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Identification
NameLidocaine
Accession NumberDB00281  (APRD00479, DB05291)
TypeSmall Molecule
GroupsApproved
Description

A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of procaine but its duration of action is shorter than that of bupivacaine or prilocaine. [PubChem]

Structure
Thumb
Synonyms
SynonymLanguageCode
2-(Diethylamino)-2',6'-acetoxylidideNot AvailableNot Available
2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamideNot AvailableNot Available
alpha-diethylamino-2,6-dimethylacetanilideNot AvailableNot Available
LidocaineNot AvailableNot Available
LidodermNot AvailableNot Available
LignocaineNot AvailableNot Available
α-diethylamino-2,6-dimethylacetanilideNot AvailableNot Available
Salts
Name/CAS Structure Properties
Lidocaine hydrochloride
Thumb Not applicable DBSALT000900
Brand names
NameCompany
After Burn Double Strength GelNot Available
After Burn Double Strength SprayNot Available
After Burn GelNot Available
After Burn SprayNot Available
AktenNot Available
AlphacaineNot Available
AnestaconNot Available
Anestacon JellyNot Available
DermaFlexNot Available
DilocaineNot Available
EsracaineNot Available
L-CaineNot Available
Laryng-O-JetNot Available
LidodermNot Available
Lidoject-1Not Available
Lidoject-2Not Available
Norwood Sunburn SprayNot Available
SolarcaineNot Available
XylocaineNot Available
Xylocaine-MPFNot Available
XylocardNot Available
Zilactin-LNot Available
ZingoNot Available
Brand mixtures
Brand NameIngredients
0.4% Lidocaine Hydrochloride and 5% Dextrose Injection UspDextrose + Lidocaine Hydrochloride
Alphacaine Hcl 2% W Epineph 1:100000Epinephrine + Lidocaine Hydrochloride
Alphacaine Hcl 2% W Epineph 1:50000Epinephrine + Lidocaine Hydrochloride
Arrow Central Venous Catheterization KitLidocaine Hydrochloride + Povidone-Iodine
Arrow Multi-Lumen Central Venous Catheter KitLidocaine Hydrochloride + Povidone-Iodine
Arrow Pneumothorax KitLidocaine Hydrochloride + Povidone-Iodine
Arrow Two-Lumen Central Venous Cathetar KitLidocaine Hydrochloride + Povidone-Iodine
Arrow Two-Lumen Jugular Catheterization KitLidocaine Hydrochloride + Povidone-Iodine
Baciguent Plus Pain Reliever OntBacitracin + Lidocaine
Bactine First Aid Spray LiqBenzalkonium Chloride + Lidocaine Hydrochloride
Banana Boat Sooth-a-Caine W.Moist.Aloe V.GelLidocaine + Menthol
Burncare KitBenzocaine + Lidocaine Hydrochloride
CaustinerfCamphor + Chlorophenol + Lidocaine + Paraformaldehyde
Central Vein Catheterization KitLidocaine Hydrochloride + Povidone-Iodine
Central Venous Catetherization KitLidocaine Hydrochloride + Povidone-Iodine
Central Venous Catheter Expanded KitLidocaine Hydrochloride + Povidone-Iodine
Central Venous Catheterization KitLidocaine Hydrochloride + Povidone-Iodine
Continuous Epidural Anesthesia TrayLidocaine Hydrochloride + Sodium Chloride
EMLALidocaine + Prilocaine
Epidural Anesthesia TrayIodine (Povidone-Iodine) + Lidocaine Hydrochloride + Sodium Chloride
Expanded Multi-Med KitLidocaine Hydrochloride + Povidone-Iodine
Family Medic First Aid Treatment - LiqBenzalkonium Chloride + Lidocaine Hydrochloride
