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Focus on
PHARMACOLOGY
ESSENTIALS FOR HEALTH PROFESSIONALS
CHAPTER
22
Drugs Used to
Treat Vascular
Conditions
Vascular System
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•
•
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Arterial pressure
Capillary pressure
Venous pressure
Blood pressure (BP): created by
pumping action of heart; in arteries, BP
rises during ventricular systole and falls
during ventricular diastole
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Factors That Affect BP
• Cardiac output: volume of blood
pumped per minute (determined by
heart rate and stroke volume—amount
of blood pumped by ventricle in one
contraction)
• Peripheral resistance: friction in arteries
as blood flows through
• Blood volume: amount of blood in
vascular system
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Figure 22-1
The structure of an artery, showing the outer protective layer, muscle
layer, elastic layer, and inner lining. © Dorling Kindersley.
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Table 22-1
Classification of Blood Pressure in Adults
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Hypertension
• Primary: 90% of cases
• Secondary: such as nephrosclerosis,
hyperaldosteronism, or
pheochromocytoma
• Hypertensive crisis: severe elevation
• Major cause of CVA
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Antihypertensive Agents
• Diuretics: reduce blood volume
• Beta-blockers: slow heart rate and
dilate vessels
• Vasodilators: dilate vessels
• Calcium channel blockers: slow heart
rate, reduce conduction irritability,
dilate vessels
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Antihypertensive Agents
• ACE inhibitors: vasodilate and increase
renal blood flow
• Angiotensin-receptor blockers (ARBs):
block vasoconstriction
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Table 22-2
Most Commonly Prescribed Antihypertensive Agents
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Table 22-2 (continued) Most Commonly Prescribed Antihypertensive Agents
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Table 22-2 (continued) Most Commonly Prescribed Antihypertensive Agents
Focus on Pharmacology: Essentials for Health Professionals, Second Edition
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Table 22-2 (continued) Most Commonly Prescribed Antihypertensive Agents
Focus on Pharmacology: Essentials for Health Professionals, Second Edition
Jahangir Moini
Table 22-2 (continued) Most Commonly Prescribed Antihypertensive Agents
Focus on Pharmacology: Essentials for Health Professionals, Second Edition
Jahangir Moini
Table 22-2 (continued) Most Commonly Prescribed Antihypertensive Agents
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Table 22-2 (continued) Most Commonly Prescribed Antihypertensive Agents
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Alpha- and Beta-Blockers: Uses
• Used to treat mild, moderate, and
severe hypertension
• Used alone or in combination with other
antihypertensive agents, especially
thiazide diuretics
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Alpha- and Beta-Blockers:
Adverse Effects
•
•
•
•
•
Postural hypotension
Dizziness or vertigo
Headache
Bronchospasm
Dyspnea
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Alpha- and Beta-Blockers:
Contraindications
• Contraindicated in bronchial asthma,
uncontrolled cardiac failure, cardiogenic
shock, severe bradycardia
• Safe use during pregnancy and
lactation, or in children not established.
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Alpha- and Beta-Blockers:
Patient Information
• Advise patients to change positions
slowly to avoid dizziness and to avoid
driving or hazardous activities until
response to drug is known.
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Alpha- and Beta-Blockers:
Use in Older Adults
• Older adults are especially sensitive to
hypotensive effects of these drugs.
• Warn patients to avoid hazardous
activities.
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Centrally Acting
Adrenergic Blockers: Uses
• Work by reducing hyperactivity in
medulla oblongata in brain to reduce
vascular resistance and cardiac output
• Used to manage hypertension and
usually combined with diuretics
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Centrally Acting Adrenergic
Blockers: Adverse Effects
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•
•
•
•
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Drowsiness or sedation
Headache
Nightmares
Anxiety
Hypotension
Congestive heart failure
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Centrally Acting Adrenergic
Blockers: Contraindications
• Contraindicated in pregnancy, lactation,
hepatitis, cirrhosis, blood dyscrasias
• Use cautiously in kidney disease,
angina, and mental depression
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Centrally Acting Adrenergic
Blockers: Patient Information
• Advise patients to avoid hazardous
activities until response to drug is
known.
• Instruct patients to check with
physician before taking OTC
medications.
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Peripherally Acting
Adrenergic Blockers: Uses
• Inhibit norepinephrine release to
reduce vascular tone in veins and
arteries
• Used for severe hypertension or as
adjunctive therapy in severe
hypertension
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Peripherally Acting Adrenergic
Blockers: Adverse Effects
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•
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Drowsiness
Fatigue
Headache
Confusion
Palpitation
Dry mouth
Dyspnea
Nausea and vomiting
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Peripherally Acting Adrenergic
Blockers: Contraindications
• Contraindications include mental
depression, acute peptic ulcer, and
ulcerative colitis
• Use cautiously in diabetes mellitus,
impaired renal or hepatic function,
coronary disease with insufficiency,
recent MI.
