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Identification
NameBretylium
Accession NumberDB01158  (APRD00830)
TypeSmall Molecule
GroupsApproved
DescriptionBretylium blocks the release of noradrenaline from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation. The primary mode of action for bretylium is thought to be inhibition of voltage-gated K(+) channels. Recent evidence has shown that bretylium may also inhibit the Na,K-ATPase by binding to the extracellular K-site.
Structure
Thumb
Synonyms
(2-Bromobenzyl)ethyldimethylaminium
2-Bromo-N-ethyl-N,N-dimethylbenzenemethanaminium
N-Ethyl-N,N-dimethyl-2-bromobenzenemethanaminium
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Bretylate Inj 50mg/mlliquid50 mgintramuscular; intravenousGlaxo Wellcome Inc.1980-12-312000-01-19Canada
Bretylium Tosylate Inj 50mg/mlsolution50 mgintramuscular; intravenousAbbott Laboratories, Limited1991-12-312007-07-31Canada
Bretylium Tosylate Injection USPsolution50 mgintramuscular; intravenousSandoz Canada Incorporated1995-12-31Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AnxyrexSanofi-Aventis
BretylolICI
BromidemNycomed
CreosedinAstraZeneca
DarenthinBurroughs Wellcome
LexotanRoche
XionilNovartis
Brand mixtures
NameLabellerIngredients
Bretylium Tosylate 0.2% and Dextrose 5% InjAbbott Laboratories, Limited
Bretylium Tosylate 0.4% and Dextrose 5% InjAbbott Laboratories, Limited
Salts
Name/CASStructureProperties
Bretylium tosylate
ThumbNot applicableDBSALT001050
Categories
UNIIRZR75EQ2KJ
CAS number59-41-6
WeightAverage: 243.163
Monoisotopic: 242.054437196
Chemical FormulaC11H17BrN
InChI KeyInChIKey=AAQOQKQBGPPFNS-UHFFFAOYSA-N
InChI
InChI=1S/C11H17BrN/c1-4-13(2,3)9-10-7-5-6-8-11(10)12/h5-8H,4,9H2,1-3H3/q+1
IUPAC Name
[(2-bromophenyl)methyl](ethyl)dimethylazanium
SMILES
CC[N+](C)(C)CC1=CC=CC=C1Br
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylmethylamines. These are compounds containing a phenylmethtylamine moiety, which consists of a phenyl group substituted by an methanamine.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylmethylamines
Direct ParentPhenylmethylamines
Alternative Parents
Substituents
  • Phenylmethylamine
  • Benzylamine
  • Aralkylamine
  • Halobenzene
  • Bromobenzene
  • Aryl halide
  • Aryl bromide
  • Quaternary ammonium salt
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organobromide
  • Organohalogen compound
  • Amine
  • Organic cation
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationFor use in the prophylaxis and therapy of ventricular fibrillation. Also used in the treatment of life-threatening ventricular arrhythmias, such as ventricular tachycardia, that have failed to respond to adequate doses of a first-line antiarrhythmic agent, such as lidocaine.
PharmacodynamicsBretylium is a bromobenzyl quaternary ammonium compound which selectively accumulates in sympathetic ganglia and their postganglionic adrenergic neurons where it inhibits norepinephrine release by depressing adrenergic nerve terminal excitability. Bretylium also suppresses ventricular fibrillation and ventricular arrhythmias.
Mechanism of actionBretylium inhibits norepinephrine release by depressing adrenergic nerve terminal excitability. The mechanisms of the antifibrillatory and antiarrhythmic actions of bretylium are not established. In efforts to define these mechanisms, the following electrophysiologic actions of bretylium have been demonstrated in animal experiments: increase in ventricular fibrillation threshold, increase in action potential duration and effective refractory period without changes in heart rate, little effect on the rate of rise or amplitude of the cardiac action potential (Phase 0) or in resting membrane potential (Phase 4) in normal myocardium, decrease in the disparity in action potential duration between normal and infarcted regions, and increase in impulse formation and spontaneous firing rate of pacemaker tissue as well as increase ventricular conduction velocity.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

No metabolites have been identified following administration in man and laboratory animals.

