Captopril


Generic Medicine Info
Indications and Dosage
Oral
Post-myocardial infarction
Adult: Short-term treatment (within 24 hours of the onset of symptoms): In clinically stable patients: 6.25 mg as a test dose, followed by 12.5 mg after 2 hours, and 25 mg after 12 hours. From the following day, increase to 100 mg daily in 2 divided doses for 4 weeks, if tolerated. Chronic treatment (>24 hours after the onset of symptoms): To improve survival in clinically stable patients with left ventricular dysfunction manifested as an ejection fraction of ≤40%: Initially, 6.25 mg to be started between days 3-16 post-infarction, followed by 12.5 mg tid for 2 days, then 25 mg tid depending on patient response. Maintenance: 75-150 mg daily in 2 or 3 divided doses.
Elderly: Initially, 6.25 mg bid. Titrate according to blood pressure response and maintain the lowest possible dose to achieve adequate control.
Child: Initially, 0.3 mg/kg. Patients requiring special precautions (e.g. premature infants, newborns and infants, or children with renal dysfunction): Initially, 0.15 mg/kg. Doses are given in 3 divided doses daily. Treatment recommendations may vary among countries and individual products (refer to specific product guidelines).

Oral
Hypertension
Adult: As monotherapy or in combination with other antihypertensive agents (e.g. thiazide diuretics): Initially, 25-50 mg daily in 2 divided doses; may increase gradually at intervals of at least 2 weeks to 100-150 mg daily in 2 divided doses as needed to reach target blood pressure. Once daily dosing may be appropriate if taken with other antihypertensive agents. Patients with strongly active renin-angiotensin-aldosterone system (e.g. hypovolaemia, renovascular hypertension, cardiac decompensation): Initially, 6.25 mg or 12.5 mg as a single dose; may increase gradually to 50 mg daily, or 100 mg daily if necessary, in 1 or 2 divided doses. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).
Elderly: Initially, 6.25 mg bid. Titrate according to blood pressure response and maintain the lowest possible dose to achieve adequate control.
Child: Initially, 0.3 mg/kg. Patients requiring special precautions (e.g. premature infants, newborns and infants, or children with renal dysfunction): Initially, 0.15 mg/kg. Doses are given in 3 divided doses daily. Treatment recommendations may vary among countries and individual products (refer to specific product guidelines).

Oral
Diabetic nephropathy in type 1 diabetes mellitus
Adult: 75-100 mg daily in divided doses.
Elderly: Initially, 6.25 mg bid. Titrate according to blood pressure response and maintain the lowest possible dose to achieve adequate control.
Child: Initially, 0.3 mg/kg. Patients requiring special precautions (e.g. premature infants, newborns and infants, or children with renal dysfunction): Initially, 0.15 mg/kg. Doses are given in 3 divided doses daily. Treatment recommendations may vary among countries and individual products (refer to specific product guidelines).

Oral
Heart failure
Adult: In combination with diuretics (or with digitalis and β-blockers, when appropriate): Initially, 6.25-12.5 mg bid or tid; may increase gradually according to patient’s response, clinical status, and tolerability at intervals of at least 2 weeks. Maintenance: 75-150 mg daily in divided doses.
Elderly: Initially, 6.25 mg bid. Titrate according to blood pressure response and maintain the lowest possible dose to achieve adequate control.
Child: Initially, 0.3 mg/kg. Patients requiring special precautions (e.g. premature infants, newborns and infants, or children with renal dysfunction): Initially, 0.15 mg/kg. Doses are given in 3 divided doses daily. Treatment recommendations may vary among countries and individual products (refer to specific product guidelines).
Renal Impairment
CrCl (mL/min) Dosage
<10 Initially, 6.25 mg daily. Max 37.5 mg daily.
10-20 Initially, 12.5 mg daily. Max: 75 mg daily.
21-40 Initially, 25 mg daily. Max: 100 mg daily.
>40 Initially, 25-50 mg daily. Max: 150 mg daily.

