Acebutolol

Name: Acebutolol

Acebutolol Side Effects

Common Side Effects of Acebutolol

Tell your doctor if any of the following side effects become severe or don't go away:

  • Diarrhea or constipation
  • Mild dizziness or lightheadedness
  • Frequent urination
  • Gas
  • Indigestion
  • Nausea
  • Headache
  • Mild drowsiness or sleepiness
  • Trouble sleeping
  • Weakness

Serious Side Effects of Acebutolol

Tell your doctor right away if you experience any of the following serious side effects:

  • Chest pain or tightness
  • Shortness of breath
  • Wheezing
  • Swelling of the hands, ankles, or feet
  • Slow heartbeat
  • Yellowing of the skin or eyes
  • Dark-colored urine
  • Pale-colored stools
  • Severe or persistent nausea or loss of appetite
  • Difficulty breathing, especially while lying down
  • Mental or mood changes
  • Confusion
  • Severe or persistent muscle or joint pain
  • Severe headache
  • Blurred vision
  • Pounding in your chest or ears
  • Signs of a severe allergic reaction, which may include rash, hives, itching or severe itching, difficulty breathing, chest tightness, or swelling of the face, mouth, lips, or tongue

How should this medicine be used?

Acebutolol comes as a capsule to take by mouth. It usually is taken once or twice a day. To help you remember to take acebutolol, take it around the same time(s) every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take acebutolol exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Acebutolol controls your condition but does not cure it. Continue to take acebutolol even if you feel well. Do not stop taking acebutolol without talking to your doctor. If you suddenly stop taking acebutolol, you may experience serious heart problems such as angina (chest pain) or heart attack.

What side effects can this medication cause?

Acebutolol may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • dizziness
  • lightheadedness
  • excessive tiredness
  • headache
  • constipation
  • diarrhea
  • upset stomach
  • muscle aches

Some side effects can be serious. If you experience any of the following symptoms, call your doctor immediately:

  • shortness of breath or wheezing
  • swelling of the feet and lower legs
  • chest pain

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).

What is the most important information I should know about acebutolol?

You should not use acebutolol 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.

What other drugs will affect acebutolol?

Tell your doctor about all your current medicines and any you start or stop using, especially:

  • reserpine;

  • cold medicines, stimulant medicines, or diet pills;

  • NSAIDs (nonsteroidal anti-inflammatory drugs)--aspirin, ibuprofen (Advil, Motrin), naproxen (Aleve), celecoxib, diclofenac, indomethacin, meloxicam, and others; or

  • other beta-blockers--atenolol, carvedilol, metoprolol, nebivolol, propranolol, sotalol, and others.

This list is not complete. Other drugs may interact with acebutolol, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

Proper Use of acebutolol

In addition to the use of acebutolol, treatment for your high blood pressure may include weight control and changes in the types of foods you eat, especially foods high in sodium. Your doctor will tell you which of these are most important for you. You should check with your doctor before changing your diet .

Many patients who have high blood pressure will not notice any signs of the problem. In fact, many may feel normal. It is very important that you take your medicine exactly as directed and that you keep your appointments with your doctor even if you feel well .

Remember that acebutolol will not cure your high blood pressure, but it does help control it. You must continue to take it as directed if you expect to lower your blood pressure and keep it down. You may have to take high blood pressure medicine for the rest of your life. If high blood pressure is not treated, it can cause serious problems such as heart failure, blood vessel disease, stroke, or kidney disease .

Do not interrupt or stop taking acebutolol without first checking with your doctor. Your doctor may want you to gradually reduce the amount you are taking before stopping it completely. Some conditions may become worse when the medicine is stopped suddenly, which can be dangerous .

Dosing

The dose of acebutolol will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of acebutolol. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (capsules):
    • For high blood pressure:
      • Adults—At first, 400 milligrams (mg) once or twice a day. Your doctor may adjust your dose as needed.
      • Children—Use and dose must be determined by your doctor .
    • For ventricular arrhythmia:
      • Adults—At first, 200 milligrams (mg) twice a day. Your doctor may increase your dose if needed.
      • Children—Use and dose must be determined by your doctor .

