Details of the Drug

General Information of Drug (ID: DML4ZOT)

Drug Name
Lidocaine
Synonyms
Alphacaine; Anestacon; Cappicaine; Cuivasil; Dalcaine; Dentipatch; DermaFlex; Dilocaine; Duncaine; EMBOLEX; Esracaine; Gravocain; Isicaina; Isicaine; Jetocaine; LIDOPEN; LQZ; Lanabiotic; Leostesin; Lidocaina; Lidocainum; Lidocaton; Lidoderm; Lignocaine; Lignocainum; Lingocaine; Maricaine; Octocaine; Remicaine; Rucaina; Solcain; Xilina; Xilocaina; Xllina; Xycaine; Xylestesin; Xylesthesin; Xylocain; Xylocaine; Xylocard; Xylocitin; Xylotox; Zingo; After Burn Double Strength Gel; After Burn Double Strength Spray; After Burn Gel; After Burn Spray; Anestacon Jelly; Cito optadren; Emla Cream; Lidocaine Carbonate; Lidocaine Hydrocarbonate; Lidocaine Monohydrochloride; Norwood Sunburn Spray; Rocephin Kit; Solarcaine aloe extraburn relief cream; Xilocaina [Italian]; Xylocaine Dental Ointment; Xylocaine Endotracheal; Xylocaine Test Dose; Xylocaine Viscous; CDS1_000283; L1026_SIGMA; Xylocaine CO2; Dentipatch (TN); ELA-Max; L-Caine; Lida-Mantle; Lidocaina [INN-Spanish]; Lidocaine (VAN); Lidocainum [INN-Latin]; Lidoject-1; Lidoject-2; Octocaine-100; Octocaine-50; Xylocaine (TN); Xylocaine 5% Spinal; Xylocaine-Mpf; Xylocaine-Mpf with Glucose; Xyloneural (free base); Zilactin-L; Lidocaine [USAN:INN:JAN]; Diethylaminoaceto-2,6-xylidide; Lidocaine (JP15/USP/INN); Alfa-Dietilamino-2,6-dimetilacetanilide; Alfa-Dietilamino-2,6-dimetilacetanilide [Italian]; Alpha-Diethylamino-2,6-dimethylacetanilide; Alpha-Diethylaminoaceto-2,6-xylidide; LIDOCAINE (73-58-6 (MONOHYDROCHLORIDE); Omega-Diethylamino-2,6-dimethylacetanilide; Alpha-(Diethylamino)-2,6-acetoxylidide; N-(2,6-dimethylphenyl)-N(2),N(2)-diethylglycinamide; N-(2,6-dimethylphenyl)-N~2~,N~2~-diethylglycinamide; 2-(Diethylamino)-2',6'-acetoxylidide; 2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamide; 2-Diethylamino-N-(2,6-dimethyl-phenyl)-acetamide; 2-Diethylamino-N-(2,6-dimethylphenyl)acetamide
Indication
Disease Entry ICD 11 Status REF
Anaesthesia 9A78.6 Approved [1]
Carpal tunnel syndrome N.A. Approved [2]
Interstitial cystitis GC00.3 Approved [2]
Long QT syndrome BC65.0 Approved [2]
Pain MG30-MG3Z Approved [2]
Pediculus capitis infestation 1G00.0 Approved [2]
Periodontitis DA0C Approved [2]
Postherpetic neuralgia 1E91.5 Approved [2]
Pthirus pubis infestation N.A. Approved [2]
Dysmenorrhea GA34.3 Phase 2 [3]
Chronic pain MG30 Investigative [2]
Neuralgia N.A. Investigative [2]
Premature ejaculation HA03.0Z Investigative [2]
Pruritus EC90 Investigative [2]
⏷ Show the Full List of Indication(s)
Therapeutic Class
Anesthetics
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 234.34
Logarithm of the Partition Coefficient (xlogp) 2.3
Rotatable Bond Count (rotbonds) 5
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 2
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [4]
Clearance
The sytemic clearance of drug is 0.64 +/- 0.18 L/min []
Elimination
The excretion of unchanged lidocaine and its metabolites occurs predominantly via the kidney with less than 5% in the unchanged form appearing in the urine [5]
Half-life
The concentration or amount of drug in body reduced by one-half in 1.5 - 2 hours []
Metabolism
The drug is metabolized via the liver []
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 18.2884 micromolar/kg/day [6]
Unbound Fraction
The unbound fraction of drug in plasma is 0.33% [7]
Vd
The volume of distribution (Vd) of drug is 0.7-1.5 L/kg [8]
Water Solubility
The ability of drug to dissolve in water is measured as 3.58 mg/mL [4]
Adverse Drug Reaction (ADR)
ADR Term Variation Related DOT DOT ID REF
Gastrointestinal disorders Not Available HSPA5 OTFUIRAO [9]
Pyrexia Not Available CRP OT0RFT8F [9]
Pyrexia Not Available GGT1 OTYDA1Z7 [9]
Pyrexia Not Available ALPP OTZU4G9W [9]
Chemical Identifiers
Formula
C14H22N2O
IUPAC Name
2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide
Canonical SMILES
CCN(CC)CC(=O)NC1=C(C=CC=C1C)C
InChI
InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17)
InChIKey
NNJVILVZKWQKPM-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
3676
ChEBI ID
CHEBI:6456
CAS Number
137-58-6
DrugBank ID
DB00281
TTD ID
D0X4RN
VARIDT ID
DR00849
INTEDE ID
DR0953
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
