Drugs Details

Drugs Info of Sectral
Drugs Details
  • Drugs Type  : Multum
  • Date : 30th Mar 2015 12:14 am
  • Brand Name : Sectral
  • Generic Name : acebutolol (Pronunciation: A se BUE toe lol)
Descriptions

Sectral (acebutolol HCl) 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 incapsule form for oral administration. Sectral (acebutolol) 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 22, FD&C Blue 1, FD&C Yellow 6, gelatin, povidone, starch, stearic acid, and titanium dioxide. The 200 mg dosage strength also contains D&C Red 28 and the 400 mg dosage strength also contains FD&C Red 40. Acebutolol HCl has the following structural formula:

 

View Enlarged Table

 

Acebutolol HCl 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.

 

What are the possible side effects of acebutolol (Sectral)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have any of these serious side effects:

  • slow or uneven heartbeats;
  • feeling light-headed, fainting;
  • feeling short of breath, even with mild exertion;
  • swelling of your ankles or feet;
  • nausea, stomach pain, low fever, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
  • depression; or
  • cold feeling...

Read All Potential Side Effects and See Pictures of Sectral »

What are the precautions when taking acebutolol (Sectral)?

Before taking acebutolol, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood circulation problems (such as Raynaud's disease, peripheral vascular disease), breathing problems (such as asthma, chronic bronchitis, emphysema), heart problems (such as heart failure, previous heart attack, heart rhythm problems), kidney problems, liver problems, mental/mood disorders (such as depression), a certain muscle disease (myasthenia gravis), overactive thyroid disease (hyperthyroidism), serious allergic...

Read All Potential Precautions of Sectral »

 

This monograph has been modified to include the generic and brand name in many instances.

Indications

Hypertension

Sectral (acebutolol) is indicated for the management of hypertension in adults. It may be used alone or in combination with other antihypertensiveagents, especially thiazide-type diuretics.

Ventricular Arrhythmias

Sectral (acebutolol) is 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.

Dosage Administration

Hypertension

The initial dosage of Sectral (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 Sectral (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.

How Supplied

Sectral® (acebutolol HCl) is available in the following dosage strengths:

200 mg, opaque purple and orange capsule marked "RP 700" and "Sectral® (acebutolol) 200"

NDC 67857-700-01, in bottles of 100 capsules.

400 mg, opaque brown and orange capsule marked "RP 701" and "Sectral® (acebutolol) 400"

NDC 67857-701-01, in bottles of 100 capsules.

Keep tightly closed

Store at controlled room temperature 20° to 25°C (68° to 77°F)

Protect from light

Dispense in a light-resistant, tight container

Use carton to protect contents from light

Distributed by: Reddy Pharmaceuticals, LLC Bridgewater, NJ 08807. Manufactured by: MOVA PHARMACEUTICAL CORPORATION., Manati, Puerto Rico 00674, USA. Revised July 2007. FDA Rev date: 9/6/2007

This monograph has been modified to include the generic and brand name in many instances.

 
 

Side Effects

Sectral (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 treatmentrelated side effects derived from controlled clinical trials in patients with hypertension, angina pectoris, andarrhythmia. These patients received Sectral (acebutolol) , propranolol, or hydrochlorothiazide as monotherapy, or placebo.

TOTAL VOLUNTEERED AND ELICITED (U.S. STUDIES)

 

BODY SYSTEM/
ADVERSE REACTION
SECTRAL PROPRANOLOL HYDROCHLOROTHIAZIDE PLACEBO
(N=1002)
%
(N=424)
%
(N=178)
%
(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 (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 erythematosushas been reported.

The incidence of drug-related adverse effects (volunteered and solicited) according to Sectral (acebutolol) dose is shown below. (Data from 266hypertensive 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% 1%
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-blockingagents and should also be considered as potential adverse effects of Sectral (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 (seeCONTRAINDICATIONS).

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 (acebutolol) during investigational use and extensive foreign clinical experience.

Read the Sectral (acebutolol) Side Effects Center for a complete guide to possible side effects

Learn More »
 
 
 

Interactions

Catecholamine-depleting drugs, such as reserpine, may have an additive effect when given with β-blocking agents. Patients treated with Sectral (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 a-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-adrenoceptor 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.

