Carvedilol

What is Carvedilol?

• Carvedilol (Coreg; Coreg CR) is an alpha/beta-adrenergic blocking agent used to treat high blood pressure, congestive heart failure (CHF), and left ventricular dysfunction.

Carvedilol

Carvedilol-I-3D-balls

Carvedilol Enantiomers Structural Formulae

What are the uses of this medicine?

Carvedilol (Coreg; Coreg CR) tablets are used, often with other medicines, for the following conditions:

• to treat patients with certain types of heart failure
• to treat patients who had a heart attack that worsened how well the heart pumps
• to treat patients with high blood pressure (hypertension)

How does this medicine work?

• Carvedilol (kar' ve dil" ol) is a unique beta-blocker and antihypertensive agent that has both alpha- and beta-adrenergic receptor blocking activity.
• The beta-blockade is nonselective, acting on both beta-1 and beta-2 adrenergic receptors.
• Beta-1 adrenergic blockade reduces the heart rate and myocardial contractility by slowing the AV conduction and suppressing automaticity.
• Beta-2 blockade affects peripheral vascular resistance and can cause bronchospasm and hypoglycemia.
• The alpha-adrenergic blockade acts on alpha-1 receptors which results in relaxation of arterial smooth muscle and vasodilation.

Who Should Not Use this medicine ?

This medicine cannot be used in:

• have severe heart failure and are hospitalized in the intensive care unit or require certain intravenous medications that help support circulation (inotropic medications).
• are prone to asthma or other breathing problems.
• have a slow heartbeat or a heart that skips a beat (irregular heartbeat).
• have liver problems.
• are allergic to any of the ingredients in carvedilol tablets.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Especially tell your doctor if you take:

• cimetidine
• clonidine (Catapres, Kapvay, in Clorpres), cyclosporine (Gengraf, Neoral, Sandimmune)
• digoxin ( Lanoxin)
• diltiazem (Cardizem, Cartia, Dilacor, Taztia, Tiazac)
• epinephrine (Epipen)
• fluoxetine (Prozac, Sarafem, Selfemra, in Symbyax)
• insulin
• oral medications for diabetes
• monoamine oxidase inhibitors (MAOIs) such as isocarboxazid (Marplan), phenelzine (Nardil), tranylcypromine (Parnate), and selegiline (Eldepryl, Emsam, Zelapar); paroxetine (Brisdelle, Paxil)
• propafenone (Rythmol)
• quinidine
• reserpine
• rifampin (Rifadin, Rimactane, in Rifater, in Rifamate)
• verapamil (Calan, Covera-HS, Verelan, in Tarka)

Is this medicine FDA approved?

• Carvedilol was approved for use in the United States in 1995 and is still in wide use with more than 2.5 million prescriptions filled yearly.
• Current indications include hypertension and heart failure.
• Carvedilol is also approved for use after myocardial infarction to reduce cardiovascular mortality. Carvedilol is also used off label to treat migraine and vascular headaches.

How should this medicine be used?

Recommended dosage: Heart failure:

• Start at 3.125 mg twice daily and increase to 6.25, 12.5, and then 25 mg twice daily over intervals of at least 2 weeks.
• Maintain lower doses if higher doses are not tolerated.

Left ventricular dysfunction following myocardial infarction:

• Start at 6.25 mg twice daily and increase to 12.5 mg then 25 mg twice daily after intervals of 3 to 10 days.
• A lower starting dose or slower titration may be used.

Hypertension:

• Start at 6.25 mg twice daily and increase if needed for blood pressure control to 12.5 mg then 25 mg twice daily over intervals of 1 to 2 weeks.

• Carvedilol tablets should not be given to patients with severe hepatic impairment.

Administration:

• Carvedilol comes as a tablet and an extended-release capsule to take by mouth.
• The tablet is usually taken twice a day with food.
• The extended-release capsule is usually taken once a day in the morning with food.
• Tell your doctor if you gain weight or have trouble breathing while taking carvedilol tablets.
• Take carvedilol tablets with food.
• If you miss a dose of carvedilol tablets, take your dose as soon as you remember, unless it is time to take your next dose.
• Take your next dose at the usual time.
• Do not take 2 doses at the same time.
• Swallow the extended-release capsules whole.
• Do not chew or crush the capsules, and do not divide the beads inside a capsule into more than one dose.
• If you are unable to swallow the capsules, you may carefully open a capsule and sprinkle all of the beads it contains over a spoonful of cool or room temperature applesauce. Swallow the entire mixture immediately without chewing.
• Your doctor will probably start you on a low dose of carvedilol and gradually increase your dose to allow your body to adjust to the medication.
• Talk to your doctor about how you feel and about any symptoms you experience during this time.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As a tablet and an extended-release capsule

This medicine is available in fallowing brand namesː

• Coreg; Coreg CR

What side effects can this medication cause?

The most common side effects of this medicine include: In Heart failure and left ventricular dysfunction following myocardial infarction:

• Dizziness, fatigue, hypotension, diarrhea, hyperglycemia, asthenia, bradycardia, weight increase

In Hypertension:

• Dizziness

Carvedilol may cause serious side effects which may include:

• Low blood pressure
• Tiredness
• Slow heartbeat
• Changes in your blood sugar
• Carvedilol may hide some of the symptoms of low blood sugar, especially a fast heartbeat.
• Carvedilol may mask the symptoms of hyperthyroidism (overactive thyroid).
• Worsening of severe allergic reactions

What special precautions should I follow?

