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Identification
NameLabetalol
Accession NumberDB00598  (APRD01062)
TypeSmall Molecule
GroupsApproved
Description

Blocker of both alpha- and beta-adrenergic receptors that is used as an antihypertensive. [PubChem]

Structure
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Synonyms
SynonymLanguageCode
3-Carboxamido-4-hydroxy-alpha-((1-methyl-3-phenylpropylamino)methyl)benzyl alcoholNot AvailableNot Available
5-(1-Hydroxy-2-(1-methyl-3-phenylpropylamino)ethyl)salicylamideNot AvailableNot Available
LabetalolNot AvailableNot Available
LabetalolumLatinINN
LabetololNot AvailableNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Labetalol Hydrochloridetablet100 mgoralCounty Line Pharmaceuticals LLC2014-12-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet200 mgoralCounty Line Pharmaceuticals LLC2014-12-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet300 mgoralCounty Line Pharmaceuticals LLC2014-12-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Trandatetablet100 mgoralPrometheus Laboratories Inc.1984-05-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Trandatetablet200 mgoralPrometheus Laboratories Inc.1984-05-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Trandatetablet300 mgoralPrometheus Laboratories Inc.1984-05-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Trandatetablet100 mgoralPaladin Labs IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Trandatetablet200 mgoralPaladin Labs IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Labetalol Hydrochloridetablet, film coated100 mgoralIVAX Pharmaceuticals, Inc.1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralIVAX Pharmaceuticals, Inc.1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated300 mgoralIVAX Pharmaceuticals, Inc.1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochlorideinjection, solution5 mg/mLintravenousHospira, Inc.2013-07-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochlorideinjection, solution5 mg/mLintravenousHospira, Inc.1999-11-29Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochlorideinjection, solution5 mg/mLintravenousHospira, Inc.1999-11-29Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated100 mgoralWatson Laboratories, Inc.1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralWatson Laboratories, Inc.1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated300 mgoralWatson Laboratories, Inc.1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-01-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated100 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2011-01-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2011-01-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated300 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2011-01-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet100 mgoralMajor Pharmaceuticals2009-06-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet200 mgoralMajor Pharmaceuticals2009-06-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet300 mgoralMajor Pharmaceuticals2009-06-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated300 mgoralSTAT Rx USA LLC1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochlorideinjection, solution5 mg/mLintravenousAkorn, Inc.2004-09-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated100 mgoralRebel Distributors Corp1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated300 mgoralRebel Distributors Corp1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralRebel Distributors Corp1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalolinjection5 mg/mLintravenousSagent Pharmaceuticals2010-02-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated100 mgoralLake Erie Medical DBA Quality Care Products LLC1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated100 mgoralREMEDYREPACK INC.2010-11-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet300 mgoralREMEDYREPACK INC.2011-06-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet200 mgoralREMEDYREPACK INC.2011-09-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated100 mgoralUnit Dose Services1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralUnit Dose Services1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated100 mgoralREMEDYREPACK INC.2013-06-04Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralPhysicians Total Care, Inc.2003-08-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated300 mgoralPhysicians Total Care, Inc.2004-08-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated100 mgoralPhysicians Total Care, Inc.2004-05-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochlorideinjection, solution5 mg/mLintravenousCardinal Health1999-11-29Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet200 mgoralCardinal Health2009-06-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralCardinal Health2011-03-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet100 mgoralCardinal Health2009-06-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated100 mgoralCardinal Health2011-01-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralCardinal Health2011-01-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetaloltablet, film coated100 mgoralSun Pharmaceutical Industries, Inc.1999-07-29Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetaloltablet, film