Missed Dose

If you miss a dose of acebutolol, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

What do I need to tell my doctor BEFORE I take Acebutolol?

  • If you have an allergy to acebutolol or any other part of acebutolol.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you have any of these health problems: Very bad heart failure (weak heart), a heartbeat that is not normal, or a very slow heartbeat.

This is not a list of all drugs or health problems that interact with this medicine.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take acebutolol with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some other side effects of Acebutolol?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

  • Dizziness.
  • Headache.
  • Feeling tired or weak.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

Acebutolol Description

Acebutolol HCl, USP is a selective, hydrophilic beta-adrenoreceptor blocking agent with mild intrinsic sympathomimetic activity for use in treating patients with hypertension and ventricular arrhythmias. It is marketed in capsule form for oral administration. Acebutolol HCl, USP capsules are provided in two dosage strengths which contain 200 or 400 mg of Acebutolol as the hydrochloride salt.

The inactive ingredients present are D&C Red 28, D&C Yellow 10, FD&C Blue 1, FD&C Red 40, gelatin, maize starch, povidone, stearic acid and titanium dioxide.

Acebutolol HCl has the following structural formula:

C18H28N2O4•HCl                                                                   M.W. 372.89

Acebutolol HCl, USP is a white or slightly off-white powder freely soluble in water, and less soluble in alcohol. Chemically it is defined as the hydrochloride salt of (±) N-[3-Acetyl-4-[2-hydroxy-3-[(1-methylethyl) amino]propoxy]phenyl] butanamide.

Acebutolol - Clinical Pharmacology

Acebutolol 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, Acebutolol 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 Acebutolol 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 Acebutolol.

Clinical studies have demonstrated β1-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 Acebutolol has also been demonstrated on the basis of the following vascular and bronchial effects:

Vascular Effects: Acebutolol 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 Acebutolol 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 Acebutolol induced no significant alteration in the blood lipid profile.

Acebutolol 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 Acebutolol 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 Acebutolol administration with maximal effects occurring between 3 and 8 hours postdosing in normal volunteers. Acebutolol 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 Acebutolol has been shown in double-blind controlled studies to be superior to placebo and similar to propranolol and hydrochlorothiazide. In addition, patients responding to Acebutolol 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 Acebutolol was compared with placebo, propranolol, and quinidine. Compared with placebo, Acebutolol significantly reduced mean total ventricular ectopic beats (VEB), paired VEB, multiform VEB, R-on-T beats, and ventricular tachycardia (VT). Both Acebutolol and propranolol significantly reduced mean total and paired VEB and VT.

Acebutolol and quinidine significantly reduced resting total and complex VEB; the antiarrhythmic efficacy of Acebutolol was also observed during exercise.

Pharmacokinetics and Metabolism                    

Acebutolol 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 Acebutolol and in cats is more cardioselective than Acebutolol;

therefore, this first-pass phenomenon does not attenuate the therapeutic effect of Acebutolol. Food intake does not have a significant effect on the area under the plasma concentration-time curve (AUC) of Acebutolol although the rate of absorption and peak concentration decreased slightly.

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

Acebutolol has a low binding affinity for plasma proteins (about 26%). Acebutolol 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 Acebutolol administration. The kinetics of Acebutolol 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 Acebutolol, but there is decreased elimination of the metabolite, diacetolol, resulting in a two- to three-fold increase in its half-life. For this reason, the drug should be administered with caution in patients with renal insufficiency (see Precautions). Acebutolol and its major metabolite are dialyzable.

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

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

Warnings

Cardiac Failure
Sympathetic stimulation may be essential for support of the circulation in individuals with diminished myocardial contractility, and its inhibition by β-adrenergic receptor blockade may precipitate more severe failure. Although β-blockers should be avoided in overt cardiac failure, Acebutolol can be used with caution in patients with a history of heart failure who are controlled with digitalis and/or diuretics. Both digitalis and Acebutolol impair AV conduction. If cardiac failure persists, therapy with Acebutolol should be withdrawn.

