Drug/Small Molecule:
lidocaine

2D structure

Overview

Generic Names: Dilocaine; L-Caine
Trade Names: After Burn Double Strength Gel; After Burn Double Strength Spray; After Burn Gel; After Burn Spray; Alphacaine; Anestacon; Anestacon Jelly; Cappicaine; Dalcaine; DermaFlex; Duncaine; Emla; Esracaine; Gravocain; Isicaina; Lanabiotic; Leostesin; Lidoderm; Lidoject-1; Lidoject-2; Lignocaine; Maricaine; Norwood Sunburn Spray; Octocaine; Octocaine-100; Octocaine-50; Rocephin Kit; Solarcaine; Solarcaine aloe extra burn relief cream; Solcain; Xylocaine; Xylocaine 5% Spinal; Xylocaine Dental Ointment; Xylocaine Endotracheal; Xylocaine Test Dose; Xylocaine Viscous; Xylocaine-MPF; Xylocaine-MPF with Glucose; Xylocard; Zilactin-L; Zingo
Brand Mixtures: 0.4% Lidocaine Hydrochloride and 5% Dextrose Injection Usp (Dextrose + Lidocaine Hydrochloride); Alphacaine Hcl 2% W Epineph 1:100000 (Epinephrine + Lidocaine Hydrochloride); Alphacaine Hcl 2% W Epineph 1:50000 (Epinephrine + Lidocaine Hydrochloride); Arrow Central Venous Catheterization Kit (Lidocaine Hydrochloride + Povidone-Iodine); Arrow Multi-Lumen Central Venous Catheter Kit (Lidocaine Hydrochloride + Povidone-Iodine); Arrow Pneumothorax Kit (Lidocaine Hydrochloride + Povidone-Iodine); Arrow Two-Lumen Central Venous Cathetar Kit (Lidocaine Hydrochloride + Povidone-Iodine); Arrow Two-Lumen Jugular Catheterization Kit (Lidocaine Hydrochloride + Povidone-Iodine); Baciguent Plus Pain Reliever Ont (Bacitracin + Lidocaine); Bactine First Aid Spray Liq (Benzalkonium Chloride + Lidocaine Hydrochloride); Banana Boat Sooth-a-Caine W.Moist.Aloe V.Gel (Lidocaine + Menthol); Burncare Kit (Benzocaine + Lidocaine Hydrochloride); Caustinerf (Camphor + Chlorophenol + Lidocaine + Paraformaldehyde); Central Vein Catheterization Kit (Lidocaine Hydrochloride + Povidone-Iodine); Central Venous Catetherization Kit (Lidocaine Hydrochloride + Povidone-Iodine); Central Venous Catheter Expanded Kit (Lidocaine Hydrochloride + Povidone-Iodine); Central Venous Catheterization Kit (Lidocaine Hydrochloride + Povidone-Iodine); Continuous Epidural Anesthesia Tray (Lidocaine Hydrochloride + Sodium Chloride); Epidural Anesthesia Tray (Iodine (Povidone-Iodine) + Lidocaine Hydrochloride + Sodium Chloride); Expanded Multi-Med Kit (Lidocaine Hydrochloride + Povidone-Iodine); Family Medic First Aid Treatment - Liq (Benzalkonium Chloride + Lidocaine Hydrochloride); Genetic Amniocentesis Tray Kit (Iodine (Povidone-Iodine) + Lidocaine Hydrochloride); Hydrocath Central Venous Catheter Kit (Lidocaine Hydrochloride + Povidone-Iodine); Jamshidi Bone Marrow Biopsy Tray (Lidocaine Hydrochloride + Povidone-Iodine); Jamshidi Menghini Soft Tissue Biopsy Tray (Lidocaine Hydrochloride + Povidone-Iodine + Sodium Chloride); Lidocaine 0.2% in 5% Dextrose Inj (Dextrose + Lidocaine Hydrochloride); Lidocaine 2% Sterile Injectable Solution (Epinephrine Racemic + Lidocaine Hydrochloride); Lidocaine 2% with Epinephrine 1:100000 (Epinephrine + Lidocaine Hydrochloride); Lidocaine Hcl 2% (Epinephrine + Lidocaine Hydrochloride); Lidocaine Hcl 2% Epinephrine Inj (Epinephrine + Lidocaine Hydrochloride); Lidocaine Hcl 2% W Epineph 1:100000inj (Epinephrine + Lidocaine Hydrochloride); Lidocaine Hcl 2% W Epinephrine (Epinephrine + Lidocaine Hydrochloride); Lidocaine Hcl 2% W Epinephrine 1:100000 (Epinephrine + Lidocaine Hydrochloride); Lidocaine Hcl 2% W Epinephrine 1:50000 (Epinephrine + Lidocaine Hydrochloride); Lidocaine Inj 2% (Epinephrine Hcl + Lidocaine Hydrochloride); Lidocaine and Epinephrine Inj.Usp2% 1:100000 (Epinephrine + Lidocaine Hydrochloride); Lidosporin Cream (Gramicidin + Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)); Lidosporin Ear Drops (Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)); Lignospan Speciale Inj (Epinephrine + Lidocaine Hydrochloride); Medi-Quik First Aid Spray (Benzalkonium Chloride + Camphor + Lidocaine); Medi-Quik First Aid Spray (Benzalkonium Chloride + Lidocaine); Medi-Quik First-Aid Spray - Aer Top (Benzalkonium Chloride + Lidocaine); Multi-Lumen Central Venous Cathet Kit (Iodine (Povidone-Iodine) + Lidocaine Hydrochloride); Octocaine 100 Needleject Inj (Epinephrine + Lidocaine Hydrochloride); Otizol Hc Liq (Hydrocortisone (Hydrocortisone Acetate) + Lidocaine (Lidocaine Hydrochloride) + Neomycin (Neomycin Sulfate)); Ozonol Antibiotic Plus - Ointment (Bacitracin + Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)); Ozonol Antibiotic Plus Ont (Bacitracin + Lidocaine Hydrochloride + Polymyxin B Sulfate); Pacing Catheter Introducer Kit Acp-001px (Lidocaine Hydrochloride + Povidone-Iodine); Paracentesis Tray W Boasberg Catheter Set (Lidocaine Hydrochloride + Povidone-Iodine); Percutaneous Sheath Intro Kit Ak-09810-S (Iodine (Povidone-Iodine) + Lidocaine Hydrochloride (Povidone-Iodine)); Percutaneous Sheath Introducer Kit (Iodine (Povidone-Iodine) + Lidocaine Hydrochloride); Percutaneous Sheath Introducer Tray (Lidocaine Hydrochloride + Povidone-Iodine); Peritoneal Lavage Kit Inj (Iodine (Povidone-Iodine) + Lidocaine Hydrochloride); Pharmassist Soothenel Gel (Benzethonium Chloride + Lidocaine Hydrochloride); Pleura-Seal Thoracentesis Kit (Iodine (Povidone-Iodine) + Lidocaine Hydrochloride); Polyderm Antibiotic Ointment (Bacitracin + Lidocaine Hydrochloride + Polymyxin B Sulfate); Polysporin Antibiotic Burn Cream (Gramicidin + Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)); Polysporin Burn Formula Cream (Gramicidin + Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)); Racestyptine Cord (Aluminum Chloride + Lidocaine + Oxyquinoline Sulfate); Single-Shot Epidural Anesthesia Tray (Lidocaine Hydrochloride + Sodium Chloride); Spinal Anaesthesia Tray (Dextrose + Epinephrine + Iodine (Povidone-Iodine) + Lidocaine Hydrochloride + Tetracaine Hydrochloride); Spinal Anaesthesia Tray (Dextrose + Epinephrine + Lidocaine Hydrochloride + Povidone-Iodine + Tetracaine Hydrochloride); Spinal Anaesthesia Tray (Dextrose + Lidocaine Hydrochloride + Povidone-Iodine + Tetracaine (Tetracaine Hydrochloride)); Spinal Anaesthesia Tray (Iodine (Povidone-Iodine) + Lidocaine Hydrochloride); Spinal Anaesthesia Tray (Lidocaine Hydrochloride + Povidone-Iodine); Spinal Anesthesia Tray (Dextrose + Ephedrine Sulfate + Epinephrine + Lidocaine Hydrochloride + Tetracaine Hydrochloride); Spinal Anesthesia Tray (Dextrose + Ephedrine Sulfate + Lidocaine Hydrochloride + Tetracaine Hydrochloride); Spinal Anesthesia Tray (Dextrose + Epinephrine + Lidocaine Hydrochloride + Tetracaine Hydrochloride); Spinal Anesthesia Tray (Dextrose + Lidocaine Hydrochloride + Tetracaine Hydrochloride); Two-Lumen Central Venous Catheter Kit (Iodine (Povidone-Iodine) + Lidocaine Hydrochloride); Xylocaine - MPF 5% with Glucose 7.5% (Dextrose + Lidocaine Hydrochloride); Xylocaine 0.5% W Epinephrine 1:100000 (Epinephrine + Lidocaine Hydrochloride); Xylocaine 0.5% W Epinephrine 1:200000 (Epinephrine + Lidocaine Hydrochloride); Xylocaine MPF 1.5% with Epinephrine (Epinephrine + Lidocaine Hydrochloride); Xylocaine Oral Spray (Cetylpyridinium Chloride + Lidocaine Hydrochloride); Xylonor Spray (Cetrimonium Bromide + Lidocaine)
PharmGKB Accession Id: PA450226

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 (source: Drug Bank)

Indication

For 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. (source: Drug Bank)

ATC Therapeutic Categories

  • A01AD:Other agents for local oral treatment
  • C01BB:Antiarrhythmics, class Ib
  • C05AD:Local anesthetics
  • D04AB:Anesthetics for topical use
  • N01BB:Amides
  • R02AD:Anesthetics, local
  • S01HA:Local anesthetics
  • S02DA:Analgesics and anesthetics

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action. (source: Drug Bank)

Pharmacology

Lidocaine 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. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Primarily hepatic. (source: Drug Bank)

Protein Binding

60-80% (source: Drug Bank)

Absorption

Information 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. (source: Drug Bank)

Toxicity

The 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. (source: Drug Bank)

Isomeric SMILES Code:

CCN(CC)CC(=O)Nc1c(cccc1C)C (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP1A2
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  • PK
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Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
EGFR Uncurated Annotation (source: Drug Bank)
SCN9A Uncurated Annotation (source: Drug Bank)
SCN5A Uncurated Annotation (source: Drug Bank)
SCN10A Uncurated Annotation (source: Drug Bank)

PharmGKB Curated Pathways

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
amitriptyline
  • CO
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
imipramine
  • CO
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
non-selective monoamine reuptake inhibitors
  • CO
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Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Kidney Failure, Chronic
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  • PK
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Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00281
KEGG Drug ID:
D00358
PubChem Compound ID:
3676
PubChem Substance ID:
151886
IUPHAR Ligand ID:
2623

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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