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    | Mechanism of Action | 
    
       Tramadol¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Tramadol and its O-desmethyl metabolite (M1) are selective, weak OP3-receptor agonists. Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. The analgesic properties of Tramadol can be attributed to norepinephrine and serotonin reuptake blockade in the CNS, which inhibits pain transmission in the spinal cord. The (+) enantiomer has higher affinity for the OP3 receptor and preferentially inhibits serotonin uptake and enhances serotonin release. The (-) enantiomer preferentially inhibits norepinephrine reuptake by stimulating alpha(2)-adrenergic receptors. 
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    | Pharmacology | 
     
       Tramadol¿¡ ´ëÇÑ Pharmacology Á¤º¸ Tramadol, a centrally-acting analgesic, exists as a racemic mixture of the trans isomer, with important differences in binding, activity, and metabolism associated with the two enantiomers. Although Tramadol is a synthetic analog of codeine, it has a significantly lower affinity for opioid receptors than codeine. Tramadol is used to treat postoperative, dental, cancer, and acute musculosketetal pain and as an adjuvant to NSAID therapy in patients with osteoarthritis. 
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    | Protein Binding | 
    
       Tramadol¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 20% 
     | 
   
  
   
    | Half-life | 
    
       Tramadol¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 23 +/- 10 minutes 
     | 
   
  
   
    | Absorption | 
    
       Tramadol¿¡ ´ëÇÑ Absorption Á¤º¸ Racemic tramadol is rapidly and almost completely absorbed after oral administration. The mean absolute bioavailability of a 100 mg oral dose is approximately 75%.The mean peak plasma concentration of racemic tramadol and M1 occurs at two and three hours, respectively, after administration in healthy adults. 
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    | Pharmacokinetics | 
    
       Tramadol HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á 
-  ÁøÅëÈ¿°ú ¹ßÇö½Ã°£ : 1½Ã°£ À̳»
 
 -  ÃÖ´ëÈ¿°ú ¹ßÇö½Ã°£ : 2-3 ½Ã°£
 
 -  Èí¼ö : °æ±¸ : ½Å¼ÓÇÏ°í °ÅÀÇ ¿ÏÀüÇÏ°Ô Èí¼öµÊ
 
 -  ºÐÆ÷ : ºÐÆ÷¿ëÀû : 2.6-2.9 L/kg
 
 -  ´ë»ç : °£¿¡¼ ¸¹Àº ¾çÀÌ ´ë»çµÇ¸ç, Ȱ¼ºÇü ´ë»çü (M1)´Â CYP 2D6¿¡ ÀÇÇØ »ý¼ºµÊ
 
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    | Biotransformation | 
    
       Tramadol¿¡ ´ëÇÑ Biotransformation Á¤º¸ The major metabolic pathways appear to be N- and O- demethylation and glucuronidation or sulfation in the liver. One metabolite (O-desmethyltramadol, denoted M1) is pharmacologically active in animal models. 
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    | Toxicity | 
    
       Tramadol¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=350mg/kg (orally in mice) 
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    | Drug Interactions | 
    
       Tramadol¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available 
     | 
   
  
   
    CYP450  Drug Interaction | 
    
      [CYP450 TableÁ÷Á¢Á¶È¸] Tramadol¿¡ ´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 
 
     | 
   
  
   
    | Description | 
    
       Tramadol¿¡ ´ëÇÑ Description Á¤º¸ A narcotic analgesic proposed for severe pain. It may be habituating. [PubChem] 
     | 
   
  
   
    | Dosage Form | 
    
       Tramadol¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet, extended release	Oral 
     | 
   
  
   
    | Drug Category | 
    
       Tramadol¿¡ ´ëÇÑ Drug_Category Á¤º¸ AnalgesicsAnalgesics, OpioidNarcotics 
     | 
   
  
   
    | Smiles String Canonical | 
    
       Tramadol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC=CC(=C1)C1(O)CCCCC1CN(C)C 
     | 
   
  
   
    | Smiles String Isomeric | 
    
       Tramadol¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC=CC(=C1)[C@@]1(O)CCCC[C@@H]1CN(C)C 
     | 
   
  
   
    | InChI Identifier | 
    
       Tramadol¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C16H25NO2/c1-17(2)12-14-7-4-5-10-16(14,18)13-8-6-9-15(11-13)19-3/h6,8-9,11,14,18H,4-5,7,10,12H2,1-3H3/t14-,16+/m1/s1 
     | 
   
  
   
    | Chemical IUPAC Name | 
    
       Tramadol¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (1R,2R)-2-(dimethylaminomethyl)-1-(3-methoxyphenyl)cyclohexan-1-ol 
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