Details of the Drug

General Information of Drug (ID: DMK8U72)

Drug Name
Labetalol
Synonyms
Albetol; Ibidomide; Labetalolum; Labetolol; NORMOZIDE; AH 5158; AH-5158; Labetalol (INN); Labetalol [INN:BAN]; Labetalolum [INN-Latin]; Normodyne (TN); Sch-19927; Trandate (TN); 2-Hydroxy-5-(1-hydroxy-2-((1-methyl-3-phenylpropyl)amino)ethyl)benzamide; 2-hydroxy-5-[1-hydroxy-2-(4-phenylbutan-2-ylamino)ethyl]benzamide; 2-hydroxy-5-{1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl}benzamide; 3-Carboxamido-4-hydroxy-alpha-((1-methyl-3-phenylpropylamino)methyl)benzyl alcohol; 5-(1-Hydroxy-2-(1-methyl-3-phenylpropylamino)ethyl)salicylamide
Indication
Disease Entry ICD 11 Status REF
Hypertension BA00-BA04 Approved [1]
Hypertension, pregnancy-induced N.A. Approved [2]
Malignant essential hypertension BA00 Approved [2]
Therapeutic Class
Antihypertensive Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 328.4
Logarithm of the Partition Coefficient (xlogp) 3.1
Rotatable Bond Count (rotbonds) 8
Hydrogen Bond Donor Count (hbonddonor) 4
Hydrogen Bond Acceptor Count (hbondacc) 4
ADMET Property
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 1.5 h [3]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [4]
Clearance
The clearance of drug is 1500 mL/min (plasma clearance) and 1100 mL/min (whole blood clearance) [5]
Elimination
Radiolabelled doses of labetalol are 55-60% recovered in the urine and 12-27% recovered in the feces [5]
Half-life
The concentration or amount of drug in body reduced by one-half in 1.7 - 6.1 hours [5]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 104.5296 micromolar/kg/day [6]
Unbound Fraction
The unbound fraction of drug in plasma is 0.5% [7]
Vd
The volume of distribution (Vd) of drug is 805 L [5]
Water Solubility
The ability of drug to dissolve in water is measured as 16 mg/mL [4]
Adverse Drug Reaction (ADR)
ADR Term Variation Related DOT DOT ID REF
Adverse drug reaction Not Available CYP2D6 OTZJC802 [8]
Chemical Identifiers
Formula
C19H24N2O3
IUPAC Name
2-hydroxy-5-[1-hydroxy-2-(4-phenylbutan-2-ylamino)ethyl]benzamide
Canonical SMILES
CC(CCC1=CC=CC=C1)NCC(C2=CC(=C(C=C2)O)C(=O)N)O
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)
InChIKey
SGUAFYQXFOLMHL-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
3869
ChEBI ID
CHEBI:6343
CAS Number
36894-69-6
DrugBank ID
DB00598
TTD ID
D0A8XN
VARIDT ID
DR01385
INTEDE ID
DR0909
ACDINA ID
D00345
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Adrenergic receptor Alpha-1 (ADRA1) TTG28O6 NOUNIPROTAC Antagonist [9]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Substrate [10]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [11]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [12]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [13]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Substrate [14]
UDP-glucuronosyltransferase 2B7 (UGT2B7) DEB3CV1 UD2B7_HUMAN Substrate [13]
UDP-glucuronosyltransferase 1A9 (UGT1A9) DE85D2P UD19_HUMAN Substrate [13]
UDP-glucuronosyltransferase 2B4 (UGT2B4) DENUPDX UD2B4_HUMAN Substrate [13]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Angiotensin-converting enzyme 2 (ACE2) OTTRZGU7 ACE2_HUMAN Gene/Protein Processing [15]
Angiotensinogen (AGT) OTBZLYR3 ANGT_HUMAN Gene/Protein Processing [16]
Beta-1 adrenergic receptor (ADRB1) OTQBWN4U ADRB1_HUMAN Gene/Protein Processing [17]
Beta-2 adrenergic receptor (ADRB2) OTSDOX4Q ADRB2_HUMAN Gene/Protein Processing [17]
Cytochrome P450 2D6 (CYP2D6) OTZJC802 CP2D6_HUMAN Drug Response [8]
Natriuretic peptides A (NPPA) OTMQNTNX ANF_HUMAN Gene/Protein Processing [18]
Phosphatidylcholine translocator ABCB4 (ABCB4) OTE6PY83 MDR3_HUMAN Gene/Protein Processing [19]
