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Dr. Mustafe Hussein Abdilahi
MBBS, MMED (Internist)
1. Cardiac glycosides
2. Antidysrhythmic agents
3. Anti-anginal drugs
4. Anti-hypertensive drugs
5. Anti-lipemic agents
6. Anti-coagulants
7. Anti-platelets
• Cardiac glycosides are drugs that increase the
rate at which the heart beats is known as
positive inotropic effects.
• Cardiac glycosides used to solve the
problems of congestive heart failure (CHF).
• In patients with congestive heart failure
occurs when the ejection fraction compared
with the total amount of blood in the ventricle
is decreased.
• Cardiac glycosides are one of the oldest and
most effective groups of drugs.
• They were originally obtained from either
digitalis purpurea or digitalis lanata plants
both commonly referred to as foxglove.
• The cardiac glycosides have been the
mainstay of therapy for CHF for more than
200 years and they continue to be one of the
most frequently used positive inotropic
agents.
1.Digoxin: is the most prescribed drug in this
group, it has less side effects.
2. Digitoxin: not frequently used because of it
is side effects.
 The primary beneficial effect of digitalis is
thought to be an increase in myocardial
contractility.
 By doing this cellular sodium concentration
and calcium concentration increases.
 Digoxin is the most commonly prescribed
digitalis glycoside.
 It is highly effective agent in the treatment of
CHF.
 May also used clinically to improve
myocardial contractility and thus reverse
Cardiogenic shock.
• Digoxin is contraindicated in patients who
have shown in:
1. Hypersensitivity
2. bradychycardia
• Digoxin is available in: 50microgram elixir,
50,100, 200 microgram liquid filled capsule,
125, 250, 500 microgram tablet and 100,
200 microgram per mal injection.
 Adult dosage is 1-1.5mg/day, 0.125-0.5 mg.
 Premature dosage is 0.015-0.025mg/kg.
 Anorexia
 Nausea
 Vomiting
 Confusion
 Colored vision
 Headache
 Fatigue
1. Discontinue the drug.
2. Determine digoxin and electrolyte level.
3. Administer potassium supplements for
hypokalemia.
4. Start ECG monitoring.
5. Administer digibind for severe overdose.
• A dysrhythmia is any deviation from the
normal rhythm of the heart, thus the more
accurate term for an irregular heart rhythm is
dysrhythmia.
• There are many conditions in which
dysrhythmia can develop:
1. Myocardial infraction
2. Cardiac surgery as a result of coronary
disease.
 There are numerous drug available to treat
dysrhytmias and these are classified based on
where and how they affect cardiac cells.
 The most commonly used system is the
Vaughan Williams classification.
• Class one
1. Class 1A
• Disopyramide
• Procainamide
• Quinidine
Class 1B
• Lidocaine
• Phenytoin
• Tocainide
• Mexiletine
• Class 1C
1. Propafenone
2. Flecainide
3. Entainide
Class Two
1. Propranaolol
2. Esmolol
3. sotalol
• Class three
1. Amiodarone
2. Bretylium
• Class four
1. Adenosine
2. Verpamil
3. Diltiazem
 Hypersensitivity
 Nausea
 Vomiting
 Diarrhoe
 Dizziness
 Headache
 Blurred vision
• The main toxic affects of the anti-
dysrhythmics involve:
1. Heart
2. Circulation
3. CNS
• Speacific antidotes are not available and the
management of an overdose involves
maintaining adequate circulation and
respiration.
 Quinidine has both direct action on the
electrical activity of the heart and indirect (ant
cholinergic) effect.
 It is ant cholinergic results in inhibition of the
parasympathetic nervous system.
 Significant adverse effects of the agent
include
1. Cardiac asystole
2. Arterial embolism
3. Ventricular ectopic beats
 Contraindicated
1. Hypersensitivity
2. AV block
3. Abnormal rhyths
 Quinidine is available in 324mg quinidine
gluconate tablets, 275 mg quinidine
polygalacturonate tablets, 300mg quinidine
sulfate tablets.
 Parentrally quinidine gluconate comes as an
80mg/ml injection.
 Adult dosage is 324 – 648 mg q8h-q12h, IM
600mg followed by 400mg q2h.
 It is similar to that of Quinidine but it differs
from Quinidine in that it is indirect effect
(anticholinergic is weaker).
 Procainamide is useful in the management of
atrial and ventricular tachydysrhymias.
 It is a pregnancy category C drug.
 Available 250, 375, 500mg capsules, 500,
750, 1000mg film coated tablets and 100,
500mg/ml injection
 Disopyramide is used primarily for the
treatment of ventricular dysrhymias.
 It can produce significant side-effects
including:
1. Anticholinergic effects
2. Cardiovascular depression
For these reasons it is use is limited, especially
in patients with poor left ventricular
function.
 Significance adverse reactions from it are
hypotension and widening of the QRS interval
on ECG.
 It is available orally in 100- 150mg capsules
 Adult dosage is 150mg q6h.
 It is one of the most effective drugs for the
treatment of ventricular dysrhytmias.
