Найз®

General characteristics. Structure:

Active agent: Nimesulide of 100 mg.
Excipients: calcium hydrophosphate of 75 mg, cellulose microcrystallic (type 114) of 40 mg, starch of corn 54 mg, carboxymethylstarch of sodium of 35 mg, magnesium stearate of 3 mg, silicon dioxide of colloid 2 mg, talc of 1 mg.

Description
Round biconvex tablets, white with yellowish shade, with a smooth surface.

Pharmacological properties:

Pharmacodynamics. Non-steroidal anti-inflammatory drug (NPVP) from a class of sulfonanilid. Is the selection competitive inhibitor of cyclooxygenase-2 (TsOG-2), slows down synthesis of prostaglandins in the inflammation center. The oppressing influence on TsOG-1 is less expressed (causes the side effects connected with oppression of synthesis of prostaglandins in healthy fabrics less often). Renders the antiinflammatory, analgeziruyushchy and expressed febrifugal action.

Pharmacokinetics. Absorption at intake – high (meal reduces absorption speed, without influencing its degree). Time of achievement of the maximum concentration (TCmax) – 1,5-2,5 h. Communication with proteins of plasma – 95%, with erythrocytes – 2%, with lipoproteins – 1%, with acid alfa1-glycoproteins – 1%. Change of a dose does not influence extent of binding. The size of the maximum concentration (Cmax) – 3,5-6,5 mg/l. Distribution volume – 0,19-0,35 l/kg. Gets into fabrics of female generative organs where after a single dose its concentration makes about 40% of concentration in plasma. Well gets into acid medium of the center of an inflammation (40%), synovial fluid (43%). Easily gets through gistogematichesky barriers.
It is metabolized in a liver by fabric monooxygenases. The main metabolite – 4 hydroxynimesulide (25%), has similar pharmacological activity, but owing to reduction of the size of molecules is capable to diffuse quickly on hydrophobic channel TsOG-2 to an active center of binding of methyl group. 4 hydroxynimesulide are water-soluble connection for which removal are not required glutathione and conjugation tests of the II phase of metabolism (sulphation, glyukuronirovany and others). The elimination half-life (T1/2) of Nimesulide – 1,56-4,95 h, 4 hydroxynimesulides – 2,89-4,78 p. 4 hydroxynimesulide is removed by kidneys (65%) and with bile (35%), is exposed to enterogepatichesky recirculation.
At patients with a renal failure (clearance of creatinine of 1,8-4,8 l/h or 30-80 ml/min.), and also at children and elderly people the pharmacokinetic profile of Nimesulide significantly is not changed.

Indications to use:

- Pseudorheumatism;
- a joint syndrome at an exacerbation of gout;
- psoriasis arthritis;
- ankylosing spondylarthritis;
- osteochondrosis with a radicular syndrome;
- osteoarthrosis;
- mialgiya of rheumatic and not rheumatic genesis;
- inflammation of sheaves, sinews, bursitis, including posttraumatic inflammation of soft tissues;
- a pain syndrome of various genesis (including in the postoperative period, at injuries, альгодисменорея, a dentagra, a headache, an arthralgia, a lyumboishalgiya).

Drug is intended for symptomatic therapy, reduction of pain and an inflammation at the time of use, does not influence progressing of a disease.

Route of administration and doses:

It is necessary to use a minimal effective dose minimum possible short course. A pill is taken with enough water preferably after food. To adults and children 12 years – inside on 1 tablet 2 times a day are more senior. In the presence of digestive tract diseases it is desirable to accept drug at the end of food or after meal. The maximum daily dose for adults – 200 mg.
Patients with a chronic renal failure need decrease in a daily dose to 100 mg.

Features of use:

