Acebutolol Hydrochloride

Name: Acebutolol Hydrochloride

Uses for Acebutolol Hydrochloride

Hypertension

Management of hypertension (alone or in combination with other classes of antihypertensive agents).1 280 500

β-Adrenergic blocking agents (β-blockers) generally not preferred for initial management of hypertension, but may be considered in patients who have a compelling indication (e.g., prior MI, ischemic heart disease, heart failure) for their use or as add-on therapy in those who do not respond adequately to the preferred drug classes (ACE inhibitors, angiotensin II receptor antagonists, calcium-channel blockers, or thiazide diuretics).361 501 502 503 504 515 523 524 527 800

Black hypertensive patients generally tend to respond better to monotherapy with calcium-channel blockers or thiazide diuretics than to β-blockers.355 359 360 500 501 504 However, diminished response to β-blockers is largely eliminated when administered concomitantly with a thiazide diuretic.500

Cardiac Arrhythmias

Treatment of frequent ventricular premature complexes (VPCs), including uniform and multiform VPCs and/or coupled VPCs, and R-on-T complexes1 2 137 185 186 187 188 189 190 193 194 195 196 197 198 199 201 204 in patients with primary arrhythmias or arrhythmias secondary to various cardiac disorders (e.g., CAD,137 185 186 187 188 189 194 acute MI,137 186 187 193 194 195 196 valvular disease).185 186 187 189 190

Management of various supraventricular tachyarrhythmias†.191 192 196 200 202 203 256 266

Angina

Management of chronic stable angina pectoris†.205 206 207 208 209 210 211 212 213 214 220 221 222 223 224 225

Acute Myocardial Infarction

Secondary prevention following acute MI† to reduce the risk of reinfarction and mortality.289 290

Acebutolol Hydrochloride Dosage and Administration

General

  • Individualize dosage according to patient response.1 2 4

  • β-Adrenergic blocking selectivity diminishes as dosage is increased.1

  • If long-term therapy is discontinued, reduce dosage gradually over a period of about 2 weeks.1 2 (See Abrupt Withdrawal of Therapy under Cautions.)

  • When substituting another β-blocker for acebutolol, initiate at a comparable dosage without interruption of β-blocker therapy.1 2

BP Monitoring and Treatment Goals

  • Carefully monitor BP during initial titration or subsequent upward adjustment in dosage.500 501

  • When available, use evidence-based dosing information (i.e., dosages shown in randomized controlled trials to reduce complications of hypertension) to determine target dosages; target dosages usually can be achieved within 2–4 weeks but may take up to several months.501

  • Goal is to achieve and maintain optimal control of BP; individualize specific target BP based on consideration of multiple factors, including patient age and comorbidities, and currently available evidence from clinical studies.500 501

Administration

Acebutolol hydrochloride is administered orally.1 2 Also been administered IV†,25 27 28 29 41 191 192 196 200 202 203 266 but a parenteral dosage form is currently not commercially available in the US.

Oral Administration

Hypertension

Usually administer as a single daily dose;1 245 however, for 24-hour BP control, some patients may require administration of the daily dose in 2 divided doses.1 142 143 144 145 149 155 500

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.4 185 186 188 189 195 198 199 203 204 248

Angina

Once-daily administration may be as effective as divided doses;4 208 249 however, further studies are needed.4

Dosage

Available as acebutolol hydrochloride; dosage expressed in terms of acebutolol.1

Adults

Hypertension Oral

Initially, 200–400 mg daily.1 245 321 Usual maintenance dosage is 400–800 mg daily, 1 140 142 143 144 145 149 150 151 152 153 154 245 246 247 500 but some patients may achieve adequate BP control with dosages as low as 200 mg daily.1 4 500 Increase dosage up to 1.2 g daily in 2 divided doses in patients with more severe hypertension or if adequate reduction of BP does not occur;1 2 4 140 142 143 144 145 149 150 151 152 154 155 alternatively, add another hypotensive agent (e.g., thiazide diuretic).1 2 4 142 144 157 158 160 161 165 166 168

If intolerable adverse effects occur, consider dosage reduction; if adverse effects worsen or fail to resolve, may need to discontinue and switch to another antihypertensive drug class.501

Ventricular Arrhythmias Oral

Initially, 200 mg twice daily.1 187 196 Increase gradually until optimum effect is achieved.1 185 186 195 198 204 Usual maintenance dosage is 600–1200 mg daily.1 2 4 185 186 189 190 195 199 204

Angina Oral

Initially, 200 mg twice daily.4 205 208 Increase dosage gradually until optimum effect is achieved.4 205 Usual maintenance dosage is 800 mg or less daily,4 206 207 208 209 210 211 212 213 214 but patients with severe angina may require higher dosages.4 205 209 211

