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    | Brandname Á¤º¸ | 
    
      Buspirone
 Brand Names/Synonyms
- Ansial 
 - Ansiced 
 - Anxiron 
 - Axoren 
 - Bespar 
 - Buspar 
 - Buspimen 
 - Buspinol 
 - Buspirona [INN-Spanish] 
 - Buspirone HCL 
 - Buspironum [INN-Latin] 
 - Buspisal 
 - Censpar 
 - Lucelan 
 - Narol 
 - Travin 
  
 Brand Name MixturesNot Available
 Chemical IUPAC Name8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-8-azaspiro[4.5]decane-7,9-dione
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    | Mechanism of Action | 
    
       Buspirone¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Buspirone binds to 5-HT type 1A serotonin receptors on presynaptic neurons in the dorsal raphe and on postsynaptic neurons in the hippocampus, thus inhibiting the firing rate of 5-HT-containing neurons in the dorsal raphe. Buspirone also binds at dopamine type 2 (DA2) receptors, blocking presynaptic dopamine receptors. Buspirone increases firing in the locus ceruleus, an area of brain where norepinephrine cell bodies are found in high concentration. The net result of buspirone actions is that serotonergic activity is suppressed while noradrenergic and dopaminergic cell firing is enhanced. 
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    | Pharmacology | 
     
       Buspirone¿¡ ´ëÇÑ Pharmacology Á¤º¸ Buspirone is used in the treatment of generalized anxiety where it has advantages over other antianxiety drugs because it does not cause sedation (drowsiness) and does not cause tolerance or physical dependence. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. in vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding in vitro or in vivo when tested in preclinical models. Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems. 
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    | Metabolism | 
    
       Buspirone¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4) 
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    | Protein Binding | 
    
       Buspirone¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 95% (approximately 70% bound to albumin, 30% bound to alpha 1 -acid glycoprotein) 
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    | Half-life | 
    
       Buspirone¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2-3 hours (although the action of a single dose is much longer than the short halflife indicates). 
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    | Absorption | 
    
       Buspirone¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly absorbed in man. Bioavailability is low and variable (approximately 5%) due to extensive first pass metabolism. 
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    | Pharmacokinetics | 
    
       Buspirone HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á 
	- ´Ü¹é°áÇÕ : 95%
	
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    | Biotransformation | 
    
       Buspirone¿¡ ´ëÇÑ Biotransformation Á¤º¸ Metabolized hepatically, primarily by oxidation by cytochrome P450 3A4 producing several hydroxylated derivatives and a pharmacologically active metabolite, 1-pyrimidinylpiperazine (1-PP) 
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    | Toxicity | 
    
       Buspirone¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral, rat LD50 = 136 mg/kg. Symptoms of overdose include dizziness, drowsiness, nausea or vomiting, severe stomach upset, and unusually small pupils. 
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    | Drug Interactions | 
    
       Buspirone¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Clarithromycin	Clarithromycin increases the effect and toxicity of buspironeDiltiazem	The calcium channel blocker increases the effect and toxicity of buspironeErythromycin	The macrolide increases the effect and toxicity of buspironeIsocarboxazid	Possible blood pressure elevationItraconazole	The macrolide increases the effect and toxicity of buspironeJosamycin	The macrolide increases the effect and toxicity of buspironeKetoconazole	The macrolide increases the effect and toxicity of buspironeNefazodone	Nefazodone increases the effect of buspironePhenelzine	Possible blood pressure elevationRasagiline	Possible blood pressure elevationRifabutin	Rifabutin decreases the effect of buspironeRifampin	Rifampin decreases the effect of buspironeRitonavir	Ritonavir increases the effect and toxicity of buspironeTranylcypromine	Possible blood pressure elevationVerapamil	The calcium channel blocker increases the effect and toxicity of buspirone 
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    CYP450  Drug Interaction | 
    
      [CYP450 TableÁ÷Á¢Á¶È¸] Buspirone¿¡ ´ëÇÑ P450 table
  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 
 
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    | Food Interaction | 
    
       Buspirone¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Take with food.Always take at the same time with respect to meals.Avoid taking grapefruit or grapefruit juice throughout treatment. 
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    | Drug Target | 
    
      
      [Drug Target]
     | 
   
  
   
    | Description | 
    
       Buspirone¿¡ ´ëÇÑ Description Á¤º¸ An anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to diazepam. [PubChem] 
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    | Drug Category | 
    
       Buspirone¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-anxiety AgentsAnxiolytics sedatives and hypnoticsSerotonin Agonists 
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    | Smiles String Canonical | 
    
       Buspirone¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)C1=NC=CC=N1 
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    | Smiles String Isomeric | 
    
       Buspirone¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)C1=NC=CC=N1 
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    | InChI Identifier | 
    
       Buspirone¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C21H31N5O2/c27-18-16-21(6-1-2-7-21)17-19(28)26(18)11-4-3-10-24-12-14-25(15-13-24)20-22-8-5-9-23-20/h5,8-9H,1-4,6-7,10-17H2 
     | 
   
  
   
    | Chemical IUPAC Name | 
    
       Buspirone¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-8-azaspiro[4.5]decane-7,9-dione 
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                          ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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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. BUSPIRONE[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)  I(Number of Rpts)  ¡Ã4(Index value)  2.4[SGPT Increase](Activity Score)  M(Number of Rpts)  ¡Ã4(Index value)  3.1[LDH Increase](Activity Score)  I(Number of Rpts)  <4(Index value)  0.4[GGT Increase](Activity Score)  I(Number of Rpts)  <4(Index value)  0.6
 
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