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                    ÄÜÅÃ600  CONTAC 600 CAP[Belladonna alkaloid , Chlorpheniramine Maleate , Phenylpropanolamine HCl]  
                    
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        642103690[A04500451]  
	    
	    
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[Drugbank ÀÇ ¼ººÐÁ¤º¸¿¶÷] [Chlorpheniramine][Phenylpropanolamine]
      
     
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      ÀÌ ¾àÀÇ º¹¿ë¿¡ ÀÇÇØ ¹ßÁø, ¹ßÀû, ±¸°¥, ±¸¿ª, ±¸Åä, ½Ä¿åºÎÁøµîÀÇ Áõ»óÀÌ ³ªÅ¸³ª¸é º¹¿ëÀ» ÁßÁöÇÒ °Í.
      
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    ´Ù¸¥ ³»º¹ ºñ¿°¿ë¾à, Ç×È÷½ºÅ¸¹ÎÁ¦, °¨±â¾àµî°ú µ¿½Ã¿¡ º¹¿ëÇÏÁö ¸» °Í. | 
   
  
    
  
  
       	
  
     
  
  
  
  
  
   
    | Related FDA Approved Drug | 
    
       
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    | DUR (ÀǾàǰ»ç¿ëÆò°¡) | 
    º´¿ë±Ý±â :
     
	 °í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
	 
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    | µ¶¼ºÁ¤º¸ | 
    Chlorpheniramine¿¡ ´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 | 
    
       Chlorpheniramine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
  Phenylpropanolamine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Phenylpropanolamine acts directly on alpha- and, to a lesser degree, beta-adrenergic receptors in the mucosa of the respiratory tract. Stimulation of alpha-adrenergic receptors produces vasoconstriction, reduces tissue hyperemia, edema, and nasal congestion, and increases nasal airway patency. PPA indirectly stimulates beta-receptors, producing tachycardia and a positive inotropic effect. 
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    | Pharmacology | 
     
       Chlorpheniramine¿¡ ´ëÇÑ Pharmacology Á¤º¸ In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Chlorpheniramine, is a histamine H1 antagonist (or more correctly, an inverse histamine agonist) of the alkylamine class. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.
  Phenylpropanolamine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Phenylpropanolamine (PPA), a sympathomimetic agent structurally similar to pseudoephedrine, is used to treat nasal congestion. Phenylpropanolamine is found in appetite suppressant formulations and with guaifenesinin in cough-cold formulations. In 2000, the FDA requested that all drug companies discontinue marketing products containing phenylpropanolamine, due to an increased risk of hemorrhagic stroke in women who used phenylpropanolamine. 
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    | Metabolism | 
    
       Chlorpheniramine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)Cytochrome P450 2D6 (CYP2D6)
  Phenylpropanolamine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Monoamine oxidase type A (MAO-A) 
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    | Protein Binding | 
    
       Chlorpheniramine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 72%
  Phenylpropanolamine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available 
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    | Half-life | 
    
       Chlorpheniramine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 21-27 hours
  Phenylpropanolamine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2.1 to 3.4 hours. 
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    | Absorption | 
    
       Chlorpheniramine¿¡ ´ëÇÑ Absorption Á¤º¸ Well absorbed in the gastrointestinal tract.
  Phenylpropanolamine¿¡ ´ëÇÑ Absorption Á¤º¸ Reduced bioavailability (about 38%) from gastrointestinal tract because of first pass metabolism by monoamine oxidase in the stomach and liver. 
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    | Pharmacokinetics | 
    
       Phenylpropanolamine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á 
- Èí¼ö : °æ±¸ : Àß Èí¼öµÊ
 