Route of eliminationNot Available
Half lifeThe terminal half-life in four normal volunteers averaged 7.8±0.6 hours (range 6.9-8.1). During hemodialysis, this patient's arterial and venous bretylium concentrations declined rapidly, resulting in a half-life of 13 hours.
ClearanceNot Available
ToxicityOral, mouse: LD50 = 400 mg/kg. In the presence of life-threatening arrhythmias, underdosing with bretylium probably presents a greater risk to the patient than potential overdosage. However, one case of accidental overdose has been reported in which a rapidly injected intravenous bolus of 30 mg/kg was given instead of an intended 10 mg/kg dose during an episode of ventricular tachycardia. Marked hypertension resulted, followed by protracted refractory hypotension. The patient expired 18 hours later in asystole, complicated by renal failure and aspiration pneumonitis. Bretylium serum levels were 8000 ng/mL.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.8406
Blood Brain Barrier+0.9484
Caco-2 permeable+0.6831
P-glycoprotein substrateSubstrate0.5105
P-glycoprotein inhibitor INon-inhibitor0.9789
P-glycoprotein inhibitor IINon-inhibitor0.8742
Renal organic cation transporterNon-inhibitor0.6279
CYP450 2C9 substrateNon-substrate0.861
CYP450 2D6 substrateNon-substrate0.6999
CYP450 3A4 substrateSubstrate0.5132
CYP450 1A2 substrateNon-inhibitor0.6973
CYP450 2C9 inhibitorNon-inhibitor0.8505
CYP450 2D6 inhibitorNon-inhibitor0.8475
CYP450 2C19 inhibitorNon-inhibitor0.8038
CYP450 3A4 inhibitorNon-inhibitor0.9752
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6854
Ames testNon AMES toxic0.9045
CarcinogenicityCarcinogens 0.5905
BiodegradationNot ready biodegradable0.9157
Rat acute toxicity2.6214 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9291
hERG inhibition (predictor II)Inhibitor0.6322
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Liquidintramuscular; intravenous50 mg
Solutionintravenous
Solutionintramuscular; intravenous50 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point238Fryer, R.I., Schmidt, R.A. and Sternbach, L.H.; U.S. Patent 3,100,770; August 13, 1963; assigned to Hoffmann-LaRoche Inc. Fryer, R.I., Schmidt, R.A. and Sternbach, L.H.; U.S. Patent 3,182,065; May 4, 1965; assigned to Hoffmann-LaRoche Inc. Fryer, R.I., Schmidt, R.A. and Sternbach, L.H.; US. Patent 3,182,067; May 4, 1965; assigned to Hoffmann-LaRoche Inc.
water solubilityFreely solubleNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.000154 mg/mLALOGPS
logP-1.4ALOGPS
logP-1.1ChemAxon
logS-6.3ALOGPS
pKa (Strongest Acidic)17.58ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count0ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area0 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity72.89 m3·mol-1ChemAxon
Polarizability23.24 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Copp, F.C. and Stephenson, D.; US. Patent 3,038,004; June 5, 1962; assigned to Burroughs
Wellcome & Co.

US3038004
General ReferencesNot Available
External Links
ATC CodesNot Available
AHFS Codes
  • 24:04.04.20
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73 KB)
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypotensive activities of Bretylium.
AcebutololBretylium may increase the bradycardic activities of Acebutolol.
AcebutololAcebutolol may increase the hypotensive activities of Bretylium.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Bretylium.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Bretylium.
AlfuzosinAlfuzosin may increase the hypotensive activities of Bretylium.
AliskirenBretylium may increase the hypotensive activities of Aliskiren.
AlprenololAlprenolol may increase the hypotensive activities of Bretylium.
AmbrisentanBretylium may increase the hypotensive activities of Ambrisentan.
AmifostineBretylium may increase the hypotensive activities of Amifostine.
