Details of the Drug

General Information of Drug (ID: DMFMDOB)

• Drug Name: Carteolol
• Synonyms: Carteololum; Carteolol HCl; Carteolol Monohydrochloride; Arteolol (TN); Arteoptic (TN); Calte (TN); Carteol (TN); Carteolol (INN); Carteolol [INN:BAN]; Carteololum [INN-Latin]; Cartrol (TN); Elebloc (TN); Endak (TN); Glauteolol (TN); Mikelan (TN); Ocupress (TN); Poenglaucol (TN); Singlauc (TN); Teoptic (TN); 5-({3-[(1,1-dimethylethyl)amino]-2-hydroxypropyl}oxy)-3,4-dihydroquinolin-2(1H)-one; 5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-1H-quinolin-2-one; 5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydroquinolin-2(1H)-one

Indication

Disease Entry	ICD 11	Status	REF
Glaucoma/ocular hypertension	9C61	Approved	[1]
Ocular hypertension	9C61.01	Approved	[2]

• Therapeutic Class: Antihypertensive Agents
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 292.37
  Logarithm of the Partition Coefficient (xlogp); 1
  Rotatable Bond Count (rotbonds); 6
  Hydrogen Bond Donor Count (hbonddonor); 3
  Hydrogen Bond Acceptor Count (hbondacc); 4
• ADMET Property:
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [3]
  Bioavailability: 88% 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 10.1 mL/min/kg [5]
  Elimination: 60% 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 4.7 hours [5]
  Metabolism: The drug is metabolized via the hepatic []
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.4886 micromolar/kg/day [6]
• Chemical Identifiers:
  Formula: C16H24N2O3
  IUPAC Name: 5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-1H-quinolin-2-one
  Canonical SMILES: CC(C)(C)NCC(COC1=CC=CC2=C1CCC(=O)N2)O
  InChI: InChI=1S/C16H24N2O3/c1-16(2,3)17-9-11(19)10-21-14-6-4-5-13-12(14)7-8-15(20)18-13/h4-6,11,17,19H,7-10H2,1-3H3,(H,18,20)
  InChIKey: LWAFSWPYPHEXKX-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 2583
  ChEBI ID: CHEBI:3437
  CAS Number: 51781-06-7
  DrugBank ID: DB00521
  TTD ID: D03GCJ
  INTEDE ID: DR0281
• 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 beta-1 (ADRB1)	TTR6W5O	ADRB1_HUMAN	Agonist	[7]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 2D6 (CYP2D6) Main DME	DECB0K3	CP2D6_HUMAN	Substrate	[8]

