General Information of Drug (ID: DM1WXA6)

Drug Name
Lofexidine
Synonyms
Britlofex; Lofexidina; Lofexidinum; Britlofex (TN); Lofexidina [INN-Spanish]; Lofexidine (INN); Lofexidine [INN:BAN]; Lofexidinum [INN-Latin]; 1H-Imidazole, 2-(1-(2,6-dichlorophenoxy)ethyl)-4,5-dihydro-(9CI); 2-(1-(2,6-Dichlorophenoxy)ethyl)-4,5-dihydro-1H-imidazole; 2-(a-(2,6-dichlorophenoxy)ethyl)2-imidazoline; 2-(alpha-(2,6-Dichlorophenoxy)ethyl)2-imidazoline; 2-(alpha-(2,6-dichlorophenoxy)ethyl) delta-2-imidazoline; 2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole; 2-{1-[(2,6-dichlorophenyl)oxy]ethyl}-4,5-dihydro-1H-imidazole
Indication
Disease Entry ICD 11 Status REF
Heroin and opiate withdrawal 6C43 Approved [1]
Opioid dependence 6C43.2Z Approved [2]
Therapeutic Class
Antihypertensive Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 259.13
Topological Polar Surface Area (xlogp) 2.6
Rotatable Bond Count (rotbonds) 3
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 2
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 46 mcgh/L [3]
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 0.5 h [3]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [4]
Bioavailability
The bioavailability of drug is 85% [3]
Clearance
The clearance of drug is 17.6 L/h [5]
Elimination
The elimination of lofexidine is primarily through the renal system and it represents 94% of the administered dose while elimination in feces corresponds to only 0.93% [6]
Half-life
The concentration or amount of drug in body reduced by one-half in 11 hours [7]
Metabolism
The drug is metabolized via the CYP2D6 and in a minor degree by CYP1A2 and CYP2C19 [8]
Vd
The volume of distribution (Vd) of drug is 300 L [5]
Chemical Identifiers
Formula
C11H12Cl2N2O
IUPAC Name
2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole
Canonical SMILES
CC(C1=NCCN1)OC2=C(C=CC=C2Cl)Cl
InChI
InChI=1S/C11H12Cl2N2O/c1-7(11-14-5-6-15-11)16-10-8(12)3-2-4-9(10)13/h2-4,7H,5-6H2,1H3,(H,14,15)
InChIKey
KSMAGQUYOIHWFS-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
30668
ChEBI ID
CHEBI:51368
CAS Number
31036-80-3
DrugBank ID
DB04948
TTD ID
D0K0MW
INTEDE ID
DR0967
ACDINA ID
D01217

