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LIDOCAINE Drug Record

  • Summary
  • Interactions
  • Claims
  • LIDOCAINE chembl:CHEMBL79 Approved

    Alternate Names:

    ALGRX 3268
    XYLOCAINE
    VAGISIL
    LIDOPEN
    LIGNOCAINE
    OCTOCAINE
    LIDOCAINE
    ORAQIX
    NSC-40030
    XYLODASE
    LIGNOCAINE HCL
    IONTOCAINE
    LMX 4
    LIDOCATON
    ANESTACON
    DENTIPATCH
    ZTLIDO
    ALGRX-3268
    ALPHACAINE
    XYLOTOX
    EMBOLEX
    LIGNOSTAB
    LIDODERM
    Α-DIETHYLAMINO-2,6-DIMETHYLACETANILIDE
    2-(DIETHYLAMINO)-N-(2,6-DIMETHYLPHENYL)ACETAMIDE
    ALPHA-DIETHYLAMINO-2,6-DIMETHYLACETANILIDE
    2-(DIETHYLAMINO)-2',6'-ACETOXYLIDIDE
    XYLOCAINE®
    chemidplus:137-58-6
    rxcui:6387
    pubchem.compound:3676
    chembl:CHEMBL79
    drugbank:00281

    Drug Info:

    Drug Indications for treatment of pelvic pain of bladder origin and interstitital cystitis
    Drug Indications for treatment of premature ejaculation
    Drug Indications anestethic
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications anesthetic
    Drug Class anesthetics, local
    Drug Class anti-arrhythmia agents
    Year of Approval approved before 1982
    Drug Categories agents for treatment of hemorrhoids and anal fissures for topical use
    Drug Categories agents that reduce seizure threshold
    Drug Categories amide local anesthetic
    Drug Categories amines
    Drug Categories analgesics and anesthetics
    Drug Categories anesthetics for topical use
    Drug Categories aniline compounds
    Drug Categories antiarrhythmic agents
    Drug Categories antiarrhythmics, class i
    Drug Categories antiarrhythmics, class ib
    Drug Categories antipruritics and local anesthetics
    Drug Categories antipruritics, incl. antihistamines, anesthetics, etc.
    Drug Categories cardiac therapy
    Drug Categories cytochrome p-450 cyp2c18 substrates
    Drug Categories cytochrome p-450 cyp2d6 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a5 substrates
    Drug Categories cytochrome p-450 cyp3a7 substrates
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories dermatologicals
    Drug Categories local anesthesia
    Drug Categories neuraxial anesthetics
    Drug Categories ophthalmologicals
    Drug Categories otologicals
    Drug Categories p-glycoprotein inhibitors
    Drug Categories throat preparations
    Drug Categories vasoprotectives
    (7 More Sources)

    Publications:

    Fedida et al., 2006, The role of late I and antiarrhythmic drugs in EAD formation and termination in Purkinje fibers., J. Cardiovasc. Electrophysiol.
    Itoh et al., 2007, A paradoxical effect of lidocaine for the N406S mutation of SCN5A associated with Brugada syndrome., Int. J. Cardiol.
    Wallace et al., 2006, Inhibition of cardiac voltage-gated sodium channels by grape polyphenols., Br. J. Pharmacol.
    Cerne et al., 2006, Pre-ovarian block versus paracervical block for oocyte retrieval., Hum. Reprod.
    Karoly et al., 2010, Fast- or slow-inactivated state preference of Na+ channel inhibitors: a simulation and experimental study., PLoS Comput. Biol.
    Muroi et al., 2009, Local anesthetics disrupt energetic coupling between the voltage-sensing segments of a sodium channel., J. Gen. Physiol.
    Isohanni et al., 1998, Effect of erythromycin and itraconazole on the pharmacokinetics of intravenous lignocaine., Eur. J. Clin. Pharmacol.
    Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
    Sheets et al., 2007, A Nav1.7 channel mutation associated with hereditary erythromelalgia contributes to neuronal hyperexcitability and displays reduced lidocaine sensitivity., J. Physiol. (Lond.)
    Matayoshi et al., 2005, Actions of brain-derived neurotrophic factor on spinal nociceptive transmission during inflammation in the rat., J. Physiol. (Lond.)
    Ekberg et al., 2006, muO-conotoxin MrVIB selectively blocks Nav1.8 sensory neuron specific sodium channels and chronic pain behavior without motor deficits., Proc. Natl. Acad. Sci. U.S.A.
    Sakaguchi et al., 2006, The antiproliferative effect of lidocaine on human tongue cancer cells with inhibition of the activity of epidermal growth factor receptor., Anesth. Analg.
    Do et al., 2002, The effects of lidocaine on the activity of glutamate transporter EAAT3: the role of protein kinase C and phosphatidylinositol 3-kinase., Anesth. Analg.
    Behbehani et al., 1996, Properties of a projection pathway from the medial preoptic nucleus to the midbrain periaqueductal gray of the rat and its role in the regulation of cardiovascular function., Brain Res.
    Leuwer M et al., 2004, An improved model for the binding of lidocaine and structurally related local anaesthetics to fast-inactivated voltage-operated sodium channels, showing evidence of cooperativity., Br J Pharmacol
    Hervé et al., 1996, 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
  • LIDOCAINE   ORM1

