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Detailed article on Coxib drugs

Synonyms

Coxib

Drug Information
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Identifiers CAS Number PubChem DrugBank ChemSpider ID UNII KEGG ChEBI ChEMBL IUPAC Name		Chemical Data C H N O Molecular Weight

Coxibs are a class of nonsteroidal anti-inflammatory drugs (NSAIDs) that selectively inhibit the cyclooxygenase-2 (COX-2) enzyme. This selectivity is intended to reduce the gastrointestinal side effects commonly associated with traditional NSAIDs, which inhibit both COX-1 and COX-2 enzymes.

Mechanism of Action

Coxibs work by selectively blocking the COX-2 enzyme, which is primarily responsible for the synthesis of prostaglandins involved in inflammation and pain. Unlike COX-1, which is involved in the protection of the gastric mucosa and platelet aggregation, COX-2 is induced during inflammatory processes. By inhibiting COX-2, coxibs reduce inflammation and pain without significantly affecting the protective functions of COX-1.

Clinical Uses

Coxibs are primarily used for the management of pain and inflammation associated with conditions such as osteoarthritis, rheumatoid arthritis, and acute pain. They are also used in the treatment of ankylosing spondylitis and dysmenorrhea.

Common Coxibs

• Celecoxib (marketed as Celebrex)
• Etoricoxib (marketed as Arcoxia)
• Parecoxib (marketed as Dynastat)

Adverse Effects

While coxibs are associated with a lower risk of gastrointestinal bleeding compared to non-selective NSAIDs, they have been linked to an increased risk of cardiovascular events such as myocardial infarction and stroke. This risk is thought to be due to the imbalance between pro-thrombotic and anti-thrombotic factors caused by selective COX-2 inhibition.

Controversies and Withdrawals

The coxib class has been subject to significant controversy, particularly following the withdrawal of Rofecoxib (Vioxx) from the market in 2004 due to concerns over increased cardiovascular risk. This event led to increased scrutiny of the safety profiles of all coxibs and NSAIDs.

Regulatory Status

Coxibs are available by prescription in many countries, with specific indications and contraindications varying by region. Regulatory agencies such as the Food and Drug Administration (FDA) and the European Medicines Agency (EMA) have issued guidelines on the use of coxibs, emphasizing the importance of assessing cardiovascular risk before prescribing these medications.

Also see

• Nonsteroidal anti-inflammatory drug
• Cyclooxygenase
• Prostaglandin
• Rofecoxib
• Cardiovascular disease