LIDOCAINE POWDER

Lidocaine is a local anesthetic and antiarrhythmic drug. It is a derivative of cocaine, but it contains no hallucinogenic and addictive component of cocaine. Lidocaine hydrochloride is white crystalline powder, which is very slightly dissolved in water and has the same toxicity as procaine, but the local anesthesia effect is strong and lasting and it has good surface penetration. It can be injected or used as topical anesthesia. Lidocaine is a very good local anesthetic. It usually takes effect after 1-3 minutes, and the effect lasts for 1-3 hours. It is used to treat oral ulcer. As a heart rhythm disorder drug, it is not often used because some people are worried that it will have long-term adverse effects. A few people are allergic to lidocaine. It was used to treat arrhythmia in 1963. It is a drug for the prevention and treatment of acute myocardial infarction and various heart diseases complicated with rapid ventricular arrhythmia. It is the first option for ventricular premature beats, ventricular tachycardia and ventricular fibrillation in acute myocardial infarction

Lidocaine  Basic Info

Foreign name
Lidocaine

Alias
Xylocaine, lidocaine, lighocaine, ligocaine

Main indications
Acute myocardial infarction, surgery

Dosage form
Injections, capsules, etc.
Athletes shall use it with caution

Drug type
Local anesthesia and antiarrhythmic drugs

Chemical Formula
C14H22N2O

Molecular Mass
234.337

CAS No
137-58-6

EINECS No
205-302-8

Appearance
White crystalline powder

Melting Point
66-69 ℃

Boiling Point
372.7 ℃

Flash Point
179.2 ℃

Density
0.9944 g/cm³

Water Solubility
Almost insoluble

Security Description
S22；S26；S36

Hazard Symbol
R22

Hazard Description
Xn

Compound Introduction
Chinese Name: lidocaine
Chinese Alias:  2-Diethylamino-N-(2,6-dimethylphenyl)acetamide; 2-diethylamino-2′,6′-acetoxylidide.
English Name: lidocaine
English Alias: L-Caine; Leostesin; 2-Diethylamino-N-(2,6-dimethylphenyl)acetamide; Esracaine; 2-diethylamino-2′,6′-acetoxylidide
CAS No:137-58-6
Molecular Formula:C14H22N2O
Molecular Mass: 234.337
Precise Mass: 234.17300
PSA：32.34000
LogP：2.65670

Physicochemical Properties
Appearance and properties: white crystalline powder
Density: 0.9944 g/cm3
Melting point:66-69°C
Boiling point: 372.7ºC at 760mmHg
Flash point: 179.2ºC

Lidocaine
Stability: stable, incompatible with strong oxidants
Storage conditions: it shall be stored in a cool and dry place, and the container shall be closed when not used.
Steam pressure:4.28E-05mmHg at 25°C

Security Information
Packing grade: III
Hazard category:6.1(b)
Customs Code: 2924299090
Dangerous goods transportation code: 3249
WGK Germany：3
WGK Germany：3
Hazard category code: R22
Safety instructions: S22-S26-S36
RTECS No.: AN7525000
Dangerous goods signs: Xn
Specifications:1. aerosol: 25g (containing 1.75g lidocaine); 2. injection: each 0.2g (10ml), 0.4g (20ml)

Purpose
The drug is an amide local anesthetic. It is widely used in topical anesthesia, infiltration anesthesia, conduction anesthesia and epidural anesthesia.

Clinical Application
It is applicable for acute ventricular arrhythmias caused by acute myocardial infarction, surgery, digitalis poisoning and cardiac catheters, including ventricular premature beats, ventricular tachycardia and ventricular fibrillation. Secondly, it is also used for patients with status epilepticus who are ineffective with other anticonvulsants and local or intraspinal anesthesia. It can also relieve tinnitus.

Usage and Dosage

External Administration
Dosage form, usage and dosage of external administration:
1. Ointment 5% can be applied to the dried mucosal surface in the mouth; 2.5% ointment is used externally to treat pruritus.

2. Gelling agent 2% is commonly applied to the outer wall of esophageal, pharyngeal, tracheal or urethral catheters in adults; when vaginal examination is performed for women, they can apply 5 ~ 7ml cotton swab to the local area; the dosage can be 400mg during urethral dilatation or cystoscopy. The 24-hour prescription is limited to 600mg.

3. Gargle 2% is used for oral diseases, adults use 15ml each time, spit it out after gargling, once every 3 hours; it is used for sore throat and it can be swallowed when necessary. The prescription is limited to 8 times in 24 hours, i.e. 2.4g, which can be reduced for children.
4, topical solution 4% is usually directly applied or sprayed on the throat or oral mucosa surface before gastroscopy, and even stuffed in the nasal cavity, the prescription may not exceed 3.0mg/kg each time in 24 hours. Children shall use it carefully.
5, aerosol or spray 2 – 4%, can be used in endoscopy, 10-30mL each time, prescription limit 3.0mg/kg.
Block anesthesia, 1 ~ 2% solution, no more than 0.4g at a time; topical anaesthesia, 1-2% solution, sprayed or dipped in medicine, not more than 0.25g at a time. Infiltration anesthesia, 1 ~ 2% solution, no more than 0.4g per hour; for the treatment of arrhythmia, intravenous injection of 1 ~ 3mg/kg at a time. If it is ineffective, it shall be injected again with the same amount after 10 ~ 15 minutes. Meanwhile, 100mg shall be added to 100 ~ 200ml of 5 ~ 10% glucose solution for intravenous drip. The total amount in one treatment is 4 ~ 6mg/kg.

Expert Comments
Lidocaine is a widely used medium effect amide local anesthetic. Because its fat solubility and protein binding rate are higher than those of procaine and its ability to penetrate cells is strong, lidocaine takes effect fast, has long action time and its action intensity is 4 times that of procaine. The effective rate of lidocaine on tachycardia caused by various causes is more than 80%, and it is safe. Therefore, lidocaine can be the first option for acute ventricular arrhythmia caused by various causes.

Preparation Method
For the synthesis of α-chloro-2′,6′-dimethylacetanilide, add lml 2′,6′-dimethylacetanilide and 0.4 ml acetic acid into a dry conical flask, add 0.6ml chloroacetyl chloride [1] drop by drop, and shake the mixture in the reaction flask constantly. Heat the mixture to 45℃. Add 20ml 5% sodium acetate solution. Cool the reactant below 10 ℃ and filter it. Wash the precipitate with water for several times to remove the acetic acid in it until the filtrate is neutral, collect the precipitate and dry it in an oven at 80-125 ℃ for 20min. The product is about 1g.

Synthesis of Lidocaine
Add α-chloro-2′,6′-dimethylacetanilide to a dry round bottom flask, and after dissolving it with lOmI toluene, add 2ml diethylamine. After heating and reflux for about 1h, the reaction process can be monitored by thin-layer chromatography until the raw material point almost disappears. Cool the mixture in an ice water to 5 ℃ and remove crystal by filtration. Place the cold filtrate in a separatory funnel and extract the filtrate twice with 3mol/L hydrochloric acid, use 6ml each time. Cool the acidic aqueous solution of lidocaine to 10 ℃, stir and slowly add 6mol/L sodium hydroxide solution until precipitation is formed, then add 2ml 6mol/L sodium hydroxide solution and cool the mixed solution to 20 ℃. The mixture is extracted twice with 5ml petroleum ether, the organic layer is washed with water and dried with anhydrous potassium carbonate. The oil is removed by distillation to obtain lidocaine crystal for about 0.3g.