Drug Breakdown: Celecoxib

Day 1: The discovery of the COX-2 channel in the early 1990s led to two new NSAIDs designed and licensed with COX-2 selective action. The new drug target implied therapeutic and adverse drug effect (ADE) superiority, but only #celecoxib endured, as rofecoxib (Vioxx) was found to have the highest cardiovascular risks.

Day 2: #celecoxib is licensed in adults for pain and inflammation in OA, RA and ankylosing spondylitis. Oral (capsule) use only; adult dose range is 200-400 mg in daily divided doses for the shortest duration possible. Not indicated for use in children and contraindicated in pregnancy.

Day 3: #celecoxib has good oral absorption taken with/without food (no advisory label). Major hepatic metabolism by CYP2C9 leads to inactive metabolites and elimination. Hepatic impairment, elderly and poor metabolisers incur increased drug levels, therefore use with caution. Contraindicated in severe hepatic or renal impairment.

Day 4: #celecoxib mechanism of action: NSAIDs all bind to membrane-bound cyclooxygenase (COX) in the cells' endoplasmic reticulum. #celecoxib blocks the active site of inducible COX-2 enzymes, which lowers prostaglandin production. This reduces pain and inflammation. COX-1 activity is relatively unaffected, so superior gut protection.