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Identification
NameAcebutolol
Accession NumberDB01193  (APRD00772)
TypeSmall Molecule
GroupsApproved
Description

A cardioselective beta-adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm as well as weak inherent sympathomimetic action. [PubChem]

Structure
Thumb
Synonyms
(+-)-Acebutolol
(±)-acebutolol
3'-acetyl-4'-(2-hydroxy-3-(isopropylamino)propoxy)butyranilide
5'-butyramido-2'-(2-hydroxy-3-isopropylaminopropoxy)acetophenone
Acebutolol
Acebutololum
Acetobutolol
N-(3-Acetyl-4-[2-hydroxy-3-(isopropylamino)propoxy]phenyl)butanamide
N-[3-Acetyl-4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]butanamide
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Acebutololtablet100 mgoralSanis Health Inc2010-02-25Not applicableCanada
Acebutololtablet400 mgoralSanis Health Inc2010-02-25Not applicableCanada
Acebutololtablet200 mgoralSanis Health Inc2010-02-25Not applicableCanada
Acebutolol - 400 - Tab 400mgtablet400 mgoralPro Doc Limitee1996-12-31Not applicableCanada
Acebutolol-100-tab 100mgtablet100 mgoralPro Doc Limitee1996-12-31Not applicableCanada
Acebutolol-200 - Tab 200mgtablet200 mgoralPro Doc Limitee1996-12-31Not applicableCanada
Ava-acebutololtablet400 mgoralAvanstra Inc2011-10-112014-08-21Canada
Ava-acebutololtablet200 mgoralAvanstra Inc2011-10-112014-08-21Canada
Ava-acebutololtablet100 mgoralAvanstra Inc2011-10-112014-08-21Canada
Monitan 100tablet100 mgoralWyeth Canada1995-12-312004-09-13Canada
Monitan 200tablet200 mgoralWyeth Canada1995-12-312007-01-22Canada
Monitan 400tablet400 mgoralWyeth Canada1994-12-312007-01-22Canada
Monitan Tab 200mgtablet200 mgoralWyeth Ltd.1987-12-311996-09-10Canada
Monitan Tab 400mgtablet400 mgoralWyeth Ltd.1990-12-311996-09-10Canada
Mylan-acebutololtablet400 mgoralMylan Pharmaceuticals Ulc1998-04-06Not applicableCanada
Mylan-acebutololtablet200 mgoralMylan Pharmaceuticals Ulc1998-04-06Not applicableCanada
Mylan-acebutololtablet100 mgoralMylan Pharmaceuticals Ulc1998-04-06Not applicableCanada
Mylan-acebutolol (type S)tablet200 mgoralMylan Pharmaceuticals Ulc1998-09-16Not applicableCanada
Mylan-acebutolol (type S)tablet100 mgoralMylan Pharmaceuticals Ulc1998-09-16Not applicableCanada
Mylan-acebutolol (type S)tablet400 mgoralMylan Pharmaceuticals Ulc1998-09-16Not applicableCanada
Novo-acebutolol (type S)tablet400 mgoralNovopharm LimitedNot applicableNot applicableCanada
Novo-acebutolol (type S)tablet200 mgoralNovopharm LimitedNot applicableNot applicableCanada
Novo-acebutolol (type S)tablet100 mgoralNovopharm LimitedNot applicableNot applicableCanada
Nu-acebutolol - Tab 100mgtablet100 mgoralNu Pharm Inc1995-12-312012-09-04Canada
Nu-acebutolol - Tab 200mgtablet200 mgoralNu Pharm Inc1995-12-312012-09-04Canada
Nu-acebutolol - Tab 400mgtablet400 mgoralNu Pharm Inc1995-12-312012-09-04Canada
Penta-acebutolol Tabletstablet200 mgoralPentapharm Ltd.Not applicableNot applicableCanada
Penta-acebutolol Tabletstablet100 mgoralPentapharm Ltd.Not applicableNot applicableCanada
Penta-acebutolol Tabletstablet400 mgoralPentapharm Ltd.Not applicableNot applicableCanada
Rhotral 100tablet100 mgoralSanofi Aventis Canada Inc1991-12-312010-10-26Canada
