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

Paper Mentions

Interventional Clinical Trial
The investigators will examine the effectiveness of non-opioid analgesia (Paracetamol versus Ibuprofen) in the early postpartum period  
ConditionsPain
InterventionDrug
Interventional Clinical Trial
This is a single centre, randomised, double-blind, double-dummy, parallel group, multiple-dose, active and placebo-controlled efficacy study to evaluate the efficacy and safety… Expand
ConditionsPain
InterventionDrug, Other
Enantioselective Pharmacokinetics of Ibuprofen and Involved Mechanisms
TLDR
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
Stereoselectivity of ibuprofen metabolism and pharmacokinetics following the administration of the racemate to healthy volunteers
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
TLDR
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
TLDR
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
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 297 REFERENCES
Clinical Pharmacokinetics of Tiaprofenic Acid and its Enantiomers
  • N. Davies
  • Chemistry, Medicine
  • Clinical pharmacokinetics
  • 1996
TLDR
The synovium is the proposed site of action of NSAIDs when used for musculoskeletal disorders, and substantial concentrations of tiaprofenic acid are attained in synovial fluid, and recent data suggest the possibility of stereoselective distribution of tiapsic acid intosynovium and cartilage. Expand
Clinical Pharmacokinetics of Flurbiprofen and its Enantiomers
  • N. Davies
  • Chemistry, Medicine
  • Clinical pharmacokinetics
  • 1995
TLDR
Flurbiprofen binds extensively to plasma albumin, apparently in a stereoselective manner, and substantial concentrations of the drug are attained in synovial fluid, which is the proposed site of action of NSAIDs. Expand
Etodolac Clinical Pharmacokinetics
TLDR
In elderly nonarthritic individuals with excellent kidney function, aging does not affect the pharmacokinetics of etodolac, and may be important because the acyl-glucuronides are renally cleared. Expand
Clinical Pharmacokinetics of Ketoprofen and Its Enantiomers
TLDR
There appears to be circadian variation, particularly in the absorption of ketoprofen, and the relationship between concentration and anti-inflammatory effect has yet to be elucidated for this drug. Expand
The relationship between the pharmacokinetics of ibuprofen enantiomers and the dose of racemic ibuprofen in humans.
TLDR
It was predicted that the metabolic intrinsic clearance of each enantiomer, and the fraction of R(-)-ib uprofen which was metabolically inverted to S(+)-ibuprofen, was independent of the administered dose. Expand
Clinical Pharmacokinetics of Naproxen
TLDR
Naproxen is a stereochemically pure nonsteroidal anti-inflammatory drug of the 2-arylpropionic acid class and relationships between the total and unbound plasma concentration, unbound synovial fluid concentration and therapeutic effect have been established. Expand
Stereoselective disposition of ibuprofen and flurbiprofen in rats.
TLDR
The pharmacokinetics of the ibuprofen and flurbiprofen enantiomers were evaluated using a two-compartment open model with conversion of the R- to S-enantiomers in the central compartment and there was a small amount of inversion of (R)-ib uprofen as determined by area analysis. Expand
Variability in the Disposition of Ibuprofen Enantiomers in Osteoarthritis Patients
TLDR
The pharmacokinetics of the enantiomers of ibuprofen have been investigated following oral administration of 300 or 600 mg of racemic ib uprofen four times daily to 45 patients with osteoarthritis, implying that patients would receive similar effective doses of active S-ibuproen in spite of large differences in kinetics. Expand
Clinical Pharmacokinetics of Ketorolac Tromethamine
TLDR
Ketorolac is a new chiral nonsteroidal anti-inflammatory drug (NSAID) which is marketed for analgesia as the racemate and has a volume of distribution comparable with those of other NSAIDs. Expand
Rapid HPLC-determination of ibuprofen and flurbiprofen in plasma for therapeutic drug control and pharmacokinetic applications.
TLDR
The applicability of the HPLC-method was demonstrated in a pharmacokinetic ibuprofen experiment in an adult person and it was demonstrated that the drug is still being investigated regarding its possible ability to reduce myocardial infarct size. Expand
...
1
2
3
4
5
...