Acebutolol

Name: Acebutolol

In case of emergency/overdose

In case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Precautions While Using acebutolol

It is very important that your doctor check your progress at regular visits to make sure acebutolol is working properly and to check for unwanted effects .

Acebutolol may cause heart failure in some patients. Check with your doctor right away if you are having chest pain or discomfort; dilated neck veins; extreme fatigue; irregular breathing; an irregular heartbeat; shortness of breath; swelling of the face, fingers, feet, or lower legs; weight gain; or wheezing .

Make sure any doctor or dentist who treats you knows that you are using acebutolol. You may need to stop using acebutolol several days before having surgery .

acebutolol may cause changes in your blood sugar levels. Also, acebutolol may cover up signs of low blood sugar, such as a rapid pulse rate. Check with your doctor if you have these problems or if you notice a change in the results of your blood or urine sugar tests .

How is this medicine (Acebutolol) best taken?

Use acebutolol as ordered by your doctor. Read all information given to you. Follow all instructions closely.

  • Take with or without food.
  • Keep taking this medicine as you have been told by your doctor or other health care provider, even if you feel well.
  • Take acebutolol at the same time of day.
  • To gain the most benefit, do not miss doses.

What do I do if I miss a dose?

  • Take a missed dose as soon as you think about it.
  • If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
  • Do not take 2 doses at the same time or extra doses.

How do I store and/or throw out Acebutolol?

  • Store at room temperature.
  • Protect from light.
  • Store in a dry place. Do not store in a bathroom.
  • Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
  • Check with your pharmacist about how to throw out unused drugs.

Consumer Information Use and Disclaimer

  • If your symptoms or health problems do not get better or if they become worse, call your doctor.
  • Do not share your drugs with others and do not take anyone else's drugs.
  • Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
  • Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
  • Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about this medicine, please talk with your doctor, nurse, pharmacist, or other health care provider.
  • If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take acebutolol or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to acebutolol. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Review Date: October 4, 2017

Dosage & administration

Hypertension
The initial dosage of Acebutolol 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.

Ventricular Arrhythmia
The usual initial dose of Acebutolol 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.

Use in Older Patients
Older patients have an approximately 2-fold increase in bioavailability and may require lower maintenance doses. Doses above 800 mg/day should be avoided in the elderly.

Package label.principal display panel

NDC 50268-050-15
Acebutolol Hydrochloride Capsules, USP
200 mg
Rx Only
50 Capsules (5 X 10) Unit Dose

5026805015

NDC 50268-050-15
Acebutolol Hydrochloride Capsules, USP
200 mg
Rx Only
50 Capsules (5 X 10) Unit Dose

5026805015

Each capsule contains: Acebutolol hydrochloride, USP equivalent to 200 mg of Acebutolol.

USUAL ADULT DOSAGE: See package insert for full prescribing information.

KEEP THIS AND ALL DRUGS OUT OF THE REACH OF CHILDREN.

Store at 20o to 25oC (68o-77oF) (SEE USP Controlled Room Temperature).

Protect from light.

Manufactured for:
AvKARE, Inc.
Pulaski, TN 38478

AvPAK
A DIVISION OF AvKARE


Mfg. Rev.11-2015-01         AV Rev. 03/16 (P)

Acebutolol HYDROCHLORIDE  
Acebutolol hydrochloride capsule
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:50268-050(NDC:65162-669)
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
Acebutolol HYDROCHLORIDE (Acebutolol) Acebutolol 200 mg
Inactive Ingredients
Ingredient Name Strength
D&c Red No. 28  
D&c Yellow No. 10  
Fd&c Blue No. 1  
Fd&c Red No. 40  
Gelatin  
Starch, Corn  
Povidone  
Titanium Dioxide  
Stearic Acid  
Product Characteristics
Color PURPLE (Lavender Opaque) , ORANGE (Bright Orange Opaque) Score no score
Shape CAPSULE (Hard Gelatin) Size 18mm
Flavor Imprint Code Amneal;669
Contains     
Packaging
# Item Code Package Description
1 NDC:50268-050-15 50 BLISTER PACK in 1 BOX, UNIT-DOSE
1 NDC:50268-050-11 1 CAPSULE in 1 BLISTER PACK
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA075047 12/01/2009
Acebutolol HYDROCHLORIDE  
Acebutolol hydrochloride capsule
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:50268-051(NDC:65162-670)
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
Acebutolol HYDROCHLORIDE (Acebutolol) Acebutolol 400 mg
Inactive Ingredients
Ingredient Name Strength
D&c Red No. 28  
D&c Yellow No. 10  
Fd&c Blue No. 1  
Fd&c Red No. 40  
Gelatin  
Starch, Corn  
Povidone  
Titanium Dioxide  
Stearic Acid  
Product Characteristics
Color PURPLE (Lavender Opaque) , ORANGE (Bring Orange Opaque) Score no score
Shape CAPSULE (Hard Gelatin) Size 23mm
Flavor Imprint Code Amneal;670
Contains     
Packaging
# Item Code Package Description
1 NDC:50268-051-15 50 BLISTER PACK in 1 BOX, UNIT-DOSE
1 NDC:50268-051-11 1 CAPSULE in 1 BLISTER PACK
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA075047 12/01/2009 08/11/2016
Labeler - AvPAK (832926666)
Revised: 08/2016   AvPAK

