Evaluation of intravenous parecoxib for the relief of acute post-surgical pain.
Parecoxib is a prodrug of valdecoxib, which is a potent and selective inhibitor of COX-2. Intravenous preparation of parecoxib is in Phase III clinical trials for the management of acute and severe post-surgical pain. It is the only COX-2 inhibitor that is available in a parenteral formulation. Clinical results compare parecoxib with ketorolac, a NSAID, which is the only non-narcotic analgesic available in parenteral formulation that can be administered for the relief of moderate to severe acute pain. Pharmacokinetic studies have shown that parecoxib is converted to valdecoxib within a short time following administration by im. or iv. injection. In clinical trials, parecoxib compares favourably with ketorolac and produces less gastric or duodenal ulcers, the predominant adverse effect, than ketorolac. Parecoxib, thus, fulfils some of the desirable characteristics of an ideal non-narcotic analgesic for severe post-surgical pain and has application in other acutely painful conditions. Parecoxib is expected to be filed for approval before the end of 2000 and is expected to be introduced in the market in 2001. It has favourable prospects for a fair share of the post-surgical pain relief market which is valued at approximately US$ 1 billion for the year 2000.
Jain
K K
KK
Jain PharmaBiotech, Bläsiring 7, CH-4057 Basel, Switzerland. jain@pharmabiotech.ch
D000208:Acute Disease; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors*; D007555:Isoxazoles / Q000494:pharmacology / Q000627:therapeutic use*; D008565:Membrane Proteins; D010149:Postoperative Pain / Q000188:drug therapy*; D011355:Prodrugs / Q000494:pharmacology / Q000627:therapeutic use*; D011451:Prostaglandin-Endoperoxide Synthases; D013449:Sulfonamides / Q000494:pharmacology / Q000627:therapeutic use; D000096926:Benzenesulfonamides
D000894:Anti-Inflammatory Agents, Non-Steroidal; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D007555:Isoxazoles; D008565:Membrane Proteins; D011355:Prodrugs; D011451:Prostaglandin-Endoperoxide Synthases; D013449:Sulfonamides; C406224:valdecoxib; D000096926:Benzenesulfonamides; C409945:parecoxib; C496540:PTGS2 protein, human