Administration
Should be taken on an empty stomach.
Contraindications
History of angioedema associated with previous ACE inhibitor therapy; hereditary or idiopathic angioneurotic oedema. Pregnancy (2nd and 3rd trimester). Concomitant use with aliskiren-containing products in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73 m2). Concomitant use or within 36 hours of switching to or from a neprilysin inhibitor (e.g. sacubitril) or sacubitril/valsartan therapy.
Special Precautions
Patient with volume and/or Na depletion, bilateral renal artery stenosis or stenosis of the artery to a single functioning kidney, diabetes mellitus, hypoaldosteronism, collagen vascular disease, left ventricular valvular and outflow tract obstruction. Patients undergoing desensitisation treatment with hymenoptera venom, haemodialysis with high-flux dialysis membranes, LDL apheresis with dextran sulfate, or major surgery. Black patients. Renal or hepatic impairment. Children and elderly. Pregnancy (1st trimester) and lactation.
Adverse Reactions
Significant: Renal insufficiency, hyperkalaemia, persistent non-productive cough; neutropenia or agranulocytosis, thrombocytopenia, anaemia; proteinuria (particularly in renally impaired patients or in high doses); angioedema of the face, mucous membranes, lips and extremities. Rarely, hypotension, intestinal angioedema.
Cardiac disorders: Chest pain, palpitations, tachycardia.
Gastrointestinal disorders: Nausea, vomiting, epigastric discomfort, peptic ulcer, dyspepsia, reversible taste impairment, gastric irritations, abdominal pain, diarrhoea, constipation, dry mouth, pancreatitis.
Investigations: Transient elevations of BUN or serum creatinine, elevated liver transaminases, alkaline phosphatase, and serum bilirubin.
Metabolism and nutrition disorders: Anorexia.
Musculoskeletal and connective tissue disorders: Arthralgia.
Nervous system disorders: Dizziness; seizure (in infants).
Psychiatric disorders: Insomnia.
Renal and urinary disorders: Oliguria.
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Rash, pruritus, pemphigoid-like lesion, photosensitivity, alopecia.
Vascular disorders: Flushing, pallor.
Potentially Fatal: Angioedema involving the tongue, glottis or larynx. Rarely, cholestatic jaundice (may progress to fulminant hepatic necrosis).
Monitoring Parameters
Monitor blood pressure; serum creatinine, BUN; electrolytes (especially in patients taking K-sparring diuretics, K supplements or salts); CBC for the 1st 3 months and periodically thereafter (in patients with renal impairment or collagen vascular disease). Assess the risk of airway obstruction if angioedema is suspected. Determine cardiac function by radionuclide ventriculography or echocardiography before starting therapy for CHF.
Overdosage
Symptoms: Severe hypotension, bradycardia, stupor, shock, electrolyte disturbance, renal failure. Management: Symptomatic treatment. Prevent absorption by gastric lavage or administration of adsorbents and Na sulfate within 30 minutes after ingestion. If hypotension occurs, place the patient in the shock position and rapidly initiate salt and volume supplementations. Administer atropine if bradycardia or extensive vagal reactions occur. The use of a pacemaker may be considered.
Drug Interactions
Increased risk of angioedema with mTOR inhibitors (e.g. sirolimus, everolimus, temsirolimus) and vildagliptin. Increased risk of hyperkalaemia with K-sparing diuretics (e.g. spironolactone, triamterene, amiloride), K supplements or K-containing salt substitutes or other drugs associated with increases in serum K (e.g. heparin, sulfamethoxazole/trimethoprim). Prior treatment with high-dose thiazide or loop diuretics may result in volume depletion and a risk of hypotension when initiating therapy with captopril. May increase serum lithium levels and symptoms of lithium toxicity. Increased hypotensive effects with other antihypertensive agents (e.g. α- or β-blockers, long-acting Ca channel blockers). May enhance the hypotensive effects of certain TCAs and antipsychotics. Increased risk of leucopenia with allopurinol, procainamide, cytostatic or immunosuppressive agents. Decreased renal clearance with probenecid. Coadministration with NSAIDs (e.g. ibuprofen, indometacin), including selective COX-2 inhibitors may result in deterioration of renal function. Sympathomimetics may reduce the antihypertensive effects of captopril. May potentiate the blood glucose-reducing effects of insulin and oral antidiabetics (e.g. sulfonylureas). Nitritoid reactions (e.g. facial flushing, nausea, vomiting, hypotension) may occur when used concomitantly with injectable gold (Na aurothiomalate). Increased risk of hypotension with anaesthetic agents.
Potentially Fatal: Increased risks of hypotension, hyperkalemia, and changes in renal function (including acute renal failure) with aliskiren. Increased risk of angioedema with a neprilysin inhibitor (e.g. sacubitril).
Food Interaction
Reduced absorption with food.
Lab Interference
May cause a false-positive urine test for acetone. May lead to false-negative aldosterone/renin ratio.
Action
Description:
Mechanism of Action: Captopril is a sulfhydryl-containing ACE inhibitor which competitively inhibits ACE to prevent the conversion of angiotensin I to angiotensin II, thereby increasing plasma renin activity and reducing aldosterone secretion.
Onset: Within 15 minutes.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Reduced absorption with food. Bioavailability: Approx 60-75%. Time to peak plasma concentration: 60-90 minutes.
Distribution: Crosses placenta and enters breast milk (small amounts). Plasma protein binding: Approx 25-30%.
Excretion: Via urine (>95%; 40-50% as unchanged drug and the remainder as inactive disulfide metabolites). Elimination half-life: Approx 2 hours.
Chemical Structure

Chemical Structure Image
Captopril

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 44093, Captopril. https://pubchem.ncbi.nlm.nih.gov/compound/Captopril. Accessed Sept. 28, 2022.

Storage
Tab: Store between 20-25°C. Protect from moisture. Oral solution: Storage recommendations may vary among countries or individual products. Refer to specific product guidelines.
MIMS Class
ACE Inhibitors/Direct Renin Inhibitors
ATC Classification
C09AA01 - captopril ; Belongs to the class of ACE inhibitors. Used in the treatment of cardiovascular disease.
References
Anon. Captopril. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 08/09/2022.

Anon. Captopril. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/09/2022.

Buckingham R (ed). Captopril. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/09/2022.

Captopril 5 mg/5 mL Oral Solution (BCM Specials Limited trading as Ten Pharma). MHRA. https://products.mhra.gov.uk. Accessed 08/09/2022.

Captopril 50 mg Tablets (Tillomed Laboratories Limited). MHRA. https://products.mhra.gov.uk. Accessed 08/09/2022.

Captopril Tablet (Ajanta Pharma USA Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 08/09/2022.

Joint Formulary Committee. Captopril. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/09/2022.

Pharmacy Retailing (NZ) Ltd trading as Healthcare Logistics. Capoten Oral Solution 5 mg/mL data sheet 15 January 2021. Medsafe. http://www.medsafe.govt.nz. Accessed 08/09/2022.

Taguar Tablets 12.5 mg/25 mg (Aurobindo Pharma Ltd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 20/09/2022.

Disclaimer: This information is independently developed by MIMS based on Captopril from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
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