Lumiracoxib.
Lumiracoxib is a selective cyclooxygenase (COX)-2 inhibitor that possesses a carboxylic acid group that makes it weakly acidic. It has good oral bioavailability; maximum plasma concentrations are reached two hours after oral administration. Despite its short elimination half-life of four hours from the plasma, the drug is distributed to inflamed tissues and is retained for up to 24 hours. This unique property suggests that lumiracoxib, while having reduced systemic exposure, can still reach sites where COX-2 inhibition is required for pain relief. Lumiracoxib is metabolized extensively with only a small amount excreted in the urine. Selectivity for COX-2 is high compared to all other similar agents. It is indicated for the relief of pain in osteoarthritis, rheumatoid arthritis, acute pain and primary dysmenorrhea. Lumiracoxib has been found to be effective at doses of 100-400 mg once a day for chronic pain and 400 mg/day for acute pain. Large clinical trials where lumiracoxib was administered to patients with osteoarthritis have demonstrated that this drug is equally effective as other COX-2 inhibitors and nonsteroidal anti-inflammatory drugs (NSAIDs). In comparison to NSAIDs, patients taking lumiracoxib experience significantly fewer adverse events and greater tolerability. It has also been shown to be effective in acute pain states, like the dental pain model and postoperative pain after orthopedic surgery. A large clinical study (TARGET) has demonstrated the gastrointestinal safety of lumiracoxib over one year. The study also showed that there was no increase in cardiovascular events in non-high-risk patients. However, a black box warning similar to those accompanying other COX-2 inhibitors has been placed by regulatory agencies that have approved this drug for clinical use. When lumiracoxib is coadministered with warfarin or aspirin, no dosage adjustment is required.
Buvanendran
Asokumar
A
Department of Anesthesiology, Rush University Medical Center, Chicago, Illinois 60612, USA. Asokumar@aol.com
Barkin
Robert
R
D002986:Clinical Trials as Topic; D051546:Cyclooxygenase 2 / Q000187:drug effects; D016861:Cyclooxygenase Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D004008:Diclofenac / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D004347:Drug Interactions; D006801:Humans
D016861:Cyclooxygenase Inhibitors; D004008:Diclofenac; D051546:Cyclooxygenase 2; C473384:lumiracoxib