AmilorideThe risk or severity of adverse effects can be increased when Amiloride is combined with Bretylium.
AmiodaroneBretylium may increase the bradycardic activities of Amiodarone.
AmlodipineAmlodipine may increase the hypotensive activities of Bretylium.
AmobarbitalAmobarbital may increase the hypotensive activities of Bretylium.
Amyl NitriteThe risk or severity of adverse effects can be increased when Bretylium is combined with Amyl Nitrite.
ApraclonidineThe risk or severity of adverse effects can be increased when Apraclonidine is combined with Bretylium.
AripiprazoleAripiprazole may increase the hypotensive activities of Bretylium.
AtenololBretylium may increase the bradycardic activities of Atenolol.
AtenololAtenolol may increase the hypotensive activities of Bretylium.
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Bretylium is combined with Azilsartan medoxomil.
BarbitalBarbital may increase the hypotensive activities of Bretylium.
BenazeprilBenazepril may increase the hypotensive activities of Bretylium.
BendroflumethiazideBretylium may increase the bradycardic activities of Bendroflumethiazide.
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Bretylium.
BenmoxinBenmoxin may increase the hypotensive activities of Bretylium.
BepridilBretylium may increase the hypotensive activities of Bepridil.
BeractantBretylium may increase the bradycardic activities of Beractant.
BetaxololBretylium may increase the bradycardic activities of Betaxolol.
BetaxololBetaxolol may increase the hypotensive activities of Bretylium.
BethanidineBethanidine may increase the hypotensive activities of Bretylium.
BimatoprostBimatoprost may increase the hypotensive activities of Bretylium.
BisoprololBretylium may increase the bradycardic activities of Bisoprolol.
BisoprololBisoprolol may increase the hypotensive activities of Bretylium.
BosentanBosentan may increase the hypotensive activities of Bretylium.
BrimonidineBretylium may increase the hypotensive activities of Brimonidine.
BrimonidineBrimonidine may increase the antihypertensive activities of Bretylium.
BumetanideThe risk or severity of adverse effects can be increased when Bumetanide is combined with Bretylium.
BupranololBretylium may increase the hypotensive activities of Bupranolol.
CalfactantBretylium may increase the bradycardic activities of Calfactant.
CanagliflozinThe risk or severity of adverse effects can be increased when Bretylium is combined with Canagliflozin.
CandesartanCandesartan may increase the hypotensive activities of Bretylium.
CandoxatrilCandoxatril may increase the hypotensive activities of Bretylium.
CaptoprilBretylium may increase the hypotensive activities of Captopril.
CaroxazoneCaroxazone may increase the hypotensive activities of Bretylium.
CarteololBretylium may increase the bradycardic activities of Carteolol.
CarteololCarteolol may increase the hypotensive activities of Bretylium.
CarvedilolBretylium may increase the bradycardic activities of Carvedilol.
CarvedilolCarvedilol may increase the hypotensive activities of Bretylium.
CeliprololBretylium may increase the hypotensive activities of Celiprolol.
CeritinibBretylium may increase the bradycardic activities of Ceritinib.
ChlorothiazideChlorothiazide may increase the hypotensive activities of Bretylium.
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Bretylium.
CilazaprilBretylium may increase the hypotensive activities of Cilazapril.
ClevidipineThe risk or severity of adverse effects can be increased when Bretylium is combined with Clevidipine.
ClonidineBretylium may increase the bradycardic activities of Clonidine.
ClonidineClonidine may increase the hypotensive activities of Bretylium.
CrizotinibBretylium may increase the bradycardic activities of Crizotinib.
CryptenamineCryptenamine may increase the hypotensive activities of Bretylium.
CyclothiazideCyclothiazide may increase the hypotensive activities of Bretylium.
DapagliflozinThe risk or severity of adverse effects can be increased when Bretylium is combined with Dapagliflozin.
DebrisoquinBretylium may increase the hypotensive activities of Debrisoquin.
DeserpidineBretylium may increase the hypotensive activities of Deserpidine.
