Pharmacokinetics of nalidixic acid associated with sodium citrate

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Abstract
A pharmacokinetic study of sachets containing nalidixic acid (0·66 g) associated with sodium citrate (3·75 g)—NSC—was carried out in 10 healthy volunteers in order to determine the influence of the urine alcalinization due to sodium citrate on the elimination of nalidixic acid (NA) and its 7‐hydroxy (HNA) and 7‐carboxy (CNA) derivatives. Urine alcaliniztion enhanced markedly the urinery excretion of HNA, but not of NA and CNA. The urinary concentrations of bacteriologically active compounds—NA + HNA—remained above five times their minimum inhibitory concentration for 10 h following each dose. After a 3‐day treatment using NSC three times daily there was no significant accumulation of NA and derivatives in the plasma and no significant change in their kinetics. Finally, from a pharmacokinetic viewpoint, the daily administration of 3 sachets of NSC each containing 0·66 g of NA seems valuable in the treatment of urinary tract infections.