    Interaction Score: 1.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8946472


    Sources:
    DrugBank

  • LIDOCAINE   ORM2

    Interaction Score: 1.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8946472


    Sources:
    DrugBank

  • LIDOCAINE   SLC1A1

    Interaction Score: 0.79

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12401608


    Sources:
    NCI

  • LIDOCAINE   SCN5A

    Interaction Score: 0.41

    Interaction Types & Directionality:
    blocker (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Pore blocker
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    16686685 17445919 17016511 16840798 20585544 19088384


    Sources:
    TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

  • LIDOCAINE   SCN9A

    Interaction Score: 0.32

    Interaction Types & Directionality:
    blocker (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes
    Trial Name ALGRX 3268,Zingo

    PMIDs:
    17430993 20585544 19088384


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • LIDOCAINE   SCN10A

    Interaction Score: 0.29

    Interaction Types & Directionality:
    blocker (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name ALGRX 3268,Zingo
    Novel drug target Established target
    Trial Name lidocaine hydrochloride, piroxicam, AK1015,Akten

    PMIDs:
    20585544 17077153 19088384


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • LIDOCAINE   MPO

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8973808


    Sources:
    NCI

  • LIDOCAINE   SCN4A

    Interaction Score: 0.14

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    14662728


    Sources:
    DrugBank ChemblInteractions

  • LIDOCAINE   SCN11A

    Interaction Score: 0.11

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TTD ChemblInteractions

  • LIDOCAINE   BDNF

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16210356


    Sources:
    NCI

  • LIDOCAINE   SCN7A

    Interaction Score: 0.06

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LIDOCAINE   SCN8A

    Interaction Score: 0.05

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LIDOCAINE   SCN3A

    Interaction Score: 0.05

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LIDOCAINE   EGFR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name PSD502, lidocaine + prilocaine
    Novel drug target Established target

    PMIDs:
    16551906


    Sources:
    TdgClinicalTrial DrugBank

  • LIDOCAINE   SCN2A

    Interaction Score: 0.05

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sodium channel alpha subunit blocker
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LIDOCAINE   G6PD

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Combination therapy Lidocaine,Prilocaine
    Combination therapy Lidocaine,Tetracaine

    PMIDs:
    None found


    Sources:
    FDA

  • LIDOCAINE   SCN1A

    Interaction Score: 0.04

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Sodium channel alpha subunit blocker

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LIDOCAINE   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9832299 9187528


    Sources:
    NCI PharmGKB

  • DrugBank: DB00281

    • Version: 5.1.7

    Alternate Names:
    LIDOCAINE DrugBank Drug Name
    137-58-6 CAS Number
    0.4% Lidocaine Hydrochloride and 5% Dextrose Injection Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Groups vet_approved

    Publications:
    Hervé et al., 1996, 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
    Sheets et al., 2007, A Nav1.7 channel mutation associated with hereditary erythromelalgia contributes to neuronal hyperexcitability and displays reduced lidocaine sensitivity., J. Physiol. (Lond.)
    Karoly et al., 2010, Fast- or slow-inactivated state preference of Na+ channel inhibitors: a simulation and experimental study., PLoS Comput. Biol.

  • TEND: LIDOCAINE

    • Version: 01-August-2011

    Alternate Names:
    LIDOCAINE Primary Drug Name

    Drug Info:
    Year of Approval approved before 1982
    Drug Class anti-arrhythmia agents
    Drug Class anesthetics, local

    Publications:

  • TdgClinicalTrial: LIDOCAINE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications anesthetic
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • NCI: LIGNOCAINE

    • Version: 14-September-2017

    Alternate Names:
    C614 NCI drug code

    Drug Info:

    Publications:
    Isohanni et al., 1998, Effect of erythromycin and itraconazole on the pharmacokinetics of intravenous lignocaine., Eur. J. Clin. Pharmacol.

  • NCI: LIDOCAINE

    • Version: 14-September-2017

    Alternate Names:
    C614 NCI drug code

    Drug Info:

    Publications:
    Matayoshi et al., 2005, Actions of brain-derived neurotrophic factor on spinal nociceptive transmission during inflammation in the rat., J. Physiol. (Lond.)
    Behbehani et al., 1996, Properties of a projection pathway from the medial preoptic nucleus to the midbrain periaqueductal gray of the rat and its role in the regulation of cardiovascular function., Brain Res.
    Do et al., 2002, The effects of lidocaine on the activity of glutamate transporter EAAT3: the role of protein kinase C and phosphatidylinositol 3-kinase., Anesth. Analg.

  • PharmGKB: lidocaine

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev

  • GuideToPharmacology: 135650521

    • Version: 29-September-2020

    Alternate Names:
    LIDOCAINE GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • TTD: Lidocaine

    • Version: 2020.06.01

    Alternate Names:
    D0X4RN TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL79

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Lidocaine

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL79

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21