Acebutolol

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Acebutolol.jpg

[edit] MECHANISM OF ACTION

Acebutolol is a β1 selective adrenergic antagonist which possesses mild intrinsic sympathomimetic activity (ISA) in its therapeutically effective dose range.

Beta blockers with intrinsic sympathomimetic activity (acebutolol and pindolol) are generally not recommended for patients with angina since they may exacerbate the angina in some patients.

[edit] INDICATIONS

  • Treatment of hypertension
    • Alone as an initial agent in those patients in whom, in the judgment of the physician, treatment should be started with a β-blocker rather than a diuretic.
    • In combination with other drugs, particularly a thiazide diuretic.
    • In combination witha diuretic and a vasodilator in patients with severe hypertension
  • Control of tachyarrhythmias.

[edit] DOSAGE

Hypertension
The initial dosage in uncomplicated mild-to-moderate hypertension is 400 mg. This can be given as a single daily dose, but in occasional patients twice daily dosing may be required for adequate 24-hour blood-pressure control. An optimal response is usually achieved with dosages of 400 to 800 mg per day, although some patients have been maintained on as little as 200 mg per day. Patients with more severe hypertension or who have demonstrated inadequate control may respond to a total of 1200 mg daily (administered b.i.d.), or to the addition of a second antihypertensive agent. Beta-1 selectivity diminishes as dosage is increased.

Arrhythmia
The usual initial dose of Sectral is 400 mg daily given as 200 mg b.i.d. Dosage should be increased gradually until an optimal clinical response is obtained, generally at 600 to 1200 mg per day. If treatment is to be discontinued, the dosage should be reduced gradually over a period of about two weeks.

[edit] CONTRAINDICATIONS

  • Patients who are hypersensitive to Acebutolol, beta-blockers, or to any ingredient in the formulation.
  • Patients exhibiting sinus bradycardia.
  • Patients with sick sinus syndrome.
  • Patients with second and third degree A-V block.
  • Patients with right ventricular failure secondary to pulmonary hypertension.
  • Patients with congestive heart failure.
  • Patients with cardiogenic shock.
  • Patients undergoing anesthesia with agents that produce myocardial depression, e.g. ether.
  • Patients with severe peripheral circulatory disorders.
  • Patients with phaeochromocytoma.

[edit] WARNINGS AND PRECAUTIONS

  • Bradycardia may occur, in such case, dosage should be reduced. Acebutolol anyway is less like to cause bradycardia because of its intrinsic sympathomatic activity (Partial agonist)
  • Cardiac Failure : beta blockade may result in further depression of myocardial contractility and precipitate more severe failure. The positive inotropic action of digitalis may be reduced by the negative inotropic effect of acebutolol when the two drugs are used concomitantly.
  • Cessation of therapy with a beta-blocker should be gradual
  • The low lipid solubility and lack of accumulation in CNS tissues of acebutolol and its active metabolite reduce the likelihood of sleep disturbances (Insomnia), depression or other central effects like vivid dreams, nightmares and hallucinations, if compared with lipophilic beta blocking agents like propranolol, metoprolol and oxprenolol.
  • Diabetes and Hypoglycemia: Beta-blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia.
  • Thyrotoxicosis: Beta Adrenergic blockade may mask certain clinical signs of hyperthyroidism (e.g. tachycardia). Abrupt withdrawal may be followed by an exacerbation of the symptoms of hyperthyroidism, including thyroid storm.
  • Bronchospastic Diseases: In general, patients with bronchospastic diseases should not receive β-blockers. Because of its relative β1 selectivity, however, low doses of Acebutolol may be used with caution in patients with bronchospastic disease who do not respond to, or who cannot tolerate, alternative treatment.

[edit] INTERACTIONS

  • Both digitalis glycosides and beta blockers slow atrioventricular conduction and decrease heart rate. Concomitant use can increase the risk of bradycardia.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category B (US). Acebutolol should be used during pregnancy only if the potential benefit justifies the risk to the fetus.
  • Nursing Mothers: Use in nursing mothers is not recommended.

[edit] SIDE EFFECTS

Common adverse reactions to Acebutolol are: Nausea (2%), Fatigue (4%), Dizziness (2%), Dyspnea (2,5 %), Hypotension (1%), Rashes (1%)

[edit] RELATED LINKS

[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)