Read the Sectral Drug Interactions Center for a complete guide to possible interactions

Learn More »
 

This monograph has been modified to include the generic and brand name in many instances.

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, Sectral (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 Sectral (acebutolol) impair AV conduction. If cardiac failure persists, therapy with Sectral (acebutolol) should be withdrawn.

In Patients Without a History of Cardiac Failure

In patients with aortic or mitral valve disease or compromised left ventricularfunction, 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, Sectral (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 Sectral (acebutolol) is planned, the patient should be carefully observed, and should be advised to limit physical activity to a minimum while Sectral (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 anginapectoris 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 insufficiency in patients withperipheral 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 Disease

PATIENTS WITH BRONCHOSPASTIC DISEASE SHOULD, IN GENERAL, NOT RECEIVE A β-BLOCKER. Because of its relative β1-selectivity, however, low doses of Sectral (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 Sectral (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.

Anesthesia and Major Surgery

The necessity, or desirability, of withdrawal of aβ-blocking therapy prior to major surgery is controversial. β-adrenergic receptor blockade impairs the ability of the heart to respond to β-adrenergically mediated reflex stimuli. While this might be of benefit in preventing arrhythmic response, the risk of excessive myocardial depression during general anesthesia may be enhanced and difficulty in restarting and maintaining the heart beat has been reported with beta-blockers. If treatment is continued, particular care should be taken when using anesthetic agents which depress the myocardium, such as ether, cyclopropane, and trichlorethylene, and it is prudent to use the lowest possible dose of Sectral (acebutolol) . Sectral (acebutolol) , like other β-blockers, is a competitive inhibitor of β-receptor agonists, and its effect on the heart can be reversed by cautious administration of such agents (e.g., dobutamine or isoproterenol — see OVERDOSAGE). Manifestations of excessive vagal tone (e.g., profound bradycardia, hypotension) may be corrected with atropine 1 to 3 mg IV in divided doses.

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 Sectral (acebutolol) therapy is to be withdrawn should be monitored closely.

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 challenge, 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. Sectral (acebutolol) should be used cautiously in patients with impaired hepatic function.

Sectral (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 Sectral (acebutolol) and its metabolite are approximately doubled in this age group.

Clinical Laboratory Findings

Sectral® (acebutolol) , like other β-blockers, has been associated with the development of antinuclear antibodies (ANA). In prospective clinical trials, patients receiving Sectral (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.

Carcinogenesis, 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 Sectral (acebutolol) . Diacetolol, the major metabolite of Sectral (acebutolol) in man, was without carcinogenic potential in rats when tested at doses as high as 1800 mg/kg/day. Sectral (acebutolol) and diacetolol were also shown to be devoid of mutagenic potential in the Ames Test. Sectral (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 Sectral (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, andmortality. 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 postimplantation 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, Sectral (acebutolol) should be used during pregnancy only if the potential benefit justifies the risk to the fetus.

Non Teratogenic Effects

Studies in humans have shown that both acebutolol and diacetolol cross theplacenta. 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 Sectral (acebutolol) on labor and delivery in pregnant women is unknown. Studies in animals have not shown any effect of Sectral (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 Sectral (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 — Pharmacokinetics and Metabolism), presumably because of agerelated 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 ADMINISTRATION — Use in Older Patients).

This monograph has been modified to include the generic and brand name in many instances.

 
 

OverDose

No specific information on emergency treatment of overdosage is available for Sectral (acebutolol) . However, overdosage with other β-blocking agents has been accompanied by extreme bradycardia, advanced atrioventricularblock, intraventricular conduction defects, hypotension, severe congestive heart failure, seizures, and in susceptible patients, bronchospasm andhypoglycemia. Although specific information on the emergency treatment of Sectral (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, levarterenol, dopamine, or dobutamine) with frequent monitoring of blood pressure and pulse rate.
  4. Bronchospasm: A theophylline derivative, such as aminophylline and/orparenteral 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 (acebutolol) is dialyzable.

ContrainDications

Sectral (acebutolol) is contraindicated in: 1) persistently severe bradycardia; 2) second- and third-degree heart block; 3) overt cardiac failure; and 4) cardiogenic shock. (See WARNINGS.)

This monograph has been modified to include the generic and brand name in many instances.

