Clinical Pharmacokinetics of Probenecid
@article{Cunningham1981ClinicalPO, title={Clinical Pharmacokinetics of Probenecid}, author={R. F. Cunningham and Zafar H. Israili and Peter G. Dayton}, journal={Clinical Pharmacokinetics}, year={1981}, volume={6}, pages={135-151} }
SummaryA review of the clinical applications and of the disposition of probenecid in man, including drug interactions, is presented.Probenecid is the classical competitive inhibitor of organic acid transport in the kidney and other organs. There are 2 primary clinical uses for probenecid: as a uricosuric agent in the treatment of chronic gout and as an adjunct to enhance blood levels of antibiotics (such as penicillins and Cephalosporins). Adsorption of probenecid is essentially complete…
202 Citations
Interindividual variation in the capacity-limited renal glucuronidation of probenecid by humans
- Biology, MedicinePharmacy World and Science
- 2005
It was inferred that probenecid acyl glucuronide is formed in the kidney during blood-to-lumen passage through the tubular cells and the plateau value in the renal excretion rate-time profile reflects itsVmax of formation.
Probenecid-induced changes in the clearance of pranoprofen enantiomers.
- Medicine, BiologyChirality
- 2003
Probenecid had a slight effect on the tissue distribution of pranoprofen at the dose used, but significantly reduced the formation of glucuronide for both enantiomers to the same extent in kidney microsomes.
Effect of probenecid on the formation and elimination kinetics of the sulphate and glucuronide conjugates of diflunisal
- Biology, ChemistryEuropean Journal of Clinical Pharmacology
- 2004
Steady state plasma concentrations of the sulphate and glucuronide conjugates of diflunisal were 2.5- to 3.1-fold higher during probenecid co-administration, due to a significant reduction in the renal clearance of the three dif lunisal conjugate.
Effects of probenecid on the pharmacokinetics and elimination of acyclovir in humans
- Medicine, BiologyAntimicrobial Agents and Chemotherapy
- 1982
It is confirmed that acyclovir is eliminated predominantly by renal clearance, both by glomerular filtration and tubular secretion; the results suggested that at least part of thetubular secretion is inhibited by probenecid.
The effect of probenecid on the renal elimination of cimetidine
- Medicine, BiologyClinical pharmacology and therapeutics
- 1989
The study demonstrates that renal interactions between organic cations and organic anions can occur in human beings and the mechanism of this interaction and the implications to other drug combinations are being explored.
Probenecid: its chromatographic determination, plasma protein binding, and in vivo pharmacokinetics in dogs.
- Biology, ChemistryThe Journal of veterinary medical science
- 2006
Observation in relation to plasma protein binding and PK parameters will serve as the basic information concerning drug-drug interactions in dogs and in other mammalian species.
The effect of probenecid on the renal tubular excretion of benzylpenicillin.
- Medicine, ChemistryBritish journal of clinical pharmacology
- 1988
Extrapolating these results to the clinical situation, the commonly used daily dose of 2 g of probenecid is likely to be close to the maximal effective dose for inhibition of the tubular excretion of benzylpenicillin.
Effect of probenecid on the pharmacokinetics of cefmenoxime
- Medicine, BiologyAntimicrobial Agents and Chemotherapy
- 1983
Tubular secretion is the predominant mechanism of clearance for cefmenoxime and that probenecid alters the pharmacokinetics of the compound by competitively inhibiting its tubular secretion without affecting either the rate or the extent of its distribution.
Pharmacology of drugs for hyperuricemia. Mechanisms, kinetics and interactions.
- Biology, MedicineContributions to nephrology
- 2005
Rasburicase probably undergoes peptide hydrolysis and in in vitro studies was shown neither to inhibit or induce cytochrome P450 isoenzymes nor to interact with several drugs, so that no relevant interaction is expected during cotreatment in patients.
Capacity-limited renal glucuronidation of probenecid by humans
- Medicine, BiologyPharmaceutisch Weekblad
- 2005
Probenecid shows dose-dependent pharmacokinetics and it is demonstrated that probenecid glucuronide must be formed in the kidney during its passage of the tubule, and the plateau value in the renal excretion rate-time profile shows itsVmax of formation.
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