DexmedetomidineBretylium may increase the bradycardic activities of Dexmedetomidine.
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Bretylium.
DiazoxideDiazoxide may increase the hypotensive activities of Bretylium.
DiclofenamideThe risk or severity of adverse effects can be increased when Diclofenamide is combined with Bretylium.
DigoxinBretylium may increase the bradycardic activities of Digoxin.
DiltiazemBretylium may increase the bradycardic activities of Diltiazem.
DiltiazemDiltiazem may increase the hypotensive activities of Bretylium.
DinutuximabThe risk or severity of adverse effects can be increased when Bretylium is combined with Dinutuximab.
DipyridamoleThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Bretylium.
DonepezilBretylium may increase the bradycardic activities of Donepezil.
DorzolamideDorzolamide may increase the hypotensive activities of Bretylium.
DoxazosinDoxazosin may increase the hypotensive activities of Bretylium.
DronedaroneBretylium may increase the bradycardic activities of Dronedarone.
DuloxetineBretylium may increase the orthostatic hypotensive activities of Duloxetine.
EfonidipineBretylium may increase the hypotensive activities of Efonidipine.
EmpagliflozinThe risk or severity of adverse effects can be increased when Bretylium is combined with Empagliflozin.
EnalaprilEnalapril may increase the hypotensive activities of Bretylium.
EnalaprilatBretylium may increase the hypotensive activities of Enalaprilat.
EplerenoneThe risk or severity of adverse effects can be increased when Eplerenone is combined with Bretylium.
EpoprostenolBretylium may increase the hypotensive activities of Epoprostenol.
EprosartanEprosartan may increase the hypotensive activities of Bretylium.
EsmololBretylium may increase the bradycardic activities of Esmolol.
EsmololThe risk or severity of adverse effects can be increased when Esmolol is combined with Bretylium.
Etacrynic acidThe risk or severity of adverse effects can be increased when Etacrynic acid is combined with Bretylium.
FelodipineFelodipine may increase the hypotensive activities of Bretylium.
FenoldopamFenoldopam may increase the hypotensive activities of Bretylium.
FingolimodBretylium may increase the bradycardic activities of Fingolimod.
FosinoprilFosinopril may increase the hypotensive activities of Bretylium.
FurazolidoneFurazolidone may increase the hypotensive activities of Bretylium.
FurosemideThe risk or severity of adverse effects can be increased when Furosemide is combined with Bretylium.
GalantamineBretylium may increase the bradycardic activities of Galantamine.
GuanabenzGuanabenz may increase the hypotensive activities of Bretylium.
GuanadrelGuanadrel may increase the hypotensive activities of Bretylium.
GuanethidineBretylium may increase the hypotensive activities of Guanethidine.
GuanfacineBretylium may increase the bradycardic activities of Guanfacine.
GuanfacineGuanfacine may increase the hypotensive activities of Bretylium.
HexamethoniumBretylium may increase the hypotensive activities of Hexamethonium.
HexobarbitalHexobarbital may increase the hypotensive activities of Bretylium.
HydracarbazineHydracarbazine may increase the hypotensive activities of Bretylium.
HydralazineBretylium may increase the hypotensive activities of Hydralazine.
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Bretylium.
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Bretylium.
IloprostIloprost may increase the hypotensive activities of Bretylium.
IndapamideIndapamide may increase the hypotensive activities of Bretylium.
IndenololBretylium may increase the hypotensive activities of Indenolol.
IndoraminBretylium may increase the hypotensive activities of Indoramin.
IproclozideIproclozide may increase the hypotensive activities of Bretylium.
IproniazidIproniazid may increase the hypotensive activities of Bretylium.
IrbesartanIrbesartan may increase the hypotensive activities of Bretylium.
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Bretylium.
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Isosorbide Dinitrate is combined with Bretylium.
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Isosorbide Mononitrate is combined with Bretylium.
IsoxsuprineThe risk or severity of adverse effects can be increased when Bretylium is combined with Isoxsuprine.
IsradipineIsradipine may increase the hypotensive activities of Bretylium.
