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Three compartment model for pyrimethamine disposition in the pig
Journal of Veterinary Pharmacology and Therapeutics
|June 1, 1981
Summary
Pyrimethamine (Py) is extensively distributed outside the central compartment in pigs after IV administration. While 90% is excreted within 24 hours, only 3% remains unchanged in urine.
Area of Science:
- Pharmacokinetics
- Veterinary Pharmacology
- Drug Metabolism
Background:
- Pyrimethamine is an antiparasitic drug.
- Understanding its distribution and excretion is crucial for effective therapeutic use.
Purpose of the Study:
- To determine the plasma concentration and urine excretion of pyrimethamine after intravenous administration in pigs.
- To model the pharmacokinetic behavior of pyrimethamine in pigs.
Main Methods:
- Intravenous administration of pyrimethamine (10 mg/kg) to four pigs.
- Analysis of plasma and urine samples using NP-FID gas chromatography.
- Application of a three-compartment pharmacokinetic model.
Main Results:
- A three-compartment model adequately described plasma concentration data.
- Extensive extravascular distribution was observed, with a large volume of distribution ratio.
- Up to 90% of the administered dose was excreted within 24 hours, with only 3% detected as unchanged drug in urine.
Conclusions:
- Pyrimethamine undergoes significant distribution into peripheral compartments in pigs.
- The majority of pyrimethamine is eliminated within 24 hours, primarily as metabolites.