Download Cardiovascular Drug Agents

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Cardiac glycosides
Antidysrhythmic agents
Anti-anginal drugs
Anti-hypertensive drugs
Anti-lipemic agents
Anti-coagulants
Anti-platelets
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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.
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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.
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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.
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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. Tachycardia
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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.
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Adult dosage is 1-1.5mg/day, 0.125-0.5 mg.
Premature dosage is 0.015-0.025mg/kg.
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Anorexia
Nausea
Vomiting
Confusion
Colored vision
Headache
Fatigue
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Discontinue the drug.
Determine digoxin and electrolyte level.
Administer potassium supplements for
hypokalemia.
Start ECG monitoring.
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.
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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
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Disopyramide
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Procainamide
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Quinidine
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Class 1B
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Lidocaine
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Phenytoin
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Tocainide
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Mexiletine
Class 1C
1. Propafenone
2. Flecainide
3. Entainide
Class Two
1. Propranaolol
2. Esmolol
3. sotalol
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Class three
1. Amiodarone
2. Bretylium
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Class four
1. Adenosine
2. Verpamil
3. Diltiazem
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Hypersensitivity
Nausea
Vomiting
Diarrhoe
Dizziness
Headache
Blurred vision
The main toxic affects of the antidysrhythmics involve:
1. Heart
2. Circulation
3. CNS
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Speacific antidotes are not available and the
management of an overdose involves
maintaining adequate circulation and
respiration.
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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
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Contraindicated
1. Hypersensitivity
2. AV block
3. Abnormal rhyths
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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
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Propafenone is contraindicated:
1. Bradycardia
2. Hypersensitivity
3. Bronchial asthma
4. Hypotension
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Available orally as 150, 300mg, and the
adult dosage is 150mg q8h.
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ID/CC: A 56 year old male comes to the
cardiology unit for evaluation of ringing in his
ears (Tinnitus), dizziness, GI distress (nausea,
vomiting, diarrhea), and headaches.
HPI: He also complains of blurred vision and
impaired hearing. The patient had a
myocardial infarction one year ago and has
been receiving oral Quinidine antiarrhythmic
therapy.
Labs: CBC: normal, widening QRS.
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Treatment: Monitor ECG and vital signs,
discontinue the drug, change to different
antiarrhythmic drug. Treat cardio toxic
effects with sodium lactate.
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Discussion: Quinidine, Procainamide, and
Disopyramide are class 1A antiarrhythmic
that acts by blocking sodium channels,
increasing the effective refractory period.
They are used for both atrial and ventricular
arrhythmias. All these agents have low
therapeutic toxic ratios and may produce
severe adverse reactions. Cinchonism is
commonly produced by drugs that are
cinchona derivatives, such as Quinidine and
quinine. The effects may occur with only one
dose.
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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.
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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
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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.
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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
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Amoidarone is contraindicated in patients
1. Hypersensitivity
2. Severe bradycardia
3. Second or third degree of heart block.
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Amiodarone is available 200mg orally tablets.
Amiodarone is a pregnancy category C agent.
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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
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It is available 40, 80, 120mg tablets, and 2.5
mg/ml injection parenterally.
It is a pregnancy category C.
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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.
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It is available parenterally as a 3mg/ml
injection.
It is a pregnancy category C.
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ID/CC: A 73 year old widow visits her
cardiologist complaining of difficulty moving
her bowels for the past week, she also reports
facial flushing.
HPI: She had been regular until she began
taking verapamil for an irregular heart beat
one month ago.
PE: Mild lower leg edema, constipation.
Labs: CBC: normal
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Treatment: increase fluids in diet, regular
exercise, fruits high bulk foods or laxatives. If
persistent, change to another calcium
channel blocker.
Discussion: Verapamil is one of the agents that
block voltage dependant calcium channels,
consequently reducing muscle contractility.
Verapamil acts more specifically on
myocardial fibers than on arteriolar smooth
muscle. It is widely used for as an
antihypertensive, as antiarrhythmic, and for
the treatment of angina pectoris.