IvabradineBretylium may increase the bradycardic activities of Ivabradine.
LabetalolBretylium may increase the bradycardic activities of Labetalol.
LabetalolLabetalol may increase the hypotensive activities of Bretylium.
LacidipineBretylium may increase the hypotensive activities of Lacidipine.
LanreotideBretylium may increase the bradycardic activities of Lanreotide.
LatanoprostLatanoprost may increase the hypotensive activities of Bretylium.
LercanidipineLercanidipine may increase the hypotensive activities of Bretylium.
LevobunololBretylium may increase the bradycardic activities of Levobunolol.
LevobunololThe risk or severity of adverse effects can be increased when Levobunolol is combined with Bretylium.
LevodopaBretylium may increase the orthostatic hypotensive activities of Levodopa.
LisinoprilLisinopril may increase the hypotensive activities of Bretylium.
LofexidineBretylium may increase the hypotensive activities of Lofexidine.
LosartanLosartan may increase the hypotensive activities of Bretylium.
LucinactantBretylium may increase the bradycardic activities of Lucinactant.
MacitentanBretylium may increase the hypotensive activities of Macitentan.
ManidipineBretylium may increase the hypotensive activities of Manidipine.
MannitolThe risk or severity of adverse effects can be increased when Mannitol is combined with Bretylium.
MebanazineMebanazine may increase the hypotensive activities of Bretylium.
MecamylamineMecamylamine may increase the hypotensive activities of Bretylium.
MethazolamideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Bretylium.
MethohexitalMethohexital may increase the hypotensive activities of Bretylium.
MethyclothiazideThe risk or severity of adverse effects can be increased when Methyclothiazide is combined with Bretylium.
MethyldopaBretylium may increase the bradycardic activities of Methyldopa.
MethyldopaMethyldopa may increase the hypotensive activities of Bretylium.
Methylene blueMethylene blue may increase the hypotensive activities of Bretylium.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Bretylium.
MethylphenobarbitalMethylphenobarbital may increase the hypotensive activities of Bretylium.
MetipranololBretylium may increase the bradycardic activities of Metipranolol.
MetipranololMetipranolol may increase the hypotensive activities of Bretylium.
MetolazoneMetolazone may increase the hypotensive activities of Bretylium.
MetoprololBretylium may increase the bradycardic activities of Metoprolol.
MetoprololMetoprolol may increase the hypotensive activities of Bretylium.
MibefradilBretylium may increase the hypotensive activities of Mibefradil.
MinaprineMinaprine may increase the hypotensive activities of Bretylium.
MinoxidilMinoxidil may increase the hypotensive activities of Bretylium.
MoclobemideMoclobemide may increase the hypotensive activities of Bretylium.
MoexiprilMoexipril may increase the hypotensive activities of Bretylium.
MolsidomineMolsidomine may increase the hypotensive activities of Bretylium.
MoxonidineBretylium may increase the hypotensive activities of Moxonidine.
NadololBretylium may increase the bradycardic activities of Nadolol.
NadololNadolol may increase the hypotensive activities of Bretylium.
NebivololBretylium may increase the bradycardic activities of Nebivolol.
NebivololNebivolol may increase the hypotensive activities of Bretylium.
NesiritideThe risk or severity of adverse effects can be increased when Bretylium is combined with Nesiritide.
NialamideNialamide may increase the hypotensive activities of Bretylium.
NicardipineNicardipine may increase the hypotensive activities of Bretylium.
NicorandilNicorandil may increase the hypotensive activities of Bretylium.
NifedipineThe risk or severity of adverse effects can be increased when Nifedipine is combined with Bretylium.
NiguldipineBretylium may increase the hypotensive activities of Niguldipine.
NilvadipineBretylium may increase the hypotensive activities of Nilvadipine.
NimodipineNimodipine may increase the hypotensive activities of Bretylium.
NisoldipineNisoldipine may increase the hypotensive activities of Bretylium.
NitrendipineNitrendipine may increase the hypotensive activities of Bretylium.
