Adult: As immediate-release tab: Initially, 12.5 mg bid for 2 days, then increase to 25 mg bid. May be increased further at intervals of at least 2 weeks, if necessary. Max: 100 mg daily in divided doses. Treatment recommendations may vary between countries and individual products (refer to specific product guidelines). Elderly: As immediate-release tab: Max: 25 mg bid. Dosage recommendations may vary between countries and individual products (refer to specific product guidelines).
Oral Left ventricular dysfunction post myocardial infarction
Adult: As immediate-release tab: Initially, 6.25 mg bid. If tolerated, may increase dose after 3-10 days to 12.5 mg bid, then to a target dose of 25 mg bid. A lower initial dose of 3.125 mg bid may be given in symptomatic patients and rate of dose increment may be slowed down if clinically indicated. As extended-release tab: Initially, 20 mg once daily. If tolerated, may increase dose after 3-10 days to 40 mg once daily, then to a target dose of 80 mg once daily. Treatment recommendations may vary between countries and individual products (refer to specific product guidelines).
Oral Hypertension
Adult: As monotherapy or in combination with other antihypertensive agents: As immediate-release tab: Initially, 12.5 mg once daily for 2 days, then increase to 25 mg once daily. May be increased further at intervals of at least 2 weeks, if necessary. Max: 50 mg once daily or in divided doses. As extended-release cap: Initially, 20 mg once daily for 1-2 weeks, then increase to 40 mg once daily if needed. Dose may be further increased at intervals of at least 1-2 weeks. Max: 80 mg once daily. Elderly: As monotherapy or in combination with other antihypertensive agents: As immediate-release tab: 12.5 mg once daily. As extended-release cap: A lower starting dose is recommended and titrate according to response. Dosage recommendations may vary between countries and individual products (refer to specific product guidelines).
Oral Chronic heart failure
Adult: As adjunct to standard therapies (e.g. diuretics, digoxin, ACE inhibitors): As immediate-release tab: Initially, 3.125 mg bid for 2 weeks. If tolerated, gradually increase dose at intervals of at least 2 weeks to 6.25 mg bid, followed by 12.5 mg bid, then 25 mg bid. Max: <85 kg: 25 mg bid. >85 kg: 50 mg bid. As extended-release tab: Initially, 10 mg once daily for 2 weeks. If tolerated, gradually increase dose at intervals of at least 2 weeks to 20 mg, followed by 40 mg, then 80 mg once daily. Treatment recommendations may vary between countries and individual products (refer to specific product guidelines).
What are the brands available for Carvedilol in Thailand?
Carvedilol is a racemic mixture of R- and S-enantiomers. Clinical pharmacokinetic studies have shown that CYP2D6 plays a major role in R- and S-carvedilol metabolism. Carvedilol is affected by genetic polymorphism, with poor metabolisers of debrisoquin (a CYP2D6 marker) having 2- to 3-fold higher plasma concentrations of R(+)-carvedilol compared to extensive metabolisers. In contrast, serum levels of S(-)-carvedilol increase by approx 20-25% in poor metabolisers, indicating that this enantiomer is metabolised to a lesser extent by CYP2D6 than R(+)-carvedilol. Although population pharmacokinetic studies confirmed the importance of the CYP2D6 genotype in the pharmacokinetics of R- and S-carvedilol, other studies did not support this finding. Consequently, it was concluded that CYP2D6 genetic polymorphism may have limited clinical significance.
CYP2D6 poor metabolisers
Patients carrying *3/*4 or *4/*4 genotypes had a 3.3-fold higher steady-state concentrations of R(+)-carvedilol and 2.4-fold higher concentrations of S(-)-carvedilol compared to normal metabolisers and intermediate metabolisers carrying CYP2D6*1/*1, *1/*3, *1/*4 genotypes. The US Food and Drug Administration (US FDA) drug labelling states that the retrospective analysis of adverse effects in clinical trials indicated that CYP2D6 poor metabolisers experienced a higher incidence of dizziness during up-titration, likely due to the vasodilating effects of higher concentrations of the α-blocking R(+)-enantiomer.