Rhotral 200tablet200 mgoralSanofi Aventis Canada Inc1991-12-312010-10-26Canada
Rhotral 400tablet400 mgoralSanofi Aventis Canada Inc1995-12-312011-01-06Canada
Sandoz Acebutololtablet400 mgoralSandoz Canada Incorporated2004-08-18Not applicableCanada
Sandoz Acebutololtablet200 mgoralSandoz Canada Incorporated2004-08-18Not applicableCanada
Sandoz Acebutololtablet100 mgoralSandoz Canada Incorporated2004-08-18Not applicableCanada
Sectralcapsule200 mg/1oralPromius Pharma, LLC1984-12-28Not applicableUs
Sectraltablet400 mgoralSanofi Aventis Canada Inc1990-12-31Not applicableCanada
Sectraltablet200 mgoralSanofi Aventis Canada Inc1986-12-31Not applicableCanada
Sectraltablet100 mgoralSanofi Aventis Canada Inc1986-12-31Not applicableCanada
Sectralcapsule400 mg/1oralPromius Pharma, LLC1984-12-28Not applicableUs
Teva-acebutololtablet400 mgoralTeva Canada Limited1996-08-16Not applicableCanada
Teva-acebutololtablet200 mgoralTeva Canada Limited1996-08-16Not applicableCanada
Teva-acebutololtablet100 mgoralTeva Canada Limited1996-08-16Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Acebutolol Hydrochloridecapsule200 mg/1oralMylan Pharmaceuticals Inc.1995-04-24Not applicableUs
Acebutolol Hydrochloridecapsule400 mg/1oralAv Pak2009-12-01Not applicableUs
Acebutolol Hydrochloridecapsule200 mg/1oralAv Pak2009-12-01Not applicableUs
Acebutolol Hydrochloridecapsule400 mg/1oralAv Kare, Inc.2009-12-14Not applicableUs
Acebutolol Hydrochloridecapsule400 mg/1oralAmneal Pharmaceuticals of New York, LLC2009-12-01Not applicableUs
Acebutolol Hydrochloridecapsule200 mg/1oralAv Kare, Inc.2009-12-14Not applicableUs
Acebutolol Hydrochloridecapsule200 mg/1oralAmneal Pharmaceuticals of New York, LLC2009-12-01Not applicableUs
Acebutolol Hydrochloridecapsule200 mg/1oralMajor Pharmaceuticals2009-12-01Not applicableUs
Acebutolol Hydrochloridecapsule200 mg/1oralbryant ranch prepack2009-12-01Not applicableUs
Acebutolol Hydrochloridecapsule400 mg/1oralMylan Pharmaceuticals Inc.1995-04-24Not applicableUs
Acebutolol Hydrochloridecapsule400 mg/1oralPhysicians Total Care, Inc.2005-04-22Not applicableUs
Apo-acebutololtablet400 mgoralApotex Inc1995-12-31Not applicableCanada
Apo-acebutololtablet200 mgoralApotex Inc1995-12-31Not applicableCanada
Apo-acebutololtablet100 mgoralApotex Inc1995-12-31Not applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
PrentBayer
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Acebutolol Hydrochloride
34381-68-5
Thumb
  • InChI Key:
  • Monoisotopic Mass:
  • Average Mass:
DBSALT000192
Categories
UNII67P356D8GH
CAS number37517-30-9
WeightAverage: 336.4259
Monoisotopic: 336.204907394
Chemical FormulaC18H28N2O4
InChI KeyInChIKey=GOEMGAFJFRBGGG-UHFFFAOYSA-N
InChI
InChI=1S/C18H28N2O4/c1-5-6-18(23)20-14-7-8-17(16(9-14)13(4)21)24-11-15(22)10-19-12(2)3/h7-9,12,15,19,22H,5-6,10-11H2,1-4H3,(H,20,23)
IUPAC Name
N-(3-acetyl-4-{2-hydroxy-3-[(propan-2-yl)amino]propoxy}phenyl)butanamide
SMILES
CCCC(=O)NC1=CC(C(C)=O)=C(OCC(O)CNC(C)C)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as n-arylamides. These are organic compounds that contain a carboxamide group that is N-linked to a aryl group. They have the generic structure RC(=O)N(R')H, R = organyl group and R'= aryl group.