coated200 mgoralSun Pharmaceutical Industries, Inc.1999-07-29Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetaloltablet, film coated300 mgoralSun Pharmaceutical Industries, Inc.1999-07-29Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated100 mgoralGolden State Medical Supply, Inc.2013-04-16Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralGolden State Medical Supply, Inc.2013-04-16Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated300 mgoralGolden State Medical Supply, Inc.2013-04-16Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated100 mgoralSt Marys Medical Park Pharmacy2014-01-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralSt Marys Medical Park Pharmacy2014-01-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralbryant ranch prepack1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated300 mgoralbryant ranch prepack1998-08-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochlorideinjection, solution5 mg/mLintravenousMylan Institutional LLC2012-06-29Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochlorideinjection, solution5 mg/mLintravenousGland Pharma Limited2012-04-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated100 mgoralAmerican Health Packaging2011-03-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralAmerican Health Packaging2011-03-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated300 mgoralAmerican Health Packaging2011-03-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralDispensing Solutions, Inc.2011-01-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Labetalol Hydrochloridetablet, film coated200 mgoralMc Kesson Contract Packaging2012-03-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter ProductsNot Available
International Brands
NameCompany
AlbetolLeiras
LatolStandard
NormadateGlaxoSmithKline
NormodyneSchering
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Labetalol Hydrochloride
Thumb
  • InChI Key: WQVZLXWQESQGIF-UHFFFAOYNA-N
  • Monoisotopic Mass: 364.155370383
  • Average Mass: 364.866
DBSALT000320
Categories
CAS number36894-69-6
WeightAverage: 328.4055
Monoisotopic: 328.178692644
Chemical FormulaC19H24N2O3
InChI KeySGUAFYQXFOLMHL-UHFFFAOYSA-N
InChI
InChI=1S/C19H24N2O3/c1-13(7-8-14-5-3-2-4-6-14)21-12-18(23)15-9-10-17(22)16(11-15)19(20)24/h2-6,9-11,13,18,21-23H,7-8,12H2,1H3,(H2,20,24)
IUPAC Name
2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide
SMILES
CC(CCC1=CC=CC=C1)NCC(O)C1=CC(C(N)=O)=C(O)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as salicylamides. These are carboxamide derivatives of salicylic acid. Salicylic acid is the ortho-hydroxylated derivative of benzoic acid.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBenzoic acids and derivatives
Direct ParentSalicylamides
Alternative Parents
Substituents
  • Salicylamide
  • Phenylpropylamine
  • Benzamide
  • Benzoyl
  • Aralkylamine
  • Phenol
  • Vinylogous acid
  • Secondary alcohol
  • Primary carboxylic acid amide
  • Carboxamide group
  • 1,2-aminoalcohol
  • Secondary amine
  • Secondary aliphatic amine
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Aromatic alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the management of hypertension (alone or in combination with other classes of antihypertensive agents), as well as chronic stable angina pectoris and sympathetic overactivity syndrome associated with severe tetanus. Labetalol is used parenterally for immediate reduction in blood pressure in severe hypertension or in hypertensive crises when considered an emergency, for the control of blood pressure in patients with pheochromocytoma and pregnant women with preeclampsia, and to produce controlled hypotension during anesthesia to reduce bleeding resulting from surgical procedures.
PharmacodynamicsLabetalol is an selective alpha-1 and non-selective beta adrenergic blocker used to treat high blood pressure. It works by blocking these adrenergic receptors, which slows sinus heart rate, decreases peripheral vascular resistance, and decreases cardiac output. Labetalol has two asymmetric centers and therefore, exists as a molecular complex of two diastereoisomeric pairs. Dilevalol, the R,R' stereoisomer, makes up 25% of racemic labetalol.
Mechanism of actionLabetalol HCl combines both selective, competitive, alpha-1-adrenergic blocking and nonselective, competitive, beta-adrenergic blocking activity in a single substance. In man, the ratios of alpha- to beta- blockade have been estimated to be approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively. The principal physiologic action of labetalol is to competitively block adrenergic stimulation of β-receptors within the myocardium (β1-receptors) and within bronchial and vascular smooth muscle (β2-receptors), and α1-receptors within vascular smooth muscle. This causes a decrease in systemic arterial blood pressure and systemic vascular resistance without a substantial reduction in resting heart rate, cardiac output, or stroke volume, apparently because of its combined α- and β-adrenergic blocking activity.
AbsorptionCompletely absorbed (100%) from the gastrointestinal tract with peak plasma levels occurring 1 to 2 hours after oral administration. The absolute bioavailability of labetalol is increased when administered with food.
Volume of distributionNot Available
Protein binding50%
Metabolism