NitroglycerinThe risk or severity of adverse effects can be increased when Nitroglycerin is combined with Bretylium.
NitroprussideNitroprusside may increase the hypotensive activities of Bretylium.
ObinutuzumabBretylium may increase the hypotensive activities of Obinutuzumab.
OctamoxinOctamoxin may increase the hypotensive activities of Bretylium.
OctreotideBretylium may increase the bradycardic activities of Octreotide.
OlmesartanOlmesartan may increase the hypotensive activities of Bretylium.
OmapatrilatOmapatrilat may increase the hypotensive activities of Bretylium.
OxprenololBretylium may increase the hypotensive activities of Oxprenolol.
PapaverineThe risk or severity of adverse effects can be increased when Papaverine is combined with Bretylium.
PargylineBretylium may increase the hypotensive activities of Pargyline.
PasireotideBretylium may increase the bradycardic activities of Pasireotide.
PenbutololBretylium may increase the bradycardic activities of Penbutolol.
PenbutololPenbutolol may increase the hypotensive activities of Bretylium.
PentobarbitalPentobarbital may increase the hypotensive activities of Bretylium.
PentoliniumPentolinium may increase the hypotensive activities of Bretylium.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Bretylium.
PerindoprilPerindopril may increase the hypotensive activities of Bretylium.
PhenelzinePhenelzine may increase the hypotensive activities of Bretylium.
PheniprazinePheniprazine may increase the hypotensive activities of Bretylium.
PhenobarbitalPhenobarbital may increase the hypotensive activities of Bretylium.
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Bretylium.
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Bretylium.
PhentolaminePhentolamine may increase the hypotensive activities of Bretylium.
PinacidilBretylium may increase the hypotensive activities of Pinacidil.
PindololBretylium may increase the bradycardic activities of Pindolol.
PindololPindolol may increase the hypotensive activities of Bretylium.
PirlindolePirlindole may increase the hypotensive activities of Bretylium.
PivhydrazinePivhydrazine may increase the hypotensive activities of Bretylium.
PolythiazideBretylium may increase the hypotensive activities of Polythiazide.
Poractant alfaBretylium may increase the bradycardic activities of Poractant alfa.
PrazosinPrazosin may increase the hypotensive activities of Bretylium.
PrimidonePrimidone may increase the hypotensive activities of Bretylium.
PropafenoneBretylium may increase the bradycardic activities of Propafenone.
PropranololBretylium may increase the bradycardic activities of Propranolol.
PropranololPropranolol may increase the hypotensive activities of Bretylium.
QuetiapineThe risk or severity of adverse effects can be increased when Bretylium is combined with Quetiapine.
QuinaprilQuinapril may increase the hypotensive activities of Bretylium.
QuinineQuinine may increase the hypotensive activities of Bretylium.
RamiprilRamipril may increase the hypotensive activities of Bretylium.
RasagilineRasagiline may increase the hypotensive activities of Bretylium.
RemikirenRemikiren may increase the hypotensive activities of Bretylium.
RescinnamineBretylium may increase the hypotensive activities of Rescinnamine.
ReserpineReserpine may increase the hypotensive activities of Bretylium.
RiociguatBretylium may increase the hypotensive activities of Riociguat.
RisperidoneBretylium may increase the hypotensive activities of Risperidone.
RituximabBretylium may increase the hypotensive activities of Rituximab.
RivastigmineBretylium may increase the bradycardic activities of Rivastigmine.
SafrazineSafrazine may increase the hypotensive activities of Bretylium.
SaprisartanBretylium may increase the hypotensive activities of Saprisartan.
SecobarbitalSecobarbital may increase the hypotensive activities of Bretylium.
SelegilineSelegiline may increase the hypotensive activities of Bretylium.
SelexipagBretylium may increase the hypotensive activities of Selexipag.
SildenafilSildenafil may increase the antihypertensive activities of Bretylium.
SitaxentanBretylium may increase the hypotensive activities of Sitaxentan.
SotalolBretylium may increase the bradycardic activities of Sotalol.