In Patients Without a History of Cardiac Failure
In patients with aortic or mitral valve disease or compromised left ventricular function, continued depression of the myocardium with β-blocking agents over a period of time may lead to cardiac failure. At the first signs of failure, patients should be digitalized and/or be given a diuretic and the response observed closely. If cardiac failure continues despite adequate digitalization and/or diuretic, Acebutolol therapy should be withdrawn.

Exacerbation of Ischemic Heart Disease Following Abrupt Withdrawal
Following abrupt cessation of therapy with certain β-blocking agents in patients with coronary artery disease, exacerbation of angina pectoris and, in some cases, myocardial infarction and death have been reported. Therefore, such patients should be cautioned against interruption of therapy without a physician’s advice. Even in the absence of overt ischemic heart disease, when discontinuation of Acebutolol is planned, the patient should be carefully observed, and should be advised to limit physical activity to a minimum while Acebutolol is gradually withdrawn over a period of about two weeks. (If therapy with an alternative β-blocker is desired, the patient may be transferred directly to comparable doses of another agent without interruption of β-blocking therapy.) If an exacerbation of angina pectoris occurs, antianginal therapy should be restarted immediately in full doses and the patient hospitalized until his condition stabilizes.

Peripheral Vascular Disease
Treatment with β-antagonists reduces cardiac output and can precipitate or aggravate the symptoms of arterial insufficiency in patients with peripheral or mesenteric vascular disease. Caution should be exercised with such patients, and they should be observed closely for evidence of progression of arterial obstruction.

Bronchospastic Diseases
PATIENTS WITH BRONCHOSPASTIC DISEASE SHOULD, IN GENERAL, NOT RECEIVE A β-BLOCKER. Because of its relative β1-selectivity, however, low doses of Acebutolol may be used with caution in patients with bronchospastic disease who do not respond to, or who cannot tolerate, alternative treatment. Since β1-selectivity is not absolute and is dose-dependent, the lowest possible dose of Acebutolol should be used initially, preferably in divided doses to avoid the higher plasma levels associated with the longer dose-interval. A bronchodilator, such as theophylline or a β2-stimulant, should be made available in advance with instructions concerning its use.

WARNINGS, Major Surgery 
Chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery; however, the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures.

Diabetes and Hypoglycemia
β-blockers may potentiate insulin-induced hypoglycemia and mask some of its manifestations such as tachycardia; however, dizziness and sweating are usually not significantly affected. Diabetic patients should be warned of the possibility of masked hypoglycemia.

Thyrotoxicosis
β-adrenergic blockade may mask certain clinical signs (tachycardia) of hyperthyroidism. Abrupt withdrawal of β-blockade may precipitate a thyroid storm; therefore, patients suspected of developing thyrotoxicosis from whom Acebutolol therapy is to be withdrawn should be monitored closely.

Adverse Reactions

Acebutolol is well tolerated in properly selected patients. Most adverse reactions have been mild, not required discontinuation of therapy, and tended to decrease as duration of treatment  increases.

The following table shows the frequency of treatment-related side effects derived from controlled clinical trials in patients with hypertension, angina pectoris, and arrhythmia. These patients received Acebutolol, propranolol, or hydrochlorothiazide as monotherapy, or placebo.

The following selected (potentially important) side effects were seen in up to 2% of Acebutolol patients:

Cardiovascular: hypotension, bradycardia, heart failure.

Central Nervous System: anxiety, hyper/hypoesthesia, impotence.

Dermatological: pruritus.

Gastrointestinal: vomiting, abdominal pain.

Genitourinary: dysuria, nocturia.

