The Biliary Excretion of Cephalothin

Abstract

The biliary excretion of cephalothin has been studied both by perfusion of isolated rabbit livers and during biliary drainage in the human. In the perfused rabbit liver, cephalothin added to the circulating blood is partly eliminated in the bile where the antibiotic activity is similar to that of the serum. Following a single injection of 1g to 10 cholecystectomized patients, the maximal concentration in the bile collected by external drainage reached after 1–3 h an average of 15.5μg/ml. Simultaneous determinations showed higher levels of cephalothin concentration in the gallbladder bile than in the common duct bile. In two patients with impaired renal function, cephalothin concentration in bile obtained by duodenal drainage was found to be more elevated than in five normal subjects. Biliary elimination of cephalothin appears to be sufficient to justify the use of this antibiotic in the treatment of biliary tract infections.

Pharmacokinetics of β-Lactam Antibiotics

“…Peak levels were noted at 2 h and antimicrobial activity was judged therapeutic for 4-6 h. Gall bladder tissue levels of antimicrobial activity were variable in comparison to serum levels, but generally exceeded them. Similar results were reported by BROGARD et al (1973).…”

“…Bilary excretion is also of some importance (RAM and WATANATITTAN 1974;BROGARD et al 1973). The major metabolic product is desacety1cephalothin (Fig.…”

Biliary excretion of aztreonam in patients with biliary tract disease

“…Agents such as cephalothin (11) and cephacetrile (1) are found in bile at relatively low levels (-15,ug/ml) after intramuscular or intravenous (i.v.) administration.…”

Studies on the Antibiotic Transfer into the Bile of Canines with Different Bile Duct Pressures

“…The devel opment of percutaneous transhepatic cholangiodrainage significantly decreased the mor tality rate of patients with AOC, and the first choice for the biliary infection are the cephamycins which act bactericidally, are stable against [1-lactamase, and have little nephro toxicity [6], The cephamycins have been inves tigated to determine whether they could be transferred into the bile after venous injec tion, and the experimental and clinical results prove that they can be transferred well. It has been reported, however, that an increase in bile duct pressure accompanied with a de crease of the antibiotic transfer into the bile occurred in patients who had suffered from AOC [7][8][9][10][11][12][13][14]. The correlation between bile duct pressure and transfer of antibiotics into the bile, measured in quantitative terms, should be made clear.…”