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Biliary elimination of mezlocillin: an experimental and clinical study
Abstract:
The biliary elimination of mezlocillin, a new semisynthetic penicillin of the acyl-ureido-penicillin group, was investigated in vitro in rabbit liver preparations and in vivo in humans. Experimentally, mezlocillin recovery in the bile during perfusion of isolted rabbit liver (3 h; n = 5) averaged 20.3% of the administrered dose (10 mg). The mean peak concentration in the bile (758 +/- 129.3 micrograms/ml) was reached between 0.5 and 1 h. Biliary clearance was 169 ml/h. In healthy subjects (n = 5), the concentrations of antibiotic measured in the duodenal fluid during a period of 4 h after intravenous administration of 5 g of mezlocillin ranged between 440 and 637 micrograms/ml. In 10 cholecystectomized patients provided with a T-tube, intramuscular injection of 1 g of mezlocillin resulted in a biliary peak concentration of 295.7 +/- 58.1 micrograms/ml. Mean total amount of antibiotic eliminated in the bile over 12 h corresponded to 2.6% of the administered dose. Assays performed during surgery after intravenous administration of 2 g of mezlocillin (n = 10) showed antibiotic activity of 895 +/- 196 micrograms/ml in the common duct bile and 402 +/- 133 micrograms/ml in the gallbladder bile. These data were compared with the values determined for 11 other beta-lactamines studied under identical conditions.
Insights
Mezlocillin, a semisynthetic penicillin, showed significant biliary elimination in rabbits and humans. This antibiotic
Area of Science:
- Pharmacology
- Hepatobiliary System
- Antibiotic Research
Background:
- Mezlocillin is a semisynthetic penicillin from the acyl-ureido-penicillin group.
- Understanding drug elimination pathways is crucial for optimizing therapeutic use.
Purpose of the Study:
- To investigate the biliary elimination of mezlocillin.
- To compare mezlocillin's biliary excretion with other beta-lactam antibiotics.
Main Methods:
- In vitro studies using isolated rabbit liver preparations.
- In vivo studies in healthy human subjects and patients with T-tubes.
- Assays of antibiotic concentrations in bile and duodenal fluid.
Main Results:
- Rabbit liver preparations showed 20.3% mezlocillin recovery in bile within 3 hours.
- Peak human biliary concentrations ranged from 295.7 to 895 mcg/ml depending on administration route and patient group.
- Total biliary elimination in humans averaged 2.6% of the administered dose over 12 hours.
Conclusions:
- Mezlocillin undergoes significant biliary excretion.
- Biliary concentrations suggest potential clinical relevance in hepatobiliary infections.
- Further comparison with other beta-lactams is warranted.