Hepatic Impairment
Severe: Contraindicated.
Administration
Carvedilol Should be taken with food. ER cap: Swallow whole & do not crush/chew. May open cap & administer dispersed pellets.
Contraindications
Decompensated heart failure requiring IV inotropic treatment, 2nd- or 3rd-degree AV block (unless a permanent pacemaker is in place), sick sinus syndrome including sinoatrial block, severe bradycardia (<50 bpm), severe hypotension (systolic blood pressure <85 mmHg), severe peripheral arterial circulatory disturbances, cardiogenic shock, metabolic acidosis, history of bronchial asthma or related bronchospastic conditions, history of obstructive airways disease. Severe hepatic impairment.
Special Precautions
Patient with suspected vasospastic angina (Prinzmetal's angina), bronchospastic disease, COPD, diabetes mellitus, heart failure with reduced ejection fraction, myasthenia gravis, peripheral vascular disease, untreated or suspected phaeochromocytoma, thyroid disease, history of serious hypersensitivity reactions, history of psoriasis. Patients undergoing surgery; desensitisation treatment. CYP2D6 poor metabolisers. Avoid abrupt withdrawal. Renal and mild to moderate hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Bradyarrhythmia (e.g. 1st- or 2nd-degree AV block, complete AV block), bronchospasm, CNS effects (e.g. fatigue, sleep disorder, insomnia), hypoglycaemia, floppy iris syndrome (particularly in cataract surgery patients who were on or previously treated with α1-blockers), symptomatic hypotension with or without syncope, arterial insufficiency (in patients with peripheral vascular disease), induction or exacerbation of psoriasis; worsening heart failure or fluid retention (especially during up-titration); exacerbation of hyperthyroidism symptoms or precipitation of thyroid storm, MI, ventricular arrhythmias, severe exacerbation of angina (following abrupt withdrawal); withdrawal symptoms. Rarely, reversible renal function deterioration (in patients with CHF). Blood and lymphatic system disorders: Anaemia. Eye disorders: Visual abnormalities, visual impairment, dry eye, eye irritation. Gastrointestinal disorders: Diarrhoea, dyspepsia, nausea, vomiting, abdominal pain. General disorders and administration site conditions: Asthenia, oedema (including generalized, peripheral oedema), hypervolaemia, fluid overload, pain. Investigations: Increased weight, impaired blood glucose control. Metabolism and nutrition disorders: Hypercholesterolaemia, hyperglycaemia. Musculoskeletal and connective tissue disorders: Pain in extremities. Nervous system disorders: Dizziness, headache. Psychiatric disorders: Depression. Renal and urinary disorders: UTI, urinary disorder. Respiratory, thoracic and mediastinal disorders: Bronchitis, pneumonia, URTI, pulmonary oedema, dyspnoea, asthma. Vascular disorders: Hypotension, orthostatic hypotension.
This drug may cause transient dizziness or tiredness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor ECG, heart rate, blood pressure, kidney function, LFTs; blood glucose (in patients with diabetes). Assess for signs and symptoms of bronchospasm in patients with existing bronchospastic disease.
Overdosage
Symptoms: Severe hypotension, bradycardia, heart failure, cardiogenic shock, cardiac arrest, dizziness, respiratory problems, bronchospasm, vomiting, disturbed consciousness, generalised seizures. Management: Symptomatic and supportive treatment. Atropine may be given for excessive bradycardia. Consider giving sympathomimetics (e.g. dobutamine, isoprenaline) or IV glucagon to support ventricular function. If a positive inotropic effect is needed, phosphodiesterase inhibitors must be considered. Administer norepinephrine with continuous monitoring of the circulation if peripheral vasodilation is the dominant feature of intoxication. Initiate pacemaker therapy in cases of drug-resistant bradycardia. Bronchospasm may be treated by β2-sympathomimetics (aerosol or IV) or IV aminophylline administered via slow IV inj or infusion. Slow IV inj of diazepam or clonazepam may be given for seizures. In cases of severe overdose accompanied by symptoms of shock, supportive treatment must be continued for an adequate duration until the patient's condition has stabilised.
