Acebutolol

Brand names: Sectral®

Chemical formula:

Drug Forms:
• Acebutolol capsules (below)
• Acebutolol Hydrochloride Oral capsule

Español:
• Cápsulas de acebutolol
• Clorhidrato de acebutolol, Cápsula oral

Acebutolol capsules

What are acebutolol capsules?

ACEBUTOLOL (Sectral®) belongs to a group of medicines called beta-blockers. Beta-blockers reduce the workload on the heart and help it to beat more regularly. Acebutolol is used to control high blood pressure (hypertension), and to treat or prevent certain heart rhythm problems (ventricular arrhythmias). Acebutolol does not cure high blood pressure. Generic acebutolol capsules are available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• asthma or bronchitis
• blood vessel disease (such as Raynaud's disease)
• depression
• diabetes
• emphysema
• history of heart attack, or heart disease
• kidney disease
• liver disease
• muscle weakness or disease
• psoriasis
• thyroid disease
• an unusual or allergic reaction to acebutolol, other beta-blockers, medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Take acebutolol capsules by mouth. Follow the directions on the prescription label. Swallow the capsules whole with a drink of water. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on your prescriber's advice.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What if I miss a dose?

What drug(s) may interact with acebutolol?

• cimetidine
• cocaine
• hawthorn
• medicines for colds and breathing difficulties
• medicines for diabetes
• medicines for high blood pressure
• medicines to control heart rhythm
• monoamine oxidase inhibitors (Azilect®, Eldepryl®, Emsam®, Marplan®, Nardil®, Parnate®, Zelapar™)
• water pills

Tell your prescriber or health care professional about all other medicines you are taking, including nonprescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking acebutolol?

Check your heart rate and blood pressure regularly while you are taking acebutolol. Ask your prescriber or health care professional what your heart rate and blood pressure should be, and when you should contact him or her.

Do not stop taking this medicine suddenly. This could lead to serious heart-related effects.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that requires mental alertness until you know how acebutolol affects you. To reduce the risk of dizzy or fainting spells, do not sit or stand up quickly. Alcohol can make you more drowsy, increase flushing, and cause rapid heartbeats. Therefore, it is best to avoid alcoholic drinks.

Acebutolol can affect blood sugar levels. If you are diabetic, check with your prescriber or health care professional before you change your diet or the dose of your diabetic medicine.

If you are going to have surgery, tell your prescriber or health care professional that you are taking acebutolol.

What side effects may I notice from taking acebutolol?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• changes in vision
• chest pain
• cold, tingling, or numb hands or feet
• confusion
• difficulty breathing, wheezing
• dizziness or fainting spells
• irregular heartbeat
• muscle aches and pains
• skin rash
• slow heart rate (less than recommended by your prescriber or health care professional)
• sweating
• swollen legs or ankles
• tremor, shakes
• vomiting

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• anxiety
• depression, nightmares
• diarrhea
• difficulty sleeping
• dry itching skin
• dry or burning eyes
• headache
• nausea
• unusual tiredness

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

The noun has one meaning:

Meaning #1: an oral beta blocker (trade name Sectral) used in treating hypertension
  Synonym: Sectral

Acebutolol
Systematic (IUPAC) name
(RS)-N-{3-acetyl-4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}butanamide
Identifiers
CAS number	37517-30-9
ATC code	C07AB04
PubChem	1978
ChemSpider	1901
Chemical data
Formula	C18H28N2O4
Mol. mass	336.426 g/mol
SMILES	eMolecules & PubChem
Physical data
Melt. point	121 °C (250 °F)
Pharmacokinetic data
Bioavailability	40% (range 35 to 50%)
Metabolism	Hepatic
Half life	3-4 hours (parent drug) 8-13 hours (active metabolite)
Excretion	Renal: 30% Biliary: 60%
Therapeutic considerations
Licence data	US FDA:link
Pregnancy cat.	C(AU) B(US)
Legal status	℞ Prescription only
Routes	oral, iv
Y(what is this?)  (verify)

Acebutolol (trade names Sectral, Prent) is a beta blocker for the treatment of hypertension and arrhythmias.