Genetic Amniocentesis Tray KitIodine (Povidone-Iodine) + Lidocaine Hydrochloride
Hydrocath Central Venous Catheter KitLidocaine Hydrochloride + Povidone-Iodine
Jamshidi Bone Marrow Biopsy TrayLidocaine Hydrochloride + Povidone-Iodine
Jamshidi Menghini Soft Tissue Biopsy TrayLidocaine Hydrochloride + Povidone-Iodine + Sodium Chloride
Lidocaine 0.2% in 5% Dextrose InjDextrose + Lidocaine Hydrochloride
Lidocaine 2% Sterile Injectable SolutionEpinephrine Racemic + Lidocaine Hydrochloride
Lidocaine 2% with Epinephrine 1:100000Epinephrine + Lidocaine Hydrochloride
Lidocaine and Epinephrine Inj.Usp2% 1:100000Epinephrine + Lidocaine Hydrochloride
Lidocaine Hcl 2%Epinephrine + Lidocaine Hydrochloride
Lidocaine Hcl 2% Epinephrine InjEpinephrine + Lidocaine Hydrochloride
Lidocaine Hcl 2% W Epineph 1:100000injEpinephrine + Lidocaine Hydrochloride
Lidocaine Hcl 2% W EpinephrineEpinephrine + Lidocaine Hydrochloride
Lidocaine Hcl 2% W Epinephrine 1:100000Epinephrine + Lidocaine Hydrochloride
Lidocaine Hcl 2% W Epinephrine 1:50000Epinephrine + Lidocaine Hydrochloride
Lidocaine Inj 2%Epinephrine Hcl + Lidocaine Hydrochloride
Lidosporin CreamGramicidin + Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)
Lidosporin Ear DropsLidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)
Multi-Lumen Central Venous Cathet KitIodine (Povidone-Iodine) + Lidocaine Hydrochloride
Octocaine 100 Needleject InjEpinephrine + Lidocaine Hydrochloride
OraqixLidocaine + Prilocaine
Otizol Hc LiqHydrocortisone (Hydrocortisone Acetate) + Lidocaine (Lidocaine Hydrochloride) + Neomycin (Neomycin Sulfate)
Ozonol Antibiotic Plus - OintmentBacitracin + Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)
Ozonol Antibiotic Plus OntBacitracin + Lidocaine Hydrochloride + Polymyxin B Sulfate
Pacing Catheter Introducer Kit Acp-001pxLidocaine Hydrochloride + Povidone-Iodine
Paracentesis Tray W Boasberg Catheter SetLidocaine Hydrochloride + Povidone-Iodine
Percutaneous Sheath Intro Kit Ak-09810-SIodine (Povidone-Iodine) + Lidocaine Hydrochloride (Povidone-Iodine)
Percutaneous Sheath Introducer KitIodine (Povidone-Iodine) + Lidocaine Hydrochloride
Percutaneous Sheath Introducer TrayLidocaine Hydrochloride + Povidone-Iodine
Peritoneal Lavage Kit InjIodine (Povidone-Iodine) + Lidocaine Hydrochloride
Pharmassist Soothenel GelBenzethonium Chloride + Lidocaine Hydrochloride
Pleura-Seal Thoracentesis KitIodine (Povidone-Iodine) + Lidocaine Hydrochloride
Polyderm Antibiotic OintmentBacitracin + Lidocaine Hydrochloride + Polymyxin B Sulfate
Polysporin Antibiotic Burn CreamGramicidin + Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)
Polysporin Burn Formula CreamGramicidin + Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)
Racestyptine CordAluminum Chloride + Lidocaine + Oxyquinoline Sulfate
Two-Lumen Central Venous Catheter KitIodine (Povidone-Iodine) + Lidocaine Hydrochloride
Xylocaine - MPF 5% with Glucose 7.5%Dextrose + Lidocaine Hydrochloride
Xylocaine 0.5% W Epinephrine 1:100000Epinephrine + Lidocaine Hydrochloride
Xylocaine 0.5% W Epinephrine 1:200000Epinephrine + Lidocaine Hydrochloride
