Acebutolol

Name: Acebutolol

What special precautions should I follow?

Before taking acebutolol,

  • tell your doctor and pharmacist if you are allergic to acebutolol, any other medications, or any ingredients in acebutolol capsules. Ask your pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking. Be sure to mention any of the following: medications for migraine headaches, diabetes, asthma, allergies, colds, or pain; other medications for high blood pressure or heart disease; and reserpine.
  • tell your doctor if you have or have ever had heart, kidney, or liver disease; asthma or other lung diseases; diseases of the blood vessels; severe allergies; diabetes; or hyperthyroidism (an overactive thyroid gland).
  • tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking acebutolol, call your doctor.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking acebutolol.
  • you should know that this medication may make you drowsy. Do not drive a car or operate machinery until you know how this medication affects you.
  • remember that alcohol can add to the drowsiness caused by this medication.

What other information should I know?

Keep all appointments with your doctor and the laboratory. Your blood pressure should be checked regularly to determine your response to acebutolol. Your doctor may ask you to check your pulse (heart rate). Ask your pharmacist or doctor to teach you how to take your pulse. If your pulse is faster or slower than it should be, call your doctor.

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

What is acebutolol?

Acebutolol is a beta-blocker. Beta-blockers affect the heart and circulation (blood flow through arteries and veins).

Acebutolol is used to treat hypertension (high blood pressure) and heart rhythm disorders.

Acebutolol may also be used for purposes not listed in this medication guide.

What should I discuss with my healthcare provider before taking acebutolol?

You should not use acebutolol if you are allergic to it, or if you have a serious heart condition such as:

  • AV block (2nd or 3rd degree);

  • severe heart failure; or

  • slow heartbeats that have caused you to faint.

To make sure acebutolol is safe for you, tell your doctor if you have:

  • coronary artery disease (hardened arteries);

  • peripheral vascular disease such as Raynaud's syndrome;

  • a history of heart failure;

  • a heart condition for which you take digoxin (digitalis) or a diuretic ("water pill");

  • asthma, chronic obstructive pulmonary disease (COPD), sleep apnea, or other breathing disorder;

  • diabetes (taking acebutolol may make it harder for you to tell when you have low blood sugar);

  • liver or kidney disease;

  • a thyroid disorder; or

  • a history of allergies.

Older adults may be more sensitive to the effects of this medicine.

It is not known whether this medicine will harm an unborn baby. However, taking acebutolol during pregnancy may cause problems after the baby is born. This includes low birth weight, slow heartbeats, and low blood pressure. Tell your doctor if you are pregnant or plan to become pregnant while taking acebutolol.

Acebutolol can pass into breast milk and may harm a nursing baby. You should not breast-feed while using this medicine.

Acebutolol dosing information

Usual Adult Dose for Hypertension:

Initial dose: 400 mg orally per day in 1 to 2 divided doses
Maintenance dose: 400 to 800 mg orally per day

Comments: Some patients may respond to as little as 200 mg orally per day; patients with inadequately controlled or more severe hypertension may respond to 600 mg orally twice a day or to the addition of a second antihypertensive; beta-1 selectivity diminishes with increasing dose.

Usual Adult Dose for Ventricular Arrhythmia:

Initial dose: 200 mg orally twice a day
Maintenance dose: 600 to 1200 mg orally per day

Commonly used brand name(s)

In the U.S.

  • Sectral

Available Dosage Forms:

  • Tablet
  • Capsule

Therapeutic Class: Cardiovascular Agent

Pharmacologic Class: Beta-Adrenergic Blocker, Cardioselective

Indications & usage

Hypertension
Acebutolol hydrochloride capsules are indicated for the management of hypertension in adults. It may be used alone or in combination with other antihypertensive agents, especially thiazide-type diuretics.

Ventricular Arrhythmias
Acebutolol hydrochloride capsules are indicated in the management of ventricular premature beats; it reduces the total number of premature beats, as well as the number of paired and multiform ventricular ectopic beats, and R-on-T beats.

Precautions

Risk of Anaphylactic Reaction
While taking beta-blockers, patients with a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenged, either accidental, diagnostic, or therapeutic. Such patients may be unresponsive to the usual doses of epinephrine used to treat allergic reaction.

Impaired Renal or Hepatic Function
Studies on the effect of Acebutolol in patients with renal insufficiency have not been performed in the U.S. Foreign published experience shows that Acebutolol has been used successfully in chronic renal insufficiency. Acebutolol is excreted through the GI tract, but the active metabolite, diacetolol, is eliminated predominantly by the kidney. There is a linear relationship between renal clearance of diacetolol and creatinine clearance. Therefore, the daily dose of Acebutolol should be reduced by 50% when the creatinine clearance is less than 50 mL/min and by 75% when it is less than 25 mL/min. Acebutolol should be used cautiously in patients with impaired hepatic function.