 It can only administer intravenously because
it has extensive first pass effect, that is when
taken orally, the liver metabolizes most of it.
 It is accomplished by blockade of sodium
channels.
 Lidocaine is the drug of choice for treating
the acute ventricular dysrhymias.
 Available 100mg/ml IM injection, 10, 20, 40,
100, 200mg/ml IV injection.
 Propafenone reduces sodium current in
purkinje fibers and to lesser extent in
myocardial fibers.
 Propafenone has a mild beta-blocking
effects.
 It is also believed to have calcium channel
blocking effects, which contributes to
propafenone mild negative inotropic effects.
 It should be used with causion in patients
with congestive heart failure, because of it is
beta-blocking agents and it is mild inotropic
effects.
 The most frequently reported adverse
reaction is dizziness.
 Patients may also complain
1. Metallic taste
2. Constipation
3. Headache
4. Nausea
 Propafenone is contraindicated:
1. Bradycardia
2. Hypersensitivity
3. Bronchial asthma
4. Hypotension
 Available orally as 150, 300mg, and the
adult dosage is 150mg q8h.
 It is a cardio-selective beta blocker that
means it blocks the beta one adrenergic
receptor.
 Atenalol also activates beta two in the lungs
and could therefore exacerbate a pre-existing
case of asthma or COPD.
 It is also useful in the treatment of
hypertension and angina pectoris.
 It is available orally 25, 50, 100mg tablets,
0.5mg/ml IV injection.
 Propranolol is one of the first beta blockers
introduced into clinical practice and this
occurred in 1967.
 It was then primarily used in the treatment of
dysrhymias.
 Propranolol is a non-speacific blocker that
blocks both beta one and beta two adrenergic
receptor in the heart and the lungs.
 Propranolol is the oldest of this class of drugs,
there are now many indications of It is use:
1. Hypertension
2. Angina pectoris
3. Dysarrythemia
 Available as 10, 20, 40, 60, 80, 90 mg
tablets, 60, 80, 120, 160 mg capsules, 20,
40, mg/5ml oral solution, 1mg/ml injection.
 Amiodarone markedly prolongs the APD
(action potential duration) and ERP (effective
refractory period).
 Amiodarone also known to block both the
alpha and beta adrenergic receptors.
 Amiodarone is a very lipophilic, there fore it
may cause un wanted effects.
 Amiodarone can cause
1. Hypothyrodism
2. Hyperthyrodism
 Amoidarone is contraindicated in patients
1. Hypersensitivity
2. Severe bradycardia
3. Second or third degree of heart block.
 Amiodarone is available 200mg orally tablets.
 Amiodarone is a pregnancy category C agent.
 Diltiazem is primarily indicated for the
temporary control of a rapid ventricular
response in a patient with atrial fibrillation.
 It is a pregnancy category C drug.
 It is available both orally and parenterally, 30,
90, 120 mg tablets and 5mg/ml injection.
 Verpamil inhibits calcium ion influx across the
slow calcium channels in cardiac conduction
tissue.
 Usually decreases the heart beat at least 20
percent.
 Verpamil is also used to treat:
1. Angina pectoris
2. Hypertension
 It is available 40, 80, 120mg tablets, and 2.5
mg/ml injection parenterally.
 It is a pregnancy category C.
 It is an unclassified antidysarhythmic drug.
 It is naturally occuring nucleoside that slows
the electrical conduction rate.
 It is contraindicated in patients with second
and third heart block.
 It is extremely short half life of less than 10
seconds, for this reason it is only
administered by IV.
 It is available parenterally as a 3mg/ml
injection.
 It is a pregnancy category C.
 The three main classes of drugs used to treat
angina pectoris are:
1. Nitrates
2. Beta-blockers
3. Calcium channel blockers
 There are three main therapeutic objectives of
anti-anginal drug therapy:
1. It must minimize the frequency of attacks
and decrease the duration of the anginal
pain.
2. Improve the patients functional capacity with
as few side-effects
3. Prevent the worst outcome, myocardial
infarction.
 Nitrates, in particular nitroglycerin have long
been the mainstay of both the prophylaxis
and treatment of angina.
 This class of anti-anginal agents was first
discovered by sir Thomas lauder brunton in
England who noted that amyl nitrate was just
effective as venesection in the management
of angina.
 Few years later, a chemically related substance
glyceryl trinitrate (nitroglycerin) was
successfully isolated.
 They are available in a wide variety of
preparations including:
1. Sublingual
2. Bucal
3. Chewable tablets
 Oral tablets
 Capsules
 Ointments
 Patches
 Inhalable sprays
 Intravenous solutions
 Nitrates can be classified into:
1. Rapid acting agents
 Amyl nitrate
 Nitroglycerin
2. Long acting agents
 Erythrityl tetra nitrate
 Isosorbide dinitrate
 Isosorbide mononitrate
 The nitrates dilate all blood vessels, but they
primarily affect the blood vessels of the
venous circulation.
 This venodilation is the result of relaxation of
the smooth muscle that surrounds veins.
