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Levofloxacin


ACCESSION NB: DB01137 (APRD00477)


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

ABSORPTION: Absorption of ofloxacin after single or multiple doses of 200 to 400 mg is predictable, and the amount of drug absorbed increases proportionately with the dose.

INDICATION:
For the treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms: Corynebacterium species, Staphylococus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus (Groups C/F/G), Viridans group streptococci, Acinetobacter lwoffii, Haemophilus influenzae, Serratia marcescens.

PHARMACODYNAMICS:
Levofloxacin, a fluoroquinolone antiinfective, is the optically active L-isomer of ofloxacin. Levofloxacin is used to treat bacterial conjunctivitis, sinusitis, chronic bronchitis, community-acquired pneumonia and pneumonia caused by penicillin-resistant strains of Streptococcus pneumoniae, skin and skin structure infections, complicated urinary tract infections and acute pyelonephritis.

MECHANISM OF ACTION:
Levofloxacin inhibits bacterial type II topoisomerases, topoisomerase IV and DNA gyrase. Levofloxacin, like other fluoroquinolones, inhibits the A subunits of DNA gyrase, two subunits encoded by the gyrA gene. This results in strand breakage on a bacterial chromosome, supercoiling, and resealing; DNA replication and transcription is inhibited.

PROTEIN BINDING:
24-38% (to plasma proteins)

METABOLISM:
Mainly excreted as unchanged drug (87%); undergoes limited metabolism in humans.

TOXICITY:
Side effects include disorientation, dizziness, drowsiness, hot and cold flashes, nausea, slurring of speech, swelling and numbness in the face

AFECTED ORGANISMS:
Enteric bacteria and other eubacteria