Clinical Pharamacology

Sectral (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, Sectral (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 Sectral (acebutolol) has been demonstrated in catecholamine-depleted rats by tachycardia induced byintravenous administration of this agent. A membrane-stabilizing effect has been detected in animals, but only with high concentrations of Sectral (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 Sectral (acebutolol) has also been demonstrated on the basis of the following vascular and bronchial effects: Vascular Effects: Sectral (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 beta2agonist, bronchodilating effects, than nonselective agents like propranolol but more than atenolol.

ISA has been observed with Sectral (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 Sectral (acebutolol) induced no significant alteration in the blood lipid profile.

Sectral (acebutolol) has been shown to delay AV conduction time and to increase the refractoriness of the AV node without significantly affectingsinus node recovery time, atrial refractory period, or the HV conduction time. The membrane-stabilizing effect of Sectral (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 Sectral (acebutolol) administration with maximal effects occurring between 3 and 8 hours postdosing in normal volunteers. Sectral (acebutolol) has demonstrated a significant effect on exerciseinduced 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 (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 Sectral (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 Sectral (acebutolol) was compared with placebo, propranolol, and quinidine. Compared with placebo, Sectral (acebutolol) significantly reduced mean total ventricular ectopic beats (VEB), paired VEB, multiform VEB, R-on-T beats, and ventricular tachycardia (VT). Both Sectral (acebutolol) and propranolol significantly reduced mean total and paired VEB and VT. Sectral (acebutolol) and quinidine significantly reduced resting total and complex VEB; the antiarrhythmic efficacy of Sectral (acebutolol) was also observed during exercise.

Pharmacokinetics and Metabolism

Sectral (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 Sectral (acebutolol) and in cats is more cardioselective than Sectral (acebutolol) ; therefore, this first-pass phenomenon does notattenuate the therapeutic effect of Sectral (acebutolol) . Food intake does not have a significant effect on the area under the plasma concentration-time curve (AUC) of Sectral (acebutolol) although the rate of absorption and peak concentration decreased slightly.

The plasma elimination half-life of Sectral (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 Sectral (acebutolol) is 2.5 hours and for diacetolol, after oral administration of Sectral (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.

Sectral (acebutolol) has a low binding affinity for plasma proteins (about 26%). Sectral (acebutolol) and its metabolite, diacetolol, are relatively hydrophilic and, therefore, only minimal quantities have been detected in thecerebrospinal 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 (acebutolol) administration. The kinetics of Sectral (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 Sectral (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). Sectral (acebutolol) and its major metabolite are dialyzable.

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

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

This monograph has been modified to include the generic and brand name in many instances.

Patient Information

Patients, especially those with evidence of coronary artery disease, should be warned against interruption or discontinuation of Sectral (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 respiratorysymptoms.

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

This monograph has been modified to include the generic and brand name in many instances.

Consumer Overview Uses

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

 

ACEBUTOLOL - ORAL

 

(A-se-BUE-toe-lol)

 

COMMON BRAND NAME(S): Sectral

 

WARNING: Do not stop taking this medication without consulting your doctor. Some conditions may become worse when you suddenly stop this drug. Some people who have suddenly stopped taking similar drugs have had chest pain, heart attack, and irregular heartbeat. If your doctor decides you should no longer use this drug, he or she may direct you to gradually decrease your dose over 1 to 2 weeks.

When gradually stopping this medication, it is recommended that you temporarily limit physical activity to decrease strain on the heart. Get medical help right away if you develop chest pain/tightness/pressure, chest pain spreading to the jaw/neck/arm, unusual sweating, trouble breathing, or fast/irregular heartbeat.

 

USES: Acebutolol is used to treat high blood pressure and irregular heartbeat (arrhythmia). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Treating irregular heartbeat helps the heart work better and with less strain. Irregular heartbeats can be serious and may sometimes even lead to a heart attack.

This medication belongs to a class of drugs known as beta blockers. It works by blocking the action of certain natural substances in your body, such as epinephrine, on the heart and blood vessels. This effect lowers heart rate, blood pressure, and strain on the heart.

 

OTHER USES: This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.

This medication may also be used to prevent chest pain (angina), heart failure, and to improve survival after a heart attack.

 

HOW TO USE: See also Warning section.

