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Coreg: Full Drug Profile

Medically reviewed by Min Clinic Staff | Updated: January 2026

Coreg - General Information

Coreg is a non-selective beta blocker indicated in the treatment of mild to moderate congestive heart failure (CHF). It blocks beta-1 and beta-2 adrenergic receptors as well as the alpha-1 adrenergic receptors.

 

Pharmacology of Coreg

Coreg is a nonselective beta-adrenergic blocking agent with alpha1-blocking activity and is indicated for the treatment of hypertension and mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin. Coreg is a racemic mixture in which nonselective b-adrenoreceptor blocking activity is present in the S(-) enantiomer and a-adrenergic blocking activity is present in both R(+) and S(-) enantiomers at equal potency. Coreg has no intrinsic sympathomimetic activity. The effect of carvedilol's b-adrenoreceptor blocking activity has been demonstrated in animal and human studies showing that carvedilol (1) reduces cardiac output in normal subjects; (2) reduces exercise-and/or isoproterenol-induced tachycardia and (3) reduces reflex orthostatic tachycardia.

 

Coreg for patients

Patients taking COREG (Carvedilol) should be advised of the following:

  • they should not interrupt or discontinue using COREG without a physician's advice.
  • congestive heart failure patients should consult their physician if they experience signs or symptoms of worsening heart failure such as weight gain or increasing shortness of breath.
  • they may experience a drop in blood pressure when standing, resulting in dizziness and, rarely, fainting. Patients should sit or lie down when these symptoms of lowered blood pressure occur.
  • if patients experience dizziness or fatigue, they should avoid driving or hazardous tasks.
  • they should consult a physician if they experience dizziness or faintness, in case the dosage should be adjusted.
  • they should take COREG with food.
  • diabetic patients should report any changes in blood sugar levels to their physician.
  • contact lens wearers may experience decreased lacrimation.

 

 

Coreg Interactions

Inhibitors of CYP2D6; poor metabolizers of debrisoquin: Interactions of carvedilol with strong inhibitors of CYP2D6 (such as quinidine, fluoxetine, paroxetine, and propafenone) have not been studied, but these drugs would be expected to increase blood levels of the R(+) enantiomer of carvedilol . Retrospective analysis of side effects in clinical trials showed that poor 2D6 metabolizers had a higher rate of dizziness during up-titration, presumably resulting from vasodilating effects of the higher concentrations of the a-blocking R(+) enantiomer.

Catecholamine-depleting Agents: Patients taking both agents with b-blocking properties and a drug that can deplete catecholamines (e.g., reserpine and monoamine oxidase inhibitors) should be observed closely for signs of hypotension and/or severe bradycardia.

Clonidine: Concomitant administration of clonidine with agents with b-blocking properties may potentiate blood-pressure- and heart-rate-lowering effects. When concomitant treatment with agents with b-blocking properties and clonidine is to be terminated, the b-blocking agent should be discontinued first. Clonidine therapy can then be discontinued several days later by gradually decreasing the dosage.

Cyclosporine: Modest increases in mean trough cyclosporine concentrations were observed following initiation of carvedilol treatment in 21 renal transplant patients suffering from chronic vascular rejection. In about 30% of patients, the dose of cyclosporine had to be reduced in order to maintain cyclosporine concentrations within the therapeutic range, while in the remainder no adjustment was needed. On the average for the group, the dose of cyclosporine was reduced about 20% in these patients. Due to wide interindividual variability in the dose adjustment required, it is recommended that cyclosporine concentrations be monitored closely after initiation of carvedilol therapy and that the dose of cyclosporine be adjusted as appropriate.

Digoxin: Digoxin concentrations are increased by about 15% when digoxin and carvedilol are administered concomitantly. Both digoxin and COREG slow AV conduction. Therefore, increased monitoring of digoxin is recommended when initiating, adjusting, or discontinuing COREG.

Inducers and Inhibitors of Hepatic Metabolism: Rifampin reduced plasma concentrations of carvedilol by about 70%. Cimetidine increased AUC by about 30% but caused no change in Cmax.

Calcium Channel Blockers: Isolated cases of conduction disturbance (rarely with hemodynamic compromise) have been observed when COREG is co-administered with diltiazem. As with other agents with b-blocking properties, if COREG is to be administered orally with calcium channel blockers of the verapamil or diltiazem type, it is recommended that ECG and blood pressure be monitored.

Insulin or Oral Hypoglycemics: Agents with b-blocking properties may enhance the blood-sugar-reducing effect of insulin and oral hypoglycemics. Therefore, in patients taking insulin or oral hypoglycemics, regular monitoring of blood glucose is recommended.

 

Coreg Contraindications

COREG is contraindicated in patients with bronchial asthma (2 cases of death from status asthmaticus have been reported in patients receiving single doses of COREG) or related bronchospastic conditions, second- or third-degree AV block, sick sinus syndrome or severe bradycardia (unless a permanent pacemaker is in place), or in patients with cardiogenic shock or who have decompensated heart failure requiring the use of intravenous inotropic therapy. Such patients should first be weaned from intravenous therapy before initiating COREG.