 Nitrates also have a potent dilating effect on
the coronary arteries.
 Nitroglycerin has traditionally been the most
important drug used in the symptomatic
treatment of ischemic heart conditions such
as angina.
 it has classified pregnancy category C agent.
 Nitroglycerin is administered many other
routes to pass first pass effect.
 Available sublingual 0.3, 0.4, 0.6 mg tablets,
0.4mg/metred dose aerosol, 5mg/ml IV,
2.6mg, 6.5mg tablets, 2.5, 6.5, 9, 13mg
capsules, 2% ointment and 0.1, 0.2, 0.3, 0.4
mg patches.
 Adult dosage is 2.5-6.5mg q8h-q12h,
sublingual 0.15-0.6mg Prn, transdermal,
apply one patch q24h.
 Isosorbide is an organic nitrate and therefore
a powerful explosive.
 When Isosorbide dinitrate is metabolized in
the liver, it is broken down into two active
metabolites.
 It is used for the acute relief of angina
pectoris and for prophylaxis.
 It is a pregnancy category C drug agent.
 Available orally 40mg capsules, 5, 10, 20, 30,
40mg tablets and 2.5, 5, 10mg sublingual
tablets.
 Adult dose is sublingual 2.5-10mg Prn and
5-30mg q8h-q12h.
 Nadolol is a non-selective beta-blocker
indicated for the prophylactic treatment of
angina and hypertension.
 It is the most hydrophilic of all beta blockers
which may be a beneficial characteristic in
elderly patients because as we age we lose
muscle mass and gain fat.
 Water soluble drugs such as nadolol will have
more consistent and reliable effect.
 It is a pregnancy category C agent.
 It is only available orally as 20, 40, 80, 120,
160mg tablets.
 Adult dosage is 80-240mg/day as a single
dose.
 Nifedipine is a calcium channel blocker drug.
 It is given by sublingually.
 It is a pregnancy category C agent.
 Available 10, 20mg capsules, 30, 60, 90mg
tablets.
 Adult dosage is 10mg Tid.
 The anti-hypertensive drugs are classified
based on their mechanism of action
1. Adrenergic agents
2. Vasodilators
3. Diuretics
4. ACEI
5. Calcium channel blockers
 Centrally acting drugs
1. Clonidine
2. Guanabenz
3. Guanfacine
4. Methyldopa
 Peripherally acting drugs
1. Guanadrel
2. Guanethidine
3. Reserpine
 The centrally acting adrenergic agents
decrease blood pressure by stimulating the
alpha 2 receptors.
 The peripherally acting adrenergic agents
decrease blood pressure by blocking alpha 1
adrenergic receptors.
 Dry mouth
 Drowsiness
 Sedation
 Constipation
 Headache
 Sleep disorders
 Nausea
 Rash
 Clonidine is primarily used for it is ability to
decrease blood pressure.
 It is also useful in the management of Opiod
withdrawal.
 It has better safety profile than the other
centrally acting adrenergics and has the
advantage of being available in several
dosage forms.
 It is a pregnancy category C agent.
 Contraindicated in a patients who have shown
hypersensitivity.
 Available 0.1, 0.2, 0.3 mg as patch, 0.1, 0.2,
0.3mg tablets orally.
 Adult dosage is 0.2-0.8mg/day divided dose.
 Reserpine is derived from rauwolfia alkaloids.
 Reserpine promote sodium and water
resorption and their anti-hypertensive effects
my diminish.
 Reserpine, always it is combined with
diuretics.
 Reserpine classified pregnancy category D.
 Contraindicated in patients who have:
1. Mental illness
2. Peptic ulcer
3. Hypersensitivity
 Available in 0.1, 0.25mg tablets.
 Adult dose is 0.1 - 0.25mg/day divided or
single dose.
 It is the oldest of the alpha 1 blockers.
 It reduces both peripheral vascular resistance
and blood pressure by dilating both arterial
and venous blood vessels.
 It is shown beneficial in the treatment of
hypertension.
 It is classified in pregnancy category C.
 Available 1, 2, 5 mg capsules.
 ACEI represent a large group of anti-
hypertensive agents.
 There are currently more than seven agents
available for clinical use.
 ACEI are beneficial in the treatment of CHF,
because they prevent sodium and water
resorption by inhibiting aldosterone
secretion.
 Dizziness
 Mood changes
 Headache
 Dry cough
 The most pronounced symptom of overdose
of ACEI is hypotension.
 Treatment is symptomatic and supportive:
1. Administering IV fluids
2. Hemodialysis is effective for the removal of
Captopril and lisinopril.
 Captopril was the first ACEI to became
available in this group.
 It is given to a hospitalized patients because
of it is short half life.
 Available 12.5, 25, 50, 100mg tablets.
 Adult dosage is 25-150mg 2-3 times aday.
 Enalapril is the only currently available ACEI
that is available in both oral and parentral
preparations.
 Parentral formulation offers the hemo-
dynamic benefit of inhibiting ACE activity in
an acutely ill patient who cannot tolerate oral
medications.
