Clinical pharmacology of cefotaxime including penetration into bile, sputum, bone and cerebrospinal fluid

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Abstract
The pharmacokinetics of cefotaxime were studied in patients with normal renal function. Mean serum levels 1 h after a dose ranged from 17.3 mg/I after 0.5g i.m. to 39.6 mg/I after 2g Lv. Half-life averaged 1.37 h. Urinary levels were very high and recovery ranged from 35 to 60% of dose. Mean levels in bile from T-tube reached 14.3 mg/I after single doses of 1 g Lm. while repeated dosage produced mean levels in gallbladder bile of up to 70 mg/I. Cefotaxime was not detectable in sputum after administration of 0.5 g Lm. × 3 in exacerbations of chronic bronchitis and only after 4 days therapy with 1 g i.m × 3 it reached mean levels of 0–1 mg/l. Concentrations in cancellous bone were low after 1 g i.m. × 4, but reached 15–4 mg/l after 2 g i.m. × 3. Cefotaxime was not detectable in CSF of 15 patients with normal meninges.

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