Voltage-gated sodium channel alpha Nav1.9 (SCN11A) TTN9VTF SCNBA_HUMAN Blocker [10]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [11]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [12]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [13]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Substrate [14]
Cytochrome P450 2A6 (CYP2A6) DEJVYAZ CP2A6_HUMAN Substrate [14]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [15]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [16]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Substrate [17]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [14]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Substrate [16]
Cytochrome P450 2C18 (CYP2C18) DEZMWRE CP2CI_HUMAN Substrate [14]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Alkaline phosphatase, placental type (ALPP) OTZU4G9W PPB1_HUMAN Drug Response [9]
Alpha-1-acid glycoprotein 1 (ORM1) OTZKSBRE A1AG1_HUMAN Protein Interaction/Cellular Processes [18]
Alpha-1-acid glycoprotein 2 (ORM2) OTRJGZP8 A1AG2_HUMAN Protein Interaction/Cellular Processes [18]
Beta-nerve growth factor (NGF) OTOLABJT NGF_HUMAN Gene/Protein Processing [19]
C-reactive protein (CRP) OT0RFT8F CRP_HUMAN Drug Response [9]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Gene/Protein Processing [20]
Caspase-9 (CASP9) OTD4RFFG CASP9_HUMAN Gene/Protein Processing [20]
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Biotransformations [21]
Cytochrome P450 3A5 (CYP3A5) OTSXFBXB CP3A5_HUMAN Biotransformations [22]
Endoplasmic reticulum chaperone BiP (HSPA5) OTFUIRAO BIP_HUMAN Drug Response [9]
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 Lidocaine
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Atracurium DM42HXN Moderate Additive neuromuscular blocking effects by the combination of Lidocaine and Atracurium. Corneal disease [9A76-9A78] [23]
Mivacurium DM473VD Moderate Additive neuromuscular blocking effects by the combination of Lidocaine and Mivacurium. Corneal disease [9A76-9A78] [23]
Pancuronium DMB0VY8 Moderate Additive neuromuscular blocking effects by the combination of Lidocaine and Pancuronium. Corneal disease [9A76-9A78] [23]
Tubocurarine DMBZIVP Moderate Additive neuromuscular blocking effects by the combination of Lidocaine and Tubocurarine. Corneal disease [9A76-9A78] [23]
Alfentanil DMVO0UB Minor Decreased metabolism of Lidocaine caused by Alfentanil mediated inhibition of CYP450 enzyme. Corneal disease [9A76-9A78] [24]
Coadministration of a Drug Treating the Disease Different from Lidocaine (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Minor Increased metabolism of Lidocaine caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [25]
Arn-509 DMT81LZ Minor Increased metabolism of Lidocaine caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [25]
Emapalumab DMZG5WL Moderate Altered metabolism of Lidocaine due to Emapalumab alters the formation of CYP450 enzymes. Adaptive immunity immunodeficiency [4A01] [26]
Mitotane DMU1GX0 Minor Increased metabolism of Lidocaine caused by Mitotane mediated induction of CYP450 enzyme. Adrenal cancer [2D11] [25]
Siltuximab DMGEATB Moderate Altered metabolism of Lidocaine due to Siltuximab alters the formation of CYP450 enzymes. Anemia [3A00-3A9Z] [26]
Dronedarone DMA8FS5 Moderate Decreased metabolism of Lidocaine caused by Dronedarone mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [27]
Methylphenobarbital DMDSWAG Minor Increased metabolism of Lidocaine caused by Methylphenobarbital mediated induction of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [25]
Voriconazole DMAOL2S Moderate Decreased metabolism of Lidocaine caused by Voriconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [28]
Posaconazole DMUL5EW Moderate Decreased metabolism of Lidocaine caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [26]
Obeticholic acid DM3Q1SM Moderate Decreased metabolism of Lidocaine caused by Obeticholic acid mediated inhibition of CYP450 enzyme. Autoimmune liver disease [DB96] [29]
Telithromycin DMZ4P3A Moderate Decreased metabolism of Lidocaine caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [30]
Pexidartinib DMS2J0Z Minor Increased metabolism of Lidocaine caused by Pexidartinib mediated induction of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [25]
Nitazoxanide DMOWLVG Moderate Increased plasma concentration of Lidocaine and Nitazoxanide due to competitive binding of plasma proteins. Bowel habit change [ME05] [31]
