Management of hypertension (alone or in combination with other classes of antihypertensive agents).
One of several preferred initial therapies in hypertensive patients with heart failure, postmyocardial infarction, ischemic heart disease, and/or diabetes mellitus.
Can be used as monotherapy for initial management of uncomplicated hypertension; however, thiazide diuretics are preferred by JNC 7.
Cardiac Arrhythmias
Treatment of frequent ventricular premature complexes (VPCs), including uniform and multiform VPCs and/or coupled VPCs, and R-on-T complexes in patients with primary arrhythmias or arrhythmias secondary to various cardiac disorders (e.g., CAD, MI, valvular disease).
Management of various supraventricular tachyarrhythmias†.
Secondary prevention following AMI† to reduce the risk of reinfarction and mortality.
Dosage and Administration
General
Individualize dosage according to patient response.
β-Adrenergic blocking selectivity diminishes as dosage is increased.
If long-term therapy is discontinued, reduce dosage gradually over a period of about 2 weeks. (See Abrupt Withdrawal of Therapy under Cautions.)
When substituting another β-adrenergic blocking agent for acebutolol, initiate at a comparable dosage without interruption of β-blocker therapy.
Hypertension
Monitor BP carefully during initial titration or subsequent dosage increases. Large or abrupt BP reductions generally should be avoided.
Angina
Adjust dosage of β-adrenergic blocking agents according to clinical response and to maintain a resting heart rate of 55–60 bpm.
Administration
Acebutolol hydrochloride is administered orally. Also been administered IV†, but a parenteral dosage form is currently not commercially available in the US.
Oral Administration
Hypertension
Usually administer as a single daily dose; however, for 24-hour BP control, some patients may require administration of the daily dose in 2 divided doses.
Ventricular Arrhythmias
Twice-daily dosing of the drug appears to be more effective than once-daily dosing for the suppression and prevention of frequent VPCs.
Angina
Once-daily administration may be as effective as divided doses; however, further studies are needed.
Dosage
Available as acebutolol hydrochloride; dosage expressed in terms of acebutolol.
Adults
Hypertension
Oral
Initially, 200–400 mg daily. Usual maintenance dosage is 200–800 mg daily, but some patients may achieve adequate BP control with dosages as low as 200 mg daily. Increase dosage up to 1.2 g daily in two divided doses in patients with more severe hypertension or if adequate reduction of BP does not occur; alternatively, add another hypotensive agent (e.g., thiazide diuretic).
Ventricular Arrhythmias
Oral
Initially, 200 mg twice daily. Increase gradually until optimum effect is achieved. Usual maintenance dosage is 600–1200 mg daily.
Angina
Oral
Initially, 200 mg twice daily. Increase dosage gradually until optimum effect is achieved. Usual maintenance dosage is 800 mg or less daily, but patients with severe angina may require higher dosages.
Prescribing Limits
Adults
Hypertension
Oral
Maximum 1.2 g daily.
Special Populations
Renal Impairment
Active metabolite (diacetolol) eliminated principally by the kidneys; dosage and/or frequency of administration must be modified in response to the degree of renal impairment.
Dosage Reductions in Patients with Renal Impairment
Reduction in Usual Daily Dosage
Clcr(mL/min)
50%
25–49 mL/minute
75%
<25 mL/minute
Acebutolol and diacetolol removed by hemodialysis; individualize dosage carefully in patients with severe renal impairment who undergo chronic intermittent hemodialysis.
Geriatric Patients
Consider reduction in maintenance dosage. Avoid dosages >800 mg daily.
Avoid use in patients with decompensated CHF; use cautiously in patients with inadequate myocardial function and, if necessary, in patients with well-compensated heart failure (e.g., those controlled with cardiac glycosides and/or diuretics).
Adequate treatment (e.g., with a cardiac glycoside and/or diuretic) and close observation recommended if signs or symptoms of impending cardiac failure occur; if cardiac failure continues, discontinue therapy, gradually if possible.
Abrupt Withdrawal of Therapy
Possible exacerbated angina symptoms or precipitation of MI in patients with CAD. Abrupt discontinuance of therapy is not recommended. Gradually decrease dosage over a period of about 2 weeks; monitor patients carefully and advise to temporarily limit their physical activity. If exacerbation of angina occurs, reinstitute therapy promptly and initiate appropriate measures for the management of unstable angina pectoris.
Peripheral Vascular Disease
Possible reduction in cardiac output and precipitation or aggravation of symptoms of arterial insufficiency. Use with caution; observe for evidence of disease progression.
Bronchospastic Disease
Possible bronchoconstriction.
Use with caution in patients with bronchospastic disease; administer the lowest effective dosage (initially in divided doses). A bronchodilator (e.g., a β2-adrenergic agonist, theophylline) should be available for immediate use, if necessary.
Major Surgery
Possible risks associated with general anesthesia (e.g., severe hypotension, maintenance of heart beat) due to decreased ability of the heart to respond to reflex β-adrenergic stimuli. Use with caution in patients undergoing major surgery involving general anesthesia; anesthetics used should not cause myocardial depression.
Diabetes and Hypoglycemia
Possible decreased signs and symptoms of hypoglycemia (e.g., tachycardia, palpitation, BP changes, tremor, feelings of anxiety, but not sweating or dizziness) and increased insulin-induced hypoglycemia.
Signs of hyperthyroidism (e.g., tachycardia) may be masked. Possible thyroid storm if therapy is abruptly withdrawn; carefully monitor patients having or suspected of developing thyrotoxicosis.