Primarily hepatic, undergoes significant first pass metabolism

Route of eliminationThese metabolites are present in plasma and are excreted in the urine, and via the bile, into the feces.
Half life6-8 hours
ClearanceNot Available
ToxicityLD50 = 66 mg/kg (Rat, IV). Side effects or adverse reactions include dizziness when standing up, very low blood pressure, severely slow heartbeat, weakness, diminished sexual function, fatigue
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+0.9943
Blood Brain Barrier-0.8313
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.7073
P-glycoprotein inhibitor INon-inhibitor0.8908
P-glycoprotein inhibitor IINon-inhibitor0.9269
Renal organic cation transporterNon-inhibitor0.8457
CYP450 2C9 substrateNon-substrate0.7448
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateNon-substrate0.6202
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 substrateNon-inhibitor0.9071
CYP450 2D6 substrateInhibitor0.8932
CYP450 2C19 substrateInhibitor0.8995
CYP450 3A4 substrateNon-inhibitor0.8256
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8383
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.9189
BiodegradationNot ready biodegradable0.945
Rat acute toxicity2.1174 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9501
hERG inhibition (predictor II)Non-inhibitor0.7398
Pharmacoeconomics
Manufacturers
  • Apothecon inc div bristol myers squibb
  • Bedford laboratories div ben venue laboratories inc
  • Claris lifesciences ltd
  • Hospira inc
  • Taylor pharmaceuticals
  • Sagent strides llc
  • Schering corp sub schering plough corp
  • Prometheus laboratories inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mutual pharmaceutical co inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Injectionintravenous5 mg/mL
Injection, solutionintravenous5 mg/mL
Tabletoral100 mg
Tabletoral200 mg
Tabletoral300 mg
Tablet, film coatedoral100 mg
Tablet, film coatedoral200 mg
Tablet, film coatedoral300 mg
Prices
Unit descriptionCostUnit
Labetalol Hydrochloride 5 mg/ml1.36USD ml
Trandate 300 mg tablet1.28USD tablet
Trandate 5 mg/ml vial1.25USD ml
Trandate 200 mg tablet1.08USD tablet
Labetalol hcl 300 mg tablet1.02USD tablet
Normodyne 200 mg tablet1.0USD tablet
Labetalol hcl 200 mg tablet0.76USD tablet
Trandate 100 mg tablet0.68USD tablet
Labetalol hcl 100 mg tablet0.53USD tablet
Trandate 200 mg Tablet0.47USD tablet
Trandate 100 mg Tablet0.27USD tablet
Labetalol hcl 5 mg/ml vial0.1USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point188 °CU.S. Patent 4,012,444.
water solubility117 mg/L (at 25 °C)MCFARLAND,JW ET AL. (2001)
logP3.09HANSCH,C ET AL. (1995)
Caco2 permeability-5.03ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.00578 mg/mLALOGPS
logP1.73ALOGPS
logP1.89ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)8.05ChemAxon
pKa (Strongest Basic)9.8ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area95.58 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity94.72 m3·mol-1ChemAxon
Polarizability36.83 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraMS
References
Synthesis Reference

U.S. Patent 4,012,444.