Lapatinib DM3BH1Y Moderate Decreased clearance of Lidocaine due to the transporter inhibition by Lapatinib. Breast cancer [2C60-2C6Y] [32]
Tucatinib DMBESUA Moderate Decreased metabolism of Lidocaine caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [33]
Secobarbital DM14RF5 Minor Increased metabolism of Lidocaine caused by Secobarbital mediated induction of CYP450 enzyme. Chronic insomnia [7A00] [25]
Phenylbutazone DMAYL0T Minor Increased metabolism of Lidocaine caused by Phenylbutazone mediated induction of CYP450 enzyme. Chronic pain [MG30] [25]
Mifepristone DMGZQEF Moderate Decreased metabolism of Lidocaine caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [28]
Pasireotide DMHM7JS Moderate Increased risk of bradycardia by the combination of Lidocaine and Pasireotide. Cushing syndrome [5A70] [34]
Osilodrostat DMIJC9X Moderate Decreased metabolism of Lidocaine caused by Osilodrostat mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [35]
Aminoglutethimide DMWFHMZ Minor Increased metabolism of Lidocaine caused by Aminoglutethimide mediated induction of CYP450 enzyme. Cushing syndrome [5A70] [25]
Ivacaftor DMZC1HS Moderate Decreased clearance of Lidocaine due to the transporter inhibition by Ivacaftor. Cystic fibrosis [CA25] [36]
Aprepitant DM053KT Moderate Decreased metabolism of Lidocaine caused by Aprepitant mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [37]
Nefazodone DM4ZS8M Moderate Decreased metabolism of Lidocaine caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [38]
Griseofulvin DMK54YG Minor Increased metabolism of Lidocaine caused by Griseofulvin mediated induction of CYP450 enzyme. Dermatophytosis [1F28] [25]
Primidone DM0WX6I Minor Increased metabolism of Lidocaine caused by Primidone mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [25]
Felbamate DM1V5ZS Minor Increased metabolism of Lidocaine caused by Felbamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [25]
Oxcarbazepine DM5PU6O Minor Increased metabolism of Lidocaine caused by Oxcarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [25]
Cenobamate DM8KLU9 Minor Increased metabolism of Lidocaine caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [25]
Rufinamide DMWE60C Minor Increased metabolism of Lidocaine caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [25]
Phenobarbital DMXZOCG Minor Increased metabolism of Lidocaine caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [26]
Carbamazepine DMZOLBI Minor Increased metabolism of Lidocaine caused by Carbamazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [25]
Tazemetostat DMWP1BH Minor Increased metabolism of Lidocaine caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [25]
Itraconazole DMCR1MV Moderate Decreased metabolism of Lidocaine caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [39]
Omeprazole DM471KJ Minor Increased metabolism of Lidocaine caused by Omeprazole mediated induction of CYP450 enzyme. Gastro-oesophageal reflux disease [DA22] [25]
Cimetidine DMH61ZB Moderate Decreased metabolism of Lidocaine caused by Cimetidine mediated inhibition of CYP450 enzyme. Gastro-oesophageal reflux disease [DA22] [40]
Sulfinpyrazone DMEV954 Minor Increased metabolism of Lidocaine caused by Sulfinpyrazone mediated induction of CYP450 enzyme. Gout [FA25] [25]
Rifampin DMA8J1G Minor Increased metabolism of Lidocaine caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [25]
Rifapentine DMCHV4I Minor Increased metabolism of Lidocaine caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [25]
Delavirdine DM3NF5G Moderate Decreased metabolism of Lidocaine caused by Delavirdine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [41]
Fosamprenavir DM4W9B3 Major Decreased metabolism of Lidocaine caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [34]
Cobicistat DM6L4H2 Moderate Decreased metabolism of Lidocaine caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [26]
Efavirenz DMC0GSJ Minor Increased metabolism of Lidocaine caused by Efavirenz mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [25]
Saquinavir DMG814N Major Decreased metabolism of Lidocaine caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [42]
Etravirine DMGV8QU Moderate Increased metabolism of Lidocaine caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [43]
Amprenavir DMLMXE0 Major Decreased metabolism of Lidocaine caused by Amprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [34]
