CARDIOVASCULAR AGENTS

Review of Cardiovascular System

- The Cardiovascular includes the heart, blood and blood vessels

- Blood rich in oxygen and nutrients and hormones moves through vessels called

arteries and narrow through a structure called arterioles.

- Capillaries transport rich nourish blood to body cells and absorbed waste

products such as carbon dioxide (CO2), urea, creatinine and ammonia.

- Deoxygenated blood returns through the venules and veins to be eliminated by

the lungs and kidneys with other waste products.

- The heart pumping action serves as the energy source that circulates to body

cells. Blockage of vessels can inhibit the blood flow.

THE HEART

- The heart has four chambers. The main muscle is called myocardium that

surrounds the atria and ventricles.

- Ventricles are thick walled especially the left ventricle to achieve the muscular

force needed to pump blood to the pulmonary and systemic circulation.

- Atria are thin walled, have less pumping action and serves as receptacles for

blood from the circulation and the lungs.

- The heart has a fibrous covering called pericardium which protects it from

injury and infection.

- It has four valves that controls the blood flow between the atria and ventricles

and between the ventricles and pulmonary artery and aorta

- There are two coronary arteries, which supplies the needed oxygenated blood to

the heart itself.

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REGULATION OF HEART RATE AND BLOOD FLOW

- The heart beats approximately 60-100 beats per minute in an average adult

pumping blood into the systemic circulation.

- The average systemic arterial pressure known as the blood pressure is 120/80

mmHg.

- Arterial blood pressure is determined by peripheral resistance and cardiac

output, the volume of blood expelled from the heart in 1 minute.

- The average cardiac output is 5-8 liters per minute

- Stroke volume refers to the amount of blood ejected from the left ventricle with

each heartbeat.

- Three factors determine stroke volume; preload, contractility, and afterload.

- Preload refers to the blood flow fore that stretches the ventricle. Contractility is

the force of ventricular contraction. Afterload is the resistance to ventricular

ejection of blood

CIRCULATION

- There are two type of circulation: pulmonary and systemic circulation

- With pulmonary circulation, the heart pumps deoxygenated blood from the

right ventricle through the pulmonary artery to the lungs. In this situation, the

artery caries blood that has a high concentration of carbon dioxide. Oxygenated

blood returns to the left atrium by the pulmonary vein.

- With systemic circulation, the heart pumps blood from the left ventricle to the

aorta and to the general circulation. Artery and arterioles carry blood to

capillary bed. Nutrients in the blood are transferred to cell in exchange for

waste products. Blood returns to the heart through the venules and veins.

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CARDIAC GLYCOSIDES

- Also called “Digitalis” are very effective in the management of congestive heart

failure (CHF). When the heart muscle weakens and enlarges, it loses its ability

to pump blood through the heart and into the systemic circulation.

- Cardiac glycosides are a group of drugs that inhibit the sodium potassium

pump thus they increase intracellular calcium which causes the cardiac muscle

fibers to contract more efficiently.

- This drug preparation has major effects on the heart muscle.

a. Positive inotropic effect (increases myocardial contractility and stroke

volume)

b. Negative chronotropic effect (decreases the heart rate)

- The increase in myocardial contractility increases cardiac, peripheral and

kidney function by increasing cardiac output, decreasing preload, improving

blood flow to the periphery and the kidneys, decreasing edema, and increasing

fluid excretion.

ANTI-ANGINAL DRUGS

- Anti-anginal drugs are used to treat angina pectoris. This is a condition of acute

cardiac pain caused by inadequate blood flow to the myocardium resulting from

either plaque occlusion within or spasms of the coronary artery.

- With decrease blood flow, there is a decrease in oxygen to the myocardium,

which result in pain.

- Anginal pain is frequently described by the clients as tightness pressure in the

center of the chest and pain radiating down the left arm.

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 - Anginal attacks may lead to myocardial infarction or heart attack. Anginal

attacks usually last for only a few minutes.

TYPES OF ANGINA PECTORIS

1. Classic (stable) angina: occurs with stress or exertion

2. Unstable (pre-infarction) angina: occurs frequently over the course of the day

with progressive severity.

