Captopril


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Hypertension Initial: 25-75 mg daily in 2-3 divided doses. Dosage is individualised according to clinical response and may be increased after at least 2 weeks, to 100-150 mg daily in 2-3 divided doses as needed to reach target BP. Patients on diuretics or with cardiac decompensation: Initially, 6.25 mg or 12.5 mg bid. Congestive heart failure Initial: 6.25-12.5 mg bid or tid. Dosage is individualised according to clinical response and may be increased incrementally, with at least 2 weeks intervals. Maintenance: 75-150 mg/day in divided doses. Post myocardial infarction Acute treatment: Initial: 6.25 mg as test dose, followed by 12.5 mg after 2 hours, and 25 mg after 12 hours. If tolerated, 50 mg bid for 4 weeks. Re-evaluate patient state according to clinical response. Chronic treatment: Initial: 6.25 mg within 3-16 days post-infarction, followed by 12.5 mg tid for 2 days, then 25 mg tid depending on patient response. Maintenance: 75-150 mg/day in 2 or 3 divided doses. Diabetic nephropathy 75-100 mg/day in divided doses.
Dosage Details
Oral
Diabetic nephropathy
Adult: 75-100 mg daily in divided doses.
Child: Neonates and infants: 0.15 mg/kg. Children and adolescents: 0.3 mg/kg. All doses are given tid according to response or based on patient response.
Elderly: Initially, 6.25 mg bid.

Oral
Post-myocardial infarction
Adult: Acute treatment (within 24 hours of the onset of symptoms): 6.25 mg as test dose, followed by 12.5 mg after 2 hours and 25 mg after 12 hours. If tolerated, 50 mg bid for 4 weeks. Re-evaluate patient state according to clinical response. Chronic treatment (>24 hours of the onset of symptoms): Initially, 6.25 mg within 3-16 days 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.
Child: Neonates and infants: 0.15 mg/kg. Children and adolescents: 0.3 mg/kg. All doses are given tid according to response or based on patient response.
Elderly: Initially, 6.25 mg bid.

Oral
Hypertension
Adult: Initially, 25-75 mg daily in 2-3 divided doses. Dosage is individualised according to clinical response and may be increased after at least 2 weeks, to 100-150 mg daily in 2-3 divided doses as needed to reach target BP. Patients on diuretics or with cardiac decompensation: Initially, 6.25 mg or 12.5 mg bid.
Child: Neonates and infants: 0.15 mg/kg. Children and adolescents: 0.3 mg/kg. All doses are given tid according to response or based on patient response.
Elderly: Initially, 6.25 mg bid.