Darunavir DMN3GCH Moderate Decreased metabolism of Lidocaine caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [44]
Atazanavir DMSYRBX Moderate Decreased metabolism of Lidocaine caused by Atazanavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [28]
Ritonavir DMU764S Moderate Decreased metabolism of Lidocaine caused by Ritonavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [45]
Teriflunomide DMQ2FKJ Minor Increased metabolism of Lidocaine caused by Teriflunomide mediated induction of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [25]
Conivaptan DM1V329 Major Decreased metabolism of Lidocaine caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [46]
Givosiran DM5PFIJ Moderate Decreased metabolism of Lidocaine caused by Givosiran mediated inhibition of CYP450 enzyme. Inborn porphyrin/heme metabolism error [5C58] [47]
Amobarbital DM0GQ8N Minor Increased metabolism of Lidocaine caused by Amobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [25]
Pentobarbital DMFNH7L Minor Increased metabolism of Lidocaine caused by Pentobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [25]
Polyethylene glycol DM4I1JP Moderate Increased risk of lowers seizure threshold by the combination of Lidocaine and Polyethylene glycol. Irritable bowel syndrome [DD91] [48]
Raloxifene DMDKF3M Minor Increased plasma concentration of Lidocaine and Raloxifene due to competitive binding of plasma proteins. Low bone mass disorder [FB83] [49]
Ceritinib DMB920Z Moderate Decreased metabolism of Lidocaine caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [26]
PF-06463922 DMKM7EW Minor Increased metabolism of Lidocaine caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [25]
Osimertinib DMRJLAT Minor Increased metabolism of Lidocaine caused by Osimertinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [25]
Capmatinib DMYCXKL Moderate Decreased metabolism of Lidocaine caused by Capmatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [50]
Selpercatinib DMZR15V Moderate Decreased metabolism of Lidocaine caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [51]
Idelalisib DM602WT Moderate Decreased metabolism of Lidocaine caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [52]
IPI-145 DMWA24P Moderate Decreased metabolism of Lidocaine caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [53]
Vemurafenib DM62UG5 Minor Increased metabolism of Lidocaine caused by Vemurafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [25]
Dabrafenib DMX6OE3 Minor Increased metabolism of Lidocaine caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [25]
Exjade DMHPRWG Minor Increased metabolism of Lidocaine caused by Exjade mediated induction of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [25]
Rifabutin DM1YBHK Minor Increased metabolism of Lidocaine caused by Rifabutin mediated induction of CYP450 enzyme. Mycobacterium infection [1B10-1B21] [25]
Bexarotene DMOBIKY Minor Increased metabolism of Lidocaine caused by Bexarotene mediated induction of CYP450 enzyme. Mycosis fungoides [2B01] [25]
Imatinib DM7RJXL Moderate Decreased metabolism of Lidocaine caused by Imatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [54]
Dasatinib DMJV2EK Moderate Decreased metabolism of Lidocaine caused by Dasatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [55]
Modafinil DMYILBE Minor Increased metabolism of Lidocaine caused by Modafinil mediated induction of CYP450 enzyme. Narcolepsy [7A20] [25]
Bupropion DM5PCS7 Major Increased risk of lowers seizure threshold by the combination of Lidocaine and Bupropion. Nicotine use disorder [6C4A] [56]
Olaparib DM8QB1D Moderate Increased metabolism of Lidocaine caused by Olaparib mediated induction of CYP450 enzyme. Ovarian cancer [2C73] [28]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Lidocaine caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [57]
Prilocaine DMI7DZ2 Major Increased risk of methemoglobinemia by the combination of Lidocaine and Prilocaine. Pain [MG30-MG3Z] [58]
Albendazole DMYZ57N Minor Increased metabolism of Lidocaine caused by Albendazole mediated induction of CYP450 enzyme. Parasitic worm infestation [1F90] [25]
Dopamine DMPGUCF Minor Increased metabolism of Lidocaine caused by Dopamine. Parkinsonism [8A00] [59]
Abametapir DM2RX0I Moderate Decreased metabolism of Lidocaine caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [60]
