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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
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| Mechanism of Action |
Sulfinpyrazone¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Sulfinpyrazone is an oral uricosuric agent (pyrazolone derivative) used to treat chronic or intermittent gouty arthritis. Sulfinpyrazone competitively inhibits the reabsorption of uric acid at the proximal convoluted tubule, thereby facilitating urinary excretion of uric acid and decreasing plasma urate concentrations. This is likely done through inhibition of the urate anion transporter (hURAT1) as well as the human organic anion transporter 4 (hOAT4). Sulfinpyrazone is not intended for the treatment of acute attacks because it lacks therapeutically useful analgesic and anti-inflammatory effects. Sulfinpyrazone and its sulfide metabolite possess COX inhibitory effects. Sulfinpyrazone has also been shown to be a UDP-glucuronsyltransferase inhibitor and a very potent CYP2C9 inhibitor. Sulfinpyrazone is also known to be a cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor as well as an inhibitor of several multridrug resistance proteins (MRPs).
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| Pharmacology |
Sulfinpyrazone¿¡ ´ëÇÑ Pharmacology Á¤º¸ Sulfinpyrazone's pharmacologic activity is the potentiation of the urinary excretion of uric acid. It is useful for reducing the blood urate levels in patients with chronic tophaceous gout and acute intermittent gout, and for promoting the resorption of tophi.
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| Metabolism |
Sulfinpyrazone¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
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| Protein Binding |
Sulfinpyrazone¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 98-99%
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| Half-life |
Sulfinpyrazone¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ Approximately 4-6 hours
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| Absorption |
Sulfinpyrazone¿¡ ´ëÇÑ Absorption Á¤º¸ Not Available
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| Pharmacokinetics |
SulfinpyrazoneÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ëÁö¼Ó½Ã°£ : ´ë°³ 4-6 ½Ã°£
- Èí¼ö : À§Àå°üÀ¸·ÎºÎÅÍ ½Å¼ÓÇÏ°í ¿ÏÀüÇÏ°Ô Èí¼öµÈ´Ù.
- ´Ü¹é°áÇÕ : 98-99%
- ´ë»ç : °£´ë»ç
- ¹Ý°¨±â : ¾à 4½Ã°£ (¹üÀ§ : 1-9 ½Ã°£)
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 1.6 ½Ã°£
- ¼Ò½Ç : 85-95% (¹Ìº¯Èü·Î´Â 22-50%)°¡ ½Å¹è¼³µÇ¸ç, 5% Á¤µµ´Â ´ëº¯À¸·Î ¹è¼³µÈ´Ù.
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| Toxicity |
Sulfinpyrazone¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include nausea, vomiting, diarrhea, epigastric pain, ataxia, labored respiration, convulsions, coma. Possible symptoms, seen after overdosage with other pyrazolone derivatives: anemia, jaundice, and ulceration.
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| Drug Interactions |
Sulfinpyrazone¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Sulfinpyrazone¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
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| Drug Target |
[Drug Target]
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| Description |
Sulfinpyrazone¿¡ ´ëÇÑ Description Á¤º¸ A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties. [PubChem]
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| Dosage Form |
Sulfinpyrazone¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
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| Drug Category |
Sulfinpyrazone¿¡ ´ëÇÑ Drug_Category Á¤º¸ Uricosuric Agents
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| Smiles String Canonical |
Sulfinpyrazone¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ O=C1C(CCS(=O)C2=CC=CC=C2)C(=O)N(N1C1=CC=CC=C1)C1=CC=CC=C1
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| Smiles String Isomeric |
Sulfinpyrazone¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ O=C1C(CC[S@](=O)C2=CC=CC=C2)C(=O)N(N1C1=CC=CC=C1)C1=CC=CC=C1
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| InChI Identifier |
Sulfinpyrazone¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C23H20N2O3S/c26-22-21(16-17-29(28)20-14-8-3-9-15-20)23(27)25(19-12-6-2-7-13-19)24(22)18-10-4-1-5-11-18/h1-15,21H,16-17H2
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| Chemical IUPAC Name |
Sulfinpyrazone¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 1,2-di(phenyl)-4-(2-phenylsulfinylethyl)pyrazolidine-3,5-dione
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