KingdomOrganic compounds
Super ClassOrganonitrogen compounds
ClassN-arylamides
Sub ClassNot Available
Direct ParentN-arylamides
Alternative Parents
Substituents
  • N-arylamide
  • Acetophenone
  • Aryl alkyl ketone
  • Aryl ketone
  • Phenol ether
  • Benzoyl
  • Alkyl aryl ether
  • Fatty acyl
  • Benzenoid
  • Fatty amide
  • Monocyclic benzene moiety
  • Secondary carboxylic acid amide
  • Secondary alcohol
  • Ketone
  • Carboxamide group
  • 1,2-aminoalcohol
  • Secondary amine
  • Ether
  • Secondary aliphatic amine
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the management of hypertension and ventricular premature beats in adults.
PharmacodynamicsAcebutolol is a cardioselective, beta-adrenoreceptor blocking agent, which possesses mild intrinsic sympathomimetic activity (ISA) in its therapeutically effective dose range. In general, beta-blockers reduce the work the heart has to do and allow it to beat more regularly. Acebutolol has less antagonistic effects on peripheral vascular ß2-receptors at rest and after epinephrine stimulation than nonselective beta-antagonists. Low doses of acebutolol produce less evidence of bronchoconstriction than nonselective agents like propranolol but more than atenolol.
Mechanism of actionAcebutolol is a selective β1-receptor antagonist. Activation of β1-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Acebutolol blocks these receptors, lowering the heart rate and blood pressure. This drug then has the reverse effect of epinephrine. In addition, beta blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels.
Related Articles
AbsorptionWell absorbed from the Gl tract with an absolute bioavailability of approximately 40% for the parent compound. In
Volume of distributionNot Available
Protein binding26%
Metabolism

Subject to extensive first-pass hepatic biotransformation (primarily to diacetolol).

Route of eliminationElimination via renal excretion is approximately 30% to 40% and by non-renal mechanisms 50% to 60%, which includes excretion into the bile and direct passage through the intestinal wall.
Half lifeThe plasma elimination half-life is approximately 3 to 4 hours. The half-life of its metabolite, diacetolol, is 8 to 13 hours.
ClearanceNot Available
ToxicitySymptoms of overdose include extreme bradycardia, advanced atrioventricular block, intraventricular conduction defects, hypotension, severe congestive heart failure, seizures, and in susceptible patients, bronchospasm, and hypoglycemia.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Acebutolol Action PathwayDrug actionSMP00296
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9156
Blood Brain Barrier-0.9659
Caco-2 permeable-0.8957
P-glycoprotein substrateSubstrate0.7378
P-glycoprotein inhibitor INon-inhibitor0.8557
P-glycoprotein inhibitor IINon-inhibitor0.8664
Renal organic cation transporterNon-inhibitor0.9466
CYP450 2C9 substrateNon-substrate0.8102
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.5752
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8721
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9639
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.849
BiodegradationNot ready biodegradable0.8538
Rat acute toxicity2.0487 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9821
hERG inhibition (predictor II)Non-inhibitor0.8555
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Capsuleoral200 mg/1
Capsuleoral400 mg/1
Tabletoral100 mg
Tabletoral200 mg
Tabletoral400 mg
Prices
Unit descriptionCostUnit
Acebutolol hcl powder7.08USD g
Sectral 400 mg capsule4.48USD capsule
Sectral 200 mg capsule3.37USD capsule
Acebutolol HCl 400 mg capsule1.39USD capsule
Acebutolol 400 mg capsule1.34USD capsule
Sectral 400 mg Tablet1.11USD tablet
Acebutolol HCl 200 mg capsule1.05USD capsule
Acebutolol 200 mg capsule1.01USD capsule
Sectral 200 mg Tablet0.56USD tablet
Acebutolol 400 mg Tablet0.51USD tablet
Apo-Acebutolol 400 mg Tablet0.51USD tablet
Mylan-Acebutolol (Type S) 400 mg Tablet0.51USD tablet
Mylan-Acebutolol 400 mg Tablet0.51USD tablet
Novo-Acebutolol 400 mg Tablet0.51USD tablet
Nu-Acebutolol 400 mg Tablet0.51USD tablet
Rhotral 400 mg Tablet0.51USD tablet
Sectral 100 mg Tablet0.37USD tablet
Acebutolol 200 mg Tablet0.26USD tablet
Apo-Acebutolol 200 mg Tablet0.26USD tablet
Mylan-Acebutolol (Type S) 200 mg Tablet0.26USD tablet
Mylan-Acebutolol 200 mg Tablet0.26USD tablet
Novo-Acebutolol 200 mg Tablet0.26USD tablet
Nu-Acebutolol 200 mg Tablet0.26USD tablet
Rhotral 200 mg Tablet0.26USD tablet
Acebutolol 100 mg Tablet0.17USD tablet
Apo-Acebutolol 100 mg Tablet0.17USD tablet
