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¾ËÄݽºÅé(µð¼³ÇǶ÷250mg) ALCOHOLSTOP TAB.[Disulfiram]
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[Drugbank ÀÇ ¼ººÐÁ¤º¸¿¶÷] [Disulfiram]
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| Related FDA Approved Drug |
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½Å°æ±Ù°èÀÌ»ó °ü·Ã¾à¹° (Neuromuscular Disorder related drugs)
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Disulfiram / N07BB01
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Disulfiram¿¡ ´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 |
Disulfiram¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Disulfiram blocks the oxidation of alcohol at the acetaldehyde stage during alcohol metabolism following disulfiram intake causing an accumulation of acetaldehyde in the blood producing highly unpleasant symptoms. Disulfiram blocks the oxidation of alcohol through its irreversible inactivation of aldehyde dehydrogenase, which acts in the second step of ethanol utilization. In addition, disulfiram competitively binds and inhibits the peripheral benzodiazepine receptor, which may indicate some value in the treatment of the symptoms of alcohol withdrawal, however this activity has not been extensively studied.
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| Pharmacology |
Disulfiram¿¡ ´ëÇÑ Pharmacology Á¤º¸ Disulfiram produces a sensitivity to alcohol which results in a highly unpleasant reaction when the patient under treatment ingests even small amounts of alcohol. Disulfiram blocks the oxidation of alcohol at the acetaldehyde stage during alcohol metabolism following disulfiram intake, the concentration of acetaldehyde occurring in the blood may be 5 to 10 times higher than that found during metabolism of the same amount of alcohol alone. Accumulation of acetaldehyde in the blood produces a complex of highly unpleasant symptoms referred to hereinafter as the disulfiram-alcohol reaction. This reaction, which is proportional to the dosage of both disulfiram and alcohol, will persist as long as alcohol is being metabolized. Disulfiram does not appear to influence the rate of alcohol elimination from the body. Prolonged administration of disulfiram does not produce tolerance; the longer a patient remains on therapy, the more exquisitely sensitive he becomes to alcohol.
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| Metabolism |
Disulfiram¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
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| Protein Binding |
Disulfiram¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
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| Half-life |
Disulfiram¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ Not Available
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| Absorption |
Disulfiram¿¡ ´ëÇÑ Absorption Á¤º¸ Disulfiram is absorbed slowly from the gastrointestinal tract (80 to 90% of oral dose).
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| Pharmacokinetics |
DisulfiramÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÃÖ´ëÈ¿°ú ¹ßÇö½Ã°£ : 12½Ã°£
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- ´ë»ç : diethyldithiocarbamate·Î ´ë»çµÈ ÈÄ carbon disulfide¿Í diethylamineÀ¸·Î »êȵȴÙ.
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| Toxicity |
Disulfiram¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=8.6g/kg (orally in rats). Symptoms of overdose include irritation, slight drowsiness, unpleasant taste, mild GI disturbances, and orthostatic hypotension.
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| Drug Interactions |
Disulfiram¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Aminophylline Increases the effect and toxicity of theophyllineAmprenavir Increased risk of side effects (oral solution)Anisindione Increases the anticoagulant effectChlorzoxazone Increases chlorzoxazone levelsCocaine Increases the cardiac toxicity of cocaineDicumarol Increases the anticoagulant effectDyphylline Increases the effect and toxicity of theophyllineEthotoin Increases the effect of phenytoinFosphenytoin Increases the effect of phenytoinIsoniazid Increased risk of CNS adverse efectsMephenytoin Increases the effect of phenytoinMetronidazole Possible acute psychosis and confusionOxtriphylline Increases the effect and toxicity of theophyllinePhenytoin Increases the effect of phenytoinTheophylline Increases the effect and toxicity of theophyllineWarfarin Increases the anticoagulant effectAcenocoumarol Disulfiram increases the anticoagulant effect
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Disulfiram¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 2E1
acetaminophen
chlorzoxazone
ethanol
INHIBITORS
CYP 2E1
**disulfiram**
INDUCERS
CYP 2E1
ethanol
isoniazid
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| Food Interaction |
Disulfiram¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Avoid alcohol for up to 14 days after treatment has been stopped.
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| Drug Target |
[Drug Target]
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| Description |
Disulfiram¿¡ ´ëÇÑ Description Á¤º¸ A carbamate derivative used as an alcohol deterrent. It is a relatively nontoxic substance when administered alone, but markedly alters the intermediary metabolism of alcohol. When alcohol is ingested after administration of disulfiram, blood acetaldehyde concentrations are increased, followed by flushing, systemic vasodilation, respiratory difficulties, nausea, hypotension, and other symptoms (acetaldehyde syndrome). It acts by inhibiting aldehyde dehydrogenase. [PubChem]
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| Drug Category |
Disulfiram¿¡ ´ëÇÑ Drug_Category Á¤º¸ Alcohol DeterrentsEnzyme Inhibitors
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| Smiles String Canonical |
Disulfiram¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCN(CC)C(=S)SSC(=S)N(CC)CC
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| Smiles String Isomeric |
Disulfiram¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CCN(CC)C(=S)SSC(=S)N(CC)CC
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| InChI Identifier |
Disulfiram¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C10H20N2S4/c1-5-11(6-2)9(13)15-16-10(14)12(7-3)8-4/h5-8H2,1-4H3
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| Chemical IUPAC Name |
Disulfiram¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ diethylcarbamothioylsulfanyl diethylaminomethanedithioate
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| Drug-Induced Toxicity Related Proteins |
DISULFIRAM ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Dopamine beta-hydroxylase Drug:disulfiram Toxicity:cerebral toxic effect. [¹Ù·Î°¡±â] Replated Protein:Aldehyde dehydrogenase Drug:disulfiram Toxicity:loss of motor function. [¹Ù·Î°¡±â] Replated Protein:Aldehyde dehydrogenase Drug:disulfiram Toxicity:sedation. [¹Ù·Î°¡±â] Replated Protein:Aldehyde dehydrogenase Drug:disulfiram Toxicity:dyspnea. [¹Ù·Î°¡±â]
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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. DISULFIRAM[GGT Increase][Composite Activity](Score) A(Marginal) 0(Active) 5[Alkaline Phosphatase Increase](Activity Score) A(Number of Rpts) ¡Ã4(Index value) 26[SGOT Increase](Activity Score) A(Number of Rpts) ¡Ã4(Index value) 58.6[SGPT Increase](Activity Score) A(Number of Rpts) ¡Ã4(Index value) 45.6[LDH Increase](Activity Score) A(Number of Rpts) ¡Ã4(Index value) 26[GGT Increase](Activity Score) A(Number of Rpts) <4(Index value) 19.5
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