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Ofloxacin


ACCESSION NB: DB01165 (APRD00502)


TYPE: small molecule


GROUP: approved


DESCRIPTION:
A synthetic fluoroquinolone (fluoroquinolones) antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. [PubChem]

VOLUME OF DISTRIBUTION: Not Available

CATEGORIES:
Anti-Infectives Anti-Bacterial Agents, Quinolones, Nucleic Acid Synthesis Inhibitors, Anti-Infective Agents, Urinary

ABSORPTION: Bioavailability of ofloxacin in the tablet formulation is approximately 98%

INDICATION:
For the treatment of infections (respiratory tract, kidney, skin, soft tissue, UTI), urethral and cervical gonorrhoea.

PHARMACODYNAMICS:
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.

MECHANISM OF ACTION:
Ofloxacin acts on DNA gyrase and toposiomerase IV, enzymes which, like human topoisomerase, prevents the excessive supercoiling of DNA during replication or transcription. By inhibiting their function, the drug thereby inhibits normal cell division.

PROTEIN BINDING:
32%

METABOLISM:
Hepatic

TOXICITY:
LD50=5450 mg/kg (orally in mice)

AFECTED ORGANISMS:
Enteric bacteria and other eubacteria