Prolactin (PRL) OTWFQGX7 PRL_HUMAN Gene/Protein Processing [20]
Renin (REN) OT52GZR2 RENI_HUMAN Gene/Protein Processing [18]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Labetalol
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Verapamil DMA7PEW Major Increased risk of cardiac depression by the combination of Labetalol and Verapamil. Hypertension [BA00-BA04] [21]
Indapamide DMGN1PW Moderate Increased risk of ventricular arrhythmias by the combination of Labetalol and Indapamide. Hypertension [BA00-BA04] [22]
Trichlormethiazide DMHAQCO Moderate Increased risk of ventricular arrhythmias by the combination of Labetalol and Trichlormethiazide. Hypertension [BA00-BA04] [22]
Felodipine DMOSW35 Moderate Increased risk of cardiac depression by the combination of Labetalol and Felodipine. Hypertension [BA00-BA04] [21]
Hydralazine DMU8JGH Minor Decreased metabolism of Labetalol caused by Hydralazine mediated interference with first-pass metabolism. Hypertension [BA00-BA04] [23]
Hydrochlorothiazide DMUSZHD Moderate Increased risk of hypertriglyceridemia by the combination of Labetalol and Hydrochlorothiazide. Hypertension [BA00-BA04] [22]
Clevidipine butyrate DMW4M97 Moderate Increased risk of cardiac depression by the combination of Labetalol and Clevidipine butyrate. Hypertension [BA00-BA04] [21]
⏷ Show the Full List of 7 DDI Information of This Drug
Coadministration of a Drug Treating the Disease Different from Labetalol (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Labetalol and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [24]
Arn-509 DMT81LZ Moderate Accelerated clearance of Labetalol due to the transporter induction by Arn-509. Acute myeloid leukaemia [2A60] [25]
Scopolamine DMOM8AL Moderate Altered absorption of Labetalol due to GI dynamics variation caused by Scopolamine. Addictive disorder [6C50-6C5Z] [25]
Bepridil DM0RKS4 Moderate Increased risk of cardiac depression by the combination of Labetalol and Bepridil. Angina pectoris [BA40] [21]
Nifedipine DMSVOZT Moderate Increased risk of cardiac depression by the combination of Labetalol and Nifedipine. Angina pectoris [BA40] [21]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Labetalol and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [26]
Methylphenobarbital DMDSWAG Moderate Increased metabolism of Labetalol caused by Methylphenobarbital mediated induction of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [27]
Oxazepam DMXNZM4 Minor Decreased metabolism of Labetalol caused by Oxazepam. Anxiety disorder [6B00-6B0Z] [28]
Zileuton DMVRIC2 Moderate Decreased metabolism of Labetalol caused by Zileuton. Asthma [CA23] [29]
Cariprazine DMJYDVK Moderate Additive hypotensive effects by the combination of Labetalol and Cariprazine. Bipolar disorder [6A60] [30]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Labetalol and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [31]
Atracurium DM42HXN Moderate Additive cardiorespiratory depression effects by the combination of Labetalol and Atracurium. Corneal disease [9A76-9A78] [32]
Mivacurium DM473VD Moderate Additive neuromuscular blocking effects by the combination of Labetalol and Mivacurium. Corneal disease [9A76-9A78] [32]
Pancuronium DMB0VY8 Moderate Additive neuromuscular blocking effects by the combination of Labetalol and Pancuronium. Corneal disease [9A76-9A78] [32]
Tubocurarine DMBZIVP Moderate Additive neuromuscular blocking effects by the combination of Labetalol and Tubocurarine. Corneal disease [9A76-9A78] [32]
Pasireotide DMHM7JS Moderate Increased risk of atrioventricular block by the combination of Labetalol and Pasireotide. Cushing syndrome [5A70] [33]
