Sandetofen Mechanism of Action

Pharmacology: FC tab: Dexketoprofen Trometamol is a tromethamine salt of S-(+)-2-(3-benzoylphenyl) propionic acid, which belongs to the nonsteroidal anti-inflammatory group of drugs (NSAIDs). Dexketoprofen Trometamol has pharmacologic actions similar to those of other prototypical NSAIDs. The drug exhibits anti-inflammatory, analgesic and antipyretic activity. The exact mechanisms have not been clearly established, but many of the actions appear to be associated principally with the inhibition of prostaglandin synthesis. The drug inhibits the synthesis of prostaglandins in body tissues by inhibiting cyclooxygenase; at least 2 isoenzymes, cyclooxygenase-1 (COX-1) and -2 (COX-2), have been identified that catalyze the formation of prostaglandins in the arachidonic acid pathway.
Inj: Dexketoprofen Trometamol is a tromethamine salt of S(+)-2-(3-benzoylphenyl) propionic acid, is an analgesic, anti-inflammatory and antipyretic belong to non-steroidal anti-inflammatory drugs (NSAIDs).
Mechanism of action of nonsteroidal anti-inflammatory drugs are associated with a reduction of prostaglandin synthesis by inhibition of cyclooxygenase pathway. Inhibition of the transformation of arachidonic acid into cyclic endoperoxide, PGG₂ and PGH₂, which produce prostaglandins; PGE₁, PGE₂, PGF_2α and PGD₂ and also prostacyclin PGI₂ and thromboxane (TxA₂ and TxB₂) specifically occur. Furthermore, inhibition of prostaglandin synthesis can affect other inflammatory mediators such as kinin, causing indirect action that strengthen direct action.
Pharmacokinetics: FC tab: Dexketoprofen Trometamol, given as tablet, is rapidly absorbed (90% bioavailability), with a time to maximum plasma concentration (t_max) of between 0.25 and 0.75 hours. The C_max of Dexketoprofen Trometamol in human is reached at 30 minutes (range 15 to 60 minutes).
The distribution half-life and the elimination half-life were approximately 0.35 hours and 1.65 hours, respectively. Dexketoprofen is strongly bound to plasma proteins (99%), particularly albumin. The volume of distribution has a mean value below 0.25 L/kg.
Dexketoprofen is eliminated following extensive biotransformation to inactive glucuroconjugated metabolites. No (R)-(-)-ketoprofen is found in the urine after administration of Dexketoprofen, confirming the absence of bioinversion of the (S)-(+)-enantiomer in human. Conjugates are excreted in urine, and virtually no drug is eliminated unchanged.
Dexketoprofen Trometamol did not show any accumulation phenomena after repeated doses and was well tolerated.
The profile of absorption was changed when Dexketoprofen is ingested with food, reducing both the rate of absorption (t_max) and the maximal plasma concentration; however the AUC did not change.