 Enalapril differs from Captopril in that it is a
prodrug and relies on a functioning liver to
be converted to it is active form.
 Although it is half life is slightly longer that of
captopril, it may in some instances still have
to be given twice daily.
 Available 2.5, 5, 10, 20mg tablets and
1.25mg/ml injection.
 It is a pregnancy category C agent.
 It is contraindicated in patients with known
hypersensitivity.
 Adult dosage is 10mg Qid 2-4 days followed
by 25mg Qid for balance of week.
 It is a pregnancy category C agent.
 Available topical 2% minoxidil solution used
to treat hair loss.
 Adult dosage is 10-40mg per day or divided
dose.
 It is contraindicated into a hypersensitive
patients.
 It is a pregnancy category C agent.
 It is contraindicated with a known
hypersensitivity patients.
 This drug use is limited to the management
of the hypertensive emergencies.
 Peadtric dosage is 0.3-10mg/kg
 Anti-lipemic agents are drugs used to lower
the rate of cholesterol and triglycerides.
 Anti-lipemic drugs can be classified based on
their mechanism of actions:
1. Bile acid sequestrants
2. Statins
3. Gemfibrotic acid
 Bile acid sequestrants also called bile acid
binding resins and ion exchange resins.
 Cholestyramine and colestipol are prime
examples of these group.
 Both these agents have been used widely for
more than 20 years and have been evaluated
extensively in well controlled clinical trials.
 Generally these drugs lower plasma
concentration of LDL cholesterol.
 The bile acid resins bind bile and this
prevents the resorption of the bile acids from
the small intestine.
 Constipation
 Heart burn
 Nausea
 Belching
 Bloating
 It is important to initiate the therapy with low
doses and instruct patients to take the drugs
with meals to reduce the side-effects.
 Because of bile acid sequestrants are not
absorbed, an overdose could cause
obstruction of the GIT, therefore treatment of
an overdose involves restoring gut motility.
 All drugs should be taken at least 1 hour
before or 4-6 hours after the administration
of the ion exchange resins.
 High dose of bile acid sequestrant will
decrease the absorption of fat soluble
vitamins. E.g vit A, D, E, K.
 It is a prescription only drug.
 It is a pregnancy category C agent.
 It may interfere distribution of the proper
amounts of fat soluble vitamins to the fetus
or pregnant women taking these agents.
 It is only available 4-9 gram packets of
powder to be taken as an oral suspension.
 Lovastatin was the first agent in this drug
class to be approved for use and this
occurred in 1987.
 It is indicated primarily for the treatment of
type 2A, and 2B hyperlipidemias.
 Effective in lowering the LDL cholesterol level
and to some degree the triglyceride levels.
 Recommended daily dose is 20-80mg/day
PO.
 It is a pregnancy category X agent.
 Gemfibrozil is a fibric acid derivative that
lowers VLDL level.
 It is highly effective for lowering the plasma
triglyceride levels.
 It is indicated for the treatment of type 4 and
5 hyperlipidemias and in some cases of the
type 2B form.
 Available as 600mg orally tablet
 It is a pregnancy category B agent
 Nicotinic acid is also known niacin, very
unique lipid lowering agent.
 Nicotinic acid is a vitamin B3 drug.
 It is an effective and inexpensive medication.
 Niacin is often given in combination with
other anti-lipemic drugs to enhance the lipid
lowering effects.
 It is a pregnancy category A agent.
 Niacin is contraindicated in:
1. Hypersensitivity
2. Peptic ulcer
3. Hepatic diseases
4. Hemorrhage
5. Lactating women
6. Severe hypotension
 Available as an over the counter drug.
 Available 25, 50, 100, 250, 500, 750mg
tablets.
 It is commonly given in 2-4 divided doses of
1.5-6g per day.
 Drugs that prevent the formation of a clot by
inhibiting certain clotting factors are called
anti-coagulants.
 These agents are only given prophylactically
because they have no direct effect on a blood
clot.
 There uses vary from preventing clot
formation to preventing the extension of
preformed clot or a thrombus.
 Once a clot forms on the wall of a blood
vessel, it may dislodge and travel through the
blood stream.
 If it goes to the brain, it causes stroke.
 If it goes to the lungs, it causes pulmonary
emboli.
 If it goes to the veins in the lungs, it causes
deep vein thrombosis.
 Anti-coagulants can prevent all of these from
occurring, if used the correct manner.
 There are both orally and parenterally
administered anti-coagulants.
 Nausea
 Vomiting
 Bleeding
 Abdominal cramp
 Hypoaldosteronism
 Symptoms that may be attributed to toxicity
or an overdose of anti-coagulants are:
1. Hematuria
2. Melena (black tarry feaces)
3. Mucous membrane bleeding
 Steps of toxicity management:
1. Discontinue the drug
2. If there is blood loss, replacement of packed
red cells.
3. Give protamine sulphate, 1mg of protamine
sulphate can reverse the effects of 100 units
of heparin.

