Article date: August 1991
By: DJ Nichols, A Bye, E Novak, in Volume 32, Issue 2, pages 255-257
The pharmacokinetics of trospectomycin (75‐1000 mg free base equivalents) were studied in 128 healthy males (eight per dose group), after a 20 min intravenous (i.v.) infusion and intramuscular (i.m.) injection of trospectomycin sulphate. The concentrations of trospectomycin in serum were described by bi‐ or tri‐exponential disposition functions indicating an initial half‐life of 1.1‐1.4 h for the i.v. dose and 1.6‐2.1 h for the i.m. dose and terminal half‐lives of over 15 h. Most of the drug was eliminated rapidly (mean residence time 5‐12 h). The distribution volume was 59‐112% of body weight and clearance was 112‐152 ml min‐1. The absorption into blood after i.m. dosing was rapid. The area under the concentration‐time curve and maximum concentration values were linearly related to dose. Serum drug concentrations fell below the minimum inhibitory concentration values for a variety of organisms by 8‐12 h, which indicates that two or three times daily dosing would be appropriate. However, the long terminal half‐life suggests that significant accumulation is likely in some tissues with an 8 h dose interval and this may prolong the action of trospectomycin.
DOI: 10.1111/j.1365-2125.1991.tb03893.x
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