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Lidocaine ¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Ãâó: ±¹¸³µ¶¼º°úÇпø µ¶¼º¹°ÁúÁ¤º¸DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do
Mechanism of Action
Lidocaine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action.Prilocaine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Prilocaine acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers.
Pharmacology
Lidocaine¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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.Prilocaine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Prilocaine, a hydantoin anticonvulsant, is used alone or with phenobarbital or other anticonvulsants to manage tonic-clonic seizures, psychomotor seizures, neuropathic pain syndromes including diabetic neuropathy, digitalis-induced cardiac arrhythmias, and cardiac arrhythmias associated with QT-interval prolongation.
Metabolism
Lidocaine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2D6 (CYP2D6)Prilocaine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
Protein Binding
Lidocaine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 60-80%Prilocaine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 98%
Half-life
Lidocaine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 109 minutesPrilocaine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ Not Available
Absorption
Lidocaine¿¡ ´ëÇÑ Absorption Á¤º¸ 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.Prilocaine¿¡ ´ëÇÑ Absorption Á¤º¸ Not Available
Pharmacokinetics
LidocaineÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
È¿°ú¹ßÇö½Ã°£ (1ȸ bolus ¿ë·®À¸·Î¼) : 45-90ÃÊ
ÀÛ¿ëÁö¼Ó½Ã°£ : 10-25ºÐ
ºÐÆ÷ (Vd) : ¸¹Àº ¿äÀο¡ µû¶ó º¯ÈµÇ¸ç, ¿ïÇ÷¼º ½ÉºÎÀü°ú °£Áúȯ¿¡¼´Â ºÐÆ÷¿ëÀûÀÌ °¨¼ÒµÊ
´Ü¹é°áÇÕ : 60-80%, ¥á1 -acid glycoprotein°ú °áÇÕ
´ë»ç : °£¿¡¼ 90% ´ë»ç
Ȱ¼ºÇü ´ë»çüÀÎ monoethylglycinexylidide(MEGX)¿Í glycinexylidide(GX)°¡ ÃàÀûµÇ¾î ÁßÃ߽Űæ°è µ¶¼ºÀ» À¯¹ßÇÒ ¼ö ÀÖ´Ù.
¹Ý°¨±â (biphasic) : ¿ïÇ÷¼º ½ÉºÎÀü, °£Áúȯ, ¼îÅ©, ÁßÁõÀÇ ½ÅÁúȯ¿¡¼ Áõ°¡
Ãʱâ : 7-30ºÐ
¸»±â : ¿µ¾Æ, ¹Ì¼÷¾Æ : 3.2½Ã°£, ¼ºÀÎ : 1.5-2½Ã°£
PrilocaineÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
ÀÛ¿ë¹ßÇö½Ã°£ : Lidocaine°ú À¯»ç (¾à 45-90ÃÊ)
ÀÛ¿ëÁö¼Ó½Ã°£ : ¾à 2½Ã°£
´ë»ç : °£´ë»ç
Biotransformation
Lidocaine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic.Prilocaine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Not Available
Toxicity
Lidocaine¿¡ ´ëÇÑ Toxicity Á¤º¸ 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.Prilocaine¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
Drug Interactions
Lidocaine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not AvailablePrilocaine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alendronate Increased risk of gastric toxicityMethotrexate The NSAID increases the effect and toxicity of methotrexateAnisindione The NSAID increases the anticoagulant effectDicumarol The NSAID increases the anticoagulant effectAcenocoumarol The NSAID increases the anticoagulant effectWarfarin The NSAID increases the anticoagulant effectCyclosporine Monitor for nephrotoxicity
CYP450 Drug Interaction
[CYP450 TableÁ÷Á¢Á¶È¸]
Food Interaction
Lidocaine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not AvailablePrilocaine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
Drug Target
[Drug Target]
Description
Lidocaine¿¡ ´ëÇÑ Description Á¤º¸ 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]Prilocaine¿¡ ´ëÇÑ Description Á¤º¸ A local anesthetic that is similar pharmacologically to lidocaine. Currently, it is used most often for infiltration anesthesia in dentistry. (From AMA Drug Evaluations Annual, 1992, p165)
Drug Category
Lidocaine¿¡ ´ëÇÑ Drug_Category Á¤º¸ AnestheticsAnesthetics, LocalAnti-Arrhythmia AgentsAntiarrhythmic AgentsPrilocaine¿¡ ´ëÇÑ Drug_Category Á¤º¸ AnestheticsAnesthetics, LocalLocal Anesthetics
Smiles String Canonical
Lidocaine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCN(CC)CC(=O)NC1=C(C)C=CC=C1CPrilocaine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCCNC(C)C(=O)NC1=CC=CC=C1C
Smiles String Isomeric
Lidocaine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CCN(CC)CC(=O)NC1=C(C)C=CC=C1CPrilocaine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CCCN[C@@H](C)C(=O)NC1=CC=CC=C1C
InChI Identifier
Lidocaine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ 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/h15HPrilocaine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C13H20N2O/c1-4-9-14-11(3)13(16)15-12-8-6-5-7-10(12)2/h5-8,11,14H,4,9H2,1-3H3,(H,15,16)/f/h15H
Chemical IUPAC Name
Lidocaine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-diethylamino-N-(2,6-dimethylphenyl)acetamidePrilocaine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ N-(2-methylphenyl)-2-propylaminopropanamide
Drug-Induced Toxicity Related Proteins
DOCA ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸Replated Protein :Aquaporin-2Drug :DOCA Toxicity :hypertension. [¹Ù·Î°¡±â] LIDOCAINE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸Replated Protein :glucose-regulated protein Drug :lidocaine Toxicity :intestinal disorder. [¹Ù·Î°¡±â] Replated Protein :Alkaline phosphataseDrug :lidocaine Toxicity :lidocaine induced hepatitis. [¹Ù·Î°¡±â] Replated Protein :C-reactive proteinDrug :lidocaine Toxicity :fever. [¹Ù·Î°¡±â] Replated Protein :C-reactive proteinDrug :lidocaine Toxicity :lidocaine induced hepatitis. [¹Ù·Î°¡±â] Replated Protein :Alpha-1-acid glycoproteinDrug :lidocaine Toxicity :lidocaine tolerance. [¹Ù·Î°¡±â] Replated Protein :Gamma-glutamyltranspeptidase Drug :lidocaine Toxicity :fever. [¹Ù·Î°¡±â] Replated Protein :Alkaline phosphataseDrug :lidocaine Toxicity :fever. [¹Ù·Î°¡±â] Replated Protein :Gamma-glutamyltranspeptidase Drug :lidocaine Toxicity :lidocaine induced hepatitis. [¹Ù·Î°¡±â]
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