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Cardiovascular Drug Agents.ppt

  • 1. Dr. Mustafe Hussein Abdilahi MBBS, MMED (Internist)
  • 2. 1. Cardiac glycosides 2. Antidysrhythmic agents 3. Anti-anginal drugs 4. Anti-hypertensive drugs 5. Anti-lipemic agents 6. Anti-coagulants 7. Anti-platelets
  • 3. • Cardiac glycosides are drugs that increase the rate at which the heart beats is known as positive inotropic effects. • Cardiac glycosides used to solve the problems of congestive heart failure (CHF). • In patients with congestive heart failure occurs when the ejection fraction compared with the total amount of blood in the ventricle is decreased.
  • 4. • Cardiac glycosides are one of the oldest and most effective groups of drugs. • They were originally obtained from either digitalis purpurea or digitalis lanata plants both commonly referred to as foxglove. • The cardiac glycosides have been the mainstay of therapy for CHF for more than 200 years and they continue to be one of the most frequently used positive inotropic agents.
  • 5. 1.Digoxin: is the most prescribed drug in this group, it has less side effects. 2. Digitoxin: not frequently used because of it is side effects.
  • 6.  The primary beneficial effect of digitalis is thought to be an increase in myocardial contractility.  By doing this cellular sodium concentration and calcium concentration increases.
  • 7.  Digoxin is the most commonly prescribed digitalis glycoside.  It is highly effective agent in the treatment of CHF.  May also used clinically to improve myocardial contractility and thus reverse Cardiogenic shock.
  • 8. • Digoxin is contraindicated in patients who have shown in: 1. Hypersensitivity 2. bradychycardia • Digoxin is available in: 50microgram elixir, 50,100, 200 microgram liquid filled capsule, 125, 250, 500 microgram tablet and 100, 200 microgram per mal injection.
  • 9.  Adult dosage is 1-1.5mg/day, 0.125-0.5 mg.  Premature dosage is 0.015-0.025mg/kg.
  • 10.  Anorexia  Nausea  Vomiting  Confusion  Colored vision  Headache  Fatigue
  • 11. 1. Discontinue the drug. 2. Determine digoxin and electrolyte level. 3. Administer potassium supplements for hypokalemia. 4. Start ECG monitoring. 5. Administer digibind for severe overdose.
  • 12. • A dysrhythmia is any deviation from the normal rhythm of the heart, thus the more accurate term for an irregular heart rhythm is dysrhythmia. • There are many conditions in which dysrhythmia can develop: 1. Myocardial infraction 2. Cardiac surgery as a result of coronary disease.
  • 13.  There are numerous drug available to treat dysrhytmias and these are classified based on where and how they affect cardiac cells.  The most commonly used system is the Vaughan Williams classification.
  • 14. • Class one 1. Class 1A • Disopyramide • Procainamide • Quinidine
  • 15. Class 1B • Lidocaine • Phenytoin • Tocainide • Mexiletine
  • 16. • Class 1C 1. Propafenone 2. Flecainide 3. Entainide Class Two 1. Propranaolol 2. Esmolol 3. sotalol
  • 17. • Class three 1. Amiodarone 2. Bretylium • Class four 1. Adenosine 2. Verpamil 3. Diltiazem
  • 18.  Hypersensitivity  Nausea  Vomiting  Diarrhoe  Dizziness  Headache  Blurred vision
  • 19. • The main toxic affects of the anti- dysrhythmics involve: 1. Heart 2. Circulation 3. CNS • Speacific antidotes are not available and the management of an overdose involves maintaining adequate circulation and respiration.
  • 20.  Quinidine has both direct action on the electrical activity of the heart and indirect (ant cholinergic) effect.  It is ant cholinergic results in inhibition of the parasympathetic nervous system.
  • 21.  Significant adverse effects of the agent include 1. Cardiac asystole 2. Arterial embolism 3. Ventricular ectopic beats  Contraindicated 1. Hypersensitivity 2. AV block 3. Abnormal rhyths
  • 22.  Quinidine is available in 324mg quinidine gluconate tablets, 275 mg quinidine polygalacturonate tablets, 300mg quinidine sulfate tablets.  Parentrally quinidine gluconate comes as an 80mg/ml injection.  Adult dosage is 324 – 648 mg q8h-q12h, IM 600mg followed by 400mg q2h.
  • 23.  It is similar to that of Quinidine but it differs from Quinidine in that it is indirect effect (anticholinergic is weaker).  Procainamide is useful in the management of atrial and ventricular tachydysrhymias.  It is a pregnancy category C drug.
  • 24.  Available 250, 375, 500mg capsules, 500, 750, 1000mg film coated tablets and 100, 500mg/ml injection
  • 25.  Disopyramide is used primarily for the treatment of ventricular dysrhymias.  It can produce significant side-effects including: 1. Anticholinergic effects 2. Cardiovascular depression For these reasons it is use is limited, especially in patients with poor left ventricular function.
  • 26.  Significance adverse reactions from it are hypotension and widening of the QRS interval on ECG.  It is available orally in 100- 150mg capsules  Adult dosage is 150mg q6h.