As Nayz® is partially removed by kidneys, its dose for patients with renal failures should be reduced, depending on indicators of clearance of creatinine.
Considering messages on vision disorders at the patients accepting other NPVP, treatment has to be immediately stopped if any vision disorder appears, and the doctor-oculist has to inspect the patient.
Drug can cause a liquid delay in fabrics therefore patients with high arterial pressure and with disturbances of cordial activity of Nayz® should apply with extra care.
Patients should undergo regular medical control if they along with Nimesulide accept medicines of which influence on digestive tract is characteristic. At emergence of signs of damage of a liver (a skin itch, yellowing of integuments, nausea, vomiting, the abdominal pain, urine darkening, increase in level of "hepatic" transaminases) should stop administration of drug and to see the attending physician. It is not necessary to use drug along with other NPVP.
Drug can change properties of thrombocytes, however does not replace preventive effect of acetylsalicylic acid at cardiovascular diseases.
Use of drug can negatively influence female fertility and is not recommended to the women planning pregnancy.
After 2 weeks of use of drug control of biochemical indicators of function of a liver is necessary.
This dosage form is contraindicated for children up to 12 years, but in need of use of Nimesulide for children 7 years are more senior tablets the dispersed 50 mg and suspension in strict accordance with the instruction on a medical use attached to them can be used.
As drug can cause drowsiness, dizziness and an illegibility of sight, it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Frequency of side effects is classified depending on the frequency of occurrence of a case: often (1-10%), sometimes (0,1-1%), it is rare (0,01-0,1%), is very rare (less than 0,01%), including separate messages.
Allergic reactions: seldom – hypersensitivity reactions; very seldom – anaphylactoid reactions.
From the central nervous system: infrequently – dizziness; seldom – feeling of fear, nervousness, dreadful dreams; very seldom – a headache, drowsiness, encephalopathy (a syndrome to Reja).
From integuments: infrequently – an itch, rash, sweating strengthening; seldom: erythema, dermatitis; very seldom: small tortoiseshell, Quincke's disease, puffiness of the person, mnogoformny exudative erythema, including Stephens-Johnson's syndrome, toxic epidermal necrolysis (Lyell's disease).
From an urinary system: infrequently – hypostases; seldom – a dysuria, a hamaturia, an ischuria, a hyperpotassemia; very seldom – a renal failure, an oliguria, intersticial nephrite.
From digestive tract: often – diarrhea, nausea, vomiting; infrequently – a lock, a meteorism, gastritis; very seldom – abdominal pains, stomatitis, a tar-like chair, gastrointestinal bleeding, an ulcer and/or perforation of a stomach or duodenum.
From a liver and bile-excreting system: often – increase in "hepatic" transaminases; very seldom – hepatitis, fulminant hepatitis, jaundice, a cholestasia.
From bodies of a hemopoiesis: seldom – anemia, an eosinophilia; very seldom – thrombocytopenia, a pancytopenia, a purpura, lengthening of a bleeding time.
From respiratory system: infrequently – an asthma; very seldom – an exacerbation of bronchial asthma, a bronchospasm.
From sense bodys: seldom – a sight illegibility.
From cardiovascular system: infrequently – arterial hypertension; seldom – tachycardia, hemorrhages, "inflows".
Others: seldom – the general weakness; very seldom – a hypothermia.

Interaction with other medicines:

Action of the medicines reducing coagulability of blood amplifies at their simultaneous use with Nimesulide.
Nimesulide can reduce effect of furosemide. Nimesulide can increase a possibility of approach of side effects at a concomitant use of a methotrexate.
Lithium level in plasma increases at a concomitant use of drugs of lithium and Nimesulide.
Nimesulide can strengthen effect of cyclosporine on kidneys.
Use with glucocorticosteroids, inhibitors of the return serotonin reuptake increases risk of development of gastrointestinal bleedings.

Contraindications:

Hypersensitivity to active agent or auxiliary components; a full or incomplete combination of bronchial asthma, the nose recuring a polypose or okolonosovy bosoms and intolerance of acetylsalicylic acid and other NPVP (including, in the anamnesis); erosive and ulcer changes of a mucous membrane of a stomach and duodenum (DPK), active gastrointestinal bleeding, cerebrovascular or other bleeding; inflammatory diseases of intestines (a disease Krone, nonspecific ulcer colitis) in an aggravation phase; hemophilia and other disturbances of coagulability of blood; dekompensirovanny heart failure; liver failure or any active disease of a liver; anamnestic data on development of hepatotoxic reactions when using drugs of Nimesulide; the accompanying use of potentially hepatotoxic substances; alcoholism, drug addiction; the expressed renal failure (clearance of creatinine less than 30 ml/min.), the progressing diseases of kidneys, the confirmed hyperpotassemia; the period after performing aortocoronary shunting; pregnancy, lactation period; children's age up to 12 years (for this dosage form see the section "Special Instructions").

With care
Coronary heart disease, cerebrovascular diseases, congestive heart failure, дислипидемия / lipidemia, diabetes mellitus, diseases of peripheral arteries, smoking, clearance of creatinine less than 60 ml/min. Anamnestic data on development of a canker of a GIT, existence of an infection of Helicobacter pylori, advanced age, long use of NPVP, frequent alcohol intake, heavy somatopathies, the accompanying therapy by anticoagulants (for example, warfarin), antiagregant (for example, acetylsalicylic acid, klopidogret), peroral glucocorticosteroids (for example, Prednisolonum), selective serotonin reuptake inhibitors (for example, to tsitalopra, fluoxetine, пароксетин, sertraline).

Overdose:

Symptoms: apathy, drowsiness, nausea, vomiting. There can be gastrointestinal bleeding, increase in arterial pressure, an acute renal failure, respiratory depression.
Treatment: the symptomatic treatment of the patient and the supporting care of it is required. There is no specific antidote. If the overdose happened within the last 4 hours, it is necessary to cause vomiting, to provide reception of absorbent carbon (60–100 g on the adult), osmotic laxatives. The artificial diuresis, a hemodialysis are inefficient because of high communication of drug with proteins.

Storage conditions:

List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children! Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 100 mg.
1, 2 or 10 PVC / aluminum blisters on 10 tablets together with the application instruction are packed into a cardboard pack.