Description
Parecoxib is a prodrug form of the COX-2 inhibitor valdecoxib . It is converted to valdecoxib by human liver microsomes
in vitro and
in vivo in rats, dogs, and cynomolgous monkeys. Parecoxib is also a cannabinoid (CB) receptor 1 agonist with an EC
50 value of 2.4 μM in HEK293 cells. It reduces hyperalgesia in a rat model of carrageenan-induced foot pad edema (ED
50 = 5 mg/kg) and decreases inflammation in a rat model of
M. butyricum-induced arthritis (ED
50 = 0.08 mg/kg).
Chemical Properties
White Solid
Uses
Anti-inflammatory, analgesic.
Indications
For the short-term treatment of acute pain and post-operative pain i.e., oral surgery, abdominal hysterectomy, myomectomy, total knee replacement, total hip arthroplasty, laparoscopic cholecystectomy, inguinal hernia repair and other general surgery like diagnostic laparoscopy, gastrectomy, hernioplasty, appendectomy, hemithyroidectomy and splenectomy. Parecoxib Sodium may be used pre-operatively to prevent or reduce post-operative pain and it can reduce opioid requirements when they are used concomitantly.
Application
Parecoxib sodium is a water-soluble sodium salt of the amide prodrug of valdecoxib. Parecoxibundergoes enzymatic hydrolysis in vivo to the active moiety valdecoxib, and is formulated as apowder for solution for parenteral administration. Valdecoxib is a selective inhibitor of the enzymeCOX-2.
Biological Functions
A water-soluble, injectable sodium salt form of parecoxib, an amide prodrug of the cyclooxygenase II (COX-2) selective, non-steroidal anti-inflammatory drug (NSAID) valdecoxib, with anti-inflammatory, analgesic, and antipyretic activities. Valdecoxib selectively binds to and inhibits COX-2. This prevents the conversion of arachidonic acid into prostaglandins, which are involved in the regulation of pain, inflammation, and fever. This NSAID does not inhibit COX-1 at therapeutic concentrations and, therefore, does not interfere with blood coagulation.
Pharmacokinetics
Parecoxib (Dynastat) is a prodrug of valdecoxib. Valdecoxib is an NSAID that exhibits antiinflammatory, analgesic and antipyretic properties in animal models. The mechanism of action is believed to be due to inhibition of prostaglandin synthesis primarily through inhibition of COX-2. At therapeutic plasma concentrations in humans valdecoxib does not inhibit cyclooxygenase-1 (COX-1).