Warnings/Precautions

Concerns related to adverse events:

• Anaphylactic reactions: Use caution with history of severe anaphylaxis to allergens; patients taking beta-blockers may become more sensitive to repeated challenges. Treatment of anaphylaxis (eg, epinephrine) in patients taking beta-blockers may be ineffective or promote undesirable effects.

Disease-related concerns:

• Bronchospastic disease: In general, patients with bronchospastic disease should not receive beta-blockers; for patients with bronchospastic disease who do not respond to or cannot tolerate other therapies, initial low doses of acebutolol may be employed and used cautiously with close monitoring. Ensure patient has an inhaled beta2-agonist immediately available.

• Conduction abnormality: Consider preexisting conditions such as sick sinus syndrome before initiating.

• Diabetes: Use with caution in patients with diabetes mellitus; may potentiate hypoglycemia and/or mask signs and symptoms.

• Heart failure (HF): Beta-blockers with intrinsic sympathomimetic activity (eg, acebutolol) are likely to worsen survival in patients with HF and should be avoided. Beta-blockers shown to improve survival in clinical trials should be used in these patients.

• Hepatic impairment: Use with caution in patients with hepatic impairment.

• Mesenteric vascular disease: Can precipitate or aggravate symptoms of arterial insufficiency in patients with mesenteric vascular disease. Use with caution in these patients. Observe closely for progression of arterial obstruction.

• Myasthenia gravis: Use with caution in patients with myasthenia gravis.

• Peripheral vascular disease (PVD) and Raynaud's disease: May precipitate or aggravate symptoms of arterial insufficiency in patients with PVD and Raynaud's disease. Use with caution and monitor for progression of arterial obstruction.

• Pheochromocytoma (untreated): Adequate alpha1-receptor blockade is required prior to use of any beta-blocker.

• Psoriasis: Beta-blocker use has been associated with induction or exacerbation of psoriasis, but cause and effect have not been firmly established.

• Psychiatric disease: Use with caution in patients with a history of psychiatric illness; may cause or exacerbate CNS depression.

• Renal impairment: Use with caution in patients with renal impairment, especially the elderly. Elimination of the metabolite, diacetolol, is reduced resulting in a two- to threefold increase in its half-life.

• Thyroid disease: May mask signs of hyperthyroidism (eg, tachycardia). If hyperthyroidism is suspected, carefully manage and monitor; abrupt withdrawal may precipitate thyroid storm. Alterations in thyroid function tests may be observed.

Concurrent drug therapy issues:

• Calcium channel blockers: Use with caution in patients on concurrent verapamil or diltiazem; bradycardia or heart block can occur.

• Cardiac glycosides: Use with caution in patients receiving digoxin; bradycardia or heart block can occur.

• Inhaled anesthetic agents: Use with caution in patients receiving inhaled anesthetic agents known to depress myocardial contractility.

Special populations:

• Elderly: Use reduced doses in elderly patients; concentrations of acebutolol and diacetolol are significantly higher in the elderly. Dose should not exceed 800 mg/day.

Other warnings/precautions:

• Abrupt withdrawal: Beta-blocker therapy should not be withdrawn abruptly (particularly in patients with CAD), but gradually tapered to avoid acute tachycardia, hypertension, and/or ischemia. Severe exacerbation of angina, ventricular arrhythmias, and myocardial infarction (MI) have been reported following abrupt withdrawal of beta-blocker therapy. Temporary but prompt resumption of beta-blocker therapy may be indicated with worsening of angina or acute coronary insufficiency.

• Major surgery: Chronic beta-blocker therapy should not be routinely withdrawn prior to major surgery.

Overdose

No specific information on emergency treatment of overdosage is available for Sectral. 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 Sectral 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, levarterenol, 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.

