General Information of Drug (ID: DM6EUL5)

Drug Name
Betaxolol
Synonyms
Betaxololum; Betazolol; KERLEDEX; Kerlone; Betaxolol HCL; SL 75212; Betaxolol (INN); Betaxolol (TN); Betaxolol [INN:BAN]; Betaxololum [INN-Latin]; Betoptic (TN); Betoptic S (TN); Kerlone (TN); Lokren (TN); SL-75212; ALO-1401-02; (+/-)-1-[p-[2-(Cyclopropylmethoxy)ethyl]phenoxy]-3-(isopropylamino)-2-propanol; 1-(4-(2-(Cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-2-propanol; 1-(isopropylamino)-3-[p-(cyclopropylmethoxyethyl)phenoxy]-2-propanol; 1-[(4-{2-[(cyclopropylmethyl)oxy]ethyl}phenyl)oxy]-3-[(1-methylethyl)amino]propan-2-ol; 1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)propan-2-ol; 1-{4-[2-(cyclopropylmethoxy)ethyl]phenoxy}-3-(propan-2-ylamino)propan-2-ol
Indication
Disease Entry ICD 11 Status REF
Hypertension BA00-BA04 Approved [1], [2]
Therapeutic Class
Antihypertensive Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 307.4
Topological Polar Surface Area (xlogp) 2.8
Rotatable Bond Count (rotbonds) 11
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 4
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [3]
Bioavailability
85% of drug becomes completely available to its intended biological destination(s) [4]
Clearance
The drug present in the plasma can be removed from the body at the rate of 3.4 mL/min/kg [5]
Elimination
15% of drug is excreted from urine in the unchanged form [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 14 - 22 hours [5]
Metabolism
The drug is metabolized via the hepatic [6]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 2.16955 micromolar/kg/day [7]
Unbound Fraction
The unbound fraction of drug in plasma is 0.4% [5]
Vd
Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 4.8 L/kg [5]
Water Solubility
The ability of drug to dissolve in water is measured as 0.451 mg/mL [3]
Chemical Identifiers
Formula
C18H29NO3
IUPAC Name
1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)propan-2-ol
Canonical SMILES
CC(C)NCC(COC1=CC=C(C=C1)CCOCC2CC2)O
InChI
InChI=1S/C18H29NO3/c1-14(2)19-11-17(20)13-22-18-7-5-15(6-8-18)9-10-21-12-16-3-4-16/h5-8,14,16-17,19-20H,3-4,9-13H2,1-2H3
InChIKey
NWIUTZDMDHAVTP-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
2369
ChEBI ID
CHEBI:3082
CAS Number
63659-18-7
DrugBank ID
DB00195
TTD ID
D03ROX
INTEDE ID
DR0206
ACDINA ID
D00065

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Adrenergic receptor beta-1 (ADRB1) TTR6W5O ADRB1_HUMAN Antagonist [8], [9]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [10]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [11]
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 Betaxolol
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Nisoldipine DM7ISKJ Moderate Increased risk of cardiac depression by the combination of Betaxolol and Nisoldipine. Hypertension [BA00-BA04] [40]
Levamlodipine DM92S6N Moderate Increased risk of cardiac depression by the combination of Betaxolol and Levamlodipine. Hypertension [BA00-BA04] [41]
Doxazosin DM9PLRH Moderate Additive hypotensive effects by the combination of Betaxolol and Doxazosin. Hypertension [BA00-BA04] [42]
Isradipine DMA5XGH Moderate Increased risk of cardiac depression by the combination of Betaxolol and Isradipine. Hypertension [BA00-BA04] [41]
Verapamil DMA7PEW Major Increased risk of cardiac depression by the combination of Betaxolol and Verapamil. Hypertension [BA00-BA04] [41]
Diltiazem DMAI7ZV Major Increased risk of cardiac depression by the combination of Betaxolol and Diltiazem. Hypertension [BA00-BA04] [41]
Amlodipine DMBDAZV Moderate Increased risk of cardiac depression by the combination of Betaxolol and Amlodipine. Hypertension [BA00-BA04] [41]
Indapamide DMGN1PW Moderate Increased risk of ventricular arrhythmias by the combination of Betaxolol and Indapamide. Hypertension [BA00-BA04] [43]
