Trimethoprim in Human Saliva, Bronchial Secretion and Lung Tissue

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Abstract
Following oral administration of trimethoprim (TMP) in doses varying from 4.0 to 11.2 mg TMP per kg body weight per 24 hours over a period of 1‐5 days, the concentration was determined in lung tissue (obtained by open biopsy), bronchial secretion or saliva, in a total of 51 cases. A microbiological method was used to determine the concentration, using B. pumilus as test organism. The concentrations of TMP found in the lung tissue, bronchial secretion and saliva (6‐13 hours after the last administration of TMP) were at a therapeutically active level (≥ MIC × 5) with regard to the majority of those bacteria usually occurring in respiratory tract infections. In 14 out of 17 patients, TMP was found in the lung tissue in concentrations which were 1 1/2 to 3 1/2 times higher than the corresponding serum concentration. In the other 3 patients, the concentrations found were 4 1/2 times, 7 times and 14 times higher in the lung tissue than in the serum. In the case of bronchial secretion, 6 patients showed a TMP concentration which was 1/2 to 4 times the corresponding serum concentration, while in 14 patients, an examination of the saliva showed a TMP concentration which was 1‐8 1/2 times that of the corresponding serum concentration.