Captopril

What is Captopril?

• Captopril (Capoten) is a specific competitive inhibitor of angiotensin I-converting enzyme (ACE), the enzyme responsible for the conversion of angiotensin I to angiotensin II.

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Captopril structure

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Captopril ball-and-stick model

Captopril structural formulae v.1

What are the uses of this medicine?

Captopril (Capoten) is used:

• to treat high blood pressure and heart failure.
• used to improve survival and reduce the risk of heart failure after a heart attack in patients a heart condition called left ventricular hypertrophy (enlargement of the walls of the left side of the heart).
• to treat kidney disease (nephropathy) caused by diabetes in patients with type 1 diabetes and retinopathy (eye disease).

• Captopril is effective alone and in combination with other antihypertensive agents, especially thiazide-type diuretics.

• High blood pressure is a common condition, and when not treated it can cause damage to the brain, heart, blood vessels, kidneys, and other parts of the body. Damage to these organs may cause heart disease, a heart attack, heart failure, stroke, kidney failure, loss of vision, and other problems. In addition to taking medication, making lifestyle changes will also help to control your blood pressure.

How does this medicine work?

• Captopril (kap' toe pril) was the first ACE inhibitor to be approved for use in the United States and is still widely used for therapy of hypertension and heart failure.
• Like other ACE inhibitors, captopril inhibits the conversion of angiotensin I, a relatively inactive molecule, to angiotensin II which is the major mediator of vasoconstriction and volume expansion induced by the renin-angiotensin system.
• Other enzymes besides that which converts angiotensin I to II may also be inhibited, which may account for some of the side effects of the ACE inhibitors.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are hypersensitive to this product or any other angiotensin-converting enzyme inhibitor.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Especially tell your doctor if you take:

• aspirin and other nonsteroidal anti-inflammatory medications (NSAIDs) such as indomethacin (Indocin, Tivorbex); diuretics ('water pills')
• lithium (Lithobid)
• nitrates such as isosorbide dinitrate (Isordil, in Bidil), isosorbide mononitrate (Monoket), and nitroglycerin (Nitro-Dur, Nitrostat, others)
• other medications for high blood pressure
• potassium supplements
• Tell your doctor and pharmacist if you are taking valsartan and sacubitril (Entresto) or if you have stopped taking it within the last 36 hours.

Is this medicine FDA approved?

• Captopril was approved for use in the United States in 1981 and current indications are for hypertension, congestive heart failure, left ventricular dysfunction after myocardial infarction, and treatment and prevention of diabetic nephropathy.

How should this medicine be used?

Recommended dosage: For Hypertension:

• The initial dose of captopril tablets USP is 25 mg bid or tid.
• If satisfactory reduction of blood pressure has not been achieved after one or two weeks, the dose may be increased to 50 mg bid or tid.
• If further blood pressure reduction is required, the dose of captopril may be increased to 100 mg bid or tid and then, if necessary, to 150 mg bid or tid (while continuing the diuretic).
• The usual dose range is 25 to 150 mg bid or tid. A maximum daily dose of 450 mg captopril should not be exceeded.

For Heart Failure:

• For most patients the usual initial daily dosage is 25 mg tid.
• After a dose of 50 mg tid is reached, further increases in dosage should be delayed, where possible, for at least two weeks to determine if a satisfactory response occurs.
• A maximum daily dose of 450 mg of captopril should not be exceeded.

For Left Ventricular Dysfunction After Myocardial Infarction:

• The recommended dose for long-term use in patients following a myocardial infarction is a target maintenance dose of 50 mg tid.
• Therapy may be initiated as early as three days following a myocardial infarction.
• After a single dose of 6.25 mg, captopril tablets therapy should be initiated at 12.5 mg tid.
• Captopril tablets should then be increased to 25 mg tid during the next several days and to a target dose of 50 mg tid over the next several weeks as tolerated.

For Diabetic Nephropathy:

• The recommended dose of Captopril tablets for long term use to treat diabetic nephropathy is 25 mg tid.

Administration:

• Captopril comes as a tablet to take by mouth. It is usually taken two or three times a day on an empty stomach, 1 hour before a meal.
• To help you remember to take captopril, take it around the same time(s) every day.
• Captopril controls high blood pressure and heart failure but does not cure them.
• Continue to take captopril even if you feel well.
• Do not stop taking captopril without talking to your doctor.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Captopril Tablets
• 12.5 mg tablets
• 25 mg tablets
• 50 mg tablets
• 100 mg tablets

This medicine is available in fallowing brand namesː

• Capoten

What side effects can this medication cause?

