Nimesulide-Teva, tablets 100 mg 30 pcs

Pharmacotherapeutic group: Non-steroidal anti-inflammatory drug (NSAID)

ATX code: M01AX17

Pharmacological properties

Pharmacodynamics. Nimesulide belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs), has anti-inflammatory, analgesic, antipyretic and antiaggregant effects. Unlike indomethacin, it inhibits cyclooxygenase 2 (COX-2) to a greater extent than COX-1 (potentially less often causing side effects associated with inhibition of prostaglandin synthesis in healthy tissues, inhibiting their synthesis mainly in the focus of inflammation).

Pharmacokinetics. Nimesulide is well absorbed when taken orally (eating reduces the rate of absorption without affecting its degree). After a single administration of 100 mg of nimesulide the maximum concentration (C_max) in blood plasma in adults reaches 3-4 mg/l and is observed after 2-3 hours. Binding with plasma proteins is 95%, with erythrocytes – 2%, with lipoproteins – 1%, with acidic alpha1-glycoproteins – 1%. Increasing the dose does not affect the degree of binding.

The area under the curve “concentration-time” (AUC) is 20-35 mg h/l. No statistically significant differences were found between these parameters after a single dose and administration for 7 days in a dose of 100 mg twice a day.

The volume of distribution is 0.19-0.35 l/kg. It easily penetrates through histohematic barriers (in female genital tissues after a single nimesulide administration its concentration is about 40% of the blood plasma concentration), including acidic environment of the inflammatory focus and synovial fluid (40% and 43% of the blood plasma concentration, respectively).

It is metabolized in liver with participation of monooxygenases, including cytochrome P450 (CYP) 2C9 system. The main metabolite is water-soluble 4-hydroxynimesulide (25%), which has pharmacological activity similar to nimesulide.

Nimesulide is excreted mainly in the urine (approximately 50% of the dose taken). The half-life (T_1/2) of nimesulide is 3-6 hours, of 4-hydroxynimesulide – 3-5 hours. 4-hydroxynimesulide is excreted by the kidneys (65%) and with the bile (35%); it undergoes enterohepatic recirculation.

Only 1-3% of nimesulide is excreted unchanged. Approximately 29% of the dose is excreted as a metabolite in the feces.

The pharmacokinetic profile of nimesulide in the elderly does not change after single and repeated administration of the drug.

In patients with mild to moderate renal impairment – creatinine clearance (CK) 30-80 ml/min, C_max of nimesulide and its main metabolite in plasma are not higher than those of healthy volunteers. Repeated administration of nimesulide is not accompanied by its cumulation.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Synopsis

Contraindications

Side effects

Overdose

Pregnancy use

Similarities