Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) of the selective COX-2 inhibitor group, used in osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute pain and menstrual cramps. It has a lower risk of gastric irritation than classic NSAIDs, but retains the cardiovascular and renal risks of the class.
Also known as: Celebrex, celecoxib
Two NSAIDs (coxib + classical): no benefit and added GI/renal/cardiovascular risk.
Combining two NSAIDs — celecoxib, a selective COX-2 inhibitor, with ibuprofen, a non-selective one — adds no analgesic efficacy but increases toxicity: gastrointestinal risk (dyspepsia, ulcer, bleeding), renal risk (sodium retention, acute kidney injury in at-risk patients) and cardiovascular risk (hypertension, thrombotic events). Coxibs keep the cardiovascular and renal risk even with the relative gastrointestinal sparing. A single NSAID at the lowest effective dose should be chosen; chronic combination of two NSAIDs should be avoided, especially in the elderly and in patients with renal or cardiovascular disease or a history of ulcer.
Celecoxib + ibuprofen (two NSAIDs): no additional analgesic benefit and increased risk of gastrointestinal, renal and cardiovascular effects. Do not combine.
Additive adverse effects on gastric mucosa, renal function and cardiovascular balance.
Renal function, blood pressure and GI symptoms.
Dyspepsia, oedema, raised blood pressure.
Do not combine NSAIDs; use a single NSAID at the lowest effective dose.
DailyMed (FDA) — approved Celecoxib label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b06ced10-81c6-4f48-a205-1e0db228cb8b ; approved Ibuprofen label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=291602fa-8ebe-4200-bba7-9798c90f8a50 — additional reference: Prontuário Terapêutico do INFARMED (11th ed., 2012)
COX-2 selective NSAID + lithium: lithium levels may increase.
Celecoxib has COX-2 preference but may reduce renal lithium clearance. The effect is less than with non-selective NSAIDs but clinically relevant.
Lithium levels, signs of toxicity.
Lithium level >1.5 mEq/L.
Monitor lithium levels if concomitant treatment >7 days.
DailyMed/FDA — approved Celecoxib label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c6dbe686
Coxib + anticoagulant: increased bleeding risk.
Celecoxib is metabolised by CYP2C9 and moderately inhibits this enzyme (Ki ~4 μM). S-warfarin (more potent enantiomer, 3-5x more active than R-warfarin) is metabolised almost exclusively by CYP2C9. The resulting inhibition increases S-warfarin levels 1.5-3-fold and INR by 1.5-3 units. The effect is more pronounced in CYP2C9 poor metabolisers (CYP2C9*3 — frequency ~7% in Caucasians). FDA recommends reducing warfarin dose by 25-50% and monitoring INR 2-3 times/week during the first 2 weeks.
Selective COX-2 inhibitor + anticoagulant: celecoxib inhibits CYP2C9, increasing S-warfarin levels 1.5-3-fold. SERIOUS bleeding risk.
Celecoxib may increase gastrointestinal bleeding risk and interact with anticoagulation.
INR and GI symptoms during the combination.
Melena, haematemesis, spontaneous ecchymosis.
Use with caution, consider gastroprotection and watch for bleeding signs.
DailyMed (FDA) — approved Celecoxib label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b06ced10-81c6-4f48-a205-1e0db228cb8b ; approved Warfarin label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=541c9a70-adaf-4ef3-94ba-ad4e70dfa057 — additional reference: Prontuário Terapêutico do INFARMED (11th ed., 2012)
Taking with food may slightly delay absorption without affecting efficacy.
May take with food if stomach discomfort occurs.
EMC-UK (MHRA) — approved Celecoxib SmPC: https://www.medicines.org.uk/emc/product/5533/smpc
Alcohol increases the risk of gastric irritation/bleeding.
Avoid alcohol during treatment.
EMC-UK (MHRA) — approved Celecoxib SmPC: https://www.medicines.org.uk/emc/product/5533/smpc
Risk of bronchospasm in NSAID-sensitive patients.
Use with caution; avoid in aspirin-sensitive asthma.
EMC-UK (MHRA) — approved Celecoxib SmPC: https://www.medicines.org.uk/emc/product/5533/smpc
NSAIDs, including coxibs, may reduce renal function.
Monitor creatinine and urine output; use the lowest dose.
EMC-UK (MHRA) — approved Celecoxib SmPC: https://www.medicines.org.uk/emc/product/5533/smpc
Coxibs increase the risk of cardiovascular thrombotic events.
Use with caution; avoid in ischaemic heart disease or recent stroke.
EMC-UK (MHRA) — approved Celecoxib SmPC: https://www.medicines.org.uk/emc/product/5533/smpc
Despite COX-2 selectivity, celecoxib still carries a risk of active ulcer complications.
Contraindicated in active ulcer; seek an alternative.
EMC-UK (MHRA) — approved Celecoxib SmPC: https://www.medicines.org.uk/emc/product/5533/smpc
Celecoxib (NSAID) should be avoided in the 3rd trimester; limited data in early pregnancy.
Avoid in the 3rd trimester; avoid in women trying to conceive (possible effect on ovulation).
Prefer paracetamol in pregnancy.
Limited data; prefer to avoid during breastfeeding.
EMC-UK (MHRA) — approved Celecoxib SmPC: https://www.medicines.org.uk/emc/product/5533/smpc
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
COX-2 selective NSAID with analgesic, anti-inflammatory and antipyretic properties, indicated for osteoarthritis, rheumatoid arthritis, juvenile idiopathic arthritis, ankylosing spondylitis, acute pain and primary dysmenorrhoea. Does not affect platelet aggregation nor prolong bleeding time — not a substitute for aspirin for cardiovascular prophylaxis. Effective half-life of about 11 hours; metabolised by CYP2C9.
The mechanism of action is believed to be inhibition of prostaglandin synthesis, primarily via inhibition of COX-2 (a potent inhibitor of prostaglandin synthesis in vitro). Reduced prostaglandins in peripheral tissues decrease sensitisation of afferent nerves and the action of bradykinin in inducing pain, and mediate the anti-inflammatory effect.
Peak plasma levels occur approximately 3 hours after an oral dose; exposure roughly dose-proportional up to 200 mg twice daily (less than proportional at higher doses, due to low solubility). Highly protein bound (~97%), mainly to albumin; apparent steady-state volume of distribution about 400 L. A high-fat meal delays the peak by 1-2 hours with a 10-20% increase in AUC. Steady state by Day 5.
Metabolised primarily via CYP2C9 into three metabolites (a primary alcohol, the corresponding carboxylic acid and its glucuronide conjugate), inactive as COX-1/COX-2 inhibitors. Eliminated predominantly by hepatic metabolism with little (<3%) unchanged drug in urine and faeces: about 57% of the dose in faeces and 27% in urine (the carboxylic acid metabolite accounts for 73% of the dose). Fluconazole (a CYP2C9 inhibitor) doubles plasma concentrations.
Effective half-life of approximately 11 hours under fasting conditions (Tmax 2.8 h; apparent plasma clearance ~500 mL/min). In patients with mild/moderate hepatic impairment (Child-Pugh A/B) steady-state AUC increases ~40% and ~180% — reduce the dose by ~50% in moderate impairment. In CYP2C9*3/*3 poor metabolisers levels may be 3-7-fold higher.
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
