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Dexketoprofen
General information
See also Non-steroidal anti-inflammatory drugs (NSAIDs)
Dexketoprofen is the dextrorotatory stereoisomer of ketoprofen. The analgesic effect of ketoprofen is due to the S(+)-enantiomer (dexketoprofen), while the R(−)-enantiomer has no analgesic activity [ ] but may be ulcerogenic [ ]. Thus, dexketoprofen should produce equivalent analgesia to twice the dose of ketoprofen, but with less risk of gastrointestinal damage.
Pharmacokinetics
Dexketoprofen is formulated as the water-soluble salt dexketoprofen trometamol, to improve its absorption [ ]. The systemic availability of oral dexketoprofen trometamol (12.5 and 25 mg) is similar to that of oral racemic ketoprofen (25 and 50 mg respectively) [ ]. Dexketoprofen trometamol is rapidly absorbed, with a t max of 0.25–0.75 hours compared with a t max of 0.5–3 hours for the S-enantiomer after the racemic drug. Of the administered dose 70–80% is recovered in the urine during the first 12 hours, mainly as the acyl-glucuronidated parent drug. R-ketoprofen is not found in the urine after administration of dexketoprofen, confirming the absence of stereoisomeric interconversion in vivo.
Drug studies
Comparative studies
Dexketoprofen and diclofenac
In a randomized, double-blind, parallel, active controlled, multicenter study in 370 out-patients with acute low back pain intramuscular dexketoprofen 25 or 50 mg bd was compared with intramuscular diclofenac 75 mg bd for 2 days [ ]. Five patients withdrew from the study because of adverse events (two who took dexketoprofen 25 mg, one who took dexketoprofen 50 mg, and two who took metamizole). Injections site reactions were common with dexketoprofen (19 patients in all, 9.3%) and did not occur with metamizole. Gastrointestinal disorders (abdominal pain, constipation, dyspepsia, nausea, vomiting, and dry mouth) occurred in 11 patients (5.4%). Otherwise adverse effects were uncommon and similar in the three groups. There were 10 serious adverse events in those who were given dexketoprofen; most were recurrences of renal pain and none was considered to be drug-related.
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