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Celecoxib

COX-2 Inhibitor · Anti-inflammatory, Analgesic

COX-2 InhibitorAnti-inflammatory, Analgesic
CDSCO approved
EXCRETION
not curated
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
Most manufacturers advise avoiding use during pregnancy or only if potential benefit outweighs risk. Avoid during the third trimester due to risk of closure of fetal ductus arteriosus in utero, possibly persistent pulmonary hypertension of the newborn, and potential delay/increase in duration of labour.
FDA category + note
Top interactionssee all 12
  • AlcoholContraindicatedTextbook-citedKDT 7e · p950
  • MethotrexateContraindicatedTextbook-citedKDT 7e · p949
  • MethylprednisoloneContraindicatedTextbook-citedKDT 7e · p950
  • CiprofloxacinSevereTextbook-citedKDT 7e · p949

Mechanism

Celecoxib is a selective inhibitor of cyclo-oxygenase-2 (COX-2). It works by inhibiting the activity of this enzyme.

Indications

Pain and inflammation in osteoarthritisPain and inflammation in rheumatoid arthritisAnkylosing spondylitisJuvenile arthritisManagement of acute painOsteoarthritisRheumatoid arthritisJuvenile rheumatoid arthritisPrimary dysmenorrheaGout (off-label use)

Dosing

Adult
For pain and inflammation in osteoarthritis: 200 mg daily in 1–2 divided doses, increased if necessary up to 200 mg twice daily. Discontinue if no improvement after 2 weeks on maximum dose. For pain and inflammation in rheumatoid arthritis: 100 mg twice daily, increased if necessary to 200 mg twice daily. Discontinue if no improvement.
Pediatric
Children >2 years: 50 mg (10–25 kg) or 100 mg (>25 kg) 2 times/day.
Renal adjustment
Avoid if possible or use with caution; avoid in moderate to severe impairment. The lowest effective dose should be used for the shortest possible duration.
Hepatic adjustment
Caution in mild to moderate impairment; avoid in hepatic failure. Consider initial dose reduction to 100 mg daily in mild to moderate impairment.
Geriatric
Potentially inappropriate if prescribed with a vitamin K antagonist, direct thrombin inhibitor or factor Xa inhibitor in combination (risk of major gastrointestinal bleeding); with concurrent antiplatelet agent(s) without proton pump inhibitor (PPI) prophylaxis (increased risk of peptic ulcer disease); or in patients with a history of peptic ulcer disease or gastrointestinal issues.
Max dose
400 mg daily

Pharmacokinetics

Onset
Peak plasma levels occur at 2 to 4 h after administration
Half-life
Approximately 11 h
Bioavailability
Protein binding
99%
Metabolism
Metabolized predominantly by CYP2C9 and inhibits CYP2D6. Minor metabolism by CYP3A4. Glucuronidation.
Excretion
Most is excreted as carboxylic acid and glucuronide metabolites in the urine and feces.

Contraindications

  • Use with a vitamin K antagonist, direct thrombin inhibitor or factor Xa inhibitor in combination (risk of major gastrointestinal bleeding)
  • Use with concurrent antiplatelet agent(s) without proton pump inhibitor (PPI) prophylaxis (increased risk of peptic ulcer disease)
  • History of peptic ulcer disease or gastrointestinal issues
  • Third trimester of pregnancy
  • Hepatic failure
  • Moderate to severe renal impairment
  • Perioperative pain in the setting of CABG surgery
  • Should be avoided in patients prone to cardiovascular disease
  • Should be avoided in patients prone to cerebrovascular disease
  • Loses its GI advantage over other NSAIDs when used in conjunction with aspirin
  • patients with history of ischaemic heart disease/hypertension/cardiac failure/cerebrovascular disease
  • use in patients at high risk of peptic ulcer, perforation or bleeds (should be administered in the lowest dose for the shortest period of time)

Side effects

Common
GI complaints (5%)Hypertension (attributed to inhibition of PG production in the kidney)Edema (attributed to inhibition of PG production in the kidney)Less ulcerogenicabdominal paindyspepsiamild diarrhoearashesedemasmall rise in BP
Serious
  • Serious gastro-intestinal events
  • Increased incidence of myocardial infarction
  • Increased incidence of stroke
  • Increased incidence of vascular death
  • Cardiovascular risk
  • Myocardial infarction (risk relates to dose and underlying CV risk)
  • Stroke (risk relates to dose and underlying CV risk)
  • Aseptic meningitis (reported)
  • Methemoglobinemia (reported)
  • Disseminated intravascular coagulation risk in pediatric patients
  • Decreased bone mineral density (chronic use, particularly in older male patients)
  • Slowed fracture healing (some suggestion)
  • Slowed tendon-to-bone healing (some suggestion)
  • increased risk of major fatal/nonfatal cardiovascular events
  • cardiovascular death
  • myocardial infarction
  • stroke
  • heart failure
  • thromboembolic event

Pregnancy & lactation

Pregnancy

Most manufacturers advise avoiding use during pregnancy or only if potential benefit outweighs risk. Avoid during the third trimester due to risk of closure of fetal ductus arteriosus in utero, possibly persistent pulmonary hypertension of the newborn, and potential delay/increase in duration of labour.

Lactation

Use with caution during breast-feeding. Manufacturer advises avoid.

Drug interactions

Alcohol
Contraindicated
Textbook-cited

Increased risk of gastric bleeding

Concurrent use is contraindicated

Source: KDT 7e · p950

Methotrexate
Contraindicated
Textbook-cited

Severe methotrexate toxicity (pancytopenia, mucositis).

Avoid concurrent use

Source: KDT 7e · p949

Methylprednisolone
Contraindicated
Textbook-cited

Significantly increased GI bleeding risk.

Concurrent use is contraindicated; if unavoidable, add PPI

Source: KDT 7e · p950

Ciprofloxacin
Severe
Textbook-cited

Enhanced CNS toxicity including seizures.

Avoid concurrent use

Source: KDT 7e · p949

Dexamethasone
Severe
Textbook-cited

Significantly increased GI bleeding risk.

Concurrent use is contraindicated; if unavoidable, add PPI

Source: KDT 7e · p950

Glibenclamide
Severe
Textbook-cited

Hypoglycemia.

Avoid concurrent use; substitute with paracetamol if analgesic needed

Source: KDT 7e · p949

Gliclazide
Severe
Textbook-cited

Hypoglycemia.

Avoid concurrent use; substitute with paracetamol if analgesic needed

Source: KDT 7e · p949

Glimepiride
Severe
Textbook-cited

Hypoglycemia.

Avoid concurrent use; substitute with paracetamol if analgesic needed

Source: KDT 7e · p949

Glipizide
Severe
Textbook-cited

Hypoglycemia.

Avoid concurrent use; substitute with paracetamol if analgesic needed

Source: KDT 7e · p949

Heparin
Severe
Textbook-cited

Increased bleeding risk.

Avoid concurrent use

Source: KDT 7e · p949

Hydrocortisone
Severe
Textbook-cited

Significantly increased GI bleeding risk.

Concurrent use is contraindicated; if unavoidable, add PPI

Source: KDT 7e · p950

Levofloxacin
Severe
Textbook-cited

Enhanced CNS toxicity, seizure risk.

Avoid concurrent use

Source: KDT 7e · p949

Related guidelines

Other COX-2 Inhibitor drugs

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e, Katzung·Verified: 2026-05-10 · House clinical team