Clinical Pharmacokinetics of Ibuprofen

@article{Davies1998ClinicalPO,
  title={Clinical Pharmacokinetics of Ibuprofen},
  author={Neal M Davies},
  journal={Clinical Pharmacokinetics},
  year={1998},
  volume={34},
  pages={101-154}
}
  • N. Davies
  • Published 1998
  • Chemistry, Medicine
  • Clinical Pharmacokinetics
Ibuprofen is a chiral nonsteroidal anti-inflammatory drug (NSAID) of the 2 arylpropionic acid (2-APA) class. A common structural feature of 2-APA NSAIDs is a sp3-hybridised tetrahedral chiral carbon atom within the propionic acid side chain moiety with the S-(+)-enantiomer possessing most of the beneficial anti-inflammatory activity. Ibuprofen demonstrates marked stereoselectivity in its pharmacokinetics. Substantial unidirectional inversion of the R-(−) to the S-(+) enantiomer occurs and thus… Expand
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Highly Influential Citations
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240 Citations

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Citation Type

Enantioselective Pharmacokinetics of Ibuprofen and Involved Mechanisms
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The chiral pharmacokinetics and involved mechanisms of ibuprofen in comparison with other NSAIDs based on recent developments are examined to provide better understanding and prediction of other chiral drugs. Expand
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TLDR
The stereoselective metabolism and pharmacokinetics of the enantiomers of ibuprofen have been investigated following the oral administration of the racemic drug to 12 healthy volunteers and analysis of the stereochemical composition of the urinary excretion products indicated that 68% of the dose of (R) -ib uprofen had undergone chiral inversion. Expand
Pharmacokinetic interaction of ibuprofen enantiomers in rabbits
TLDR
The enantiomeric interaction in the pharmacokinetic behaviour of ibuprofen after racemic administration is considered to be a result of an alteration in the metabolic or excretion phase (or both) rather than stereoselective protein binding in the systemic distribution. Expand
Clinical Pharmacokinetics of Oxaprozin
  • N. Davies
  • Chemistry, Medicine
  • Clinical pharmacokinetics
  • 1998
TLDR
After administration of multiple doses, the apparent oral clearance and volume of distribution of total oxaprozin increased while those of the unbound drug decreased significantly, and patients with renal impairment demonstrate an increase in unbound plasma concentrations of oxAProzin. Expand
Solubility of ( ± )-Ibuprofen and S ( + )-Ibuprofen in the Presence of Cosolvents and Cyclodextrins
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Of the two compounds studied, higher equilibrium solubilities were observed for SIB as compared with racIB, and the solubilization process is discussed in terms of solvent polarity and differential solid-state structure of racIB and SIB. Expand
Sila-Ibuprofen.
TLDR
The synthesis, characterization, biological activity and toxicology of sila-ibuprofen, a silicon derivative of the most common non-steroidal anti-inflammatory drug, is reported and the understanding of the mechanism of action of the inhibition process is improved. Expand
Comparative study of anti-inflammatory, ulcerogenic and cytotoxic activities of racemate and S-ibuprofen
TLDR
The present findings suggest that the S-enantiomer of ibuprofen could be considered a therapeutic alternative to minimize gastrointestinal side effects, since the chiral inversion of R(-)-ib uprofen to S(+)-ibuprofeno did not result in an improved anti-inflammatory response. Expand
Pharmacology Review: Intravenous Ibuprofen for Preterm Newborns
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This review examines the published data on ibuprofen up to June 2005 and concludes that ib uprofen lysine is a safe and effective drug for PDA closure in newborns. Expand
Pharmacologic, pharmacodynamic, and pharmacokinetic considerations with intravenous Ibuprofen lysine.
  • E. Capparelli
  • Medicine
  • The journal of pediatric pharmacology and therapeutics : JPPT : the official journal of PPAG
  • 2007
TLDR
IV ibuprofen lysine is a COX inhibitor that demonstrates similar efficacy to indomethacin with few adverse effects and is a safe, effective pharmacologic agent to promote closure of PDAs in preterm infants. Expand
Influence of age on the enantiomeric disposition of ibuprofen in healthy volunteers.
TLDR
The elderly have an increased exposure to the active ibuprofen enantiomer and thus some caution may be required when using this drug in this age group, with the elderly having increased free concentrations and lower unbound clearance of the S-enantiomer in comparison with the young. Expand
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