Mylan-Acebutolol (Type S) 100 mg Tablet0.17USD tablet
Mylan-Acebutolol 100 mg Tablet0.17USD tablet
Novo-Acebutolol 100 mg Tablet0.17USD tablet
Nu-Acebutolol 100 mg Tablet0.17USD tablet
Rhotral 100 mg Tablet0.17USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point136-138Merck Index 13
water solubility259 mg/LNot Available
logP1.71HANSCH,C ET AL. (1995)
Caco2 permeability-5.83ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.172 mg/mLALOGPS
logP1.43ALOGPS
logP1.53ChemAxon
logS-3.3ALOGPS
pKa (Strongest Acidic)13.91ChemAxon
pKa (Strongest Basic)9.57ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area87.66 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity94.87 m3·mol-1ChemAxon
Polarizability38.51 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

DrugSyn.org

US3857952
General ReferencesNot Available
External Links
ATC CodesC07AB04C07BB04
AHFS Codes
  • 24:24.00
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcepromazineAcepromazine may increase the hypotensive activities of Acebutolol.
AcetaminophenThe risk or severity of adverse effects can be increased when Acebutolol is combined with Acetaminophen.
AcetylcholineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Acetylcholine.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acebutolol is combined with Acetylsalicylic acid.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Acebutolol.
AlfuzosinAcebutolol may increase the orthostatic hypotensive activities of Alfuzosin.
AmifostineAcebutolol may increase the hypotensive activities of Amifostine.
AminophyllineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Aminophylline.
AmiodaroneAmiodarone may increase the bradycardic activities of Acebutolol.
AmphetamineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Amphetamine.
ArformoterolThe risk or severity of adverse effects can be increased when Acebutolol is combined with Arformoterol.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Acebutolol.
ArmodafinilThe risk or severity of adverse effects can be increased when Acebutolol is combined with Armodafinil.
ArticaineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Articaine.
AtomoxetineAtomoxetine may increase the hypertensive activities of Acebutolol.
BenzphetamineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Benzphetamine.
BretyliumBretylium may increase the bradycardic activities of Acebutolol.
BrimonidineBrimonidine may increase the antihypertensive activities of Acebutolol.
BupivacaineThe serum concentration of Bupivacaine can be increased when it is combined with Acebutolol.
ButabarbitalThe serum concentration of Acebutolol can be decreased when it is combined with Butabarbital.
ButalbitalThe risk or severity of adverse effects can be increased when Acebutolol is combined with Butalbital.
ButethalThe serum concentration of Acebutolol can be decreased when it is combined with Butethal.
CabergolineAcebutolol may increase the vasoconstricting activities of Cabergoline.
CaffeineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Caffeine.
CarbacholThe risk or severity of adverse effects can be increased when Acebutolol is combined with Carbachol.
CeritinibAcebutolol may increase the bradycardic activities of Ceritinib.
ChloroquineThe metabolism of Acebutolol can be decreased when combined with Chloroquine.
ChlorpropamideAcebutolol may increase the hypoglycemic activities of Chlorpropamide.
CocaineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Cocaine.
DexmethylphenidateThe risk or severity of adverse effects can be increased when Acebutolol is combined with Dexmethylphenidate.
DextroamphetamineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Dextroamphetamine.
DiazoxideDiazoxide may increase the hypotensive activities of Acebutolol.
DiethylpropionThe risk or severity of adverse effects can be increased when Acebutolol is combined with Diethylpropion.
DigoxinAcebutolol may increase the bradycardic activities of Digoxin.
DihydrocodeineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Dihydrocodeine.
DipivefrinThe risk or severity of adverse effects can be increased when Acebutolol is combined with Dipivefrin.
DipyridamoleDipyridamole may increase the bradycardic activities of Acebutolol.
DisopyramideDisopyramide may increase the bradycardic activities of Acebutolol.
DobutamineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Dobutamine.
DopamineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Dopamine.
DoxapramThe risk or severity of adverse effects can be increased when Acebutolol is combined with Doxapram.
