Comparative pharmacokinetics of ciprofloxacin and temafloxacin in humans: a review

Abstract

Temafloxacin is a new antibacterial agent of the fluoroquinolone group. In comparison with ciprofloxacin, the current leading quinolone, temafloxacin shows higher and longer lasting plasma concentrations after equivalent doses due to an almost complete gastrointestinal absorption and a lower total clearance. Temafloxacin absorption is little influenced by food intake. Concomitant administration of antacids should be avoided; a time interval of at least 2 hours should elapse between intake of either quinolone and an antacid. Both quinolones are excreted mainly by the kidney. They differ in tubular secretion, which is high for ciprofloxacin and low for temafloxacin. The overall nonrenal elimination is similar for both compounds. Ciprofloxacin has a slightly higher extent of metabolism, while temafloxacin probably has a higher transintestinal elimination. The biliary excretion of both compounds is in the same range. The longer half-life of temafloxacin enables a once-daily dose regimen, whereas the usual recommended dosage of ciprofloxacin is twice daily. For both quinolones the apparent volumes of distribution per body weight are significantly above unity, indicating good tissue penetration with intracellular uptake. The concentrations in the extracellular fluids are directly related to the corresponding plasma concentrations. The penetration of temafloxacin into the body fluids investigated--tears, nasal secretion, saliva, sweat, prostatic and seminal fluid--in general exceeds that of ciprofloxacin (with the exception of seminal fluid). Unlike ciprofloxacin, there is no drug interaction with methylxanthines. Comparative clinical studies reflecting the complex interrelating factors of host and pathogens are needed to demonstrate the significance of the pharmacokinetic differences between temafloxacin and ciprofloxacin.