Nimesin

General characteristics. Structure:

Active ingredient: 100 mg of Nimesulide.

Excipients: laktozaa monohydrate; sodium of a kroskarmelloz; silicon dioxide colloid anhydrous; starch corn; povidone; sodium docusate; polysorbate-80; magnesium stearate.

The antiinflammatory and anesthetizing drug for treatment of inflammatory diseases oporno - the motive device, pain of various genesis. Has febrifugal and analgeziruyushchy effect.

Pharmacological properties:

Pharmacodynamics. Non-steroidal anti-inflammatory drug, the high-selection TsOG-2 inhibitor. Has antiinflammatory, analgeziruyushchy and febrifugal effect. Suppresses education of free oxygen radicals without influence on a hemostasis and phagocytosis. Inhibits myeloperoxidase enzyme release.

Pharmacodynamics. At oral administration Nimesulide is well soaked up from a digestive tract. After reception of a single dose of 100 mg of Nimesulide peak concentration in plasma - 3-4 mg/l - are reached in 2-3 hours. AUC (the area under a curve "concentration - time") represents 20-35 mg/l in an hour. At reception of 100 mg of Nimesulide twice a day within 7 days statistically reliable difference from above-mentioned figures was not revealed. About 97,5% to Nimesulide contact proteins of plasma.

Nimesulide is metabolized in a liver. The main metabolite of Nimesulide - parahydroxyderivative to which pharmacological activity is inherent too. The period through which this metabolite appears in blood is rather short - about 0,8 hours, however a constant of its education low. The period of its semi-removal makes 3,2-6 hours.

Nimesulide is removed from an organism preferential with urine (about 60% of the accepted dose). Only 1-3% are removed in an invariable look. Gidroksinimesulid, his main metabolite, appears in urine only in the form of a glyukuronidny conjugate. About 29% of a dose are removed with a stake after metabolism.

The Pharmakokinetichny profile at elderly people does not change.

At a moderate renal failure (clearance of creatinine of 30-80 ml/min.) the maximum concentration of Nimesulide and its main metabolite in plasma is not higher, than at healthy volunteers. Repeated reception does not lead to drug accumulation.

Indications to use:

Acute pain. A symptomatic treatment of an osteoarthritis with a pain syndrome. Primary dysmenorrhea.

Route of administration and doses:

Nimesin appoint after careful assessment of a ratio risk/advantage. Apply minimum effective dose during the shortest time to ease of side effects.

Apply inside after food and wash down with enough liquid.

Adults, children aged from 12 years and patients of advanced age: 100 mg (1 tablet) 2 times for days (in the morning and in the evening). The maximum duration of a course of treatment - 15 days.

Patients with a renal failure: with easy or moderate degree of a renal failure (clearance of creatinine of 30-80 ml/min.) of correction of a dose it is not necessary for patients. At a heavy renal failure (clearance of creatinine <30 ml/min.) of drug use contraindicated.

Features of use:

Use of drug during pregnancy and feeding by a breast is not recommended.

Use of Nimesulide is contraindicated in ІІІ a pregnancy trimester through potential risk of developing of bleeding at mother and the child.

Drug is contraindicated to children aged up to 12 years.

Because Nimesulide at acceptance inside can entail dizziness, drowsiness and occasionally - vision disorders, during treatment by drug it is necessary to abstain from occupations which need the increased concentration of attention and speed of psychomotor reactions.

It is necessary to apply minimum effective dose to decrease in risk of development of side effects and as much as possible to reduce drug use term. If the condition of the patient does not improve, treatment needs to be stopped. At prolonged treatment it is necessary to carry out control of indicators of a functional condition of a liver and kidneys.

At emergence in patients who accept Nimesin of symptoms which indicate injury of a liver (anorexia, nausea, vomits, jaundice, etc.), or abnormal results of functional hepatic trials, drug should be cancelled. Such patient forbids to appoint further Nimesin.

With care it is necessary to appoint Nimesin sick with a round ulcer, gastrointestinal disturbances or with disturbances of a blood coagulation in the anamnesis.

With care it is necessary to appoint drug sick with renal or heart failure as its appendix can lead to deterioration in function of kidneys. In case of deterioration in function of kidneys drug should be cancelled.

Use of non-steroidal anti-inflammatory drugs (NPVP) can mask the temperature increase connected with a background bacterial infection. In case of fervescence or emergence of grippopodobny symptoms in patients who apply Nimesulide administration of drug needs to be cancelled.

With care it is necessary to appoint drug sick which receive the accompanying therapy by drugs, which inherent strong allergenic properties (NPVP lactose antibiotics, diuretics, APF inhibitors), especially to patients with allergic reactions in the anamnesis. It is necessary to recommend to patients to abstain from use of other anesthetics during treatment. Simultaneous use of different NPVP is not recommended.

If the patient at use Nimesin had disturbances of clearness of sight, then treatment by drug it is necessary to cancel and conduct examination at the ophthalmologist.

