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8) Ç︮ÄÚ¹ÚÅÍ ÆÄÀϷθ® ¾ç¼ºÀÎ À§¡¤½ÊÀÌÁöÀå±Ë¾ç ȯÀÚ : ¼¼±Õ¹Ú¸êÀ» À§ÇÑ ³ë·ÂÀÌ ÇÊ¿äÇÏ´Ù.  | 
   
  
  
  
   
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1) ½ÃÅäÅ©·ÒP450È¿¼Ò(CYP1A2, CYP2C9, CYP2D6, CP3A3/A4, CYP2C19)ÀÇ ¾ïÁ¦ : À̵é È¿¼Ò¸¦ ¾ïÁ¦ÇÔÀ¸·Î½á Äí¸¶¸°°è Ç×ÀÀ°íÁ¦(¿Í¸£ÆÄ¸° µî), »ïȯ°è Ç׿ì¿ï¾à(¾Æ¹ÌÆ®¸³Æ¿¸° µî), Ŭ·¡½º¥°Ç׺ÎÁ¤¸ÆÁ¦(¸®µµÄ«ÀÎ, Äû´Ïµò µî), Ä®½·Ã¤³ÎÂ÷´ÜÁ¦(´ÏÆäµðÇÉ, µôƼ¾ÆÁª µî), ¼³Æ÷´Ò¿ì·¹¾Æ°è °æ±¸Ç÷´ç°ÇÏÁ¦(±Û¸®ÇÇÁöµå µî), Æä´ÏÅäÀÎ, Å׿ÀÇʸ°, ¸ÞÅäÇÁ·Ñ·Ñ, ½ÃŬ·Î½ºÆ÷¸°, Ÿũ·Ñ¸®¹«½º, µð¾ÆÁ¦ÆÊ µî ƯÁ¤ ¾à¹°ÀÇ Ç÷Áß ³óµµ¸¦ Áõ°¡½ÃŲ´Ù. 
2) À¯±â¾çÀ̿¼ö¼Ûü ´Ü¹éÁú(organic cationic transporter(OCT) proteins)À» ÅëÇÑ ½Å¼¼´¢°ü ºÐºñ¸¦ ¾ïÁ¦ : ÇÁ·ÎÄ«Àξƹ̵å, Äû´Ïµò, ¸ÞÆ®Æ÷¸£¹Î, µµÆäÆ¿¶óÀÌµå µî Æ¯Á¤ ¾à¹°ÀÇ Ç÷Áß ³óµµ¸¦ Áõ°¡½ÃŲ´Ù. 
3) À§ pHÀÇ º¯È : ¾à¹°ÀÇ »ýüÀÌ¿ë·ü¿¡ ¿µÇâÀ» ÁÖ¾î Èí¼ö¸¦ Áõ°¡½ÃŰ°Å³ª(¾ÆÅ¸ÀÚ³ªºñ¾î µî) Èí¼ö¸¦ °¨¼Ò½ÃŲ´Ù(¾ÆÁ¹°è Ç×Áø±ÕÁ¦(ÄÉÅäÄÚ³ªÁ¹, ÀÌÆ®¶óÄÚ³ªÁ¹, Æ÷»çÄÚ³ªÁ¹) µî). 
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    Cimetidine¿¡ ´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  | 
   
  
   
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       Cimetidine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Cimetidine binds to an H2-receptor located on the basolateral membrane of the gastric parietal cell, blocking histamine effects. This competitive inhibition results in reduced gastric acid secretion and a reduction in gastric volume and acidity. 
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       Cimetidine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Cimetidine is a histamine H2-receptor antagonist. It reduces basal and nocturnal gastric acid secretion and a reduction in gastric volume, acidity, and amount of gastric acid released in response to stimuli including food, caffeine, insulin, betazole, or pentagastrin. It is used to treat gastrointestinal disorders such as gastric or duodenal ulcer, gastroesophageal reflux disease, and pathological hypersecretory conditions. Cimetidine inhibits many of the isoenzymes of the hepatic CYP450 enzyme system. Other actions of Cimetidine include an increase in gastric bacterial flora such as nitrate-reducing organisms. 
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    | Metabolism | 
    
       Cimetidine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 11A1 (CYP11A1)Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2D6 (CYP2D6) 
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    | Protein Binding | 
    
       Cimetidine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 15-20% 
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       Cimetidine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2 hours 
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    | Absorption | 
    
       Cimetidine¿¡ ´ëÇÑ Absorption Á¤º¸ Rapid 60-70% 
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       Cimetidine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic 
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    | Toxicity | 
    
