Carvedilol

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Carvedilol.jpg

[edit] MECHANISM OF ACTION

Carvedilol is a non-selective beta-adrenoceptor blocker, it blocks both β1 and β2 adrenergic receptors, reducing ability of the sympathetic nervous system to increase the myocardial contractile force and rate.

Carvedilol is also a potent α1-adrenergic receptors blocker, it inhibits the binding of norepinephrine to the α1 receptors causing relaxation in peripheral vascular resistance which results in a decrease in blood pressure.

[edit] INDICATIONS

  • Treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.
  • Mild to severe chronic heart failure
  • Left ventricular dysfunction following myocardial infarction in clinically stable patients

[edit] DOSAGE

Take with food. Individualize dosage and monitor during up-titration.

Normal tablets:

  • 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


Extended-release Capsules (Coreg CR)

  • Heart failure: Start at 10 mg once daily and increase to 20, 40, and then 80 mg once 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 20 mg once daily and increase to 40 mg then 80 mg once daily after intervals of 3 to 10 days. A lower starting dose or slower titration may be used.
  • Hypertension: Start at 20 mg once daily and increase if needed for blood pressure control to 40 mg then 80 mg once daily over intervals of 1 to 2 weeks.

[edit] CONTRAINDICATIONS

  • Bronchial asthma or related bronchospastic conditions
  • Second- or third-degree AV block
  • Sick sinus syndrome
  • Severe bradycardia
  • Patients in cardiogenic shock or decompensated heart failure requiring the use of IV inotropic therapy.
  • Severe hepatic impairment
  • History of serious hypersensitivity reaction (e.g., Stevens-Johnson syndrome, anaphylactic reaction, angioedema) to any component of this medication or other medications containing carvedilol

[edit] WARNINGS AND PRECAUTIONS

  • Acute exacerbation of coronary artery disease upon cessation of therapy: Do not abruptly discontinue.
  • Bradycardia, hypotension, worsening heart failure/fluid retention may occur. Reduce the dose as needed.
  • Non-allergic bronchospasm (e.g., chronic bronchitis and emphysema): Avoid β-blockers. However, if deemed necessary, use with caution and at lowest effective dose.
  • Diabetes: Monitor glucose as β-blockers may mask symptoms of hypoglycemia or worsen hyperglycemia

[edit] INTERACTIONS

  • CYP2D6 enzyme inhibitors may increase and rifampin may decrease carvedilol levels.
  • Hypotensive agents (e.g., reserpine, MAO inhibitors, clonidine) may increase the risk of hypotension and/or severe bradycardia.
  • Cyclosporine or digoxin levels may increase.
  • Both digitalis glycosides and β-blockers slow atrioventricular conduction and decrease heart rate. Concomitant use can increase the risk of bradycardia.
  • Amiodarone may increase carvedilol levels resulting in further slowing of the heart rate or cardiac conduction.
  • Verapamil or diltiazem-type calcium channel blockers may affect ECG and/or blood pressure.
  • Insulin and oral hypoglycemics action may be enhanced.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Carvedilol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Nursing Mothers: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from β-blockers, especially bradycardia, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. The effects of other α- and β-blocking agents have included perinatal and neonatal distress.

[edit] SIDE EFFECTS

Most common adverse events

  • Heart failure and left ventricular dysfunction following myocardial infarction (≥10%): Dizziness, fatigue, hypotension, diarrhea, hyperglycemia, asthenia, bradycardia, weight increase
  • Hypertension (≥5%): Dizziness

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

http://us.gsk.com/products/assets/us_coreg.pdf

[edit] REFERENCES

Antihypertensives
ACE inhibitors Benazepril (Lotensin)   Captopril (Capoten)   Cilazapril   Delapril   Enalapril (Renitec, Vasotec)   Fosinopril (Monopril)  Lisinopril (Prinivil, Zestril)   Moexipril (Univasc)  Perindopril (Aceon)  Quinapril (Accupril)  Ramipril (Altace, Triatec)   Trandolapril (Mavik)  Zofenopril (Bifril, Zopranol)
Angiotensin II receptor antagonist Azilsartan (Edarbi)   Candesartan (Atacand)   Eprosartan (Teveten)   Irbesartan (Aprovel, Avapro, Karvea)   Losartan (Cozaar)   Olmesartan (Benicar, Olmetec)   Telmisartan (Micadis)   Valsartan (Diovan, Tareg)
Renin inhibitors Aliskiren (Rasilez, Tekturna)
Alpha-1 blockers Doxazosin (Cardura)   Prazosin (Minipress)   Terazosin (Hytrin)
Alpha-2 agonists (centrally acting) Clonidine (Oral route)   Clonidine (Transdermal) (Catapresan)   Guanfacine (Tenex)   Methyldopa (Aldomet)
Calcium channel blockers Dihydropyridines‎ Amlodipine (Norvasc)   Barnidipine (Vasexten)   Felodipine (Plendil)   Isradipine (Dynacirc)   Lacidipine (Lacipil, Motens)   Lercanidipine (Zanidip)   Manidipine   Nicardipine   Nifedipine (Adalat)   Nisoldipine   Nitrendipine
Benzothiazepine‎ Diltiazem (Cardizem, Taztia XT, Tiazac, Tildiem)
Phenylalkylamine‎ Gallopamil   Verapamil (Calan)
Beta blockers Beta1 selective (cardioselective) Acebutolol (Sectral)   Atenolol (Tenormin)   Betaxolol (Kerlon)   Bisoprolol (Concor)   Celiprolol (Cordiax)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Nebivolol (Bystolic, Lobivon, Nebilox)
Nonselective (Beta1 and Beta2 blockers) Oxprenolol (Trasitensin)   Propranolol (Inderal)   Timolol (Blocadren)
Nonselective (Beta1, Beta2 and Alpha1 blockers) Carvedilol (Dilatrend)   Labetalol (Trandate)
Beta blocker with intrinsic sympathomimetic activity (ISA) Acebutolol (Sectral)   Celiprolol (Cordiax)
Lipophilic Beta blockers Propranolol (Inderal)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Oxprenolol (Trasitensin)
Diuretics Carbonic anhydrase inhibitors Acetazolamide (Diamox)
Loop diuretics Bumetanide   Etacrynic acid   Furosemide (Lasix)   Piretanide   Torasemide (Demadex)
Thiazide diuretics Chlorothiazide (Diuril)   Hydrochlorothiazide (Esidrex)
Thiazide-like diuretics Chlortalidone (Hygroton)   Indapamide (Lozol, Lozide)   Metolazone
Potassium-sparing diuretics Epithelial sodium channel blockers: Amiloride (Midamor)   Triamterene (Dyrenium)
Aldosterone receptor antagonists: Potassium canrenoate   Eplerenone (Inspra)   Spironolactone (Aldactone)
Osmotic diuretics Mannitol
Combination therapy Amiloride/Hydrochlorothiazide (Moduretic)   Spironolactone/Hydrochlorothiazide (Aldactazide)