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Captopril
Overview
Captopril is a sulfhydryl containing ACE
inhibitor. Captopril is used to treat
hypertension (high blood pressure),
congestive heart failure and kidney
diseases in diabetic patients.

Categories
12 Cardiovascular drugs
12.3 Anti-hypertensives
12.3.3 ACE inhibitors

12 Cardiovascular drugs
12.4 Drugs used in heart failure

Page headings
Overview

Primary Characterstics

Indications

Pharmacokinetics

Contraindications

Drug Interactions

Side Effects

Dosage

High Risk Groups

Warning / Precautions

Storage Conditions

Interference in Pathology

Brands of Captopril

Manufacturers of
Captopril

Primary Characterstics
It is of Synthetic
origin and
belongs to
Mercapto L-
Proline. It belongs
to Angiotensin
converting enzyme inhibitor-ACEI
pharmacological group on the basis of
mechanism of action and also classified in
Antihypertensive Agents pharmacological
group.The Molecular Weight of Captopril is
217.30.

Its pKa is 3.7, 9.8.

Indications
Captopril is primarily indicated in
conditions like Congestive heart failure,
Congestive heart failure (adjunct), Diabetic
nephropathy, Diabetic retinopathy,
Essential hypertension, Essential
hypertension (mild to moderate), severe
hypertension resistant to other treatment,
Gastric acid reduction during anaesthesia,
Hypertension, Iron deficiency anaemia,
Prophylaxis of acid aspiration, Renal
hypertension, Scleroderma renal crisis.

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Pharmacokinetics
Oral absorption of Captopril is found to be
72% ±4. Volume of distribution is found to
be 0.7 l/kg and plasma protien binding is
30%. Presystemic metabolism is noted to
be 8.5% ±5.5 and metabolism is reported
rapid & extensive via liver. Renal Excretion
accounts for 85% and plasma half life is 1-2
hr.
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Contraindications
Captopril is contraindicated in conditions
like Renal diseases, Collagen vascular
disease, Renal artery stenosis.

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Drug Interactions
Captopril is known to interact with other
drugs, the details of drug interactions is as
follows:

Severity N/A
Procainamide (HCl) Azathioprine

Probenecid Clonidine (HCl)

Alprostadil Baclofen

Porcine Insulin Alcohol

Human Insulin Cyclophosphamide

Bovine Insulin Diazoxide

Digoxin Potassium
Glycerophosphate

Aldesleukin Technetium
Succimer Tc-99m

Major
Allopurinol Cyclosporin A

Moderate
Indomethacin Spironolactone

Lithium Metolazone

Moderate (Sequence
important)
Frusemide or Furosemide

These interactions are sometimes

beneficial and sometimes may pose
threats to life. Always consult your
physician for the change of dose
regimen or an alternative drug of
choice that may strictly be required.

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Side Effects
The severe or irreversible adverse effects of
Captopril, which give rise to further
complications include Renal damage,
Proteinuria.

Captopril produces potentially life-

threatening effects which include
Hyperkalemia, Neutropenia. which are
responsible for the discontinuation of
Captopril therapy.

The signs and symptoms that are

produced after the acute overdosage of
Captopril include Angioedema, Laryngeal
obstruction, Respiratory distress,
Hypotension.

The symptomatic adverse reactions

produced by Captopril are more or less
tolerable and if they become severe, they
can be treated symptomatically, these
include Skin rash, Taste disturbance,
Cough.

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Dosage
Captopril's dosage details are as follows:
Dose Single Frequency Route Instructions
Dose

Adult Dosage
12.5 to 31 12 hourly PO
50 mg (31.25)

Paedriatic Dosage (20kg)

0.5 to 1.2 8 hourly Oral Gradually increase the
2 (1.25) Dose
mg/kg

Neonatal Dosage (3kg)

0.5 to 1.2 8 hourly Oral Gradually increase the
2 (1.25) Dose
mg/kg

High Risk Groups

Drug should not be given to Pregnant

Mothers, and Neonates.

If prescribing authority justifies the

benefits of the drug against the possible
damages he/she should reevaluate them
and consult the reference material and
previous studies.

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Warning / Precautions

White blood cells (W.B.Cs) counts and

urinary protein estimation should be
done before and during treatment
Captopril therapy can cause
neutropenia or agranulocytosis.
Patients with renal disease, patients
with immunosuppression or receiving
immunosuppressives, and patients
with collagen vascular disease or
autoimmune disease are at a greater
risk for developing these complications.
It should be used with caution in
patients with pre-existing bone marrow
depression. The dose should be
adjusted in patients with renal
impairment. It should be used
cautiously in patients with congestive
heart failure. Initial doses should be
lower than in the treatment of
hypertension becauseof a greater risk
of developing hypotension. It should
not be administered to patients with
pre-existing renal artery stenosis. Renal
function should be monitored closely
during the first 2 weeks after initiating
therapy. It should be discontinued if
renal function worsens acutely. Other
types of renal disease can actually
improve during captopril therapy. The
dose should be adjusted inpatients
with renal impairment. It should be
used with caution patients with
hyperkalemia. It is classified as
pregnancy category C and should be
used with caution during pregnancy
only if clearly needed.

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Storage Conditions
Tab
Store in a well closed container, at room
temperature, Below 30°C. Protect from
Sunlight and Moisture.

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Interference in Pathology

False +ve test for Urinary Nitrites and

Acetone

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Brands / Trade Names of

Captopril
Click on the desired strength of the dosage
form to view its available brands.

Single Ingredient
Tabs: 25 mg, 50 mg, 12.5 mg,

Multi ingredient
Tabs: 25 mg, 50 mg,

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Manufacturers of Captopril in
Pakistan
Akhai
Alfalah Pharma
Atco
Benson
Bex
Biolabs
Bryon
Davis
Drugs
Efroze
Evron
Fynk
GSK
Helicon
Innvotek
Macquins
Makson
Mediceena
Medimpex
Novartis
Pearl
Pharmacare
Pharmix
Siza
Spencer
Valor
Werrick
Zafa
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