Drug Interactions
May increase the bioavailability of drugs transported by P-glycoprotein. May increase serum concentrations of digoxin and ciclosporin. Reduced serum concentrations with rifampicin. Enhanced bradycardic effect and increased serum concentration with amiodarone. May result in stereoselective inhibition of metabolism with fluoxetine. Increased risk of AV conduction disturbances with phenylalkylamine, class I anti-arrhythmic agents, verapamil, diltiazem, or other antiarrhythmics. May increase the blood sugar-reducing effect of insulin and oral hypoglycaemics. May result in additive AV conduction time prolongation with digoxin. Enhanced blood pressure- and heart rate-lowering effects with clonidine. May enhance the effects of other antihypertensive agents (e.g. α1-receptor antagonists) and other medicines with antihypertensive adverse effects (e.g. barbiturates, phenothiazines, TCAs, vasodilating agents). May cause synergistic, negative inotropic and hypotensive effects with anaesthetics.
Action
Description: Mechanism of Action: Carvedilol is a non-cardioselective β-blocker. It inhibits the renin-angiotensin-aldosterone system by blocking β-receptors, thereby decreasing renin release and minimising fluid retention. It also reduces peripheral vascular resistance via selective blockade of α1-adrenoceptors. Onset: Antihypertensive: Within 30 minutes (α-blockade); within 1 hour (β-blockade). Pharmacokinetics: Absorption: Rapidly and extensively absorbed from the gastrointestinal tract. High-fat meal increases exposure and concentration. Bioavailability: Approx 25-35% (immediate-release). Time to peak plasma concentration: 1-2 hours. Distribution: Distributed into extravascular tissues. Plasma protein binding: >98%, mainly to albumin. Volume of distribution: 115 L. Metabolism: Extensively metabolised in the liver mainly via aromatic ring oxidation and glucuronidation by CYP2D6 and CYP2C9 isoenzymes; oxidative metabolites are further metabolised by conjugation via glucuronidation and sulfation; undergoes first-pass effect. Excretion: Mainly via faeces; urine (<2% as unchanged drug). Elimination half-life: Approx 6-10 hours.
Chemical Structure
Carvedilol Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2585, Carvedilol. https://pubchem.ncbi.nlm.nih.gov/compound/Carvedilol. Accessed Aug. 27, 2025.
Storage
Immediate-release tab: Store below 30°C. Extended-release tab: Store between 15-30°C. Protect from light.
C07AG02 - carvedilol ; Belongs to the class of alpha and beta blocking agents. Used in the treatment of cardiovascular diseases.
References
Annotation of FDA Label for Carvedilol and CYP2D6. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org. Accessed 06/03/2025.Annotation of Swissmedic Label for Carvedilol and CYP2D6. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org. Accessed 06/03/2025.Brayfield A, Cadart C (eds). Carvedilol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/03/2025.Carvedilol 6.25 mg Tablets (Cadila Pharmaceuticals [UK] Limited). MHRA. https://products.mhra.gov.uk. Accessed 06/03/2025.Carvedilol. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 06/03/2025.Carvedilol. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 06/03/2025.Carvedilol. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 06/03/2025.Coreg CR Capsule, Extended Release (Waylis Therapeutics LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 06/03/2025.Coreg Tablet, Film Coated (Waylis Therapeutics LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 06/03/2025.CYP2D6 - Carvedilol. UpToDate Lexidrug, Pharmacogenomics Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 06/03/2025.Joint Formulary Committee. Carvedilol. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/03/2025.Sandoz New Zealand Limited. Carvedilol Sandoz, Tablets, Uncoated, 6.25 mg, 12.5 mg, and 25 mg data sheet 20 March 2023. Medsafe. http://www.medsafe.govt.nz. Accessed 06/03/2025.Vacodil 25 mg Tablet (Unimed Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 06/03/2025.
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