General ReferenceNot Available
External Links
ATC CodesC07AG01
AHFS Codes
  • 24:24.00
PDB EntriesNot Available
FDA labelDownload (401 KB)
MSDSDownload (53.7 KB)
Interactions
Drug Interactions
Drug
AcetylcholineBeta-Blockers may enhance the adverse/toxic effect of Cholinergic Agonists. Of particular concern are the potential for cardiac conduction abnormalities and bronchoconstriction.
AmifostineAntihypertensives may enhance the hypotensive effect of Amifostine.
AminophyllineMay enhance the adverse/toxic effect of other Sympathomimetics.
AmiodaroneMay enhance the bradycardic effect of Beta-Blockers. Possibly to the point of cardiac arrest. Amiodarone may increase the serum concentration of Beta-Blockers.
AmphetamineMay enhance the adverse/toxic effect of other Sympathomimetics.
ArformoterolMay enhance the adverse/toxic effect of other Sympathomimetics.
armodafinilMay enhance the adverse/toxic effect of other Sympathomimetics.
ArticaineMay enhance the adverse/toxic effect of other Sympathomimetics.
AtomoxetineAtoMOXetine may enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics.
BenzphetamineMay enhance the adverse/toxic effect of other Sympathomimetics.
BretyliumMay enhance the bradycardic effect of Bradycardia-Causing Agents. Bretylium may also enhance atrioventricular (AV) blockade in patients receiving AV blocking agents.
BupivacaineBeta-Blockers may increase the serum concentration of Bupivacaine.
ButabarbitalMay decrease the serum concentration of Beta-Blockers.
ButethalMay decrease the serum concentration of Beta-Blockers.
CaffeineMay enhance the adverse/toxic effect of other Sympathomimetics.
CarbacholBeta-Blockers may enhance the adverse/toxic effect of Cholinergic Agonists. Of particular concern are the potential for cardiac conduction abnormalities and bronchoconstriction.
CocaineMay enhance the adverse/toxic effect of other Sympathomimetics.
DexmethylphenidateMay enhance the adverse/toxic effect of other Sympathomimetics.
DextroamphetamineMay enhance the adverse/toxic effect of other Sympathomimetics.
DiazoxideMay enhance the hypotensive effect of Antihypertensives.
DiethylpropionMay enhance the adverse/toxic effect of other Sympathomimetics.
DihydrocodeineMay enhance the adverse/toxic effect of other Sympathomimetics.
DipivefrinMay enhance the adverse/toxic effect of other Sympathomimetics.
DipyridamoleMay enhance the bradycardic effect of Beta-Blockers.
DisopyramideMay enhance the bradycardic effect of Beta-Blockers. Beta-Blockers may enhance the negative inotropic effect of Disopyramide.
DobutamineMay enhance the adverse/toxic effect of other Sympathomimetics.
DopamineMay enhance the adverse/toxic effect of other Sympathomimetics.
DoxapramMay enhance the adverse/toxic effect of other Sympathomimetics.
DronabinolCannabinoid-Containing Products may enhance the tachycardic effect of Sympathomimetics.
DronedaroneMay enhance the bradycardic effect of Beta-Blockers. Dronedarone may increase the serum concentration of Beta-Blockers. This likely applies only to those agents that are metabolized by CYP2D6.
DuloxetineHypotensive Agents may enhance the orthostatic hypotensive effect of DULoxetine.
FenoterolMay enhance the adverse/toxic effect of other Sympathomimetics.
FingolimodBeta-Blockers may enhance the bradycardic effect of Fingolimod.
FloctafenineMay enhance the adverse/toxic effect of Beta-Blockers.
Fluticasone furoateMay enhance the adverse/toxic effect of other Sympathomimetics.
FormoterolMay enhance the adverse/toxic effect of other Sympathomimetics.
HeptabarbitalMay decrease the serum concentration of Beta-Blockers.
HexobarbitalMay decrease the serum concentration of Beta-Blockers.
IndacaterolMay enhance the adverse/toxic effect of other Sympathomimetics.
IobenguaneMay diminish the therapeutic effect of Iobenguane I 123.
Ipratropium bromideMay enhance the adverse/toxic effect of other Sympathomimetics.
IsomethepteneMay enhance the adverse/toxic effect of other Sympathomimetics.
LacosamideBradycardia-Causing Agents may enhance the AV-blocking effect of Lacosamide.
LevonordefrinMay enhance the adverse/toxic effect of other Sympathomimetics.
LinezolidLinezolid may enhance the hypertensive effect of Sympathomimetics.
LisdexamfetamineMay enhance the adverse/toxic effect of other Sympathomimetics.
MepivacaineBeta-Blockers may increase the serum concentration of Mepivacaine.
MethacholineBeta-Blockers may enhance the adverse/toxic effect of Methacholine.
MethamphetamineMay enhance the adverse/toxic effect of other Sympathomimetics.
MethohexitalMay decrease the serum concentration of Beta-Blockers.
MethylphenidateMay enhance the adverse/toxic effect of other Sympathomimetics.
MidodrineMay enhance the adverse/toxic effect of other Sympathomimetics.
ModafinilMay enhance the adverse/toxic effect of other Sympathomimetics.
NabiloneCannabinoid-Containing Products may enhance the tachycardic effect of Sympathomimetics.
NaphazolineMay enhance the adverse/toxic effect of other Sympathomimetics.
NorepinephrineMay enhance the adverse/toxic effect of other Sympathomimetics.
ObinutuzumabAntihypertensives may enhance the hypotensive effect of Obinutuzumab.
OrciprenalineMay enhance the adverse/toxic effect of other Sympathomimetics.
OxymetazolineMay enhance the adverse/toxic effect of other Sympathomimetics.
PentobarbitalMay decrease the serum concentration of Beta-Blockers.
PentoxifyllineMay enhance the hypotensive effect of Antihypertensives.
PhendimetrazineMay enhance the adverse/toxic effect of other Sympathomimetics.
PheniramineMay enhance the adverse/toxic effect of other Sympathomimetics.
PhentermineMay enhance the adverse/toxic effect of other Sympathomimetics.
PhenylephrineMay enhance the adverse/toxic effect of other Sympathomimetics.
PirbuterolMay enhance the adverse/toxic effect of other Sympathomimetics.
PrimidoneMay decrease the serum concentration of Beta-Blockers.
PropafenoneMay increase the serum concentration of Beta-Blockers. Propafenone possesses some independent beta blocking activity.
PropylhexedrineMay enhance the adverse/toxic effect of other Sympathomimetics.
PseudoephedrineMay enhance the adverse/toxic effect of other Sympathomimetics.
RegorafenibMay enhance the bradycardic effect of Beta-Blockers.
ReserpineMay enhance the hypotensive effect of Beta-Blockers.
RisperidoneHypotensive Agents may enhance the hypotensive effect of RisperiDONE.
RituximabAntihypertensives may enhance the hypotensive effect of RiTUXimab.
RivastigmineMay enhance the bradycardic effect of Beta-Blockers.
RuxolitinibMay enhance the bradycardic effect of Bradycardia-Causing Agents.
SalbutamolMay enhance the adverse/toxic effect of other Sympathomimetics.
SalmeterolMay enhance the adverse/toxic effect of other Sympathomimetics.
SecobarbitalMay decrease the serum concentration of Beta-Blockers.
TadalafilMay enhance the antihypertensive effect of Antihypertensives.
Tedizolid PhosphateTedizolid may enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics.
TerbutalineMay enhance the adverse/toxic effect of other Sympathomimetics.
TheophyllineMay enhance the adverse/toxic effect of other Sympathomimetics.
TofacitinibMay enhance the bradycardic effect of Bradycardia-Causing Agents.
TriprolidineMay enhance the adverse/toxic effect of other Sympathomimetics.
VardenafilMay enhance the antihypertensive effect of Antihypertensives.
YohimbineMay diminish the antihypertensive effect of Antihypertensives.
Food Interactions
  • Take without regard to meals.