Acebutolol has been used successfully and without problems in elderly patients in the U.S. clinical trials without specific adjustment of dosage. However, elderly patients may require lower maintenance doses because the bioavailability of both Acebutolol and its metabolite are approximately doubled in this age group.

Information of Patients
Patients, especially those with evidence of coronary ar tery disease, should be warned against interruption or discontinuation of Acebutolol therapy without a physician’s supervision.  Although cardiac failure rarely occurs in properly selected patients, those being treated with β-adrenergic blocking agents should be advised to consult a physician if they develop signs or symptoms suggestive of impending CHF, or unexplained respiratory symptoms.

Patients should also be warned of possible severe hypertensive reactions from concomitant use of α-adrenergic stimulants, such as the nasal decongestants commonly used in OTC cold preparations and nasal drops.

Clinical Laboratory Findings
Acebutolol, like other β-blockers, has been associated with the development of antinuclear antibodies (ANA). In prospective clinical trials, patients receiving Acebutolol had a dose-dependent increase in the development of positive ANA titers, and the overall incidence was higher than that observed with propranolol. Symptoms (generally persistent arthralgias and myalgias) related to this laboratory abnormality were infrequent (less than 1% with both drugs). Symptoms and ANA titers were reversible upon discontinuation of treatment.

Drug Interactions
Catecholamine-depleting drugs, such as reserpine, may have an additive effect when given with β-blocking agents. Patients treated with Acebutolol plus catecholamine depletors should, therefore, be observed closely for evidence of marked bradycardia or hypotension which may present as vertigo, syncope/presyncope, or orthostatic changes in blood pressure without compensatory tachycardia. Exaggerated hypertensive responses have been reported from the combined use of β-adrenergic antagonists and α-adrenergic stimulants, including those contained in proprietary cold remedies and vasoconstrictive nasal drops. Patients receiving β-blockers should be warned of this potential hazard.

Blunting of the antihypertensive effect of beta-adrenoreceptor blocking agents by nonsteroidal anti-inflammatory drugs has been reported.

No significant interactions with digoxin, hydrochlorothiazide, hydralazine, sulfinpyrazone, oral contraceptives, tolbutamide, or warfarin have been observed.

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

Carcinogeneis, Mutagenesis, Impairment of Fertility
Chronic oral toxicity studies in rats and mice, employing dose levels as high as 300 mg/kg/day, which is equivalent to 15 times the maximum recommended (60 kg) human dose, did not indicate a carcinogenic potential for Acebutolol. Diacetolol, the major metabolite of Acebutolol in man, was without carcinogenic potential in rats when tested at doses as high as 1800 mg/kg/day. Acebutolol and diacetolol were also shown to be devoid of mutagenic potential in the Ames Test. Acebutolol, administered orally to two generations of male and female rats at doses of up to 240 mg/kg/day (equivalent to 12 times the maximum recommended therapeutic dose in a 60-kg human) and diacetolol, administered to two generations of male and female rats at doses of up to 1000 mg/kg/day, had no significant impact on reproductive performance or fertility.

Pregnancy

Teratogenic Effects:

Pregnancy Category B: Reproduction studies have been performed with Acebutolol in rats (up to 630 mg/kg/day) and rabbits (up to 135 mg/kg/day). These doses are equivalent to approximately 31.5 and 6.8 times the maximum recommended therapeutic dose in a 60-kg human, respectively. The compound was not teratogenic in either species. In the rabbit, however, doses of 135 mg/kg/day caused slight fetal growth retardation; this effect was considered to be a result of maternal toxicity, as evidenced by reduced food intake, a lowered rate of body weight gain, and mortality. Studies have also been performed in these species with diacetolol (at doses of up to 450 mg/kg/day in rabbits and up to 1800 mg/kg/day in rats). Other than a significant elevation in post-implantation loss with 450 mg/kg/day diacetolol, a level at which food consumption and body weight gain were reduced in rabbit dams and a nonstatistically significant increase in incidence of bilateral cataract in rat fetuses from dams treated with 1800 mg/kg/day diacetolol, there was no evidence of harm to the fetus. There are no adequate and well-controlled trials in pregnant women. Because animal teratology studies are not always predictive of the human response, Acebutolol should be used during pregnancy only if the potential benefit justifies the risk to the fetus.

Nonteratogenic Effects:

Studies in humans have shown that both Acebutolol and diacetolol cross the placenta. Neonates of mothers who have received Acebutolol during pregnancy have reduced birth weight, decreased blood pressure, and decreased heart rate. In the newborn the elimination half-life of Acebutolol was 6 to 14 hours, while the half-life of diacetolol was 24 to 30 hours for the first 24 hours after birth, followed by a half-life of 12 to 16 hours. Adequate facilities for monitoring these infants at birth should be available.

