Nimesulide, tablets 100 mg 20 pcs

Non-steroidal anti-inflammatory drugs (NSAIDs)

ATX code: M01AX17

Pharmacodynamics

Nimesulide is a non-steroidal anti-inflammatory drug of sulfonamide class. It has anti-inflammatory, analgesic and antipyretic effect. Unlike non-selective NSAIDs, nimesulide mainly inhibits cyclooxygenase-2 (COX-2), inhibits synthesis of prostaglandins in inflammation focus, has less pronounced inhibitory effect on cyclooxygenase-1 (COX-1).

Pharmacokinetics

Nimesulide is well absorbed from the gastrointestinal tract (GIT)

Maximal concentration in blood plasma (Stah) after oral administration of a single dose of nimesulide, 100 mg, is reached on average after 2-3 hours and is 3-4 mg/l. The area under the curve “concentration-time” (AUC) is 20-35 mg/hl.

Binding with blood plasma proteins is up to 97.5%.

Metabolized in the liver by cytochrome Р450 isoenzyme (CYP)2C9. The main metabolite is pharmacologically active parahydroxy derivative of nimesulide – hydroxynimesulide, which is found exclusively as glucuronate.

Nimesulide is excreted mainly with urine (about 50% of the dose taken), about 29% is metabolized with feces.

The half-life (T1/2) is 3.2-6 hours.

Pharmacokinetic profile of nimesulide in elderly patients and in patients with renal insufficiency of mild and moderate severity is not changed when using single and multiple/repeated doses.

In a study conducted in patients with mild to moderate renal insufficiency (creatinine clearance 30-80 ml/min), the rates of nimesulide and its main metabolite were not higher than in healthy volunteers. AUC and Tj/2 were 50% higher, but were within the values of AUC and Tj/2 observed in healthy volunteers on nimesulide.

Repeated use did not lead to nimesulide cumulation.

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