  • 27.  It is one of the most effective drugs for the treatment of ventricular dysrhytmias.  It can only administer intravenously because it has extensive first pass effect, that is when taken orally, the liver metabolizes most of it.  It is accomplished by blockade of sodium channels.
  • 28.  Lidocaine is the drug of choice for treating the acute ventricular dysrhymias.  Available 100mg/ml IM injection, 10, 20, 40, 100, 200mg/ml IV injection.
  • 29.  Propafenone reduces sodium current in purkinje fibers and to lesser extent in myocardial fibers.  Propafenone has a mild beta-blocking effects.  It is also believed to have calcium channel blocking effects, which contributes to propafenone mild negative inotropic effects.
  • 30.  It should be used with causion in patients with congestive heart failure, because of it is beta-blocking agents and it is mild inotropic effects.  The most frequently reported adverse reaction is dizziness.
  • 31.  Patients may also complain 1. Metallic taste 2. Constipation 3. Headache 4. Nausea
  • 32.  Propafenone is contraindicated: 1. Bradycardia 2. Hypersensitivity 3. Bronchial asthma 4. Hypotension  Available orally as 150, 300mg, and the adult dosage is 150mg q8h.
  • 33.  It is a cardio-selective beta blocker that means it blocks the beta one adrenergic receptor.  Atenalol also activates beta two in the lungs and could therefore exacerbate a pre-existing case of asthma or COPD.  It is also useful in the treatment of hypertension and angina pectoris.  It is available orally 25, 50, 100mg tablets, 0.5mg/ml IV injection.
  • 34.  Propranolol is one of the first beta blockers introduced into clinical practice and this occurred in 1967.  It was then primarily used in the treatment of dysrhymias.  Propranolol is a non-speacific blocker that blocks both beta one and beta two adrenergic receptor in the heart and the lungs.
  • 35.  Propranolol is the oldest of this class of drugs, there are now many indications of It is use: 1. Hypertension 2. Angina pectoris 3. Dysarrythemia
  • 36.  Available as 10, 20, 40, 60, 80, 90 mg tablets, 60, 80, 120, 160 mg capsules, 20, 40, mg/5ml oral solution, 1mg/ml injection.
  • 37.  Amiodarone markedly prolongs the APD (action potential duration) and ERP (effective refractory period).  Amiodarone also known to block both the alpha and beta adrenergic receptors.  Amiodarone is a very lipophilic, there fore it may cause un wanted effects.
  • 38.  Amiodarone can cause 1. Hypothyrodism 2. Hyperthyrodism  Amoidarone is contraindicated in patients 1. Hypersensitivity 2. Severe bradycardia 3. Second or third degree of heart block.
  • 39.  Amiodarone is available 200mg orally tablets.  Amiodarone is a pregnancy category C agent.
  • 40.  Diltiazem is primarily indicated for the temporary control of a rapid ventricular response in a patient with atrial fibrillation.  It is a pregnancy category C drug.  It is available both orally and parenterally, 30, 90, 120 mg tablets and 5mg/ml injection.
  • 41.  Verpamil inhibits calcium ion influx across the slow calcium channels in cardiac conduction tissue.  Usually decreases the heart beat at least 20 percent.  Verpamil is also used to treat: 1. Angina pectoris 2. Hypertension
  • 42.  It is available 40, 80, 120mg tablets, and 2.5 mg/ml injection parenterally.  It is a pregnancy category C.
  • 43.  It is an unclassified antidysarhythmic drug.  It is naturally occuring nucleoside that slows the electrical conduction rate.  It is contraindicated in patients with second and third heart block.  It is extremely short half life of less than 10 seconds, for this reason it is only administered by IV.
  • 44.  It is available parenterally as a 3mg/ml injection.  It is a pregnancy category C.
  • 45.  The three main classes of drugs used to treat angina pectoris are: 1. Nitrates 2. Beta-blockers 3. Calcium channel blockers
  • 46.  There are three main therapeutic objectives of anti-anginal drug therapy: 1. It must minimize the frequency of attacks and decrease the duration of the anginal pain. 2. Improve the patients functional capacity with as few side-effects 3. Prevent the worst outcome, myocardial infarction.
  • 47.  Nitrates, in particular nitroglycerin have long been the mainstay of both the prophylaxis and treatment of angina.  This class of anti-anginal agents was first discovered by sir Thomas lauder brunton in England who noted that amyl nitrate was just effective as venesection in the management of angina.
  • 48.  Few years later, a chemically related substance glyceryl trinitrate (nitroglycerin) was successfully isolated.  They are available in a wide variety of preparations including: 1. Sublingual 2. Bucal 3. Chewable tablets
  • 49.  Oral tablets  Capsules  Ointments  Patches  Inhalable sprays  Intravenous solutions
  • 50.  Nitrates can be classified into: 1. Rapid acting agents  Amyl nitrate  Nitroglycerin 2. Long acting agents  Erythrityl tetra nitrate  Isosorbide dinitrate  Isosorbide mononitrate
  • 51.  The nitrates dilate all blood vessels, but they primarily affect the blood vessels of the venous circulation.  This venodilation is the result of relaxation of the smooth muscle that surrounds veins.  Nitrates also have a potent dilating effect on the coronary arteries.