3. Variant (Prinzmetal, Vasospastic) angina: this type of angina occurs during rest.

 Anti-anginal drugs increase blood flow either by increasing oxygen supply or by

decreasing oxygen demand by the myocardium.

Three types of anti-anginal drugs:

1. Nitrates

2. Beta blockers

3. Calcium channel blockers

NITRATES

- Affects blood vessels in the venous circulation and coronary arteries

- They cause generalized vascular and coronary vasodilation, thus increasing

blood flow through the coronary arteries to the myocardial cells.

- This group of drugs reduces myocardial ischemia but can cause hypotension.

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Exercise V-A
Instruction. Complete this activity by providing the necessary information in the study
of the following cardiac glycosides and anti-anginal drugs.

1. Digoxin(Lanoxin)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

2. Amrinone Lactate (Inocor)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

3. Digoxin Immune Fab (Digibind)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

125
4. Nitroglycerin (Nitrostat)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

5. Isosorbide dinitrate (Isordil)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

6. Isosorbide Mononitrate (Imdur)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

126
Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

ANTI-DYSRYTHMIC DRUGS

- A cardiac dysrhythmia is defined as any deviation from the normal rate or

pattern of the heartbeat.

- This includes heart rate that are too slow (bradycardia), too fast (tachycardia),

and irregular.

- The term dysrhythmia (disturbance in heart rhythm) and arrhythmia (absence

of heart rhythm) are used interchangeably despite the slight differences in

meaning.

- The ECG identifies the type of dysrhythmia

- Cardiac dysrhythmia frequently follows myocardial infarction (heart attack) or

can result from hypoxia, hypercapnia or electrolyte imbalance.

TYPES OF ANTI-DYSRYTHMIC DRUGS

- The desired action of anti-dysrythmic drugs is to restore the cardiac rhythm to

normal.

- The anti-dysrythmic drugs are grouped into four classes:

1. Fast (Sodium) channel blockers IA, IB, IC

2. Beta Blockers

3. Drugs that prolong repolarization

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 4. Slow (Calcium) channel blockers

Exercise V-B
Instruction. Complete this activity by providing the necessary information in the
study of the following anti-anginal drugs.

1. Disopyramide Phosphate (Norpace)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

2. Procainamide HCL (Pronestyl)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

3. Mexiletine HCL (Mexitil)

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Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

4. Flecainide (Tambocor)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

5. Esmolol (Brevibloc)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

6. Adenosine (Adenocard)
Classification: ______________________________________________________________________

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Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

Exercise V-C. Study Questions.

1. Drugs interactions are associated with digitalis drugs. What are the effects of
potassium wasting diuretics and cortisone with digitalis?

2. What effect do electrolytes have on digitalis toxicity?

130
 3. How are nitroglycerin products administered? Explain. What is a common
temporary side effect of nitrates? How is this side effect treated?

DIURETIC

- Diuretics are used for two main purposes.

a. To decreases hypertension (lower blood pressure)

b. To decrease edema (pulmonary and peripheral) in congestive heart

failure and renal or liver disorders.

- Diuretics produce increase urine flow (diuresis) by inhibiting sodium and water

reabsorption from the kidney tubules.

- Most sodium and water reabsorption occurs throughout the renal tubular

segments.

- Diuretics can affect one or more segment of the renal tubules

- The diuretic effect depends on the drug reaching the kidneys and its

concentration in the renal tubules.

- Diuretics have antihypertensive effect by promoting sodium and water loss by

blocking sodium and chloride. This will cause a decrease in fluid volume and

lowering blood pressure.

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Categories of Diuretics

1. Thiazide and thiazide like diuretics:

- This category of diuretics acts on the distal convoluted tubule beyond the Loop

of Henle, to promote sodium, chloride and water excretion.

- Thiazides are used to treat hypertension and peripheral edema

- The thiazides diuretics are used primarily for clients with normal kidney

function

- Thiazides causes a loss of sodium, potassium, magnesium but they promote

calcium absorption.

2. Loop (High Ceiling) Diuretics

- This category of diuretics acts on the ascending loop of henle by inhibiting

chloride transport of sodium into the circulation. As a result, sodium and water

are loss. Loop diuretics can affects blood sugar and increase uric acid level.

This drug is more potent than thiazides as diuretics, inhibiting reabsorption of

sodium two to three times more effectively, but they are less effective as

antihypertensive agents.

