Drug Reference

carvedilol

Beta-adrenergic blockers· Brands: Coreg, Dilatrend, Eucardic, CarvilPO

Mechanism of action
Carvedilol is a non-selective beta-adrenergic blocker with additional alpha-1 adrenergic blocking activity. By blocking beta-1 and beta-2 receptors, it reduces heart rate, myocardial contractility, and renin release from the kidneys. Alpha-1 blockade causes vasodilation of peripheral blood vessels, reducing systemic vascular resistance and blood pressure. This dual action reduces cardiac workload and oxygen demand, and is beneficial in heart failure by improving ventricular function.
Pharmacokinetics
Carvedilol is well absorbed after oral administration but undergoes extensive first-pass metabolism, resulting in a bioavailability of approximately 25% to 35%. It is highly lipophilic and extensively metabolised in the liver, primarily by CYP2D6 and CYP2C9. The elimination half-life is 6 to 10 hours. The drug is mainly excreted in the faeces via bile, with a minor renal component. Plasma concentrations are not reliably related to dose, making clinical response monitoring important.
Indications & dosing

Chronic heart failure (NYHA class II-IV)

Start low and titrate slowly; take with food; monitor blood pressure and heart rate.

  • adult · PO: 3.125–25 mg twice daily · Start low and titrate slowly; take with food; monitor blood pressure and heart rate.

Hypertension

May be used alone or in combination with other antihypertensive agents.

  • adult · PO: 6.25–25 mg twice daily · May be used alone or in combination with other antihypertensive agents.

Angina pectoris

For chronic stable angina; reduce angina attacks.

  • adult · PO: 12.5–25 mg twice daily · For chronic stable angina; reduce angina attacks.

Left ventricular dysfunction after myocardial infarction

Initiate after MI; titrate as tolerated to reduce mortality.

  • adult · PO: 12.5–25 mg twice daily · Initiate after MI; titrate as tolerated to reduce mortality.
Contraindications & precautions
  • Severe bradycardia · Heart rate <55 bpm; risk of AV block.
  • Second or third degree atrioventricular block · Unless a pacemaker is present.
  • Cardiogenic shock · Further reduces cardiac output.
  • Decompensated heart failure · May worsen symptoms; initiate only in stable heart failure.
  • Severe asthma or bronchospastic disease · Beta-blockade can precipitate bronchospasm.
  • Sick sinus syndrome · Risk of severe bradycardia.
  • Severe hepatic impairment · Reduced metabolism; contraindicated.
  • Do not discontinue carvedilol abruptly; taper over 1-2 weeks to avoid rebound hypertension or angina.
  • Monitor blood pressure, heart rate, and signs of heart failure during dose titration.
  • Use with caution in patients with diabetes mellitus; beta-blockers may mask hypoglycaemia symptoms.
  • Use with caution in patients with peripheral vascular disease; beta-blockade may worsen symptoms.
  • Avoid use in patients with asthma or chronic obstructive pulmonary disease unless no alternative is available.
  • Concomitant use with calcium channel blockers (e.g., verapamil, diltiazem) may increase risk of bradycardia and heart block.
Adverse effects
  • Dizziness
  • Hypotensionserious
  • Bradycardiaserious
  • Fatigue
  • Nausea
  • Diarrhoea
  • Bronchospasmserious
  • Worsening heart failureserious
  • Headache
  • Oedema
Interactions
  • salbutamolmajorAvoid concomitant use of carvedilol with salbutamol in patients with a history of asthma or bronchospastic disease. If beta-blocker therapy is necessary, consider a cardioselective beta-blocker (e.g., bisoprolol, metoprolol) which has lower affinity for beta-2 receptors. Use salbutamol only when needed and monitor respiratory status closely; consider alternative bronchodilators or adjust dose if signs of worsening airway function occur. In patients with heart failure, the benefits of carvedilol may outweigh the risks, but caution and monitoring are essential.
  • verapamilmajorAvoid coadministration, particularly in patients with heart failure or conduction abnormalities. If necessary, use cautiously with baseline ECG and monitoring of heart rate, blood pressure, and signs of heart failure. Reduce doses as needed.
  • amiodaronemajorMonitor heart rate, blood pressure, and ECG at baseline and regularly during co-therapy. Use low initial doses of carvedilol and titrate cautiously. Consider alternative agents if severe bradycardia or heart block occurs. If co-prescription is necessary, ensure close follow-up.
  • diltiazemmajorUse with caution. Assess baseline heart rate, blood pressure, ECG and left ventricular function. Consider initiating at lower doses and titrating slowly. Monitor heart rate, blood pressure and for symptoms of heart failure or syncope, particularly during the first few days after starting or changing doses. If resting heart rate falls below 50 bpm or symptomatic bradycardia occurs, reduce the dose or discontinue one of the agents.
  • digoxinmoderateMonitor serum digoxin concentrations and electrocardiogram (heart rate and PR interval) after initiation or dose changes of carvedilol. Adjust the digoxin dose as needed. Advise patients to report symptoms of toxicity or bradycardia.
  • warfarinminorMonitor INR closely when initiating, discontinuing, or changing the dose of carvedilol in patients taking warfarin. Perform a repeat INR within 3–5 days of any change and adjust the warfarin dose accordingly. Advise patients to report signs of bleeding.
Renal & hepatic adjustment
  • eGFR 0+: No dose adjustment required in renal impairment; use caution in severe renal impairment.
  • Hepatic impairment (mild): Use caution; consider dose reduction and titrate slowly.
  • Hepatic impairment (moderate): Use caution; consider dose reduction and titrate slowly.
  • Hepatic impairment (severe): Avoid use due to increased plasma levels and risk of adverse effects. (avoid)
Monitoring, pregnancy & toxicity
  • Heart rate and blood pressure · Baseline and during dose titration
  • Signs of worsening heart failure such as weight gain, dyspnoea · Regularly during treatment
  • Blood glucose in diabetic patients · Periodic
  • Liver function tests · If hepatic impairment present
  • Pregnancy: Carvedilol is not recommended in pregnancy unless the potential benefit outweighs the risk. Beta-blockers may cause fetal bradycardia, hypoglycaemia, and growth restriction. Monitor the neonate for bradycardia and hypoglycaemia if used.
  • Toxicity: Bradycardia and hypotension · Supportive care; atropine for bradycardia, IV fluids, and glucagon for severe cardiac depression.
  • Toxicity: Bronchospasm · Administer inhaled beta-2 agonist such as salbutamol; monitor respiratory function.
  • Toxicity: Heart failure exacerbation · Supportive; consider inotropic support and glucagon.
  • Toxicity: Hypoglycaemia · Monitor blood glucose; correct with IV glucose.
Antidotes & reversal
  • Glucagon · Additional alpha-blockade may cause refractory shock - consider vasopressors early as well as glucagon.
Clinical notes
Carvedilol is used for hypertension, stable chronic heart failure, and to reduce mortality after myocardial infarction. It is also used in angina. In heart failure, initiation should be at a low dose and titrated gradually under close supervision to avoid worsening symptoms. It may cause dizziness, fatigue, bradycardia, and hypotension. It can mask symptoms of hypoglycaemia and is contraindicated in severe asthma, high-grade heart block, and decompensated heart failure. Abrupt withdrawal should be avoided.

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BNF; local formulary