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8806498012806 |
8806498012820 |
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| Mechanism of Action |
Mepivacaine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Local anesthetics block the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers. Clinically, the order of loss of nerve function is as follows: pain, temperature, touch, proprioception, and skeletal muscle tone.
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| Pharmacology |
Mepivacaine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Mepivicaine is a local anesthetic of the amide type. Mepivicaine as a reasonably rapid onset and medium duration and is known by the proprietary names as Carbocaine and Polocaine. Mepivicaine is used in local infiltration and regional anesthesia. Systemic absorption of local anesthetics produces effects on the cardiovascular and central nervous systems. At blood concentrations achieved with normal therapeutic doses, changes in cardiac conduction, excitability, refractoriness, contractility, and peripheral vascular resistance are minimal.
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| Metabolism |
Mepivacaine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
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| Protein Binding |
Mepivacaine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Mepivacaine is approximately 75% bound to plasma proteins. Generally, the lower the plasma concentration of drug, the higher the percentage of drug bound to plasma.
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| Half-life |
Mepivacaine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ The half-life of mepivacaine in adults is 1.9 to 3.2 hours and in neonates 8.7 to 9 hours.
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| Absorption |
Mepivacaine¿¡ ´ëÇÑ Absorption Á¤º¸ Absorbed locally. The rate of systemic absorption of local anesthetics is dependent upon the total dose and concentration of drug administered, the route of administration, the vascularity of the administration site, and the presence or absence of epinephrine in the anesthetic solution.
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| Pharmacokinetics |
Mepivacaine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ë¹ßÇö½Ã°£ : °æ¸·¿Ü ¸¶Ãë : 7-15ºÐ À̳»
- ÀÛ¿ëÁö¼Ó½Ã°£ : 2-2.5 ½Ã°£. ħÀ±½Ã¿¡µµ ÀÛ¿ë¹ßÇö½Ã°£, Áö¼Ó½Ã°£Àº À¯»çÇÏ´Ù.
- ´Ü¹é°áÇÕ : 70-85%
- ´ë»ç : ÁÖ·Î °£¿¡¼ N-demethylation, hydroxylation, glucuronidationµÊ
- ¹Ý°¨±â : 1.9 ½Ã°£
- ¼Ò½Ç : ½Å¹è¼³ (95%°¡ ´ë»çü·Î)
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| Biotransformation |
Mepivacaine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Rapidly metabolized, with only a small percentage of the anesthetic (5 percent to 10 percent) being excreted unchanged in the urine. The liver is the principal site of metabolism, with over 50% of the administered dose being excreted into the bile as metabolites.
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| Toxicity |
Mepivacaine¿¡ ´ëÇÑ Toxicity Á¤º¸ The mean seizure dosage of mepivacaine in rhesus monkeys was found to be 18.8 mg/kg with mean arterial plasma concentration of 24.4 µg/mL. The intravenous and subcutaneous LD 50 in mice is 23 mg/kg to 35 mg/kg and 280 mg/kg respectively.
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| Drug Interactions |
Mepivacaine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Mepivacaine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
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| Drug Target |
[Drug Target]
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| Description |
Mepivacaine¿¡ ´ëÇÑ Description Á¤º¸ A local anesthetic that is chemically related to bupivacaine but pharmacologically related to lidocaine. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168)
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| Drug Category |
Mepivacaine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anesthetics, Local
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| Smiles String Canonical |
Mepivacaine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN1CCCCC1C(=O)NC1=C(C)C=CC=C1C
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| Smiles String Isomeric |
Mepivacaine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN1CCCC[C@@H]1C(=O)NC1=C(C)C=CC=C1C
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| InChI Identifier |
Mepivacaine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C15H22N2O/c1-11-7-6-8-12(2)14(11)16-15(18)13-9-4-5-10-17(13)3/h6-8,13H,4-5,9-10H2,1-3H3,(H,16,18)/f/h16H
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| Chemical IUPAC Name |
Mepivacaine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ N-(2,6-dimethylphenyl)-1-methylpiperidine-2-carboxamide
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