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[Evaluation of the biliary excretion of penicillin G. (author's transl)]
Abstract:
Biliary excretion of penicillin G was studied experimentally by perfusion of isolated rabbit liver. Under these conditions, bile recovery accounted for 5% of the amount of penicillin G added to the perfusing blood (10 mg); peak biliary level averaged 135.3 micrograms/ml. In man after intravenous administration of a 599 mg dose of penicillin G (1 MU) to patients provided with T-tube drainage (n = 10), the maximum biliary concentration averaged 18.0 +/- 8.0 micrograms/ml at 2 hours; biliary recovery of penicillin G accounts for 0.12% of the administered dose. The excretion of penicillin G in the juice collected through duodenal tubing in normal subjects averaged 0.07% of the administered dose (599 mg IV). Per-operative assays showed that the concentration determined at 1 hour after intravenous administration of the drug (599 mg) in the gallbladder bile (45.7 +/- 16.7 micrograms/ml) and common duct bile (93.5 +/- 16.3 micrograms/ml) were definitely higher (4.5--9 times) than the serum levels measured simultaneously. The biliary excretion of penicillin G is compared with the biliary elimination of a certain number of beta-lactam derivatives studied under the same conditions (ampicillin, metampicillin, carbenicillin, cefalothin, cefaloridine, cefacetrile, cefalexin, cefazolin).
Insights
Penicillin G shows significant biliary excretion in rabbits and humans, with higher concentrations in bile than serum after intravenous administration. This study quantifies penicillin G
Area of Science:
- Pharmacokinetics
- Drug Metabolism
- Biliary Physiology
Context:
- Biliary excretion is a key elimination route for many drugs.
- Understanding drug concentrations in bile is crucial for managing potential hepatotoxicity and optimizing dosing.
- Penicillin G's biliary elimination has been less characterized compared to other beta-lactam antibiotics.
Purpose:
- To investigate and quantify the biliary excretion of penicillin G in experimental animal models and human subjects.
- To compare the biliary elimination of penicillin G with other related beta-lactam antibiotics.
- To determine the relationship between serum and biliary concentrations of penicillin G.
Summary:
- Penicillin G undergoes significant biliary excretion, with experimental rabbit liver perfusion showing 5% recovery.
- In humans, intravenous penicillin G administration resulted in peak biliary concentrations of 18.0 µg/ml, with 0.12% of the dose recovered in bile.
- Bile concentrations of penicillin G were notably higher (4.5-9 times) than simultaneous serum levels, particularly in gallbladder and common duct bile.
Impact:
- Provides quantitative data on penicillin G's biliary excretion in humans and animals.
- Offers comparative insights into the biliary elimination of various beta-lactam antibiotics.
- Informs clinical practice regarding penicillin G dosing and potential biliary-related side effects.