3. Osmotic Diuretics

- This category of diuretics increases the osmolality (concentration) of the plasma

and fluid in the renal tubules.

- Sodium, chloride, potassium and water are excreted

- This group of drugs are used to prevent kidney failure, to decrease intracranial

pressure and to decrease intraocular pressure.

4. Carbonic Anhydrase Inhibitor

- This type of diuretic blocks the action of the enzyme carbonic anhydrase which

is needed to maintain acid base balance.

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 - Inhibition of this enzyme causes increase sodium, potassium and bicarbonate

excretion. This group of drug is used primarily to decrease IOP in clients with

glaucoma.

5. Potassium sparing diuretics

- This kind of diuretics are considered weaker than thiazide and loop diuretics.

They are used as mild diuretics or in combination with another diuretic.

Continued use of this drug requires a daily oral potassium supplement because

the kidneys excretes potassium, sodium and body water.

Exercise V-D
Instruction. Complete this activity by providing the necessary information in the
study of the following diuretic drugs
1. Chlorothiazide (Diuril)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

2. Hydrochlorothiazide (Hydrodiuril)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

133
3. Chlorthalidone (Hygroton)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

4. Isosorbide dinitrate (Isordil)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

5. Furosemide (Lasix)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

134
Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

6. Bumetanide (Bumex)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

7. Mannitol

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

8. Acetazolamide (Diamox)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

135
Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

9. Spironolactone (Aldactone)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

Exercise V-E. Critical Thinking Study

1. How does hydrochlorothiazide differ from furosemide? What are their

similarities and differences?

2. Why is it necessary for the client to eat foods rich in potassium when taking
high ceiling or Loop diuretics? Explain.

136
 3. A client takes triamterene. What type of diuretic is triamterene? What effect can
this have on the potassium level?

ANTIHYPERTENSIVE DRUGS

Hypertension

- is an increase in blood pressure such as that systolic pressure greater than

140 mmHg and the diastolic pressure is greater than 90 mmHg.
- Essential hypertension is the most common type of hypertension affecting
90% of persons with high blood pressure. The origin of essential
hypertension is unknown but there are contributing factors like:
1. Family history of hypertension
2. Hyperlipidemia
3. African American background
4. Diabetes
5. Obesity
6. Aging
7. Stress
8. Excessive smoking and alcohol congestion

137
Selected regulator of blood pressure

- The kidneys and blood vessels strives to regulate and maintain a blood
pressure
- The kidneys regulate blood pressure via the renin-angiotensin aldosterone
system.
- Baroreceptors in the aorta and carotid sinus in the medulla also assist in
regulation of blood pressure. Catecholamines such as norepinephrine
release from the sympathetic terminals and epinephrine release from the
adrenal medulla increased blood pressure through vasoconstriction activity.

- Other hormones that contribute to blood pressure regulation are the

antidiuretic hormone (ADH) and the anti-natriuretic factor (ANP). The ADH
is release from the posterior pituitary gland upon stimulation of the
hypothalamus. ANP is release by the atrium of the heart and respond to
fluid overload by stimulating the kidneys to increase glomerular filtration
rate thereby increasing elimination of Na and water.

Physiologic Factors that contributes to hypertension

- A diet with increase fat and carbohydrate can increase blood pressure.
Carbohydrate intake can increase sympathetic nervous system activity
- Alcohol increase renin secretions causing the production of angiotensin II.
- Obesity affects the sympathetic activity and cardiovascular system by
increasing cardiac output, stroke volume and left ventricular filling.
Non-pharmacologic control of hypertension

- There are many non-pharmacologic ways to decrease blood pressure

a. Stress reduction technique
b. Exercise
c. Salt restriction
d. Reduction in alcohol and smoking
e. Weight reduction

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Pharmacologic control of hypertension

- Antihypertensive drugs used either alone or in combination with other

drugs. They are classified into six categories. A) Diuretics B) Sympatholytics
(beta/alpha/beta and alpha adrenergic blockers, centrally acting alpha
agonist) C) Direct acting arteriolar vasodilators D) ACE inhibitors E)
Angiotensin receptor II blockers F) Calcium channel blockers
Diuretics

- Promotes sodium depletion, which decreases extracellular fluid volume. It is

one of the first line drug in the management of hypertension.
Beta Adrenergic Blockers

- Frequently called beta-blockers are used as step I antihypertensive drugs or

in combination with a diuretic as step II approach in hypertension
management. Also use as anti-anginals and anti-dysrythmics.
- Beta adrenergic blockers reduce cardiac output by diminishing the
sympathetic nervous system response thereby decreasing the basal
sympathetic tone. With continued used of beta-blockers vascular resistance
is diminished and blood pressure is lowered.

