Captopril

Class
Antihypertensives
Subclass
Angiotensin-converting enzyme inhibitors
Substance name
Captopril
Brand names
Capoten®
Common formulations
Tablet
Dosage and administration
Adults patients
Congestive HF
•
Start at: 25 mg PO TID
•
Maintenance: 50-100 mg PO TID
•
Maximum: 450 mg per day
Administered in combination with diuretics. Consider starting at 6.25-12.5 mg TID in patients with possible salt or volume depletion. Taken 1 hour before meals
Alternative
•
Start at: 6.25 mg PO TID
•
Maintenance: 50 mg PO TID
Taken 1 hour before meals
Diabetic nephropathy in patients with diabetic retinopathy • Due to T1DM
•
25 mg PO TID
Taken 1 hour before meals
Hypertension
•
Start at: 25 mg PO BID-TID for 1-2 weeks
•
Maintenance: 25-150 mg PO BID-TID
•
Maximum: 450 mg per day
Taken 1 hour before meals
Alternative
•
Start at: 25 mg PO BID
•
Maintenance: 75-100 mg PO BID
Taken 1 hour before meals
LV dysfunction in patients with myocardial infarction • Ejection fraction ≤ 40%
•
Loading: 6.25 mg PO once
•
Subsequently: 12.5 mg PO TID
•
Maintenance: 25-50 mg PO TID
Taken 1 hour before meals
STEMI • Off-label
•
Start at: 6.25-12.5 mg PO TID within 24 hours after myocardial infarction
•
Maintenance: 25-50 mg PO TID
Taken 1 hour before meals
Other off-label uses
•
Treatment of HF
•
Treatment of hypertension
•
Treatment of NSTEMI
•
Treatment of proteinuria in patients with CKD
•
Treatment of scleroderma renal crisis
Indications for use
Labeled indications
Adults
•
Treatment of congestive HF
•
Treatment of diabetic nephropathy in patients with diabetic retinopathy (due to T1DM)
•
Treatment of hypertension
•
Treatment of LV dysfunction in patients with myocardial infarction (ejection fraction ≤ 40%)
Off-label indications
Adults
•
Treatment of STEMI
•
Treatment of NSTEMI
•
Treatment of proteinuria in patients with CKD
•
Treatment of scleroderma renal crisis
Children
•
Treatment of HF
•
Treatment of hypertension
Safety risks
Boxed warnings
Fetal toxicity
•
Do not use in pregnant patients. Discontinue captopril as soon as possible when pregnancy is detected.
Contraindications
Hypersensitivity to captopril or its components
History of ACEi-induced angioedema, hereditary angioedema, or idiopathic angioedema
Concomitant use of aliskiren in patients with diabetes
Warnings and precautions
ACE inhibitor-induced angioedema
•
Use caution in patients taking mTOR inhibitors.
Anaphylactoid reactions
•
Use caution in patients on hemodialysis with high-flux membranes, desensitizing treatment with hymenoptera venom, or LDL apheresis with dextran sulfate absorption.
Decreased blood neutrophil count, agranulocytosis
•
Use caution in patients with connective tissue disease (such as SLE or systemic sclerosis) or impaired renal function.
Hypotension
•
Use caution in patients with HF or volume or salt depletion, such as receiving diuretics or undergoing dialysis.
Increased serum potassium
•
Use caution in patients with risk factors for hyperkalemia, including renal impairment, diabetes mellitus, or taking medications causing hyperkalemia or potassium supplements.
Increased urine protein, jaundice, ALF
•
Maintain a high level of suspicion, as captopril has been associated with an increased risk for these adverse events. Discontinue in case of jaundice or a marked increase of liver enzymes.
Specific populations
Renal impairment
GFR > 50 mL/min
•
Use acceptable. No dose adjustment required.
GFR 10-50 mL/min
•
Reduce dose by 25%. Titrate to response. Monitor for hyperkalemia.
GFR < 10 mL/min
•
Reduce dose by 50%. Titrate to response. Monitor for hyperkalemia.
Renal replacement therapy
Continuous renal replacement
•
Reduce dose. Titrate to response. Monitor for hyperkalemia.
Intermittent hemodialysis
•
Administer the dose after dialysis session. Titrate to response. Monitor for hyperkalemia.
Peritoneal dialysis
•
Reduce dose. Titrate to response. Monitor for hyperkalemia.
Hepatic impairment
Any severity
•
Use acceptable. No dose adjustment required.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: D
•
Do not use. Evidence of fetal harm in humans. Discontinue captopril when pregnancy is detected.
•
Use of RAAS inhibitors during the second and third trimesters can cause reduced fetal renal function leading to anuria and renal failure, oligohydramnios, fetal lung hypoplasia, and skeletal deformations, including skull hypoplasia, hypotension, and death.
Breastfeeding
Use with caution during breastfeeding.
•
Consider alternative agents that may be safer. Because of the low levels of captopril in breastmilk, amounts ingested by breastfed infants are small and would not be expected to cause any adverse effects.
Unknown drug levels in breastfed infants.
May potentially cause adverse effects in breastfed infants.
Some adverse effects on lactation reported.
Adverse reactions
Common 1-10%
•
Acute liver failure, hepatic necrosis, ↑ urine protein, maculopapular rash, pallor, peptic ulcer disease, abdominal pain, anorexia, change in taste, chest pain, constipation, cough, diarrhea, dizziness, dysgeusia, dyspnea, fatigue, hair loss, headache, insomnia, malaise, nausea, palpitations, paresthesia, pruritus, vomiting, tachycardia
Uncommon < 1%
•
Acute liver failure, contact dermatitis, ↓ blood glucose, ↓ urine output, lichen planus, myocardial infarction, nephrotic syndrome, pericarditis, psoriasis, raynaud's phenomenon, renal failure, angina pectoris, polyuria, skin flushing
Unknown frequency
•
Acute pancreatitis, agranulocytosis, anaphylaxis, anemia, angioedema, ataxia, bronchospasm, cardiac arrest, ↓ blood neutrophil count, ↓ platelet count, ↓ serum sodium, eosinophilic pneumonia, erythema multiforme, exacerbation of arrhythmia, exfoliative dermatitis, extrahepatic cholestasis, glossitis, gynecomastia, hemolytic anemia, hypotension, ↑ WBC count, ↑ blood eosinophil count, ↑ liver enzymes, ↑ serum potassium, jaundice, myasthenia gravis, orthostatic hypotension, photosensitivity of skin, arthralgia, asthenia, blurred vision, confusion, depression, dry mouth, dyspepsia, fever, myalgia, somnolence, syncope, weight loss, rhinitis, Stevens-Johnson syndrome, teratogenesis, vasculitis
Interactions
Drug(s)
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