• Patients should not interrupt or discontinue using carvedilol tablets without a physician's advice. Severe exacerbation of angina and the occurrence of myocardial infarction and ventricular arrhythmias have been reported in patients with angina following the abrupt discontinuation of therapy with β-blockers.
• Carvedilol tablets can cause you to feel dizzy, tired, or faint. Do not drive a car, use machinery, or do anything that needs you to be alert if you have these symptoms.
• Bradycardia, hypotension, worsening heart failure/fluid retention may occur. Reduce the dose as needed.
• Patients with heart failure should consult their physician if they experience signs or symptoms of worsening heart failure such as weight gain or increasing shortness of breath.
• Patients 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.
• Patients with bronchospastic disease (e.g., chronic bronchitis, emphysema) should, in general, not receive β-blockers. Carvedilol may be used with caution, however, in patients who do not respond to, or cannot tolerate, other antihypertensive agents.
• Patients should consult a physician if they experience dizziness or faintness, in case the dosage should be adjusted.
• In patients with heart failure and diabetes, carvedilol therapy may lead to worsening hyperglycemia, which responds to intensification of hypoglycemic therapy. It is recommended that blood glucose be monitored when carvedilol dosing is initiated, adjusted, or discontinued. Diabetic patients should report any changes in blood sugar levels to their physician.
• In general, β-blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia.
• Contact lens wearers may experience decreased lacrimation.
• β-blockers can precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease. Caution should be exercised in such individuals.
• Carvedilol has been linked to at least one instance of clinically apparent liver injury.
• Chronically administered β-blocking therapy should not be routinely withdrawn prior to major surgery.
• β-adrenergic blockade may mask clinical signs of hyperthyroidism, such as tachycardia. Abrupt withdrawal of β-blockade may be followed by an exacerbation of the symptoms of hyperthyroidism or may precipitate thyroid storm.
• Caution should be taken in the administration of carvedilol to patients suspected of having pheochromocytoma.
• Agents with non-selective β-blocking activity may provoke chest pain in patients with Prinzmetal's variant angina. Caution should be taken in the administration of carvedilol to patients suspected of having Prinzmetal's variant angina.
• Intraoperative Floppy Iris Syndrome (IFIS) has been observed during cataract surgery in some patients treated with alpha-1 blockers (carvedilol is an alpha/beta blocker).
• It is not known if carvedilol passes into your breast milk. Talk with your doctor about the best way to feed your baby if you are taking carvedilol tablets.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• severe hypotension
• bradycardia
• cardiac insufficiency
• cardiogenic shock
• cardiac arrest
• Respiratory problems
• bronchospasms
• vomiting
• lapses of consciousness
• generalized seizures

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• The patient should be placed in a supine position and, where necessary, kept under observation and treated under intensive-care conditions.

The following agents may be administered:

• For excessive bradycardia: Atropine, 2 mg IV.
• To support cardiovascular function: Glucagon, 5 to 10 mg IV rapidly over 30 seconds, followed by a continuous infusion of 5 mg per hour; sympathomimetics (dobutamine, isoprenaline, adrenaline) at doses according to body weight and effect.
• If peripheral vasodilation dominates, it may be necessary to administer adrenaline or noradrenaline with continuous monitoring of circulatory conditions.
• For therapy-resistant bradycardia, pacemaker therapy should be performed.
• For bronchospasm, β-sympathomimetics (as aerosol or IV) or aminophylline IV should be given.
• In the event of seizures, slow IV injection of diazepam or clonazepam is recommended.

Can this medicine be used in pregnancy?

• It is not known if carvedilol is safe for your unborn baby.
• You and your doctor should talk about the best way to control your high blood pressure during pregnancy.
• Available data regarding use of carvedilol in pregnant women are insufficient to determine whether there are drug-associated risks of adverse developmental outcomes.
• The use of beta blockers during the third trimester of pregnancy may increase the risk of hypotension, bradycardia, hypoglycemia, and respiratory depression in the neonate.

Can this medicine be used in children?

• Effectiveness of carvedilol in patients younger than 18 years has not been established.

What are the active and inactive ingredients in this medicine?

• Active Ingredient: carvedilol, USP
• Inactive Ingredients: colloidal silicon dioxide, crospovidone, hypromellose, lactose monohydrate, magnesium stearate, polyethylene glycol, polysorbate, povidone, and titanium dioxide.

Who manufactures and distributes this medicine?

Manufactured For:

• Teva Pharmaceuticals USA, Inc.
• North Wales, PA

What should I know about storage and disposal of this medication?

• Store carvedilol tablets at 68° to 77°F (20° to 25°C). Keep the tablets dry.
• Safely, throw away carvedilol tablets that are out of date or no longer needed.
• Keep carvedilol tablets and all medicines out of the reach of children.

Carvedilol Resources
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• FDA Carvedilol

Carvedilol Resources
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Antihypertensive agents