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    Dextromethorphan¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â 
Ephedrine¿¡ ´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 | 
    
       Dextromethorphan¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Dextromethorphan is an opioid-like drug that binds to and acts as antagonist to the NMDA glutamatergic receptor, it is an agonist to the opioid sigma 1 and sigma 2 receptors, it is also an alpha3/beta4 nicotinic receptor antagonist and targets the serotonin reuptake pump. Dextromethorphan is rapidly absorbed from the gastrointestinal tract, where it enters the bloodstream and crosses the blood-brain barrier. The first-pass through the hepatic portal vein results in some of the drug being metabolized into an active metabolite of dextromethorphan, dextrorphan, the 3-hydroxy derivative of dextromethorphan.
  Guaifenesin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Guaifenesin may act as an irritant to gastric vagal receptors, and recruit efferent parasympathetic reflexes that cause glandular exocytosis of a less viscous mucus mixture. Cough may be provoked. This combination may flush tenacious, congealed mucopurulent material from obstructed small airways and lead to a temporary improvement in dyspnea or the work of breathing.
  Pseudoephedrine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Pseudoephedrine acts directly on both alpha- and, to a lesser degree, beta-adrenergic receptors. Through direct action on alpha-adrenergic receptors in the mucosa of the respiratory tract, pseudoephedrine produces vasoconstriction. Pseudoephedrine relaxes bronchial smooth muscle by stimulating beta2-adrenergic receptors. Like ephedrine, pseudoephedrine releasing norepinephrine from its storage sites, an indirect effect. 
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    | Pharmacology | 
     
       Dextromethorphan¿¡ ´ëÇÑ Pharmacology Á¤º¸ Dextromethorphan suppresses the cough reflex by a direct action on the cough center in the medulla of the brain. Dextromethorphan shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist and acts as a non-competitive channel blocker. It is one of the widely used antitussives, and is also used to study the involvement of glutamate receptors in neurotoxicity.
  Guaifenesin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Guaifenesin is an expectorant which increases the output of phlegm (sputum) and bronchial secretions by reducing adhesiveness and surface tension. The increased flow of less viscous secretions promotes ciliary action and changes a dry, unproductive cough to one that is more productive and less frequent. By reducing the viscosity and adhesiveness of secretions, guaifenesin increases the efficacy of the mucociliary mechanism in removing accumulated secretions from the upper and lower airway.
  Pseudoephedrine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Pseudoephedrine is a sympathomimetic agent, structurally similar to ephedrine, used to relieve nasal and sinus congestion and reduce air-travel-related otalgia in adults. The salts pseudoephedrine hydrochloride and pseudoephedrine sulfate are found in many over-the-counter preparations either as single-ingredient preparations, or more commonly in combination with antihistamines and/or paracetamol/ibuprofen. Unlike antihistamines, which modify the systemic histamine-mediated allergic response, pseudoephedrine only serves to relieve nasal congestion commonly associated with colds or allergies. The advantage of oral pseudoephedrine over topical nasal preparations, such as oxymetazoline, is that it does not cause rebound congestion (rhinitis medicamentosa). 
     | 
   
  
   
    | Metabolism | 
    
       Dextromethorphan¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2D6 (CYP2D6)
  Pseudoephedrine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Monoamine oxidase type A (MAO-A) 
     | 
   
  
   
    | Protein Binding | 
    
       Pseudoephedrine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Pseudoephedrine does not bind to human plasma proteins over the concentration range of 50 to 2000 ng/mL 
     | 
   
  
   
    | Half-life | 
    
       Dextromethorphan¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 3-6 hours
  Guaifenesin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 1 hour
  Pseudoephedrine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 9-16 hours 
     | 
   
  
   
    | Absorption | 
    
       Dextromethorphan¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly absorbed from the gastrointestinal tract.
  Guaifenesin¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly absorbed from the GI tract
  Pseudoephedrine¿¡ ´ëÇÑ Absorption Á¤º¸ Pseudoephedrine is readily and almost completely absorbed from the GI tract and there is no evidence of first-pass metabolism. 
     | 
   
  
   
    | Pharmacokinetics | 
    
       Dextromethorphan HBrÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á 
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 GuaifenesinÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á 
	- Èí¼ö : À§Àå°üÀ¸·ÎºÎÅÍ Àß Èí¼öµÊ.
	
 - ´ë»ç : 60%°¡ °£´ë»çµÊ.
	
