Related Experiment Videos
Pharmacokinetics of teicoplanin
S Ripa1, L Ferrante, F Mignini
1Department of Cellular Biology, Faculty of Pharmacy, University of Camerino, Italy.
Chemotherapy
|January 1, 1988
Summary
Teicoplanin exhibits excellent bioavailability (92.4%) after intramuscular administration, with pharmacokinetic properties similar to intravenous dosing. This suggests effective absorption and distribution in healthy individuals.
Area of Science:
- Pharmacokinetics
- Clinical Pharmacology
- Drug Metabolism
Background:
- Teicoplanin is an important antibiotic for treating Gram-positive bacterial infections.
- Understanding its pharmacokinetic profile is crucial for optimizing therapeutic efficacy and safety.
Purpose of the Study:
- To characterize the pharmacokinetic properties of teicoplanin following intravenous (i.v.) and intramuscular (i.m.) administration.
- To evaluate drug absorption, distribution, metabolism, and excretion in healthy male subjects.
Main Methods:
- A three-compartment open model was utilized to analyze teicoplanin pharmacokinetics.
- Subjects received 200 mg of teicoplanin via i.v. and i.m. routes.
- Plasma levels, clearances, volume of distribution, and bioavailability were determined.
Main Results:
- Mean peak plasma teicoplanin levels were 7.16 µg/mL at 2.26 hours post-i.v. administration.
- Half-life was approximately 44-45 hours, with plasma clearance around 15.31 mL/min for both routes.
- Intramuscular bioavailability (F) was high at 92.4%, indicating near-complete absorption.
Conclusions:
- Teicoplanin demonstrates favorable pharmacokinetic properties with high bioavailability after i.m. administration.
- The drug distributes extensively, with volumes of distribution near total body water.
- Renal clearance and low unbound fraction suggest potential tubular reabsorption of teicoplanin.