Sertraline DM0FB1J Moderate Decreased metabolism of Labetalol caused by Sertraline mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [34]
Trimipramine DM1SC8M Moderate Increased plasma concentrations of Labetalol and Trimipramine due to competitive inhibition of the same metabolic pathway. Depression [6A70-6A7Z] [35]
Paroxetine DM5PVQE Moderate Decreased metabolism of Labetalol caused by Paroxetine mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [34]
OPC-34712 DMHG57U Moderate Additive hypotensive effects by the combination of Labetalol and OPC-34712. Depression [6A70-6A7Z] [30]
Clomipramine DMINRKW Moderate Increased plasma concentrations of Labetalol and Clomipramine due to competitive inhibition of the same metabolic pathway. Depression [6A70-6A7Z] [35]
Doxepin DMPI98T Moderate Increased plasma concentrations of Labetalol and Doxepin due to competitive inhibition of the same metabolic pathway. Depression [6A70-6A7Z] [35]
Mepenzolate DM8YU2F Moderate Altered absorption of Labetalol due to GI dynamics variation caused by Mepenzolate. Digestive system disease [DE2Z] [25]
Oxybutynine DMJPBAX Moderate Altered absorption of Labetalol due to GI dynamics variation caused by Oxybutynine. Discovery agent [N.A.] [25]
Diazepam DM08E9O Minor Decreased metabolism of Labetalol caused by Diazepam. Epilepsy/seizure [8A61-8A6Z] [28]
Primidone DM0WX6I Moderate Increased metabolism of Labetalol caused by Primidone mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [36]
Phenobarbital DMXZOCG Moderate Increased metabolism of Labetalol caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [36]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Labetalol and Cannabidiol. Epileptic encephalopathy [8A62] [25]
Ethacrynic acid DM60QMR Moderate Increased risk of ventricular arrhythmias by the combination of Labetalol and Ethacrynic acid. Essential hypertension [BA00] [22]
Phenoxybenzamine DM8KSQH Moderate Additive hypotensive effects by the combination of Labetalol and Phenoxybenzamine. Essential hypertension [BA00] [37]
Nicardipine DMCDYW7 Moderate Increased risk of cardiac depression by the combination of Labetalol and Nicardipine. Essential hypertension [BA00] [21]
Tolterodine DMSHPW8 Moderate Altered absorption of Labetalol due to GI dynamics variation caused by Tolterodine. Functional bladder disorder [GC50] [25]
Terbinafine DMI6HUW Moderate Decreased metabolism of Labetalol caused by Terbinafine mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [38]
Propantheline DM2EN6G Moderate Altered absorption of Labetalol due to GI dynamics variation caused by Propantheline. Gastric ulcer [DA60] [25]
Chlorothiazide DMLHESP Moderate Increased risk of ventricular arrhythmias by the combination of Labetalol and Chlorothiazide. Heart failure [BD10-BD1Z] [22]
Furosemide DMMQ8ZG Moderate Increased risk of hypertriglyceridemia by the combination of Labetalol and Furosemide. Heart failure [BD10-BD1Z] [22]
Bumetanide DMRV7H0 Moderate Increased risk of ventricular arrhythmias by the combination of Labetalol and Bumetanide. Heart failure [BD10-BD1Z] [22]
Hydroflumethiazide DMVPUQI Moderate Increased risk of hypertriglyceridemia by the combination of Labetalol and Hydroflumethiazide. Heart failure [BD10-BD1Z] [22]
Rifampin DMA8J1G Moderate Increased metabolism of Labetalol caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [39]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Labetalol and Brentuximab vedotin. Hodgkin lymphoma [2B30] [40]
Efavirenz DMC0GSJ Moderate Increased risk of hepatotoxicity by the combination of Labetalol and Efavirenz. Human immunodeficiency virus disease [1C60-1C62] [41]
