Document Detail


Pharmacokinetic-pharmacodynamic relationships of bromfenac in mice and humans.
MedLine Citation:
PMID:  8947993     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The relationship between pharmacodynamic effect and plasma concentrations of the analgesic bromfenac was assessed retrospectively. The drug was administered in single doses of 5, 10, 25, 50, or 100 mg to patients with oral surgery pain. Concentration-effect curves were generated by a semiparametric pharmacokinetic-pharmacodynamic procedure. The bromfenac EC50 (the effect site concentration giving 50% of the maximum effect) was estimated to be 0.36 microgram/ml in patients when all five dose groups were combined, and an Emax model was used for pharmacodynamic response. A similar EC50 value, 0.40 microgram/ml, was obtained when bromfenac was tested in a mouse pain model. On the basis of combined-dose data, effect site concentrations were predicted to be above the analgesic EC50 for approximately 7-8 hours after a 50-mg bromfenac dose was taken in the fasting state. Predictions based on a pharmacokinetic-pharmacodynamic modeling procedure were in reasonable agreement with the clinical observations.
Authors:
S T Chiang; J C Ermer; M Osman; T Chau; D Hicks; S Wheeler; I Vavra
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  Pharmacotherapy     Volume:  16     ISSN:  0277-0008     ISO Abbreviation:  Pharmacotherapy     Publication Date:    1996 Nov-Dec
Date Detail:
Created Date:  1997-03-21     Completed Date:  1997-03-21     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  8111305     Medline TA:  Pharmacotherapy     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1179-87     Citation Subset:  IM    
Affiliation:
Wyeth-Ayerst Research, Princeton, New Jersey, USA.
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MeSH Terms
Descriptor/Qualifier:
Adult
Analgesics / administration & dosage*,  pharmacokinetics*
Animals
Benzophenones / administration & dosage*,  pharmacokinetics*
Biological Availability
Bromobenzenes / administration & dosage*,  pharmacokinetics*
Double-Blind Method
Fasting
Female
Food-Drug Interactions
Humans
Male
Metabolic Clearance Rate
Mice
Models, Biological
Pain / drug therapy*
Randomized Controlled Trials as Topic
Retrospective Studies
Chemical
Reg. No./Substance:
0/Analgesics; 0/Benzophenones; 0/Bromobenzenes; 91714-94-2/bromfenac

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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