Using pharmacokinetic principles to optimize pain therapy

Publikation: Beitrag in FachzeitschriftÜbersichtsartikel (Review)BeigetragenBegutachtung

Beitragende

Abstract

Cyclo-oxygenase (COX) inhibitors are widely used to relieve musculoskeletal pain. These agents block the production of prostaglandins (PGs) at sites of inflammation by inhibiting the activity of two COX enzymes necessary for PG production and normal organ homeostasis. Inhibition of PG production at sites unrelated to pain is associated with adverse drug reactions (ADRs). The degree of analgesic efficacy, as well as the incidence and the localization of ADRs, are critically influenced by the pharmacokinetics (absorption, distribution and elimination) of these drugs. Ideally, sufficient and permanent inhibition of COX enzymes should be achieved in target tissues, with minimal ADRs. To minimize underdosing or overdosing, which result in therapeutic failure or ADRs, the COX inhibitor with the most appropriate pharmacokinetic properties should be selected on the basis of a thorough pharmacokinetic-pharmacodynamic analysis. In this Review, the pharmacokinetics of the prevailing COX inhibitors will be discussed and enigmatic aspects of these intensively used drugs will be considered.

Details

OriginalspracheEnglisch
Seiten (von - bis)589-598
Seitenumfang10
FachzeitschriftNature Reviews. Rheumatology
Jahrgang6
Ausgabenummer10
PublikationsstatusVeröffentlicht - Okt. 2010
Peer-Review-StatusJa

Externe IDs

PubMed 20820196
ORCID /0000-0003-0845-6793/work/139025244

Schlagworte

ASJC Scopus Sachgebiete