DGIdb - LIDOCAINE Drug Record

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:

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

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

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

Trial Name	PSD502, lidocaine + prilocaine
Novel drug target	Established target

Combination therapy	Lidocaine,Prilocaine
Combination therapy	Lidocaine,Tetracaine

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

Drug Type	small molecule
Drug Groups	approved
Drug Groups	vet_approved

blocker (inhibitory)
inhibitor (inhibitory)

blocker (inhibitory)
inhibitor (inhibitory)

blocker (inhibitory)
inhibitor (inhibitory)

LIDOCAINE Drug Record

LIDOCAINE chembl:CHEMBL79 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8946472

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8946472

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12401608

Sources: NCI

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

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

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8973808

Sources: NCI

Interaction Types & Directionality: blocker (inhibitory)

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

PMIDs: 14662728

Sources: DrugBank ChemblInteractions

Interaction Types & Directionality: blocker (inhibitory)

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

PMIDs: None found

Sources: TTD ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16210356

Sources: NCI

Interaction Types & Directionality: blocker (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: blocker (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: blocker (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 16551906

Sources: TdgClinicalTrial DrugBank

Interaction Types & Directionality: blocker (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: FDA

Interaction Types & Directionality: blocker (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9832299 9187528

Sources: NCI PharmGKB

DrugBank: DB00281

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

Interaction Types & Directionality:

n/a

PMIDs:
8946472

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
8946472

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
12401608

Sources:
NCI

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

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

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

Interaction Types & Directionality:

n/a

PMIDs:
8973808

Sources:
NCI

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
14662728

Sources:
DrugBank ChemblInteractions

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
TTD ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
16210356

Sources:
NCI

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name PSD502, lidocaine + prilocaine

Novel drug target Established target

PMIDs:
16551906

Sources:
TdgClinicalTrial DrugBank

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Combination therapy Lidocaine,Prilocaine

Combination therapy Lidocaine,Tetracaine

PMIDs:
None found

Sources:
FDA

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
9832299 9187528

Sources:
NCI PharmGKB

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

Alternate Names:

LIDOCAINE Primary Drug Name

Drug Info:

Year of Approval approved before 1982

Drug Class anti-arrhythmia agents

Drug Class anesthetics, local

Drug Info:

Drug Indications anesthetic

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

C614 NCI drug code

Publications:

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

Alternate Names:

C614 NCI drug code

Publications:

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

Alternate Names:

LIDOCAINE GuideToPharmacology Ligand Name

Alternate Names:

D0X4RN TTD Drug ID