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Dapsone¿¡ ´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 |
Dapsone¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Dapsone acts against bacteria and protozoa in the same way as sulphonamides, that is by inhibiting the synthesis of dihydrofolic acid through competition with para-amino-benzoate for the active site of dihydropteroate synthetase. The anti-inflammatory action of the drug is unrelated to its antibacterial action and is still not fully understood.
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| Pharmacology |
Dapsone¿¡ ´ëÇÑ Pharmacology Á¤º¸ Dapsone is a sulfone with anti-inflammatory immunosuppressive properties as well as antibacterial and antibiotic properties. Dapsone is the principal drug in a multidrug regimen recommended by the World Health Organization for the treatment of leprosy. As an anti-infective agent, it is also used for treating malaria and, recently, for Pneumocystic carinii pneumonia in AIDS patients. Dapsone is absorbed rapidly and nearly completely from the gastrointestinal tract. Dapsone is distributed throughout total body water and is present in all tissues. However, it tends to be retained in skin and muscle and especially in the liver and kidney: traces of the drug are present in these organs up to 3 weeks after therapy cessation.
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| Metabolism |
Dapsone¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2C9 (CYP2C9)Cytochrome P450 2E1 (CYP2E1)
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| Protein Binding |
Dapsone¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 70 to 90%
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| Half-life |
Dapsone¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 28 hours (range 10-50 hours)
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| Absorption |
Dapsone¿¡ ´ëÇÑ Absorption Á¤º¸ Bioavailability is 70 to 80% following oral administration.
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| Biotransformation |
Dapsone¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic, mostly CYP2E1-mediated.
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| Toxicity |
Dapsone¿¡ ´ëÇÑ Toxicity Á¤º¸ Overdosage might be expected to produce nasal congestion, syncope, or hallucinations. Measures to support blood pressure should be taken if necessary.
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| Drug Interactions |
Dapsone¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Rifabutin Decreased levels of dapsoneRifampin Decreased levels of dapsoneTrimethoprim Increased toxicity of both productsAluminium Formation of non-absorbable complexesCalcium Formation of non-absorbable complexesMagnesium oxide Formation of non-absorbable complexesMagnesium Formation of non-absorbable complexes
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Dapsone¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.
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| Drug Target |
[Drug Target]
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| Description |
Dapsone¿¡ ´ëÇÑ Description Á¤º¸ A sulfone active against a wide range of bacteria but mainly employed for its actions against mycobacterium leprae. Its mechanism of action is probably similar to that of the sulfonamides which involves inhibition of folic acid synthesis in susceptible organisms. It is also used with pyrimethamine in the treatment of malaria. (From Martindale, The Extra Pharmacopoeia, 30th ed, p157-8)
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| Dosage Form |
Dapsone¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
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| Drug Category |
Dapsone¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Infective AgentsAnti-InfectivesAnti-inflammatory AgentsAntimalarialsAntimycobacterialsFolic Acid AntagonistsLeprostatic Agents
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| Smiles String Canonical |
Dapsone¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ NC1=CC=C(C=C1)S(=O)(=O)C1=CC=C(N)C=C1
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| Smiles String Isomeric |
Dapsone¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ NC1=CC=C(C=C1)S(=O)(=O)C1=CC=C(N)C=C1
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| InChI Identifier |
Dapsone¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C12H12N2O2S/c13-9-1-5-11(6-2-9)17(15,16)12-7-3-10(14)4-8-12/h1-8H,13-14H2
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| Chemical IUPAC Name |
Dapsone¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 4-(4-aminophenyl)sulfonylaniline
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| Drug-Induced Toxicity Related Proteins |
DAPSONE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Myeloperoxidase Drug:dapsone Toxicity:lupus. [¹Ù·Î°¡±â] Replated Protein:Myeloperoxidase Drug:dapsone Toxicity:agranulocytosis. [¹Ù·Î°¡±â]
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