Mipomersen DMGSRN1 Major Increased risk of hepatotoxicity by the combination of Labetalol and Mipomersen. Hyper-lipoproteinaemia [5C80] [42]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Labetalol and Teriflunomide. Hyper-lipoproteinaemia [5C80] [33]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Labetalol and BMS-201038. Hyper-lipoproteinaemia [5C80] [43]
Belladonna DM2RBWK Moderate Altered absorption of Labetalol due to GI dynamics variation caused by Belladonna. Infectious gastroenteritis/colitis [1A40] [25]
Amobarbital DM0GQ8N Moderate Increased metabolism of Labetalol caused by Amobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [36]
Propiomazine DMKY8V1 Moderate Additive hypotensive effects by the combination of Labetalol and Propiomazine. Insomnia [7A00-7A0Z] [30]
ITI-007 DMUQ1DO Moderate Additive hypotensive effects by the combination of Labetalol and ITI-007. Insomnia [7A00-7A0Z] [30]
Clidinium DMUMQZ0 Moderate Altered absorption of Labetalol due to GI dynamics variation caused by Clidinium. Irritable bowel syndrome [DD91] [25]
Dicyclomine DMZSDGX Moderate Altered absorption of Labetalol due to GI dynamics variation caused by Dicyclomine. Irritable bowel syndrome [DD91] [25]
Glycerol phenylbutyrate DMDGRQO Moderate Decreased metabolism of Labetalol caused by Glycerol phenylbutyrate mediated inhibition of CYP450 enzyme. Liver disease [DB90-DB9Z] [25]
Lumefantrine DM29GAD Moderate Decreased metabolism of Labetalol caused by Lumefantrine mediated inhibition of CYP450 enzyme. Malaria [1F40-1F45] [24]
Chloroquine DMSI5CB Minor Decreased metabolism of Labetalol caused by Chloroquine mediated inhibition of CYP450 enzyme. Malaria [1F40-1F45] [44]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Labetalol and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [45]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Labetalol and Idelalisib. Mature B-cell leukaemia [2A82] [46]
Clofarabine DMCVJ86 Moderate Increased risk of hepatotoxicity by the combination of Labetalol and Clofarabine. Mature B-cell lymphoma [2A85] [47]
Lanthanum carbonate DMMJQSH Moderate Decreased absorption of Labetalol due to formation of complexes caused by Lanthanum carbonate. Mineral absorption/transport disorder [5C64] [33]
Thalidomide DM70BU5 Moderate Increased risk of ventricular arrhythmias by the combination of Labetalol and Thalidomide. Multiple myeloma [2A83] [24]
Siponimod DM2R86O Major Increased risk of bradycardia by the combination of Labetalol and Siponimod. Multiple sclerosis [8A40] [24]
Fingolimod DM5JVAN Major Increased risk of atrioventricular block by the combination of Labetalol and Fingolimod. Multiple sclerosis [8A40] [48]
Ozanimod DMT6AM2 Moderate Increased risk of atrioventricular block by the combination of Labetalol and Ozanimod. Multiple sclerosis [8A40] [49]
Imatinib DM7RJXL Moderate Decreased metabolism of Labetalol caused by Imatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [50]
Promethazine DM6I5GR Moderate Additive hypotensive effects by the combination of Labetalol and Promethazine. Nausea/vomiting [MD90] [30]
Polythiazide DMCH80F Moderate Increased risk of hyperglycemia by the combination of Labetalol and Polythiazide. Oedema [MG29] [22]
Dextropropoxyphene DM23HCX Moderate Decreased metabolism of Labetalol caused by Dextropropoxyphene mediated inhibition of CYP450 enzyme. Pain [MG30-MG3Z] [51]
Biperiden DME78OA Moderate Altered absorption of Labetalol due to GI dynamics variation caused by Biperiden. Parkinsonism [8A00] [25]
Methylscopolamine DM5VWOB Moderate Altered absorption of Labetalol due to GI dynamics variation caused by Methylscopolamine. Peptic ulcer [DA61] [25]
Enzalutamide DMGL19D Moderate Increased metabolism of Labetalol caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [52]