Trichlormethiazide DMHAQCO Moderate Increased risk of hypertriglyceridemia by the combination of Betaxolol and Trichlormethiazide. Hypertension [BA00-BA04] [43]
Felodipine DMOSW35 Moderate Increased risk of cardiac depression by the combination of Betaxolol and Felodipine. Hypertension [BA00-BA04] [41]
Hydrochlorothiazide DMUSZHD Moderate Increased risk of ventricular arrhythmias by the combination of Betaxolol and Hydrochlorothiazide. Hypertension [BA00-BA04] [43]
Clevidipine butyrate DMW4M97 Moderate Increased risk of cardiac depression by the combination of Betaxolol and Clevidipine butyrate. Hypertension [BA00-BA04] [41]
⏷ Show the Full List of 12 DDI Information of This Drug
Coadministration of a Drug Treating the Disease Different from Betaxolol (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Sucralfate DMP9HBO Minor Decreased absorption of Betaxolol due to formation of complexes caused by Sucralfate. Acne vulgaris [ED80] [44]
Scopolamine DMOM8AL Moderate Altered absorption of Betaxolol due to GI dynamics variation caused by Scopolamine. Addictive disorder [6C50-6C5Z] [45]
Bepridil DM0RKS4 Moderate Increased risk of cardiac depression by the combination of Betaxolol and Bepridil. Angina pectoris [BA40] [41]
Dronedarone DMA8FS5 Moderate Increased risk of atrioventricular block by the combination of Betaxolol and Dronedarone. Angina pectoris [BA40] [46]
Nifedipine DMSVOZT Moderate Increased risk of cardiac depression by the combination of Betaxolol and Nifedipine. Angina pectoris [BA40] [41]
Promazine DMZAL7W Moderate Additive hypotensive effects by the combination of Betaxolol and Promazine. Appearance/behaviour symptom [MB23] [47]
Zileuton DMVRIC2 Moderate Decreased metabolism of Betaxolol caused by Zileuton. Asthma [CA23] [48]
Cariprazine DMJYDVK Moderate Additive hypotensive effects by the combination of Betaxolol and Cariprazine. Bipolar disorder [6A60] [47]
Atracurium DM42HXN Moderate Additive neuromuscular blocking effects by the combination of Betaxolol and Atracurium. Corneal disease [9A76-9A78] [49]
Mivacurium DM473VD Moderate Additive neuromuscular blocking effects by the combination of Betaxolol and Mivacurium. Corneal disease [9A76-9A78] [49]
Pancuronium DMB0VY8 Moderate Additive neuromuscular blocking effects by the combination of Betaxolol and Pancuronium. Corneal disease [9A76-9A78] [49]
Tubocurarine DMBZIVP Moderate Additive neuromuscular blocking effects by the combination of Betaxolol and Tubocurarine. Corneal disease [9A76-9A78] [49]
Nimodipine DMQ0RKZ Moderate Increased risk of cardiac depression by the combination of Betaxolol and Nimodipine. Coronary vasospastic disease [BA85] [41]
Pasireotide DMHM7JS Moderate Increased risk of bradycardia by the combination of Betaxolol and Pasireotide. Cushing syndrome [5A70] [50]
OPC-34712 DMHG57U Moderate Additive hypotensive effects by the combination of Betaxolol and OPC-34712. Depression [6A70-6A7Z] [47]
Hyoscyamine DM804UR Moderate Antagonize the effect of Betaxolol when combined with Hyoscyamine. Digestive system disease [DE2Z] [45]
Mepenzolate DM8YU2F Moderate Antagonize the effect of Betaxolol when combined with Mepenzolate. Digestive system disease [DE2Z] [45]
Oxybutynine DMJPBAX Moderate Altered absorption of Betaxolol due to GI dynamics variation caused by Oxybutynine. Discovery agent [N.A.] [45]
Trihexyphenidyl DMB19L8 Moderate Antagonize the effect of Betaxolol when combined with Trihexyphenidyl. Dystonic disorder [8A02] [45]
Bendroflumethiazide DM7EVLC Moderate Increased risk of hypertriglyceridemia by the combination of Betaxolol and Bendroflumethiazide. Essential hypertension [BA00] [43]
Phenoxybenzamine DM8KSQH Moderate Additive hypotensive effects by the combination of Betaxolol and Phenoxybenzamine. Essential hypertension [BA00] [42]
Nicardipine DMCDYW7 Moderate Increased risk of cardiac depression by the combination of Betaxolol and Nicardipine. Essential hypertension [BA00] [41]