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Carteolol (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Scopolamine	DMOM8AL	Moderate	Antagonize the effect of Carteolol when combined with Scopolamine.	Addictive disorder [6C50-6C5Z]	[9]
Bepridil	DM0RKS4	Moderate	Increased risk of cardiac depression by the combination of Carteolol and Bepridil.	Angina pectoris [BA40]	[10]
Dronedarone	DMA8FS5	Moderate	Decreased metabolism of Carteolol caused by Dronedarone mediated inhibition of CYP450 enzyme.	Angina pectoris [BA40]	[11]
Nifedipine	DMSVOZT	Moderate	Increased risk of cardiac depression by the combination of Carteolol and Nifedipine.	Angina pectoris [BA40]	[12]
Cariprazine	DMJYDVK	Moderate	Additive hypotensive effects by the combination of Carteolol and Cariprazine.	Bipolar disorder [6A60]	[13]
Atracurium	DM42HXN	Moderate	Additive cardiorespiratory depression effects by the combination of Carteolol and Atracurium.	Corneal disease [9A76-9A78]	[14]
Mivacurium	DM473VD	Moderate	Additive neuromuscular blocking effects by the combination of Carteolol and Mivacurium.	Corneal disease [9A76-9A78]	[14]
Pancuronium	DMB0VY8	Moderate	Additive neuromuscular blocking effects by the combination of Carteolol and Pancuronium.	Corneal disease [9A76-9A78]	[14]
Tubocurarine	DMBZIVP	Moderate	Additive neuromuscular blocking effects by the combination of Carteolol and Tubocurarine.	Corneal disease [9A76-9A78]	[15]
Pasireotide	DMHM7JS	Moderate	Increased risk of bradycardia by the combination of Carteolol and Pasireotide.	Cushing syndrome [5A70]	[16]
OPC-34712	DMHG57U	Moderate	Additive hypotensive effects by the combination of Carteolol and OPC-34712.	Depression [6A70-6A7Z]	[13]
Mepenzolate	DM8YU2F	Moderate	Altered absorption of Carteolol due to GI dynamics variation caused by Mepenzolate.	Digestive system disease [DE2Z]	[17]
Oxybutynine	DMJPBAX	Moderate	Antagonize the effect of Carteolol when combined with Oxybutynine.	Discovery agent [N.A.]	[9]
Ethacrynic acid	DM60QMR	Moderate	Increased risk of hyperglycemia by the combination of Carteolol and Ethacrynic acid.	Essential hypertension [BA00]	[18]
Phenoxybenzamine	DM8KSQH	Moderate	Additive hypotensive effects by the combination of Carteolol and Phenoxybenzamine.	Essential hypertension [BA00]	[19]
Nicardipine	DMCDYW7	Moderate	Increased risk of cardiac depression by the combination of Carteolol and Nicardipine.	Essential hypertension [BA00]	[12]
Benzthiazide	DMQWZ0H	Moderate	Increased risk of hyperglycemia by the combination of Carteolol and Benzthiazide.	Essential hypertension [BA00]	[18]
Tolterodine	DMSHPW8	Moderate	Antagonize the effect of Carteolol when combined with Tolterodine.	Functional bladder disorder [GC50]	[9]
Propantheline	DM2EN6G	Moderate	Altered absorption of Carteolol due to GI dynamics variation caused by Propantheline.	Gastric ulcer [DA60]	[20]
Chlorothiazide	DMLHESP	Moderate	Increased risk of ventricular arrhythmias by the combination of Carteolol and Chlorothiazide.	Heart failure [BD10-BD1Z]	[18]
Furosemide	DMMQ8ZG	Moderate	Increased risk of hyperglycemia by the combination of Carteolol and Furosemide.	Heart failure [BD10-BD1Z]	[18]
Bumetanide	DMRV7H0	Moderate	Increased risk of hyperglycemia by the combination of Carteolol and Bumetanide.	Heart failure [BD10-BD1Z]	[18]
Hydroflumethiazide	DMVPUQI	Moderate	Increased risk of hyperglycemia by the combination of Carteolol and Hydroflumethiazide.	Heart failure [BD10-BD1Z]	[18]
Levamlodipine	DM92S6N	Moderate	Increased risk of cardiac depression by the combination of Carteolol and Levamlodipine.	Hypertension [BA00-BA04]	[12]
Doxazosin	DM9PLRH	Moderate	Additive hypotensive effects by the combination of Carteolol and Doxazosin.	Hypertension [BA00-BA04]	[19]
Verapamil	DMA7PEW	Major	Increased risk of cardiac depression by the combination of Carteolol and Verapamil.	Hypertension [BA00-BA04]	[12]
Indapamide	DMGN1PW	Moderate	Increased risk of ventricular arrhythmias by the combination of Carteolol and Indapamide.	Hypertension [BA00-BA04]	[18]
Trichlormethiazide	DMHAQCO	Moderate	Increased risk of hypertriglyceridemia by the combination of Carteolol and Trichlormethiazide.	Hypertension [BA00-BA04]	[18]
Felodipine	DMOSW35	Moderate	Increased risk of cardiac depression by the combination of Carteolol and Felodipine.	Hypertension [BA00-BA04]	[12]
Hydrochlorothiazide	DMUSZHD	Moderate	Increased risk of hyperglycemia by the combination of Carteolol and Hydrochlorothiazide.	Hypertension [BA00-BA04]	[18]
Clevidipine butyrate	DMW4M97	Moderate	Increased risk of cardiac depression by the combination of Carteolol and Clevidipine butyrate.	Hypertension [BA00-BA04]	[12]
Belladonna	DM2RBWK	Moderate	Antagonize the effect of Carteolol when combined with Belladonna.	Infectious gastroenteritis/colitis [1A40]	[9]
