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Lidocaine

description Chemical property Uses
Lidocaine
Lidocaine structure
CAS No.
137-58-6
Chemical Name:
Lidocaine
Synonyms
Xilina;Xllina;Xyline;Anbesol;L-Caine;Rucaina;Solcain;Xycaine;Xylotox;Cuivasil
CBNumber:
CB9128024
Molecular Formula:
C14H22N2O
Formula Weight:
234.34
MOL File:
137-58-6.mol

Lidocaine Properties

Melting point:
66-69°C
Boiling point:
bp4 180-182°; bp2 159-160°
Density 
0.9944 (rough estimate)
refractive index 
1.5110 (estimate)
Flash point:
9℃
storage temp. 
Store at RT
solubility 
ethanol: 4 mg/mL
form 
powder
pka
pKa 7.88(H2O)(Approximate)
color 
White to slightly yellow
Water Solubility 
practically insoluble
Merck 
14,5482
Stability:
Stable. Incompatible with strong oxidizing agents.
InChIKey
NNJVILVZKWQKPM-UHFFFAOYSA-N
CAS DataBase Reference
137-58-6(CAS DataBase Reference)
NIST Chemistry Reference
Lidocaine(137-58-6)
EPA Substance Registry System
Acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl)- (137-58-6)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  Xn,T,F
Risk Statements  22-39/23/24/25-23/24/25-11
Safety Statements  22-26-36-45-36/37-16-7
RIDADR  3249
WGK Germany  3
RTECS  AN7525000
HazardClass  6.1(b)
PackingGroup  III
HS Code  29242990
Hazardous Substances Data 137-58-6(Hazardous Substances Data)
Symbol(GHS):
Signal word: Danger
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H225 Highly Flammable liquid and vapour Flammable liquids Category 2 Danger P210,P233, P240, P241, P242, P243,P280, P303+ P361+P353, P370+P378,P403+P235, P501
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning P264, P270, P301+P312, P330, P501
H370 Causes damage to organs Specific target organ toxicity, single exposure Category 1 Danger P260, P264, P270, P307+P311, P321,P405, P501
Precautionary statements:
P210 Keep away from heat/sparks/open flames/hot surfaces. — No smoking.
P260 Do not breathe dust/fume/gas/mist/vapours/spray.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P311 Call a POISON CENTER or doctor/physician.
P301+P310 IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

Lidocaine price More Price(10)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich L1026 Lidocaine analytical standard 137-58-6 1vl $97.8 2018-11-20 Buy
Sigma-Aldrich 1366002 Lidocaine United States Pharmacopeia (USP) Reference Standard 137-58-6 250mg $348 2018-11-13 Buy
TCI Chemical L0156 Lidocaine >99.0%(HPLC)(T) 137-58-6 25g $38 2018-11-22 Buy
TCI Chemical L0156 Lidocaine >99.0%(HPLC)(T) 137-58-6 100g $114 2018-11-22 Buy
Cayman Chemical 20081 Lidocaine ≥98% 137-58-6 5mg $48 2018-11-19 Buy

Lidocaine Chemical Properties,Uses,Production

description

Lidocaine is a local anesthetic, also known as Xylocaine, in recent years it has been replaced procaine, widely used in local infiltration anesthesia in cosmetic plastic surgery, it can block the nerve excitability and conduction by inhibiting the sodium channels of nerve cell membrane. The fat soluble and protein binding rate of lidocaine is higher than procaine, its cell penetrating ability is strong, fast onset, long duration of action, the interaction strength is 4 times of procaine.
Lidocaine is used in infiltration anesthesia, epidural anesthesia, topical anesthesia (including thoracoscopy or abdominal surgery for mucosal anesthesia) and nerve block. In order to extend the time of anesthesia, reduce the poisoning of lidocaine and other side effects, can be added in the anesthetic epinephrine.
Lidocaine can also be used for the treatment of ventricular premature beat after acute myocardial infarction, ventricular tachycardia, digitalis poisoning, cardiac surgery and cardiac catheterization-induced ventricular arrhythmias, including ventricular premature beats, ventricular tachycardia and ventricular fibrillation. Lidocaine is also used for duration status of epilepsy which other anti-seizure drugs are not effective, as well as local or spinal anesthesia. But it is usually ineffective for supraventricular arrhythmias.

Chemical property

Lidocaine is white needle like crystals, and its melting point is 68-69℃; boiling point is 180-182℃ (0.53kPa), soluble in ethanol in 159-160℃ (0.267kPa), ether, benzene, chloroform and oil, do not dissolve in water. In common use radical hydrochloride, lidocaine hydrochloride (C14H22N2O • HCL, [73-78-9]) is a white crystalline powder. Melting point 127-129℃, and the monohydrate melting point is 77-78℃. Easily soluble in water, 0.5% aqueous solution pHO 4.0-5.5. Odorless, bitter taste.

