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| º¸°ü»ó ÁÖÀÇ |
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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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| Mechanism of Action |
Nefazodone¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Within the serotonergic system, nefazodone acts as an antagonist at type 2 serotonin (5-HT2) post-synaptic receptors and, like fluoxetine-type antidepressants, inhibits pre-synaptic serotonin (5-HT) reuptake. These mechanisms increase the amount of serotonin available to interact with 5-HT receptors. Within the noradrenergic system, nefazodone inhibits norepinephrine uptake minimally. Nefazodone also antagonizes alpha(1)-adrenergic receptors, producing sedation, muscle relaxation, and a variety of cardiovascular effects. Nefazodone's affinity for benzodiazepine, cholinergic, dopaminergic, histaminic, and beta or alpha(2)-adrenergic receptors is not significant.
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| Pharmacology |
Nefazodone¿¡ ´ëÇÑ Pharmacology Á¤º¸ Nefazodone, an antidepressant synthetically derived phenylpiperazine, is used to treat major depression. Although it is structurally similar to trazodone, nefazodone has a mechanism of action different from other antidepressants and, hence, lacks the risk for major cardiovascular toxicity seen with tricyclics and insomnia and inhibition of REM sleep seen with the selective serotonin reuptake inhibitors.
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| Metabolism |
Nefazodone¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)Cytochrome P450 2D6 (CYP2D6)
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| Protein Binding |
Nefazodone¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Greater than 99% (in vitro, human plasma proteins).
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| Half-life |
Nefazodone¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2-4 hours
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| Absorption |
Nefazodone¿¡ ´ëÇÑ Absorption Á¤º¸ Nefazodone is rapidly and completely absorbed. Its absolute bioavailability is low (about 20%).
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| Pharmacokinetics |
Nefazodone HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ë¹ßÇö½Ã°£ : Ä¡·áÈ¿°ú°¡ ³ªÅ¸³ª±â±îÁö´Â Àû¾îµµ 2ÁÖ°¡ ÇÊ¿äÇÏ´Ù.
- ´ë»ç : °£¿¡¼ ´ÙÀ½ 3°¡Áö Ȱ¼ºÇü ´ë»çü·Î ´ë»çµÊ :
- Triazoledione, hydroxynefazodone, m-chlorophenylpiperazine (mCPP)
- ¹Ý°¨±â :
- ¹Ìº¯Èü : 2-4 ½Ã°£
- ´ë»çüÀÇ ¹Ý°¨±â´Â ´õ ±æ´Ù.
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 30ºÐ, À½½Ä¹°°ú ÇÔ²² Åõ¿©½Ã Áö¿¬µÊ
- ¼Ò½Ç : ÁÖ·Î ´ë»çü·Î ´¢¸¦ ÅëÇØ ¹è¼³µÇ°í, ÀϺδ ´ëº¯À¸·Îµµ ¹è¼³µÊ
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| Biotransformation |
Nefazodone¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
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| Toxicity |
Nefazodone¿¡ ´ëÇÑ Toxicity Á¤º¸ Cases of life-threatening hepatic failure have been reported in patients treatedwith nefazodone.
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| Drug Interactions |
Nefazodone¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Almotriptan Increased risk of CNS adverse effectsEletriptan Increased risk of CNS adverse effectsNaratriptan Increased risk of CNS adverse effectsEletriptan Increased risk of CNS adverse effectsFrovatriptan Increased risk of CNS adverse effectsZolmitriptan Increased risk of CNS adverse effectsRizatriptan Increased risk of CNS adverse effectsSumatriptan Increased risk of CNS adverse effectsTriazolam Nefazodone increases the effect of triazolamTrazodone This strong CYP3A4 inhibitor increases the effect and toxicity of trazodoneTacrolimus Nefazodone increases the effect and toxicity of tacrolimusSunitinib Possible increase in sunitinib levelsSt. John's Wort St. John's Wort increases the effect and toxicity of the SSRIPimozide Nefazodone increases the effect and toxicity of pimozideBuspirone Nefazodone increases the effect of buspironeCarbamazepine Nefazodone increases the effect of carbamazepineCilostazol Nefazodone increases the effect of cilostazolCisapride Nefazodone increases serum levels of cisaprideEplerenone Nefazodone increases the effect and toxicity of eplerenoneErlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinibAprepitant This CYP3A4 inhibitor increases the effect and toxicity of aprepitantAtorvastatin Nefazodone increases the effect and toxicity of the statin drugCerivastatin Nefazodone increases the effect and toxicity of the statin drugCyclosporine The antidepressant increases the effect and toxicity of cyclosporineLovastatin Nefazodone increases the effect and toxicity of the statin drugSimvastatin Nefazodone increases the effect and toxicity of the statin drugSolifenacin This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolismDarifenacin This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolismTranylcypromine Possible severe adverse reaction with this combinationRasagiline Possible severe adverse reaction with this combinationPhenelzine Possible severe adverse reaction with this combinationIsocarboxazid Possible severe adverse reaction with this combinationAstemizole Increased risk of cardiotoxicity and arrhythmiasLoratadine Increased risk of cardiotoxicityTerfenadine Increased risk of cardiotoxicity and arrhythmiasTramadol Increased risk of serotonin syndromeSibutramine Risk of serotoninergic syndromeLinezolid Combination associated with possible serotoninergic syndromeDihydroergotamine Possible ergotism and severe ischemia with this combinationErgotamine Possible ergotism and severe ischemia with this combination
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Nefazodone¿¡ ´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 |
Nefazodone¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Take this medication either consistently with or without food as instructed by your doctor.Limit garlic, ginger, gingko, and horse chestnut.Avoid avocado.
