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Dr. Binu Babu PH.D., M.Sc. (N), MBA Mrs. Jincy Ealias M.Sc. (N)
Dr. Binu Babu PH.D., M.Sc. (N), MBA Mrs. Jincy Ealias M.Sc. (N)
Jincy Ealias
Ph.D., M.Sc. (N), MBA M.Sc. (N)
Anti - anginal drugs are the drugs that
prevent or terminate attacks
of angina pectoris.
• Eg: Nitroglycerin (GTN), isosorbide
Nitrates dinitrate, isosorbide mononitrate,
pentaerythritol tetranitrate.
Calcium channel • Eg: Verapamil, diltiazem, amlodipine,
blockers nifedipine.
Vasodilation
1. Reduction of preload
2. Reduction of afterload
3. Coronary dilation
4. Other actions
1. Dilation of other vasculature
2. Relaxation of other smooth muscles
3. Effects on platelets.
Nitrates are vasodilators.
1. Reduction of preload 2. Reduction of afterload
Venodilation reduces Arteriolar dilation reduces
venous return to the heart vascular resistance thus
thereby reduce preload. decrease afterload
3. Coronary dilation
Nitrates cause coronary vasodilation, thus relieves
vasospasm and increases coronary blood flow.
4. Other actions
Dilation of other vasculature Relaxation of other smooth
• Dilation of blood vessels in muscles
skin results in flushing. Nitrates relax the bronchial,
• Dilation of meningeal gastrointestinal and
vessels results in headache. genitourinary smooth muscles
for a short period.
Effects on platelets
Nitric oxide from nitrates inhibits platelet aggregation.
Nitrates are available for oral, Sublingual, spray
parenteral, ointment and transdermal patch.
Nitrates are well-absorbed orally, but they
undergo extensive first pass metabolism.
So the oral bioavailability of nitrate is poor.
Sublingual route is preferred in case of
emergency for rapid absorption and better
bioavailability.
Sublingual tablets acts within 1-2 minutes
whereas Sublingual spray acts faster than tablets.
Transdermal patch
Sublingual Spray
Drug Dose Route
Nitroglycerin (GTN) 0.5 mg Sublingual
5 mg Oral
2% Ointment
0.4-0.8 mg Sublingual spray
5-20 μg/min IV
14-16 hrs/day Transdermal patch
Isosorbide dinitrate (Sorbitrate) 5-10 mg Sublingual
10-20 mg Oral
Isosorbide mononitrate (Ismo) 10-20 mg Oral
pentaerythritol tetranitrate 10-40 mg Oral
Headache (common)
Flushing of face
Nausea and vomiting
Sweating
Tachycardia
Palpitation
Weakness
Postural hypotension
Rashes
Contact dermatitis
for topical use
Local hypersensitivity reaction
Exertional angina
Acute anginal attacks :
▪ Sublingual nitroglycerin
▪ Drug of choice for acute anginal attacks.
▪ Relieves pain in 2 to 5 minutes.
▪ If the pain is not relieved, the dose is repeated-upto 3 tablets in 15
minutes.
Prophylaxis of angina
▪ NTG can be used for chronic prophylaxis.
▪ Longer acting nitrates are preferred.
▪ Nitroglycerin ointment or Transdermal patch may be used.
Vasospastic angina
Unstable angina
Acute coronary syndrome
Cardiac failure
Myocardial infarction
Cyanide poisoning
Nitrates are life saving in cyanide poisoning.
Amylnitrite is given by inhalation and sodium
nitrite by IV injection (10 ml of 3% solution). Then
Sodium thiosulphate is given IV (50 ml of 25%
solution).
Role of nitrates in cyanide poisoning.
Nitrates (Amylnitrite and sodium nitrite) convert
hemoglobin into methemoglobin, which has high
affinity for cyanide and forms cyano-
methemoglobin.
Cyano-methemoglobin reacts with Sodium
thiosulphate to form thiocyanate which is easily
excreted by the kidneys.
Relieve esophageal spasm
Sublingual NTG is taken just before meals to
counter the spasm.
Relieve biliary colic
Sublingual NTG is also useful as a spasmolytic.
Monitor BP before and after administration.
Nitroglycerine is sensitive to light, heat and
moisture, so stored in tightly closed amber
colored glass bottles.
Give sublingual preparations under the tongue
or in the buccal pouch.
Nitroglycerine IV preparation is mixed in 5%
Dextrose Injection or 0.9% Sodium Chloride.
Instruct the patient that a sublingual dose may
be repeated in 5 minutes if pain is not relieved,
for a total of 3 doses.
Calcium channel blockers (CCBs) are the
drugs that disrupt calcium movement by
blocking voltage-dependent Ca2+ channels
used to treat angina and supraventricular
tachydysrhythmias as well as hypertension.
Eg: Isradipine,
2nd
Nicardipine,
generation
Dihydropyridines Felodipine
3rd Eg:
generation Amlodipine
Calcium
channel
blockers Phenilalkylamines Eg: Verapamil
Decrease myocardial O2
Consumption
Beta antagonist.
• Eg: Propranolol, nadolol, timolol,
Nonselective sotalol
• Eg: Celiprolol
β1 blocker β2 agonist
1. Nonselective
Blocks both β1 and β2 receptors.
2. Cardioselective (β1)
Blocks cardiac specific β1 receptors. β2 receptor
blockade is weak.
3. Partial agonists
Have some sympathomimetic action due to partial β
agonist property.
4. With additional alpha blocking property
Blocks both α and β (β1 and β2) receptors.
5. β1 blocker β2 agonist
Blocks only cardiac specific β1 receptors.
1st generation
(Non selective)
Eg: Propranolol, timolol, sotalol,
2nd generation
(Cardioselective)
Eg: Metoprolol, atenolol, acebutolol, esmolol
3rd generation
(With additional α blocking property & vasodilator
property)
Eg: Labetalol, carvedilol, Celiprolol
Blocks beta receptors