 - ¼Ò½Ç : ´ë»çü ¹× ¹Ìº¯Èü·Î ½Å¹è¼³µÊ.
  
 Pseudoephedrine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á 
	- ºñÃæÇ÷Á¦°Å È¿°úÀÇ ¹ßÇö½Ã°£ (°æ±¸Åõ¿©½Ã) : 15-30ºÐ
	
 - ÀÛ¿ëÁö¼Ó½Ã°£ : 4-6 ½Ã°£ (¼¹æÇü Á¦Á¦´Â 12½Ã°£ Áö¼Ó)
	
 - ´ë»ç : °£¿¡¼ ÀϺΠ´ë»ç 
	
 - ¹Ý°¨±â : 9-16 ½Ã°£ 
	
 - ¼Ò½Ç : Åõ¿©·®ÀÇ 70-90%°¡ ¹Ìº¯Èü·Î, 1-6%°¡ norpseudoephedrineÀ¸·Î ¼Òº¯À¸·Î ¹è¼³µÊ. ½Å¹è¼³Àº ´¢ pH¿Í ´¢·®¿¡ ÀÇÇØ º¯ÈµÇ¸ç ¾ËÄ®¸®´¢´Â pseudoephedrineÀÇ ½Å¹è¼³À» °¨¼Ò½ÃÅ´.
  
     | 
   
  
   
    | Biotransformation | 
    
       Dextromethorphan¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Rapidly and extensively metabolized to dextrorphan (active metabolite). One well known metabolic catalyst involved is a specific cytochrome P450 enzyme known as 2D6, or CYP2D6.
  Guaifenesin¿¡ ´ëÇÑ Biotransformation Á¤º¸ Rapidly hydrolyzed (60% within seven hours) and then excreted in the urine, with beta-(2-methoxyphenoxy)-lactic acid as its major urinary metabolite.
  Pseudoephedrine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. 
     | 
   
  
   
    | Toxicity | 
    
       Dextromethorphan¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
  Guaifenesin¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50 1510 mg/kg (rat, oral)
  Pseudoephedrine¿¡ ´ëÇÑ Toxicity Á¤º¸ Common adverse reactions include nervousness, restlessness, and insomnia. Rare adverse reactions include difficult/painful urination, dizziness/lightheadedness, heart palpitations, headache, increased sweating, nausea/vomiting, trembling, troubled breathing, unusual paleness, and weakness. 
     | 
   
  
   
    | Drug Interactions | 
    
       Dextromethorphan¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Dihydroquinidine barbiturate	Quinidine increases the toxicity of dextromethorphanQuinidine	Quinidine increases the toxicity of dextromethorphanQuinidine barbiturate	Quinidine increases the toxicity of dextromethorphanFluoxetine	Combination associated with possible serotoninergic syndromeIsocarboxazid	Possible severe adverse reactionMemantine	Increased risk of CNS adverse effectsMoclobemide	Increased CNS toxicityParoxetine	Combination associated with possible serotoninergic syndromePhenelzine	Possible severe adverse reactionRasagiline	Possible severe adverse reactionSelegiline	Combination associated with possible serotoninergic syndromeSibutramine	Combination associated with possible serotoninergic syndromeTerbinafine	Terbinafine increases dextromethorphan levelsTranylcypromine	Possible severe adverse reaction
  Guaifenesin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
  Pseudoephedrine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alseroxylon	Increased arterial pressureIsocarboxazid	Increased arterial pressureLinezolid	Possible increase of arterial pressureMethyldopa	Increased arterial pressureBromocriptine	The sympathomimetic increases the toxicity of bromocriptineTranylcypromine	Increased arterial pressureMidodrine	Increased arterial pressureMoclobemide	Moclobemide increases the sympathomimetic effectPargyline	Increased arterial pressurePhenelzine	Increased arterial pressureRasagiline	Increased arterial pressureReserpine	Increased arterial pressureTrimipramine	The tricyclic increases the sympathomimetic effectProtriptyline	The tricyclic increases the sympathomimetic effectNortriptyline	The tricyclic increases the sympathomimetic effectAmitriptyline	The tricyclic increases the sympathomimetic effectAmoxapine	The tricyclic increases the sympathomimetic effectClomipramine	The tricyclic increases the sympathomimetic effectImipramine	The tricyclic increases the sympathomimetic effectDesipramine	The tricyclic increases the sympathomimetic effectDoxepin	The tricyclic increases the sympathomimetic effectDeserpidine	Increased arterial pressureGuanethidine	The agent decreases the effect of guanethidine 
     | 
   
