Celecoxib
💊 Celecoxib is a highly selective COX-2 inhibitor.
⚠️ It theoretically reduces gastric side effects (e.g. ulceration) compared with traditional NSAIDs, but may increase cardiovascular risk (MI, stroke) — evidence still under investigation.
Always check the BNF link here before prescribing.
📖 About
- 🎯 Highly selective COX-2 inhibitor.
- ⬇️ Lower risk of peptic ulceration than NSAIDs (main selling point).
- ⚠️ No platelet effect and ❌ no cardioprotection (unlike aspirin).
- ⬆️ Evidence of prothrombotic tendency (cardiovascular caution).
🧪 Properties
- Contains a sulphonamide group → may cause hypersensitivity rash.
- Does not inhibit platelet aggregation.
⚙️ Action
- COX-1 → “housekeeping” enzyme: gastric mucosal protection, renal blood flow, thromboxane production.
- COX-2 → induced during inflammation: prostaglandins mediating pain, fever, swelling.
- Celecoxib inhibits COX-2 activity ~10–20× more than COX-1.
💉 Indications / Dose
- Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis.
- Dysmenorrhoea (menstrual pain).
- Familial adenomatous polyposis → reduces polyp burden (specialist use).
- Dose: 100–200 mg PO twice daily.
⚠️ Always use the lowest effective dose for the shortest duration.
🔄 Interactions
- 🩸 Aspirin offsets gastroprotection.
- ⬆️ Methotrexate toxicity risk.
- ⚠️ Risk of renal impairment if combined with ACE inhibitors, ARBs, ciclosporin, or diuretics.
⚠️ Cautions
- ⬆️ May cause a prothrombotic state → use with caution in IHD, cerebrovascular disease, peripheral vascular disease.
- 💧 Risk of renal toxicity and fluid retention → may worsen cardiac failure or hypertension.
- Monitor renal function and blood pressure if used long term.
⛔ Contraindications
- Severe renal or hepatic impairment.
- Active GI ulceration or bleeding.
- Established cardiovascular disease (MI, stroke, severe HF).
- Hypersensitivity (esp. to sulphonamides).
💥 Side Effects
- ⚠️ Prothrombotic risk: MI, stroke, angina.
- 💧 Oedema, hypertension, fluid retention.
- 🤢 GI upset: diarrhoea, dyspepsia, abdominal pain (though less ulcer risk than NSAIDs).
- 🌡️ Rash, cough, headache.
📚 References