Liver and Biliary System: A small number of cases of liver abnormalities (increased SGOT, SGPT, LDH) have been reported in association with Acebutolol therapy. In some cases increased bilirubin or alkaline phosphatase, fever, malaise, dark urine, anorexia, nausea, headache, and/or other symptoms have been reported. In some of the reported cases, the symptoms and signs were confirmed by rechallenge with Acebutolol. The abnormalities were reversible upon cessation of Acebutolol therapy.

Musculoskeletal: back pain, joint pain.

Respiratory: pharyngitis, wheezing.

Special Senses: conjunctivitis, dry eye, eye pain.

Autoimmune: In extremely rare instances, systemic lupus erythematosus has been reported.

The incidence of drug-related adverse effects (volunteered and solicited) according to Acebutolol dose is shown below. (Data from 266 hypertensive patients treated for 3 months on a constant dose.)

Potential Adverse Events

In addition, certain adverse effects not listed above have been reported with other β-blocking agents and should also be considered as potential adverse effects of Acebutolol.

Central Nervous System: Reversible mental depression progressing to catatonia (an acute syndrome characterized by disorientation for time and place), short-term memory loss, emotional lability, slightly clouded sensorium, and decreased performance (neuropsychometrics).

Cardiovascular: Intensification of AV block (see CONTRAINDICATIONS).

Allergic: Erythematous rash, fever combined with aching and sore throat, laryngospasm, and respiratory distress.

Hematologic: Agranulocytosis, nonthrombocytopenic, and thrombocytopenic purpura.

Gastrointestinal: Mesenteric arterial thrombosis and ischemic colitis.

Miscellaneous: Reversible alopecia and Peyronie’s disease. The oculomucocutaneous syndrome associated with the β-blocker practolol has not been reported with Acebutolol during investigational use and extensive foreign clinical experience.

Pharmacologic Category

  • Antiarrhythmic Agent, Class II
  • Antihypertensive
  • Beta-Blocker With Intrinsic Sympathomimetic Activity

Onset of Action

1 to 2 hours

Time to Peak

2 to 4 hours

Special Populations Elderly

Bioavailability increased about 2-fold.

Dosing Renal Impairment

CrCl 25 to 49 mL/minute: Reduce dose by 50%.

CrCl <25 mL/minute: Reduce dose by 75%.

Other Requirements

  • Store acebutolol at room temperature 20° to 25°C (68° to 77°F). 
  • Keep tightly closed.
  • Protect from light.
  • Keep this and all medicines out of the reach of children.

 

Adverse Effects

>10%

Fatigue (11%)

1-10%

Dizziness (6%)

Headache (6%)

Constipation (4%)

Diarrhea (4%)

Dyspnea (4%)

Dyspepsia (4%)

Nausea (4%)

Flatulence (3%)

Insomnia (3%)

Abdominal pain (2%)

Bradycardia (2%)

Chest pain (2%)

Dysuria (2%)

Edema (2%)

Heart failure (2%)

Hypotension (2%)

Impotence (2%)

Myalgia (2%)

Pharyngitis (2%)

Pruritus (2%)

Rhinitis (2%)

Vomiting (2%)

Wheezing (2%)

<1%

Hepatotoxicity

SLE

Frequency Not Defined

Bronchospasm, depression, decreased exercise tolerance, Raynaud's phenomenon

May increase triglyceride levels and insulin resistance, and decrease HDL levels

What should i avoid while taking acebutolol (sectral)?

Acebutolol can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert.

Avoid drinking alcohol, which could increase drowsiness and dizziness while you are taking acebutolol.

Side effects

Sectral is well tolerated in properly selected patients. Most adverse reactions have been mild, not required discontinuation of therapy, and tended to decrease as duration of treatment increases. The following table shows the frequency of treatment-related side effects derived from controlled clinical trials in patients with hypertension, angina pectoris, and arrhythmia. These patients received Sectral, propranolol, or hydrochlorothiazide as monotherapy, or placebo.

