QuickView for Lidocaine (compound)

Summary
General Info

PubChem

PubChem Compound 11436229

Name:	Lidocaine
PubChem Compound ID:	11436229
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.
Molecular formula:	C₁₄H₂₂N₂O
Molecular weight:	233.338 g/mol

DrugBank

Identification

Name:	Lidocaine
Name (isomeric):	DB00281
Drug Type:	small molecule
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.
Synonyms:	L-Caine; Dilocaine
Brand:	Xylocaine-MPF with Glucose, Emla, Xylocaine Dental Ointment, Xylocaine, Solarcaine, Isicaina, Duncaine, Xylocaine-MPF, Xylocaine Endotracheal, Solcain, Rocephin Kit, Xylocard, Lignocaine, Lidoject-1, Lidoject-2, Solarcaine aloe extra burn relief cream, Xylocaine Viscous, Octocaine-50, Octocaine, Xylocaine Test Dose, Esracaine, Maricaine, After Burn Gel, Dalcaine, Leostesin, After Burn Spray, Lanabiotic, Alphacaine, Gravocain, Anestacon, After Burn Double Strength Spray, DermaFlex, Lidoderm, Anestacon Jelly, Octocaine-100, Xylocaine 5% Spinal, Norwood Sunburn Spray, Zingo, Cappicaine, Zilactin-L, After Burn Double Strength Gel
Brand name mixture:	Jamshidi Menghini Soft Tissue Biopsy Tray(Lidocaine Hydrochloride + Povidone-Iodine + Sodium Chloride), Caustinerf(Camphor + Chlorophenol + Lidocaine + Paraformaldehyde), Octocaine 100 Needleject Inj(Epinephrine + Lidocaine Hydrochloride), Polysporin Antibiotic Burn Cream(Gramicidin + Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)),... show more » Jamshidi Menghini Soft Tissue Biopsy Tray(Lidocaine Hydrochloride + Povidone-Iodine + Sodium Chloride), Caustinerf(Camphor + Chlorophenol + Lidocaine + Paraformaldehyde), Octocaine 100 Needleject Inj(Epinephrine + Lidocaine Hydrochloride), Polysporin Antibiotic Burn Cream(Gramicidin + Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)), Pharmassist Soothenel Gel(Benzethonium Chloride + Lidocaine Hydrochloride), Xylocaine - MPF 5% with Glucose 7.5%(Dextrose + Lidocaine Hydrochloride), Lidocaine and Epinephrine Inj.Usp2% 1:100000(Epinephrine + Lidocaine Hydrochloride), Peritoneal Lavage Kit Inj(Iodine (Povidone-Iodine) + Lidocaine Hydrochloride), Central Venous Catetherization Kit(Lidocaine Hydrochloride + Povidone-Iodine), Alphacaine Hcl 2% W Epineph 1:50000(Epinephrine + Lidocaine Hydrochloride), Arrow Central Venous Catheterization Kit(Lidocaine Hydrochloride + Povidone-Iodine), Bactine First Aid Spray Liq(Benzalkonium Chloride + Lidocaine Hydrochloride), Burncare Kit(Benzocaine + Lidocaine Hydrochloride), Percutaneous Sheath Intro Kit Ak-09810-S(Iodine (Povidone-Iodine) + Lidocaine Hydrochloride (Povidone-Iodine)), Lidocaine 2% Sterile Injectable Solution(Epinephrine Racemic + Lidocaine Hydrochloride), Family Medic First Aid Treatment - Liq(Benzalkonium Chloride + Lidocaine Hydrochloride), Ozonol Antibiotic Plus Ont(Bacitracin + Lidocaine Hydrochloride + Polymyxin B Sulfate), Multi-Lumen Central Venous Cathet Kit(Iodine (Povidone-Iodine) + Lidocaine Hydrochloride), Xylonor Spray(Cetrimonium Bromide + Lidocaine), Xylocaine MPF 1.5% with Epinephrine(Epinephrine + Lidocaine Hydrochloride), Continuous Epidural Anesthesia Tray(Lidocaine Hydrochloride + Sodium Chloride), Genetic Amniocentesis Tray Kit(Iodine (Povidone-Iodine) + Lidocaine Hydrochloride), Polysporin Burn Formula Cream(Gramicidin + Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)), Lidocaine Hcl 2% W Epinephrine 1:50000(Epinephrine + Lidocaine Hydrochloride), Lidosporin Cream(Gramicidin + Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)), Xylocaine 0.5% W Epinephrine 1:200000(Epinephrine + Lidocaine Hydrochloride), Banana Boat Sooth-a-Caine W.Moist.Aloe V.Gel(Lidocaine + Menthol), Alphacaine Hcl 2% W Epineph 1:100000(Epinephrine + Lidocaine Hydrochloride), Xylocaine 0.5% W Epinephrine 1:100000(Epinephrine + Lidocaine Hydrochloride), Hydrocath Central Venous Catheter Kit(Lidocaine Hydrochloride + Povidone-Iodine), Lidocaine Hcl 2% W Epinephrine 1:100000(Epinephrine + Lidocaine Hydrochloride), Xylocaine Oral Spray(Cetylpyridinium Chloride + Lidocaine Hydrochloride), Arrow Two-Lumen Jugular Catheterization Kit(Lidocaine Hydrochloride + Povidone-Iodine), Expanded Multi-Med Kit(Lidocaine Hydrochloride + Povidone-Iodine), Paracentesis Tray W Boasberg Catheter Set(Lidocaine Hydrochloride + Povidone-Iodine), Pleura-Seal Thoracentesis Kit(Iodine (Povidone-Iodine) + Lidocaine Hydrochloride), Ozonol Antibiotic Plus - Ointment(Bacitracin + Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)), Percutaneous Sheath Introducer Tray(Lidocaine Hydrochloride + Povidone-Iodine), Central Vein Catheterization Kit(Lidocaine Hydrochloride + Povidone-Iodine), Percutaneous Sheath Introducer Kit(Iodine (Povidone-Iodine) + Lidocaine Hydrochloride), Arrow Multi-Lumen Central Venous Catheter Kit(Lidocaine Hydrochloride + Povidone-Iodine), Lidocaine Hcl 2%(Epinephrine + Lidocaine Hydrochloride), Epidural Anesthesia Tray(Iodine (Povidone-Iodine) + Lidocaine Hydrochloride + Sodium Chloride), Pacing Catheter Introducer Kit Acp-001px(Lidocaine Hydrochloride + Povidone-Iodine), Central Venous Catheter Expanded Kit(Lidocaine Hydrochloride + Povidone-Iodine), Lidocaine Hcl 2% W Epineph 1:100000inj(Epinephrine + Lidocaine Hydrochloride), Jamshidi Bone Marrow Biopsy Tray(Lidocaine Hydrochloride + Povidone-Iodine), Baciguent Plus Pain Reliever Ont(Bacitracin + Lidocaine), Two-Lumen Central Venous Catheter Kit(Iodine (Povidone-Iodine) + Lidocaine Hydrochloride), 0.4% Lidocaine Hydrochloride and 5% Dextrose Injection Usp(Dextrose + Lidocaine Hydrochloride), Racestyptine Cord(Aluminum Chloride + Lidocaine + Oxyquinoline Sulfate), Otizol Hc Liq(Hydrocortisone (Hydrocortisone Acetate) + Lidocaine (Lidocaine Hydrochloride) + Neomycin (Neomycin Sulfate)), Polyderm Antibiotic Ointment(Bacitracin + Lidocaine Hydrochloride + Polymyxin B Sulfate), Lidocaine Hcl 2% Epinephrine Inj(Epinephrine + Lidocaine Hydrochloride), Arrow Pneumothorax Kit(Lidocaine Hydrochloride + Povidone-Iodine), Lidosporin Ear Drops(Lidocaine Hydrochloride + Polymyxin B (Polymyxin B Sulfate)), Arrow Two-Lumen Central Venous Cathetar Kit(Lidocaine Hydrochloride + Povidone-Iodine), Lidocaine 0.2% in 5% Dextrose Inj(Dextrose + Lidocaine Hydrochloride), Lidocaine Hcl 2% W Epinephrine(Epinephrine + Lidocaine Hydrochloride), Lidocaine Inj 2%(Epinephrine Hcl + Lidocaine Hydrochloride), Lidocaine 2% with Epinephrine 1:100000(Epinephrine + Lidocaine Hydrochloride), Central Venous Catheterization Kit(Lidocaine Hydrochloride + Povidone-Iodine) show less «
Category:	Antiarrhythmic Agents, Anesthetics, Anti-Arrhythmia Agents, Anesthetics, Local
CAS number:	137-58-6

