Etodolac Clinical Pharmacokinetics
@article{Brocks1994EtodolacCP, title={Etodolac Clinical Pharmacokinetics}, author={Dion R. Brocks and Fakhreddin Jamali}, journal={Clinical Pharmacokinetics}, year={1994}, volume={26}, pages={259-274} }
SummaryEtodolac is a chiral nonsteroidal anti-inflammatory drug (NSAID) that is marketed as the racemate. Currently, the drug is available in several countries for the treatment of arthritis and the alleviation of pain.Etodolac possesses several unique disposition features mainly due to its stereoselective pharmacokinetics. In plasma, the concentrations of the ‘inactive’ R-enantiomer are about 10-fold higher than those of the active S-enantiomer, an observation that is novel among the chiral…
51 Citations
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This proposed enantioselective pharmacodynamic-informed approach presents the first quantitative time-course model for COX-2 induced pain inhibition in patients.
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Data demonstrate that bioequivalence between 2 products of etodolac based on enantiomerically nonspecific criteria alone may not generalise to the pharmacologically relevant (S)-enantiomer, and suggests that enantiospecific assays are necessary for bioEquivalence assessments.
Pharmacokinetic modeling and simulation of etodolac following single oral administration in dogs
- Medicine, ChemistryXenobiotica; the fate of foreign compounds in biological systems
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Etodolac is a nonsteroidal anti-inflammatory drug with selective cyclooxygenase-2 inhibition to treat pain and inflammation associated with osteoarthritis in humans and dogs and a two-compartment pharmacokinetic model with first-order absorption and elimination rate constants was successfully explained.
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Results suggested that AA could affect drug efficacies after stereoselective changes in the pharmacokinetics of R-IB and S-IB, an animal model of inflammation.
Pharmacokinetic and Pharmacodynamic Action of Etodolac in Patients after Oral Surgery
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A single 1200 mg dose of etodolac ER given once daily was shown to provide substantial efficacy for 13 hours after dose, modest effect through 24 hours, and a more sustained duration of action than the IR dosage form.
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Pharmacokinetics of etodolac in the horse following oral and intravenous administration.
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It was showed that etodolac is well absorbed in the horse after oral administration, and may offer a useful alternative for anti-inflammatory treatment of various conditions in thehorse.
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