TOTAL VOLUNTEERED AND ELICITED (U.S. STUDIES)

Body System/
Adverse Reaction
SECTRAL
(N=1002) %
Propranolol
(N=424) %
Hydrochloro- thiazide
(N=178) %
Placebo
(N=314) %
Cardiovascular
  Chest Pain 2 4 4 1
  Edema 2 2 4 1
Central Nervous System
  Depression 2 1 3 1
  Dizziness 6 7 12 2
  Fatigue 11 17 10 4
  Headache 6 9 13 4
  Insomnia 3 6 5 1
  Abnormal dreams 2 3 0 1
Dermatologic
  Rash 2 2 4 1
Gastrointestinal
  Constipation 4 2 7 0
  Diarrhea 4 5 5 1
  Dyspepsia 4 6 3 1
  Flatulence 3 4 7 1
  Nausea 4 6 3 0
Genitourinary
  Micturition (frequency) 3 1 9 < 1
Musculoskeletal
  Arthralgia 2 1 3 2
  Myalgia 2 1 4 0
Respiratory
  Cough 1 1 2 0
  Dyspnea 4 6 4 2
  Rhinitis 2 1 4 < 1
Special Senses
  Abnormal Vision 2 2 3 0

The following selected (potentially important) side effects were seen in up to 2% of Sectral patients:

Cardiovascular: hypotension, bradycardia, heart failure.

Central Nervous System: anxiety, hyper/hypoesthesia, impotence.

Dermatological: pruritus.

Gastrointestinal: vomiting, abdominal pain.

Genitourinary: dysuria, nocturia.

Liver and Biliary System: A small number of cases of liver abnormalities (increased SGOT, SGPT, LDH) have been reported in association with acebutolol therapy. In some cases increased bilirubin or alkaline phosphatase, fever, malaise, dark urine, anorexia, nausea, headache, and/or other symptoms have been reported. In some of the reported cases, the symptoms and signs were confirmed by rechallenge with acebutolol. The abnormalities were reversible upon cessation of acebutolol therapy.

Musculoskeletal: back pain, joint pain.

Respiratory: pharyngitis, wheezing.

Special Senses: conjunctivitis, dry eye, eye pain.

Autoimmune: In extremely rare instances, systemic lupus erythematosus has been reported.

The incidence of drug-related adverse effects (volunteered and solicited) according to Sectral dose is shown below. (Data from 266 hypertensive patients treated for 3 months on a constant dose.)

Body System 400 mg/day
(N=132)
800 mg/day
(N=63)
1200 mg/day
(N=71)
Cardiovascular 5% 2% 1%
Gastrointestinal 3% 3% 7%
Musculoskeletal 2% 3% 4%
Central Nervous System 9% 13% 17%
Respiratory 1% 5% 6%
Skin 1% 2% 1%
Special Senses 2% 2% 6%
Genitourinary 2% 3% 1%

Potential Adverse Events

In addition, certain adverse effects not listed above have been reported with other β-blocking agents and should also be considered as potential adverse effects of Sectral.

Central Nervous System: Reversible mental depression progressing to catatonia (an acute syndrome characterized by disorientation for time and place), short-term memory loss, emotional lability, slightly clouded sensorium, and decreased performance (neuropsychometrics).

Cardiovascular: Intensification of AV block (see CONTRAINDICATIONS).

Allergic: Erythematous rash, fever combined with aching and sore throat, laryngospasm, and respiratory distress.

Hematologic: Agranulocytosis, nonthrombocytopenic, and thrombocytopenic purpura.

Gastrointestinal: Mesenteric arterial thrombosis and ischemic colitis.

Miscellaneous: Reversible alopecia and Peyronie's disease. The oculomucocutaneous syndrome associated with the β-blocker practolol has not been reported with Sectral during investigational use and extensive foreign clinical experience.

Read the entire FDA prescribing information for Sectral (Acebutolol)

Read More »
  • Beta Blockers
  • High Blood Pressure (Hypertension) Medications
  • Treatment with Beta Blockers

In Summary

Commonly reported side effects of acebutolol include: fatigue. Other side effects include: constipation, diarrhea, dizziness, dyspepsia, and nausea. See below for a comprehensive list of adverse effects.

