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5. ¸¶Ãë½Ã Ç÷¾Ð°ÇÏ  
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    | Mechanism of Action | 
    
       Labetalol¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Labetalol has two asymmetric centers and therefore, exists as a molecular complex of two diastereoisomeric pairs. Dilevalol, the R,R' stereoisomer, makes up 25% of racemic labetalol. Labetalol HCl combines both selective, competitive, alpha-1-adrenergic blocking and nonselective, competitive, beta-adrenergic blocking activity in a single substance. In man, the ratios of alpha- to beta- blockade have been estimated to be approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively. Beta-2-agonist activity has been demonstrated in animals with minimal beta-1-agonist (ISA) activity detected. In animals, at doses greater than those required for alpha- or beta- adrenergic blockade, a membrane stabilizing effect has been demonstrated. 
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    | Pharmacology | 
     
       Labetalol¿¡ ´ëÇÑ Pharmacology Á¤º¸ Labetalol is an alpha-1 and beta adrenergic blocker used to treat high blood pressure. It works by blocking these adrenergic receptors, which slows sinus heart rate, decreases peripheral vascular resistance, and decreases cardiac output. 
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    | Protein Binding | 
    
       Labetalol¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 50% 
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       Labetalol¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 6-8 hours 
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    | Absorption | 
    
       Labetalol¿¡ ´ëÇÑ Absorption Á¤º¸ Completely absorbed (100%) from the gastrointestinal tract with peak plasma levels occurring 1 to 2 hours after oral administration. The absolute bioavailability of labetalol is increased when administered with food. 
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    | Pharmacokinetics | 
    
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    | Biotransformation | 
    
       Labetalol¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic, undergoes significant first pass metabolism 
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    | Toxicity | 
    
       Labetalol¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50 = 66 mg/kg (Rat, IV). Side effects or adverse reactions include dizziness when standing up, very low blood pressure, severely slow heartbeat, weakness, diminished sexual function, fatigue 
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    | Drug Interactions | 
    
       Labetalol¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Acetohexamide	The beta-blocker decreases the symptoms of hypoglycemiaChlorpropamide	The beta-blocker decreases the symptoms of hypoglycemiaDisopyramide	The beta-blocker increases toxicity of disopyramideGliclazide	The beta-blocker decreases the symptoms of hypoglycemiaGlipizide	The beta-blocker decreases the symptoms of hypoglycemiaGlisoxepide	The beta-blocker decreases the symptoms of hypoglycemiaGlibenclamide	The beta-blocker decreases the symptoms of hypoglycemiaGlycodiazine	The beta-blocker decreases the symptoms of hypoglycemiaInsulin	The beta-blocker decreases the symptoms of hypoglycemiaLidocaine	The beta-blocker increases the effect and toxicity of lidocaineRepaglinide	The beta-blocker decreases the symptoms of hypoglycemiaTolazamide	The beta-blocker decreases the symptoms of hypoglycemiaTolbutamide	The beta-blocker decreases the symptoms of hypoglycemiaCimetidine	Cimetidine increases the effect of the beta-blockerClonidine	Increased hypertension when clonidine stoppedDihydroergotamine	Ischemia with risk of gangreneDihydroergotoxine	Ischemia with risk of gangreneErgonovine	Ischemia with risk of gangreneErgotamine	Ischemia with risk of gangreneMethysergide	Ischemia with risk of gangreneEnflurane	Monitor arterial pressure closelyHalothane	Monitor arterial pressure closelyIsoflurane	Monitor arterial pressure closelyEpinephrine	Hypertension, then bradycardiaFenoterol	AntagonismFormoterol	AntagonismOrciprenaline	AntagonismIsoproterenol	AntagonismPirbuterol	AntagonismTerbutaline	AntagonismSalmeterol	AntagonismSalbutamol	AntagonismProcaterol	AntagonismVerapamil	Increased effect of both drugsIbuprofen	Risk of inhibition of renal prostaglandinsIndomethacin	Risk of inhibition of renal prostaglandinsPiroxicam	Risk of inhibition of renal prostaglandinsPrazosin	Risk of hypotension at the beginning of therapy 
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    CYP450  Drug Interaction | 
    
      [CYP450 TableÁ÷Á¢Á¶È¸] 
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    | Food Interaction | 
    
       Labetalol¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals. 
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    | Drug Target | 
    
      
      [Drug Target]
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    | Description | 
    
       Labetalol¿¡ ´ëÇÑ Description Á¤º¸ Blocker of both alpha- and beta-adrenergic receptors that is used as an antihypertensive. [PubChem] 
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    | Dosage Form | 
    
       Labetalol¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid	IntravenousTablet	Oral 
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    | Drug Category | 
    
       Labetalol¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic alpha-AntagonistsAdrenergic beta-AntagonistsAntihypertensive AgentsSympatholytics 
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    | Smiles String Canonical | 
    
       Labetalol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(CCC1=CC=CC=C1)NCC(O)C1=CC(C(N)=O)=C(O)C=C1 
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    | Smiles String Isomeric | 
    
       Labetalol¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ C[C@H](CCC1=CC=CC=C1)NC[C@@H](O)C1=CC(C(N)=O)=C(O)C=C1 
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    | InChI Identifier | 
    
       Labetalol¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C19H24N2O3/c1-13(7-8-14-5-3-2-4-6-14)21-12-18(23)15-9-10-17(22)16(11-15)19(20)24/h2-6,9-11,13,18,21-23H,7-8,12H2,1H3,(H2,20,24)/f/h20H2 
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    | Chemical IUPAC Name | 
    
       Labetalol¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-hydroxy-5-[1-hydroxy-2-(4-phenylbutan-2-ylamino)ethyl]benzamide 
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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. LABETALOL[GGT Increase][Composite Activity](Score)  I(Marginal)  1(Active)  0[Alkaline Phosphatase Increase](Activity Score)  I(Number of Rpts)  ¡Ã4(Index value)  0.9[SGOT Increase](Activity Score)  M(Number of Rpts)  ¡Ã4(Index value)  3[SGPT Increase](Activity Score)  I(Number of Rpts)  ¡Ã4(Index value)  1.1[LDH Increase](Activity Score)  I(Number of Rpts)  <4(Index value)  0.4[GGT Increase](Activity Score)  I(Number of Rpts)  <4(Index value)  0
 
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