anti anginal drugs ppt by anjali kotwal
DESCRIPTION
TRANSCRIPT
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ANTI- ANGINAL DRUGS
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CONTENT
Anti anginal drugs Angina pectoris Types Classification Nitrates Calcium channel
blockers b blockers Combination therapy
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ANTI-ANGINAL DRUGS
Antianginal drugs may relieve attacks of acute myocardial
ischemia by increasing myocardial oxygen supply or by decreasing myocardial oxygen demand Three groups of pharmacological agents have been shown to be effective in reducing the
frequency, severity, or both of primary or secondary angina. These agents include the nitrates, adrenoceptor
antagonists, and calcium entry blockers. To understand the beneficial actions of these
agents, it is important to be familiar with the major factors regulating the balance between
myocardial oxygen supply and demand.
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ANGINA PECTORIS
It is the principal symptoms of patient with ischemic heart disease.
Manifested by sudden, severe, pressing substernal pain that often radiates to the left shoulder and along the flexor surface of the left arm.
Usually precipitated by exercise, excitement or a heavy meal.
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TYPES OF ANGINA PECTORIS
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NITRATES
Classification of nitrates:1. Rapidly acting nitrates
* used to terminate acute attack of angina * e.g.- Nitroglycerin and Amyl nitrate * usually administered sublingually
2. Long acting nitrates * used to prevent an attack of angina * e.g. – tetra nitrate, Iso sorbide di nitrate,
Penta erythrytol tetra nitrate * administered orally or topically
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ORGANIC NITRATES
Organic nitrates & nitrites are simple nitric & nitrous esters of glycerol.
These agents cause a rapid decrease in myocardial oxygen demand leading to rapid resolution of symptoms.
Nitrates are effective for all types of angina.
Activation of guanylate cyclase increases cGMP activating a cGMP kinase leading to dephosphorylation of myosin light chains decreasing contractile force.
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1ST MECHANISM OF ACTION
Coronary artery dilatation
Decrease coronary bed resistance (Relieved coronary vasospasm)
Increase coronary blood flow
Increase oxygen supply
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2ND MECHANISM OF ACTION
Reduction on peripheral resistance(Secondary to dilatation of aorta)
Decrease blood pressure
Decrease after load
Decrease workload
Decrease oxygen consumption
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3RD MECHANISM OF ACTION
Reduced venous return(Due to dilatation of the veins)
Decrease left ventricular volume
Decrease preload
Decrease workload
Decrease oxygen consumption
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ROUTE OF ADMINISTRATION
1. Sublingual route – rational and effective for the treatment of acute attacks of angina pectoris. Half-life depend only on the rate at which they are delivered to the liver.
2. Oral route – to provide convenient and prolonged prophylaxis against attacks of angina
3. Intravenous Route – useful in the treatment of coronary vasospasm and acute ischemic syndrome.
4. Topical route – used to provide gradual absorption of the drug for prolonged prophylactic purpose.
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Drug Usual single dose Route of administration
Duration of action
Short actingNitroglycerin
0.15-1.2 mg sublingual 10 - 30 min
Isosorbide dinitrate 2.5-5 mg sublingual 10 – 60 min
Amyl nitrite 0.18 – 3 ml inhalation 3 – 5 min
Long actingNitroglycerin sustained action
6.5 – 13 mg q 6-8 hrs oral 6 – 8 hrs
Nitroglycerin 2% ointment
1 – 1.5 inches q hr topical 3 – 6 hrs
Niroglycerin slow released
1 –2 mg per 4 hrs Buccal mucosa 3 – 6 hrs
Nitroglycerin slow released
10 – 25 mg /24hrs (one patch/day}
transdermal 8 –10 hrs
Isosorbide dinitrate 2.5 – 10 mg per 2 hrs sublingual 1.5 – 2 hrs
Isosorbide dinitrate 10 –60 mg per 4-6 hrs oral 4 – 6 hrs
Isosorbide dinitrate chewable
5 – 10 mg per 2-4 hrs oral 2 – 3 hrs
Isosorbide mononitrate 20 mg per 12 hrs oral 6 –10 hrs
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EFFECTS
1. Coronary artery dilatation2. Reduction of peripheral arterial
resistance – decrease after load3. Reduce venous return – decrease
preload
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PHARMACOKINETICSThe difference between nitrate preparations is
mainly in time of onset of action. Nitroglycerin suffers marked 1st pass
metabolism so administration is sublingual. t1/2 ~10 minutes. Occasionally as nitroglycerin is metabolized
anginal symptoms will return. Transdermal administration either as patch or
paste provides a depot of agent for a steady availability.
Nitro-Bid is an oral or topical preparation which saturates the hepatic catabolic pathways allowing a prolonged level of nitroglycerine.
Isosorbide mono nitrate & Isosorbide di nitrate are long acting nitrates that are relatively resistant to hepatic catabolism ……t1/2 ~ 1 hour.
