Analgesic

Celecoxib

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Celecoxib, Celebrex

  • See Also
  1. COX2 Inhibitor
  2. Nonsteroidal Anti-inflammatory
  • Indications
  1. FDA approved indications in adults
    1. Osteoarthritis
    2. Ankylosing Spondylitis
    3. Rheumatoid Arthritis
    4. Acute Pain
    5. Dysmenorrhea
    6. Familial Adenoma Polyposis
  2. FDA approved indications in children
    1. Juvenile Rheumatoid Arthritis
  • Contraindications
  1. Sulfonamide Allergy
  2. Immediate Post-Operative CABG state
  • Metabolism
  1. See COX2 Inhibitor
  2. Celecoxib is an NSAID that is more COX2 selective (COX2 Inhibitor)
  3. Diaryl-substituted pyrazole
  • Medications
  1. Celecoxib (Celebrex) capsules 50, 100, 200, 400 mg
  2. Celecoxib capsules may be opened, sprinkled into applesauce and immediately taken with water
  • Dosing
  • Adult
  1. Osteoarthritis or Ankylosing Spondylitis
    1. Dose: 200 mg orally daily (or 100 mg orally twice daily)
  2. Rheumatoid Arthritis, Acute Pain, Dysmenorrhea
    1. Dose: 100 to 200 mg orally daily to twice daily
  3. Familial Adenoma Polyposis
    1. Dose: 400 mg orally twice daily
  4. Dosing adjustments
    1. Decrease dose to 50% in moderate liver dysfunction
  • Dosing
  • Child
  1. Juvenile Rheumatoid Arthritis (age 2 to 17 years)
    1. Weight 10 to 25 kg: 50 mg orally twice daily
    2. Weight >25 kg: 100 mg orally twice daily
  • Adverse Effects
  1. See COX2 Inhibitor
  2. Precautions
    1. NSAID Renal Adverse Effects also apply to COX2 Inhibitors
  3. Gastrointestinal
    1. Less gastrointestinal adverse effects than other NSAIDs
      1. See NSAID Gastrointestinal Adverse Effects
    2. Abdominal Pain
    3. Diarrhea
    4. Dyspepsia
    5. Peptic Ulcer Disease risk (see COX2 Inhibitor)
  4. Cardiovascular
    1. Celebrex appears safer than Ibuprofen in terms of Cardiovascular Risk
      1. Ruschitzka (2017) Eur Heart J +PMID:29020251 [PubMed]
    2. As with NSAIDs, avoid COX2 Inhibitors immediately after CABG
    3. COX2 Inhibitors may also result in fluid retention, edema and worsening Congestive Heart Failure
  5. Hematologic
    1. Does not increase Bleeding Time or affect Platelets
  • Safety
  1. See NSAID
  2. Unknown safety in Lactation
  3. Celecoxib is Pregnancy Category C (except for Category D in third trimester)
  4. As with NSAIDs, avoid COX2 Inhibitor in pregnancy outside the first part of the second trimester (13 to 20 weeks)
    1. Teratogenic in first trimester
    2. Risk of premature ductus arteriosus closure in the fetus in third trimester
    3. Most NSAIDs carry a legacy system Pregnancy Category B or C designation (aside from third trimester)
      1. However, many obstetricians avoid NSAIDs entirely in pregnancy (even in second trimester)
  • Pharmacokinetics
  1. Oral Bioavailability: 22 to 40%
  2. Half Life: 11 hours
  • Drug Interactions
  1. CYP2C9 Inhibitors
    1. Celecoxib levels raised by, for example, Zafirlukast, Fluconazole, and Fluvastatin
  2. Celecoxib Inhibits CYP2D6
    1. Increases levels of Beta Blockers, Lithium and other psychotropics
  • Resources
  1. Celecoxib (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8709cbe7-3de1-4908-a0a9-53002bcee15b
  • References
  1. Michalets (1998) Pharmacotherapy 18:84 [PubMed]
  2. (1999) Med Lett Drugs Ther 41(1045): 11-14 [PubMed]