Effect of pefloxacin on the urinary excretion of rifampicin.

The effect of pefloxacin on the urinary excretion of rifampicin was investigated in 5 healthy volunteers between the ages of 20 and 35 years. The investigation was carried out in 2 different phases, with a 1-week drug washout separating the phases. Each subject received 600 mg rifampicin with 350 mL of water. After 1 week, the subjects were given 600 mg rifampicin plus 500 mg pefloxacin with 350 mL of water. Urinary levels of rifampicin were measured spectrophotometrically for the 2 phases from 0 to 72 hours. Coadministration of rifampicin with pefloxacin led to 20.1% urinary recovery of rifampicin. The increased rifampicin excretion rate following pefloxacin coadministration is supported by the competitive liver clearance between rifampicin and pefloxacin, which favors pefloxacin and causes rifampicin secretion, thus increasing its elimination through the kidney. Pefloxacin increases the absorption and urinary excretion of rifampicin by decreasing the gastrointestinal motility through chelation mechanisms.

Salivary and urinary excretion and plasma-saliva concentration ratios of isoniazid in the presence of Co-administered ciprofloxacin.

Salivary and urinary excretion and plasma-saliva concentration ratios of isoniazid (INH) in the absence and presence of ciprofloxacin (CP) were investigated in healthy female volunteers. Results obtained indicated an absorption form of interaction between INH and CP. This led to delay in gastric emptying and onset of absorption of INH in the upper part of the gastrointestinal tract, resulting in a corresponding delay in the onset of salivary and urinary excretion of the drugs. There was a 1-hour reduction in the time to attain peak saliva concentration of INH (tmax), an insignificant difference in peak saliva concentration (Cmax), and a significant (P = 0.05) increase in AUC(0-24h) of INH in the presence of CP. Cumulative amount of INH excreted in the urine increased approximately 38% in the presence of CP. The calculated plasma-saliva concentration ratios of INH were reduced in the presence of CP and were slightly lower than the experimental values. This indicates increased amount of the drug secreted into saliva in the presence of CP and possible buccal partitioning of the drug. Overall, results of the current study indicate that CP delayed the onset but not the extent of INH absorption. Therefore, concurrent administration of the two drugs was considered relatively safe, and the absorption interaction that may have occurred may not be of reasonable clinical consequence.