Captopril

Pharmacological Properties
 Introduction

RAS/RAAS  Renin-Angiotensin-Aldosterone System

Renin secreted when:

decrease of arterial blood pressure,
decrease of Na+ in macula densa,
and increase of sympathetic nervous activity
Captopril
Captopril is a sulfhydryl containing dipeptide, a
potent, competitive inhibitor of angiotensin-
converting enzyme (ACE), the enzyme responsible
for the conversion of angiotensin I (ATI) to
angiotensin II (ATII).

• Pharmacologic classification: ACE inhibitor

• Therapeutic classification: antihypertensive,
adjunctive treatment of heart failure
• Pregnancy risk category C (D second and third
trimesters)

Captopril is available under the following different

brand names: Capoten and Captoril.
Captopril
Indication
• Hear failure with
preserved ejection
fraction
• Patient with all stages of
left ventricle failure
• Hypertension
• Myocardial infarction
• Patient with diabetes or
chronic renal disease
Contraindication
• Hypersensitivity to ACE
Inhibitor
• Pregnancy
• Angioneurotic edema
after other ACE
inhibitors
• Bilateral renal artery
stenosis
Pharmacokinetics
• Absorption: 60% to 75% of an oral dose is absorbed through
the GI tract; food may reduce absorption by up to 40%,
antihypertensive effect begins in 15 minutes
• Distribution: bound mostly with albumin about 25-30%
• Metabolism: about 50% is metabolized in the liver
• Excretion: primarily in urine
Pharmacodynamics
Antihypertensive action: Captopril inhibits ACE, preventing
conversion of angiotensin I to angiotensin II, a potent
vasoconstrictor. Reduced formation of angiotensin II decreases
peripheral arterial resistance, which results in decreased
aldosterone secretion, thus reducing sodium and water
retention and lowering blood pressure.

Cardiac load-reducing action: Captopril decreases systemic

vascular resistance (afterload) and pulmonary capillary wedge
pressure (preload), thus increasing cardiac output in patients
with heart failure.
Mechanism of Action
Side Effect
• dry cough (should go away after you stop taking captopril)
• dizziness
• skin rash
• a change in the way that foods taste
Dosage Consideration
• Beneficial for many patients at risk for heart disease; reduces
risk of myocardial infaction, stroke, diabetic nephropathy,
micoalbuminuria, new onset of DM
• Consider starting an ACE inhibitor in high-risk patients, even if
no hypertension or congestive heart failure
• May prolong survival in congestive heart failure, may preserve
renal function in diabetes mellitus
• Good choice in hyperlipidemia patients
• Requires weeks for full effect; to start, use low dose
• Take on an empty stomach.
Dosage
• Suggested initial dose  50-75 mg/d
• Maintenance dose range  75-150mg/d
• Decrease dose required in moderate renal insufficiency

Heart Failure
Adults: 25 mg P.O. t.i.d.
If patient takes a diuretic or is hyponatremic or hypovolemic,
give an initial dosage of 6.25 to 12.5 mg t.i.d.
Maintenance dosage is 50 to 100 mg t.i.d.

For elderly patients and those with renal failure, use lower initial daily doses
and smaller increments for adjustment. Adjust at 1- to 2-week intervals.
Take as directed
• If you don’t take it at all: Your high blood pressure and heart
problems will get worse. This will increase your risk of a heart
attack or stroke.
• If you stop taking it suddenly: Stopping the drug suddenly
can cause your blood pressure to get higher. This may increase
your risk of a heart attack or stroke.
• If you don’t take it on schedule: Your blood pressure and
other heart problems may not improve and may get worse.
• What to do if you miss a dose: Take it as soon as you
remember. If it’s just a few hours until the time for your next
dose, then wait and only take one dose at that time.
Never try to catch up by taking two doses at once. This could
cause serious side effects.
• If you take too much: significant drop in blood pressure.
Self management and
monitoring
• Patient may need to check BP at home. Bring the BP diary
when check up.

Clinical monitoring
• blood pressure
• liver function
• kidney function
• blood potassium