Targets

1. Beta-1 adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Beta-1 adrenergic receptor P08588 Details

References:

  1. Riva E, Mennini T, Latini R: The alpha- and beta-adrenoceptor blocking activities of labetalol and its RR-SR (50:50) stereoisomers. Br J Pharmacol. 1991 Dec;104(4):823-8. Pubmed
  2. Monopoli A, Bamonte F, Forlani A, Ongini E, Parravicini L: Effects of the R, R-isomer of labetalol, SCH 19927, in isolated tissues and in spontaneously hypertensive rats during a repeated treatment. Arch Int Pharmacodyn Ther. 1984 Dec;272(2):256-63. Pubmed
  3. Sassard J, Zech PY, Pozet N, Cuisinaud G, Vincent M: [Comparative effects of an alpha 1 and beta 1-2 blocker (labetalol) and a beta-1 blocker (atenolol) in the hypertensive patient] J Pharmacol. 1983;14 Suppl 2:121-9. Pubmed
  4. Nakagawa Y, Takeda K, Sakurai H, Mitomi A, Imai S: [Antihypertensive effects of labetalol in three types of hypertensive models of rats (author’s transl)] Nippon Yakurigaku Zasshi. 1981 Apr;77(4):435-45. Pubmed
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  6. Pujos E, Cren-Olive C, Paisse O, Flament-Waton MM, Grenier-Loustalot MF: Comparison of the analysis of beta-blockers by different techniques. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Dec 1;877(31):4007-14. Epub 2009 Oct 17. Pubmed
  7. Rosendorff C: Beta-blocking agents with vasodilator activity. J Hypertens Suppl. 1993 Jun;11(4):S37-40. Pubmed
  8. van Zwieten PA: An overview of the pharmacodynamic properties and therapeutic potential of combined alpha- and beta-adrenoceptor antagonists. Drugs. 1993 Apr;45(4):509-17. Pubmed