DronabinolDronabinol may increase the tachycardic activities of Acebutolol.
DronedaroneDronedarone may increase the bradycardic activities of Acebutolol.
DuloxetineAcebutolol may increase the orthostatic hypotensive activities of Duloxetine.
DyphyllineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Dyphylline.
EphedrineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Ephedrine.
EpinephrineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Epinephrine.
EsmololEsmolol may increase the bradycardic activities of Acebutolol.
FenoterolThe risk or severity of adverse effects can be increased when Acebutolol is combined with Fenoterol.
FingolimodAcebutolol may increase the bradycardic activities of Fingolimod.
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Acebutolol.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Acebutolol is combined with Fluticasone Propionate.
FormoterolThe risk or severity of adverse effects can be increased when Acebutolol is combined with Formoterol.
HeptabarbitalThe serum concentration of Acebutolol can be decreased when it is combined with Heptabarbital.
HexobarbitalThe serum concentration of Acebutolol can be decreased when it is combined with Hexobarbital.
IndacaterolThe risk or severity of adverse effects can be increased when Acebutolol is combined with Indacaterol.
InfliximabInfliximab may decrease the antihypertensive activities of Acebutolol.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Acebutolol.
Ipratropium bromideThe risk or severity of adverse effects can be increased when Acebutolol is combined with Ipratropium bromide.
IsomethepteneThe risk or severity of adverse effects can be increased when Acebutolol is combined with Isometheptene.
IvabradineAcebutolol may increase the bradycardic activities of Ivabradine.
LacosamideAcebutolol may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LevodopaAcebutolol may increase the orthostatic hypotensive activities of Levodopa.
LevonordefrinThe risk or severity of adverse effects can be increased when Acebutolol is combined with Levonordefrin.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Acebutolol.
LinezolidLinezolid may increase the hypertensive activities of Acebutolol.
LisdexamfetamineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Lisdexamfetamine.
MepivacaineThe serum concentration of Mepivacaine can be increased when it is combined with Acebutolol.
MethacholineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Methacholine.
MethamphetamineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Methamphetamine.
MethohexitalThe serum concentration of Acebutolol can be decreased when it is combined with Methohexital.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Acebutolol.
MidodrineAcebutolol may increase the bradycardic activities of Midodrine.
ModafinilThe risk or severity of adverse effects can be increased when Acebutolol is combined with Modafinil.
MolsidomineMolsidomine may increase the hypotensive activities of Acebutolol.
MoxonidineMoxonidine may increase the hypotensive activities of Acebutolol.
NabiloneNabilone may increase the tachycardic activities of Acebutolol.
NaphazolineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Naphazoline.
NicorandilNicorandil may increase the hypotensive activities of Acebutolol.
NifedipineNifedipine may increase the hypotensive activities of Acebutolol.
NorepinephrineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Norepinephrine.
ObinutuzumabAcebutolol may increase the hypotensive activities of Obinutuzumab.
OctreotideOctreotide may increase the bradycardic activities of Acebutolol.
OlodaterolThe risk or severity of adverse effects can be increased when Acebutolol is combined with Olodaterol.
OrciprenalineAcebutolol may decrease the activities of Orciprenaline.
OxymetazolineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Oxymetazoline.
PentobarbitalThe serum concentration of Acebutolol can be decreased when it is combined with Pentobarbital.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Acebutolol.
PhendimetrazineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Phendimetrazine.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Acebutolol.
PheniramineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Pheniramine.
PhentermineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Phentermine.
PhenylephrineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Phenylephrine.
PirbuterolThe risk or severity of adverse effects can be increased when Acebutolol is combined with Pirbuterol.
PrazosinAcebutolol may increase the orthostatic hypotensive activities of Prazosin.
PrimidoneThe serum concentration of Acebutolol can be decreased when it is combined with Primidone.
PropafenoneThe serum concentration of Acebutolol can be increased when it is combined with Propafenone.
PropylhexedrineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Propylhexedrine.
PseudoephedrineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Pseudoephedrine.
QuinineQuinine may increase the hypotensive activities of Acebutolol.
RacepinephrineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Racepinephrine.
RegorafenibRegorafenib may increase the bradycardic activities of Acebutolol.
ReserpineReserpine may increase the hypotensive activities of Acebutolol.
RisperidoneAcebutolol may increase the hypotensive activities of Risperidone.