Lindane DMB8CNL Moderate Increased risk of lowers seizure threshold by the combination of Lidocaine and Lindane. Pediculosis [1G00] [61]
Lefamulin DME6G97 Moderate Decreased metabolism of Lidocaine caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [62]
Lonafarnib DMGM2Z6 Moderate Decreased metabolism of Lidocaine caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [63]
Enzalutamide DMGL19D Minor Increased metabolism of Lidocaine caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [25]
Ustekinumab DMHTYK3 Moderate Altered metabolism of Lidocaine due to Ustekinumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [26]
Ixekizumab DMXW92T Moderate Altered metabolism of Lidocaine due to Ixekizumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [26]
Bosentan DMIOGBU Minor Increased metabolism of Lidocaine caused by Bosentan mediated induction of CYP450 enzyme. Pulmonary hypertension [BB01] [25]
Temsirolimus DMS104F Moderate Increased plasma concentrations of Lidocaine and Temsirolimus due to competitive inhibition of the same metabolic pathway. Renal cell carcinoma [2C90] [64]
Tocilizumab DM7J6OR Moderate Altered metabolism of Lidocaine due to Tocilizumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [26]
Canakinumab DM8HLO5 Moderate Altered metabolism of Lidocaine due to Canakinumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [26]
Rilonacept DMGLUQS Moderate Altered metabolism of Lidocaine due to Rilonacept alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [26]
Golimumab DMHZV7X Moderate Altered metabolism of Lidocaine due to Golimumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [26]
Dexamethasone DMMWZET Minor Increased metabolism of Lidocaine caused by Dexamethasone mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [25]
Nafcillin DMN9RPO Minor Increased metabolism of Lidocaine caused by Nafcillin mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [25]
Sarilumab DMOGNXY Moderate Altered metabolism of Lidocaine due to Sarilumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [26]
Larotrectinib DM26CQR Moderate Decreased metabolism of Lidocaine caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [28]
Armodafinil DMGB035 Minor Increased metabolism of Lidocaine caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [25]
Ibutilide DMKXY2R Moderate Increased risk of bradycardia by the combination of Lidocaine and Ibutilide. Supraventricular tachyarrhythmia [BC81] [65]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Lidocaine caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [66]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Lidocaine due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [57]
Pipecuronium DM5F84A Moderate Additive neuromuscular blocking effects by the combination of Lidocaine and Pipecuronium. Tonus and reflex abnormality [MB47] [23]
Doxacurium DMKE7L9 Moderate Additive neuromuscular blocking effects by the combination of Lidocaine and Doxacurium. Tonus and reflex abnormality [MB47] [23]
Vecuronium DMP0UK2 Moderate Additive neuromuscular blocking effects by the combination of Lidocaine and Vecuronium. Tonus and reflex abnormality [MB47] [23]
Cisatracurium DMUZPJ5 Moderate Additive neuromuscular blocking effects by the combination of Lidocaine and Cisatracurium. Tonus and reflex abnormality [MB47] [23]
Rocuronium DMY9BMK Moderate Additive neuromuscular blocking effects by the combination of Lidocaine and Rocuronium. Tonus and reflex abnormality [MB47] [23]
Sirolimus DMGW1ID Moderate Increased plasma concentrations of Lidocaine and Sirolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [64]
Tacrolimus DMZ7XNQ Moderate Increased plasma concentrations of Lidocaine and Tacrolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [64]
Elagolix DMB2C0E Minor Increased metabolism of Lidocaine caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [25]
Bretylium DM1FX74 Moderate Increased risk of atrioventricular block by the combination of Lidocaine and Bretylium. Ventricular tachyarrhythmia [BC71] [65]
Amiodarone DMUTEX3 Moderate Decreased metabolism of Lidocaine caused by Amiodarone mediated inhibition of CYP450 enzyme. Ventricular tachyarrhythmia [BC71] [67]
Tocainide DMYNMDP Moderate Additive CNS depression effects by the combination of Lidocaine and Tocainide. Ventricular tachyarrhythmia [BC71] [68]
⏷ Show the Full List of 109 DDI Information 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: 2623).
