Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
320.128468635
InChI
InChI=1S/C15H17FN4O3/c1-2-19-8-10(15(22)23)12(21)9-7-11(16)14(18-13(9)19)20-5-3-17-4-6-20/h7-8,17H,2-6H2,1H3,(H,22,23)
InChI Key
InChIKey=IDYZIJYBMGIQMJ-UHFFFAOYSA-N
IUPAC Name
1-ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
Traditional IUPAC Name
enoxacin
SMILES
CCN1C=C(C(O)=O)C(=O)C2=CC(F)=C(N=C12)N1CCNCC1
pKa (strongest acidic)
5.5
pKa (Strongest Basic)
8.59
Refractivity
83.95 m3·mol-1
Dược Lực Học :
Enoxacin is a quinolone/fluoroquinolone antibiotic. Enoxacin 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. Enoxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. Enoxacin may be active against pathogens resistant to drugs that act by different mechanisms.
Cơ Chế Tác Dụng :
A broad-spectrum 6-fluoronaphthyridinone antibacterial agent (fluoroquinolones) structurally related to nalidixic acid. [PubChem]
Enoxacin exerts its bactericidal action via the inhibition of the essential bacterial enzyme DNA gyrase (DNA Topoisomerase II).
Dược Động Học :
▧ Absorption :
Rapidly absorbed following oral administration, with an absolute oral bioavailability of approximately 90%.
▧ Protein binding :
Enoxacin is approximately 40% bound to plasma proteins in healthy subjects and is approximately 14% bound to plasma proteins in patients with impaired renal function.
▧ Metabolism :
Hepatic. Some isozymes of the cytochrome P-450 hepatic microsomal enzyme system are inhibited by enoxacin. After a single dose, greater than 40% was recovered in urine by 48 hours as unchanged drug.
▧ Half Life :
Plasma half-life is 3 to 6 hours.
Chỉ Định :
For the treatment of adults (≥18 years of age) with the following infections caused by susceptible strains of the designated microorganisms: (1) uncomplicated urethral or cervical gonorrhea due to Neisseria gonorrhoeae, (2) uncomplicated urinary tract infections (cystitis) due to Escherichia coli, Staphylococcus epidermidis, or Staphylococcus saprophyticus, and (3) complicated urinary tract infections due to Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Staphylococcus epidermidis, or Enterobacter cloacae.
Tương Tác Thuốc :
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Aminophylline
Enoxacin may increase the effect of aminophylline.
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Calcium
Formation of non-absorbable complexes
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Cimetidine
Cimetidine may decrease the absorption of enoxacin.
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Eltrombopag
Affects hepatic enzyme CYP1A2 metabolism and may increase the level of eltrombopag.
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Esomeprazole
Esomeprazole may decrease the absorption of enoxacin.
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Famotidine
Famotidine may decrease the absorption of enoxacin.
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Iron Dextran
Formation of non-absorbable complexes
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Lansoprazole
Lansoprazole may decrease the absorption of enoxacin.
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Magnesium
Formation of non-absorbable complexes
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Nizatidine
Nizatidine may decrease the absorption of enoxacin.
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Omeprazole
Omeprazole may decrease the absorption of enoxacin.
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Oxtriphylline
Enoxacin may increase the effect of oxtriphylline.
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Pantoprazole
Pantoprazole may decrease the absorption of enoxacin.
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Rabeprazole
Rabeprazole may decrease the absorption of enoxacin.
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Ramelteon
Enoxacin increases levels/toxicity of ramelteon
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Theophylline
Enoxacin may increase the effect of theophylline.
Liều Lượng & Cách Dùng :
Tablet, film coated - Oral
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