Xylocaine MPF 1.5% with EpinephrineEpinephrine + Lidocaine Hydrochloride
Xylocaine Oral SprayCetylpyridinium Chloride + Lidocaine Hydrochloride
Xylonor SprayCetrimonium Bromide + Lidocaine
Categories
CAS number137-58-6
WeightAverage: 234.3373
Monoisotopic: 234.173213336
Chemical FormulaC14H22N2O
InChI KeyNNJVILVZKWQKPM-UHFFFAOYSA-N
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)
IUPAC Name
2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide
SMILES
CCN(CC)CC(=O)NC1=C(C)C=CC=C1C
Mass Specshow(7.18 KB)
Taxonomy
KingdomOrganic Compounds
SuperclassOrganic Acids and Derivatives
ClassCarboxylic Acids and Derivatives
SubclassAmino Acids, Peptides, and Analogues
Direct parentAlpha Amino Acid Amides
Alternative parentsAnilides; Toluenes; Secondary Carboxylic Acid Amides; Tertiary Amines; Enolates; Carboxylic Acids; Polyamines
Substituentsacetanilide; toluene; benzene; carboxamide group; tertiary amine; secondary carboxylic acid amide; enolate; carboxylic acid; polyamine; amine; organonitrogen compound
Classification descriptionThis compound belongs to the alpha amino acid amides. These are amide derivatives of alpha amino acids.
Pharmacology
IndicationFor production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks.
PharmacodynamicsLidocaine is an anesthetic agent indicated for production of local or regional anesthesia and in the treatment of ventricular tachycardia occurring during cardiac manipulation, such as surgery or catheterization, or which may occur during acute myocardial infarction, digitalis toxicity, or other cardiac diseases. The mode of action of the antiarrhythmic effect of Lidocaine appears to be similar to that of procaine, procainamide and quinidine. Ventricular excitability is depressed and the stimulation threshold of the ventricle is increased during diastole. The sinoatrial node is, however, unaffected. In contrast to the latter 3 drugs, Lidocaine in therapeutic doses does not produce a significant decrease in arterial pressure or in cardiac contractile force. In larger doses, lidocaine may produce circulatory depression, but the magnitude of the change is less than that found with comparable doses of procainamide.
Mechanism of actionLidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action. Lidocaine alters signal conduction in neurons by blocking the fast voltage gated sodium (Na+) channels in the neuronal cell membrane that are responsible for signal propagation. With sufficient blockage the membrane of the postsynaptic neuron will not depolarize and will thus fail to transmit an action potential. This creates the anaesthetic effect by not merely preventing pain signals from propagating to the brain but by aborting their birth in the first place.
AbsorptionInformation derived from diverse formulations, concentrations and usages reveals that lidocaine is completely absorbed following parenteral administration, its rate of absorption depending, for example, upon various factors such as the site of administration and the presence or absence of a vasoconstrictor agent.
Volume of distribution
  • 0.7 to 2.7 L/kg [healthy volunteers]
Protein binding60-80%
Metabolism