Sensitivity Reactions
Anaphylactic Reactions
Patients with a history of anaphylactic reactions to a variety of allergens may be more reactive to repeated accidental, diagnostic, or therapeutic challenges with such allergens while taking β-blocking agents. Such patients may be unresponsive to usual doses of epinephrine.
Specific Populations
Pregnancy
Category B.
Lactation
Distributed into milk in higher concentrations than in maternal plasma. Use not recommended by manufacturer.
Pediatric Use
Safety and efficacy not established in children <12 years of age.
Geriatric Use
Insufficient experience in patients >65 years of age to determine whether geriatric patients respond differently than younger adults. However, reduction of maintenance dosage may be necessary, since bioavailability of acebutolol and diacetolol (active metabolite) may be increased compared with that in younger adults. (See Geriatric Patients under Dosage and Administration.)
Hepatic Impairment
Use with caution. Cirrhosis does not appear to substantially affect the pharmacokinetics of acebutolol or diacetolol; however, the effects of hepatic impairment on elimination of the drug have not been fully evaluated.
Renal Impairment
Use with caution; dosage should be reduced based on the degree of renal impairment. (See Renal Impairment under Dosage and Administration.)
Observe closely for evidence of marked bradycardia or hypotension (e.g., vertigo, presyncope or syncope, or orthostatic changes in BP without compensatory tachycardia)
Well absorbed from the GI tract following oral administration; undergoes extensive first-pass metabolism in the liver.
Peak plasma acebutolol and diacetolol concentrations occur within 2–2.5 hours (range: 1–4 hours) and 4 hours (range: 2.4–5 hours), respectively, in healthy individuals or patients with hypertension or arrhythmias.
Absolute bioavailability is approximately 35–50%.
Food
Food may slightly decrease the rate of absorption and peak plasma concentrations of acebutolol and its major metabolite (diacetolol), but the extent of absorption is not substantially affected.
Onset
Effect on resting, reflex, or exercise-induced heart rate and systolic BP begins within 1–1.5 hours, in healthy or hypertensive individuals.
Duration
Effect may persist for up to 24 hours or longer.
Special Populations
In geriatric patients, peak plasma concentrations and AUCs of acebutolol and diacetolol are increased twofold compared with those observed in younger patients.
Distribution
Extent
Acebutolol and diacetolol readily cross the placenta and can accumulate in the fetus.
Acebutolol and diacetolol are distributed into milk at concentrations higher than those in maternal plasma. (See Lactation under Cautions.)
Plasma Protein Binding
Approximately 11–25% (acebutolol) and 6–9% (diacetolol). Approximately 50% bound to erythrocytes.
Elimination
Metabolism
Rapidly and extensively metabolized in the liver to metabolites (acetolol and diacetolol).
Elimination Route
Acebutolol and its metabolites are excreted in feces and urine.
Half-life
About 3 hours in the initial distribution phase (t½α) and about 11 hours (range: 6–12 hours) in the terminal phase (t½β). About 7.5 (range: 7–11 hours) and 3 hours, respectively, for diacetolol and acetolol following a single oral dose.
Special Populations
Renal impairment may reduce clearances of acebutolol and diacetolol. Acebutolol and diacetolol are removed by hemodialysis.
Stability
Storage
Oral
Capsules
Tight containers at room temperature (approximately 25°C).
Protect from light.
Actions
Pharmacologic effects result from both the unchanged drug and diacetolol, which is equipotent to acebutolol.
Inhibits response to adrenergic stimuli by competitively blocking β1-adrenergic receptors within the myocardium. Blocks β2-adrenergic receptors within bronchial and vascular smooth muscle only at high doses.
Decreases exercise-induced heart rate, inhibits reflex orthostatic tachycardia, and may decrease or leave unchanged cardiac output at rest or during exercise. Decreases systolic and diastolic BP at rest and during exercise.
Precise mechanism of hypotensive action has not been determined. May reduce BP by blocking peripheral (especially cardiac) adrenergic receptors (decreasing cardiac output), by decreasing sympathetic outflow from the CNS, and/or by suppressing renin release.
Can produce nervous system effects, although the frequency and/or severity of such effects may be less than those observed with some other β-adrenergic blocking agents.
Unlike some β-adrenergic blocking agents does not consistently suppress plasma renin activity (PRA).
May increase airway resistance and decrease ventilatory capacity, especially in patients with asthma and/or COPD or when high dosages are used.
Does not appear to substantially affect glucose metabolism; however, the drug may potentiate insulin-induced hypoglycemia in diabetic patients receiving oral hypoglycemic agents. (See Interactions.)
Advice to Patients
Importance of taking acebutolol exactly as prescribed.
Importance of not interrupting or discontinuing therapy without consulting clinician; patients should temporarily limit physical activity when discontinuing therapy.
Importance of immediately informing clinician at the first sign or symptom of impending cardiac failure (e.g., weight gain, increased shortness of breath) or if any difficulty in breathing occurs.
In patients with heart failure, importance of informing clinician of signs or symptoms of exacerbation (e.g., weight gain, difficulty in breathing).
Importance of patients informing anesthesiologist or dentist that they are receiving acebutolol therapy prior to undergoing major surgery.
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs as well as any concomitant illnesses.
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.
Importance of informing patients of other important precautionary information. (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Comparative Pricing
This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 09/2009. For the most current and up-to-date pricing information, please visit www.drugstore.com. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.
† Use is not currently included in the labeling approved by the US Food and Drug Administration.
Remember, keep this and all other medicines out of the reach of children,
never share your medicines with others, and use this medication only for the indication prescribed.
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