Pronunciation: ass-cee-BYOO-toe-lahl HIGH-droe-KLOR-ide
Class: Beta-adrenergic blocking agent
- Capsules 200 mg
- Capsules 400 mg
Gen-Acebutolol (Type S) (Canada)
Blocks beta-receptors, primarily affecting heart (slows rate), vascular musculature (decreases BP), and lungs (reduces function).
Well absorbed. T max is 2.5 h (acebutolol) and 3.5 h (diacetolol). Bioavailability is about 40%. Food may decrease the rate of absorption and C max slightly.
About 26% protein bound. Hydrophilic (minimally excreted into CSF). Crosses placenta and is excreted in breast milk.
Extensive first-pass hepatic biotransformation. Major metabolite is diacetolol (active; equipotent to acebutolol).
T ½ is about 3 to 4 h (acebutolol) and 8 to 13 h (diacetolol). About 30% to 40% eliminated by kidneys, 50% to 60% eliminated by nonrenal mechanisms (ie, bile, feces). Dialyzable.
3 to 8 h.
Special PopulationsRenal Function Impairment
Decreased elimination of diacetolol resulting in a 2- to 3-fold increase in its t ½ . Administer with caution.Elderly
Bioavailability increased about 2-fold.
Indications and Usage
Management of hypertension and premature ventricular contractions.
Hypersensitivity to beta-blockers; persistently severe bradycardia; greater than first-degree heart block; CHF, unless secondary to tachyarrhythmia treatable with beta-blockers; overt cardiac failure; sinus bradycardia; cardiogenic shock.
Dosage and AdministrationHypertension
PO 400 mg daily initially in single or divided doses; usual response range is 200 to 1,200 mg/day.Elderly
May require lower maintenance doses. Do not exceed 800 mg daily.Ventricular Arrhythmia
PO 400 mg (200 mg twice daily); may be titrated up to 1,200 mg daily.
Store at room temperature.
May enhance or reverse acebutolol's antihypertensive effect; potentially life-threatening situations may occur, especially on withdrawal.NSAIDs
Some agents may impair antihypertensive effect.Prazosin
May cause increase in orthostatic hypotension.Verapamil
Effects of both drugs may be increased.
Laboratory Test Interactions
Antinuclear antibodies may develop; usually reversible on discontinuation. Acebutolol may interfere with glucose or insulin tolerance tests. May cause changes in serum lipids.
Hypotension; bradycardia; CHF; cold extremities; heart block.
Insomnia; fatigue; dizziness; depression; lethargy; drowsiness; forgetfulness.
Rash; hives; fever; alopecia.
Dry eyes; blurred vision; tinnitus; slurred speech; sore throat.
Nausea; vomiting; diarrhea; dry mouth.
Impotence; painful, difficult or frequent urination.
Agranulocytosis; thrombocytopenia purpura.
Bronchospasm; dyspnea; wheezing.
Weight changes; facial swelling; muscle weakness.
Category B .
Excreted in breast milk.
Safety and efficacy not established.
Reduction in daily dose is advised.
Reduction in daily dose is advised.
Abrupt withdrawal is associated with adverse reactions; gradually decrease dose over 1 to 2 wk.
Serious reactions may occur; aggressive therapy may be required.
Administer cautiously in patients taking digitalis and diuretics for CHF.
Acebutolol may mask signs of hypoglycemia (eg, tachycardia, BP changes). May potentiate insulin-induced hypoglycemia.
Nonallergic bronchospasm (eg, chronic bronchitis, emphysema)
In general, do not give beta blockers to patients with bronchospastic disease.
Peripheral vascular disease
Acebutolol may precipitate or aggravate symptoms of arterial insufficiency.
Acebutolol may mask clinical signs of developing or continuing hyperthyroidism (eg, tachycardia). Abrupt withdrawal may exacerbate symptoms of hyperthyroidism, including thyroid storm.
- Teach patient to take pulse every day and record. If less than 60 bpm, tell not to take medication and to notify health care provider.
- Instruct diabetic patients to monitor blood sugar level every 6 h. Drug may mask symptoms of hypoglycemia.
- Caution patient not to stop taking drug suddenly because doing so may exacerbate angina and increase possibility of MI.
- Explain that drug may cause dizziness. Advise patient to avoid sudden position changes to prevent orthostatic hypotension.
- Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.
Copyright © 2009 Wolters Kluwer Health.