Labor and Delivery
The effect of Acebutolol on labor and delivery in pregnant women is unknown. Studies in animals have not shown any effect of Acebutolol on the usual course of labor and delivery.

Nursing Mothers
Acebutolol and diacetolol also appear in breast milk with a milk:plasma ratio of 7.1 and 12.2, respectively. Use in nursing mothers is not recommended.

Pediatric Use
Safety and effectiveness in pediatric patients have not been established.

Geriatric Use
Clinical studies of Acebutolol and other reported clinical experience is inadequate to determine whether there are differences in safety or effectiveness between patients above or below age 65. Elderly subjects evidence greater bioavailability of Acebutolol (see CLINICAL PHARMACOLOGY - Pharmacokentics and Metabolism), presumably because of age-related reduction in first-pass metabolism and renal function. Therefore, it may be appropriate to start elderly patients at the low end of the dosing range (see DOSAGE AND ADMISTRATION - Use in Older Patients).

Overdosage

No specific information on emergency treatment of overdosage is available for Acebutolol.

However, overdosage with other β-blocking agents has been accompanied by extreme bradycardia, advanced atrioventricular block, intraventricular conduction defects, hypotension, severe congestive heart failure, seizures, and in susceptible patients, bronchospasm and hypoglycemia. Although specific information on the emergency treatment of Acebutolol overdose is not available on the basis of the pharmacological actions and the observations in treating overdoses with other β-blockers, the following general measures should be considered:

1. Empty stomach by emesis or lavage.

2. Bradycardia: IV atropine (1 to 3 mg in divided doses). If antivagal response is inadequate, administer isoproterenol cautiously since larger than usual doses of isoproterenol may be required.

3. Persistent hypotension in spite of correction of bradycardia: Administer vasopressor (e.g., epinephrine, norepinephrine, dopamine, or dobutamine) with frequent monitoring of blood pressure and pulse rate.

4. Bronchospasm: A theophylline derivative, such as aminophylline and/or parenteral β2-stimulant, such as terbutaline.

5. Cardiac failure: Digitalize the patient and/or administer a diuretic. It has been reported that glucagon is useful in this situation.

Acebutolol is dialyzable.

Dosing Geriatric

Refer to adult dosing. Consider dose reduction due to age-related increase in bioavailability; do not exceed 800 mg/day. In the management of hypertension, consider lower initial dose (eg, 200 to 400 mg/day) and titrate to response (Aronow, 2011).

Dietary Considerations

May be taken without regard to meals.

Monitoring Parameters

Blood glucose (especially in patients with diabetes mellitus); blood pressure, orthostatic hypotension, heart rate, CNS effects, ECG

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience headache or loss of strength and energy. Have patient report immediately to prescriber signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), severe dizziness, passing out, shortness of breath, excessive weight gain, swelling of arms or legs, bradycardia, or abnormal heartbeat (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

Acebutolol Overview

Acebutolol is a prescription medication used to treat high blood pressure and irregular heartbeat (known medically as ventricular arrhythmia). This medication belongs to a group of drugs called beta blockers. It works to decrease blood pressure, heart rate, and the workload of the heart by blocking beta receptors. 

Acebutolol comes in capsule form. It is usually taken once or twice daily, with or without food.

Common side effects include tiredness, headaches, and dizziness. Do not drive or operate heavy machinery until you know how it affects you. 

Acebutolol Interactions

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

  • reserpine (Serpalan)
  • decongestant medications such as pseudoephedrine (Sudafed) and pheylephrine (Sudafed PE)
  • digoxin (Lanoxin)

This is not a complete list of acebutolol drug interactions.  Ask your doctor or pharmacist for more information.

Acebutolol Food Interactions

Medications can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of acebutolol, there are no specific foods that you must exclude from your diet when receiving this medication.

Acebutolol Dosage

Take acebutolol exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The acebutolol dose your doctor recommends will be based on the following:

  • the condition being treated
  • other medical conditions you have
  • other medications you are taking
  • how you respond to this medication
  • age

The recommended dose range for acebutolol is 200 mg to 1200 mg taken once or twice a day.

 

Acebutolol Overdose

If you take too much acebutolol, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

If acebutolol is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

What is acebutolol (sectral)?

Acebutolol is in a group of drugs called beta-blockers. Beta-blockers affect the heart and circulation (blood flow through arteries and veins).

Acebutolol is used to treat hypertension (high blood pressure) and heart rhythm disorders.

Acebutolol may also be used for other purposes not listed in this medication guide.

Liver Dose Adjustments

Use with caution

Precautions

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

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