Contents 1 Pharmacology 2 Pharmacokinetics 3 Indications 4 Contraindications 5 Contraindications and Precautions 6 Side effects 7 Dosage 8 External links

Pharmacology

Acebutolol is a cardioselective beta blocker with ISA (Intrinsic Sympathomimetic Activity, see article on Pindolol). It is therefore more suitable than non cardioselective beta blockers, if a patient with Asthma bronchiale or chronic obstructive pulmonary disease (COPD) needs treatment with a beta blocker. In doses lower than 800mg daily its constricting effects on the bronchial system and smooth muscle vessels are only 10% to 30% of those observed under Propranolol treatment, but there is experimental evidence that the cardioselective properties diminish at doses of 800mg/day or more.

The drug has lipophilic properties, and therefore crosses the Blood-Brain Barrier. Acebutolol has no negative impact on serum lipids (cholesterol and triglycerides). No HDL decrease has been observed. In this regard, it is unlike many other beta blockers which have this unfavourable property.

The drug works in hypertensive patients with high, normal, or low renin plasma concentrations, although acebutolol may be more efficient in patients with high or normal renin plasma concentrations. In clinically relevant concentrations, a membrane-stabilizing effect does not appear to play an important role.

Pharmacokinetics

Acebutolol is well absorbed from the GI tract, but undergoes substantial first-pass-metabolization, leading to a bioavailability of only 35% to 50%. Peak plasma levels of acebutolol are reached within 2 to 2.5 hours after oral dosing. Peak levels of the main active metabolite, diacetolol, are reached after 4 hours. Acebutolol has a halflife of 3 to 4 hours, and diacetolol a halflife of 8 to 13 hours.

Acebutolol undergoes extensive hepatic metabolization resulting in the desbutyl amine acetolol which is readily converted into diacetolol. Diacetolol is as active as acebutolol (equipotency) and appears to have the same pharmacologic profile. Geriatric patients tend to have higher peak plasma levels of both acebutolol and diacetolol and a slightly prolonged excretion. Excretion is substantially prolonged in patients with renal impairment, and so a dose reduction may be needed. Liver cirrhosis does not seem to alter the pharmacokinetic profile of the parent drug and metabolite.

Indications

• hypertension
• ventricular and atrial cardiac arrhythmia
• acute myocardial infarction in high-risk patients
• Smith-Magenis syndrome

Contraindications

• Stable or Unstable Angina (due to its partial agonist or ISA activity)

Contraindications and Precautions

Further information: Propranolol

Acebutolol may not be suitable in patients with Asthma bronchiale or COPD due to its bronchoconstricting (β2 antagonistic) effects.

Side effects

Further information: Propranolol

The development of anti-nuclear antibodies (ANA) has been found in 10 to 30% of patients under treatment with acebutolol. A systemic disease with arthralgic pain and myalgias has been observed in 1%. A lupus erythematosus-like syndrome with skin rash and multiforme organ involvement is even less frequent. The incidence of both ANA and symptomatic disease under acebutolol is higher than under Propranolol. Female patients are more likely to develop these symptoms than male patients. Some few cases of hepatotoxicity with increased liver enzymes (ALT, AST) have been seen. Altogether, 5 to 6% of all patients treated have to discontinue acebutolol due to intolerable side effects. When possible, the treatment should be discontinued gradually in order to avoid a withdrawal syndrome with increased frequency of angina and even precipitation of myocardial infarction.

Dosage

The daily dose is 200mg - 1,200mg in a single dose or in 2 divided doses as dictated by the severity of the condition to be treated. Treatment should be initiated with low doses, and the dose should be increased cautiously according to the response of the patient. Acebutolol is particularly suitable for antihypertensive combination treatment with diuretics, if acebutolol alone proves insufficient. In some countries injectable forms for i.v.-injection with 25mg acebutolol exist, but these are only for cases of emergency under strict clinical monitoring. The initial dose is 12.5 to 25mg, but additional doses may be increased to 75 to 100mg, if needed. If further treatment is required, it should be oral.