Oral
Congestive heart failure
Adult: Initially, 6.25-12.5 mg bid or tid. Dosage is individualised according to clinical response and may be increased incrementally, with at least 2 weeks intervals. Maintenance: 75-150 mg daily in divided doses.
Child: Neonates and infants: 0.15 mg/kg. Children and adolescents: 0.3 mg/kg. All doses are given tid according to response or based on patient response.
Elderly: Initially, 6.25 mg bid.
Renal Impairment
CrCl (mL/min) Dosage
<10 6.25 mg daily. Max 37.5 mg daily.
10-20 12.5 mg daily. Max: 75 mg daily.
21-40 25 mg daily. Max: 100 mg daily.
>40 25-50 mg daily. Max: 150 mg daily.
Administration
Should be taken on an empty stomach. Take 1 hr before or 2 hr after meals.
Contraindications
History of angioedema related to ACE treatment, hereditary or idiopathic angioneurotic oedema. Concomitant use with aliskiren esp in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73m2) and neprilysin inhibitor (e.g. sacubitril). Pregnancy.
Special Precautions
Patient with volume and/or Na depletion, ischaemic cardiovascular or cerebrovascular disease, aortic stenosis, unstented unilateral/bilateral renal artery stenosis, hypertrophic and outflow tract obstruction, collagen vascular disease. Patient undergoing major surgery or during anaesthetics. Desensitisation treatment (e.g. hymenoptera venom). Black race. Renal impairment. Children and elderly. Lactation.
Adverse Reactions
Significant: Hypotension, intestinal or peripheral angioedema, non-productive and persistent cough; cholestatic jaundice, proteinuria, neutropenia, agranulocytosis, thrombocytopenia, renal impairment or failure and hyperkalaemia.
Cardiac disorders: Dyspnoea.
Gastrointestinal disorders: Nausea, vomiting, diarrhea, constipation, dry mouth, epigastric discomfort, abdominal pain, peptic ulcer, dyspepsia.
General disorders and admin site conditions: Asthenia.
Metabolism and nutrition disorders: Anorexia, symptomatic hyponatremia, hypoglycaemia.
Nervous system disorders: Taste impairment, dizziness.
Psychiatric disorders: Sleep disorders, rarely, confusion, depression.
Renal and urinary disorders: Rarely, polyuria, oliguria, pollakiuria.
Reproductive system and breast disorders: Rarely, gynaecomastia.
Skin and subcutaneous tissue disorders: Rash, pruritus with or without rash, alopecia.
Potentially Fatal: Angioedema involving the tongue, glottis or larynx; rarely, fulminant hepatic necrosis.
Patient Counseling Information
May impair ability to drive or operate machinery.
MonitoringParameters
Monitor blood pressure, BUN, serum creatinine, CBC with differentials, and electrolytes. Monitor for signs of angioedema and assess pregnancy status.
Overdosage
Symptoms: Severe hypotension, shock, stupor, bradycardia, electrolyte disturbances, and renal failure. Management: Prevent absorption of recent ingestion by employing gastric lavage, administration of adsorbents and Na sulphate within 30 minutes post intake. For hypotension, place in shock position and rapidly initiate salt and volume supplementations. Administer atropine and consider the use of pacemaker for pacemaker and bradycardia.
Drug Interactions
Increases lithium concentration and toxicity. Increased risk of leucopenia with procainamide and immunosuppresants. Decreased renal clearance with probenecid. Enhances hypotensive effect of TCA and antipsychotics. Decreased antihypertensive effects with sympathomimetic agents. Increased hypotensive effect with adrenergic blocking agents and NSAIDs (e.g. indomethacin, ibuprofen). Potentiates blood glucose-lowering effects of insulin and oral antidiabetics (e.g. sulphonylureas). May result in volume depletion and risk of hypotension with thiazide or loop diuretics (except furosemide and hydrochlorothiazide). May increase serum K with K-sparing diuretics (e.g. amiloride, spironolactone, triamterene), K-containing salt substitutes or supplements. Increased risk of low renal function due to serum K increase with NSAIDs. Increased risk of angioedema with neprilysin inhibitor and mammalian target of rapamycin inhibitor (e.g. temsirolimus, everolimus).
Potentially Fatal: Increased risk of hypotension, hyperkalaemia and impaired renal function with aliskiren. Increased risk of angioedema with neprilysin inhibitors (e.g. sacubitril). May cause anaphylactoid reactions with dextran sulfate in LDL apheresis.
Food Interaction
Decreased serum concentration with food.
Lab Interference
May cause false-positive urine test for acetone determination using nitroprusside reagent. May result to false-negative aldosterone/renin ratio (ARR).
Action
Description: Captopril is a sulfhydryl-containing ACE inhibitor which competitively inhibits ACE to prevent 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 (approx. 60-75%). Decreased serum concentration with food. Bioavailability: Approx 60-75%. Time to peak plasma concentration: Within 1-2 hours.
Distribution: Crosses placenta and enters breast milk (small amounts). Volume of distribution at steady state: 0.7 L/kg. Plasma protein binding: 25%-30%.
Excretion: Via urine (>95%; 40-50% as unchanged drug). Elimination half-life: 2-3 hours.
Chemical Structure

Click on icon to see table/diagram/image
Storage
Store between 20-25°C. Protect from moisture.
ATC Classification
C09AA01 - captopril ; Belongs to the class of ACE inhibitors. Used in the treatment of cardiovascular disease.
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 © 2020 MIMS. All rights reserved. Powered by MIMS.com
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