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Lidocaine hydrochloride

Lidocaine hydrochloride structure

CAS No:
73-78-9
Formula:
C14H22N2O.ClH
Chemical Name:
Lidocaine hydrochloride
Synonyms:
Acetamide,2-(diethylamino)-N-(2,6-dimethylphenyl)-,hydrochloride (1:1);2′,6′-Acetoxylidide,2-(diethylamino)-,monohydrochloride;Acetamide,2-(diethylamino)-N-(2,6-dimethylphenyl)-,monohydrochloride;2-(Diethylamino)-2′,6′-acetoxylidide hydrochloride;2-(Diethylamino)-2′,6′-dimethylacetanilide hydrochloride;Lignocaine hydrochloride;Xylocaine hydrochloride;Lidocaine hydrochloride;Xycaine hydrochloride;Lidocain hydrochloride;Xylocard;Metaclopromide hydrochloride;Xilina hydrochloride;Lidothesin;Xylotox;Alphacaine;DioCaine;Lidocaine monohydrochloride;Irtopan;Odontalg;Lidesthesin;Xyloneural;Versicane;Lignavet;Sedagul;Xylocaine Astra;Luan;Proliferol;Rapidocaine;Xylanaest purum;Jetmonal;2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamide hydrochloride
Categories:
Active Pharmaceutical Ingredients > Anesthetic Agents

Description

Lidocaine Hcl salt, an amide local anesthetic, has anti-inflammatory properties in vitro and in vivo, possibly due to an attenuation of pro-inflammatory cytokines, intracellular adhesion molecule-1 (ICAM-1), and reduction of neutrophils influx.Target: Lidocaine is a common local anesthetic and antiarrhythmic drug. Lidocaine is used topically to relieve itching, burning and pain from skin inflammations, injected as a dental anesthetic or as a local anesthetic for minor surgery. Lidocaine,

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.

Lidocaine hydrochloride Basic Attributes

Molecular Weight：

270.8

Exact Mass：

270.149902

EC Number：

200-803-8

UNII：

EC2CNF7XFP

NSC Number：

757420

DSSTox ID：

DTXSID4058782

HScode：

2924299090

Characteristics

PSA：

32.3

XLogP3：

3.45870

Appearance：

White crystal powder

Melting Point：

77-78 °C

Boiling Point：

350.8ºC at 760 mmHg

Flash Point：

166ºC

Storage Conditions：

Refrigerator

Toxicity：

LD50 oral in mouse: 220mg/kg

Collision Cross Section：

155.4 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

3249

GHS Classification：

|Danger|H301 (44.62%): Toxic if swallowed [Danger Acute toxicity, oral]|P261, P264, P270, P271, P273, P280, P285, P301+P310, P301+P312, P302+P352, P304+P340, P304+P341, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P342+P311, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 65 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|H301 (81.97%): Toxic if swallowed [Danger Acute toxicity, oral]|P264, P270, P301+P310, P301+P312, P321, P330, P405, and P501|Aggregated GHS information provided by 183 companies from 14 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Prevention of pain during cataract surgery

MeSH：

Agents used for the treatment or prevention of cardiac arrhythmias. They may affect the polarization-repolarization phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibers. Anti-arrhythmia agents are often classed into four main groups according to their mechanism of action: sodium channel blockade, beta-adrenergic blockade, repolarization prolongation, or calcium channel blockade. (See all compounds classified as Anti-Arrhythmia Agents.)|A class of drugs that inhibit the activation of VOLTAGE-GATED SODIUM CHANNELS. (See all compounds classified as Voltage-Gated Sodium Channel Blockers.)|Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate. (See all compounds classified as Anesthetics, Local.)

MeSH Entry Terms：

2-(Diethylamino)-N-(2,6-Dimethylphenyl)Acetamide

Lidocaine hydrochloride Use and Manufacturing

Uses

Anesthetic (local); antiarrhythmic (class IB). Long-acting, membrane stabilizing agent against ventricular arrhythmia. Originally developed as a local anesthetic.

Manufacturing Info：

Acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl)-, hydrochloride (1:1): ACTIVE

Use Classification：

Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:270.80
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:2
Rotatable Bond Count:5
Exact Mass:270.1498911
Monoisotopic Mass:270.1498911
Topological Polar Surface Area:32.3
Heavy Atom Count:18
Complexity:228
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Lidocaine is used as a local anesthetic to block peripheral nerve impulses by inhibiting voltage-gated sodium channels. It has analgesic effects on mechanical noxious responses, reduces spinal nociceptive responses induced by peripheral pressure stimuli, and decreases the frequency of spontaneous excitatory postsynaptic currents without altering their amplitude. It does not affect spontaneous inhibitory postsynaptic currents and generates output currents in SG neurons.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

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Registered Holders

スペラネクサス株式会社

Japan
Active
CAMBREX KARLSKOGA AB

France
Active
PROFARMACO SRL

United States
Inactive

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