Source: Health Products Regulatory Authority (ZA) Revision Year: 2021 Publisher: LeBasi Pharmaceuticals (Pty) Ltd, San Domenico Building, Unit 6, Ground Floor, 10 Church Street, Durbanville, 7551
Category and class: A 2.7 Antipyretic or antipyretic and anti-inflammatory analgesic
Pharmacotherapeutic group: Propionic acid derivatives
ATC code: M01AE17
Dexketoprofen trometamol is the tromethamine salt of S-(+)2(3-benzoylphenyl)propionic acid, an analgesic, anti-inflammatory and antipyretic medicine, which belongs to the non-steroidal antiinflammatory group of medicines (M01AE).
Dexketoprofen has been demonstrated to be an inhibitor for COX-1 and COX-2 activities in experimental animals and humans.
Clinical studies performed on several pain models demonstrated effective analgesic activity of dexketoprofen. The onset of the analgesic activity was obtained in some studies at 30 minutes post-administration. The analgesic effect persists for 4 to 6 hours.
After oral administration of dexketoprofen trometamol to humans, the Cmax is reached at 30 min (range 15 to 60 min). When administered concomitantly with food, the AUC does not change, however the Cmax of dexketoprofen decreases and its absorption rate is delayed (increased tmax).
The distribution half-life and elimination half-life values of dexketoprofen are 0,35 and 1,65 hours, respectively. As with other medicines with a high plasma protein binding (99%), its volume of distribution has a mean value below 0,25 L/kg. In multiple-dose pharmacokinetic studies, it was observed that the AUC after the last administration is not different from that obtained following a single dose, indicating that no medicine accumulation occurs.
After administration of dexketoprofen trometamol only the S-(+) enantiomer is obtained in urine, demonstrating that no conversion to the R-(-) enantiomer occurs in humans. The main elimination route for dexketoprofen is glucuronide conjugation followed by renal excretion.
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