Adjust dosage of β-blockers according to clinical response4 205 and to maintain a resting heart rate of 55–60 bpm.211 216

Prescribing Limits

Adults

Hypertension Oral

Maximum 1.2 g daily.1 2 4 140 142 143 144 145 149 150 151 152 154 155

Special Populations

Renal Impairment

Active metabolite (diacetolol) eliminated principally by the kidneys;1 123 125 dosage and/or frequency of administration must be modified in response to the degree of renal impairment.1 2 86 123 124 125 126 127

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;1 125 127 individualize dosage carefully in patients with severe renal impairment who undergo chronic intermittent hemodialysis.124 125

Geriatric Patients

Consider reduction in maintenance dosage.1 2 Avoid dosages >800 mg daily.1 2

Interactions for Acebutolol Hydrochloride

Specific Drugs

Drug

Interaction

Comments

α-Adrenergic agonists1

Possible exaggerated hypertensive reactions1

Warn patients of potential hazard1

Calcium-channel blockers

Potential additive depressant effects on SA or AV nodal conduction318 319

Cardiac glycosides (digoxin)

Potential additive depressant effects on SA or AV nodal conduction318 319

Pharmacokinetic interaction unlikely1

Diuretics

Possible increased hypotensive effect1 2 142 144 157 158 160

Careful dosage adjustment recommended1 2 144 157 158 160

Glyburide

Possible decreased hypoglycemic action in type II diabetic patients, presumably by decreasing insulin secretion244

Hydralazine

Pharmacokinetic interaction unlikely1

Hydrochlorothiazide

Pharmacokinetic interaction unlikely1

Hypotensive agents

Possible increased hypotensive effect1 2 142 144 157 158 160

Careful dosage adjustment recommended1 2 144 157 158 160

NSAIAs

Potential blunting of hypotensive effects1

Oral contraceptives

Pharmacokinetic interaction unlikely1

Reserpine

Possible additive pharmacologic effects1

Observe closely for evidence of marked bradycardia or hypotension (e.g., vertigo, presyncope or syncope, or orthostatic changes in BP without compensatory tachycardia)1

Sulfinpyrazone

Pharmacokinetic interaction unlikely1

Sympathomimetic agents

Antagonism of β1-adrenergic stimulating effects (e.g., bronchodilation)1 2 57 58 59 62

Increased dosage of β-adrenergic agonist bronchodilators may be required 268 277

Tolbutamide

Interaction unlikely1

Warfarin

Interaction unlikely1

Actions

  • Pharmacologic effects result from both the unchanged drug and diacetolol, 1 2 114 115 116 117 which is equipotent to acebutolol.1 2 114 115 116 117

  • Inhibits response to adrenergic stimuli by competitively blocking β1-adrenergic receptors within the myocardium.1 2 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 34 35 36 37 38 Blocks β2-adrenergic receptors within bronchial and vascular smooth muscle only at high doses.4 24 35 178

  • Decreases exercise-induced heart rate,1 2 4 11 12 13 23 24 25 27 inhibits reflex orthostatic tachycardia,1 2 4 11 12 13 23 24 and may decrease1 2 25 28 29 140 193 or leave unchanged 26 140 cardiac output at rest2 25 140 193 or during exercise.1 28 29 Decreases systolic and diastolic BP at rest1 2 13 19 23 56 57 139 and during exercise.1 2 155 160 171

  • Precise mechanism of hypotensive action has not been determined.7 22 26 34 35 139 178 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.7 26 34 35 140

  • Exhibits antiarrhythmic activity;1 2 137 185 186 187 188 189 190 193 194 195 196 199 204 considered a class II antiarrhythmic agent.254

  • Can produce nervous system effects,1 2 4 6 150 152 154 158 170 198 although the frequency and/or severity of such effects may be less than those observed with some other β-blockers.152 154 156 262

  • Unlike some β-blockers,147 148 does not consistently suppress plasma renin activity (PRA).26 71 139 140 141 142 143

  • May increase airway resistance and decrease ventilatory capacity,51 52 53 54 57 58 59 60 61 62 63 64 155 158 especially in patients with asthma and/or COPD or when high dosages are used.52 53 57 58 59 60 61 62 63 64 158 268

  • Does not appear to substantially affect glucose metabolism;73 75 however, the drug may potentiate insulin-induced hypoglycemia in diabetic patients receiving oral hypoglycemic agents.74 (See Interactions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Acebutolol Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules

200 mg (of acebutolol)*

Acebutolol Hydrochloride Capsules

Sectral

Promius

400 mg (of acebutolol)*

Acebutolol Hydrochloride Capsules

Sectral

Promius

(web3)