Benzthiazide DMQWZ0H Moderate Increased risk of hyperglycemia by the combination of Betaxolol and Benzthiazide. Essential hypertension [BA00] [43]
Phenylephrine DMZHUO5 Moderate Additive hypertensive effects by the combination of Betaxolol and Phenylephrine. Faecal incontinence [ME07] [51]
Tolterodine DMSHPW8 Moderate Altered absorption of Betaxolol due to GI dynamics variation caused by Tolterodine. Functional bladder disorder [GC50] [45]
Propantheline DM2EN6G Moderate Altered absorption of Betaxolol due to GI dynamics variation caused by Propantheline. Gastric ulcer [DA60] [45]
Cimetidine DMH61ZB Moderate Decreased metabolism of Betaxolol caused by Cimetidine mediated inhibition of CYP450 enzyme. Gastro-oesophageal reflux disease [DA22] [52]
Spironolactone DM2AQ5N Moderate Increased risk of hyperglycemia by the combination of Betaxolol and Spironolactone. Heart failure [BD10-BD1Z] [43]
Triamterene DM2HU9I Moderate Increased risk of hyperglycemia by the combination of Betaxolol and Triamterene. Heart failure [BD10-BD1Z] [43]
Prazosin DMCD9YG Moderate Additive hypotensive effects by the combination of Betaxolol and Prazosin. Heart failure [BD10-BD1Z] [42]
Chlorothiazide DMLHESP Moderate Increased risk of hyperglycemia by the combination of Betaxolol and Chlorothiazide. Heart failure [BD10-BD1Z] [43]
Furosemide DMMQ8ZG Moderate Increased risk of hyperglycemia by the combination of Betaxolol and Furosemide. Heart failure [BD10-BD1Z] [43]
Bumetanide DMRV7H0 Moderate Increased risk of hyperglycemia by the combination of Betaxolol and Bumetanide. Heart failure [BD10-BD1Z] [43]
Hydroflumethiazide DMVPUQI Moderate Increased risk of hyperglycemia by the combination of Betaxolol and Hydroflumethiazide. Heart failure [BD10-BD1Z] [43]
Torasemide DMXKJ6C Moderate Increased risk of hyperglycemia by the combination of Betaxolol and Torasemide. Heart failure [BD10-BD1Z] [43]
Ritonavir DMU764S Moderate Decreased metabolism of Betaxolol caused by Ritonavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [53]
Belladonna DM2RBWK Moderate Antagonize the effect of Betaxolol when combined with Belladonna. Infectious gastroenteritis/colitis [1A40] [45]
Propiomazine DMKY8V1 Moderate Additive hypotensive effects by the combination of Betaxolol and Propiomazine. Insomnia [7A00-7A0Z] [47]
ITI-007 DMUQ1DO Moderate Additive hypotensive effects by the combination of Betaxolol and ITI-007. Insomnia [7A00-7A0Z] [47]
Clidinium DMUMQZ0 Moderate Additive CNS depression effects by the combination of Betaxolol and Clidinium. Irritable bowel syndrome [DD91] [45]
Dicyclomine DMZSDGX Moderate Additive CNS depression effects by the combination of Betaxolol and Dicyclomine. Irritable bowel syndrome [DD91] [45]
Glycerol phenylbutyrate DMDGRQO Moderate Decreased metabolism of Betaxolol caused by Glycerol phenylbutyrate mediated inhibition of CYP450 enzyme. Liver disease [DB90-DB9Z] [45]
Lanthanum carbonate DMMJQSH Moderate Decreased absorption of Betaxolol due to formation of complexes caused by Lanthanum carbonate. Mineral absorption/transport disorder [5C64] [50]
Thalidomide DM70BU5 Moderate Increased risk of ventricular arrhythmias by the combination of Betaxolol and Thalidomide. Multiple myeloma [2A83] [54]
Siponimod DM2R86O Major Increased risk of bradycardia by the combination of Betaxolol and Siponimod. Multiple sclerosis [8A40] [54]
Fingolimod DM5JVAN Major Increased risk of atrioventricular block by the combination of Betaxolol and Fingolimod. Multiple sclerosis [8A40] [55]
Ozanimod DMT6AM2 Moderate Increased risk of bradycardia by the combination of Betaxolol and Ozanimod. Multiple sclerosis [8A40] [56]
Prochlorperazine DM53SRA Moderate Additive hypotensive effects by the combination of Betaxolol and Prochlorperazine. Nausea/vomiting [MD90] [47]