RituximabAcebutolol may increase the hypotensive activities of Rituximab.
RivastigmineRivastigmine may increase the bradycardic activities of Acebutolol.
RuxolitinibRuxolitinib may increase the bradycardic activities of Acebutolol.
SalbutamolThe risk or severity of adverse effects can be increased when Acebutolol is combined with Salbutamol.
SalmeterolThe risk or severity of adverse effects can be increased when Acebutolol is combined with Salmeterol.
SecobarbitalThe serum concentration of Acebutolol can be decreased when it is combined with Secobarbital.
SufentanilSufentanil may increase the bradycardic activities of Acebutolol.
TacrineTacrine may increase the bradycardic activities of Acebutolol.
TadalafilTadalafil may increase the antihypertensive activities of Acebutolol.
Tedizolid PhosphateTedizolid Phosphate may increase the hypertensive activities of Acebutolol.
TerbutalineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Terbutaline.
TheophyllineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Theophylline.
TofacitinibTofacitinib may increase the bradycardic activities of Acebutolol.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Acebutolol.
TreprostinilTreprostinil may increase the hypotensive activities of Acebutolol.
TriprolidineThe risk or severity of adverse effects can be increased when Acebutolol is combined with Triprolidine.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Acebutolol.
VardenafilVardenafil may increase the antihypertensive activities of Acebutolol.
VilanterolThe risk or severity of adverse effects can be increased when Acebutolol is combined with Vilanterol.
YohimbineYohimbine may decrease the antihypertensive activities of Acebutolol.
Food Interactions
  • Take without regard to meals; absorption rate and maximal concentration are slightly reduced but the extent of absorption is not affected.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
partial agonist
General Function:
Receptor signaling protein activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
Gene Name:
ADRB1
Uniprot ID:
P08588
Molecular Weight:
51322.1 Da
References
  1. van den Meiracker AH, Man in 't Veld AJ, Fischberg DJ, Molinoff PB, van Eck HJ, Boomsma F, Derkx FH, Schalekamp MA: Acute and long-term effects of acebutolol on systemic and renal hemodynamics, body fluid volumes, catecholamines, active renin, aldosterone, and lymphocyte beta-adrenoceptor density. J Cardiovasc Pharmacol. 1988 Apr;11(4):413-23. [PubMed:2453744 ]
  2. Abrahamsson T: Characterization of the beta 1-adrenoceptor stimulatory effects of the partial beta 1-agonists acebutolol, xamoterol, H142/08 and H201/70. Eur J Pharmacol. 1989 May 2;164(1):121-8. [PubMed:2568935 ]
  3. Fraysse B, Garric J: Prediction and experimental validation of acute toxicity of beta-blockers in Ceriodaphnia dubia. Environ Toxicol Chem. 2005 Oct;24(10):2470-6. [PubMed:16268148 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
partial agonist
General Function:
Protein homodimerization activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine.
Gene Name:
ADRB2
Uniprot ID:
P07550
Molecular Weight:
46458.32 Da
References
  1. Fraysse B, Garric J: Prediction and experimental validation of acute toxicity of beta-blockers in Ceriodaphnia dubia. Environ Toxicol Chem. 2005 Oct;24(10):2470-6. [PubMed:16268148 ]
  2. Varma DR, Shen H, Deng XF, Peri KG, Chemtob S, Mulay S: Inverse agonist activities of beta-adrenoceptor antagonists in rat myocardium. Br J Pharmacol. 1999 Jun;127(4):895-902. [PubMed:10433496 ]
  3. Lima JJ: Relationship between beta adrenoceptor occupancy and receptor down-regulation induced by beta antagonists with intrinsic sympathomimetic activity. J Recept Signal Transduct Res. 1996 Sep-Nov;16(5-6):357-72. [PubMed:8968966 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Zhang L, Schaner ME, Giacomini KM: Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). J Pharmacol Exp Ther. 1998 Jul;286(1):354-61. [PubMed:9655880 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Troutman MD, Thakker DR: Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium. Pharm Res. 2003 Aug;20(8):1210-24. [PubMed:12948019 ]
  2. Terao T, Hisanaga E, Sai Y, Tamai I, Tsuji A: Active secretion of drugs from the small intestinal epithelium in rats by P-glycoprotein functioning as an absorption barrier. J Pharm Pharmacol. 1996 Oct;48(10):1083-9. [PubMed:8953513 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23