External links

• AHFS Database

v • d • e Adrenergics Receptor Ligands α α1 Agonists: Amidephrine • Cirazoline • Dopamine • Epinephrine (Adrenaline) • Etilefrine • Isoprenaline • Levonordefrin • Metaraminol • Methoxamine • Methyldopa • Norepinephrine (Noradrenaline) • Oxymetazoline • Phenylephrine Antagonists: Alfuzosin • Arotinolol • Carvedilol • Doxazosin • Indoramin • L-765,314 • Labetalol • Moxisylyte • Nantenine • Phentolamine • Phenoxybenzamine • Prazosin • Silodosin • Tamsulosin • Terazosin • Tolazoline • Trimazosin • Urapidil α2 Agonists: (R)-3-Nitrobiphenyline • 4-NEMD • Amitraz • Apraclonidine • Brimonidine • Clonidine • Detomidine • Dexmedetomidine • Dopamine • Epinephrine (Adrenaline) • Etilefrine • Guanabenz • Guanfacine • Guanethidine • Guanoxabenz • Levonordefrin • Lofexidine • Medetomidine • Methyldopa • Norepinephrine (Noradrenaline) • Octopamine • Romifidine • Tizanidine • Tolonidine • Xylazine • Xylometazoline Antagonists: 1-PP • Atipamezole • BRL-44408 • Buspirone • Cirazoline • Efaroxan • Gepirone • Idazoxan • Ipsapirone • Mianserin • Mirtazapine • NAN-190 • Phentolamine • Phenoxybenzamine • Rauwolscine • SB-269,970 • Setiptiline • Spiroxatrine • Tandospirone • Tolazoline • Yohimbine α? Agonists: Anisodamine • Ephedrine • Ergotamine • Indanidine • Mephentermine • Midodrine • Mivazerol • Naphazoline • Phenylpropanolamine • Pseudoephedrine • Rilmenidine • Synephrine • Talipexole • Tetrahydrozoline β β1 Agonists: Denopamine • Dobutamine • Dopamine • Epinephrine (Adrenaline) • Etilefrine • Levonordefrin • Methyldopa • Norepinephrine (Noradrenaline) Antagonists: Acebutolol • Alprenolol • Amosulalol • Arotinolol • Atenolol • Bupranolol • Carvedilol • Celiprolol • Betaxolol • Bisoprolol • Dichloroisoprenaline • Esmolol • Labetalol • Metipranolol • Metoprolol • Nadolol • Nebivolol • Oxprenolol • Penbutolol • Pindolol • Practolol • Pronethalol • Propranolol • Sotalol • Tertatolol • Timolol • Tilisolol • Xamoterol β2 Agonists: Arformoterol • Bambuterol • Bitolterol • Carbuterol • Clenbuterol • Dopamine • Dopexamine • Epinephrine (Adrenaline) • Etilefrine • Fenoterol • Formoterol • Hexoprenaline • Indacaterol • Levonordefrin • Levosalbutamol • Methyldopa • Norepinephrine (Noradrenaline) • Orciprenaline • Pirbuterol • Procaterol • Reproterol • Rimiterol • Ritodrine • Salbutamol (Albuterol) • Salmeterol • Terbutaline • Tulobuterol Antagonists: Alprenolol • Amosulalol • Arotinolol • Bupranolol • Butaxamine • Carvedilol • Dichloroisoprenaline • ICI 118551 • Labetalol • Metipranolol • Nadolol • Oxprenolol • Penbutolol • Pindolol • Pronethalol • Propranolol • Sotalol • Tertatolol • Timolol • Tilisolol β3 Agonists: Amibegron • Arotinolol • Dopamine • Epinephrine (Adrenaline) • Etilefrine • Labetalol • Levonordefrin • Methyldopa • Norepinephrine (Noradrenaline) • Solabegron Antagonists: Carvedilol • SR 59230A β? Agonists: Arbutamine • BAAM • Befunolol • Broxaterol • Buphenine • Cimaterol • Ephedrine • Higenamine • Isoetarine • Isoxsuprine • Mabuterol • Methoxyphenamine • Oxyfedrine • Prenalterol • Pseudoephedrine • Ractopamine • Tretoquinol • Zilpaterol • Zinterol Reuptake Inhibitors Plasmalemmal NET Inhibitors Norepinephrine Reuptake Inhibitors: Atomoxetine (Tomoxetine) • Ciclazindol • Mazindol • Nisoxetine • Reboxetine • Tandamine • Tapentadol • Viloxazine; Norepinephrine-Dopamine Reuptake Inhibitors: Amineptine • Bupropion (Amfebutamone) • Fencamine • Fencamfamine • Lefetamine • LR-5182 • Manifaxine • Methylphenidate • Nomifensine • O-2172 • Radafaxine; Serotonin-Norepinephrine Reuptake Inhibitors: Bicifadine • Desvenlafaxine • Duloxetine • Milnacipran • Sibutramine • Tramadol • Venlafaxine; Serotonin-Norepinephrine-Dopamine Reuptake Inhibitors: Brasofensine • Diclofensine • DOV-102,677 • DOV-21,947 • DOV-216,303 • JNJ-7925476 • JZ-IV-10 • Methylnaphthidate • Naphyrone • NS-2359 • PRC200-SS • SEP-225,289 • SEP-227,162 • Tesofensine; Tricyclic Antidepressants: Amitriptyline • Butriptyline • Cianopramine • Clomipramine • Desipramine • Dosulepin • Doxepin • Imipramine • Lofepramine • Nortriptyline • Protriptyline • Trimipramine; Tetracyclic Antidepressants: Amoxapine • Maprotiline • Mianserin • Oxaprotiline; Others: Cocaine • Nefazodone • Nefopam • Ziprasidone TRPC6 Activators Adhyperforin • Hyperforin Vesicular VMAT Inhibitors Ibogaine • Reserpine • Tetrabenazine Releasing Agents Oxazolines: 4-Methylaminorex (4-MAR, 4-MAX) • Aminorex • Clominorex • Cyclazodone • Fenozolone • Fluminorex • Pemoline • Thozalinone; Phenethylamines (also Amphetamines, Cathinones, Phentermines, etc): 2-Hydroxyphenethylamine (2-OH-PEA) • 4-Methylamphetamine (4-MA) • 4-Methylmethamphetamine (4-MMA) • α-Ethylphenethylamine (α-Et-PEA) • Alfetamine • Amphetamine (Dextroamphetamine, Levoamphetamine) • Amphetaminil • Amfepentorex • β-Methylphenethylamine (β-Me-PEA) • Benzodioxolylbutanamine (BDB) • Benzodioxolylhydroxybutanamine (BOH) • Benzphetamine • Buphedrone • Butylone • Cathine • Cathinone • Clobenzorex • Clortermine • Diethylcathinone (Diethylpropion, Amfepramone) • Dibutylone • Dimethoxyamphetamine (DMA) • Dimethoxymethamphetamine (DMMA) • Dimethylamphetamine • Dimethylcathinone (Dimethylpropion, Metamfepramone) • Ephedrine (EPH) • Ethcathinone (Ethylpropion) • Ethylamphetamine • Ethylbenzodioxolylbutanamine (EBDB) • Ethylone • Fenethylline • Fenproporex • Flephedrone • Fludorex • Furfenorex • Hordenine • Indanorex • Indanylamphetamine (IAP) • Lisdexamfetamine • Lophophine (Homomyristicylamine) • Mefenorex • Mephedrone • Mephentermine • Methamphetamine (Desoxyephedrine, Methedrine; Dextromethamphetamine, Levomethamphetamine) • Methcathinone (Methylpropion) • Methedrone • Methoxymethylenedioxyamphetamine (MMDA) • Methoxymethylenedioxymethamphetamine (MMDMA) • Methylbenzodioxolylbutanamine (MBDB) • Methylenedioxyamphetamine (MDA; Tenamfetamine) • Methylenedioxyethylamphetamine (MDEA) • Methylenedioxyhydroxyamphetamine (MDOH) • Methylenedioxymethamphetamine (MDMA) • Methylenedioxymethylphenethylamine (MDMPEA; Homarylamine) • Methylenedioxyphenethylamine (MDPEA; Homopiperonylamine) • Methylone • Naphthylamphetamine (NAP) • Ortetamine • Oxaflozane • Parabromoamphetamine (PBA) • Parachloroamphetamine (PCA) • Parafluoroamphetamine (PFA) • Parafluoromethamphetamine (PFMA) • Parahydroxyamphetamine (PHA) • Paraiodoamphetamine (PIA) • Paramethoxyamphetamine (PMA) • Paramethoxyethylamphetamine (PMEA) • Paramethoxymethamphetamine (PMMA) • Paredrine (Norpholedrine, Oxamphetamine) • Phendimetrazine • Phenethylamine (PEA) • Phenmetrazine • Pholedrine • Phenpentermine • Phenpromethamine • Phentermine • Phenylpropanolamine (PPA) • Propylamphetamine • Pseudoephedrine (PSE) • Tiflorex (Flutiorex) • Tyramine (TRA) • Xylopropamine • Zylofuramine; Piperazines: 2,5-Dimethoxy-4-bromobenzylpiperazine (2C-B-BZP) • Benzylpiperazine (BZP) • Methoxyphenylpiperazine (MeOPP; Paraperazine) • Methylbenzylpiperazine (MBZP) • Methylenedioxybenzylpiperazine (MDBZP; Piperonylpiperazine) • Parafluorophenylpiperazine (pFPP; Fluoperazine); Others: 2-Aminoindane (2-AI) • 2-Aminotetralin (2-AT) • 2-Benzylpiperidine (2-BP) • 4-Benzylpiperidine (4-BP) • Clofenciclan • Cyclopentamine • Cypenamine • Cyprodenate • Feprosidnine • Gilutensin • Heptaminol • Hexacyclonate • Isometheptene • Methylhexanamine • Octodrine • Phthalimidopropiophenone • Propylhexedrine (PHX) • Tuaminoheptane (Tuamine) Enzyme Inhibitors Anabolism PAH Inhibitors 3,4-Dihydroxystyrene TH Inhibitors 3-Iodotyrosine • Aquayamycin • Bulbocapnine • Metirosine • Oudenone AAAD Inhibitors Benserazide • Carbidopa DBH Inhibitors Disulfiram • Nepicastat • Tropolone PNMT Inhibitors CGS-19281A • SKF-64139 • SKF-7698 Catabolism MAO Inhibitors Nonselective: Iproclozide • Iproniazid • Isocarboxazid • Nialamide • Phenelzine • Pheniprazine • Tranylcypromine; MAO-A Selective: Befloxatone • Brofaromine • Cimoxatone • Clorgiline • Harmala Alkaloids • Minaprine • Moclobemide • Pirlindole • Toloxatone • Tyrima; MAO-B Selective: Lazabemide • Pargyline • Rasagiline • Selegiline * Note that MAO-B inhibitors also influence norepinephrine/epinephrine levels since they inhibit the breakdown of their precursor dopamine. COMT Inhibitors Entacapone • Tolcapone Others Precursors L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) → Dopamine • L-DOPS (Droxidopa) Cofactors Ferrous Iron (Fe2+) • S-Adenosyl-L-Methionine • Vitamin B3 (Niacin, Nicotinamide → NADPH) • Vitamin B6 (Pyridoxine, Pyridoxamine, Pyridoxal → Pyridoxal Phosphate) • Vitamin B9 (Folic Acid → Tetrahydrofolic Acid) • Vitamin C (Ascorbic Acid) • Zinc (Zn2+) Others Activity Enhancers: Benzofuranylpropylaminopentane (BPAP) • Phenylpropylaminopentane (PPAP); Release Blockers: Bretylium • Guanethidine

This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)