Nimesol

Trade name: Nimesol

International nonproprietary name: Nimesulid

Dosage band: tablets

Formula: 1 tablet contains: active substance- Nimesulid 100mg;

Additives: Natrium dioctyl sulfosuccinate, hyprolose, lactose monohydrate, microcrystalline cellulose, hydrogenised oil, magnesium stearate, starch, natrium glycolate.

Pharmacotheraputical group: non-steroid anti-inflammatory agent.

Pharmacological qualities: Pharmacodynamics

Nimesol- non-steroid anti-inflammatory preparation with antipyretic and analgetic activity. Nimesol — selective inhibitor of cyclooxygenase ferment COX-2, regulating prostaglandin synthesis more in the inflammatory site than in the mucous coat of stomach and kidneys. Therapeutical effect of Nimesol is connected not only with antiprostaglandine action that is not as strong as in some anti-inflammatory preparations, but also with competitive influence on inflammatory response on the whole. Nimesol influences neutrophil function in development of inflammatory response in 2 stages of cell-mediated response. It limits the production of superoxide radicals at the moment of neutrophils’ interaction with chemotaxis agents (direct cytolergy) without influencing cell kinetics and at the moment of phagocytosis with the decrease of neutrophils’ peptic action.

Pharmacokinetics Nimesol is quickly absorbed after oral intake. After intake of 100mg dose, concentration of nimesulide in plasma comprises 3,4 + 1,8 mgr/ml in 1,5 — 2,5 hours. Nimesol is quickly absorbed from gastrointestinal tract. Maximal concentration of the preparation (in 10mkg/ml) in single intake of 200mg is reached during 2–3 hours. Preparation possesses high ability of connecting with blood proteins (97%). Metabolism of Nimesol takes place in liver. Newly formed metabolite hydroxynimesulide possesses the same pharmacological qualities as parent molecule. The effect of Nimesol in synovial fluid begins to decrease in 6–12 hours. It eliminates from the body through urine (65%) and feces (35%).

Indications:

• Conditions requiring analgesia;
• Orthopedic diseases, i.e. arthritis
• Inflammation symptoms and post-surgical pains
• As anti-inflammatory and analgetic agent in upper air-passages infections.
• Traumas, contusions, dislocations.
• Dysmenorrhea.
• Toothache.

Contraindications:

• Acute gastrointestinal bleeding;
• Stomach and dodecadactylon peptic ulcer
• Severe kidney disfunction (creatine clearance < 30 ml/min);
• Pregnancy;
• Lactation (breast feeding);
• Hypersensitivity to any active ingredient or to other components of the preparation; to acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs.

Special warnings and precaution measures:

Nimesol can be applied only for treatment of adults. With care should be prescribed to patients with tendency to bleeding, in simultaneous intake of medicines decreasing blood coagulation and affecting thrombocyte aggregation. With care should be prescribed to patients with high arterial blood pressure or other cardiovascular system diseases due to the possible liquid detention in the body. With care should be prescribed to elderly patients (especially to asthenized patients).

Influence on driving ability and mechanism management:

Patients whose work requires high attention and quick psychomotor abilities should be warned about potential drowsiness and dizziness.

Pregnancy and lactation:

The preparation is contraindicated during pregnancy and lactation period.

Side effects:

In therapeutical doses Nimesol is tolerated well.

• digestive tract — dyspepsia;
• central nervous system — headaches, dizziness, drowsiness;
• allergic reactions — skin rash, erythema, hives.

Overdosage:

Symptoms: intensification of side effects

Treatment: gastric lavage, activated carbon, symptomatic therapy if necessary.

Drug interaction:

In simultaneous intake of Nimesol, effects of some medications lowering blood coagulation increase. In simultaneous intake of Nimesol and lithium preparations, Nimesol increases lithium concentration in plasma.

Method of application and dosage:

1 tablet (100mg) 2 times a day after mealtimes. If necessary preparation dose can be increased (to 200mg 2 times a day) depending on the severity of the condition and efficiency of the preparation.

Preparation is applied for reduction of acute pain syndrome and for long-term therapy.

Storage conditions:

Should be stored in a package and kept out of reach of children, under temperature — not above 25 С, in the dark place.

Form of issue:

Package contains 2 blisters with to tablets in each, package insert.

Conditions of delivery at chemistry stores:

Delivered according to prescription.

Expiry period:

Do not use the preparation after the expiry date.