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ofloxacin / S01AE01
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Mechanism of Action
Ofloxacin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Ofloxacin acts on DNA gyrase, an enzyme which, like human topoisomerase, prevents the excessive supercoiling of DNA during replication or transcription.
Pharmacology
Ofloxacin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Ofloxacin is a quinolone/fluoroquinolone antibiotic. Ofloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Ofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.
Metabolism
Ofloxacin¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)
Protein Binding
Ofloxacin¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 32%
Half-life
Ofloxacin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 9 hours
Absorption
Ofloxacin¿¡ ´ëÇÑ Absorption Á¤º¸ Bioavailability of ofloxacin in the tablet formulation is approximately 98%
Pharmacokinetics
OfloxacinÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
Èí¼ö : Àß Èí¼öµÈ´Ù. À½½Ä¹°¿¡ ÀÇÇÑ ¿µÇâÀº ¹Ì¹ÌÇÏ´Ù.
ºÐÆ÷ : ºÐÆ÷¿ëÀû : 2.4-3.5 L/kg
´Ü¹é°áÇÕ : 20%
¹Ý°¨±â : 5-7.5 ½Ã°£
¼Ò½Ç : ÁÖ·Î ¹Ìº¯Èü·Î ½Å¹è¼³
Biotransformation
Ofloxacin¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic
Toxicity
Ofloxacin¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50 =5450 mg/kg (orally in mice)
Drug Interactions
Ofloxacin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Aluminium Formation of non-absorbable complexesBismuth Formation of non-absorbable complexesCalcium Formation of non-absorbable complexesIron Formation of non-absorbable complexesMagnesium oxide Formation of non-absorbable complexesMagnesium Formation of non-absorbable complexesSucralfate Formation of non-absorbable complexesZinc Formation of non-absorbable complexesWarfarin The quinolone increases the anticoagulant effectAcenocoumarol The quinolone increases the anticoagulant effectDicumarol The quinolone increases the anticoagulant effectAnisindione The quinolone increases the anticoagulant effectDihydroquinidine barbiturate Increased risk of cardiotoxicity and arrhythmiasQuinidine Increased risk of cardiotoxicity and arrhythmiasQuinidine barbiturate Increased risk of cardiotoxicity and arrhythmiasFoscarnet Increased risk of convulsionsProcainamide The quinolone increases the effect of procainamide
CYP450 Drug Interaction
[CYP450 TableÁ÷Á¢Á¶È¸]
Food Interaction
Ofloxacin¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Avoid high doses of caffeine.
Drug Target
[Drug Target]
Description
Ofloxacin¿¡ ´ëÇÑ Description Á¤º¸ A synthetic fluoroquinolone (fluoroquinolones) antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. [PubChem]
Drug Category
Ofloxacin¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Bacterial AgentsAnti-Infective Agents, UrinaryAnti-InfectivesNucleic Acid Synthesis InhibitorsQuinolones
Smiles String Canonical
Ofloxacin¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC1COC2=C3N1C=C(C(O)=O)C(=O)C3=CC(F)=C2N1CCN(C)CC1
Smiles String Isomeric
Ofloxacin¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ C[C@H]1COC2=C3N1C=C(C(O)=O)C(=O)C3=CC(F)=C2N1CCN(C)CC1
InChI Identifier
Ofloxacin¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C18H20FN3O4/c1-10-9-26-17-14-11(16(23)12(18(24)25)8-22(10)14)7-13(19)15(17)21-5-3-20(2)4-6-21/h7-8,10H,3-6,9H2,1-2H3,(H,24,25)/f/h24H
Chemical IUPAC Name
Ofloxacin¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (+/-)-9-fluoro-2, 3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1, 2, 3-de]-1, 4-benzoxazine-6-carboxylic acid
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