosis is the build-up of cholesterol and fatty deposits (called plaques)
inside the arteries.
Example –
 Angina Pectoris (Ischemic Heart Disease)
 Acute Coronary Syndrome
 Unstable Angina
 non-ST elevation myocardial infarction (NSTEMI)
 ST-segment elevation myocardial infarction (STEMI)

Angina - Angina pectoris refers to a strangling or pressure-like pain caused by cardiac ischemia. The pain
is usually located substernal but is sometimes perceived in the neck, shoulder and arm, or epigastrium.
Women develop angina at a later age than men and are less likely to have classic substernal pain.
Antianginal drugs are those that prevent, abort or terminate attacks of angina pectoris.
Symptoms

Symptoms of Angina –
Angina symptoms include – Women may also have symptoms such
as:
 chest pain and discomfort,
Nausea
 possibly described as pressure,
Shortness of breath.
 squeezing,
Abdominal pain.
 burning or fullness
Discomfort in the neck,
jaw or back.
Stabbing pain instead of chest pressure
Causes

Angina Causes -
 Angina usually happens because of heart disease.
 A fatty substance called plaque builds up in your arteries, blocking blood flow to your heart muscle.
 This forces your heart to work with less oxygen.
 That causes pain.
 You may also have blood clots in the arteries of your heart, which can cause heart attacks.

Less common causes of chest pain include:


A blockage in a major artery of your lungs (pulmonary embolism)An enlarged or thickened heart
(hypertrophic cardiomyopathy)Narrowing of a valve in the main part of your heart (aortic
stenosis)Swelling of the sac around your heart (pericarditis)Tearing in the wall of your aorta, the
largest artery in your body (aortic dissection)
Types

Types of Angina –

 Stable angina – Results from coronary artery abstraction by atheromatous plaque. Triggered by 4 ‘E
s’: exercise, emotion, cold & eating. Pain – last for 1 – 15 minutes, builds gradually to max: intensity.
Relieved by rest/ administration of nitroglycerin.
 Variant angina (Prinz metal's Angina) – Occurs at rest. Nitroglycerin relieves pain. Calcium
channel blockers – main form of treatment to reduce the incidence of acute events.
 Unstable angina – Result of atherosclerotic progression. High chance of getting MI. Precipitated by
the factors for angina. It occurs at rest (or with minimal exertion) lasting for more than 20 minutes.
Extremely significant to dentistry because of the associated risk of MI.
Risk Factors

Risk factors –
Factors that increase the risk of angina pectoris include:

• Family History: Individuals having a family history of heart disease are at greater risk of developing angina.

• Older Age: Males with 45 years and female with 55 years or more are at increased risk of angina.

• An Inactive Lifestyle: An inactive lifestyle increases cholesterol level and blood pressure, which contribute to angina.

• Stress: Stress raises the blood pressure and also releases the hormones that narrow the artery and increases the risk of angina.

• Smoking and Tobacco Use: Smoking and use of tobacco in any other form damages the walls of an artery and leads to the
formation of plaque (deposits of cholesterol).

• Diabetes: Diabetes increases cholesterol levels and fastens the process of atherosclerosis that leads to angina.

• High Blood Pressure: High blood pressure damages the arteries by hardening them; damaged arteries increase the risk of
angina.

• High blood cholesterol levels: High blood cholesterol levels lead to narrowing of the arteries and reduce the blood flow to the
heart, which leads to angina.
Complications

Complications –
▪ Untreated angina pectoris may lead to several life-threatening complications, such as:
• Severe arrhythmias (irregular heartbeat)
• Heart attack
• Cardiac arrest (unexpected loss of heart functioning)
• Atrioventricular block (loss of electric conduction between arteries and ventricles)
Diagnosis

Diagnosis of Angina Pectoris:


The doctor initiates diagnosis by collecting the family history, medical history and signs and
symptoms of the patient. The doctor recommends diagnostic tests that help in confirming the
condition, it includes:
▪ Electrocardiogram (ECG or EKG): An ECG is a painless procedure that helps in monitoring the
heart health of the patient. An ECG records the electrical impulses produced by the heart. It helps
the doctor to determine the blood flow through the heart.
▪ Stress Test: Angina can be easily diagnosed when the heart is working hard. In this test, the
individual is advised to walk on a treadmill to determine the blood pressure, which is monitored by
ECG. This test helps to identify if physical activity increases the patient’s symptoms.
▪ Echocardiogram: An echocardiogram uses sound waves to capture images of the heart. The
doctor uses these images to determine the location of damaged heart muscles due to poor blood
flow. An echocardiogram is done along with the stress test, which helps in determining the areas of
the heart that are not getting proper blood supply.
Diagnosis (Cont…)

Diagnosis of Angina Pectoris:


▪ Nuclear Stress Test: A nuclear stress test is performed to determine the blood flow to the heart muscle at
rest and during stress. This test uses a radioactive substance and a scanner, which helps in capturing the
images of the heart muscle. This test helps in determining the area of the heart where the blood flow is poor.
▪ Chest X-ray: Chest X-ray is performed to capture the images of the heart and lungs, which helps in
determining the abnormalities in the heart, such as an enlarged heart.
▪ Coronary Angiography: Coronary angiography uses an X-ray and a special dye to examine the blood flow
through the arteries in the heart.
▪ Cardiac Computerized Tomography (CT) Scan: Cardiac CT scan is performed to view the heart and
blood vessels by injecting a specialized dye into the bloodstream. It uses X-rays to capture the detailed
images of the heart, which helps the doctor to determine the structure of the heart and the adjacent blood
vessels without doing any incisions.
▪ Cardiac MRI (Magnetic Resonance Imaging): Cardiac MRI is performed by using a powerful magnetic
field and radio waves to produce detailed images of the heart.
Treatment

Non pharmacological treatments –

You can help prevent angina by making the same lifestyle changes that might improve your symptoms if you
already have angina. These include:
 Quitting smoking.

 Monitoring and controlling other health conditions, such as high blood pressure, high cholesterol and diabetes.

 Eating a healthy diet and maintaining a healthy weight.4.Increasing your physical activity after you get your
doctor's OK. Aim for 150 minutes of moderate activity each week. Plus, it's recommended that you get 10
minutes of strength training twice a week and to stretch three times a week for five to 10 minutes each time.
 Reducing your stress level.

 Limiting alcohol consumption to two drinks or fewer a day for men, and one drink a day or less for women.

 Getting an annual flu shot to avoid heart complications from the virus.
Treatment (Cont…)
Treatment –
Pharmacological treatments –
Doctor might prescribe medicines including:
 Nitrates or calcium channel blockers to relax and widen blood vessels, letting more blood flow to
heart.
 Beta-blockers to slow heart down so it doesn't have to work as hard Blood thinners or antiplatelet
medications to prevent blood clots. Statins to lower your cholesterol levels and stabilize plaque.
These are anti anginal agents.
Classification of Anti – anginal Drugs

Classification of Drugs

Organic Calcium Channel


Beta Blockers
Nitrates Blockers

Dihydropyridines Benzothiazepines Phenylalkylamines Beta 1-selective


Nitroglycerin,
Glyceryl Trinitrate Blockers
Nifedipine Diltiazem 1 - verapamil

Non selective Beta


Blockers

Propranolol Atenolol
(Inderal)
Organic Nitrate

Definition – Organic nitrates are potent vasodilators and are the most widely used antianginal agents
during acute events. They selectively dilate epicardial coronaries and also enhance collateral flow; they
also inhibit platelet aggregation.
They are first line drug; they are effective in stable, unstable & Variant angina. They are simple nitrous &
nitric acid esters of alcohols. They are used in both treatment & prophylaxis against angina attacks.
Examples –
Nitroglycerin (such as Nitro-Dur, Nitro lingual, Nitrostat).
Isosorbide (such as Dilatate, Isoradial).
Nitroprusside (such as Nitro press).
Amyl nitrite or amyl nitrate
Organic Nitrate (Cont….)

Mechanism of action –
Glyceryl trinitrate, isosorbide dinitrate, and isosorbide-5-mononitrate are organic nitrate esters
commonly used in the treatment of angina pectoris, myocardial infarction, and congestive heart failure.
Organic nitrate esters have a direct relaxant effect on vascular smooth muscles, and the dilation of
coronary vessels improves oxygen supply to the myocardium. The dilation of peripheral veins, and in
higher doses peripheral arteries, reduces preload and after-load, and thereby lowers myocardial oxygen
consumption. Inhibition of platelet aggregation is another effect that is probably of therapeutic value.
Effects on the central nervous system and the myocardium have been shown but not scrutinized for
therapeutic importance. Both the relaxing effect on vascular smooth muscle and the effect on platelets
are considered to be due to a stimulation of soluble guanylate cyclase by nitric oxide derived from the
organic nitrate ester molecule through metabolization catalyzed by enzymes such as glutathione S-
transferase, cytochrome P-450, and possibly esterase's. The cyclic GMP produced by the guanylate
cyclase acts via cGMP-dependent protein kinase. Ultimately, through various processes, the protein
kinase lowers intracellular calcium; an increased uptake to and a decreased release from intracellular
stores seem to be particularly important.
Organic Nitrate (Cont….)
Structural Activity Relationship (SAR) –
▪ In a cell free system, the potency of organic nitrate for guanylate cyclase activation is mainly
determined by the number of nitrate groups.
▪ Since nitrate induced activation of guanylate cyclase involve the formation of nitric oxide free radicals,
potency therefore increases as nitric group increases in the group
▪ Increase in lipophilicity due to esterification of the free OH group in isosorbide mononitrate had no
major influence on guanylate cyclase activation

Nitroglycerin Glyceryl trinitrate


Organic Nitrate (Cont….)

