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    112  (ÃÖ¸éÁøÁ¤Á¦                                                      )
      
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    | Mechanism of Action | 
    
       Estazolam¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Benzodiazepines bind nonspecifically to benzodiazepine receptors, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. 
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    | Pharmacology | 
     
       Estazolam¿¡ ´ëÇÑ Pharmacology Á¤º¸ Estazolam, a triazolobenzodiazepine derivative, is an oral hypnotic agent with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than diazepam or nitrazepam. 
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    | Metabolism | 
    
       Estazolam¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4) 
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    | Protein Binding | 
    
       Estazolam¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 93% protein bound, independant of concentration. 
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    | Half-life | 
    
       Estazolam¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ The range of estimates for the mean elimination half-life of estazolam varies from 10 to 24 hours. 
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    | Absorption | 
    
       Estazolam¿¡ ´ëÇÑ Absorption Á¤º¸ Tablets have been found to be equivalent in absorption to an orally administered solution of estazolam. In healthy subjects who received up to three times the recommended dose, peak estazolam plasma concentrations occurred within two hours after dosing (range 0.5 to 6.0 hours) and were proportional to the administered dose, suggesting linear pharmacokinetics over the dosage range tested. 
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    | Biotransformation | 
    
       Estazolam¿¡ ´ëÇÑ Biotransformation Á¤º¸ Extensively metabolized in the liver. In vitro studies with human liver microsomes indicate that the biotransformation of estazolam to the major circulating metabolite 4-hydroxy-estazolam is mediated by cytochrome P450 3A (CYP3A). 
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    | Toxicity | 
    
       Estazolam¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include confusion, depressed breathing, drowsiness and eventually coma, lack of coordination, and slurred speech. 
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    | Drug Interactions | 
    
       Estazolam¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Cimetidine	Cimetidine increases the effect of the benzodiazepineClozapine	Increased risk of toxicityEthotoin	Possible increased levels of the hydantoin, decrease of benzodiazepineFluconazole	Fluconazole increases the effect of the benzodiazepineFosphenytoin	Possible increased levels of the hydantoin, decrease of benzodiazepineIndinavir	The protease inhibitor increases the effect of the benzodiazepineNelfinavir	The protease inhibitor increases the effect of the benzodiazepineRitonavir	The protease inhibitor increases the effect of the benzodiazepineSaquinavir	The protease inhibitor increases the effect of the benzodiazepineMephenytoin	Possible increased levels of the hydantoin, decrease of benzodiazepinePhenytoin	Possible increased levels of the hydantoin, decrease of benzodiazepineItraconazole	The imidazole increases the effect of the benzodiazepineKetoconazole	The imidazole increases the effect of the benzodiazepineVoriconazole	The imidazole increases the effect of the benzodiazepineKava	Kava increases the effect of the benzodiazepineOmeprazole	Omeprazole increases the effect of benzodiazepine 
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    CYP450  Drug Interaction | 
    
      [CYP450 TableÁ÷Á¢Á¶È¸] 
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    | Food Interaction | 
    
       Estazolam¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Avoid alcohol. 
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    | Drug Target | 
    
      
      [Drug Target]
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    | Description | 
    
       Estazolam¿¡ ´ëÇÑ Description Á¤º¸ A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than diazepam or nitrazepam. [PubChem] 
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    | Dosage Form | 
    
       Estazolam¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet	Oral 
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    | Drug Category | 
    
       Estazolam¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-anxiety AgentsAnticonvulsantsGABA Modulators 
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    | Smiles String Canonical | 
    
       Estazolam¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ ClC1=CC2=C(C=C1)N1C=NN=C1CN=C2C1=CC=CC=C1 
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    | Smiles String Isomeric | 
    
       Estazolam¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ ClC1=CC2=C(C=C1)N1C=NN=C1CN=C2C1=CC=CC=C1 
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    | InChI Identifier | 
    
       Estazolam¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C16H11ClN4/c17-12-6-7-14-13(8-12)16(11-4-2-1-3-5-11)18-9-15-20-19-10-21(14)15/h1-8,10H,9H2 
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    | Chemical IUPAC Name | 
    
       Estazolam¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 8-chloro-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine 
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  The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ¡Ã4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. ESTAZOLAM[GGT Increase][Composite Activity](Score)  I(Marginal)  0(Active)  0[Alkaline Phosphatase Increase](Activity Score)  I(Number of Rpts)  <4(Index value)  0[SGOT Increase](Activity Score)  I(Number of Rpts)  <4(Index value)  0.8[SGPT Increase](Activity Score)  I(Number of Rpts)  <4(Index value)  0.8[LDH Increase](Activity Score)  I(Number of Rpts)  <4(Index value)  0[GGT Increase](Activity Score)  I(Number of Rpts)  <4(Index value)  0.8
 
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