Constipation is common side-effect, other
side-effect include dizziness, facial flushing
and peripheral edema.
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ID/CC: A 45 year old female who works as a
preschool teacher complains of fatigue,
headache, dizziness, dry cough, shortness of
breath and constipation.
HPI: She has been receiving Amiodarone for 1
year for treatment for chronic palpitation that
arose spontaneously, with tachycardia that
reaches 220 beats per minute and increase
when she drinks coffee, is under stress or
smoking.
PE: Bradycardia, well hydrated, conscious,
wheezes in both lungs.
Treatment
 Discontinue the drug
 Continues monitor of ECG
 Supportive therapy
 Sodium bicarbonate
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Discussion: Amiodarone is a class 1A and
class III anti-arrhythmic drug. Adverse
reactions require careful monitoring and
include thyroid dysfunction, constipation and
pulmonary fibrosis, which may be fatal.
It may also produce bradycardia, and heart
block in susceptible individuals. Amiodarone
has a long half life.
Angina pectoris is a pain syndrome due to
induction of an adverse oxygen supply/
demand situation in a portion of the
myocardium.
 Two principal forms are recognized:
1. Classical angina (stable): is the most
common one and attacks are predictably
provoked by exercise, eating. The underlying
pathology is severe arteriosclerotic affliction
of larger coronary arteries.
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2. variant/prinzmetals/unstable angina: is an
uncommon form and attacks occur at rest or
during sleep and are unpredictable. They are
due to recurrent localized (occasionally
diffuse) coronary vasospasm which may be
superimposed on arteriosclerotic coronary
artery disease.
The three main classes of drugs used to treat
angina pectoris are:
1. Nitrates
2. Beta-blockers
3. Calcium channel blockers
4. Potassium channel blockers e.g Nicorandil.
5. Others. E.g Dipyradimole, Trimetazidane,
Ranolazine and oxyphedrine.
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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.
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Organic nitrates were introduced into
medicine in the 19th century, de-nitrition in
the smooth muscle cell releases nitric oxide
which is the main physiological vasodilator.
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
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Oral tablets
Capsules
Ointments
Patches
Inhalable sprays
Intravenous solutions
Nitrates can be classified into:
1. Rapid acting agents
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Amyl nitrate
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Nitroglycerin
2. Long acting agents
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Erythrityl tetra nitrate
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Isosorbide dinitrate
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Isosorbide mononitrate
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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.
Activation of nitric oxide, stimulates
guanosine mono-phosphate, and this results
relaxation then vasodilation.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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ID/CC: A 58 year old man comes to see his
cardiologist because of an increased need for
nitroglycerin patches in order to control his
oppressive exercise induced chest pain
(Angina).
HPI: In the past, taking one tablet five
minutes before physical activity controlled his
symptoms, now he has to take two tablets.
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The patient has continued to smoke two
packs of cigarettes each day and is concerned
that his cardiac condition is worsening
because of his increased need for medication.
PE: Obese male, BP: normal
Labs: CBC: elevated hematocrit, elevated
glucose and hypercholestremia.
Imaging: CXR: normal
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Treatment: adjust timing of nitrate
administration in order to have an 8 hour
period free of nitroglycerin. Consider
alternating with beta-blockers, calcium
channel blocking agents, beta-blockers or
other coronary vasodilators.
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Tolerance is manifested as a poor response to
a previously effective dose of nitroglycerin.
Increasing the dosage does not yield relief of
symptoms. The use of other agents, shorter
acting nitroglycerin formulations or intervals
free of nitroglycerin dosing can be tried in an
attempt to regain sensitivity to the nitrate.
Tolerance and headaches are the main
drawbacks of nitrate use for the treatment of
angina. Progression of coronary artery
disease must always be considered with
increasing nitroglycerin requirements.
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
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Centrally acting drugs
1. Clonidine
2. Guanabenz
3. Guanfacine
4. Methyldopa
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Peripherally acting drugs
1. Guanadrel
2. Guanethidine
3. Reserpine
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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.