Patients cannot appoint Nimesulide with chronic hepatitises. There is potentiality of developing of encephalopathy (a syndrome to Reja).

Use of Nimesulide can lead to disturbance of female fertility and is not recommended to women who plan to become pregnant.

It is necessary to control carefully indicators of a functional condition of a liver at the simultaneous appendix from a methotrexate as Nimesin reduces renal clearance of a methotrexate, therefore increases its toxicity.

Nimesini's tablets contain lactose therefore they patients need to appoint with care with a lactose intolerance.

Side effects:

At drug use, it is preferential within the first week from an initiation of treatment, there can be such side effects:

from skin: most often there are an erythema, urticaria, an itch; in single cases - Stephens-Johnson's syndrome, a toxic epidermal necrolysis, a multiformny erythema;

from a digestive tract: stomatitis, nausea, pain in epigastriums; abdominal pain, diarrhea, lock, gastrointestinal bleeding, stomach ulcer or duodenum, perforation of an ulcer;

from a liver: increase in level of liver enzymes  (transaminase, a glutamiltransferaza alkalinfosfataza), a cholestasia, sometimes chances of an acute hepatitis, even with the lethal end;

from the central nervous system: dizziness, drowsiness, headache; in single cases - encephalopathies (Rae's syndrome є);

from kidneys: oliguria, dysuria, mocheotdeleniye delay, intersticial nephrite, hypostases; in single cases - a hamaturia and a renal failure;

from system of blood: in isolated cases - purple, thrombocytopenia, a pancytopenia, a granulocytopenia, anemia, an eosinophilia;

from cardiovascular system: tachycardia, arterial hypertension, bleeding, fluctuations of arterial pressure, inflows;

from immune system: anaphylactic reactions, Quincke's edema;

from respiratory system: in edinochny cases - anaphylactic reactions: диспноэ and asthma, especially at patients with hypersensitivity to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs;

metabolism disturbance: hyperpotassemia;

mental disturbances: alarm, nervousness, dreadful dreams.

Also during administration of drug the hypothermia, disturbance of clearness of sight, a loss of consciousness are possible.

Interaction with other medicines:

There is potentially possible interaction of Nimesin with glibenclamide, theophylline, warfarin, digoxin, Cimetidinum and an antacid (a combination of aluminum and magnesium of hydroxide), but the researches in vivo did not reveal clinically significant pharmakokinetichny interactions.

The antagonistic effect in relation to diuretics is inherent to Nimesulide. Co-administration of Nimesulide and furosemide to patients with disturbance of renal or cordial function needs care.

At the simultaneous appendix with anticoagulants and antiagregant, including acetylsalicylic acid, there is an increased risk of development of bleedings.

NPVP reduce clearance of lithium which leads to increase in concentration of lithium in plasma and increases in its toxicity. Therefore at simultaneous use of Nimesin and lithium it is necessary to control carefully concentration of lithium in plasma.

Nimesin's use is compatible to other NPVP or alcohol exponentiates its hepatotoxic.

It is necessary to be careful at the simultaneous appendix from a methotrexate. Nimesin reduces renal clearance of a methotrexate, therefore its quantity in serum and toxicity increases. It is necessary to be careful if Nimesin is applied less than per day then or per day to use of a methotrexate. Possible increase in nephrotoxicity of cyclosporines at simultaneous use with Nimesin.

Contraindications:

Hypersensitivity to Nimesulide or to any component of drug is known; allergic reactions in the anamnesis (a bronchospasm, rhinitis, urticaria) in connection with use of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs; a peptic ulcer of a stomach or duodenum in an aggravation phase; recurrent ulcers or bleedings in a gastric path; cerebrovascular bleedings or other defeats which are followed by bleedings; heavy disturbances of a blood coagulation; heavy heart failure, heavy renal failures (clearance of creatinine <30 ml/min.), liver failure; the simultaneous appendix with potentially hepatotoxic means; children's age up to 12 years; ІІІ trimester of pregnancy and period of feeding by a breast; suspicion of acute surgical pathology, the increased body temperature and grippopodobny symptoms, alcoholism and drug addiction.

Overdose:

At acute overdose of drug the lethargy, drowsiness, nausea are usually observed, vomits also pain in the nadbryushny site. These symptoms usually oborotna at the supporting treatment. Gastrointestinal bleeding, arterial hypertension, an acute renal failure, anaphylactic reactions, oppressions of breath and a comma can be observed.

At overdose of drug the symptomatic and supporting treatment is recommended. There is no specific antidote.

The gastric lavage and administration of absorbent carbon (60-100 mg for adults) and a purgative of osmotic type is recommended to patients who arrived to a hospital with overdose symptoms drug (within 4 hours after its reception or after reception of a high dose). Necessary careful control of function of a liver and kidneys. The hemodialysis is inefficient.

Storage conditions:

To store in original packaging, in the dry places not available to children, at a temperature not above 25 degrees Celsius.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister. On 1 or 10 blisters in cardboard packaging.