• Interact with alcohol, reserpine,
norepinephrine, and antidepressants
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Peripherally Acting Adrenergic
Blockers: Patient Information
• Advise patients to change positions
carefully and slowly to avoid dizziness.
• Instruct patients to take at same time
each day.
• Advise patients to check with their
physician before taking OTC drugs.
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ACE Inhibitors: Uses
• Decrease formation of angiotensin II,
which lowers blood volume and BP
• Used to treat severe hypertension and
CHF; drug of choice for primary
hypertension
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Figure 22-2
The renin–angiotensin system.
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ACE Inhibitors: Adverse Effects
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•
•
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Loss of taste
Photosensitivity
Severe hypotension
Hyperkalemia
Renal impairment
Blood dyscrasias
Dizziness
Angioedema
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ACE Inhibitors:
Contraindications
• Contraindicated in angioedema, CHF,
pregnancy and lactation, renal
impairment, scleroderma, lupus
erythematosus, hypovolemia
• Interact with potassium-sparing
diuretics, aspirin and NSAIDs, lithium
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ACE Inhibitors:
Patient Information
• Instruct patients to report vomiting or
diarrhea and to check with physician
before taking OTC drugs.
• Advise patients to inform surgeons or
dentists of ACE inhibitor use.
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ACE Inhibitors and Diabetes
• ACE inhibitors can produce
hypoglycemia in diabetic patients.
• Advise patients to monitor blood
glucose levels during first few weeks of
ACE inhibitor therapy.
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ARBs: Uses
• Inhibit binding of angiotensin II to
angiotensin I receptor in vascular
smooth muscle, thereby blocking
vasoconstriction and aldosterone
secretion
• Used to manage hypertension and treat
CHF
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ARBs: Adverse Effects
• Common: similar to those of ACE
inhibitors
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ARBs: Contraindications
• Contraindicated in bilateral artery
stenosis, overt cardiac failure,
cardiogenic shock, pregnancy, lactation
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ARBs: Contraindications
• Use cautiously in asthma, COPRD,
peripheral vascular disease, diabetes,
hyperthyroidism, renal and hepatic
insufficiency.
• Interact with amiodarone and betablockers
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ARBs: Patient Information
• Advise patients to report dizziness.
• Advise female patients to immediately
report pregnancy and to avoid
breastfeeding.
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Vasodilators: Uses
• Produce direct relaxation of vascular
smooth muscle, resulting in
vasodilation
• Used with beta-blockers and diuretics
to treat hypertension
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Vasodilators: Adverse Effects
•
•
•
•
Headache
Dizziness
Tachycardia
Nausea and vomiting
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Vasodilators: Contraindications
• Use of fenoldopam and beta-blockers is
contraindicated.
• Use of hydralazine is contraindicated in
CAD, mitral valvular rheumatic heart
disease, and MI.
• Use cautiously in CVA, renal
impairment, CAD.
• Interact with epinephrine,
norepinephrine, guanethidine
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Congestive Heart Failure (CHF)
• Heart pumps at insufficient rate
• Kidneys retain sodium and water
• Fluid accumulates in interstitial space
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Figure 22-3 Human heart with atrium and ventricles highlighted to illustrate the flow
of blood through the chambers and pulmonary blood vessels. Arrows depict the path of
blood through the open valves. © Dorling Kindersley.
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Figure 22-4
Signs of congestive heart failure with pulmonary congestion.
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Table 22-4
Main Classes of Drugs Used for Congestive Heart Failure
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Table 22-4 (continued) Main Classes of Drugs Used for Congestive Heart Failure
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Figure 22-5
Mechanisms of action of drugs used for congestive heart failure, including
cardiac glycosides.
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Cardiac Glycosides: Uses
• Work by increasing cell calcium
concentration to enhance contractility
of cardiac muscle
• Include cardiac glycosides and betaadrenergic agonists
• Used to relieve CHF symptoms; do not
reverse CHF
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Cardiac Glycosides:
Adverse Effects
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•
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Fatigue
Muscle weakness
Headache
Mental depression
Visual disturbances
Anorexia
Nausea and vomiting
Diarrhea
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Cardiac Glycosides:
Contraindications
• Contraindicated in ventricular
fibrillation, ventricular tachycardia
• Use cautiously in renal insufficiency,
hypokalemia, advanced heart disease,
acute MI, hypothyroidism, pregnancy,
lactation, and in older adults.