Exercise V-F.

Instruction. Complete this activity by providing the necessary information in the

study of the following categories of drugs.

1. Atenolol (Tenormin)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

139
2. Acebutolol HCL (Sectral)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

3. Propranolol (Inderal)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

4. Clonidine (Catapres)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

5. Methydopa (Aldomet)

140
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

6. Prazosin HCL (Minipress)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

7. Reserpine (Serpasil)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

141
Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

8. Hydralazine HCL (Apresoline)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

9. Phentolamine (Regitine)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

Angiotensin Converting Enzymes Inhibitors (ACE Inhibitors)

- Drugs in this group inhibit ACE, which in turn inhibit the formation of
Angiotensin II, a vasoconstrictor and blocks the release of aldosterone. When
aldosterone is blocked, sodium is excreted along with water and potassium

142
 is retained. ACE inhibitors cause little change in cardiac output or heart
rate and they lower peripheral resistance.

Angiotensin II Receptor Antagonist

- These are new groups of anti-hypertensive drugs

- This group is similar to ACE inhibitors and that they prevent the release of
aldosterone (sodium retaining hormone).
- They acts on the renin angiotensin system

Calcium Chanel Blockers

- Slow calcium channels are found in the myocardium (heart muscle) and
smooth muscle cells.
- Free calcium increases muscle contractility, peripheral resistance and blood
pressure.
- This drug is also called calcium antagonist, decreasing calcium levels and
promote vasodilation.

143
 - The large central arteries are not as sensitive to calcium blockers as the
coronary and cerebral arteries and the peripheral resistance vessels.

Exercise V-G.

Instruction. Complete this activity by providing the necessary information in the

study of the following categories of antihypertensive drugs.
1. Captopril (Capoten)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

2. Enalapril Maleate (Vasotec)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

144
3. Benazepril HCL (Lotensin)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

4. Lozartan Potassium (Cozaar)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

5. Verapamil (Calan)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

145
Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

6. Diltiazem HCL (Cardizem)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

7. Amlodipine (Norvasc)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

8. Nifidipine (Procardia)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

146
Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

9. Nicardipine HCL (Cardene)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

Exercise V-H. Critical thinking case study

1. Why should the client’s blood glucose level should be monitored while taking
hydrochlorothiazide?

2. What are the similarities and differences between ACE inhibitors and
Angiotensin receptor II blockers?

147
 3. What is the purpose of stepped-care approach or modified pharmacologic
approach in the treatment of hypertension? Explain the function of diuretic in
controlling blood pressure?

ANTICOAGULANTS, ANTIPLATELES AND THROMBOLTYTICS

Introduction

Various drugs are used to maintain or restore circulation. The three major
groups of these drugs are (1) anticoagulants, (2) antiplatelet (antithrombotic)
and (3) thrombolytic. The anticoagulants prevent the formation of clots that
inhibit circulation. The antiplatelet prevent platelet aggravation (clumping
together of platelets to from a clot) the thrombolytic, popularly called clot
busters, attack and dissolve blood clots that have already formed.

148
Thrombus Formation

Thrombosis is the formation of a clot in an arterial or venous vessel. The

formation of an arterial thrombus could be caused by blood stasis (because of
decreased circulation), platelet aggregation on the blood vessel wall, and blood
coagulation.

Arterial clots are usually made up of both white and red clots with the white
clots (platelets) initiating the process, followed by fibrin formation and the
trapping of red blood cells in the fibrin mesh.

Blood clots found in the veins are from platelet aggregation with fibrin that
attaches to red blood cells. Both types of thrombus can be dislodged from the
vessel and become an embolus moving blood clot through the blood stream.