Sectral is dialyzable.

Clinical pharmacology

Sectral is a cardioselective, β-adrenoreceptor blocking agent, which possesses mild intrinsic sympathomimetic activity (ISA) in its therapeutically effective dose range.

Pharmacodynamics

β1 -cardioselectivity has been demonstrated in experimental animal studies. In anesthetized dogs and cats, Sectral is more potent in antagonizing isoproterenol-induced tachycardia (β1) than in antagonizing isoproterenol-induced vasodilatation (β2).In guinea pigs and cats, it is more potent in antagonizing this tachycardia than in antagonizing isoproterenol- induced bronchodilatation (β2). ISA of Sectral has been demonstrated in catecholamine-depleted rats by tachycardia induced by intravenous administration of this agent. A membrane-stabilizing effect has been detected in animals, but only with high concentrations of Sectral.

Clinical studies have demonstrated β -blocking activity at the recommended doses by: a) reduction in the resting heart rate and decrease in exercise-induced tachycardia; b) reduction in cardiac output at rest and after exercise; c) reduction of systolic and diastolic blood pressures at rest and postexercise; d) inhibition of isoproterenol-induced tachycardia.

The β1-selectivity of Sectral has also been demonstrated on the basis of the following vascular and bronchial effects:

Vascular Effects

Sectral has less antagonistic effects on peripheral vascular β2-receptors at rest and after epinephrine stimulation than nonselective β-antagonists.

Bronchial Effects

In single-dose studies in asthmatics examining effects of various beta-blockers on pulmonary function, low doses of acebutolol produce less evidence of bronchoconstriction and less reduction of beta2 agonist, bronchodilating effects, than nonselective agents like propranolol but more than atenolol.

ISA has been observed with Sectral in man, as shown by a slightly smaller (about 3 beats per minute) decrease in resting heart rate when compared to equivalent β-blocking doses of propranolol, metoprolol or atenolol. Chronic therapy with Sectral induced no significant alteration in the blood lipid profile.

Sectral has been shown to delay AV conduction time and to increase the refractoriness of the AV node without significantly affecting sinus node recovery time, atrial refractory period, or the HV conduction time. The membrane-stabilizing effect of Sectral is not manifest at the doses used clinically.

Significant reductions in resting and exercise heart rates and systolic blood pressures have been observed 1.5 hours after Sectral administration with maximal effects occurring between 3 and 8 hours postdosing in normal volunteers. Sectral has demonstrated a significant effect on exercise-induced tachycardia 24 to 30 hours after drug administration.

There are significant correlations between plasma levels of acebutolol and both the reduction in resting heart rate and the percent of β-blockade of exercise-induced tachycardia.

The antihypertensive effect of Sectral has been shown in double-blind controlled studies to be superior to placebo and similar to propranolol and hydrochlorothiazide. In addition, patients responding to Sectral administered twice daily had a similar response whether the dosage regimen was changed to once daily administration or continued on a b.i.d. regimen. Most patients responded to 400 to 800 mg per day in divided doses.

The antiarrhythmic effect of Sectral was compared with placebo, propranolol, and quinidine. Compared with placebo, Sectral significantly reduced mean total ventricular ectopic beats (VEB), paired VEB, multiform VEB, R-on-T beats, and ventricular tachycardia (VT). Both Sectral and propranolol significantly reduced mean total and paired VEB and VT. Sectral and quinidine significantly reduced resting total and complex VEB; the antiarrhythmic efficacy of Sectral was also observed during exercise.

Pharmacokinetics And Metabolism

Sectral is well absorbed from the GI tract. It is subject to extensive first-pass hepatic biotransformation, with an absolute bioavailability of approximately 40% for the parent compound. The major metabolite, an N-acetyl derivative (diacetolol), is pharmacologically active. This metabolite is equipotent to Sectral and in cats is more cardioselective than Sectral; therefore, this first-pass phenomenon does not attenuate the therapeutic effect of Sectral. Food intake does not have a significant effect on the area under the plasma concentration-time curve (AUC) of Sectral although the rate of absorption and peak concentration decreased slightly.

The plasma elimination half-life of Sectral is approximately 3 to 4 hours, while that of its metabolite, diacetolol, is 8 to 13 hours. The time to reach peak concentration for Sectral is 2.5 hours and for diacetolol, after oral administration of Sectral, 3.5 hours.