Primarily hepatic.

SubstrateEnzymesProduct
Lidocaine
3-hydroxylidocaineDetails
Lidocaine
monoethylglycinexylidideDetails
Lidocaine
Not Available
2,6-Dimethylaniline (2,6-Xylidine)Details
3-hydroxylidocaine
Not Available
3-HydroxymonoethylglycinexylidideDetails
monoethylglycinexylidide
Not Available
3-HydroxymonoethylglycinexylidideDetails
monoethylglycinexylidide
Not Available
2,6-Dimethylaniline (2,6-Xylidine)Details
monoethylglycinexylidide
Not Available
Glycinexylidide (GX)Details
Glycinexylidide (GX)
Not Available
2,6-Dimethylaniline (2,6-Xylidine)Details
2,6-Dimethylaniline (2,6-Xylidine)
Not Available
2-Amino-3-methylbenzoateDetails
2,6-Dimethylaniline (2,6-Xylidine)
Not Available
4-Hydroxy-2,6-dimethylanilineDetails
2,6-Dimethylaniline (2,6-Xylidine)
Not Available
2-Amino-3-methylbenzoateDetails
2,6-Dimethylaniline (2,6-Xylidine)
Not Available
2-Amino-3-methylbenzoateDetails
2,6-Dimethylaniline (2,6-Xylidine)
Not Available
4-Hydroxy-2,6-dimethylanilineDetails
2,6-Dimethylaniline (2,6-Xylidine)
Not Available
4-Hydroxy-2,6-dimethylanilineDetails
Route of eliminationLidocaine and its metabolites are excreted by the kidneys.
Half life109 minutes
Clearance
  • 0.64 +/- 0.18 L/min
ToxicityThe oral LD 50 of lidocaine HCl in non-fasted female rats is 459 (346-773) mg/kg (as the salt) and 214 (159-324) mg/kg (as the salt) in fasted female rats. Symptoms of overdose include convulsions, hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Lidocaine (Local Anaesthetic) Metabolism PathwayDrug metabolismSMP00620
Lidocaine (Antiarrhythmic) Action PathwayDrug actionSMP00328
Lidocaine (Local Anaesthetic) Action PathwayDrug actionSMP00398
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption Not Available Not Available
Blood Brain Barrier Not Available Not Available
Caco-2 permeable Not Available Not Available
P-glycoprotein substrate Not Available Not Available
P-glycoprotein inhibitor I Not Available Not Available
P-glycoprotein inhibitor II Not Available Not Available
Renal organic cation transporter Not Available Not Available
CYP450 2C9 substrate Not Available Not Available
CYP450 2D6 substrate Not Available Not Available
CYP450 3A4 substrate Not Available Not Available
CYP450 1A2 substrate Not Available Not Available
CYP450 2C9 substrate Not Available Not Available
CYP450 2D6 substrate Not Available Not Available
CYP450 2C19 substrate Not Available Not Available
CYP450 3A4 substrate Not Available Not Available
CYP450 inhibitory promiscuity Not Available Not Available
Ames test Not Available Not Available
Carcinogenicity Not Available Not Available
Biodegradation Not Available Not Available
Rat acute toxicity Not Available Not applicable
hERG inhibition (predictor I) Not Available Not Available
hERG inhibition (predictor II) Not Available Not Available
Pharmacoeconomics
Manufacturers
  • Astrazeneca lp
  • Noven pharmaceuticals inc
  • Carlisle laboratories inc
  • E fougera div altana inc
  • Graham chemical co
  • Taro pharmaceuticals usa inc
  • Teikoku pharma usa inc
  • Abbott laboratories pharmaceutical products div
  • Abbott laboratories hosp products div
  • Abraxis pharmaceutical products
  • Akorn inc
  • Baxter healthcare corp anesthesia and critical care
  • Bel mar laboratories inc