As the thrombus inhibits blood flow, fibrin, platelets, and red blood cells
(erythrocytes) surround the clot, building the clots size and structure. As the
clot occludes the blood vessel, tissue ischemia occurs

Anticoagulants

Anticoagulants are used to inhibit clot formation. Unlike thrombolytic, they do

not dissolve clots that have already formed but rather act prophylactically to
prevent new clots from forming, anticoagulants are used in clients with venous
arterial vessel disorders that put them at high risks for clot formation.

The venous problems include deep vein thrombosis (DVT) and pulmonary
embolism, and the arterial problems include coronary thrombosis (myocardial
infarction), presence of artificial heart valves, and cerebrovascular accidents
(CVA, or stroke)

149
Heparin

Heparin introduced in 1938, as natural substance in the liver that prevents

clot information. It was first used in blood transfusions to prevent clotting.

Heparin is used in open-heart surgery to prevent blood from clotting and in the
critically ill client with disseminated intravascular coagulation (DIC). Its
primary use is to prevent venous thrombosis which can lead to pulmonary
embolism or stroke.

Heparin prolongs clotting time, partial thromboplastin time (PTT) and activated
partial thromboplastin time (ApTT) are monitored during therapy. Heparin can
be decrease the platelet count, causing thrombocytopenia. If hemorrhage
occurs, the anticoagulant antagonist protamine sulfate is given IV

Oral Anticoagulants

Warfarin (Coumadin) is the most commonly prescribed oral anticoagulant.

Before warfarin is synthesized from dicumarol. Before warfarin was available
for human use, it was used in rodenticides to kill rats by causing hemorrhage.

Oral Anticoagulant inhibit hepatic synthesis of vitamin K, thus affecting the

clotting factors II, VII, IX and X.

These drugs are used mainly to prevent thromboembolic condition such as

thrombophlebitis, pulmonary embolism, and embolism formation caused by
atrial fibrillation, which can lead to a stroke (CVA).

Oral Anticoagulant pro long clotting time and are monitored by the
prothrombin time (PT). This laboratory test is usually performed before
administering the next drug dose until the therapeutic level has been reached.

International normalized ratio (INR) is a new laboratory test introduced to

account for the variability in reported PT test are compared with an

150
international reference standard and the reported as the INR. The normal INR
is 1.3 to 1.2. Clients on warfarin therapy are maintained at an INR of 2 to 3.

HEPARIN AND WARFARIN SODIUM

Drug class: Anticoagulant

Trade Name: Heparin: Lipo-Hepin,
calciparine, hepalean, calcilean

Warfarin: Coumadin, warfilone

Pregnancy category: D

Drug-Lab-Food Interactions
Drug: increase the effect with aspirin,
NSAIDs thrombolytic, probenecid:

Contraindications decreased effect with nitroglycerin,

Heparin warfarin: bleeding disorder, protamine

peptic ulcer, severe. Hepatic or renal Warfarin: Increase effect with

disease, hemophilia, CVA amiodarone, aspirin, NSAIDs,

Warfarin: blood dyscrasias, eclampsia sulfonamides, thyroid drugs,

allopurinol, histamine, blockers, oral
antibiotics, vitamin E; decrease effect
with barbiturates, laxatives,
phenytoin, estrogens, vitamins C and
K, oral contraceptives, rifampin.
Lab: May increase AST, ALT
Food: Decrease diet rich in vitamin K

151
Therapeutic Effects/ Uses
Heparin/warfarin: to prevent
blooding clotting
Mode of Action: heparin: inhibits
thrombin, which prevents the
conversion of fibrinogen to fibrin
Warfarin: depression of hepatic
synthesis of vitamin K clotting factors

Side effects
Heparin: itching, burning
Warfarin: anorexia, nausea, vomiting,
diarrhea, abdominal cramps, rash,
fever

Comparison of oral and parenteral anticoagulants

Factors to consider Heparin Warfarin (Coumadin)

Methods of Subcutaneously Primarily orally
administration Intravenously
Drug action Blinds with anti- Inhibits hepatic
thrombin III, which synthesis of vitamin K,
inactivates thrombin which decreases
and clotting factors, prothrombin and the
thus inhibiting fibrin clotting factors VII, IX,
formation X.
Uses Treatment of venous Treatment of deep
thrombosis, pulmonary venous thrombosis,