ITI-007	DMUQ1DO	Moderate	Additive hypotensive effects by the combination of Carteolol and ITI-007.	Insomnia [7A00-7A0Z]	[13]
Clidinium	DMUMQZ0	Moderate	Antagonize the effect of Carteolol when combined with Clidinium.	Irritable bowel syndrome [DD91]	[9]
Dicyclomine	DMZSDGX	Moderate	Antagonize the effect of Carteolol when combined with Dicyclomine.	Irritable bowel syndrome [DD91]	[9]
Lanthanum carbonate	DMMJQSH	Moderate	Decreased absorption of Carteolol due to formation of complexes caused by Lanthanum carbonate.	Mineral absorption/transport disorder [5C64]	[16]
Thalidomide	DM70BU5	Moderate	Increased risk of ventricular arrhythmias by the combination of Carteolol and Thalidomide.	Multiple myeloma [2A83]	[20]
Siponimod	DM2R86O	Major	Increased risk of bradycardia by the combination of Carteolol and Siponimod.	Multiple sclerosis [8A40]	[20]
Fingolimod	DM5JVAN	Major	Increased risk of bradycardia by the combination of Carteolol and Fingolimod.	Multiple sclerosis [8A40]	[21]
Ozanimod	DMT6AM2	Moderate	Increased risk of bradycardia by the combination of Carteolol and Ozanimod.	Multiple sclerosis [8A40]	[22]
Promethazine	DM6I5GR	Moderate	Additive hypotensive effects by the combination of Carteolol and Promethazine.	Nausea/vomiting [MD90]	[13]
Metolazone	DMB39LO	Moderate	Increased risk of hyperglycemia by the combination of Carteolol and Metolazone.	Oedema [MG29]	[18]
Polythiazide	DMCH80F	Moderate	Increased risk of hyperglycemia by the combination of Carteolol and Polythiazide.	Oedema [MG29]	[18]
Biperiden	DME78OA	Moderate	Antagonize the effect of Carteolol when combined with Biperiden.	Parkinsonism [8A00]	[23]
Methylscopolamine	DM5VWOB	Moderate	Antagonize the effect of Carteolol when combined with Methylscopolamine.	Peptic ulcer [DA61]	[9]
Terazosin	DM3JCVS	Moderate	Additive hypotensive effects by the combination of Carteolol and Terazosin.	Prostate hyperplasia [GA90]	[19]
Silodosin	DMJSBT6	Moderate	Additive hypotensive effects by the combination of Carteolol and Silodosin.	Prostate hyperplasia [GA90]	[19]
Fluphenazine	DMIT8LX	Moderate	Additive hypotensive effects by the combination of Carteolol and Fluphenazine.	Psychotic disorder [6A20-6A25]	[13]
Quetiapine	DM1N62C	Moderate	Additive hypotensive effects by the combination of Carteolol and Quetiapine.	Schizophrenia [6A20]	[13]
Mesoridazine	DM2ZGAN	Moderate	Additive hypotensive effects by the combination of Carteolol and Mesoridazine.	Schizophrenia [6A20]	[24]
Aripiprazole	DM3NUMH	Moderate	Additive hypotensive effects by the combination of Carteolol and Aripiprazole.	Schizophrenia [6A20]	[13]
Iloperidone	DM6AUFY	Moderate	Additive hypotensive effects by the combination of Carteolol and Iloperidone.	Schizophrenia [6A20]	[13]
Paliperidone	DM7NPJS	Moderate	Additive hypotensive effects by the combination of Carteolol and Paliperidone.	Schizophrenia [6A20]	[13]
Molindone	DMAH70G	Moderate	Additive hypotensive effects by the combination of Carteolol and Molindone.	Schizophrenia [6A20]	[13]
Thiothixene	DMDINC4	Moderate	Additive hypotensive effects by the combination of Carteolol and Thiothixene.	Schizophrenia [6A20]	[13]
Trifluoperazine	DMKBYWI	Moderate	Additive hypotensive effects by the combination of Carteolol and Trifluoperazine.	Schizophrenia [6A20]	[13]
Risperidone	DMN6DXL	Moderate	Additive hypotensive effects by the combination of Carteolol and Risperidone.	Schizophrenia [6A20]	[13]
Amisulpride	DMSJVAM	Moderate	Additive hypotensive effects by the combination of Carteolol and Amisulpride.	Schizophrenia [6A20]	[13]
Asenapine	DMSQZE2	Moderate	Additive hypotensive effects by the combination of Carteolol and Asenapine.	Schizophrenia [6A20]	[13]
Pipecuronium	DM5F84A	Moderate	Additive cardiorespiratory depression effects by the combination of Carteolol and Pipecuronium.	Tonus and reflex abnormality [MB47]	[15]
Doxacurium	DMKE7L9	Moderate	Additive neuromuscular blocking effects by the combination of Carteolol and Doxacurium.	Tonus and reflex abnormality [MB47]	[15]
Vecuronium	DMP0UK2	Moderate	Additive neuromuscular blocking effects by the combination of Carteolol and Vecuronium.	Tonus and reflex abnormality [MB47]	[14]
Cisatracurium	DMUZPJ5	Moderate	Additive neuromuscular blocking effects by the combination of Carteolol and Cisatracurium.	Tonus and reflex abnormality [MB47]	[14]
Rocuronium	DMY9BMK	Moderate	Additive cardiorespiratory depression effects by the combination of Carteolol and Rocuronium.	Tonus and reflex abnormality [MB47]	[14]
Atropine	DMEN6X7	Moderate	Antagonize the effect of Carteolol when combined with Atropine.	Unspecific substance harmful effect [NE6Z]	[9]
Amiodarone	DMUTEX3	Moderate	Increased risk of atrioventricular block by the combination of Carteolol and Amiodarone.	Ventricular tachyarrhythmia [BC71]	[25]