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Dry mouth
Drowsiness
Sedation
Constipation
Headache
Sleep disorders
Nausea
Rash
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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.
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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.
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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
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Available in 0.1, 0.25mg tablets.
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Adult dose is 0.1 - 0.25mg/day divided or
single dose.
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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.
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ACEI represent a large group of antihypertensive 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.
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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.
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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.
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Enalapril is the only currently available ACEI
that is available in both oral and parentral
preparations.
Parentral formulation offers the hemodynamic benefit of inhibiting ACE activity in
an acutely ill patient who cannot tolerate oral
medications.
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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.
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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.
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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.
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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
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Diuretics are drugs, which increase renal
excretion of salt and water: are principally
used to remove excessive extracellular fluid
from the body.
In order to understand the action of diuretics
it is important to have some knowledge of the
basic processes that take place in the
nephron (unit structure of kidney.
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Approximately 180 liters of fluid is filtered
from the glomerulus into the nephron per
day. The normal urine out put is 1-5 liters
per day. The remaining is reabsorbed in
different areas of nephron.
There are three mechanisms involved in urine
formation:
a) Glomerular filtration
b) Tubular reabsorption
c) Tubular secretion. These processes normally
maintain the fluid volume, electrolyte
concentration and PH of the body fluids.
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Most of the diuretics used therapeutically act
by interfering with sodium reabsorption by
the tubules. The major groups are:
I. Thiazides and related diuretics: e.g.
Hydrochlorothiazide , chlorthalidone,
bendrofluazide.
II. Loop diuretics.
a. furosemide,
b. ethacrynic acid
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III. Potassium sparing diuretics.
a. triamterene,
b. amiloride,
c. spironolactone.
IV. Carbonic anhydrase inhibitors.
a. acetazolamide
V. Osmotic diuretics.
a. Mannitol
b. glycerol
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Loop diuretics like furosemide inhibit Na+K – 2Cl symporter in the ascending limb.
Adverse effects: Hypokalemia, nausea,
anorexia, vomiting epigastric distress, fatigue
weakness muscle cramps, drowsiness,
Dizziness, hearing impairment and deafness
are usually reversible.
Therapeutic uses: acute pulmonary edema,
edema of cardiac, hepatic and renal disease.
Hypertension, cerebral edema, in drug
overdose it can be used to produce forced
diuresis to facilitate more rapid elimination of
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Potassium sparing diuretics mechanism of
action: Potassium sparing diuretics
(spironolactone, triamterene, amiloride) are
mild diuretics causing diuresis by increasing
the excretion of sodium, calcium and
bicarbonate but decrease the excretion of
potassium.
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Adverse effects: G.I. disturbances, dry mouth,
rashes confusion, orthostatic hypotension,
hyperkalaemia, Hyponatraemia .
Therapeutic uses: used with conjunction with
thiazides or loop diuretics in edema due to,
cardiac failure nephrotic syndrome and
hepatic disease.
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IV. Carbonic anhydrase inhibitors: these
drugs like acetazolamide inhibit the enzyme
carbonic anhydrase in renal tubular cells and
lead to increased excretion of bicarbonate,
sodium and potassium ions in urine. In eye it
results in decrease information of aqueous
humor. Therefore these are used in treatment
of acute angle glaucoma. Main adverse
effects of these agents are drowsiness,
hypokalemia, metabolic acidosis and
epigastric distress.
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Osmotic diuretics: these drugs like mannitol
and glycerine (glycerol) are freely filtered at
the glomerulus and are relatively inert
pharmacologically and undergo limited
reabsorption by renal tubule. These are
administered to increase significantly the
osmolality of plasma and tubular fluid. Some
times they produce nausea, vomiting,
electrolyte imbalances. They are used in
cerebral edema and management of
poisoning.
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
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Statins
e.g, lovastatin, simvastatin, pravastatin,
atorvastatin and rosuvastatin.
2. Bile acid sequestrants (Resins)
e.g, cholestyramine, colestipol.
3. Activate lipoprotein lipase (fibric acid
derivatives)
e.g, clofibrate, gemfibrozil, bezafibrate and
fenofibrate.