2 Lidocaine FDA Label
3 ClinicalTrials.gov (NCT00651313) Efficacy and Safety Study of Lidocaine Vaginal Gel for Recurrent Dysmenorrhea (Painful Periods). U.S. National Institutes of Health.
4 BDDCS applied to over 900 drugs
5 Electronic Medicines Compendium: Lidocaine 1% w/v solution for injection Monograph
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 StatPearls Internet: Lidocaine Profile
9 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.
10 Mechanisms of analgesia of intravenous lidocaine. Rev Bras Anestesiol. 2008 May-Jun;58(3):280-6.
11 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
12 Pharmacokinetics of lidocaine hydrochloride metabolized by CYP3A4 in Chinese Han volunteers living at low altitude and in native Han and Tibetan Chinese volunteers living at high altitude. Pharmacology. 2016;97(3-4):107-13.
13 Involvement of CYP1A2 and CYP3A4 in lidocaine N-deethylation and 3-hydroxylation in humans. Drug Metab Dispos. 2000 Aug;28(8):959-65.
14 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
15 Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218.
16 Drug Interactions Flockhart Table
17 Insights into CYP2B6-mediated drug-drug interactions. Acta Pharm Sin B. 2016 Sep;6(5):413-425.
18 Binding of disopyramide, methadone, dipyridamole, chlorpromazine, lignocaine and progesterone to the two main genetic variants of human alpha 1-acid glycoprotein: evidence for drug-binding differences between the variants and for the presence of two separate drug-binding sites on alpha 1-acid glycoprotein. Pharmacogenetics. 1996 Oct;6(5):403-15. doi: 10.1097/00008571-199610000-00004.
19 Lidocaine prevents breast cancer growth by targeting neuronatin to inhibit nerve fibers formation. J Toxicol Sci. 2021;46(7):329-339. doi: 10.2131/jts.46.329.
20 Apoptosis and mitochondrial dysfunction in human chondrocytes following exposure to lidocaine, bupivacaine, and ropivacaine. J Bone Joint Surg Am. 2010 Mar;92(3):609-18. doi: 10.2106/JBJS.H.01847.
21 The effect of mild and moderate hepatic impairment on the pharmacokinetics of valdecoxib, a selective COX-2 inhibitor. Eur J Clin Pharmacol. 2005 Jun;61(4):247-56.
22 Evidence of significant contribution from CYP3A5 to hepatic drug metabolism. Drug Metab Dispos. 2004 Dec;32(12):1434-45. doi: 10.1124/dmd.104.001313. Epub 2004 Sep 21.