Terazosin DM3JCVS Moderate Additive hypotensive effects by the combination of Labetalol and Terazosin. Prostate hyperplasia [GA90] [37]
Silodosin DMJSBT6 Moderate Additive hypotensive effects by the combination of Labetalol and Silodosin. Prostate hyperplasia [GA90] [37]
Levomepromazine DMIKFEL Moderate Additive hypotensive effects by the combination of Labetalol and Levomepromazine. Psychotic disorder [6A20-6A25] [30]
Fluphenazine DMIT8LX Moderate Additive hypotensive effects by the combination of Labetalol and Fluphenazine. Psychotic disorder [6A20-6A25] [30]
Leflunomide DMR8ONJ Major Increased risk of hepatotoxicity by the combination of Labetalol and Leflunomide. Rheumatoid arthritis [FA20] [33]
Quetiapine DM1N62C Moderate Additive hypotensive effects by the combination of Labetalol and Quetiapine. Schizophrenia [6A20] [30]
Mesoridazine DM2ZGAN Moderate Additive hypotensive effects by the combination of Labetalol and Mesoridazine. Schizophrenia [6A20] [30]
Thioridazine DM35M8J Moderate Additive hypotensive effects by the combination of Labetalol and Thioridazine. Schizophrenia [6A20] [30]
Aripiprazole DM3NUMH Moderate Additive hypotensive effects by the combination of Labetalol and Aripiprazole. Schizophrenia [6A20] [30]
Iloperidone DM6AUFY Moderate Additive hypotensive effects by the combination of Labetalol and Iloperidone. Schizophrenia [6A20] [30]
Paliperidone DM7NPJS Moderate Additive hypotensive effects by the combination of Labetalol and Paliperidone. Schizophrenia [6A20] [30]
Perphenazine DMA4MRX Moderate Additive hypotensive effects by the combination of Labetalol and Perphenazine. Schizophrenia [6A20] [30]
Molindone DMAH70G Moderate Additive hypotensive effects by the combination of Labetalol and Molindone. Schizophrenia [6A20] [30]
Thiothixene DMDINC4 Moderate Additive hypotensive effects by the combination of Labetalol and Thiothixene. Schizophrenia [6A20] [30]
Trifluoperazine DMKBYWI Moderate Additive hypotensive effects by the combination of Labetalol and Trifluoperazine. Schizophrenia [6A20] [30]
Risperidone DMN6DXL Moderate Additive hypotensive effects by the combination of Labetalol and Risperidone. Schizophrenia [6A20] [30]
Amisulpride DMSJVAM Moderate Increased risk of ventricular arrhythmias by the combination of Labetalol and Amisulpride. Schizophrenia [6A20] [25]
Asenapine DMSQZE2 Moderate Additive hypotensive effects by the combination of Labetalol and Asenapine. Schizophrenia [6A20] [30]
Trabectedin DMG3Y89 Moderate Increased risk of hepatotoxicity by the combination of Labetalol and Trabectedin. Solid tumour/cancer [2A00-2F9Z] [25]
Naltrexone DMUL45H Moderate Increased risk of hepatotoxicity by the combination of Labetalol and Naltrexone. Substance abuse [6C40] [53]
Pipecuronium DM5F84A Moderate Additive neuromuscular blocking effects by the combination of Labetalol and Pipecuronium. Tonus and reflex abnormality [MB47] [32]
Vecuronium DMP0UK2 Moderate Additive neuromuscular blocking effects by the combination of Labetalol and Vecuronium. Tonus and reflex abnormality [MB47] [32]
Rocuronium DMY9BMK Moderate Additive neuromuscular blocking effects by the combination of Labetalol and Rocuronium. Tonus and reflex abnormality [MB47] [32]
Methdilazine DMAUHQX Moderate Additive hypotensive effects by the combination of Labetalol and Methdilazine. Vasomotor/allergic rhinitis [CA08] [30]
Trimeprazine DMEMV9D Moderate Additive hypotensive effects by the combination of Labetalol and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [54]
Amiodarone DMUTEX3 Moderate Increased risk of atrioventricular block by the combination of Labetalol and Amiodarone. Ventricular tachyarrhythmia [BC71] [55]
⏷ Show the Full List of 94 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
