anti hypertensive drugs_ace inhibitor
TRANSCRIPT
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ACE Inhibitors
PHRM 306: Drugs affecting CVS
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Introduction
The ACE inhibitors are recommended when
the preferred first-line agents (diuretics or -
blockers) are contraindicated or ineffective.
Despite their widespread use, it is not clear if
antihypertensive therapy with ACE inhibitors
increases the risk of other major diseases.
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Classification
Dicarboxylate-
containing ACE
inhibitors
EnalaprilRamipril
Quinapril
Perindopril
LisinoprilBezazepril
Moexipril
Sulfhydryl-
containing ACE
inhibitors
Captopril
Phosphonate-
containing ACE
inhibitors
Fosinolpril
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Actions
The ACE inhibitors lower blood pressure by
reducing peripheral vascular resistance
without reflexively increasing cardiac output,
rate, or contractility.
These drugs block the ACE that cleaves
angiotensin I to form the potent
vasoconstrictor angiotensin II.
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Figure
Effects of angiotensin-converting enzyme (ACE)
inhibitors.
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Actions
The converting enzyme is also responsible for
the breakdown of bradykinin.
ACE inhibitors decrease angiotensin II andincrease bradykinin levels.
Vasodilation occurs as a result of the
combined effects of lower vasoconstriction
caused by diminished levels of angiotensin II
and the potent vasodilating effect of increased
bradykinin.
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Actions
By reducing circulating angiotensin II levels,
ACE inhibitors also decrease the secretion of
aldosterone, resulting in decreased sodium
and water retention.
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Therapeutic uses
Like -blockers, ACE inhibitors are most
effective in hypertensive patients who are
white and young.
However, when used in combination with a
diuretic, the effectiveness of ACE inhibitors is
similar in white and black patients with
hypertension.
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Therapeutic uses
Along with the angiotensin-receptor blockers
(ARBs), ACE inhibitors slow the progression of
diabetic nephropathy and decrease
albuminuria.
ACE inhibitors are also effective in the
management of patients with chronic heart
failure.
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Therapeutic uses
ACE inhibitors are a standard in the care of a
patient following a myocardial infarction.
Therapy is started 24 hours after the end of
the infarction.
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Adverse effects
Common side effects include dry cough, rash,
fever, altered taste, hypotension (in
hypovolemic states), and hyperkalemia.
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Adverse effects
The dry cough, which occurs in about 10
percent of patients, is thought to be due to
increased levels ofbradykinin in the
pulmonary tree. (mainly women)
Angioedema (rash) is a rare but potentially
life-threatening reaction and may also be due
to increased levels of bradykinin.
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Adverse effects
Hyperkalemia: Potassium levels must be
monitored, and potassium supplements (or a
high potassium diets) or potassium-sparing
diuretics are contraindicated.
Because of the risk ofangioedema and first-
dose syncope, ACE inhibitors may be first
administered in the physician's office with
close observation.
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Adverse effects
Reversible renal failure can occur in patients
with severe bilateral renal artery stenosis.
ACE inhibitors are fetotoxic and should not beused by women who are pregnant.