23 Bruckner J, Thomas KC, Bikhazi GB, Foldes FF "Neuromuscular drug interactions of clinical importance." Anesth Analg 59 (1980): 678-82. [PMID: 7191227]
24 Kharasch ED, Thummel KE "Human alfentanil metabolism by cytochrome P450 3A3/4. An explanation for the interindividual variability in alfentanil clearance?" Anesth Analg 76 (1993): 1033-9. [PMID: 8484504]
25 Heinonen J, Takki S, Jarho L "Plasma lidocaine levels in patients treated with potential inducers of microsomal enzymes." Acta Anaesthesiol Scand 14 (1970): 89-95. [PMID: 5428253]
26 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
27 Product Information. Multaq (dronedarone). sanofi-aventis , Bridgewater, NJ.
28 Cerner Multum, Inc. "Australian Product Information.".
29 Product Information. Ocaliva (obeticholic acid). Intercept Pharmaceuticals, Inc., New York, NY.
30 Product Information. Ketek (telithromycin). Aventis Pharmaceuticals, Bridgewater, NJ.
31 Product Information. Alinia (nitazoxanide). Romark Laboratories L.C., Tampa, FL.
32 Product Information. Tykerb (lapatinib). Novartis Pharmaceuticals, East Hanover, NJ.
33 Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA.
34 Canadian Pharmacists Association.
35 Product Information. Isturisa (osilodrostat). Recordati Rare Diseases Inc, Lebanon, NJ.
36 Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
37 Product Information. Emend (aprepitant). Merck & Company Inc, West Point, PA.
38 Product Information. Serzone (nefazodone). Bristol-Myers Squibb, Princeton, NJ.
39 Auclair B, Berning SE, Huitt GA, Peloquin CP "Potential interaction between itraconazole and clarithromycin." Pharmacotherapy 19 (1999): 1439-44. [PMID: 10600094]
40 Berk SI, Gal P, Bauman JL, et al "The effect of oral cimetidine on total and unbound serum lidocaine concentrations in patients with suspected myocardial infarction." Int J Cardiol 14 (1987): 91-4. [PMID: 3804509]
41 Product Information. Rescriptor (delavirdine). Pharmacia and Upjohn, Kalamazoo, MI.
42 Product Information. Fortovase (saquinavir) Roche Laboratories, Nutley, NJ.
43 Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
44 Product Information. Prezista (darunavir). Ortho Biotech Inc, Bridgewater, NJ.
45 Olkkola KT, Palkama VJ, Neuvonen PJ "Ritonavir's role in reducing fentanyl clearance and prolonging its half-life." Anesthesiology 91 (1999): 681-5. [PMID: 10485779]
46 Product Information. Vaprisol (conivaptan). Cumberland Pharmaceuticals Inc, Nashville, TN.
47 Product Information. Givlaari (givosiran). Alnylam Pharmaceuticals, Cambridge, MA.
48 Product Information. Suprep Bowel Prep Kit (magnesium/potassium/sodium sulfates). Braintree Laboratories, Braintree, MA.
49 Product Information. Evista (raloxifene). Lilly, Eli and Company, Indianapolis, IN.
50 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
51 Product Information. Retevmo (selpercatinib). Lilly, Eli and Company, Indianapolis, IN.
52 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
53 Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
54 Product Information. Gleevec (imatinib mesylate). Novartis Pharmaceuticals, East Hanover, NJ.
55 Product Information. Sprycel (dasatinib). Bristol-Myers Squibb, Princeton, NJ.
56 Product Information. Wellbutrin XL (buPROPion). GlaxoSmithKline, Philadelphia, PA.
57 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
58 Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
59 Sprung J, Bourke DL, Schoenwald PK, Whalley D, Gottlieb A, Mascha EJ, Kapural L "Small-dose dopamine increases epidural lidocaine requirements during peripheral vascular surgery in elderly patients." Anesth Analg 90 (2000): 388-92. [PMID: 10648327]
60 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
61 Matsuoka LY "Convulsions following application of gamma benzene hexachloride." J Am Acad Dermatol 5 (1981): 98-9. [PMID: 6168673]
62 Product Information. Fycompa (perampanel). Eisai Inc, Teaneck, NJ.
63 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
64 Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL.
65 Keidar S, Grenadier E, Palant A "Sinoatrial arrest due to lidocaine injection in sick sinus syndrome during amiodarone administration." Am Heart J 104 (1982): 1384-5. [PMID: 7148661]
66 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
67 Ha HR, Candinas R, Stieger B, Meyer UA, Follath F "Interaction between amiodarone and lidocaine." J Cardiovasc Pharmacol 28 (1996): 533-9. [PMID: 8891878]
68 Product Information. Tonocard (tocainide). Merck & Co, Inc, West Point, PA.