Celecoxib; Uses, Dosage, Side Effects, Interaction, Pregnancy

Celecoxib
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Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) with a diaryl-substituted pyrazole structure. Celecoxib selectively inhibits cyclooxygenase-2 activity (COX-2); COX-2 inhibition may result in apoptosis and a reduction in tumor angiogenesis and metastasis.

Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis. Inhibition of PGE2 synthesis may lead to sodium and water retention through increased fluid reabsorption in the renal medullary thick ascending loop of Henle and perhaps other segments of the distal nephron. In the collecting ducts, PGE2 appears to inhibit water reabsorption by counteracting the action of antidiuretic hormone.

Mechanism of Action of Celecoxib

The mechanism of action of celecoxib is believed to be due to inhibition of prostaglandin synthesis. Unlike most NSAIDs, which inhibit both types of cyclooxygenases (COX-1 and COX-2), celecoxib is a selective noncompetitive inhibitor of cyclooxygenase-2 (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.

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Celecoxibis a nonsteroidal anti-inflammatory drug that exhibits antiinflammatory, analgesic, and antipyretic activities in animal models. The mechanism of action of celecoxib is believed to be due to inhibition of prostaglandin synthesis, primarily via inhibition of cyclooxygenase-2 (COX-2), and at therapeutic concentrations in humans, celecoxib does not inhibit the cyclooxygenase-1 (COX-1) isoenzyme. In animal colon tumor models, celecoxib reduced the incidence and multiplicity of tumors.

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Indications of Celecoxib

Contra-Indications of Celecoxib

Dosage of Celecoxib

Strengths: 50 mg; 100 mg; 200 mg; 400 mg

Osteoarthritis

  • Usual dose: 200 mg orally once a day OR 100 mg orally twice a day

Rheumatoid Arthritis

  • Usual dose: 100 or 200 mg orally twice a day

Ankylosing Spondylitis

  • Usual dose: 200 mg orally once a day OR 100 mg orally twice a day
  • If no effect after 6 weeks, consider increasing dose to 400 mg orally daily
  • Maximum dose: 400 mg per day

Acute Pain

  • Day 1: 400 mg orally once followed by an additional 200 mg orally if needed
  • Usual dose: 200 mg orally twice a day as needed

Dysmenorrhea

  • Day 1: 400 mg orally once followed by an additional 200 mg orally if needed
  • Usual dose: 200 mg orally twice a day as needed

Pediatric Dose for Juvenile Rheumatoid Arthritis

Age: 2 years or older

  • Weight: 10 kg to 25 kg: 50 mg orally twice a day
  • Weight: Greater than 25 kg: 100 mg orally twice a day

Side Effects of Celecoxib

The common

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More common

Less common

Rare

Drug Interactions of Celecoxib

Celecoxib may interact with following drugs, supplyments & may change the efficacy of drugs

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Pregnancy & Lactation of Celecoxib

FDA pregnancy category C

Pregnancy

Celecoxib capsules must not be used by women who are pregnant or can become pregnant (i.e. women of child bearing potential who are not using adequate contraception) during ongoing treatment. If you become pregnant during treatment with celecoxib capsules you should discontinue the treatment and contact your doctor for alternative treatment.

Lactation

Celecoxib capsules must not be used during breast-feeding.

References

 

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