Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) with COX-2 preference, used to treat pain and inflammation. It is more selective than other NSAIDs, with lower gastrointestinal risk. Available as tablets, oral suspension, and topical cream.
Also known as: nimesulide, nise, aulin, mesulid
Prontuário Terapêutico — Group 14 (Dermatology); EMC-EMC Portugal — Nimesulide SPC
Prontuário Terapêutico; EMC-EMC Portugal
NSAID + antimetabolite: methotrexate renal clearance may be reduced.
Nimesulide may reduce tubular secretion of methotrexate. The effect is less than with non-selective NSAIDs, but clinically relevant at high methotrexate doses.
Blood count, methotrexate levels.
Pancytopenia, mucositis.
Avoid NSAIDs during high-dose methotrexate. If necessary, monitor blood count.
Prontuário Terapêutico; EMC-EMC Portugal — Nimesulide
NSAID + biguanide: NSAID may reduce GFR and increase risk of lactic acidosis.
Nimesulide reduces renal blood flow via prostaglandin inhibition, potentially reducing GFR. In patients with borderline renal impairment, this may precipitate metformin accumulation and lactic acidosis.
GFR, creatinine, signs of lactic acidosis.
Lactic acidosis (nausea, vomiting, abdominal pain, lethargy).
Monitor GFR before and during concomitant treatment. Avoid if eGFR <45.
Prontuário Terapêutico; EMC-EMC Portugal — Nimesulide
Two NSAIDs: additive anti-inflammatory effects without benefit. Increased GI risk.
Combination of two NSAIDs offers no additional therapeutic benefit and significantly increases GI toxicity risk (ulcer, bleeding). Low-dose aspirin (antiplatelet) may be maintained with caution.
Signs of GI bleeding (epigastric pain, haematuria, melaena).
GI bleeding, gastric ulcer.
Do not combine two NSAIDs. If antiplatelet aspirin is necessary, administer 30 min before nimesulide.
Prontuário Terapêutico; EMC-EMC Portugal — Nimesulide
H2 blocker + NSAID: cimetidine may slightly reduce nimesulide absorption.
Cimetidine may slightly reduce oral bioavailability of nimesulide, but the clinical effect is minimal. No dose adjustment required.
No specific monitoring required.
No dose adjustment required.
Prontuário Terapêutico; EMC-EMC Portugal — Nimesulide
COX-2 selective NSAID + anticoagulant: increased bleeding risk. Platelet inhibition + anticoagulant effect.
Nimesulide is an NSAID with strong COX-2 preference (selectivity ~100:1 in vitro). However, it also partially inhibits platelet COX-1, especially at higher doses. Warfarin anticoagulates via inhibition of vitamin K-dependent coagulation factors. The combination of partial platelet inhibition + anticoagulation increases bleeding risk. The short half-life (2-3 h) is an advantage over long half-life NSAIDs (piroxicam: 50 h), but anti-inflammatory potency is high. The Portuguese Prontuário Terapêutico recommends avoiding the combination or monitoring INR weekly.
COX-2 selective NSAID + anticoagulant: increased bleeding risk. Residual platelet inhibition + anticoagulant effect. Short half-life (2-3 h) reduces risk vs. long NSAIDs.
Nimesulide preferentially inhibits COX-2 but has residual COX-1 platelet effect. Combined with warfarin, GI bleeding risk increases significantly. The short half-life (2-3 h) reduces risk compared to long half-life NSAIDs, but anti-inflammatory potency is high.
INR, signs of bleeding (bruising, haematuria, melaena).
Major bleeding, Hb drop >2 g/dL.
Avoid combination if possible. If necessary, monitor INR weekly. Low-dose nimesulide and short duration.
Prontuário Terapêutico; EMC-EMC Portugal — Nimesulide
NSAID + lithium: lithium levels may increase. Risk of lithium toxicity.
Nimesulide reduces renal blood flow via prostaglandin inhibition, decreasing lithium clearance. COX-2 selectivity and short half-life (2-3 h) make the effect smaller compared to indomethacin or naproxen. However, the effect is clinically relevant with prolonged treatment. Monitor lithium levels if co-administration >7 days.
COX-2 selective NSAID + lithium: lithium levels may increase. Less effect than non-selective NSAIDs due to short half-life.
Nimesulide may reduce renal lithium clearance via prostaglandin inhibition. The effect is less than with indomethacin or naproxen, due to short half-life and COX-2 selectivity.
Lithium levels, signs of toxicity (tremor, nausea).
Lithium level >1.5 mEq/L.
Monitor lithium levels if prolonged concomitant treatment. Consider reducing lithium dose by 10-20%.
Prontuário Terapêutico; EMC-EMC Portugal — Nimesulide
Food does not significantly affect nimesulide absorption. May be taken with or without food.
Take with food to reduce GI discomfort, if needed.
Partial renal excretion (50%). Accumulation in renal impairment. Risk of aggravated nephrotoxicity.
eGFR 30-50: reduce dose. eGFR <30: avoid. Monitor creatinine.
Prontuário Terapêutico; EMC-EMC Portugal — Nimesulide
CONTRAINDICATED in hepatic impairment. Nimesulide is potentially hepatotoxic — risk of fulminant hepatitis.
Do not administer in patients with hepatic impairment. Discontinue immediately if signs of hepatotoxicity.
Prontuário Terapêutico; EMC-EMC Portugal — Nimesulide
NSAIDs may precipitate bronchospasm in patients with NSAID-sensitive asthma (aspirin-induced asthma)
Avoid in patients with NSAID-sensitive asthma. If necessary, monitor pulmonary function.
Prontuário Terapêutico; EMC-EMC Portugal — Nimesulide
CONTRAINDICATED in pregnancy. NSAID — risk of premature ductus arteriosus closure and oligohydramnios.
All trimesters: CONTRAINDICATED.
Excreted in breast milk in low concentrations. Avoid during breastfeeding.
May affect fertility. Use reliable contraception.
Prontuário Terapêutico; EMC-EMC Portugal — Nimesulide
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Preferential COX-2 inhibition (selectivity ~100:1 in vitro). Also inhibits 5-LOX, reducing leukotriene formation. Anti-inflammatory, analgesic, and antipyretic activity. Significant local topical effect.
Preferential inhibition of COX-2 over COX-1. Additional 5-LOX inhibition confers additional anti-inflammatory properties. Also inhibits pro-inflammatory cytokine production (IL-1, IL-6, TNF-α).
Rapid and complete oral absorption. Bioavailability: 100%. Peak: 1-2 h. Food does not significantly affect absorption. Topical form: minimal systemic absorption.
Extensively metabolised in the liver. CYP2C9 (major) and CYP3A4. Inactive metabolites. Renal excretion (50%) and biliary (50%).
2-3 h (short). Does not accumulate significantly with 2x/day dosing.
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