Promethazine DM6I5GR Moderate Additive hypotensive effects by the combination of Betaxolol and Promethazine. Nausea/vomiting [MD90] [47]
Thiethylperazine DMU3IET Moderate Additive hypotensive effects by the combination of Betaxolol and Thiethylperazine. Nausea/vomiting [MD90] [47]
Chlorthalidone DM4DMBT Moderate Increased risk of ventricular arrhythmias by the combination of Betaxolol and Chlorthalidone. Oedema [MG29] [43]
Metolazone DMB39LO Moderate Increased risk of ventricular arrhythmias by the combination of Betaxolol and Metolazone. Oedema [MG29] [43]
Polythiazide DMCH80F Moderate Increased risk of hypertriglyceridemia by the combination of Betaxolol and Polythiazide. Oedema [MG29] [43]
Biperiden DME78OA Moderate Antagonize the effect of Betaxolol when combined with Biperiden. Parkinsonism [8A00] [45]
Benztropine DMGZOVN Moderate Antagonize the effect of Betaxolol when combined with Benztropine. Parkinsonism [8A00] [57]
Procyclidine DMHFJDT Moderate Altered absorption of Betaxolol due to GI dynamics variation caused by Procyclidine. Parkinsonism [8A00] [45]
Methylscopolamine DM5VWOB Moderate Altered absorption of Betaxolol due to GI dynamics variation caused by Methylscopolamine. Peptic ulcer [DA61] [45]
Terazosin DM3JCVS Moderate Additive hypotensive effects by the combination of Betaxolol and Terazosin. Prostate hyperplasia [GA90] [42]
Silodosin DMJSBT6 Moderate Additive hypotensive effects by the combination of Betaxolol and Silodosin. Prostate hyperplasia [GA90] [42]
Alfuzosin DMZVMKF Moderate Additive hypotensive effects by the combination of Betaxolol and Alfuzosin. Prostate hyperplasia [GA90] [42]
Levomepromazine DMIKFEL Moderate Additive hypotensive effects by the combination of Betaxolol and Levomepromazine. Psychotic disorder [6A20-6A25] [47]
Fluphenazine DMIT8LX Moderate Additive hypotensive effects by the combination of Betaxolol and Fluphenazine. Psychotic disorder [6A20-6A25] [47]
Triflupromazine DMKFQJP Moderate Additive hypotensive effects by the combination of Betaxolol and Triflupromazine. Psychotic disorder [6A20-6A25] [47]
Celecoxib DM6LOQU Moderate Decreased metabolism of Betaxolol caused by Celecoxib mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [58]
Quetiapine DM1N62C Moderate Additive hypotensive effects by the combination of Betaxolol and Quetiapine. Schizophrenia [6A20] [47]
Mesoridazine DM2ZGAN Moderate Additive hypotensive effects by the combination of Betaxolol and Mesoridazine. Schizophrenia [6A20] [47]
Aripiprazole DM3NUMH Moderate Additive hypotensive effects by the combination of Betaxolol and Aripiprazole. Schizophrenia [6A20] [47]
Iloperidone DM6AUFY Moderate Additive hypotensive effects by the combination of Betaxolol and Iloperidone. Schizophrenia [6A20] [47]
Paliperidone DM7NPJS Moderate Additive hypotensive effects by the combination of Betaxolol and Paliperidone. Schizophrenia [6A20] [47]
Loxapine DM8AI9U Moderate Additive hypotensive effects by the combination of Betaxolol and Loxapine. Schizophrenia [6A20] [47]
Perphenazine DMA4MRX Moderate Additive hypotensive effects by the combination of Betaxolol and Perphenazine. Schizophrenia [6A20] [47]
Molindone DMAH70G Moderate Additive hypotensive effects by the combination of Betaxolol and Molindone. Schizophrenia [6A20] [47]
Chlorpromazine DMBGZI3 Moderate Additive hypotensive effects by the combination of Betaxolol and Chlorpromazine. Schizophrenia [6A20] [47]
Thiothixene DMDINC4 Moderate Additive hypotensive effects by the combination of Betaxolol and Thiothixene. Schizophrenia [6A20] [47]
Clozapine DMFC71L Moderate Additive hypotensive effects by the combination of Betaxolol and Clozapine. Schizophrenia [6A20] [47]
Trifluoperazine DMKBYWI Moderate Additive hypotensive effects by the combination of Betaxolol and Trifluoperazine. Schizophrenia [6A20] [47]
Ziprasidone DMM58JY Moderate Additive hypotensive effects by the combination of Betaxolol and Ziprasidone. Schizophrenia [6A20] [47]
