Uses and Toxicity of Oxolinic acid

Oxolinic acid is a quinolone antibiotic developed in Japan in the 1970s.It also acts as a dopamine reuptake inhibitor and has stimulant effects in mice.Dosages 12–20 mg/kg orally administered for five to ten days. The antibiotic works by inhibiting the enzyme DNA gyrase. 

Structure

A quinolinemonocarboxylic acid having the carboxy group at position 7 as well as oxo and ethyl groups at positions 4 and 1 respectively and a dioxolo ring fused at the 5- and 6-positions. A synthetic antibiotic, it is used in veterinary medicine for the treatment of bacterial infections in cattle, pigs and poultry.

Uses

Oxolinic acid has been used in human medicine in several countries in the past. Its use in human medicine has largely been replaced by the fluoroquinolone antibiotics.

Metabolise

In humans, oxolinic acid was metabolised to at least 8 urinary metabolites. At least 2 metaboliteshad microbiological activity. The radioactivity of urine collected 0 to 6 hours after an oral dose of1g ¹⁴C-oxolinic acid consisted of 43% oxolinic acid glucuronide, 1.4% of a labile complex of oxolinic acid, 37.5% of glucuronides derived from oxolinic acid metabolites and 18% non-glucuronide metabolites.

Toxicity

Oxolinic acid was of low acute toxicity to adult animals. Acute oral LDs0 values in adult mice ranged from 1890 to more than 6000 mgkg bw. It was more acutely toxic to neonatal animals with acute oral LDso values in the range from 128 mg/kg bw (mice) to 573 mg/kg bw (rat).