FD&C blue no. 1 E00263 19700 Colorant
FD&C blue no. 2 E00446 2723854 Colorant
Kyselina citronova E00014 311 Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
methylparaben E00149 7456 Antimicrobial preservative
Propylparaben sodium E00567 23679044 Antimicrobial preservative
Quinoline yellow WS E00309 24671 Colorant
Sodium benzoate E00432 517055 Antimicrobial preservative; lubricant
Sunset yellow FCF E00255 17730 Colorant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Crospovidone E00626 Not Available Disintegrant
Dextrose anhydrous E00394 107526 Binding agent; Diluent; Flavoring agent; Tonicity agent
Edetate disodium E00186 8759 Complexing agent
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Hypromellose E00634 Not Available Coating agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 3350 E00652 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 400 E00653 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polysorbate 80 E00665 Not Available Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Polyvinyl alcohol E00666 Not Available Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Sodium hydroxide E00234 14798 Alkalizing agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Triacetin E00080 5541 Humectant; Plasticizing agent; Solvent
Water E00035 962 Solvent
Pregelatinized starch E00674 Not Available Binding agent; Diluent; Disintegrant
⏷ Show the Full List of 28 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Labetalol 300 mg tablet 300 mg Oral Tablet Oral
Labetalol Hydrochloride 100mg tablet 100mg Tablet Oral
Labetalol 100 mg tablet 100 mg Oral Tablet Oral
Labetalol 200 mg tablet 200 mg Oral Tablet Oral
Labetalol Hydrochloride 5mg/ml injectable 5mg/ml Injectable Injection
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7207).
2 Labetalol FDA Label
3 European Medicines Agency (EMA): DIACOMIT Summary of Product Characteristics
4 BDDCS applied to over 900 drugs
5 Clinical pharmacokinetics of labetalol. Clin Pharmacokinet. 1984 Mar-Apr;9(2):157-67. doi: 10.2165/00003088-198409020-00003.
6 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
7 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
8 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
9 Beta-blockers in the treatment of hypertension: are there clinically relevant differences Postgrad Med. 2009 May;121(3):90-8.
10 Involvement of influx and efflux transport systems in gastrointestinal absorption of celiprolol. J Pharm Sci. 2009 Jul;98(7):2529-39.
11 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
12 Comparison of verapamil, diltiazem, and labetalol on the bioavailability and metabolism of imipramine. J Clin Pharmacol. 1992 Feb;32(2):176-83.
13 Regulation of UDP-glucuronosyltransferase (UGT) 1A1 by progesterone and its impact on labetalol elimination. Xenobiotica. 2008 Jan;38(1):62-75.
14 Drug Interactions Flockhart Table
15 Prediction of off-target effects on angiotensin-converting enzyme 2. J Biomol Screen. 2011 Sep;16(8):878-85. doi: 10.1177/1087057111413919. Epub 2011 Aug 22.
16 Labetalol (AH5158), a competitive alpha- and beta-receptor blocking drug, in the management of hypertension. Aust N Z J Med. 1976 Aug;6(3 Suppl):83-8. doi: 10.1111/j.1445-5994.1976.tb03341.x.
17 Preclinical pharmacologic properties of dilevalol, an antihypertensive agent possessing selective beta 2 agonist-mediated vasodilation and beta antagonism. Am J Cardiol. 1989 Jun 5;63(19):3I-6I. doi: 10.1016/0002-9149(89)90120-3.
18 Hemodynamic and humoral effects of intravenous dilevalol in patients with moderate hypertension. Am J Cardiol. 1989 Jun 5;63(19):34I-37I. doi: 10.1016/0002-9149(89)90126-4.
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