Risperidone DMN6DXL Moderate Additive hypotensive effects by the combination of Betaxolol and Risperidone. Schizophrenia [6A20] [47]
Olanzapine DMPFN6Y Moderate Additive hypotensive effects by the combination of Betaxolol and Olanzapine. Schizophrenia [6A20] [47]
Amisulpride DMSJVAM Moderate Increased risk of ventricular arrhythmias by the combination of Betaxolol and Amisulpride. Schizophrenia [6A20] [45]
Asenapine DMSQZE2 Moderate Additive hypotensive effects by the combination of Betaxolol and Asenapine. Schizophrenia [6A20] [47]
Succinylcholine DM2ET1M Moderate Additive cardiorespiratory depression effects by the combination of Betaxolol and Succinylcholine. Tonus and reflex abnormality [MB47] [49]
Pipecuronium DM5F84A Moderate Additive neuromuscular blocking effects by the combination of Betaxolol and Pipecuronium. Tonus and reflex abnormality [MB47] [49]
Doxacurium DMKE7L9 Moderate Additive neuromuscular blocking effects by the combination of Betaxolol and Doxacurium. Tonus and reflex abnormality [MB47] [49]
Vecuronium DMP0UK2 Moderate Additive neuromuscular blocking effects by the combination of Betaxolol and Vecuronium. Tonus and reflex abnormality [MB47] [49]
Cisatracurium DMUZPJ5 Moderate Additive neuromuscular blocking effects by the combination of Betaxolol and Cisatracurium. Tonus and reflex abnormality [MB47] [49]
Trospium DMX6RTG Moderate Antagonize the effect of Betaxolol when combined with Trospium. Tonus and reflex abnormality [MB47] [45]
Rocuronium DMY9BMK Moderate Additive neuromuscular blocking effects by the combination of Betaxolol and Rocuronium. Tonus and reflex abnormality [MB47] [49]
Atropine DMEN6X7 Moderate Antagonize the effect of Betaxolol when combined with Atropine. Unspecific substance harmful effect [NE6Z] [45]
Methdilazine DMAUHQX Moderate Additive hypotensive effects by the combination of Betaxolol and Methdilazine. Vasomotor/allergic rhinitis [CA08] [47]
Trimeprazine DMEMV9D Moderate Additive hypotensive effects by the combination of Betaxolol and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [59]
Disopyramide DM5SYZP Major Increased risk of prolong QT interval by the combination of Betaxolol and Disopyramide. Ventricular tachyarrhythmia [BC71] [60]
Amiodarone DMUTEX3 Moderate Increased risk of bradycardia by the combination of Betaxolol and Amiodarone. Ventricular tachyarrhythmia [BC71] [61]
⏷ Show the Full List of 93 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
Acrylic acid E00132 6581 Other agent
Hydrochloric acid E00015 313 Acidulant
Mannitol E00103 6251 Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Stearic acid E00079 5281 Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Benzalkonium chloride E00536 21988052 Antimicrobial preservative; Penetration agent; Solubilizing agent; Surfactant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Edetate disodium E00186 8759 Complexing agent
Hypromellose E00634 Not Available Coating agent
Magnesium stearate E00208 11177 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
Sodium chloride E00077 5234 Diluent; Tonicity agent
Sodium hydroxide E00234 14798 Alkalizing agent
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Water E00035 962 Solvent
Hydrophobic colloidal silica E00285 24261 Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
⏷ Show the Full List of 17 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Betaxolol 10 mg tablet 10 mg Oral Tablet Oral
Betaxolol 20 mg tablet 20 mg Oral Tablet Oral
Betaxolol Hydrochloride eq 0.25% base suspension eq 0.25% base Suspension Ophthalmic
Betaxolol Hydrochloride 10mg tablet 10mg Tablet Oral
Betaxolol Hydrochloride eq 0.5% base solution eq 0.5% base Solution Ophthalmic
Jump to Detail Pharmaceutical Formulation Page of This Drug

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