Nimesulid

Products

Nimesulide is commercially available as tablets and granules (Nisulide, Aulin). It has been approved in many countries since 1991. Nisulide gel is no longer available.

Structure and properties

Nimesulide (C13H12N2O5S, Mr = 308.3 g/mol) belongs to the sulfonanilide group. It exists as a yellowish crystalline powder that is practically insoluble in water.

Effects

Nimesulide (ATC M01AX17) has analgesic, antipyretic, and anti-inflammatory properties. The effects are due to inhibition of prostaglandin synthesis by inhibition of cyclooxygenase COX-2.

Indications

As a 2nd-line agent for the treatment of acute pain and primary dysmenorrhea. Indications were narrowed in 2011 due to potential adverse effects on the liver.

Dosage

According to the drug label. Nimesulide is preferably taken after meals.

Contraindications

For complete precautions, see the drug label.

Interactions

Nimesulide is metabolized CYP2C9 and is a CYP2C9 inhibitor. Interactions have been described with lithium, anticoagulants, acetylsalicylic acid, furosemide, and methotrexate, among others.

Adverse effects

The most common adverse effects include digestive symptoms such as diarrhea, nausea, vomiting, and elevation of liver enzymes. Occasionally, drowsiness, hypertension, shortness of breath, constipation, flatulence, gastritis, pruritus, rash, increased sweating, and edema have also been observed. Very rarely, severe liver damage (including fatal cases), hepatitis, jaundice, and cholestasis have occurred.