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[A12250761]
[º¸ÇèÄڵ忡 µû¸¥ ¾àǰ±âº»Á¤º¸ Á÷Á¢Á¶È¸]
\0 ¿ø/1Á¤(2007.03.01)(ÇöÀç¾à°¡)
\41 ¿ø/1Á¤(2004.02.01)(º¯°æÀü¾à°¡)
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[Drugbank ÀÇ ¼ººÐÁ¤º¸¿¶÷] [Sulfadiazine][Trimethoprim]
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| Related FDA Approved Drug |
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 FDA : Dµî±Þ
(sulfadiazine; )
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»ó±â ÀÓºÎÅõ¿©¿¡ ´ëÇÑ Á¤º¸´Â Àü»êó¸® µÇ¸é¼ ÀÔ·Â ¿À·ù °¡´É¼ºÀÌ Á¸ÀçÇÕ´Ï´Ù. ¿À·ù °¡´É¼ºÀ» ÃÖ¼ÒÈÇϱâ À§ÇÏ¿© ¸¹Àº ³ë·ÂÀ» ±â¿ïÀ̰í ÀÖÀ¸³ª, ±× Á¤È®¼º¿¡ ´ëÇÏ¿© È®½ÅÀ» µå¸± ¼ö ¾ø½À´Ï´Ù. ÀÌ¿¡ ´ëÇØ ȸ»ç´Â Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù.
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º´¿ë±Ý±â :
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| Mechanism of Action |
Sulfadiazine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Sulfadiazine is a competitive inhibitor of bacterial para-aminobenzoic acid (PABA), a substrate of the enzyme dihydropteroate synthetase. The inhibited reaction is necessary in these organisms for the synthesis of folic acid.
Trimethoprim¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Trimethoprim binds to bacterial dihydrofolate reductase, subsequently interfering with the uptake of p-aminobenzoic acid (PABA) into folic acid. As folic acid is a coenzyme responsible for the transport of one-carbon fragments from one molecule to another, it is an essential component of bacterial development. Sulfonamides inhibit bacterial dihydrofolate synthetase, the enzyme immediately preceding dihydrofolate reductase, and therefore act synergistically with trimethoprim.
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| Pharmacology |
Sulfadiazine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Sulfadiazine is a sulfonamide antibiotic. The sulfonamides are synthetic bacteriostatic antibiotics with a wide spectrum against most gram-positive and many gram-negative organisms. However, many strains of an individual species may be resistant. Sulfonamides inhibit multiplication of bacteria by acting as competitive inhibitors of p-aminobenzoic acid in the folic acid metabolism cycle. Bacterial sensitivity is the same for the various sulfonamides, and resistance to one sulfonamide indicates resistance to all. Most sulfonamides are readily absorbed orally. However, parenteral administration is difficult, since the soluble sulfonamide salts are highly alkaline and irritating to the tissues. The sulfonamides are widely distributed throughout all tissues. High levels are achieved in pleural, peritoneal, synovial, and ocular fluids. Although these drugs are no longer used to treat meningitis, CSF levels are high in meningeal infections. Their antibacterial action is inhibited by pus.
Trimethoprim¿¡ ´ëÇÑ Pharmacology Á¤º¸ Trimethoprim, a synthetic antiinfective agent, is used to treat and prevent urinary tract infections, diarrhea, and, when combined with either sulfamethoxazole or dapsone, Pneumocystis carinii infections.
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| Metabolism |
Sulfadiazine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
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| Protein Binding |
Sulfadiazine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
Trimethoprim¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Approximately 45%
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| Half-life |
Sulfadiazine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ Not Available
Trimethoprim¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 8-10 hours
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| Absorption |
Sulfadiazine¿¡ ´ëÇÑ Absorption Á¤º¸ Not Available
Trimethoprim¿¡ ´ëÇÑ Absorption Á¤º¸ Not Available
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| Pharmacokinetics |
TrimethoprimÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : °æ±¸ : ´ëºÎºÐÀÌ ½±°Ô Àß Èí¼öµÈ´Ù.