4. Inhibit Triglyceride Synthesis. E.g nicotine.
1.
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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.
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The bile acid resins bind bile and this
prevents the resorption of the bile acids from
the small intestine.
Decrease LDL 15-30% and Triglyceride is not
affected (effects).
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Constipation
Heart burn
Nausea
Belching
Bloating
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It is important to initiate the therapy with low
doses and instruct patients to take the drugs
with meals to reduce the side-effects.
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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.
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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.
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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.
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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.
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Decrease LDL 20-55% and Triglyceride 1035%.
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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
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Decrease LDL 5-20% and Triglyceride 2050%.
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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
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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.
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Decrease LDL 15-20% AND Triglyceride 2050%.
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Coagulants are substances which promote
coagulation, and are indicated in hemorrhagic
states.
Fresh whole blood or plasma provide all the
factors needed for coagulation and are the
best therapy for deficiency of any clotting
factor; also they act immediately.
1.
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Vitamin K. E.g, vit k1 (phytonadione), vit k3
(menadione, acetomenaphtone). Vit k can
be water soluble or fat soluble.
1929 dam produced bleeding disorder in
chicken by feeding deficient diet. This was
later found to be due to decreased
concentration of prothrombin in blood.
In 1939, alfalfa grass isolated- vit k1, while
sardine (sea fish) is isolated-vitk2, and
synthetic compounds have been produced
by vit k3.
1.
2.
3.
4.
5.
6.
7.
Dietary deficiencies.
Prolonged antimicrobial therapy.
Obstructive jaundice
Liver disease (viral hepatitis)
Newborn
Overdose of anticoagulant
Prolonged high dose of Salicylates.
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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.
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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.
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Anti-coagulants can prevent all of these from
occurring, if used the correct manner.
There are both orally and parenterally
administered anti-coagulants.
1.
2.
3.
4.
Heparin
Warfarin
Phenindione
Hydroxy coumarin
1.
2.
3.
4.
5.
6.
Deep vein thrombosis
Myocardial infarction
Unstable angina
Rheumatic heart disease. E.g Warfarin is
effective in this case.
Cerebrovascular disease.
Vascular surgery.
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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 feces)
3. Mucous membrane bleeding
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Steps of toxicity management:
1. Discontinue the drug
2. If there is blood loss, replacement of packed
red cells.
3. Give protamine sulphate (obtained by sperm
fish), 1mg of protamine sulphate can reverse
the effects of 100 units of heparin.
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These are drugs which interfere with platelet
function and are useful in the prophylaxis of
thromboembolic disorders.
 The clinically important antiplatelt drugs are:
1. Aspirin
2. Dipyridamole
3. Ticlopidine
4. Clopidogrel
5. Abciximab
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It inhibits the enzyme COX 1 & TX-synthaseinactivating them irreversibly.
Aspirin induced prolongation of bleeding
time lasts for 5-7 days.
Maximal inhibition of platelet function occurs
at 160mg aspirin per day.
It is available 75mg, 80mg, 300mg, 360mg,
and 600mg.
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ID/CC: A 32 year old with a prosthetic heart
valve complains to his family doctor of black
tarry stools.
HPI: He had been receiving oral Warfarin to
prevent thrombus formation. Two years ago,
he had an aortic valve replacement due to
destruction of the valve secondary to
bacterial endocarditis.
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PE: BP is normal, hemorrhage, bleeding gums,
generalized bleeding.
Labs: hematuria, markedly elevated PT
(Prothrombin Time)
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Discussion: This patient has generalized
bleeding, including GI tract bleeding
secondary to Warfarin treatment. Warfarin
compounds inhibit epoxide reductase and
hepatic production of the vitamin Kdependant clotting factors (2, 7, 9, & 10).
Effects of Warfarin last between 5 to 7 days.
Warfarin crosses the placenta and is thus
contraindicated in pregnant women.
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Treatment: If significant bleeding and volume
depletion have occurred, consider fresh
frozen plasma and transfusions. Vitamin K
may be required.
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