  • Dell laboratories inc
  • Elkins sinn div ah robins co inc
  • Gd searle llc
  • Hospira inc
  • International medication systems ltd
  • International medication system
  • Luitpold pharmaceuticals inc
  • Miles laboratories inc
  • Watson laboratories inc
  • Wyeth ayerst laboratories
  • Baxter healthcare corp
  • B braun medical inc
  • App pharmaceuticals llc
  • Meridian medical technologies inc
  • Dentsply pharmaceutical
  • Polymedica industries inc
  • Teva pharmaceuticals usa
  • Hi tech pharmacal co inc
  • Wockhardt eu operations (swiss) ag
  • Actavis mid atlantic llc
  • Vintage pharmaceuticals llc
  • Roxane laboratories inc
  • Kendall co
  • Paco research corp
  • Anesiva inc
Packagers
Dosage forms
FormRouteStrength
AerosolTopical
Aerosol, meteredTopical
CreamTopical
GelTopical
JellyTopical
JellyUrethral
LiquidBuccal
LiquidDental
LiquidInfiltration
LiquidIntravenous
LiquidOral
LiquidTopical
LotionTopical
OintmentTopical
SolutionInfiltration
SolutionIntramuscular
SolutionIntravenous
SolutionOral
SolutionTopical
SprayTopical
SwabTopical
Prices
Unit descriptionCostUnit
Rocephin 10 gm vial478.32USDeach
Lidocaine HCl 3% Lotion 177ml Bottle230.3USDbottle
Rocephin 2 gm vial97.5USDeach
Rocephin 1 gm vial62.02USDeach
EMLA 2.5-2.5% Cream 30 gm Tube58.4USDtube
Lidocaine-Prilocaine 2.5-2.5% Cream 30 gm Tube47.79USDtube
Lidocaine HCl 2% Gel 10ml Syringe17.99USDsyringe
Lidocaine HCl 2% Gel 30ml Tube17.99USDtube
Lidocaine HCl 4% Solution 50ml Bottle16.99USDbottle
Lidocaine Viscous 2% Solution 100ml Bottle13.99USDbottle
Lidocaine hcl 1% syringe9.76USDml
Lidocaine HCl 4% Solution 4ml Bottle9.42USDbottle
Lidoderm 1 Box = 30 Patches8.03USDpatch
Akten 3.5% drops7.5USDml
Lidocaine 5% in d7.5w ampul3.06USDml
Lidocaine 3% cream2.91USDg
Lidamantle 3% cream2.03USDg
Zilactin-l cold sore liquid0.99USDml
Xylocaine 2% jelly0.68USDml
Lidocaine hcl 10% vial0.55USDml
Xylocaine 5% ointment0.42USDg
Xylocaine Jelly 2 % Jelly0.41USDg
Xylocaine 2% Solution0.34USDml
Xylocaine 5 % Ointment0.29USDg
Lidocaine HCl 1% Solution0.24USDml
Lidocaine hcl powder0.24USDg
Lidocaine base powder0.22USDg
Lidocaine hcl 4% solution0.18USDml
Xylocaine 0.5% vial0.18USDml
Lidodan 5 % Ointment0.16USDg
Xylocaine Viscous 2 % Liquid0.1USDml
Lidocaine hcl 0.5% vial0.08USDml
Solarcaine aerosol0.06USDg
Lidodan Viscous 2 % Liquid0.06USDml
Lidocaine 2% viscous solution0.03USDml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States60042861997-03-172017-03-17
United States52349571994-02-272011-02-27
Properties
Statesolid
Experimental Properties
PropertyValueSource
melting point68.5 °CPhysProp
boiling point159-160 °C at 2.00E+00 mm HgPhysProp
water solubility4100 mg/L (at 30 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.44AVDEEF,A (1997)
logS-1.76ADME Research, USCD
Caco2 permeability-4.21ADME Research, USCD
pKa8.01SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.593ALOGPS
logP1.81ALOGPS
logP2.84ChemAxon
logS-2.6ALOGPS
pKa (Strongest Acidic)13.78ChemAxon
pKa (Strongest Basic)7.75ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area32.34 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity73.93 m3·mol-1ChemAxon
Polarizability27.77 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Spectra
Spectra1D NMR
References
Synthesis Reference