       Cimetidine¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include nausea, vomiting, diarrhea, increased saliva production, difficulty breathing, and a fast heartbeat. 
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    | Drug Interactions | 
    
       Cimetidine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alfentanil	Increases the effect of the narcoticAlprazolam	Increases the effect of the benzodiazepineAminophylline	Increases the effect of theophyllineAmitriptyline	Increases the effect of tricyclic agentAmoxapine	Increases the effect of tricyclic agentAnisindione	The ANTI-H2 increases the anticoagulant effectAstemizole	Increased risk of cardiotoxicity and arrhythmiasAtazanavir	This gastric pH modifier decreases the levels/effects of atazanavirCarbamazepine	Increases the effect of carbamazepineCarmustine	Increases myelosuppression caused by carmustineChlordiazepoxide	Increases the effect of the benzodiazepineClomipramine	Increases the effect of tricyclic agentClonazepam	Increases the effect of the benzodiazepineClorazepate	Increases the effect of the benzodiazepineClozapine	Increases the effect of clozapineCodeine	Increases the effect of the narcoticDesipramine	Increases the effect of tricyclic agentDiazepam	Increases the effect of the benzodiazepineDicumarol	The anti-H2 increases the anticoagulant effectDihydroquinidine barbiturate	Increases the effect of quinidineDyphylline	Increases the effect of theophyllineDofetilide	Increases effect/toxicity of dofetilideDonepezil	Possible antagonism of actionDoxepin	Increases the effect of tricyclic agentDyphylline	Increases the effect of theophyllineEnoxacin	The agent decreases the absorption of enoxacinEpirubicin	Cimetidine can increase epirubicin levelsEstazolam	Increases the effect of the benzodiazepineEthotoin	Increases the effect of hydantoinFentanyl	Increases the effect of the narcoticFlecainide	Increases serum levels of flecainideFluorouracil	Increases the effect of and toxicity of fluorouacilFlurazepam	Increases the effect of the benzodiazepineFosphenytoin	Increases the effect of hydantoinGalantamine	Possible antagonism of actionHalazepam	Increases the effect of the benzodiazepineHydrocodone	Increases the effect of the narcoticHydromorphone	Increases the effect of the narcoticImipramine	Increases the effect of tricyclic agentItraconazole	The anti-H2 decreases the absorption of the imidazoleLevorphanol	Increases the effect of the narcoticKetoconazole	The anti-H2 decreases the absorption of the imidazoleLidocaine	Increases the effect and toxicity of lidocaineMeperidine	Increases the effect of the narcoticMephenytoin	Increases the effect of hydantoinMetformin	Increases the effect of metforminMethadone	Increases the effect of the narcoticMetoprolol	Increases the effect of the beta-blockerMidazolam	Increases the effect of the benzodiazepineMoclobemide	Increases the effect of moclobemideMorphine	Increases the effect of the narcoticNalbuphine	Increases the effect of the narcoticAcenocoumarol	The anti-H2 increases the anticoagulant effectNimodipine	Increases the effect of the calcium channel blockerNifedipine	Increases the effect of the calcium channel blockerNitrendipine	Increases the effect of the calcium channel blockerNortriptyline	Increases the effect of tricyclic agentOxtriphylline	Increases the effect of theophyllineOxycodone	Increases the effect of the narcoticOxymorphone	Increases the effect of the narcoticPentazocine	Increases the effect of the narcoticPhenytoin	Increases the effect of hydantoinPosaconazole	Significant decrease of posaconazole levelsPramipexole	Increases the effect and toxicity of pramipexolePropoxyphene	Increases the effect of the narcoticProcainamide	The histamine H2-receptor antagonist increases the effect of procainamidePropranolol	Increases the effect of the beta-blockerProtriptyline	Increases the effect of tricyclic agentQuinidine	Increases the effect of quinidineQuinidine barbiturate	Increases the effect of quinidineRivastigmine	Possible antagonism of actionSildenafil	Increases the effect and toxicity of sildenafilSufentanil	Increases the effect of the narcoticTacrine	Increases the effect and toxicity of tacrineTerfenadine	Increased risk of cardiotoxicity and arrhythmiasTheophylline	Increases the effect of theophyllineTimolol	Increases the effect of the beta-blockerTolazoline	Anticipated loss of efficacy of tolazolineTriazolam	Increases the effect of the benzodiazepineTrimipramine	Increases the effect of tricyclic agentWarfarin	The anti-H2 increases the anticoagulant effectZaleplon	Increases the effect and toxicity of zaleplonHeroin	Cimetidine increases the effect of the narcoticKetazolam	Cimetidine increases the effect of the benzodiazepineLabetalol	Cimetidine increases the effect of the beta-blockerPrazepam	Cimetidine increases the effect of the benzodiazepineQuazepam	Cimetidine increases the effect of the benzodiazepine 
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    CYP450  Drug Interaction | 
    
