Nimesulide

Absorption

Rapidly absorbed following oral administration.

Toxicity

Oral TDLO (human): 1.429 mg/kg; Oral TDLO (woman): 2 mg/kg; Oral LD50 (rat): 200 mg/kg; Oral LD50 (mouse): 392 mg/kg

Background

Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Its approved indications are the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old. Due to concerns about the risk of hepatotoxicity, nimesulide has been withdrawn from market in many countries.

Definition

ChEBI: Nimesulide is an aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups. It has a role as a cyclooxygenase 2 inhibitor and a non-steroidal anti-inflammatory drug. It is a C-nitro compound, a sulfonamide and an aromatic ether. It is functionally related to a nitrobenzene.

Pharmacokinetics

Food, gender and advanced age have negligible effects on nimesulide pharmacokinetics.

Metabolism

Hepatic. Extensive biotransformation, mainly to 4-hydroxynimesulide (which also appears to be biologically active).

The Uses of Nimesulide

Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) having analgesic and antipyretic effects that are primarily COX-2 selective. This medication is used to relieve pain. It relieves mild to moderate pain caused by menstrual cramps and osteoarthritis in adults and teenagers over the age of 12. Nimesulide reduces the intensity of pain signals transmitted to the brain and also prevents the synthesis of prostaglandins (substances that relay pain and heat signals to the brain).