The most common side effects of this medicine include:

• dizziness, fatigue, headache, cough, gastrointestinal upset and skin rash

Less common side effects may include:

• Body as a whole : Anaphylactoid reactions
• General : Asthenia, gynecomastia.
• Cardiovascular : Cardiac arrest, cerebrovascular accident / insufficiency, rhythm disturbances, orthostatic hypotension, syncope.
• Dermatologic : Bullous pemphigus, erythema multiforme (including Stevens-Johnson syndrome), exfoliative dermatitis.
• Gastrointestinal : Pancreatitis, glossitis, dyspepsia.
• Hematologic : Anemia, including aplastic and hemolytic.
• Hepatobiliary : Jaundice, hepatitis, including rare cases of necrosis, cholestasis.
• Metabolic : Symptomatic hyponatremia.
• Musculoskeletal : Myalgia, myasthenia.
• Nervous/Psychiatric : Ataxia, confusion, depression, nervousness, somnolence.
• Respiratory : Bronchospasm, eosinophilic pneumonitis, rhinitis.
• Special Senses : Blurred vision.
• Urogenital : Impotence.

What special precautions should I follow?

• Patients should be advised to immediately report to their physician any signs or symptoms suggesting angioedema (e.g., swelling of face, eyes, lips, tongue, larynx and extremities; difficulty in swallowing or breathing; hoarseness) and to discontinue therapy.
• Patients should be told to report promptly any indication of infection (e.g., sore throat, fever), which may be a sign on neutropenia, or of progressive edema which might be related to proteinuria and nephrotic syndrome.
• All patients should be cautioned that excessive perspiration and dehydration may lead to an excessive fall in blood pressure because of reduction in fluid volume. Other causes of volume depletion such as vomiting or diarrhea may also lead to a fall in blood pressure; patients should be advised to consult with the physician.
• Patients should be advised not to use potassium-sparing diuretics, potassium supplements or potassium-containing salt substitutes without consulting their physician.
• Patients should be warned against interruption or discontinuation of medication unless instructed by the physician.
• Heart failure patients on captopril therapy should be cautioned against rapid increases in physical activity.
• Patients should be informed that captopril tablets USP should be taken one hour before meals.
• Angioedema involving the extremities, face, lips, mucous membranes, tongue, glottis or larynx has been seen in patients treated with ACE inhibitors, including captopril. Swelling confined to the face, mucous membranes of the mouth, lips and extremities has usually resolved with discontinuation of captopril; some cases required medical therapy.
• Anaphylactoid reactions have been reported in patients dialyzed with high-flux membranes and treated concomitantly with an ACE inhibitor.
• Neutropenia (<1000/mm3) with myeloid hypoplasia has resulted from use of captopril. In general, neutrophils returned to normal in about two weeks after captopril was discontinued, and serious infections were limited to clinically complex patients.
• Total urinary proteins greater than 1 g per day were seen in about 0.7 percent of patients receiving captopril.
• Excessive hypotension was rarely seen in hypertensive patients but is a possible consequence of captopril use in salt/volume depleted persons, patients with heart failure or those patients undergoing renal dialysis.
• Captopril is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• hypotension

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Correction of hypotension would be of primary concern.
• Volume expansion with an intravenous infusion of normal saline is the treatment of choice for restoration of blood pressure.
• While captopril may be removed from the adult circulation by hemodialysis, there is inadequate data concerning the effectiveness of hemodialysis for removing it from the circulation of neonates or children.
• Peritoneal dialysis is not effective for removing captopril; there is no information concerning exchange transfusion for removing captopril from the general circulation.

Can this medicine be used in pregnancy?

• Categories C (first trimester) and D (second and third trimesters).
• ACE inhibitors can cause fetal and neonatal morbidity and death when administered to pregnant women.
• The use of ACE inhibitors during the second and third trimesters of pregnancy has been associated with fetal and neonatal injury, including hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure, and death.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• captopril

Inactive ingredients:

• cellulose, microcrystalline
• starch, corn
• anhydrous lactose
• silicon dioxide
• talc
• palmitic acid

Who manufactures and distributes this medicine?

Manufactured by:

• Wochardt Limited
• Mumbai, India

Package by:

• Legacy Pharmaceutical Packaging
• Earth City, MO

Distributed by:

• Wal-Mart
• Bentonville, AR

What should I know about storage and disposal of this medication?

• Do not store above 30°C (86°F) Keep bottles tightly closed (protect from moisture).

• Dailymed label info on Captopril
• FDA Captopril

Captopril Resources
Latest articles Most recent articles Ongoing trials	Wikipedia

Common ACE inhibitors include the following:

• Benazepril
• Captopril
• Enalapril
• Fosinopril
• Lisinopril
• Moexipril
• Perindopril
• Quinapril
• Ramipril
• Trandolapril