Celecoxib

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DRUGS
Celecoxib

Celecoxib is a non-steroial anti inflammatory drug (NSAID) which is a selective inhibitor of cyclooxygenase-2 (COX-2). It works by reducing hormones that cause inflammation and pain in the body. Celecoxib is used in the treatment of rheumatoid arthritis and osteoarthritis. It is also used for ankylosing spondylitis.

Introduction

Celecoxib is a non-steroial antiinflammatory drug (NSAID) which is a selective inhibitor of cyclooxygenase-2 (COX-2). It works by reducing hormones that cause inflammation and pain in the body. Celecoxib is used in the treatment of rheumatoid arthritis and osteoarthritis. It is also used for ankylosing spondylitis.

Pharmacological Class: NSAID 

Indications

  • Osteoarthritis
  • Rheumatoid arthritis
  • Dysmenorrhoea
  • Ankylosing spondylitis
  • Acute Pain

Pharamcological Action

Celecoxib, a selective COX-2 inhibitor, is classified as a NSAID, used to treat rheumatoid arthritis, osteoarthritis, and familial adenomatous polyposis (FAP). Celecoxib inhibits the prostaglandin synthesis. Unlike most NSAIDs, which inhibit both types of cyclooxygenases (COX-1 and COX-2), celecoxib is a selective noncompetitive inhibitor of COX-2 enzyme. It binds with its polar sulfonamide side chain to a hydrophilic side pocket region, close to the active COX-2 binding site. Both COX-1 and COX-2 catalyze the conversion of arachidonic acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane.

Dosage

  • Osteoarthritis: 200 mg orally, daily as a single dose
  • Rheumatoid arthritis: 100 to 200 mg oral dose, twice daily
  • Ankylosing spondylitis: 200 mg daily in single (once per day) or divided (twice per day) doses
  • Dysmenorrhoea & Acute Pain: 400 mg for the first dose followed by a 200 mg dose about 8–12 hours later, if needed.

Pharmacokinetics

Well absorbed in the gastrointestinal tract. When a single dose of 200 mg is given to healthy subjects, peak plasma levels occur 3 hours after an oral dose. The peak plasma level is 705 ng/mL. Absolute bioavailability studies have not been conducted. Volume of distribution is found to be 500 l/kg and plasma protein binding is 97%. Metabolism occurs in liver. Renal Excretion accounts for < 1% and plasma half life is ~97.

Contraindications

  • In patients with known hypersensitivity to celecoxib, aspirin, or other NSAIDs
  • In patients who have demonstrated allergic-type reactions to sulfonamides
  • In patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Some of severe anaphylactic reactions to NSAIDs are fatal.
  • For treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery
  • In patients with active gastrointestinal bleeding

Drug Interactions

  • Combining alcohol with celecoxib increases risk of stomach bleeding
  • Celecoxib may increase the levels of lithium in body. Signs of lithium toxicity include slurred speech and tremors.
  • Celecoxib may reduce the blood pressure-lowering effects of few drugs (ACE inhibitors & angiotensin II receptor blockers)

Side effects

Common (affecting between 1 in10 to 1 in 100)

  • Diarrhea
  • Bloating
  • Sore throat
  • Cold symptoms
  • Constipation
  • Nausea & Vomiting
  • Dizziness
  • Headache

Uncommon (affecting 1 in 100 to 1 in 1000)

  • Excessive tiredness
  • Unusual bleeding or bruising
  • Loss of appetite
  • Pain in the upper right part of the stomach
  • Fever
  • Rash
  • Hives
  • Swelling of face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
  • Back pain

Very rare (affecting less than 1 in 10,000)

  • Chest pain
  • Difficult or painful urination
  • Frequent urination, especially at night
  • Difficulty swallowing or breathing
  • Unexplained weight gain
  • Hoarseness
  • Cloudy, discolored, or bloody urine

Precautions

  • Avoid in patients who are hypersensitive to celecoxib, sulfonamides, aspirin or other NSAIDs.
  • Drug should not be given in kidney dysfunction, neonates and in pregnancy.

Clinic Evidence

  • Celecoxib efficacy and upper gastrointestinal (UGI) safety evaluated as compared with nonspecific NSAIDs, among patients with osteoarthritis. Significantly more ulcer complications occurred within the nonselective NSAID group (0.8/100 patient-years) compared to celecoxib group (0.1/100 patient-years) (odds ratio = 7.02; 95% confidence interval [CI], 1.46 to 33.80; P =.008). There were fewer ulcer complications in the celecoxib group than NSAID group, both in patients taking concomitant aspirin and those not taking aspirin, but the difference reached statistical significance only in the latter comparison. Celecoxib is as effective as nonspecific NSAIDs (naproxen and diclofenac), but has significantly fewer serious upper gastrointestinal events.1
  • Celecoxib  was evaluated in AS in 12-week randomized, double-blind, placebo-controlled study with 4 treatment arms: celecoxib 200 mg qd, celecoxib 400 mg qd, naproxen 500 mg bid, and placebo. Celecoxib 400 mg was as effective as naproxen; however, naproxen was more effective than celecoxib 200 mg. Celecoxib was well tolerated, with an adverse event profile similar to placebo. However, 3 naproxen-treated patients experienced serious treatment-related GI adverse events (one severe gastric ulcer, one moderate GI hemorrhage, one severe GI hemorrhage). In this study, both celecoxib 200 mg qd and 400 mg qd were efficacious and well tolerated in treating signs and symptoms of AS.2

References

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