DrugSyn.org

US2441498A
General Reference
  1. Khaliq W, Alam S, Puri N: Topical lidocaine for the treatment of postherpetic neuralgia. Cochrane Database Syst Rev. 2007 Apr 18;(2):CD004846. Pubmed
  2. Thomson PD, Melmon KL, Richardson JA, Cohn K, Steinbrunn W, Cudihee R, Rowland M: Lidocaine pharmacokinetics in advanced heart failure, liver disease, and renal failure in humans. Ann Intern Med. 1973 Apr;78(4):499-508. Pubmed
External Links
ResourceLink
KEGG DrugD00358
PubChem Compound3676
PubChem Substance46505060
ChemSpider3548
ChEBI6456
ChEMBLCHEMBL79
Therapeutic Targets DatabaseDAP000121
PharmGKBPA450226
IUPHAR2623
Guide to Pharmacology2623
Drug Product Database712884
RxListhttp://www.rxlist.com/cgi/generic2/xylocaineinj.htm
Drugs.comhttp://www.drugs.com/cdi/lidocaine-gel.html
WikipediaLidocaine
ATC CodesC01BB01C05AD01D04AB01N01BB02R02AD02S01HA07S02DA01A01AD11
AHFS Codes
  • 24:04.04
  • 52:16.00
  • 24:04.04.08
  • 72:00.00
  • 84:08.00
PDB EntriesNot Available
FDA labelshow(548 KB)
MSDSshow(74.6 KB)
Interactions
Drug Interactions
Drug
AcebutololThe beta-blocker, acebutolol, may increase the effect and toxicity of lidocaine.
AtazanavirIncreased risk of cardiotoxicity and arrhythmias
AtenololThe beta-blocker, atenolol, may increase the effect and toxicity of lidocaine.
BisoprololThe beta-blocker, bisoprolol, may increase the effect and toxicity of lidocaine.
CarvedilolThe beta-blocker, carvedilol, may increase the effect and toxicity of lidocaine.
CimetidineIncreases the effect and toxicity of lidocaine
DarunavirPossible increase in lidocaine levels
EsmololThe beta-blocker, esmolol, may increase the effect and toxicity of lidocaine.
EtravirineLidocaine, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to monitor lidocaine therapy.
LabetalolThe beta-blocker, labetalol, may increase the effect and toxicity of lidocaine.
MetoprololThe beta-blocker, metoprolol, may increase the effect and toxicity of lidocaine
NadololThe beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
OxprenololThe beta-blocker increases the effect and toxicity of lidocaine
PenbutololPenbutolol increases the volume of distribution of lidocaine in normal subjects. This could result in a requirement for higher loading doses of lidocaine.
PindololThe beta-blocker increases the effect and toxicity of lidocaine
PropranololThe beta-blocker, propranolol, may increase the effect and toxicity of lidocaine.
QuinupristinThis combination presents an increased risk of toxicity
TacrineThe metabolism of Tacrine, a CYP1A2 substrate, may be reduced by strong CYP1A2 inhibitors such as Lidocaine. Consider modifying therapy to avoid Tacrine toxicity. Monitor the efficacy and toxicity of Tacrine if Lidocaine is initiated, discontinued or if the dose is changed.
TamoxifenLidocaine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy.
TamsulosinLidocaine, a CYP3A4/2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4/2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Lidocaine is initiated, discontinued, or dose changed.
TelithromycinTelithromycin may reduce clearance of Lidocaine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Lidocaine if Telithromycin is initiated, discontinued or dose changed.
TerbinafineTerbinafine may reduce the metabolism and clearance of Lidocaine. Consider alternate therapy or monitor for therapeutic/adverse effects of Lidocaine if Terbinafine is initiated, discontinued or dose changed.
ThiothixeneThe strong CYP1A2 inhibitor, Lidocaine, may decrease the metabolism and clearance of Thiothixene, a CYP1A2 substrate. Consider alternate therapy or monitor for changes in Thiothixene therapeutic and adverse effects if Lidocaine is initiated, discontinued or dose changed.
TimololThe beta-blocker, timolol, may increase the effect and toxicity of lidocaine.
TizanidineLidocaine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
TolterodineLidocaine may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.
TramadolLidocaine may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. Lidocaine may decrease the effect of Tramadol by decreasing active metabolite production.
TrazodoneThe CYP3A4 inhibitor, Lidocaine, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Lidocaine is initiated, discontinued or dose changed.
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of lidocaine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of lidocaine if voriconazole is initiated, discontinued or dose changed.
Food InteractionsNot Available

Targets

1. Sodium channel protein type 10 subunit alpha

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Sodium channel protein type 10 subunit alpha Q9Y5Y9 Details

References:

  1. Ekberg J, Jayamanne A, Vaughan CW, Aslan S, Thomas L, Mould J, Drinkwater R, Baker MD, Abrahamsen B, Wood JN, Adams DJ, Christie MJ, Lewis RJ: 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. 2006 Nov 7;103(45):17030-5. Epub 2006 Oct 31. Pubmed
  2. Muroi Y, Chanda B: Local anesthetics disrupt energetic coupling between the voltage-sensing segments of a sodium channel. J Gen Physiol. 2009 Jan;133(1):1-15. Epub 2008 Dec 15. Pubmed
  3. Karoly R, Lenkey N, Juhasz AO, Vizi ES, Mike A: Fast- or slow-inactivated state preference of Na+ channel inhibitors: a simulation and experimental study. PLoS Comput Biol. 2010 Jun 17;6(6):e1000818. Pubmed

2. Sodium channel protein type 9 subunit alpha

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Sodium channel protein type 9 subunit alpha Q15858 Details

References:

  1. Sheets PL, Jackson JO 2nd, Waxman SG, Dib-Hajj SD, Cummins TR: A Nav1.7 channel mutation associated with hereditary erythromelalgia contributes to neuronal hyperexcitability and displays reduced lidocaine sensitivity. J Physiol. 2007 Jun 15;581(Pt 3):1019-31. Epub 2007 Apr 12. Pubmed
  2. Muroi Y, Chanda B: Local anesthetics disrupt energetic coupling between the voltage-sensing segments of a sodium channel. J Gen Physiol. 2009 Jan;133(1):1-15. Epub 2008 Dec 15. Pubmed
  3. Karoly R, Lenkey N, Juhasz AO, Vizi ES, Mike A: Fast- or slow-inactivated state preference of Na+ channel inhibitors: a simulation and experimental study. PLoS Comput Biol. 2010 Jun 17;6(6):e1000818. Pubmed

3. Sodium channel protein type 5 subunit alpha

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Sodium channel protein type 5 subunit alpha Q14524 Details

References:

  1. Itoh H, Tsuji K, Sakaguchi T, Nagaoka I, Oka Y, Nakazawa Y, Yao T, Jo H, Ashihara T, Ito M, Horie M, Imoto K: A paradoxical effect of lidocaine for the N406S mutation of SCN5A associated with Brugada syndrome. Int J Cardiol. 2007 Oct 18;121(3):239-48. Epub 2007 Apr 18. Pubmed
  2. Fedida D, Orth PM, Hesketh JC, Ezrin AM: The role of late I and antiarrhythmic drugs in EAD formation and termination in Purkinje fibers. J Cardiovasc Electrophysiol. 2006 May;17 Suppl 1:S71-S78. Pubmed
  3. Wallace CH, Baczko I, Jones L, Fercho M, Light PE: Inhibition of cardiac voltage-gated sodium channels by grape polyphenols. Br J Pharmacol. 2006 Nov;149(6):657-65. Epub 2006 Oct 3. Pubmed
  4. Cerne A, Bergh C, Borg K, Ek I, Gejervall AL, Hillensjo T, Olofsson JI, Stener-Victorin E, Wood M, Westlander G: Pre-ovarian block versus paracervical block for oocyte retrieval. Hum Reprod. 2006 Nov;21(11):2916-21. Epub 2006 Jul 13. Pubmed
  5. Muroi Y, Chanda B: Local anesthetics disrupt energetic coupling between the voltage-sensing segments of a sodium channel. J Gen Physiol. 2009 Jan;133(1):1-15. Epub 2008 Dec 15. Pubmed
  6. Karoly R, Lenkey N, Juhasz AO, Vizi ES, Mike A: Fast- or slow-inactivated state preference of Na+ channel inhibitors: a simulation and experimental study. PLoS Comput Biol. 2010 Jun 17;6(6):e1000818. Pubmed

4. Epidermal growth factor receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Epidermal growth factor receptor P00533 Details

References:

  1. Sakaguchi M, Kuroda Y, Hirose M: The antiproliferative effect of lidocaine on human tongue cancer cells with inhibition of the activity of epidermal growth factor receptor. Anesth Analg. 2006 Apr;102(4):1103-7. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  3. Wang JS, Backman JT, Taavitsainen P, Neuvonen PJ, Kivisto KT: Involvement of CYP1A2 and CYP3A4 in lidocaine N-deethylation and 3-hydroxylation in humans. Drug Metab Dispos. 2000 Aug;28(8):959-65. Pubmed

2. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

3. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

4. Cytochrome P450 3A7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A7 P24462 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

5. Cytochrome P450 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 1A2 P05177 Details

References:

  1. Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  3. Wang JS, Backman JT, Taavitsainen P, Neuvonen PJ, Kivisto KT: Involvement of CYP1A2 and CYP3A4 in lidocaine N-deethylation and 3-hydroxylation in humans. Drug Metab Dispos. 2000 Aug;28(8):959-65. Pubmed
  4. Lexicomp

6. Cytochrome P450 2C9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

7. Cytochrome P450 2C8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

8. Cytochrome P450 2C18

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C18 P33260 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

9. Cytochrome P450 2A6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2A6 P11509 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

10. Cytochrome P450 2B6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2B6 P20813 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

Transporters

1. Solute carrier family 22 member 5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 5 O76082 Details

References:

  1. Ohashi R, Tamai I, Nezu Ji J, Nikaido H, Hashimoto N, Oku A, Sai Y, Shimane M, Tsuji A: Molecular and physiological evidence for multifunctionality of carnitine/organic cation transporter OCTN2. Mol Pharmacol. 2001 Feb;59(2):358-66. Pubmed

2. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Wang E, Lew K, Barecki M, Casciano CN, Clement RP, Johnson WW: Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4. Chem Res Toxicol. 2001 Dec;14(12):1596-603. Pubmed
  2. Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on October 08, 2013 14:24