      [CYP450 TableÁ÷Á¢Á¶È¸] Cimetidine¿¡ ´ëÇÑ P450 table
  SUBSTRATES 
CYP 1A2 
clozapine 
cyclobenzaprine 
imipramine 
mexiletine 
naproxen 
riluzole 
tacrine 
theophylline 
 INHIBITORS 
CYP 1A2 
**cimetidine** 
fluoroquinolones 
fluvoxamine 
ticlopidine 
 INDUCERS 
CYP 1A2 
tobacco 
  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 
 SUBSTRATES 
CYP 3A4/3A5/3A7 
Macrolide antibiotics: 
clarithromycin 
erythromycin 
NOT azithromycin 
telithromycin 
Anti-arrhythmics: 
quinidine 
Benzodiazepines: 
alprazolam 
diazepam 
midazolam 
triazolam 
Immune Modulators: 
cyclosporine 
tacrolimus (FK506) 
HIV Protease Inhibitors: 
indinavir 
ritonavir 
saquinavir 
Prokinetic: 
cisapride 
Antihistamines: 
astemizole 
chlorpheniramine 
Calcium Channel Blockers: 
amlodipine 
diltiazem 
felodipine 
nifedipine 
nisoldipine 
nitrendipine 
verapamil 
HMG CoA Reductase Inhibitors: 
atorvastatin 
cerivastatin 
lovastatin 
NOT pravastatin 
simvastatin 
aripiprazole 
buspirone 
gleevec 
haloperidol (in part) 
methadone 
pimozide 
quinine 
NOT rosuvastatin 
sildenafil 
tamoxifen 
trazodone 
vincristine 
 INHIBITORS 
CYP 3A4/3A5/3A7 
HIV Protease Inhibitors: 
indinavir 
nelfinavir 
ritonavir 
amiodarone 
NOT azithromycin 
**cimetidine** 
clarithromycin 
diltiazem 
erythromycin 
fluvoxamine 
grapefruit juice 
itraconazole 
ketoconazole 
mibefradil 
nefazodone 
troleandomycin 
verapamil 
 INDUCERS 
CYP 3A4/3A5/3A7 
carbamazepine 
phenobarbital 
phenytoin 
rifabutin 
rifampin 
St. John's wort 
troglitazone 
     | 
   
  
   
    | Food Interaction | 
    
       Cimetidine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Best effect when taken with food.Limit caffeine intake.Avoid alcohol. 
     | 
   
  
   
    | Drug Target | 
    
      
      [Drug Target]
     | 
   
  
   
    | Description | 
    
       Cimetidine¿¡ ´ëÇÑ Description Á¤º¸ A histamine congener, it competitively inhibits histamine binding to histamine H2 receptors. Cimetidine has a range of pharmacological actions. It inhibits gastric acid secretion, as well as pepsin and gastrins output. It also blocks the activity of cytochrome P-450 which might explain proposals for use in neoadjuvant therapy. [PubChem] 
     | 
   
  
   
    | Drug Category | 
    
       Cimetidine¿¡ ´ëÇÑ Drug_Category Á¤º¸ AdjuvantsAnalgesicsAnti-Ulcer AgentsEnzyme InhibitorsHistamine AntagonistsHistamine H2 Antagonists 
     | 
   
  
   
    | Smiles String Canonical | 
    
       Cimetidine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN=C(NCCSCC1=C(C)NC=N1)NC 
     | 
   
  
   
    | Smiles String Isomeric | 
    
       Cimetidine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ C\N=C(\NCCSCC1=C(C)NC=N1)NC 
     | 
   
  
   
    | InChI Identifier | 
    
       Cimetidine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C10H16N6S/c1-8-9(16-7-15-8)5-17-4-3-13-10(12-2)14-6-11/h7H,3-5H2,1-2H3,(H,15,16)(H2,12,13,14)/f/h13-15H/b12-10- 
     | 
   
  
   
    | Chemical IUPAC Name | 
    
       Cimetidine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3-cyano-2-methyl-1-[2-[(5-methyl-1H-imidazol-4-yl)methylsulfanyl]ethyl]guanidine 
     | 
   
  
   
    | Drug-Induced Toxicity Related Proteins | 
    
      CIMETIDINE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Calcineurin Drug:cimetidine Toxicity:secondary hyperparathyroidism.  [¹Ù·Î°¡±â] 
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