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| Drug Target |
[Drug Target]
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| Description |
Nefazodone¿¡ ´ëÇÑ Description Á¤º¸ Nefazodone hydrochloride (trade name Serzone) is an antidepressant drug marketed by Bristol-Myers Squibb. Its sale was discontinued in 2003 in some countries, due to the small possibility of hepatic (liver) injury, which could lead to the need for a liver transplant, or even death. The incidence of severe liver damage is approximately 1 in 250,000 to 300,000 patient-years. On May 20, 2004, Bristol-Myers Squibb discontinued the sale of Serzone in the United States. [Wikipedia]
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| Drug Category |
Nefazodone¿¡ ´ëÇÑ Drug_Category Á¤º¸ AnalgesicsAntidepressantsAntidepressive Agents, Second-GenerationSerotonin Agents
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| Smiles String Canonical |
Nefazodone¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCC1=NN(CCCN2CCN(CC2)C2=CC(Cl)=CC=C2)C(=O)N1CCOC1=CC=CC=C1
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| Smiles String Isomeric |
Nefazodone¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CCC1=NN(CCCN2CCN(CC2)C2=CC(Cl)=CC=C2)C(=O)N1CCOC1=CC=CC=C1
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| InChI Identifier |
Nefazodone¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C25H32ClN5O2/c1-2-24-27-31(25(32)30(24)18-19-33-23-10-4-3-5-11-23)13-7-12-28-14-16-29(17-15-28)22-9-6-8-21(26)20-22/h3-6,8-11,20H,2,7,12-19H2,1H3
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| Chemical IUPAC Name |
Nefazodone¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-[3-[4-(3-chlorophenyl)piperazin-1-yl]propyl]-5-ethyl-4-[2-(phenoxy)ethyl]-1,2,4-triazol-3-one
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| Drug-Induced Toxicity Related Proteins |
NEFAZODONE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:CYP3A4 Drug:Nefazodone Toxicity:idiosyncratic hepatotoxicity. [¹Ù·Î°¡±â]
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ÃÖ±ÙÁ¤º¸¼öÁ¤ÀÏ 2016-11-21
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»ó¼¼Á¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×À» Åä´ë·Î ÀÛ¼ºµÇ¾úÀ¸¸ç ¿ä¾àÁ¤º¸´Â »ó¼¼Á¤º¸ ¹× ±âŸ¹®ÇåÀ» ±â¹ÝÀ¸·Î µå·°ÀÎÆ÷¿¡¼ ÆíÁýÇÑ ³»¿ëÀÔ´Ï´Ù. Á¦Ç°Çã°¡»çÇ×ÀÇ ¸ñÂ÷¿Í ´Ù¼Ò »óÀÌÇÒ ¼ö ÀÖ½À´Ï´Ù. |
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µå·°ÀÎÆ÷ ÀǾàÇмúÁ¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×, Çмú¹®Çå, Á¦¾àȸ»ç Á¦°øÁ¤º¸ µîÀ» ±Ù°Å·Î ÀÛ¼ºµÈ Âü°í Á¤º¸ÀÔ´Ï´Ù.
Á¤º¸ÀÇ Á¤È®¼ºÀ» À§ÇØ ³ë·ÂÇϰí ÀÖÀ¸³ª ÆíÁý»óÀÇ ¿À·ù, Çã°¡»çÇ× º¯°æ, Ãß°¡ÀûÀÎ Çмú¿¬±¸ ¶Ç´Â Àӻ󿬱¸ ¹ßÇ¥ µîÀ¸·Î ÀÎÇØ ¹ß»ýÇÏ´Â ¹®Á¦¿¡ ´ëÇØ µå·°ÀÎÆ÷´Â
Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù. ÀÚ¼¼ÇÑ ³»¿ëÀº ¡°Ã¥ÀÓÀÇ ÇÑ°è ¹× ¹ýÀû°íÁö¡±¸¦ ÂüÁ¶ÇØ ÁֽʽÿÀ.
¹Ýµå½Ã Á¦Á¶¡¤¼öÀÔ»ç, ÆÇ¸Å»ç, ÀÇ»ç, ¾à»ç¿¡°Ô ÃÖÁ¾ÀûÀ¸·Î È®ÀÎÇϽñ⠹ٶø´Ï´Ù.
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. NEFAZODONE[GGT Increase][Composite Activity](Score) I(Marginal) 2(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 1.1[SGOT Increase](Activity Score) M(Number of Rpts) ¡Ã4(Index value) 3.6[SGPT Increase](Activity Score) M(Number of Rpts) ¡Ã4(Index value) 3.3[LDH Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 1.1[GGT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 1.1
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