152
 embolism, pulmonary embolism,
thromboembolic transient ischematic
complications (e.g heart attack, prophylactic for
surgery, disseminated cardiac valves.
intravascular
coagulation)
Contraindication/caution Hemophilia peptic Hemophilia, peptic
ulcer, severe (stage 3 or bleeding ulcer, blood
4) hypertension, severe dyscrasias, severe liver
liver or renal disease, or kidney disease, acute
dissecting aneurysm myocardial infarction,
alcoholism
Laboratory Tests test partial Prothrombin time (PT):
thromboplastin time 11-15 sec
(PTT): 60-70 sec Anticoagulant: 1.25-2.5
anticoagulant: 1.5-2 X X control in seconds
control in seconds International
activated partial normalized ration (INR):
thromboplastin time 1.3-2.0
(Aptt): 20-35 sec Anticoagulant: INR 2.0-
3.0
Anticoagulant: INR 2.0-
3.0
Prosthetic heart valves:
INR up to 3.5

153
Anticoagulants, Antiplatelet and Anticoagulant antagonists

Exercise V-I

Instruction. Complete this activity by providing the necessary information in

the study of the following categories of drugs.

1. Heparin
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

154
2. Coumarins dicumatol (bishydroxycoumarin)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

3. Warfarin (Coumadin)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

4. Anagrelide HCI: (Agrylin)

Classification: _______________________________________________________________

Action:______________________________________________________________________________
_______________________________________________________________________

Uses/Indication: _____________________________________________________________

Basis for therapeutic effect: __________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
________________________________________________________

5. Aspirin
Classification: _______________________________________________________________

155
Action:______________________________________________________________________________
_______________________________________________________________________

Uses/Indication: _____________________________________________________________

Basis for therapeutic effect: __________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
________________________________________________________

6. Cilostazol (pletal)
Classification: _______________________________________________________________

Action:______________________________________________________________________________
_______________________________________________________________________

Uses/Indication: _____________________________________________________________

Basis for therapeutic effect: __________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
________________________________________________________

7. Clopidogrel (Plavix), dipyridamole (persantine)

Classification: _______________________________________________________________

Action:_______________________________________________________________________
______________________________________________________________________________

Uses/Indication:
_____________________________________________________________

Basis for therapeutic effect: __________________________________________________

Drug/food/lab/
interactions:_________________________________________________________________
_______________________________________________________________

156
8. Ticlopidine (Ticlid)
Classification: _______________________________________________________________

Action:_______________________________________________________________________
______________________________________________________________________________

Uses/Indication:
_____________________________________________________________

Basis for therapeutic effect: __________________________________________________

Drug/food/lab/
interactions:_________________________________________________________________
_______________________________________________________________

9. Vitamin K, phytonadione (aquamephyton, mephyton, konakion)

Classification: _______________________________________________________________

Action:_______________________________________________________________________
______________________________________________________________________________

Uses/Indication:
_____________________________________________________________

Basis for therapeutic effect: __________________________________________________

Drug/food/lab/
interactions:_________________________________________________________________
_______________________________________________________________

Oral anticoagulant

Bleeding occurs in about 10% of clients taking oral anticoagulants. Vitamin K,

(phytonadione), antagonist of warfarin, is used for warfarin overdose or
uncontrollable bleeding. Usually to 1 to 10 mg of vitamin K, is given at once if

157
bleeding occurs. If vitamin K, fails to control bleeding then fresh whole blood or
fresh-frozen plasma or platelets are generally given

Antiplatelet Drugs

Antiplatelet are used to prevent thrombosis in the arteries by suppressing

platelet aggregation. Heparin and warfarin prevent thrombosis in the veins.

Antiplatelet drug therapy us mainly for prophylactic use such as prevention of

myocardial infarction or stroke for clients with familial history, prevention of a
repeat myocardial infarction or stroke prevention of a stroke for clients having
transient ischemic attacks (TIAs)

Thrombolytics

Thromboembolism (occlusion of an artery or vein caused by a thrombus or

embolus results in ischemia (deficient blood flow) that causes necrosis (death)
of the tissue distal to the obstructed area it takes approximately 1 to 2 weeks
for the blood clot to disintegrate by natural fibrinolytic mechanisms. If a new
thrombus or embolus can be dissolved more quickly, the tissue necrosis is
minimized and blood flow to the area is reestablished faster. This is the basis
for thrombolytic therapy.

