[Cefpiramide, a new cephalosporin with high hepatic elimination; experimental evaluation of its biliary passage and disposition in the liver].
The biliary elimination and hepatic disposition of cefpiramide were studied using an isolated and perfused rabbit liver model. Five experiments were performed, each lasting 3 hours. After addition of 10 mg of cefpiramide to the circulating blood, the biliary concentration reached a mean peak of 741 +/- 15 micrograms/ml between the 30th and 60th minute; the cumulated biliary elimination of the drug amounted 4042 +/- 1099 micrograms, corresponding to 40.4% of the injected dose. The hepato-biliary clearance was 54.5 ml/hr and the biliary elimination rate constant 0.2019(hr-1). At the end of the perfusion, 21.7% of the dose was still present in the circulating blood and 1.4% is found in the liver. Control experiments showed that 36.2% of the cefpiramide added into the experimental device was submitted to degradation. Thus, it was possible to calculate the rate of liver biotransformation of cefpiramide, which accounted for 0.3%. These experimental results confirm the major role of the liver in the elimination of cefpiramide and prove that the drug is not submitted to hepatic metabolisation.
Brogard
J M
JM
Département de Médecine Interne de la Clinique Médicale B, Centre Hospitalier Universitaire, Strasbourg.
Blickle
J F
JF
Adloff
M
M
Jehl
F
F
Monteil
H
H
D000818:Animals; D000900:Anti-Bacterial Agents / Q000493:pharmacokinetics; D001652:Bile Ducts / Q000378:metabolism*; D002511:Cephalosporins / Q000097:blood / Q000493:pharmacokinetics*; D066298:In Vitro Techniques; D008099:Liver / Q000378:metabolism*; D008657:Metabolic Clearance Rate; D011817:Rabbits
D000900:Anti-Bacterial Agents; D002511:Cephalosporins; C036666:cefpiramide
Le cefpiramide, nouvelle céphalosporine à forte élimination hépatique; évaluation expérimentale de son passage biliaire et de sa disposition au niveau du foie.