Take this medication by mouth with or without food as directed by your doctor, usually once or twice daily. The dosage is based on your medical condition and response to treatment.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time(s) each day.

For the treatment of high blood pressure, it may take several weeks before you get the full benefit of this drug. It is important to continue taking this medication even if you feel well. Most people with high blood pressure do not feel sick.

Tell your doctor if your condition does not improve or if it worsens (for example, if your routine blood pressure readings remain high or increase).

Consumer Overview Side Effect

SIDE EFFECTS: See also Warning and Precautions sections.

Tiredness, dizziness, lightheadedness, nausea, upset stomach, slow heartbeat, or trouble sleeping may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.

This drug may reduce blood flow to your hands and feet, causing them to feel cold. Smoking may worsen this effect. Dress warmly and avoid tobacco use.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: symptoms of asthma (for example, feelings of tightness in the chest, shortness of breath, cough, wheezing), blue fingers/toes, fainting, very slow heartbeat, new or worsening symptoms of heart failure (such as swelling ankles/feet, severe tiredness, shortness of breath, unexplained/sudden weight gain), mental/mood changes (such as confusion, depression, memory problems), vision changes, symptoms of liver disease (such as dark urine, persistent nausea, vomiting, stomach/abdominal pain, yellowing eyes/skin).

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

 

Read the Sectral (acebutolol) Side Effects Center for a complete guide to possible side effects

Learn More »
 

PRECAUTIONS: Before taking acebutolol, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood circulation problems (such as Raynaud's disease, peripheral vascular disease), breathing problems (such as asthma, chronic bronchitis, emphysema), heart problems (such as heart failure, previous heart attack, heart rhythm problems), kidney problems, liver problems, mental/mood disorders (such as depression), a certain muscle disease (myasthenia gravis), overactive thyroid disease (hyperthyroidism), serious allergic reactions, including those needing treatment with epinephrine.

This drug may make you dizzy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Limit alcoholic beverages.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

If you have diabetes, this product may prevent the fast/pounding heartbeat you would usually feel when your blood sugar level falls too low (hypoglycemia). Other symptoms of low blood sugar level, such as dizziness and sweating, are unaffected by this drug. This product may also make it harder to control your blood sugar levels. Check your blood sugar levels regularly as directed by your doctor. Tell your doctor right away if you have symptoms of high blood sugar such as increased thirst/urination. Your doctor may need to adjust your diabetes medication, exercise program, or diet.

During pregnancy, this medication should be used only when clearly needed. Babies born to mothers taking this drug during pregnancy may have a low birth weight and require monitoring for problems such as low blood pressure and slow heartbeat. Discuss the risks and benefits with your doctor.

This drug passes into breast milk. Consult your doctor before breast-feeding.

Consumer Overview Missed Dose

DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.

A product that may interact with this drug is: fingolimod.

Check the labels on all your medicines (such as cough-and-cold products, diet aids, or NSAIDs such as ibuprofen, naproxen) because they may contain ingredients that could increase your blood pressure or heart rate. Ask your pharmacist for more details.

 

OVERDOSE: If overdose is suspected, contact a poison control center or emergency room immediately. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: unusually slow heartbeat, fainting, severe weakness.

 

NOTES: Do not share this medication with others.

Lifestyle changes such as stress reduction programs, exercise, and dietary changes may increase the effectiveness of this medicine. Talk to your doctor or pharmacist about lifestyle changes that might benefit you.

Check your blood pressure and pulse (heart rate) regularly while taking this medication. Learn how to check your blood pressure and pulse at home, and share the results with your doctor.

 

MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

 

STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

 

MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

 

Information last revised April 2013. Copyright(c) 2013 First Databank, Inc.

Patient Detailed Side Effect

Brand Names: Sectral

Generic Name: acebutolol (Pronunciation: A se BUE toe lol)

  • What is acebutolol (Sectral)?
  • What are the possible side effects of acebutolol (Sectral)?
  • What is the most important information I should know about acebutolol (Sectral)?
  • What should I discuss with my healthcare provider before taking acebutolol (Sectral)?
  • How should I take acebutolol (Sectral)?
  • What happens if I miss a dose (Sectral)?
  • What happens if I overdose (Sectral)?
  • What should I avoid while taking acebutolol (Sectral)?
  • What other drugs will affect acebutolol (Sectral)?
  • Where can I get more information?