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ADVERSE EFFECTS
1. Throbbing headache2. Flushing of the face3. Dizziness – especially at the
beginning of treatment4. Postural Hypotension – due to pooling
of blood in the dependent portion of the body
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CONTRAINDICATIONS
1. Renal ischemia2. Acute myocardial infarction3. Patients receiving other
antihypertensive agent
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BETA- BLOCKERS
β-Blockers decrease oxygen demands of the myocardium by lowering the heart rate and contractility (decrease CO) particularly the increased demand associated with exercise.
They also reduce PVR by direct vasodilatations of both arterial & venous vessels reducing both pre- and after load.
These effects are caused by blocking β1 receptors, selective β1 antagonists (atenolol, metoprolol ) lose their selectivity at high doses and at least partially block β2 receptors.
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β1 antagonists reduce the frequency and severity of anginal episodes particularly when used in combination with nitrates.
β1 antagonists have been shown to improve survival in post MI patients and decrease the risk of subsequent cardiac events & complications.
There are a number of contraindications for β blockers: asthma, diabetes, bradycardia, PVD & COPD.
β-Blockers in combination with nitrates can be quite effective
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HEMODYNAMIC EFFECT
1. Decrease heart rate2. Reduced blood pressure and cardiac
contractility without appreciable decrease in cardiac output
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MECHANISM OF ACTION
Decrease heart rate & Contractility
Increase duration of diastole Decrease
workload Increase coronary blood flow Decrease
oxy.consumptionIncrease oxygen supply
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CONTRAINDICATIONS
1. Congestive heart failure2. Asthma3. Complete heart block
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CALCIUM CHANNEL BLOCKERS Ca+2 channel blockers protect tissue by inhibiting the
entrance of Ca+2 into cardiac and smooth muscle cells of the coronary and systemic arterial beds.
All Ca+2 channel blockers produce some vasodilation (↓ PVR) and (-) inotropes.
Some agents also show cardiac conduction particularly through the AV node thus serving to control cardiac rhythm.
Some agents have more effect on cardiac muscle than others but all serve to lower blood pressure.
CHF patients may suffer exacerbation of their failure as these are (-) inotropes.
They are useful in Prinzmetal angina in conjunction with nitrates.
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AGENTS
Nifedipine: This Ca+2 channel blocker works mainly on the
arteriolar vasculature decreasing after load it has minimal effect of conduction or HR.
It is metabolized in the liver and excreted in both the urine & the feces.
It causes flushing, headache, hypotension and peripheral edema.
It also has some slowing effect on the GI musculature resulting in constipation.
A reflex tachycardia associated with the vasodilatation may elicit myocardial ischemia in tenuous patients, as such it is generally avoided in non-hypertensive coronary artery disease.
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VERAPAMIL
The agents has its main effect on cardiac conduction decreasing HR and thereby O2 demand.
It also has much more (-) inotropic effect than other Ca+2 channel blockers
It is a weak vasodilator. Because of its focused myocardial effects it is
not used as an antianginal unless there is a tachyarrhythmia. It is metabolized in the liver.
It interferes with digoxin levels causing elevated plasma levels; caution and monitoring of drug levels are necessary wit concomitant use.
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DILTIAZEM
This agent function similarly to Verapamil however it is more effective against Prinzmetal angina.
It has less effect on HR. It has similar metabolism and side
effects as Verapamil.
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Drugs Onset of action Peak of action Half-life
Nifedipine 20 minutes 1 hour 3-4 hours
Verafamil 1-2 hours 5 hours 8-10 hours
Diltiazem 15 minutes 30 minutes 3-4 hours
Nicardifine 20 minutes 45 minutes 2-4 hours
Felodipine 2-5 hours 6-7 hours 11-16 hour
pharmacokinetics
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ADVERSE EFFECT
Nausea and vomiting Dizziness Flushing of the face Tachycardia – due to hypotension
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CONTRAINDICATIONS
Cardiogenic shock Recent myocardial infarction Heart failure Atria-ventricular block
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COMBINATION THERAPY
1. Nitrates and B-blockers The additive efficacy is primarily a
result of one drug blocking the adverse effect of the other agent on net myocardial oxygen consumption
B-blockers – blocks the reflex tachycardia associated with nitrates
Nitrates – attenuate the increase in the left ventricular end diastolic volume associated with B-lockers by increasing venous capacitance
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CALCIUM CHANNEL BLOCKERS +BETA BLOCKERS
Useful in the treatment of exertional angina that is not controlled adequately with nitrates and B-blockers
B-blockers – attenuate reflex tachycardia produce by nifedipine
These two drugs produce decrease blood pressure
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CALCIUM CHANNEL BLOCKER+NITRATES
Useful in severe vasospastic or exertional angina (particularly in patient with exertional angina with congestive heart failure and sick sinus syndrome)
Nitrates reduce preload and after load Ca channels reduces the after load Net effect is on reduction of oxygen
demand
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TRIPLE DRUGS:-NITRATES+CALCIUM CHANNEL BLOCKERS+BETA BLOCKER
Useful in patients with exertional angina not controlled by the administration of two types of anti-anginal agent
Nifidipine – decrease after load Nitrates – decrease preload B-blockers – decrease heart rate &
myocardial contractility
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ANJALI KOTWAL5TH SEMESTER B.PHARMACYSHOOLINI UNIVERSITY
Presented by: