Мексим®

General characteristics. Structure:

Active ingredient: 100 mg of Nimesulide in 1 tablet.

Excipients: sodium carboxymethylcellulose, cellulose microcrystallic PH 102, lactose anhydrous, aerosil 200, эксплотаб, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Meksim - non-steroidal anti-inflammatory drug (NPVS). The chemical structure of Nimesulide differs from other NPVS in what does not support carboxyl group in the structure, and contains sulfonanilidny group. Meksim selectively inhibits cyclooxygenase-2 (TsOG-2) which is responsible for formation of prostaglandins from arachidonic acid. Meksim's action is explained by inhibition of synthesis of prostaglandins which play a key role in an inflammation, emergence of pain and temperature increase.

The physiological role of prostaglandins consists in participation in protective mechanisms, such as maintenance of blood supply of fabrics, a homeostasis, integrity mucous a stomach, function of kidneys and an inflammation. Meksim has antiinflammatory, soothing and febrifugal activity. Activity of binding of free radicals medicinal means Meksim promotes the antiinflammatory action caused by suppression of prostaglandins. Education of free radicals due to activation of neutrophils is suppressed with Meksim without influence on their phagocytal activity or hemotoksichny activity. In addition considerably activity of synthesis of myeloperoxidase decreases.

Pharmacokinetics. Nimesulide quickly and almost is completely absorbed after reception. After oral administration of 100-200 mg average maximum plasma concentration (C max) are reached in 2-3 hours (t max). More than 97,5% of Nimesulide are in blood connected with proteins of plasma. After absorption Nimesulide is distributed in extracellular liquid. Thus, concentration in synovial fluid reaches 44% in 12 hours and remains longer in synovial fluid, than in plasma.

The elimination half-life (t1/2) makes from 3.2 to 6 hours. Nimesulide is extensively metabolized in a liver to the main metabolite of 4-IT-Nimesulide which also has considerable antiinflammatory activity. Only 1-3% of a dose are excreted in not changed view with urine. 70% of metabolites are removed with urine and 29% are removed with excrements.

Indications to use:

- treatment of acute pains;

- a symptomatic treatment of an osteoarthritis with a pain syndrome;

- treatment of primary dysmenorrhea.

It is necessary to appoint Nimesulide only as the second line. The decision on therapy has to be made by Nimesulide on the basis of assessment of all risks for the specific patient.

Route of administration and doses:

In order to avoid irritant action on a stomach Meksim accept after meal.

The recommended dose for adults on 100 mg 1 or 2 times a day. The maximum single dose - 100 mg; daily - 200 mg.

With normal function of kidneys dose adjustment is not required from elderly people.

Features of use:

At fervescence and emergence of grippoobrazny symptoms in patients reception of Nimesulide should be cancelled.

With care it is necessary to appoint drug at arterial hypertension, heart failure, a non-insulin-dependent diabetes mellitus (the II type).

Careful observation in cases is required if the patient receives antiagregantny and anticoagulating therapy. As at patients with a slight renal failure (speed of clearance of creatinine of 30-80 ml/min.), plasma concentration 4 hydroxynimesulides do not change, correction of a dosage is not required. But at patients with average degree of a renal failure (speed of clearance of creatinine <30 ml/min.) is required correction of a dosage. As it was in rare instances reported on heavy reactions like Stephens-Johnson's syndrome, a toxic epidermal necrolysis (Lyell's disease) and anaphylactic reactions, it is important to consider these reactions of hypersensitivity at the patients who are on treatment by Nimesulide.

Features of influence of medicine on ability to manage the vehicle or potentially dangerous mechanisms. With care appoint drug to the patients who are engaged in potentially dangerous types of activity requiring special attention.

Side effects:

- dyspepsia, nausea, vomiting, heartburn, stomach aches, gastritis, digestive tract erosive cankers, lock, meteorism, melena;

 - dizziness, headache, drowsiness, sensation of fear, nervousness, indisposition, adynamy;

- anemia, eosinophilia, thrombocytopenia, pancytopenia;

- short wind, tachycardia, hemorrhage, arterial hypertension, inflows;

- hypostases, dysuria, hamaturia, oliguria;

- an erythema, dermatitis, the increased sweating, a purpura;

- urticaria, rash, itch, bronchospasm, acute anaphylaxis;

- temporary and reversible increase in level of transaminases, hepatitis.

Interaction with other medicines:

At combined use of MEKSIM medicine with:

- a methotrexate, can increase its concentration in plasma, by replacement from communication of proteins of plasma, i.e. toxicity of a methotrexate increases. Therefore drug should be taken for 24 h to or in 24 h after reception of a methotrexate;

- furosemide, can suppress diuretic effect of furosemide. Therefore with care patients should appoint this combination with renal failures and cardiovascular diseases;

- anticoagulants, including warfarin and antiagregant (acetylsalicylic acid), the risk of development of bleeding increases. If joint appointment was obligatory, the thicket should control blood coagulation indicators;

- lithium drugs, increases concentration of lithium in a blood plasma and toxicity. It is necessary to watch lithium level in a blood plasma;

- cyclosporine - increases toxicity of cyclosporine;

- ethanol the risk of development of side reaction from a liver increases;

- theophylline efficiency of slowly released theophylline drugs decreases.

Contraindications:

- hypersensitivity in Nimesulide and other components of drug, acetylsalicylic acid and other non-steroidal anti-inflammatory drugs;

- digestive tract erosive cankers in the period of an aggravation, gastrointestinal bleedings;

- heavy disturbances of system of a blood coagulation;

- acute disorders of cerebral circulation;

- heavy abnormal liver functions and kidneys;

- pregnancy and period of a lactation;

- children's and teenage age up to 18 years.

Overdose:

Symptoms - apathy, drowsiness, vomiting, pain in epigastriums, increase in arterial pressure, an acute renal failure, spasms, gastrointestinal bleeding, respiratory depression, a coma, anaphylactoid reactions.

Treatment - there is no specific antidote. Correction of water and electrolytic balance, symptomatic therapy, gastric lavage, purpose of absorbent carbon.

Patients have to be under careful observation. The artificial diuresis, urine alkalifying, a hemodialysis, hemoperfusion are ineffective.

Storage conditions:

To store in dry, protected from light, the place at a temperature from 15 °C to 30 °C. To store in the place, unavailable to children! Period of storage 2 years. Not to apply after the storage expiration.

Issue conditions:

According to the recipe

Packaging:

Tablets of 100 mg. On 10 tablets in a blister strip packaging from a film of polyvinyl chloride and printing aluminum foil.

1 or 3 planimetric packagings together with the instruction on a medical use in the state and Russian languages place in a cardboard pack with the hologram of manufacturing firm.