Use of COREG in patients with clinically manifest hepatic impairment is not recommended.

COREG is contraindicated in patients with hypersensitivity to any component of the product.

 

Additional information about Coreg

Coreg Indication: For the treatment of mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin. Mechanism Of Action: Coreg is a racemic mixture in which nonselective beta-adrenoreceptor blocking activity is present in the S(-) enantiomer and alpha-adrenergic blocking activity is present in both R(+) and S(-) enantiomers at equal potency. Coreg's beta-adrenergic receptor blocking ability decreases the heart rate, myocardial contractility, and myocardial oxygen demand. Coreg also decreases systemic vascular resistance via its alpha adrenergic receptor blocking properties. Coreg and its metabolite BM-910228 (a less potent beta blocker, but more potent antioxidant) have been shown to restore the inotropic responsiveness to Ca2+ in OH- free radical-treated myocardium. Coreg and its metabolites also prevent OH- radical-induced decrease in sarcoplasmic reticulum Ca2+-ATPase activity. Therefore, carvedilol and its metabolites may be beneficial in chronic heart failure by preventing free radical damage. Drug Interactions: Acetohexamide The beta-blocker decreases the symptoms of hypoglycemia Chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia Citalopram The SSRI increases the effect of the beta-blocker Clonidine Increased hypertension when clonidine stopped Cyclosporine Increases the effect and toxicity of cyclosporine Digoxin Increases levels/effect of digoxin Dihydroergotamine Ischemia with risk of gangrene Dihydroergotoxine Ischemia with risk of gangrene Disopyramide The beta-blocker increases toxicity of disopyramide Epinephrine Hypertension, then bradycardia Ergonovine Ischemia with risk of gangrene Ergotamine Ischemia with risk of gangrene Escitalopram The SSRI increases the effect of the beta-blocker Fenoterol Antagonism Fluoxetine The SSRI increases the effect of the beta-blocker Formoterol Antagonism Gliclazide The beta-blocker decreases the symptoms of hypoglycemia Glipizide The beta-blocker decreases the symptoms of hypoglycemia Glisoxepide The beta-blocker decreases the symptoms of hypoglycemia Glibenclamide The beta-blocker decreases the symptoms of hypoglycemia Glycodiazine The beta-blocker decreases the symptoms of hypoglycemia Ibuprofen Risk of inhibition of renal prostaglandins Indomethacin Risk of inhibition of renal prostaglandins Insulin The beta-blocker decreases the symptoms of hypoglycemia Insulin-aspart The beta-blocker decreases the symptoms of hypoglycemia Insulin-detemir The beta-blocker decreases the symptoms of hypoglycemia Insulin-glargine The beta-blocker decreases the symptoms of hypoglycemia Insulin-glulisine The beta-blocker decreases the symptoms of hypoglycemia Insulin-lispro The beta-blocker decreases the symptoms of hypoglycemia Isoproterenol Antagonism Lidocaine The beta-blocker increases the effect and toxicity of lidocaine Methysergide Ischemia with risk of gangrene Orciprenaline Antagonism Paroxetine The SSRI increases the effect of the beta-blocker Pirbuterol Antagonism Piroxicam Risk of inhibition of renal prostaglandins Prazosin Risk of hypotension at the beginning of therapy Procaterol Antagonism Repaglinide The beta-blocker decreases the symptoms of hypoglycemia Salbutamol Antagonism Salmeterol Antagonism Sertraline The SSRI increases the effect of the beta-blocker Terbutaline Antagonism Tolazamide The beta-blocker decreases the symptoms of hypoglycemia Tolbutamide The beta-blocker decreases the symptoms of hypoglycemia Verapamil Increased effect of both drugs Food Interactions: Take with food, food slows the absorption rate and reduces the incidence of adverse effects (extent of absorption is not affected). Generic Name: Carvedilol Synonyms: Carvedilolum [Latin] Drug Category: Vasodilator Agents; Antihypertensive Agents; Adrenergic Agents Drug Type: Small Molecule; Approved Other Brand Names containing Carvedilol: Coreg; Absorption: Carvedilol is rapidly and extensively absorbed following oral administration, with an absolute bioavailability of approximately 25% to 35% due to a significant degree of first-pass metabolism. Toxicity (Overdose): Not expected to be toxic following ingestion. Protein Binding: 98% Biotransformation: Hepatic. Carvedilol is metabolized primarily by aromatic ring oxidation and glucuronidation. The oxidative metabolites are further metabolized by conjugation via glucuronidation and sulfation. Demethylation and hydroxylation at the phenol ring produce three active metabolites with b-receptor blocking activity. The 4'-hydroxyphenyl metabolite is approximately 13 times more potent than carvedilol for b-blockade. Half Life: 7-10 hours Dosage Forms of Coreg: Tablet Oral Chemical IUPAC Name: 1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol Chemical Formula: C24H26N2O4 Carvedilol on Wikipedia: https://en.wikipedia.org/wiki/Carvedilol Organisms Affected: Humans and other mammals