	 -  »ýü³»ÀÌ¿ë·ü : °ÅÀÇ 100%
 
	 -  ´ë»ç : °£¿¡¼ norephedrineÀ¸·Î ´ë»çµÊ
 
	 -  ¹Ý°¨±â : 4.6-6.6 ½Ã°£ 
 
	 -  ¼Ò½Ç : ÁÖ·Î ¹Ìº¯Èü·Î¼(80-90%) ´¢¸¦ ÅëÇØ ¹è¼³µÊ
  
 Belladonna alkaloidÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á 
- Èí¼ö : À§Àå°üÀ¸·ÎºÎÅÍ Àß Èí¼öµÈ´Ù.
 - ºÐÆ÷ : À¯Áó ºÐºñ
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 Chlorpheniramine MaleateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á 
	- ´Ü¹é°áÇÕ : 69-72%
	
 - ´ë»ç : °£´ë»ç
	
 - ¹Ý°¨±â : 20-24 ½Ã°£
	
 - ¼Ò½Ç : ´ë»çü, ¾à¹°(3-4%)ÀÌ ½Å¹è¼³µÇ¸ç, 48½Ã°£³»¿¡ ÀüüÀÇ 35%°¡ ¼Ò½ÇµÈ´Ù.
  
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    | Biotransformation | 
    
       Chlorpheniramine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic via Cytochrome P450 (CYP450) enzymes.
  Phenylpropanolamine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic 
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    | Toxicity | 
    
       Chlorpheniramine¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50 = 306 mg/kg in humans, mild reproductive toxin to women of childbearing age.
  Phenylpropanolamine¿¡ ´ëÇÑ Toxicity Á¤º¸ May induce ventricular extrasystoles and short paroxysms of ventricular tachycardia, a sensation of fullness in the head and tingling of the extremities; LD50=1490mg/kg (orally in rat) 
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    | Drug Interactions | 
    
       Chlorpheniramine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Donepezil	Possible antagonism of actionGalantamine	Possible antagonism of actionRivastigmine	Possible antagonism of actionEthotoin	The antihistamine increases the effect of hydantoinFosphenytoin	The antihistamine increases the effect of hydantoinMephenytoin	The antihistamine increases the effect of hydantoinPhenytoin	The antihistamine increases the effect of hydantoin
  Phenylpropanolamine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Acetophenazine	Decreased anorexic effect, may increase psychotic symptomsChlorpromazine	Decreased anorexic effect, may increase psychotic symptomsEthopropazine	Decreased anorexic effect, may increase psychotic symptomsFluphenazine	Decreased anorexic effect, may increase psychotic symptomsMethotrimeprazine	Decreased anorexic effect, may increase psychotic symptomsGuanethidine	The agent decreases the effect of guanethidineMesoridazine	Decreased anorexic effect, may increase psychotic symptomsThioridazine	Decreased anorexic effect, may increase psychotic symptomsMethdilazine	Decreased anorexic effect, may increase psychotic symptomsTrimeprazine	Decreased anorexic effect, may increase psychotic symptomsPropericiazine	Decreased anorexic effect, may increase psychotic symptomsPerphenazine	Decreased anorexic effect, may increase psychotic symptomsProchlorperazine	Decreased anorexic effect, may increase psychotic symptomsPromazine	Decreased anorexic effect, may increase psychotic symptomsPromethazine	Decreased anorexic effect, may increase psychotic symptomsPropiomazine	Decreased anorexic effect, may increase psychotic symptomsThiethylperazine	Decreased anorexic effect, may increase psychotic symptomsTrifluoperazine	Decreased anorexic effect, may increase psychotic symptomsTriflupromazine	Decreased anorexic effect, may increase psychotic symptomsMoclobemide	Moclobemide increases the sympathomimetic effectAmitriptyline	The tricyclic increases the sympathomimetic effectAmoxapine	The tricyclic increases the sympathomimetic effectBromocriptine	The sympathomimetic increases the toxicity of bromocriptineClomipramine	The tricyclic increases the sympathomimetic effectDesipramine	The tricyclic increases the sympathomimetic effectDoxepin	The tricyclic increases the sympathomimetic effectImipramine	The tricyclic increases the sympathomimetic effectNortriptyline	The tricyclic increases the sympathomimetic effectProtriptyline	The tricyclic increases the sympathomimetic effectTrimipramine	The tricyclic increases the sympathomimetic effectVenlafaxine	Risk of serotoninergic syndromeFluvoxamine	Risk of serotoninergic syndromeParoxetine	Risk of serotoninergic syndromeFluoxetine	Risk of serotoninergic syndromeAlseroxylon	Increased arterial pressureDeserpidine	Increased arterial pressureIsocarboxazid	Increased arterial pressureLinezolid	Possible increase of arterial pressureTranylcypromine	Increased arterial pressureRasagiline	Increased arterial pressureReserpine	Increased arterial pressurePhenelzine	Increased arterial pressurePargyline	Increased arterial pressureMethyldopa	Increased arterial pressureMidodrine	Increased arterial pressure 
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    CYP450  Drug Interaction | 
    
