Pharmacokinetics of pipemidic` acid in healthy middle-aged volunteers and elderly patients with renal insufficiency

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Abstract
1. Pipemidic acid in bacteriological screening was more potent than nalidixinic acid, notably against Pseudomonas. 2. In a study in middle-aged female volunteers, the relative bioavailability of a single 500 mg tablet of pipemidic acid was good. The main pharmacokinetic parameters were: tmax, 2.3 h; Cmax, 3.3 μg/ml; t1/2,4.6 h; Vares, 2.041/kg; Cltot 5-48 ml/min per kg; Clren, 3.05 ml/min per kg; Ae0-24, 55.7% of dose. 3. In elderly inpatients with normal renal function, the main alterations from middle-aged volunteers were: slightly elevated Cmax (+ 28%) and AUC (+ 13%) and significantly decreased Varea (-51%), Clren (-34%) and Ae0-24 (-31%). 4. In elderly inpatients with renal insufficiency, Clren (— 58%) was decreased compared with elderly inpatients with normal renal function. Concn. of pipemidic acid in urine still exceeded several-fold the MIC values of the most pathogenic bacteria. 5. Among all the subjects, there was a negative correlation between Clcreat and AUC0-∞, and a positive correlation between Clcreat and Cltot, and Ae0-24. 6. In the treatment of urinary-tract infections with pipemidic acid, a mild renal insufficiency (Clcreat 30 ml/min or more) does not necessitate dose adjustments.

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