Nemulex, 100 mg/2 g 2 g 30 pcs.

Pharmgroup:

NSAIDs.

Pharmic action:

Nemulex – NSAID, has anti-inflammatory, analgesic, antipyretic and antiaggregant effect.
Unlike other NSAIDs it selectively inhibits COX-2, inhibits synthesis of Pg in inflamed area; less pronounced inhibitory effect on COX-1 (side effects related to inhibition of Pg synthesis in healthy tissues are less frequent).

Pharmacokinetics:

Absorption when oral administration is high (eating reduces absorption rate, without affecting its degree). Time of reaching maximum concentration in blood plasma (TStah) – 1.5-2.5 h. Binding with plasma proteins is 95%, with erythrocytes – 2%, with lipoproteins -1%, with acidic alpha1-glycoprotein -1%. Changing the dose does not affect the degree of binding. Maximum concentration (Stah) is 3.5-6.5 mg/l. Volume of distribution is 0.19-0.35 l/kg. It penetrates well into the acidic environment of the inflammation focus (40%), synovial fluid (43%).

It easily penetrates through histohematic barriers. It is metabolized in liver by tissue monooxygenases. The main metabolite is 4-hydroxynimesulide (25%), which has similar pharmacological activity, but due to the reduced size of molecules it is able to rapidly diffuse through COX-2 hydrophobic channel to active binding center of methyl group. 4-Hydroxynymesulide is a water-soluble compound that does not require glutathione and phase II metabolic conjugation reactions (sulfation, glucuronidation, etc.) for elimination.

The half-life (T1/2) of nimesulide is 1.56-4.95 h, 4-hydroxynimesulide is 2.89-4.78 h. 4-hydroxynimesulide is excreted by the kidneys (65%) and with the bile (35%), is subjected to enterohepatic recirculation.

Indications

Active ingredient

Composition

Active substance:

Nimesulide 100 mg;

Auxiliary substances:

macrogoal cetostearate (Cremophor A25) – 100 mg;

citric acid anhydrous – 19 mg;

Colloidal silicon dioxide (aerosil) – 40 mg;

sucrose – 1721 mg;

orange flavoring – 20 mg.

How to take, the dosage

Ingestion.The contents of 1 sachet of Nemulex granulate is dissolved in 80-100 ml of water. The recommended dose for adults and adolescents aged 12-18 years is 100 mg (1 sachet of Nemulex) 2 times a day after meals.

The maximum daily dose for adults and adolescents aged 12-18 years is 200 mg. No dose reduction is required for elderly patients. Patients with chronic renal insufficiency need to reduce the daily dose to 100 mg.

The lowest effective dose of Nemulex should be administered for as short a period as possible to minimize the risk of adverse reactions.

The maximum duration of Nemulex should not exceed 15 days.

Interaction

Special Instructions

To reduce the risk of side effects, Nemulex should be used in the lowest effective dose with the shortest duration. If the patient’s condition does not improve, the treatment should be stopped. The drug should be discontinued in case of fever or development of flu-like symptoms while taking the drug.

In patients taking Nimesulide, if symptoms indicating liver damage (e.g., anorexia, nausea, vomiting, abdominal pain, increased fatigue, dark urine) or increased “liver” transaminases are present, the drug should be stopped. It is not recommended to prescribe Nimesulide to such patients in the future. Gastrointestinal bleeding or gastric or duodenal ulcer/perforation may develop at any time when using the drug, which may not be accompanied by clinically pronounced symptoms (including pain syndrome). If gastrointestinal bleeding or ulceration occurs, the drug should be discontinued.

In case of worsening of renal function, the drug Nemulex should be discontinued. In case of using the drug for more than 2 weeks, monitoring of liver function parameters is necessary. In patients with cirrhosis or with renal failure with hypoalbuminemia or hyperbilirubinemia the binding of nimesulide is reduced.

In elderly patients, the most common side effects when taking the drug include gastrointestinal bleeding, perforations, heart, renal and hepatic dysfunction. Therefore, regular clinical monitoring of the patient is recommended. The use of nimesulide may adversely affect female fertility and is not recommended for women planning to become pregnant.

In case when using the drug Nemulex undesirable effects of the central nervous system and sensory organs occur, it is necessary to refrain from driving and engaging in activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

Side effects

Overdose

Similarities