      [CYP450 TableÁ÷Á¢Á¶È¸] Chlorpheniramine¿¡ ´ëÇÑ P450 table
  SUBSTRATES 
CYP 2D6 
Beta Blockers: 
S-metoprolol 
propafenone 
timolol 
Antidepressants: 
amitriptyline 
clomipramine 
desipramine 
imipramine 
paroxetine 
Antipsychotics: 
haloperidol 
risperidone 
thioridazine 
aripiprazole 
codeine 
dextromethorphan 
duloxetine 
flecainide 
mexiletine 
ondansetron 
tamoxifen 
tramadol 
venlafaxine 
 INHIBITORS 
CYP 2D6 
amiodarone 
buproprion 
**chlorpheniramine** 
cimetidine 
clomipramine 
duloxetine 
fluoxetine 
haloperidol 
methadone 
mibefradil 
paroxetine 
quinidine 
ritonavir 
 INDUCERS 
CYP 2D6 
N/A 
 
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    | Food Interaction | 
    
       Chlorpheniramine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with food.Avoid alcohol.
  Phenylpropanolamine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Limit caffeine intake. 
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    | Drug Target | 
    
      
      [Drug Target]
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    | Description | 
    
       Chlorpheniramine¿¡ ´ëÇÑ Description Á¤º¸ A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than promethazine. [PubChem]
  Phenylpropanolamine¿¡ ´ëÇÑ Description Á¤º¸ Phenylpropanolamine has been withdrawn in Canada. In November 2000, the Food and Drug Administration (FDA) issued a public health advisory against the use of the drug. 
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    | Dosage Form | 
    
       Chlorpheniramine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Syrup	OralTablet	OralTablet, extended release	Oral
  Phenylpropanolamine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Not Available 
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    | Drug Category | 
    
       Chlorpheniramine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Allergic AgentsAntihistaminesAntipruriticsHistamine H1 Antagonists
  Phenylpropanolamine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic alpha-AgonistsAppetite DepressantsNasal DecongestantsSympathomimetics 
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    | Smiles String Canonical | 
    
       Chlorpheniramine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)CCC(C1=CC=C(Cl)C=C1)C1=CC=CC=N1
  Phenylpropanolamine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(N)C(O)C1=CC=CC=C1 
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    | Smiles String Isomeric | 
    
       Chlorpheniramine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)CC[C@H](C1=CC=C(Cl)C=C1)C1=CC=CC=N1
  Phenylpropanolamine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ C[C@@H](N)[C@@H](O)C1=CC=CC=C1 
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    | InChI Identifier | 
    
       Chlorpheniramine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C16H19ClN2/c1-19(2)12-10-15(16-5-3-4-11-18-16)13-6-8-14(17)9-7-13/h3-9,11,15H,10,12H2,1-2H3
  Phenylpropanolamine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C9H13NO/c1-7(10)9(11)8-5-3-2-4-6-8/h2-7,9,11H,10H2,1H3/t7-,9-/m1/s1 
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    | Chemical IUPAC Name | 
    
       Chlorpheniramine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3-(4-chlorophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine
  Phenylpropanolamine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (1S,2R)-2-amino-1-phenylpropan-1-ol 
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    | Drug-Induced Toxicity Related Proteins | 
    
      MALEATE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Intercellular adhesion molecule 1  Drug:maleate Toxicity:hepatic injury.  [¹Ù·Î°¡±â] 
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