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Grepafloxacin


ACCESSION NB: DB00365 (APRD01003)


TYPE: small molecule


GROUP: approved, withdrawn


DESCRIPTION:
Grepafloxacin hydrochloride (Raxar®, Glaxo Wellcome) is an oral broad-spectrum quinoline antibacterial agent used to treat bacterial infections. Grepafloxacin was withdrawn in the United States due to its side effect of lengthening the QT interval on the electrocardiogram, leading to cardiac events and sudden death. [Wikipedia]

VOLUME OF DISTRIBUTION: Not Available

CATEGORIES:
Anti-Infectives Anti-Bacterial Agents Quinolones Antibiotics

ABSORPTION: Rapidly and extensively absorbed following oral administration. The absolute bioavailability is approximately 70%.

INDICATION:
For treatment of adults with mild to moderate infections caused by susceptible strains of Haemophilus influenzae, Streptococcus pneumoniae, or Moraxella catarrhalis.

PHARMACODYNAMICS:
Grepafloxacin has in vitro activity against a wide range of gram-positive and gram-negative aerobic microorganisms, as well as some atypical microorganisms.

MECHANISM OF ACTION:
Grepafloxacin exerts its antibacterial activity by inhibiting bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, essential enzymes for duplication, transcription, and repair of bacterial DNA.

PROTEIN BINDING:
50%

METABOLISM:
Primarily hepatic via CYP1A2 and CYP3A4. The major metabolite is a glucuronide conjugate; minor metabolites include sulfate conjugates and oxidative metabolites. The oxidative metabolites are formed mainly by the cytochrome P450 enzyme CYP1A2, while the cytochrome P450 enzyme CYP3A4 plays a minor role. The nonconjugated metabolites have little antimicrobial activity compared with the parent drug, and the conjugated metabolites have no antimicrobial activity

TOXICITY:
Withdrawn from the US market in 1999 due to associations with QTc prolongation and adverse cardiovascular events.

AFECTED ORGANISMS:
Enteric bacteria and other eubacteria