Celecoxib (Dosage)

Celecoxib is a non-steroidal anti-inflammatory drug indicated for pain in patients with osteoarthritis and rheumatoid arthritis. The presence of genetic polymorphisms in the CYP2C9 cytochrome gene may have an important impact on drug response.

Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) selective cyclooxygenase-2 (COX-2) inhibitor, 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 and other 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 bleeding.

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 estimated creatinine clearance 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 NYHA classification).


PRECAUTIONS

Avoid 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, gastrointestinal bleeding or if corticosteroids or oral anticoagulants are taken simultaneously.

Since the cardiovascular risk of celecoxib may increase with dose and duration of treatment, the lowest effective daily dose and shortest possible duration of treatment should be used. The need for symptomatic relief and response to treatment should be reassessed periodically.

Selective COX-2 inhibitors do not produce any antiplatelet effect, so they are not a substitute for 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 taking diuretics or at risk of hypovolemia.

If during treatment, there is deterioration of renal and/or hepatic function, discontinue treatment, as well as if skin rash, mucosal lesions or any other sign of hypersensitivity appears. 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 allergy; insomnia; dizziness, hypertonia; acute myocardial infarction, hypertension; pharyngitis, rhinitis, cough, dyspnea; abdominal pain, diarrhea, dyspepsia, flatulence, vomiting, dysphagia; rash, pruritus; flu-like symptoms, peripheral edema/fluid retention.


DRUG INTERACTIONS

Celecoxib increases the nephrotoxic effect of cyclosporine and tacrolimus.

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

Potentiates lithium toxicity.

Reduces the effect of diuretics and antihypertensives.

Action and toxicity potentiated by: fluconazole.

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


BRAND NAMES

  • Artilog®
  • Celebrex® Celebrex® Celebrex® Celebrex® Celebrex® Celebrex® Celebrex

Genes analyzed

CYP2C9

Bibliography

Agúndez JA, García-Martín E, Martínez C. Genetically based impairment in CYP2C8- and CYP2C9-dependent NSAID metabolism as a risk factor for gastrointestinal bleeding: is a combination of pharmacogenomics and metabolomics required to improve personalized medicine? Expert Opin Drug Metab Toxicol. 2009 Jun;5(6):607-20.

Dean L, Kane M. Celecoxib Therapy and CYP2C9 Genotype. 2016 Aug 18 [updated 2021 Jan 25]. In: Pratt VM, Scott SA, Pirmohamed M, Esquivel B, Kattman BL, Malheiro AJ, editors. Medical Genetics Summaries [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2012-.

McCormack PL. Celecoxib: a review of its use for symptomatic relief in the treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. Drugs. 2011 Dec 24;71(18):2457-89.

Theken KN, Lee CR, Gong L, et al . Clinical Pharmacogenetics Implementation Consortium Guideline (CPIC) for CYP2C9 and Nonsteroidal Anti-Inflammatory Drugs. Clin Pharmacol Ther. 2020 Aug;108(2):191-200.

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