References

• [1] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [2] Carteolol FDA Label
• [3] BDDCS applied to over 900 drugs
• [4] Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches
• [5] Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
• [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] Partial agonistic effects of carteolol on atypical beta-adrenoceptors in the guinea pig gastric fundus. Jpn J Pharmacol. 2000 Nov;84(3):287-92.
• [8] Involvement of CYP2D1 in the metabolism of carteolol by male rat liver microsomes. Xenobiotica. 1997 Nov;27(11):1121-9.
• [9] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [10] Henry M, Kay MM, Viccellio P "Cardiogenic shock associated with calcium-channel and beta blockers: reversal with intravenous calcium chloride." Am J Emerg Med 3 (1985): 334-6. [PMID: 2860911]
• [11] Product Information. Multaq (dronedarone). sanofi-aventis , Bridgewater, NJ.
• [12] Anastassiades CJ "Nifedipine and beta-blocker drugs." Br Med J 281 (1980): 1251-2. [PMID: 6107167]
• [13] Aronowitz JS, Chakos MH, Safferman AZ, Lieberman JA "Syncope associated with the combination of clozapine and enalapril." J Clin Psychopharmacol 14 (1994): 429-30. [PMID: 7884028]
• [14] Chapple DJ, Clark JS, Hughes R "Interaction between atracurium and drugs used in anaesthesia." Br J Anaesth 55 Suppl 1 (1983): s17-22. [PMID: 6688011]
• [15] Harrah MD, Way WL, Katzung BG "The interaction of d-tubocurarine with antiarrhythmic drugs." Anesthesiology 33 (1970): 406-10. [PMID: 5512329]
• [16] Canadian Pharmacists Association.
• [17] Gilman AG, Rall TW, Nies AS, Taylor P, eds. "Goodman and Gilman's the Pharmacological Basis of Therapeutics. 8th ed." New York, NY: Pergamon Press Inc. (1990):.
• [18] Dean S, Kendall MJ, Potter S, Thompson MH, Jackson DA "Nadolol in combination with indapamide and xipamide in resistant hypertensives." Eur J Clin Pharmacol 28 (1985): 29-33. [PMID: 3987783]
• [19] Chrysant SG "Experience with terazosin administered in combination with other antihypertensive agents." Am J Med 80 (1986): 55-61. [PMID: 2872808]
• [20] Cerner Multum, Inc. "Australian Product Information.".
• [21] Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
• [22] Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
• [23] Briant RH, Dorrington RE, Ferry DG, Paxton JW "Bioavailability of metoprolol in young adults and the elderly, with additional studies on the effects of metoclopramide and probanthine." Eur J Clin Pharmacol 25 (1983): 353-6. [PMID: 6628522]
• [24] Product Information. Clozaril (clozapine). Novartis Pharmaceuticals, East Hanover, NJ.
• [25] Leor J, Levartowsky D, Sharon C, Farfel Z "Amiodarone and beta-adrenergic blockers: an interaction with metoprolol but not with atenolol." Am Heart J 16 (1988): 206-7. [PMID: 3394625]