Uses

1, This product is a local anesthetics of amide derivatives,and widely used in surface anesthesia, anesthesia, conduction anesthesia and epidural anesthesia. The LD50 of oral lidocaine hydrochloride to mice was 290 mg/kg.
2, Used as a local anesthetic.

Chemical Properties

solid

Uses

Lidocaine (Alphacaine)is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. [1] Histamine is responsible for many features of allergic reactions. Lidocaine (Alphacaine)is a second-generation antihistamine agent closely st

Uses

Antiarrhythmic Agents, Anesthetics;Anticonvulsant;antihypertensive

Definition

ChEBI: The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline.

Indications

Experimentally, lidocaine has been found to prevent VF arising during myocardial ischemia or infarction by preventing the fragmentation of organized largewavefronts into heterogeneous wavelets. Although lidocaine is of proven benefit in preventing VF early after clinical myocardial infarction, there is no evidence that it reduces mortality. To the contrary, lidocaine may increase mortality after myocardial infarction by approximately 40% to 60%.There are no controlled studies of lidocaine in secondary prevention of recurrence of VT or VF.
Lidocaine terminates organized monomorphic spontaneous VT or induced sustained VT in only approximately 20% of cases and is less effective than many other antiarrhythmic drugs. In a blinded, randomized study of intravenous lidocaine versus intravenous amiodarone in out-of-hospital VF resistant to defibrillation, lidocaine was associated with half the likelihood of survival to hospital admission compared with amiodarone.

brand name

Alphacaine (Carlisle); Lidoderm (Teikoku); Xylocaine (AstraZeneca).

General Description

Lidocaine was the first amino amide synthesized in 1948and has become the most widely used local anesthetic. Thetertiary amine has a pKa of 7.8 and it is formulated as thehydrochloride salt with a pH between 5.0 and 5.5. When lidocaineis formulated premixed with epinephrine the pH ofthe solution is adjusted to between 2.0 and 2.5 to prevent the hydrolysis of the epinephrine. Lidocaine is also availablewith or without preservatives. Some formulations of lidocainecontain a methylparaben preservative that maycause allergic reactions in PABA-sensitive individuals. Thelow pKa and medium water solubility provide intermediateduration of topical anesthesia of mucous membranes.Lidocaine can also be used for infiltration, peripheral nerveand plexus blockade, and epidural anesthesia.

Biological Activity

Anasthetic and class Ib antiarrhythmic agent.? Blocks voltage-gated sodium channels in the inactivated state.

Contact allergens

Lidocaine is an anesthetic of the amide group, like articaine or bupivacaine. Immediate-type IgE-dependent reactions are rare, and delayed-type contact dermatitis is exceptional. Cross-reactivity between the different amide anesthetics is not systematic.

Pharmacokinetics

Lidocaine is administered intravenously because extensive first-pass transformation by the liver prevents clinically effective plasma concentrations orally. The drug is dealkylated and eliminated almost entirely by the liver; therefore, dosage adjustments are necessary in the presence of hepatic disease or dysfunction. Lidocaine clearance exhibits the time dependency common to high-clearance agents. With a continuous infusion lasting more than 24 hours, there is a decrease in total lidocaine clearance and an increase in elimination half-life compared with a single dose. Lidocaine free plasma levels can vary in certain patients owing to binding with albumin and the acutephase reactant a1-acid glycoprotein. Levels of a1-acid glycoprotein are increased in patients after surgery or acute myocardial infarction, whereas levels of both a1-acid glycoprotein and serum albumin are decreased in chronic hepatic disease or heart failure and in those who are malnourished. This is an essential consideration because it is the unbound fraction that is pharmacologically active.

Clinical Use

The metabolism of lidocaine is typical of the amino amideanesthetics . The liver is responsiblefor most of the metabolism of lidocaine and any decreasein liver function will decrease metabolism. Lidocaineis primarily metabolized by de-ethylation of the tertiary nitrogento form monoethylglycinexylidide (MEGX). At lowlidocaine concentrations, CYP1A2 is the enzyme responsiblefor most MEGX formation. At high lidocaine concentrations,both CYP1A2 and CYP3A4 are responsible for the formationof MEGX.