Other Comments

Patient advice:
-Caution patients against interruption of therapy without a physician's advice.
-When discontinuing this drug, advise the patient to minimize physical activity.
-Advise patients to consult a physician if they develop signs or symptoms suggestive of impending congestive heart failure or unexplained respiratory symptoms.
-Warn patients of possible severe hypertensive reactions from concomitant use of alpha adrenergic stimulants, such as common over-the-counter nasal decongestants.
-Warn diabetic patients of the possibility of masked hypoglycemia.

Acebutolol Levels and Effects while Breastfeeding

Summary of Use during Lactation

Because of the relatively extensive excretion of acebutolol and its active metabolite diacetolol into breastmilk and their extensive renal excretion, other agents may be preferred, especially while nursing a newborn or preterm infant.[1][2][3]

Drug Levels

The excretion of beta-adrenergic blocking drugs into breastmilk is largely determined by their protein binding. Those with low binding such as acebutolol (25%) are more extensively excreted into breastmilk.[4] Diacetolol is a renally excreted metabolite with equal beta-blocking activity that is more extensively excreted into breastmilk than acebutolol. In newborn infants, the apparent half-lives of acebutolol and diacetolol averaged 10.1 to 15.6 hours and 19.8 hours, respectively.[5][6] It is estimated that a fully breastfed infant would receive about 3.5% of the maternal weight-adjusted dosage of acebutolol.[7]

Maternal Levels.One mother with renal impairment taking 400 mg/day of acebutolol 3 days postpartum had milk levels of 1.5 mg/L of acebutolol and 2.6 mg/L of diacetolol at an unspecified time after the dose. Another mother with renal impairment taking 1200 mg/day of acebutolol 3 days postpartum had milk levels of 1.1 mg/L before a 400 mg dose and 4.1 mg/L 1.5 hours after the dose. Diacetolol milk levels were 6.3 and 6.6 mg/L, respectively, at the same times. A third mother with no renal impairment had milk acebutolol levels ranging from 0.5 to 0.7 mg/L and diacetolol levels of 1.2 to 1.8 at unspecified times while taking 200 to 600 mg/day of acebutolol from 6 to 9 days postpartum.[1]

Infant Levels. Relevant published information was not found as of the revision date.

Effects in Breastfed Infants

A study of mothers taking beta-blockers during nursing found a numerically, but not statistically significant increased number of adverse reactions in those taking any beta-blocker. Although the ages of infants were matched to control infants, the ages of the affected infants were not stated. One mother reported no adverse effects in her breastfed infant (age unstated) during acebutolol use.[8]

Hypotension, bradycardia, and transient tachypnea occurred in a newborn infant, probably because of acebutolol and diacetolol in breastmilk. The mother was taking 400 mg/day of acebutolol and had renal impairment. Two other neonates in this report who were breastfed had no adverse reactions noted.[1]

Effects on Lactation and Breastmilk

Relevant published information on the effects of beta-blockade or acebutolol during normal lactation was not found as of the revision date. A study in 6 patients with hyperprolactinemia and galactorrhea found no changes in serum prolactin levels following beta-adrenergic blockade with propranolol.[9]

Alternate Drugs to Consider

Propranolol, Labetalol, Metoprolol

References

1. Boutroy MJ, Bianchetti G, Dubruc C et al. To nurse when receiving acebutolol: is it dangerous for the neonate? Eur J Clin Pharmacol. 1986;30:737-9. PMID: 3770068

2. Chow T, Galvin J, McGovern B. Antiarrhythmic drug therapy in pregnancy and lactation. Am J Cardiol. 1998;82:58I-62I. PMID: 9737655

3. Hale TW. Medications in breastfeeding mothers of preterm infants. Pediatr Ann. 2003;32:337-47. PMID: 12774709

4. Riant P, Urien S, Albengres E et al. High plasma protein binding as a parameter in the selection of betablockers for lactating women. Biochem Pharmacol. 1986;35:4579-81. PMID: 2878668

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