Dexibuprofen: pharmacology, therapeutic uses and safety

Abstract

Dexibuprofen is the single pharmacologically effective enantiomer of rac-ibuprofen. Racibuprofen and dexibuprofen differ in their physico-chemical properties, in terms of their pharmacological properties and their metabolic profiles. Several clinical trials and post-marketing surveillance studies were performed to broaden the findings on dexibuprofen. In the last 5 years 4836 patients have been exposed to dexibuprofen in clinical trials and PMS trials. Only in 3.7% of patients adverse drug reactions have been reported and 3 serious adverse drug reactions (0.06%) were observed. In the dose ratio of 1 : 0.5 (rac-ibuprofen vs. dexibuprofen) at least equivalent efficacy was proven in acute mild to severe somatic and visceral pain models. Dexibuprofen has proven at least comparable efficacy to diclofenac, naproxen and celecoxib and has shown a favourable tolerability. The results suggest that dexibuprofen processed in a special crystal form is a safe and effective treatment for different pain conditions.

ADIDAC Trial: Analgesia with Dexibuprofen versus Ibuprofen in Patients Suffering from Primary Dysmenorrhea: A Crossover Trial

“…The influence of concomitant diseases on the extent of inversion remains largely unexplored. Furthermore, it was shown that the metabolism of S -ibuprofen is cleaner and R -ibuprofen might contribute to adverse effects as shown in a be thanechol-induced gastric irritation model [14] . The removal of R -ibuprofen does not involve lipid metabolism and, in contrast to conventional ibuprofen, which underlies variable chiral inversion, S -ibuprofen avoids variability.…”

“…The presence of R -ibuprofen decreased the potency of S -ibuprofen much more than theoretically expected [25] . Bridging studies versus conventional ibuprofen and studies versus other NSAIDs including celecoxib confirm the good relative efficacy and tolerability profile of dexibuprofen [14,[16][17][18] . Results from clinical trials demonstrate that at a dose ratio of 0.5: 1 dexibuprofen is at least equally effective and safe as conventional ibuprofen [14,[16][17][18] .…”

“…This weak acidity results in a relatively long residence time in the acidic gastric environment, slowing its absorption. With its special crystal form, dexibuprofen possesses a 2.5-fold solubility in water and a 2.1-fold higher solubility in acidic media than conventional ibuprofen [14] . Using formulations of the S -enantiomer instead of the conventional racemate substrate could have remarkable benefits such as less xenobiotic, metabolic and renal load for the recipient.…”

“…In clinical trials and in postmarketing surveillance studies, more than 12,000 patients were treated with dexibuprofen in a special crystal form. The results of these trials show that a dose ratio of 0.5: 1 of dexibuprofen versus conventional ibuprofen provided adequate analgesia [14,[16][17][18] .…”

S-Ibuprofen Effectively Inhibits Thromboxane B₂ Levels and Platelet Function in an Experimental Model of Lipopolysaccharide-Stimulated and Non-Stimulated Whole Blood

“…Ibuprofen, a non-selective NSAID, is a racemic mixture of the S-and R-enantiomer [7] . The two enantiomers differ in terms of their pharmacological properties, and may be regarded as two individual active pharmaceutical moieties.…”