CLOPIDOGREL BISULFATE

Drug Class: Antiplatelet

Trade name: Plavix

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Contraindications: Intracranial hemorrhage, ulcer

Caution: Liver, disease, GI bleeding, surgery, bleeding

Drug-Lab-Food Interactions

Drug: may increase when taken with NSAIDs interferes with metabolism of
phenytoin, warfarin, and fluvastatin.

Lab: prolongs, bleeding time

Herb: may increase bleeding when taken with ginger, garlic, ginkgo, and
feverfew.

Therapeutic Effects/ Uses

To prevent reoccurrence of a MI, stroke and prevent vascular death

Mode of Action: it inhibits platelet aggregation. It prevents the enzyme, ADP,

from binding with ADP platelet receptor

Side Effects/ Uses

Upper RTI, flulike symptoms, dizziness, headaches, fatigue, chest pain,

diarrhea

TISSUE PLASMINOGEN ACTIVATOR (TPA)

Drug Class: Thrombolytic agent

Trade name: TPA, alteplase

159
Contraindications: bleeding disorders

Therapeutic Effects/ Uses : To dissolve clot following an acute MI, pulmonary

embolism, acute ischemic stroke

Mode of action: TPA promotes of plasminogen to plasmin: an enzyme, digests

the fibrin matrix of clots. TPA initiated fibrinolysis

Side Effects : Bleeding

Exercise V-J

Instruction. Complete this activity by providing the necessary information in

the study of the following category of drugs.

160
1. Thrombolytics anistreplase (APSAC, Eminase)
Classification: _______________________________________________________________

Action:_______________________________________________________________________
______________________________________________________________________________

Uses/Indication:
_____________________________________________________________

Basis for therapeutic effect: __________________________________________________

Drug/food/lab/
interactions:_________________________________________________________________
_______________________________________________________________

2. Reteplase (Retavase)
Classification: _______________________________________________________________

Action:_______________________________________________________________________
______________________________________________________________________________

Uses/Indication:
_____________________________________________________________

Basis for therapeutic effect: __________________________________________________

Drug/food/lab/
interactions:_________________________________________________________________
_______________________________________________________________

3. Streptokinase (stretase, kabikinase)

Classification: _______________________________________________________________

Action:_______________________________________________________________________
______________________________________________________________________________

Uses/Indication:
_____________________________________________________________

Basis for therapeutic effect: __________________________________________________

Drug/food/lab/
interactions:_________________________________________________________________
_______________________________________________________________

161
Exercise V-K. Study Questions

1. In what routes can heparin be administered? When? Why? Give

rationales.

2. What drugs enhance the action of warfarin (Coumadin) therapy

monitored? Explain

3. Explain how protamine is used. What is its action?

4. What are the differences between an anticoagulant and a thrombolytic?

162
ANTILIPIDEMICS AND PERIPHERAL VASODILATORS

Various drugs are used to maintain or decrease blood lipid concentrations and
promote dilation of vessels. Antilipidemics that lower blood lipids are also
called hypolipidemics or antilipidemics. Peripheral vasodilators are drugs that
dilate vessels that have been narrowed by vasospasm.

Antilipidemics

Antilipidemics lower abnormal blood lipid levels. Lipids composed of

cholesterol, triglycerides and phospholipids are transported in the body are
bound to protein in various amounts. These lipoproteins are classified as very
low- density lipoproteins (LDL)

The HDL (friendly or good lipoproteins) have a higher percentage of protein and
less lipids. Their function is to remove cholesterol and triglycerides and
contribute to atherosclerotic cholesterol plaque in the blood vessels; they are
bad lipoproteins.