Side effects

Central nervous system side effects such as drowsiness, slurred speech, paresthesias, agitation, and confusion predominate. These symptoms may progress to convulsions and respiratory arrest with higher plasma concentrations. A rare adverse effect is malignant hyperthermia.
Cimetidine significantly reduces the systemic clearance of lidocaine as well as the volume of distribution at steady state and the degree of plasma protein binding. Beta blockers also reduce lidocaine clearance owing to a decrease in hepatic blood flow. For the same reason, clearance is reduced in congestive heart failure or low-output states.
Amiodarone may also influence the pharmacokinetics of lidocaine. In patients receiving amiodarone, single doses of intravenous lidocaine do not influence the pharmacokinetics of either agent. When amiodarone treatment is started in patients who are already receiving lidocaine infusion, there is a decrease in lidocaine clearance, which can result in toxic lidocaine levels.

Safety Profile

Poison by ingestion, intravenous, intraperitoneal, and subcutaneous routes. Human systemic effects: blood pressure lowering, changes in heart rate, coma, convulsions, dlstorted perceptions, dyspnea, excitement, hallucinations, muscle contraction or spasticity, pulse rate, respiratory depression, toxic psychosis. An experimental teratogen. Other experimental reproductive effects. A local anesthetic. Mutation data reported. When heated to decomposition it emits toxic fumes of NOx.

Veterinary Drugs and Treatments

Besides its use as a local and topical anesthetic agent, lidocaine is used to treat ventricular arrhythmias, principally ventricular tachycardia and ventricular premature complexes in all species. Cats may be more sensitive to the drug and some clinicians feel that it should not be used in this species as an antiarrhythmic, but this remains controversial. In horses, lidocaine may be useful to prevent postoperative ileus and reperfusion injury.

Electrophysiologic Effects

Experimentally, lidocaine has been found to prevent VF arising during myocardial ischemia or infarction by preventing the fragmentation of organized largewavefronts into heterogeneous wavelets. Although lidocaine is of proven benefit in preventing VF early after clinical myocardial infarction, there is no evidence that it reduces mortality. To the contrary, lidocaine may increase mortality after myocardial infarction by approximately 40% to 60%.There are no controlled studies of lidocaine in secondary prevention of recurrence of VT or VF.
Lidocaine terminates organized monomorphic spontaneous VT or induced sustained VT in only approximately 20% of cases and is less effective than many other antiarrhythmic drugs. In a blinded, randomized study of intravenous lidocaine versus intravenous amiodarone in out-of-hospital VF resistant to defibrillation, lidocaine was associated with half the likelihood of survival to hospital admission compared with amiodarone.

Drug interactions

The concurrent administration of lidocaine with cimetidine but not ranitidine may cause an increase (15%) in the plasma concentration of lidocaine. This effect is a manifestation of cimetidine reducing the clearance and volume of distribution of lidocaine. The myocardial depressant effect of lidocaine is enhanced by phenytoin administration.

Precautions

Contraindications include hypersensitivity to local anesthetics of the amide type (a very rare occurrence), severe hepatic dysfunction, a history of grand mal seizures due to lidocaine, and age 70 or older. Lidocaine is contraindicated in the presence of second- or thirddegree heart block, since it may increase the degree of block and can abolish the idioventricular pacemaker responsible for maintaining the cardiac rhythm.

Lidocaine Preparation Products And Raw materials

Raw materials

Preparation Products


Lidocaine Suppliers

Global( 291)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Hebei Minshang Biotechnology Co., Ltd
+86-13230167943
cathy@hbminshang.com CHINA 278 58
Hebei Ruishun Trade Co.,LTD
17052563120
Mike@rsbiology.com CHINA 303 58
Cangzhou Wanyou New Material Technology Co.,Ltd
18631714998
sales@czwytech.com CHINA 348 58
Hefei TNJ Chemical Industry Co.,Ltd.
86-0551-65418684 18949823763
86-0551-65418684 info@tnjchem.com China 1815 55
Hebei Chisure Biotechnology Co., Ltd.
+8613292890173
0311 66567340 luna@speedgainpharma.com CHINA 1019 58
Hebei Guanlang Biotechnology Co., Ltd.
+86-0311-66562153 whatsapp +8615203118427
+86-0311-66562153 sales@crovellbio.com CHINA 406 50
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3203 55
Shanghai Bojing Chemical Co.,Ltd.
+86-21-37122233
+86-21-37127788 Candy@bj-chem.com CHINA 495 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32452 55
PI & PI BIOTECH INC.
020-81716320
020-81716319 Sales@pipitech.com CHINA 2543 55

View Lastest Price from Lidocaine manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-07-05 Lidocaine
137-58-6
US $10.00 / KG 1KG 99% 10 mt Hebei Guanlang Biotechnology Co., Ltd.
2018-12-15 Lidocaine
137-58-6
US $1.00 / kg 1kg 99% Customized career henan chemical co
2019-03-29 LIDOCAINE-D6
137-58-6
US $200.00 / kg 100g 99.9% 10TONS Hebei Jimi Trading Co., Ltd.

Lidocaine Spectrum


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