Therapeutic uses –
▪ Angina pectoris: Classical and variant Types
▪ Acute Coronary syndromes: Unstable angina and associated with MI (Combination Drugs)
▪ Myocardial Infarction: In evolving MI : IV administration is useful in relieving – 3 things: chest pain,
congestions of chest and reducing the infarct size favouring blood supply to ischemic zone
▪ CHF and LVF: Pooling of blood
▪ Biliary colic: Sl administration
▪ Esophageal spasm: Reduction in esophageal tone (achalasia)
▪ Cyanide Poisoning: Nitrates counter cyanide by producing Methemoglobin – then
Cyanmethemoglobin (Sod. Thiosulfate is given to form Sod. Thiocyanate)
Organic Nitrate (Cont….)

Adverse Effect –
▪ Headache ( dilatation of meningeal artery, disappears with continued use)
▪ Flushing (Cutaneous dilatation of arterioles of the face and neck)
▪ Orthostatic hypotension,
▪ Dizziness
▪ Reflex tachycardia (activation of baroreceptor reflex mechanism)
▪ Salt and water retention
Organic Nitrate (Cont….)
Drug Information –
Drug Name Dose Dosage Form Brand Name Manufacturer
Nitroglycerin 0.3mg, 4mg, 6mg Tablet Nitrosol Beximco
0.4mg powder Pharmaceuticals
Ltd.

Drug Name Dose Dosage Form Brand Name Manufacturer


Glyceryl Trinitrate 400 mcg Spray Anril Square
Pharmaceuticals
Ltd.
2.6mg Tablet Angist ACME
Laboratories Ltd.
Calcium Channel Blockers

Definition – Calcium channel blockers, calcium channel antagonists or calcium antagonists are a group of
medications that disrupt the movement of calcium through calcium channels. Calcium channel blockers
are used as antihypertensive drugs, i.e., as medications to decrease blood pressure in patients with
hypertension.
Examples of calcium channel blockers include:
Amlodipine (Norvasc)
Diltiazem (Cardizem, Tiazac, others)
Felodipine.
Nicardipine.
Nifedipine (Adalat CC, Procardia)
Verapamil (Callan, Verlan)
Calcium Channel Blockers (Cont.)

Mechanism of Action –
Several types of calcium channels occur, with a number of classes of blockers, but almost all of them
preferentially or exclusively block the L-type voltage-gated calcium channel.

• 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 arteria dilators that cause a decrease in vascular resistance. Cause peripheral
arterial vasodilation
• Reduce miocardio contractility (-ve inotropia action)
• Result: decreased myocardial oxygen demand
Calcium Channel Blockers (Cont.)

Mechanism of Action –
Calcium Channel Blockers (Cont.)

Structural Activity Relationship (SAR) –


A structure-activity relationship study has been done on 8 compounds with the activity known as ‘Ca2+
channel blockers’. Conformational analysis was carried out using a molecular mechanics method. The
3D-QSAR approach was used and the most polar functional groups present in all the molecules were
considered. Eight interatomic distances are necessary to define the relative spatial disposition of these
relevant molecular fragments. The structure-activity relationship between interatomic distances and
biological activity was performed using statistic and chemometric methods. In particular, with Principal
Component Analysis, it was possible to reduce the number of interatomic distances: only six of the eight
distances are sufficient to describe the system in a useful way. A classification method was iteratively used
to select the most probable conformations linked to the biological activity and to build a model able to
classify conformations according to their biological behavior. Cluster analysis on the active selected
conformations subsequently allowed the identification of two different geometrical patterns for the active
compounds. Finally the validity of the model was verified by correctly predicting the activity of other
molecules not used in the construction of the model but possessing known activity.
Calcium Channel Blockers (Cont.)

Dihydropyridine Verapamil Nifedipine

Benzothiazepine
Phenylalkylamines
Diltiazem
Calcium Channel Blockers (Cont.)

Therapeutic Uses –
 In addition to high blood pressure, doctors prescribe calcium channel blockers to prevent, treat or
improve symptoms in a variety of conditions, such as:
 Coronary artery disease
 Chest pain (angina)
 Irregular heartbeats (arrhythmia)
 Some circulatory conditions, such as Raynaud's disease
 For black people and older people, calcium channel blockers might work better than other blood
pressure medications, such as beta blockers, angiotensin-converting enzyme (ACE) inhibitors or
angiotensin II receptor blockers.
Calcium Channel Blockers (Cont.)

