Nimesulide

General characteristics. Structure:

Active ingredient: 100 mg of Nimesulide.

Excipients: cellulose microcrystallic, starch corn, sodium carboxymethylstarch, коповидон, polyethyleneglycol, polysorbate 80, magnesium stearate, silicon dioxide colloid.

Pharmacological properties:

Pharmacodynamics. NPVS in which structure there is a sulfonilidny group. Believe that Nimesulide belongs to the selection TsOG-2 inhibitors. Renders expressed antiinflammatory, and also analgetic and to a lesser extent febrifugal action. The mechanism of action is connected with inhibition of synthesis of prostaglandins. Suppresses synthesis of prostaglandins in the field of an inflammation more than in mucous a stomach or kidneys that TsOG-2 is caused by inhibition preferential.

Besides, in the mechanism of antiinflammatory effect of Nimesulide its ability to suppress education of free oxygen radicals (without influence on a hemostasis and phagocytosis) and to oppress myeloperoxidase enzyme release matters.

Pharmacokinetics. After intake Nimesulide is well absorbed from a GIT, Cmax in a blood plasma is reached in 1-2 h.

Linkng with proteins makes 99%. After intake of a single dose of 100 mg Nimesulide is present at fabrics of female generative organs in the concentration making 40% of concentration in plasma.

It is metabolized in a liver, the main metabolite hydroxynimesulide has pharmacological activity.

T1/2 makes 2-3 h of plasma. It is brought out of an organism preferential with urine, about 98% of a dose are removed during 24 h. At long therapy of cumulation of Nimesulide it is not observed.

Indications to use:

Osteoarthritis, extraarticular rheumatic diseases, pains and inflammatory processes after an operative measure, pains and fever at acute inflammatory processes in upper respiratory tracts, the pains connected with a dysmenorrhea.

Route of administration and doses:

Inside the adult on 100-200 mg of 2 times/days, children - 1.5 mg/kg of 2-3 times/days.

The maximum dose for children - 5 mg/kg/days in 2-3 receptions.

Features of use:

Use at pregnancy and feeding by a breast. Nimesulide is contraindicated to use at pregnancy and in the period of a lactation.

Direct instructions on embriotoksichesky and tokolitichesky effect of Nimesulide are not available.

Use at abnormal liver functions. It is contraindicated at the moderated and expressed liver failure.

Use at renal failures. It is contraindicated at a renal failure (KK less than 30 ml/min.).

Use for children. At use in pediatrics it is necessary to use the dosage forms intended for children. Control of the doctor outwardly is required from children under 6 years at Nimesulide use.

Use for elderly patients. At external use control of the doctor of a condition of patients of advanced age with renal failures is required, to a liver, with congestive heart failure.

Special instructions. With care it is necessary to apply inside at patients with renal failures, at arterial hypertension, at disturbances of action of the heart, vision disorders.

At external use control of the doctor of a condition of patients of advanced age with renal failures is required, to a liver, with congestive heart failure.

At use in pediatrics it is necessary to use the dosage forms intended for children. Control of the doctor outwardly is required from children under 6 years at Nimesulide use.

Influence on ability to driving of motor transport and to control of mechanisms. Because Nimesulide at intake can cause dizziness and drowsiness it is necessary to apply with care it at the patients who are engaged in potentially dangerous types of activity demanding the increased concentration of attention and bystry psychomotor reactions.

Side effects:

From the alimentary system: heartburn, nausea, stomach aches; in some cases - the tar-like chair, a melena (connected with bleedings and erosive cankers of a GIT).

From TsNS: seldom - headaches, dizziness, drowsiness.

Allergic reactions: skin rash, erythema, small tortoiseshell.

Others: seldom - an oliguria, a liquid delay in an organism, local or system hypostases; in some cases - a Werlhof's disease.

Interaction with other medicines:

Manifestations of medicinal interaction at a concomitant use in Nimesulide with digoxin, Phenytoinum, lithium drugs, diuretics, anti-hypertensive drugs, other NPVS, anticoagulants, cyclosporine, a methotrexate, peroral hypoglycemic means are possible.

Contraindications:

The peptic ulcer of a stomach and duodenum in an aggravation phase, acute bleeding from a GIT moderated and the expressed liver failure, renal failure (KK less than 30 ml/min.), pregnancy, a lactation; hypersensitivity to Nimesulide and other NPVS (including acetylsalicylic acid).

Issue conditions:

Without recipe

Packaging:

On 10, 20, 30 or 100 pieces in blister strip packagings and cardboard packs.