LIPOPROTEIN GROUPS

Composition of the Lipoproteins

163
 Lipoproteins Protein % Cholesterol % Triglycerides Phospholipids
Subgroups % %
Chylomicrons 1-2 1-3 80-95 3-6
Very low 6-10 8-20 45-65 15-20
density
(VLDL)
Low density 18-22 45-50 4-8 18-24
(LDL)
High density 45-55 15-20 2-7 26-32
(HDL)

Types of Antilipidemics

Drugs that lower lipid levels include bile-acid sequesstrants fibrates (fibric
acid), nicotinic acid and hepatic 3 hydroxy 3 thylutaryl coenzyme A (HMG-CoA)
reductase inhibitors (statins). The statins have fewer adverse effects and are
well tolerated.

If antilipidemic therapy is withdraws, cholesterol and LDL levels. The client

taking an antilipidemic should understand that antilipidemic drug therapy is a
lifetime commitment for maintaining a decrease in serum lipid levels. Abruptly
stopping the stain drug could cause the client to have a threefold more
rebound effect that may cause death form an AMI

ATORVASTATIN

Drug class

Antilipidemic: HMG- CoA reductase Inhibitor

Trade Name: Lipitor

164
Contraindications

Active liver disease, pregnancy

Cause: History of liver disease, increase alcohol ingestion, trauma, severe

metabolic endocrine disorders, uncontrolled seizures

Dug-Lab-Food Interactions

Drug: Decrease effect with antacids, propranolol. May increase digoxin level,
oral contraceptives. Increase effects with macrolide antibiotics, antifungals

Exercise V-L.

Instruction. Complete this activity by providing necessary information in the

study of the following drugs.

1. Bile-Acid Sequestrants cholestyramibe resin (Questran)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

2. Fibrates (Fibric acid) clofibrate (Atromid S)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

165
Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

3. Gemfibrozil (Lopid)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

Peripheral Vasodilators

A common problem in older adults is peripheral arterial (vascular) disease

(PAD, PVD). It is characterized by numbness and coolness of the extremities,
intermittent claudication (pain and weakness of limb when walking but no
symptoms at rest) and possible lug ulcers. The primary cause is
arteriosclerosis and hyperlipidemia resulting in atherosclerosis

Exercise V-M.

Instruction: Complete this activity by providing necessary information in the

study of the following drugs

1. Atorvastatin calcium (Lipitor)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

166
Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

2. Pravastatin sodium (Pravachol)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

ISOXSUPRINE HCI

Dug class: Peripheral Vasodilator

Trade Name: Vasodilan, Vasoprine

Contraindications

Arterial bleeding, severe hypertension, postpartum. Tachycardia

Caution: Bleeding disorders, tachycardia

Drug-Lab-Food Interactions

Drug: Decrease blood pressure with antihypertensive

Therapeutic Effects/ Uses

To increase circulation caused by peripheral vascular disease and

cerebrovascular insufficiency

Mode of action: action is directly on vascular smooth muscle.

167
Side effects

Nausea, vomiting, dizziness, syncope, weakness, tremors, rash, flush,

abdominal distention, chest pain.

Pentoxifylline

Pentoxifylline (Trental) classified as a hemorrheologic agent, improves

microcirculation and tissue perfusion by decreasing blood viscosity and
improving the flexibility of erythrocytes thus increasing tissue oxygenation.

It is not a vasodilator, although it dilates rigid arteriosclerotic blood vessels

including arterioles, capillaries and venules.

Exercise V-N

Instruction. Complete this activity by providing the necessary information in

the study of the following categories of drugs.

1. Isoxuprine HCI (Vasodilan)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

2. Tolazoline HCI
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

168
Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

3. Priscoline HCI
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

Exercise V-O

Instruction. Complete this activity by providing the necessary information in

the study of the following drugs.

1. Ergoloid mesylates (Hydergine)

Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

2. Papaverine (Pavabid)
Classification: ______________________________________________________________________

169
Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

3. Cilostazol (Pletal)
Classification: ______________________________________________________________________

Action:______________________________________________________________________________
_____________________________________________________________________________________

Uses/Indication: ____________________________________________________________________

Basis for therapeutic effect: _________________________________________________________

Drug/food/lab/
interactions:________________________________________________________________________
______________________________________________________________________

Exercise V-P. Critical thinking case study

1. How does simvastin differ from genfibrozil?

2. J. H is on vacation and does not have enough simvastin tablets. What

should he do?

170
3. Explain how the stain drugs decrease cholesterol?

4. What are the uses of peripheral vasodilators? What two common side
effects can occur?

171