  • 52.  Nitroglycerin has traditionally been the most important drug used in the symptomatic treatment of ischemic heart conditions such as angina.  it has classified pregnancy category C agent.  Nitroglycerin is administered many other routes to pass first pass effect.
  • 53.  Available sublingual 0.3, 0.4, 0.6 mg tablets, 0.4mg/metred dose aerosol, 5mg/ml IV, 2.6mg, 6.5mg tablets, 2.5, 6.5, 9, 13mg capsules, 2% ointment and 0.1, 0.2, 0.3, 0.4 mg patches.  Adult dosage is 2.5-6.5mg q8h-q12h, sublingual 0.15-0.6mg Prn, transdermal, apply one patch q24h.
  • 54.  Isosorbide is an organic nitrate and therefore a powerful explosive.  When Isosorbide dinitrate is metabolized in the liver, it is broken down into two active metabolites.  It is used for the acute relief of angina pectoris and for prophylaxis.
  • 55.  It is a pregnancy category C drug agent.  Available orally 40mg capsules, 5, 10, 20, 30, 40mg tablets and 2.5, 5, 10mg sublingual tablets.  Adult dose is sublingual 2.5-10mg Prn and 5-30mg q8h-q12h.
  • 56.  Nadolol is a non-selective beta-blocker indicated for the prophylactic treatment of angina and hypertension.  It is the most hydrophilic of all beta blockers which may be a beneficial characteristic in elderly patients because as we age we lose muscle mass and gain fat.
  • 57.  Water soluble drugs such as nadolol will have more consistent and reliable effect.  It is a pregnancy category C agent.  It is only available orally as 20, 40, 80, 120, 160mg tablets.  Adult dosage is 80-240mg/day as a single dose.
  • 58.  Nifedipine is a calcium channel blocker drug.  It is given by sublingually.  It is a pregnancy category C agent.  Available 10, 20mg capsules, 30, 60, 90mg tablets.  Adult dosage is 10mg Tid.
  • 59.  The anti-hypertensive drugs are classified based on their mechanism of action 1. Adrenergic agents 2. Vasodilators 3. Diuretics 4. ACEI 5. Calcium channel blockers
  • 60.  Centrally acting drugs 1. Clonidine 2. Guanabenz 3. Guanfacine 4. Methyldopa
  • 61.  Peripherally acting drugs 1. Guanadrel 2. Guanethidine 3. Reserpine
  • 62.  The centrally acting adrenergic agents decrease blood pressure by stimulating the alpha 2 receptors.  The peripherally acting adrenergic agents decrease blood pressure by blocking alpha 1 adrenergic receptors.
  • 63.  Dry mouth  Drowsiness  Sedation  Constipation  Headache  Sleep disorders  Nausea  Rash
  • 64.  Clonidine is primarily used for it is ability to decrease blood pressure.  It is also useful in the management of Opiod withdrawal.  It has better safety profile than the other centrally acting adrenergics and has the advantage of being available in several dosage forms.
  • 65.  It is a pregnancy category C agent.  Contraindicated in a patients who have shown hypersensitivity.  Available 0.1, 0.2, 0.3 mg as patch, 0.1, 0.2, 0.3mg tablets orally.  Adult dosage is 0.2-0.8mg/day divided dose.
  • 66.  Reserpine is derived from rauwolfia alkaloids.  Reserpine promote sodium and water resorption and their anti-hypertensive effects my diminish.  Reserpine, always it is combined with diuretics.  Reserpine classified pregnancy category D.
  • 67.  Contraindicated in patients who have: 1. Mental illness 2. Peptic ulcer 3. Hypersensitivity  Available in 0.1, 0.25mg tablets.  Adult dose is 0.1 - 0.25mg/day divided or single dose.
  • 68.  It is the oldest of the alpha 1 blockers.  It reduces both peripheral vascular resistance and blood pressure by dilating both arterial and venous blood vessels.  It is shown beneficial in the treatment of hypertension.  It is classified in pregnancy category C.  Available 1, 2, 5 mg capsules.
  • 69.  ACEI represent a large group of anti- hypertensive agents.  There are currently more than seven agents available for clinical use.  ACEI are beneficial in the treatment of CHF, because they prevent sodium and water resorption by inhibiting aldosterone secretion.
  • 70.  Dizziness  Mood changes  Headache  Dry cough
  • 71.  The most pronounced symptom of overdose of ACEI is hypotension.  Treatment is symptomatic and supportive: 1. Administering IV fluids 2. Hemodialysis is effective for the removal of Captopril and lisinopril.
  • 72.  Captopril was the first ACEI to became available in this group.  It is given to a hospitalized patients because of it is short half life.  Available 12.5, 25, 50, 100mg tablets.  Adult dosage is 25-150mg 2-3 times aday.
  • 73.  Enalapril is the only currently available ACEI that is available in both oral and parentral preparations.  Parentral formulation offers the hemo- dynamic benefit of inhibiting ACE activity in an acutely ill patient who cannot tolerate oral medications.