Pharmacology

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.
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 antiarrhy... show more » 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. show less «
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. 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. ... show more » Lidocaine 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. show less «
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.
Protein binding:	60-80%
Biotransformation:	Primarily hepatic.
Route of elimination:	Lidocaine and its metabolites are excreted by the kidneys.
Half Life:	109 minutes
Clearance:	0.64 +/- 0.18 L/min
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.
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

Cimetidine	Increases the effect and toxicity of lidocaine
Bisoprolol	The beta-blocker, bisoprolol, may increase the effect and toxicity of lidocaine.
Tizanidine	Lidocaine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Tramadol	Lidocaine may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. Lidocaine may decrease the effect of Tramadol by decreasing active metabolite production.
Tamoxifen	Lidocaine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy.

Cimetidine	Increases the effect and toxicity of lidocaine
Bisoprolol	The beta-blocker, bisoprolol, may increase the effect and toxicity of lidocaine.
Tizanidine	Lidocaine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Tramadol	Lidocaine may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. Lidocaine may decrease the effect of Tramadol by decreasing active metabolite production.
Tamoxifen	Lidocaine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy.
Metoprolol	The beta-blocker, metoprolol, may increase the effect and toxicity of lidocaine
Darunavir	Possible increase in lidocaine levels
Trazodone	The 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.
Voriconazole	Voriconazole, 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.
Tacrine	The 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.
Carvedilol	The beta-blocker, carvedilol, may increase the effect and toxicity of lidocaine.
Thiothixene	The 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.
Atenolol	The beta-blocker, atenolol, may increase the effect and toxicity of lidocaine.
Atazanavir	Increased risk of cardiotoxicity and arrhythmias
Nadolol	The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
Propranolol	The beta-blocker, propranolol, may increase the effect and toxicity of lidocaine.
Oxprenolol	The beta-blocker increases the effect and toxicity of lidocaine
Quinupristin	This combination presents an increased risk of toxicity
Acebutolol	The beta-blocker, acebutolol, may increase the effect and toxicity of lidocaine.
Telithromycin	Telithromycin 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.
Timolol	The beta-blocker, timolol, may increase the effect and toxicity of lidocaine.
Pindolol	The beta-blocker increases the effect and toxicity of lidocaine
Esmolol	The beta-blocker, esmolol, may increase the effect and toxicity of lidocaine.
Tolterodine	Lidocaine may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.
Labetalol	The beta-blocker, labetalol, may increase the effect and toxicity of lidocaine.
Tamsulosin	Lidocaine, 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.
Terbinafine	Terbinafine 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.