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.

Acebutolol 200 mg-AMN

capsule, orange/purple, imprinted with AMNEAL, 669

What are the possible side effects of acebutolol (Sectral)?

 

Get emergency medical help if you have any of thesesigns of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have any of these serious side effects:

  • slow or uneven heartbeats;
  • feeling light-headed, fainting;
  • feeling short of breath, even with mild exertion;
  • swelling of your ankles or feet;
  • nausea, stomach pain, low fever, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
  • depression; or
  • cold feeling in your hands and feet.

Less serious side effects may include:

  • decreased sex drive, impotence, or difficulty having an orgasm;
  • sleep problems (insomnia);
  • tired feeling; or
  • anxiety, nervousness.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the Sectral (acebutolol) Side Effects Center for a complete guide to possible side effects

Learn More »
 

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

 

Do not stop taking acebutolol without first talking to your doctor. Stopping suddenly may make your condition worse.

If you need to have any type of surgery, you may need to temporarily stop using acebutolol. Be sure the surgeon knows ahead of time that you are using acebutolol.

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.

Acebutolol is only part of a complete program of treatment for hypertension that may also include diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely if you are being treated for hypertension.

Keep using this medicine as directed, even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.

Side Effects Centers
  • Sectral

Patient Detailed How Take

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.

How should I take acebutolol (Sectral)?

 

Take acebutolol exactly as it was prescribed for you. Do not take the medication in larger amounts or for longer than recommended by your doctor. Follow the directions on your prescription label.

Take this medication with a full glass of water.

Take acebutolol at the same time every day.

Do not skip doses or stop taking acebutolol without first talking to your doctor. Stopping suddenly may make your condition worse.

To be sure this medication is helping your condition, your blood pressure will need to be checked on a regular basis. It is important that you not miss any scheduled visits to your doctor.

If you need to have any type of surgery, tell the surgeon that you are using acebutolol. You may need to briefly stop using acebutolol before having surgery.

Acebutolol is only part of a complete program of treatment for hypertension that may also include diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely if you are being treated for hypertension.

Keep using this medicine as directed, even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.

Store acebutolol at room temperature away from moisture and heat.

Side Effects Centers
  • Sectral

Patient Detailed Avoid Taking

What happens if I miss a dose (Sectral)?

 

Take the missed dose as soon as you remember. If your next dose is less than 4 hours away, skip the missed dose and take the medicine at the next regularly scheduled time. Do not take extra medicine to make up the missed dose.

What happens if I overdose (Sectral)?

 

Seek emergency medical attention if you think you have used too much of this medicine.

Overdose symptoms may include uneven heartbeats, shortness of breath, bluish-colored fingernails, dizziness, weakness, fainting, or seizure (convulsions).

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.

What other drugs will affect acebutolol (Sectral)?

 

Before taking acebutolol, tell your doctor if you are using:

  • allergy treatments (or if you are undergoing allergy skin-testing);
  • clonidine (Catapres);
  • guanabenz (Wytensin);
  • an MAO inhibitor such as isocarboxazid (Marplan), tranylcypromine (Parnate), phenelzine (Nardil), or selegiline (Eldepryl, Emsam);
  • a diabetes medication such as insulin, glyburide (Diabeta, Micronase, Glynase), glipizide (Glucotrol), chlorpropamide (Diabinese), or metformin (Glucophage);
  • a heart medication such as nifedipine (Procardia, Adalat), reserpine (Serpasil), verapamil (Calan, Verelan, Isoptin), diltiazem (Cartia, Cardizem);
  • medicine for asthma or other breathing disorders, such as albuterol (Ventolin, Proventil), metaproterenol (Alupent), pirbuterol (Maxair), terbutaline (Brethaire, Brethine, Bricanyl), and theophylline (Theo-Dur, Theolair); or
  • cold medicines, stimulant medicines, or diet pills.

This list is not complete and there may be other drugs that can interact with acebutolol. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.

Where can I get more information?

 

Your pharmacist can provide more information about acebutolol.


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.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2013 Cerner Multum, Inc. Version: 8.05. Revision date: 12/15/2010.

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