  • 74.  Enalapril differs from Captopril in that it is a prodrug and relies on a functioning liver to be converted to it is active form.  Although it is half life is slightly longer that of captopril, it may in some instances still have to be given twice daily.  Available 2.5, 5, 10, 20mg tablets and 1.25mg/ml injection.
  • 75.  It is a pregnancy category C agent.  It is contraindicated in patients with known hypersensitivity.  Adult dosage is 10mg Qid 2-4 days followed by 25mg Qid for balance of week.
  • 76.  It is a pregnancy category C agent.  Available topical 2% minoxidil solution used to treat hair loss.  Adult dosage is 10-40mg per day or divided dose.  It is contraindicated into a hypersensitive patients.
  • 77.  It is a pregnancy category C agent.  It is contraindicated with a known hypersensitivity patients.  This drug use is limited to the management of the hypertensive emergencies.  Peadtric dosage is 0.3-10mg/kg
  • 78.  Anti-lipemic agents are drugs used to lower the rate of cholesterol and triglycerides.  Anti-lipemic drugs can be classified based on their mechanism of actions: 1. Bile acid sequestrants 2. Statins 3. Gemfibrotic acid
  • 79.  Bile acid sequestrants also called bile acid binding resins and ion exchange resins.  Cholestyramine and colestipol are prime examples of these group.  Both these agents have been used widely for more than 20 years and have been evaluated extensively in well controlled clinical trials.  Generally these drugs lower plasma concentration of LDL cholesterol.
  • 80.  The bile acid resins bind bile and this prevents the resorption of the bile acids from the small intestine.
  • 81.  Constipation  Heart burn  Nausea  Belching  Bloating
  • 82.  It is important to initiate the therapy with low doses and instruct patients to take the drugs with meals to reduce the side-effects.
  • 83.  Because of bile acid sequestrants are not absorbed, an overdose could cause obstruction of the GIT, therefore treatment of an overdose involves restoring gut motility.
  • 84.  All drugs should be taken at least 1 hour before or 4-6 hours after the administration of the ion exchange resins.  High dose of bile acid sequestrant will decrease the absorption of fat soluble vitamins. E.g vit A, D, E, K.
  • 85.  It is a prescription only drug.  It is a pregnancy category C agent.  It may interfere distribution of the proper amounts of fat soluble vitamins to the fetus or pregnant women taking these agents.  It is only available 4-9 gram packets of powder to be taken as an oral suspension.
  • 86.  Lovastatin was the first agent in this drug class to be approved for use and this occurred in 1987.  It is indicated primarily for the treatment of type 2A, and 2B hyperlipidemias.  Effective in lowering the LDL cholesterol level and to some degree the triglyceride levels.  Recommended daily dose is 20-80mg/day PO.  It is a pregnancy category X agent.
  • 87.  Gemfibrozil is a fibric acid derivative that lowers VLDL level.  It is highly effective for lowering the plasma triglyceride levels.  It is indicated for the treatment of type 4 and 5 hyperlipidemias and in some cases of the type 2B form.  Available as 600mg orally tablet  It is a pregnancy category B agent
  • 88.  Nicotinic acid is also known niacin, very unique lipid lowering agent.  Nicotinic acid is a vitamin B3 drug.  It is an effective and inexpensive medication.  Niacin is often given in combination with other anti-lipemic drugs to enhance the lipid lowering effects.  It is a pregnancy category A agent.
  • 89.  Niacin is contraindicated in: 1. Hypersensitivity 2. Peptic ulcer 3. Hepatic diseases 4. Hemorrhage 5. Lactating women 6. Severe hypotension
  • 90.  Available as an over the counter drug.  Available 25, 50, 100, 250, 500, 750mg tablets.  It is commonly given in 2-4 divided doses of 1.5-6g per day.
  • 91.  Drugs that prevent the formation of a clot by inhibiting certain clotting factors are called anti-coagulants.  These agents are only given prophylactically because they have no direct effect on a blood clot.  There uses vary from preventing clot formation to preventing the extension of preformed clot or a thrombus.
  • 92.  Once a clot forms on the wall of a blood vessel, it may dislodge and travel through the blood stream.  If it goes to the brain, it causes stroke.  If it goes to the lungs, it causes pulmonary emboli.  If it goes to the veins in the lungs, it causes deep vein thrombosis.
  • 93.  Anti-coagulants can prevent all of these from occurring, if used the correct manner.  There are both orally and parenterally administered anti-coagulants.
  • 94.  Nausea  Vomiting  Bleeding  Abdominal cramp  Hypoaldosteronism
  • 95.  Symptoms that may be attributed to toxicity or an overdose of anti-coagulants are: 1. Hematuria 2. Melena (black tarry feaces) 3. Mucous membrane bleeding
  • 96.  Steps of toxicity management: 1. Discontinue the drug 2. If there is blood loss, replacement of packed red cells. 3. Give protamine sulphate, 1mg of protamine sulphate can reverse the effects of 100 units of heparin.