Celecoxib Uses, Side Effects, and More

 Celecoxib 

Brand name:- Celact, Revibra , Colcibra 100, 200mg caps

Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) called COX-2 inhibitors. It works by blocking the release of certain chemical messengers that are responsible for pain and inflammation (redness and swelling).

Pharmacodynamic:- 

Celecoxib inhibits cyclooxygenase 2 (COX-2) enzyme, reducing pain and inflammation. It is important to note that though the risk of bleeding with celecoxib is lower than with certain other NSAIDS, it exists nonetheless and caution must be observed when it is administered to those with a high risk of gastrointestinal bleeding.

A note on the risk of cardiovascular events

Significant concerns regarding the safety of COX-2 selective NSAIDs emerged in the early 2000s. Rofecoxib, another member of the COX-2 inhibitor drug class, also known as Vioxx, was withdrawn from the market due to prothrombotic cardiovascular risks.Following an FDA Advisory Committee meeting in 2005, in which data from large clinical outcome trials were evaluated, the FDA concluded that the risk for cardiovascular thrombotic events for both COX-2 selective NSAIDs and nonselective NSAIDs was evident.It was determined that the benefits of celecoxib treatment, however, outweighed the risks. Postmarketing cardiovascular outcomes trial (PRECISION) revealed that the lowest possible dose of celecoxib was similar in cardiovascular safety to moderate strength doses of both naproxen and ibuprofen. Patients who had previous cardiovascular events including acute MI, coronary revascularization, or coronary stent insertion were not evaluated in the trial. It is not advisable to administer NSAIDS to these groups of patients.

Mechanism of action:-

Anti-inflammatory 

A highly selective reversible inhibitor of the COX-2 isoform of cyclooxygenase, celecoxib inhibits the transformation of arachidonic acid to prostaglandin precursors. Therefore, it has analgesic and anti-inflammatory properties. Nonselective NSAIDs (such as aspirin, naproxen, and ibuprofen) inhibit both COX-1 and COX-2. Inhibition of COX-1 (which celecoxib does not inhibit at therapeutic concentrations) inhibits the production of prostaglandins and the production of thromboxane A2, a platelet activator. COX-1 is traditionally defined as a constitutively expressed "housekeeping" enzyme and plays a role in the protection of the gastrointestinal mucosa, kidney hemodynamics, and platelet thrombogenesis.COX-2, on the contrary, is extensively expressed in cells involved in inflammation and is upregulated by bacterial lipopolysaccharides, cytokines, growth factors, and tumor promoters. Celecoxib is approximately 10-20 times more selective for COX-2 inhibition over COX-1. It binds with its polar sulfonamide side chain to a hydrophilic side pocket region close to the active COX-2 binding site.In theory, this selectivity allows celecoxib and other COX-2 inhibitors to reduce inflammation (and pain) while minimizing gastrointestinal adverse drug reactions (e.g. stomach ulcers) that are common with nonselective NSAIDs

Anti- cancer 

For its use in reducing colon polyps, celecoxib affects genes and pathways involved in inflammation and malignant transformation in tumors, but not normal tissues.

Celecoxib binds to Cadherin-11 (which may explain the reduction in cancer progression).[citation needed]

 Used:- 

Used to treat migraines. It helps to relieve headache, pain, and other migraine symptoms (including nausea, sensitivity to light/sound). Prompt treatment helps you return to your normal routine and may decrease your need for other pain medications. Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID), specifically a COX-2 inhibitor. It works by blocking your body's production of certain natural substances that cause inflammation. 

Side effects:-

Diarrhea, Headache, Dyspepsia, Upper respiratory tract infection, Sinus inflammation.

 Dose:-  250- 500 mg BD , children half dose. As directed by your doctor.