Actions of Dexketonal in details
Pharmacology: Mechanism of Action: The mechanism of action of NSAIDs is related to the reduction of prostaglandin synthesis by the inhibition of cyclooxygenase pathway. Dexketonal has been demonstrated to be an inhibitor for COX-1 and COX-2 activities in experimental animals and humans. Specifically, there is an inhibition of the transformation of arachidonic acid into cyclic endoperoxides, PGG2 and PGH2, which produce prostaglandins PGE1, PGE2, PGF2α and PGD2 and also prostacyclin PGI2, and thromboxanes (TxA2 and TxB2). Inhibition of the synthesis of prostaglandins may also affect other inflammatory mediators like kinins which is an indirect action. Clinical studies performed on several pain models demonstrated effective analgesic activity of Dexketonal trometamol. The onset of the analgesic activity was obtained in some studies at 30 min post-administration. The analgesic effect persists for 4-6 hrs.
Pharmacokinetics: After oral administration of Dexketonal trometamol to humans, the peak plasma concentration-time curve (Cmax) is reached at 30 min (range 15-60 min). When administered concomitantly with food, the AUC does not change, however the Cmax of Dexketonal trometamol decreases and its absorption rate is delayed (increased Tmax). The distribution half-life (t½) and elimination t½ values of Dexketonal trometamol are 0.35 and 1.65 hrs, respectively. As with other drugs with a high plasma protein-binding (99%), its volume of distribution has a mean value <0.25 L/kg. The main elimination route for Dexketonal is glucuronide conjugation followed by renal excretion. There is no conversion of Dexketonal to the R-(-) enantiomer in humans. Dexketonal does not accumulate after multiple doses in humans.
Dexketonal administration
Should be taken on an empty stomach. Take 30 min before meals, esp for quick relief of acute pain.
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Information checked by Dr. Sachin Kumar, MD Pharmacology