Within the single oral dose range of 200 to 400 mg, the kinetics are dose proportional. However, this linearity is not seen at higher doses, probably due to saturation of hepatic biotransformation sites. In addition, after multiple dosing the lack of linearity is also seen by AUC increases of approximately 100% as compared to single oral dosing. Elimination via renal excretion is approximately 30% to 40% and by nonrenal mechanisms 50% to 60%, which includes excretion into the bile and direct passage through the intestinal wall.

Sectral has a low binding affinity for plasma proteins (about 26%). Sectral and its metabolite, diacetolol, are relatively hydrophilic and, therefore, only minimal quantities have been detected in the cerebrospinal fluid (CSF).

Drug interaction studies with tolbutamide and warfarin indicated no influence on the therapeutic effects of these compounds. Digoxin and hydrochlorothiazide plasma levels were not affected by concomitant Sectral administration. The kinetics of Sectral were not significantly altered by concomitant administration of hydrochlorothiazide, hydralazine, sulfinpyrazone, or oral contraceptives.

In patients with renal impairment, there is no effect on the elimination half-life of Sectral, but there is decreased elimination of the metabolite, diacetolol, resulting in a two- to three-fold increase in its halflife. For this reason, the drug should be administered with caution in patients with renal insufficiency (see PRECAUTIONS). Sectral and its major metabolite are dialyzable.

Sectral crosses the placental barrier and is secreted in breast milk.

In geriatric patients, the bioavailability of Sectral and its metabolite is increased, approximately twofold, probably due to decreases in the first-pass metabolism and renal function in the elderly.

Acebutolol Drug Class

Acebutolol is part of the drug class:

  • Beta blocking agents, selective

Acebutolol and Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed.

Acebutolol has been detected in human breast milk. Because of the possibility for adverse reactions in nursing infants from acebutolol, a choice should be made whether to stop nursing or to stop use of this medication. The importance of the drug to the mother should be considered.

 

Pregnancy & Lactation

Pregnancy Category: B; D in 2nd and 3rd trimesters (expert analysis). Neonates of mothers who have received acebutolol during pregnancy have reduced birth weight, decreased blood pressure, and decreased heart rate.

Lactation: excreted into milk/not recommended

Pregnancy Categories

A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA:Information not available.

Pharmacology

Mechanism of Action

Cardioselective for beta-1 at low doses; has intrinsic sympathomimetic activity, ie, can lower BP with less decrease in HR

Class 2 antiarrhythmic

Pharmacokinetics

Peak Plasma Time: 2-3 hr

Toxic range: acetabutalol >15-20 mcg/mL, & diacetolol (the active metabolite) < 90-150 mcg/mL

Onset: 1.5-3 hr (initial response); 3-8 hr (peak response)

Duration: 12-24 hr

Bioavailability: 40%

Absorption: 40% (oral)

Protein Bound: 10-26%

Vd: 1.2 L/kg

Metabolism: metabolized in the liver to active met, diacetolol

Metabolites: diacetolol (active), free amine of acebutolol (inactive)

Excretion: principally in feces 56%, urine 30-40%, bile 3-8%

Dialyzable: Yes (HD)

Less effective than thiazide diuretics in black and geriatric patients  Shown to decrease mortality in hypertension and post-myocardial infarction

Half-Life

  • Parent drug (acebutalol): 3-4 hr
  • Active metabolite (diacetolol): 8-13 hr

What should i discuss with my healthcare provider before taking acebutolol (sectral)?

If you have any of these conditions, you may not be able to use acebutolol, or you may need a dosage adjustment or special tests during treatment:

  • asthma, bronchitis, emphysema;
  • diabetes;
  • low blood pressure;
  • a heart problem such as heart block, sick sinus syndrome, slow heart rate, or congestive heart failure;
  • depression;
  • liver or kidney disease;
  • a thyroid disorder;
  • myasthenia gravis;
  • pheochromocytoma; or
  • problems with circulation (such as Raynaud's syndrome).

FDA pregnancy category B. This medication is not expected to be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment.

Acebutolol can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

Usual Adult Dose for Ventricular Arrhythmia

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

Renal Dose Adjustments

CrCl less than 50 mL/min: Reduce daily dose by 50%
CrCl less than 25 mL/min: Reduce daily dose by 75%

Dialysis

Data not available

Administrative Information

LactMed Record Number

282

Last Revision Date

20130907

Disclaimer

Information presented in this database is not meant as a substitute for professional judgment. You should consult your healthcare provider for breastfeeding advice related to your particular situation. The U.S. government does not warrant or assume any liability or responsibility for the accuracy or completeness of the information on this Site.

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