SotalolThe risk or severity of adverse effects can be increased when Sotalol is combined with Bretylium.
SpiraprilBretylium may increase the hypotensive activities of Spirapril.
SpironolactoneThe risk or severity of adverse effects can be increased when Spironolactone is combined with Bretylium.
SufentanilBretylium may increase the bradycardic activities of Sufentanil.
TadalafilTadalafil may increase the antihypertensive activities of Bretylium.
TelmisartanTelmisartan may increase the hypotensive activities of Bretylium.
TemocaprilBretylium may increase the hypotensive activities of Temocapril.
TerazosinThe risk or severity of adverse effects can be increased when Bretylium is combined with Terazosin.
TerlipressinBretylium may increase the hypotensive activities of Terlipressin.
ThiamylalThiamylal may increase the hypotensive activities of Bretylium.
ThiopentalThiopental may increase the hypotensive activities of Bretylium.
TiboloneBretylium may increase the hypotensive activities of Tibolone.
TicrynafenBretylium may increase the hypotensive activities of Ticrynafen.
TimololBretylium may increase the bradycardic activities of Timolol.
TimololTimolol may increase the hypotensive activities of Bretylium.
TizanidineBretylium may increase the bradycardic activities of Tizanidine.
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Bretylium.
TolazolineTolazoline may increase the hypotensive activities of Bretylium.
ToloxatoneToloxatone may increase the hypotensive activities of Bretylium.
TorasemideTorasemide may increase the hypotensive activities of Bretylium.
TrandolaprilTrandolapril may increase the hypotensive activities of Bretylium.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Bretylium.
TranylcypromineTranylcypromine may increase the hypotensive activities of Bretylium.
TravoprostTravoprost may increase the hypotensive activities of Bretylium.
TreprostinilTreprostinil may increase the hypotensive activities of Bretylium.
TriamtereneThe risk or severity of adverse effects can be increased when Triamterene is combined with Bretylium.
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Bretylium.
TrimazosinBretylium may increase the hypotensive activities of Trimazosin.
TrimethaphanTrimethaphan may increase the hypotensive activities of Bretylium.
UdenafilUdenafil may increase the antihypertensive activities of Bretylium.
UnoprostoneBretylium may increase the hypotensive activities of Unoprostone.
ValsartanValsartan may increase the hypotensive activities of Bretylium.
VardenafilVardenafil may increase the antihypertensive activities of Bretylium.
VerapamilBretylium may increase the bradycardic activities of Verapamil.
VerapamilThe risk or severity of adverse effects can be increased when Verapamil is combined with Bretylium.
XylometazolineBretylium may increase the hypotensive activities of Xylometazoline.
YohimbineYohimbine may decrease the antihypertensive activities of Bretylium.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Steroid hormone binding
Specific Function:
This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates the electrochemical gradient of sodium and potassium ions, providing the energy for active transport of various nutrients.
Gene Name:
ATP1A1
Uniprot ID:
P05023
Molecular Weight:
112895.01 Da
References
  1. Dzimiri N, Almotrefi AA: Inhibition of myocardial Na(+)-K(+)-ATPase activity by bretylium: role of potassium. Arch Int Pharmacodyn Ther. 1992 Jul-Aug;318:76-85. [PubMed:1334399 ]
  2. Helms JB, Arnett KL, Gatto C, Milanick MA: Bretylium, an organic quaternary amine, inhibits the Na,K-ATPase by binding to the extracellular K-site. Blood Cells Mol Dis. 2004 May-Jun;32(3):394-400. [PubMed:15121098 ]
  3. Dzimiri N, Almotrefi AA: Interaction of bretylium tosylate with guinea-pig myocardial Na(+)-K(+)-ATPase. Gen Pharmacol. 1991;22(5):935-8. [PubMed:1662173 ]
  4. Tiku PE, Nowell PT: Selective inhibition of K(+)-stimulation of Na,K-ATPase by bretylium. Br J Pharmacol. 1991 Dec;104(4):895-900. [PubMed:1667290 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23