  
   
    CYP450  Drug Interaction | 
    
      [CYP450 TableÁ÷Á¢Á¶È¸] Dextromethorphan¿¡ ´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 
 
     | 
   
  
   
    | Food Interaction | 
    
       Guaifenesin¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with a full glass of water.Take without regard to meals.
  Pseudoephedrine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals. 
     | 
   
  
   
    | Drug Target | 
    
      
      [Drug Target]
     | 
   
  
   
    | SNP Á¤º¸ | 
    
      Name:Dextromethorphan (DB00514)
 Interacting Gene/Enzyme:Cytochrome P450 2D6 (Gene symbol = CYP2D6) Swissprot P10635
 SNP(s):CYP2D6*6 rs5030655 (T deletion, homozygote)
 Effect:Poor drug metabolizer, lower dose requirements
 Reference(s):Bradford LD, Gaedigk A, Leeder JS: High frequency of CYP2D6 poor and "intermediate" metabolizers in black populations: a review and preliminary data. Psychopharmacol Bull. 1998;34(4):797-804. [PubMed] 
     | 
   
  
   
    | Description | 
    
       Dextromethorphan¿¡ ´ëÇÑ Description Á¤º¸ The d-isomer of the codeine analog of levorphanol. Dextromethorphan shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (receptors, N-methyl-D-aspartate) and acts as a non-competitive channel blocker. It is one of the widely used antitussives, and is also used to study the involvement of glutamate receptors in neurotoxicity. [PubChem]
  Guaifenesin¿¡ ´ëÇÑ Description Á¤º¸ An expectorant that also has some muscle relaxing action. It is used in many cough preparations. [PubChem]
  Pseudoephedrine¿¡ ´ëÇÑ Description Á¤º¸ An alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used in the treatment of several disorders including asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists. [PubChem] 
     | 
   
  
   
    | Dosage Form | 
    
       Dextromethorphan¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule	OralLiquid	OralLozenge	OralStrip	OralSuspension	OralSyrup	OralTablet	Oral
  Guaifenesin¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid	OralSyrup	Oral
  Pseudoephedrine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid	OralSyrup	OralTablet	OralTablet, extended release	Oral 
     | 
   
  
   
    | Drug Category | 
    
       Dextromethorphan¿¡ ´ëÇÑ Drug_Category Á¤º¸ Analgesics, OpioidAntitussive AgentsExcitatory Amino Acid Antagonists
  Guaifenesin¿¡ ´ëÇÑ Drug_Category Á¤º¸ Expectorants
  Pseudoephedrine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic AgentsBronchodilator AgentsCentral Nervous System AgentsNasal DecongestantsSympathomimeticsVasoconstrictor Agents 
     | 
   
  
   
    | Smiles String Canonical | 
    
       Dextromethorphan¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC2=C(CC3C4CCCCC24CCN3C)C=C1
  Guaifenesin¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC=CC=C1OCC(O)CO
  Pseudoephedrine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CNC(C)C(O)C1=CC=CC=C1 
     | 
   
  
   
    | Smiles String Isomeric | 
    
       Dextromethorphan¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC2=C(C[C@H]3[C@H]4CCCC[C@@]24CCN3C)C=C1
  Guaifenesin¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC=CC=C1OC[C@H](O)CO
  Pseudoephedrine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN[C@@H](C)[C@@H](O)C1=CC=CC=C1 
     | 
   
  
   
    | InChI Identifier | 
    
       Dextromethorphan¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C18H25NO/c1-19-10-9-18-8-4-3-5-15(18)17(19)11-13-6-7-14(20-2)12-16(13)18/h6-7,12,15,17H,3-5,8-11H2,1-2H3/t15-,17+,18-/m1/s1
  Guaifenesin¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C10H14O4/c1-13-9-4-2-3-5-10(9)14-7-8(12)6-11/h2-5,8,11-12H,6-7H2,1H3
  Pseudoephedrine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C10H15NO/c1-8(11-2)10(12)9-6-4-3-5-7-9/h3-8,10-12H,1-2H3/t8-,10+/m0/s1 
     | 
   
  
   
    | Chemical IUPAC Name | 
    
       Dextromethorphan¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ Not Available
  Guaifenesin¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3-(2-methoxyphenoxy)propane-1,2-diol
  Pseudoephedrine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (1S,2S)-2-methylamino-1-phenylpropan-1-ol 
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