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Celecoxib Metabolization

Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) selective inhibitor of cyclooxygenase-2 (COX-2), better tolerated and less ulcerogenic than conventional NSAIDs. It is approved for the treatment of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and acute pain. Celecoxib has also shown promise in the prevention of colorectal cancer and other types of cancers.

CONTRAINDICATIONS

Celecoxib is contraindicated in patients with a history of hypersensitivity to the active substance and to any of the excipients, or with known hypersensitivity to sulfonamides.

Contraindicated in patients with active peptic ulcer or gastrointestinal hemorrhage.

Do not prescribe celecoxib in patients who have experienced asthma, acute rhinitis, nasal polyps, angioneurotic edema, urticaria or other allergic-type reactions after taking acetylsalicylic acid or other NSAIDs, including COX-2 inhibitors.

Celecoxib is contraindicated in patients with severe hepatic dysfunction (serum albumin levels <25g / L or Child-Pugh ≥ 10).

Contraindications in patients with creatinine clearance estimated at less than 30 ml / min.

Do not prescribe in patients with inflammatory bowel disease or in patients with congestive heart failure (functional classes II-IV, according to the NYHA classification).

CAUTIONS

Avoid the concomitant use of other potentially gastroerosive agents (alcohol, steroids, other NSAIDs or acetylsalicylic acid). Prophylaxis for gastroprotection is recommended if there is a history of gastrointestinal ulcer or perforation, digestive hemorrhage or oral corticosteroids or anticoagulants are taken simultaneously.

Since the cardiovascular risk of celecoxib can be increased with the dose and duration of treatment, the lowest effective daily dose and the shortest possible treatment duration should be used. The need for symptomatic relief and response to treatment should be re-evaluated periodically.

Selective COX-2 inhibitors do not produce any antiplatelet effect, so they do not replace acetylsalicylic acid or other antiplatelet agents in the prophylaxis of cardiovascular thromboembolic diseases.

It should be administered with caution in patients with a history of heart failure, hypertension or edema of any cause, as well as in those who take diuretics or are at risk of hypovolemia.

If during the treatment, there is deterioration of the renal and/or hepatic function, suspend it, as well as if rash appears, lesions of the mucous membranes or any other sign of hypersensitivity. Warnings and precautions when associated with warfarin and other oral anticoagulants.

Celecoxib masks fever and other signs of inflammation. Avoid concomitant use with an NSAID other than ASA.

SIDE EFFECTS

Sinusitis, upper respiratory tract infection, urinary tract infection; worsening of the allergy; insomnia; dizziness, hypertonia; acute myocardial infarction, hypertension aretrial; pharyngitis, rhinitis, cough, dyspnea; abdominal pain, diarrhea, dyspepsia, flatulence, vomiting, dysphagia; rash, pruritus; flu-like symptoms, peripheral edema/fluid retention.

PHARMACOLOGIC INTERACTIONS

Celecoxib increases the nephrotoxic effect of ciclosporin and tacrolimus.

Celecoxib increases plasma concentrations of drugs metabolized by CYP2D6 (tricyclic antidepressants and serotonin reuptake inhibitors, neuroleptics, antiarrhythmics, etc.).

Celecoxib potentiate the toxicity of lithium.

Reduces the effect of diuretics and antihypertensives.

The action and toxicity of ceñlecoxib can be potentiated by fluconazole.

Plasma concentrations of celecoxib are reduced by rifampicin, carbamazepine and barbiturates.

BRAND NAMES

  • Artilog ®
  • Celebrex ®

Gene or region studied

  • CYP2C9
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