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Adrenergic receptor Alpha-2 (ADRA2) TTQ8AFT NOUNIPROTAC Agonist [9], [1]
Adrenergic receptor alpha-2A (ADRA2A) TTWG9A4 ADA2A_HUMAN Agonist [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [10]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_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 Disease Different from Lofexidine (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Lofexidine and Ivosidenib. Acute myeloid leukaemia [2A60] [61]
Midostaurin DMI6E0R Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Midostaurin. Acute myeloid leukaemia [2A60] [62]
Arn-509 DMT81LZ Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Arn-509. Acute myeloid leukaemia [2A60] [63]
Gilteritinib DMWQ4MZ Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Gilteritinib. Acute myeloid leukaemia [2A60] [64]
Ivabradine DM0L594 Major Increased risk of ventricular arrhythmias by the combination of Lofexidine and Ivabradine. Angina pectoris [BA40] [63]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Lofexidine and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [65]
Levalbuterol DM5YBO1 Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Levalbuterol. Asthma [CA23] [66]
Retigabine DMGNYIH Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Retigabine. Behcet disease [4A62] [62]
Eribulin DM1DX4Q Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Eribulin. Breast cancer [2C60-2C6Y] [62]
Bosutinib DMTI8YE Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Bosutinib. Breast cancer [2C60-2C6Y] [62]
PF-04449913 DMSB068 Moderate Increased risk of prolong QT interval by the combination of Lofexidine and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [67]
Olodaterol DM62B78 Moderate Increased risk of ventricular arrhythmias by the combination of Lofexidine and Olodaterol. Chronic obstructive pulmonary disease [CA22] [68]
Vilanterol DMF5EK1 Moderate Increased risk of ventricular arrhythmias by the combination of Lofexidine and Vilanterol. Chronic obstructive pulmonary disease [CA22] [66]
Indacaterol DMQJHR7 Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Indacaterol. Chronic obstructive pulmonary disease [CA22] [68]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Lofexidine and Pasireotide. Cushing syndrome [5A70] [62]
Osilodrostat DMIJC9X Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Osilodrostat. Cushing syndrome [5A70] [63]
OPC-34712 DMHG57U Moderate Additive hypotensive effects by the combination of Lofexidine and OPC-34712. Depression [6A70-6A7Z] [69]
Esketamine DMVU687 Moderate Additive CNS depression effects by the combination of Lofexidine and Esketamine. Depression [6A70-6A7Z] [70]
Ingrezza DMVPLNC Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Ingrezza. Dystonic disorder [8A02] [62]
Fostemsavir DM50ILT Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [71]
Rilpivirine DMJ0QOW Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [62]
ITI-007 DMUQ1DO Moderate Additive hypotensive effects by the combination of Lofexidine and ITI-007. Insomnia [7A00-7A0Z] [69]
Polyethylene glycol DM4I1JP Moderate Increased risk of ventricular arrhythmias by the combination of Lofexidine and Polyethylene glycol. Irritable bowel syndrome [DD91] [63]
Crizotinib DM4F29C Major Increased risk of prolong QT interval by the combination of Lofexidine and Crizotinib. Lung cancer [2C25] [72]
Ceritinib DMB920Z Major Increased risk of prolong QT interval by the combination of Lofexidine and Ceritinib. Lung cancer [2C25] [62]
Osimertinib DMRJLAT Major Increased risk of prolong QT interval by the combination of Lofexidine and Osimertinib. Lung cancer [2C25] [73]
Lumefantrine DM29GAD Major Increased risk of prolong QT interval by the combination of Lofexidine and Lumefantrine. Malaria [1F40-1F45] [70]
Inotuzumab ozogamicin DMAC130 Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Inotuzumab ozogamicin. Malignant haematopoietic neoplasm [2B33] [63]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Lofexidine and Vemurafenib. Melanoma [2C30] [62]
Allopregnanolone DMNLHAC Moderate Additive CNS depression effects by the combination of Lofexidine and Allopregnanolone. Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z] [74]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Lofexidine and Lasmiditan. Migraine [8A80] [75]
Panobinostat DM58WKG Major Increased risk of prolong QT interval by the combination of Lofexidine and Panobinostat. Multiple myeloma [2A83] [76]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Lofexidine and Siponimod. Multiple sclerosis [8A40] [70]
Fingolimod DM5JVAN Major Increased risk of ventricular arrhythmias by the combination of Lofexidine and Fingolimod. Multiple sclerosis [8A40] [62]
Ozanimod DMT6AM2 Major Increased risk of ventricular arrhythmias by the combination of Lofexidine and Ozanimod. Multiple sclerosis [8A40] [77]
Romidepsin DMT5GNL Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Romidepsin. Mycosis fungoides [2B01] [62]
Entrectinib DMMPTLH Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Entrectinib. Non-small cell lung cancer [2C25] [70]
Rucaparib DM9PVX8 Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Rucaparib. Ovarian cancer [2C73] [62]
Triclabendazole DMPWGBR Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Triclabendazole. Parasitic worm infestation [1F90] [62]
Safinamide DM0YWJC Moderate Additive hypotensive effects by the combination of Lofexidine and Safinamide. Parkinsonism [8A00] [78]
Pimavanserin DMR7IVC Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Pimavanserin. Parkinsonism [8A00] [79]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Lofexidine and Macimorelin. Pituitary gland disorder [5A60-5A61] [80]
Lefamulin DME6G97 Major Increased risk of prolong QT interval by the combination of Lofexidine and Lefamulin. Pneumonia [CA40] [81]
Degarelix DM3O8QY Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Degarelix. Prostate cancer [2C82] [63]
ABIRATERONE DM8V75C Moderate Increased risk of prolong QT interval by the combination of Lofexidine and ABIRATERONE. Prostate cancer [2C82] [63]
Enzalutamide DMGL19D Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Enzalutamide. Prostate cancer [2C82] [63]
Relugolix DMK7IWL Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Relugolix. Prostate cancer [2C82] [63]
Asenapine DMSQZE2 Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Asenapine. Schizophrenia [6A20] [62]
LEE011 DMMX75K Major Increased risk of prolong QT interval by the combination of Lofexidine and LEE011. Solid tumour/cancer [2A00-2F9Z] [62]
Vandetanib DMRICNP Major Increased risk of prolong QT interval by the combination of Lofexidine and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [62]
Triptorelin DMTK4LS Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Triptorelin. Solid tumour/cancer [2A00-2F9Z] [63]
Pitolisant DM8RFNJ Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Pitolisant. Somnolence [MG42] [63]
Telavancin DM58VQX Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [62]
Lenvatinib DMB1IU4 Moderate Increased risk of prolong QT interval by the combination of Lofexidine and Lenvatinib. Thyroid cancer [2D10] [62]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Lofexidine and Cabozantinib. Thyroid cancer [2D10] [63]
⏷ Show the Full List of 55 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. 2 E00446 2723854 Colorant
Kyselina citronova E00014 311 Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sunset yellow FCF E00255 17730 Colorant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Calcium stearate E00244 15324 lubricant
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
⏷ Show the Full List of 8 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Lofexidine 0.18 mg tablet 0.18 mg Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

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