Adverse Effects –
 Constipation & Dizziness
 Fast heartbeat (palpitations)
 Fatigue
 Flushing
 Headache, Nausea & Rash
 Swelling in the feet and lower legs
 Avoid grapefruit products while taking certain calcium channel blockers.
 Grapefruit juice interacts with the drug and can affect heart rate and blood pressure. This can cause
symptoms such as headaches and dizziness.
Calcium Channel Blockers (Cont.)

Drug Information –
Drug name Dose Dosage Form Brand Name Manufacturer
Verapamil 40 & 80 mg Tablet Veracal Icepta
Pharmaceuticals
LTD.
Nifedipine 20 mg Tablet Nidipine – SR Square
Pharmaceuticals
LTD.
Diltiazem 90 mg Tablet Diltizem - SR Square
Pharmaceuticals
LTD.
Beta Blockers
Definition - Beta blockers, also known as beta-adrenergic blocking agents, are medications that reduce
your blood pressure. Beta blockers work by blocking the effects of the hormone epinephrine, also known as
adrenaline. Beta blockers cause your heart to beat more slowly and with less force, which lowers blood
pressure.
Examples –
o Acebutolol (Sectral)
o Atenolol (Tenormin)
o Bisoprolol (Zebeta)
o Metoprolol (Lopressor, Toprol XL)
o Nadolol (Corgard)
o Nebivolol (Bystolic)
o Propranolol (Inderal, InnoPran XL)
Beta Blockers (Cont.)

Mechanism of Action –
 Beta-blockers are a class of drugs used to control symptoms of heart failure that are made worse by
certain hormones called catecholamines.
 The body releases these hormones as part of its response to heart failure. For this and other reasons,
beta-blockers have been shown to be effective for treating most people who have heart failure.
 Beta-blockers may work by slowing the heart rate, which allows the left ventricle (the main pumping
chamber of the heart) to fill more completely.
 Some of these medicines may also help open or widen blood vessels in the body.
 This makes them especially useful in some people with certain forms of heart failure who may also have
high blood pressure.
 Bisoprolol, carvedilol, and metoprolol are some of the beta-blockers that have been tested for use in the
treatment of heart failure.”
Beta Blockers (Cont.)

Structural Activity Relationship (SAR) –


▪ Beta Blockers: derived from isoproterenol (beta agonist)
▪ Substitutions on the benzene ring determines if drug is antagonist or agonist
▪ Levorotatory forms of beta agonists/antagonists more potent than Dextrorotatory forms
▪ Example: Dextrorotatory isomer of Propranolol has <1% of the potency of the Levorotatory form

Propranolol Atenolol
Beta Blockers (Cont.)

Therapeutic uses –

 Myocardial infarction: Propranolol & other beta blockers have a protective effect on the myocardium.

 Migraine: Propranolol is effective in reducing migraine episodes when used prophylactically.

 Hyperthyroidism: In acute hyperthyroidism beta blockers may be lifesaving in protecting against serious cardiac
arrhythmias.

Adverse effect –

 Adverse effect commonly reported by people taking beta blockers include:

 Feeling tired,

 Dizzy or lightheaded (these can be signs of a slow heart rate)

 Cold fingers or toes (beta blockers may affect the blood supply to your hands and feet)

 Difficulties sleeping or nightmares & feeling sick.


Beta Blockers (Cont.)

Drug Information -
Drug Name Dose Dosage Form Brand Name Manufacturer
Propranolol 10 & 40 mg Tablet Indever ACI
Pharmaceutical
s LTD.
Atenolol 50 & 100 mg Tablet Cardipro Square
Pharmaceutical
s LTD.
Conclusion

Antianginal drugs should be prescribed to relieve symptoms. Beta Blockers should be used unless
contraindicated or not tolerated. Combined antianginal drug therapy successfully relieved symptoms in
most elderly patients with chronic angina but failed to do so in 43%. Patients who needed
revascularization for refractory symptoms reported less angina, despite lower drug use during long-term
follow-up and had a better long-term survival.
Reference –
Thank You
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https://www.slideshare.net/mobile/AhmadAlJifri1/angina-and-antianginal-drugs
https://www.webmd.com/heart-disease/heart-disease-angina
https://link.springer.com/article/10.1007/BF00877117#:~:text=Organic%20nitrate%20esters%20have%20a,th
ereby%20lowers%20myocardial%20oxygen%20consumption
https://www.slideshare.net/mobile/JimmyPotter/nitrates-in-angina-pectoris
https://www.slideshare.net/mobile/Pharmacologist/antianginal-drugs-36415783
https://www.slideshare.net/mobile/pankajrana87/antianginal-drug-97906468

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