- ´Ü¹é°áÇÕ : 42-46%
- ´ë»ç : ºÎºÐÀûÀ¸·Î °£´ë»ç
- ¹Ý°¨±â : 8-14½Ã°£, ½Å ¼Õ»ó½Ã ¿¬Àå
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 1-4 ½Ã°£ À̳»
- ¼Ò½Ç : 60-80%°¡ ¹Ìº¯Èü·Î ½Å¹è¼³
SulfadiazineÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : °æ±¸ : Àß Èí¼öµÈ´Ù.
- ºÐÆ÷ : ü³» Á¶Á÷°ú ´Á¸·¾×, º¹¸·¾×, Ȱ¾×, ¹æ¼ö µîÀ» Æ÷ÇÔÇÑ Ã¼¾×¿¡ ³Î¸® ºÐÆ÷
- ³úô¼ö¾×À¸·Î ½±°Ô È®»êµÈ´Ù.
- À¯ÁóºÐºñ
- ´ë»ç : N-acetylation
- ¹Ý°¨±â : 10½Ã°£
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 3-6 ½Ã°£ À̳»
- ¼Ò½Ç : 15-40%°¡ ´ë»çü·Î, 43-60%°¡ ¹Ìº¯Èü·Î ½Å¹è¼³
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| Biotransformation |
Sulfadiazine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Not Available
Trimethoprim¿¡ ´ëÇÑ Biotransformation Á¤º¸ Not Available
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| Toxicity |
Sulfadiazine¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral LD50 in mouse is 1500 mg/kg.
Trimethoprim¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=4850 (orally in mice)
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| Drug Interactions |
Sulfadiazine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
Trimethoprim¿¡ ´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 |
Sulfadiazine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
Trimethoprim¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take on empty stomach: 1 hour before or 2 hours after meals.Take with a full glass of water.Do not take calcium, aluminium, magnesium or iron supplements within 2 hours of taking this medication.
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| Drug Target |
[Drug Target]
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| Description |
Sulfadiazine¿¡ ´ëÇÑ Description Á¤º¸ One of the short-acting sulfonamides used in combination with pyrimethamine to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections. [PubChem]
Trimethoprim¿¡ ´ëÇÑ Description Á¤º¸ A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to pyrimethamine. The interference with folic acid metabolism may cause a depression of hematopoiesis. It is potentiated by sulfonamides and the trimethoprim-sulfamethoxazole combination is the form most often used. It is sometimes used alone as an antimalarial. trimethoprim resistance has been reported. [PubChem]
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| Dosage Form |
Sulfadiazine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Not Available
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| Drug Category |
Sulfadiazine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Infective AgentsAnti-InfectivesAntiprotozoal AgentsAntiprotozoalsCoccidiostats
Trimethoprim¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Infective Agents, UrinaryAnti-InfectivesAntimalarialsFolic Acid Antagonists
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| Smiles String Canonical |
Sulfadiazine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ NC1=CC=C(C=C1)S(=O)(=O)NC1=NC=CC=N1
Trimethoprim¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC(CC2=CN=C(N)N=C2N)=CC(OC)=C1OC
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| Smiles String Isomeric |
Sulfadiazine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ NC1=CC=C(C=C1)S(=O)(=O)NC1=NC=CC=N1
Trimethoprim¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC(CC2=CN=C(N)N=C2N)=CC(OC)=C1OC
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| InChI Identifier |
Sulfadiazine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C10H10N4O2S/c11-8-2-4-9(5-3-8)17(15,16)14-10-12-6-1-7-13-10/h1-7H,11H2,(H,12,13,14)/f/h14H
Trimethoprim¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C14H18N4O3/c1-19-10-5-8(6-11(20-2)12(10)21-3)4-9-7-17-14(16)18-13(9)15/h5-7H,4H2,1-3H3,(H4,15,16,17,18)/f/h15-16H2
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| Chemical IUPAC Name |
Sulfadiazine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 4-amino-N-pyrimidin-2-ylbenzenesulfonamide
Trimethoprim¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 5-[(3,4,5-trimethoxyphenyl)methyl]pyrimidine-2,4-diamine
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