| 항목 |
내용 |
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| 화학구조 및 물성 |
[Lidocaine]
[Lidocaine]
CAS number/137-58-6
ATC code/N01BB02 C01BB01 D04AB01 S02DA01 C05AD01
PubChem/3676
DrugBank/APRD00479
Formula/C14H22N2O
Mol. mass/234.34 g/mol
Bioavailability/35% (oral)
3% (topical)
Metabolism/Hepatic, 90% CYP1A2-mediated
Excretion/renal
Pregnancy cat./
A(AU)
Legal status/
Prescription Only (S4)(AU)
Routes/IV, subcutaneous, topical
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| 독성정보 |
Lidocaine에 대한 독성정보 : 정보보기
출처: 국립독성과학원 독성물질정보DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do |
| Mechanism of Action |
Lidocaine에 대한 Mechanism_Of_Action 정보
Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action.
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| Pharmacology |
Lidocaine에 대한 Pharmacology 정보
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.
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| Metabolism |
Lidocaine에 대한 Metabolism 정보
# Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2D6 (CYP2D6)
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| Protein Binding |
Lidocaine에 대한 단백결합 정보
60-80%
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| Half-life |
Lidocaine에 대한 반감기 정보
109 minutes
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| Absorption |
Lidocaine에 대한 Absorption 정보
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.
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| Pharmacokinetics |
Lidocaine의 약물동력학자료
- 효과발현시간 (1회 bolus 용량으로서) : 45-90초
- 작용지속시간 : 10-25분
- 분포 (Vd) : 많은 요인에 따라 변화되며, 울혈성 심부전과 간질환에서는 분포용적이 감소됨
- 단백결합 : 60-80%, α1-acid glycoprotein과 결합
- 대사 : 간에서 90% 대사
- 활성형 대사체인 monoethylglycinexylidide(MEGX)와 glycinexylidide(GX)가 축적되어 중추신경계 독성을 유발할 수 있다.
- 반감기 (biphasic) : 울혈성 심부전, 간질환, 쇼크, 중증의 신질환에서 증가
- 초기 : 7-30분
- 말기 : 영아, 미숙아 : 3.2시간, 성인 : 1.5-2시간
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| Biotransformation |
Lidocaine에 대한 Biotransformation 정보
Primarily hepatic.
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| Toxicity |
Lidocaine에 대한 Toxicity 정보
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.
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| Drug Interactions |
Lidocaine에 대한 Drug_Interactions 정보
Not Available
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CYP450
Drug Interaction |
[CYP450 Table직접조회]
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| Food Interaction |
Lidocaine에 대한 Food Interaction 정보
Not Available
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| Drug Target |
[Drug Target]
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| Description |
Lidocaine에 대한 Description 정보
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]
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| Dosage Form |
Lidocaine에 대한 Dosage_Form 정보
Aerosol TopicalAerosol, metered TopicalCream TopicalGel TopicalJelly TopicalJelly UrethralLiquid BuccalLiquid DentalLiquid InfiltrationLiquid IntravenousLiquid OralLiquid TopicalLotion TopicalOintment TopicalSolution InfiltrationSolution IntramuscularSolution IntravenousSolution OralSolution TopicalSpray TopicalSwab Topical
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| Drug Category |
Lidocaine에 대한 Drug_Category 정보
AnestheticsAnesthetics, LocalAnti-Arrhythmia AgentsAntiarrhythmic Agents
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| Smiles String Canonical |
Lidocaine에 대한 Smiles_String_canonical 정보
CCN(CC)CC(=O)NC1=C(C)C=CC=C1C
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| Smiles String Isomeric |
Lidocaine에 대한 Smiles_String_isomeric 정보
CCN(CC)CC(=O)NC1=C(C)C=CC=C1C
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| InChI Identifier |
Lidocaine에 대한 InChI_Identifier 정보
InChI=1/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17)/f/h15H
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| Chemical IUPAC Name |
Lidocaine에 대한 Chemical_IUPAC_Name 정보
2-diethylamino-N-(2,6-dimethylphenyl)acetamide
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| Drug-Induced Toxicity Related Proteins |
DOCA 의 Drug-Induced Toxicity Related Protein정보
Replated Protein:Aquaporin-2
Drug:DOCA
Toxicity:hypertension.
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LIDOCAINE 의 Drug-Induced Toxicity Related Protein정보
Replated Protein:glucose-regulated protein
Drug:lidocaine
Toxicity:intestinal disorder.
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Replated Protein:Alkaline phosphatase
Drug:lidocaine
Toxicity:lidocaine induced hepatitis.
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Replated Protein:C-reactive protein
Drug:lidocaine
Toxicity:fever.
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Replated Protein:C-reactive protein
Drug:lidocaine
Toxicity:lidocaine induced hepatitis.
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Replated Protein:Alpha-1-acid glycoprotein
Drug:lidocaine
Toxicity:lidocaine tolerance.
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Replated Protein:Gamma-glutamyltranspeptidase
Drug:lidocaine
Toxicity:fever.
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Replated Protein:Alkaline phosphatase
Drug:lidocaine
Toxicity:fever.
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Replated Protein:Gamma-glutamyltranspeptidase
Drug:lidocaine
Toxicity:lidocaine induced hepatitis.
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전문/일반
