BSN Tracker

celecoxib

Brand: Celebrex

⚠ BBW Beers Criteria Prototype Drug
Drug Class: nonsteroidal anti-inflammatory drug (NSAID)
Drug Family: NSAID
Subclass: selective COX-2 inhibitor (coxib)
Organ Systems: cnsmusculoskeletal

Mechanism of Action

Selectively inhibits COX-2 (the inducible isoform induced by inflammation) while sparing COX-1 (the constitutive isoform responsible for GI mucosal protection and platelet thromboxane synthesis). Reduced GI toxicity compared to non-selective NSAIDs, but greater cardiovascular thromboembolic risk due to unopposed prostacyclin reduction without compensatory thromboxane reduction.

COX-2 (cyclooxygenase-2 selective inhibitor)

Indications

  • osteoarthritis
  • rheumatoid arthritis
  • acute pain
  • dysmenorrhea
  • ankylosing spondylitis
  • familial adenomatous polyposis (FAP)

Contraindications

  • sulfonamide allergy (structural similarity)
  • perioperative CABG pain
  • third trimester pregnancy

Adverse Effects

Common

  • GI upset (less than non-selective NSAIDs)
  • hypertension
  • peripheral edema
  • headache

Serious

  • cardiovascular events (MI, stroke — class effect elevated vs. no NSAID use)
  • AKI
  • hepatotoxicity (rare)
  • Stevens-Johnson syndrome (rare)

Pharmacokinetics (ADME)

Absorption well absorbed orally; bioavailability ~40%
Distribution protein binding ~97%; Vd ~429 L
Metabolism primarily CYP2C9; inactive metabolites
Excretion fecal (~57%) and renal (~27%)
Half-life 11 hours
Onset 1-2 hours for analgesia
Peak 3 hours
Duration 12 hours (twice-daily dosing)
Protein Binding 97%
Vd 429 L

Drug Interactions

Drug / Agent Mechanism Severity
CYP2C9 inhibitors (fluconazole) increase celecoxib levels moderate
CYP2C9 substrates (warfarin) celecoxib may inhibit CYP2C9; monitor INR moderate
lithium reduce lithium clearance moderate
ACE inhibitors/ARBs AKI risk; antihypertensive antagonism major

Nursing Considerations

  1. Sulfonamide allergy cross-reactivity: celecoxib contains a sulfonamide group; use with caution in patients with sulfonamide hypersensitivity (risk debated but real).
  2. GI advantage of celecoxib over non-selective NSAIDs is reduced but not eliminated; GI protection is important in high-risk patients.
  3. Cardiovascular risk is a class effect of COX-2 inhibitors; avoid in patients with recent MI or established cardiovascular disease.
  4. Celecoxib has no antiplatelet activity (does not affect COX-1-mediated thromboxane in platelets); no aspirin interaction and no protective antiplatelet effect.

Clinical Pearls

  • The development of COX-2 selective inhibitors was based on the hypothesis that separating anti-inflammatory COX-2 inhibition from GI-protective COX-1 inhibition would improve safety; the GI benefit was real, but cardiovascular risk was a consequence of unbalancing the prostacyclin/thromboxane ratio.
  • Rofecoxib (Vioxx) was withdrawn in 2004 after demonstrating increased MI risk; celecoxib was retained with cardiovascular BBW; the PRECISION trial showed celecoxib comparable cardiovascular risk to ibuprofen and naproxen in arthritis patients.

Safety Profile

Pregnancy avoid
Lactation use-with-caution
Renal Adjustment Required
Hepatic Adjustment Required
TDM Not required

Concordance Terms

Cross-referenced clinical concepts — click any term to see all content where it appears.

Acute Pain Ankylosing Spondylitis Dysmenorrhea Familial Adenomatous Polyposis (FAP) Nonsteroidal Anti-inflammatory Drug (NSAID) Osteoarthritis Rheumatoid Arthritis
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