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Cardiac Glycosides:
Patient Information
• Advise patients to report any of the
following:
– Anorexia
– Nausea and vomiting
– Diarrhea
– Visual disturbances (which may be signs of
toxicity)
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Digoxin and Foxglove
• Digoxin is derived from foxglove, a
purple flowering plant.
• Oleander and lily of the valley also have
cardiac glycoside properties.
• Patient must not take digoxin along
with oleander or lily of the valley.
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Other Agents for CHF
• Beta-agonists: improve cardiac
performance by positive inotropic
effects and vasodilation
• Phosphodiesterase inhibitors (amrinone
and milrinone): increase force of heart
contraction and cause vasodilation
• Diuretics: relieve pulmonary congestion
and peripheral edema by decreasing
plasma volume
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Hyperlipidemia
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High-density lipoproteins (HDL)
Low-density lipoproteins (LDL)
Very-low-density lipoproteins (VLDL)
Triglycerides (TG)
Hypercholesterolemia: several types
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Table 22-5
Antihyperlipidemic Drugs
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Table 22-5 (continued) Antihyperlipidemic Drugs
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Bile Acid Sequestrants: Uses
• Increase binding of cholesterol to bile
acids that are excreted in feces; lowers
levels of circulating LDL and cholesterol
• Used to treat primary hyperlipidemias
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Bile Acid Sequestrants:
Adverse Effects
•
•
•
•
Constipation
Nausea
Flatulence
Impaired absorption of fat-soluble
vitamins
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Bile Acid Sequestrants:
Contraindications
• Contraindicated in bowel obstruction,
dysphagia, swallowing disorders, major
GI tract surgery
• Safety in pregnancy and lactation or in
children not known.
• Interact with intestinal absorption of
many drugs
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Bile Acid Sequestrants:
Patient Information
• Advise patients to report severe gastric
distress.
• Inform patients to increase fluid intake
to avoid constipation.
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Statins: Uses
• Reduce LDL and total triglyceride
production
• Used to treat hyperlipidemia
• Often given with other
antihyperlipidemic drugs
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Statins: Adverse Effects
• Common: abdominal pain, flatulence,
constipation, dyspepsia, headache,
cramping
• Serious: rhabdomyolysis
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Statins: Contraindications
• Contraindicated in myopathy, active
liver disease, unexplained persistent
transaminase elevations, or during
pregnancy and lactation
• Interact with digoxin, norethindrone,
ethinyl estradiol
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Statins: Patient Information
• Instruct patients to follow dosing
instructions of physician.
• Advise patients to report muscle
tenderness or pain, especially if
accompanied by fever or malaise.
• Advise patients to avoid alcohol.
• Warn female patients to avoid if
pregnant or lactating.
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Grapefruit and Statins
• Advise patients to avoid
grapefruit/grapefruit juice when taking
simvastatin.
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Statins in Children
• The safety of statins in children and
adolescents is not established .
• These drugs should not be prescribed
for this age group.
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Nicotinic Acid: Uses
• Appears to reduce levels of VLDL, LDL,
and total cholesterol by decreasing liver
triacylglycerol synthesis
• Used as adjuvant treatment of
hypercholesterolemia in patient who do
not respond to diet or weight loss
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Nicotinic Acid: Adverse Effects
• Common: cutaneous flush and pruritus,
nausea and abdominal pain, syncope,
nervousness, blurred vision
• Serious: hepatotoxicity
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Nicotinic Acid: Contraindications
• Avoid in hepatic impairment, severe
hypotension, active peptic ulcer,
pregnancy, lactation, and in children
younger than 16.
• Use cautiously in patients with history
of gallbladder disease, liver disease,
peptic ulcer, glaucoma, CAD, and
diabetes.
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Nicotinic Acid:
Patient Information
• Warn patients of cutaneous flush that
may occur within 2 hours of oral
ingestion and last for several hours.
• Relief can be obtained by reducing the
dosage and then increasing dose in
small increments over time.
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Fibric Acid Derivatives: Uses
• Block lipolysis of stored triglycerides in
adipose tissues and inhibit liver uptake
of fatty acids
• Used to treat hypertriglyceridemia and
severe familial hypercholesterolemia
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Fibric Acid Derivatives:
Adverse Effects
• Common: GI disturbances, dizziness,
blurred vision
• Serious: cancer (clofibrate)
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Fibric Acid Derivatives:
Contraindications
• Contraindicated in gallbladder disease,
biliary cirrhosis, hepatic or severe renal
dysfunction, and during pregnancy and
lactation
• Safe use in children younger than 18
not established.
• May increase hypoprothrombinemic
effects of anticoagulants
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Fibric Acid Derivatives:
Patient Information
• Instruct patients to report unexplained
bleeding, including:
– Easy bruising
– Epistaxis
– Hematuria
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