2. Beta-2 adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Beta-2 adrenergic receptor P07550 Details

References:

  1. Doggrell SA: The effects of labetalol and dilevalol on isolated cardiovascular preparations of the guinea-pig and rat. J Pharm Pharmacol. 1992 Dec;44(12):1001-6. Pubmed
  2. Doggrell SA: Relaxant and beta 2-adrenoceptor blocking activities of labetalol, dilevalol, amosulalol and KF-4317 on the rat isolated aorta. J Pharm Pharmacol. 1988 Nov;40(11):812-5. Pubmed
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  4. Sassard J, Zech PY, Pozet N, Cuisinaud G, Vincent M: [Comparative effects of an alpha 1 and beta 1-2 blocker (labetalol) and a beta-1 blocker (atenolol) in the hypertensive patient] J Pharmacol. 1983;14 Suppl 2:121-9. Pubmed
  5. Pujos E, Cren-Olive C, Paisse O, Flament-Waton MM, Grenier-Loustalot MF: Comparison of the analysis of beta-blockers by different techniques. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Dec 1;877(31):4007-14. Epub 2009 Oct 17. Pubmed
  6. Rosendorff C: Beta-blocking agents with vasodilator activity. J Hypertens Suppl. 1993 Jun;11(4):S37-40. Pubmed
  7. van Zwieten PA: An overview of the pharmacodynamic properties and therapeutic potential of combined alpha- and beta-adrenoceptor antagonists. Drugs. 1993 Apr;45(4):509-17. Pubmed

3. Alpha-1 adrenergic receptor

Kind: protein group

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Alpha-1A adrenergic receptor P35348 Details
Alpha-1B adrenergic receptor P35368 Details
Alpha-1D adrenergic receptor P25100 Details

References:

  1. Bernstein JS, Ebert TJ, Stowe DF, Schmeling WT, Nelson MA, Woods MP: Partial attenuation of hemodynamic responses to rapid sequence induction and intubation with labetalol. J Clin Anesth. 1989;1(6):444-51. Pubmed
  2. Nakamura T, Maruyama K, Ohnuki T, Hattori K, Watanabe K, Nagatomo T: Tamsulosin: assessment of affinityof (3)H-P razosin binding to two alpha-1- adrenoceptor subtypes in the canine aorta. Pharmacology. 1999 Nov;59(5):234-8. Pubmed
  3. Sassard J, Zech PY, Pozet N, Cuisinaud G, Vincent M: [Comparative effects of an alpha 1 and beta 1-2 blocker (labetalol) and a beta-1 blocker (atenolol) in the hypertensive patient] J Pharmacol. 1983;14 Suppl 2:121-9. Pubmed
  4. Pedersen ME, Cockcroft JR: The vasodilatory beta-blockers. Curr Hypertens Rep. 2007 Aug;9(4):269-77. Pubmed
  5. Shiraishi K, Moriya M, Miyake N, Takayanagi I: Alpha 1-adrenoceptor blocking activities of bevantolol hydrochloride(NC-1400) and labetalol in rat isolated thoracic aorta—do they distinguish between subtypes? Gen Pharmacol. 1992 Sep;23(5):843-5. Pubmed
  6. Rosendorff C: Beta-blocking agents with vasodilator activity. J Hypertens Suppl. 1993 Jun;11(4):S37-40. Pubmed
  7. van Zwieten PA: An overview of the pharmacodynamic properties and therapeutic potential of combined alpha- and beta-adrenoceptor antagonists. Drugs. 1993 Apr;45(4):509-17. Pubmed

Enzymes

1. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

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. Epub 2009 Nov 24. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on May 05, 2014 12:21