Nimesulide

Nimesulide – drug with the antiinflammatory and anesthetizing action.

Form of release and structure

Nimesulide is produced in the form of tablets: oblong shape with the rounded ends, biconvex, light yellow with a weak greenish shade, with risky (in blister strip packagings from the aluminum varnished printing foil and a polyvinyl chloride film on 10, 15, 20, 30 pieces, on 1-6 packagings in a cardboard pack).

Is a part of 1 tablet:

• Active agent: Nimesulide – 100 mg;
• Auxiliary components: microcrystallic cellulose – 66,8 mg, povidone – 14 mg, monohydrate of lactose – 68 mg, potato starch – 68 mg, sodium carboxymethylstarch (glikolit sodium starch) – 36 mg, talc – 3,6 mg, magnesium stearate – 3,6 mg.

Indications to use

Nimesulide is appointed at an acute pain, a pain syndrome at an osteoarthritis (symptomatic therapy), primary dysmenorrhea.

Contraindications

Absolute:

• Digestive tract erosive cankers (at an aggravation);
• Heavy disturbances of coagulant system of blood;
• Gastrointestinal bleedings or any other states which are followed by bleeding;
• Heavy heart failure;
• Cerebrovascular hemorrhages;
• The expressed functional disturbances of kidneys (at clearance of creatinine it is less than 30 ml in a minute);
• Functional disturbances of a liver;
• Medicinal dependence;
• Alcoholism;
• Intolerance of non-steroidal anti-inflammatory drugs;
• Simultaneous use with other hepatotoxic drugs;
• Pregnancy and period of a lactation;
• Children's age up to 12 years;
• Hypersensitivity to drug components.

Relative (Nimesulide should be applied with care in the presence of the following diseases / states):

• Infectious diseases;
• Digestive tract diseases (including in the anamnesis);
• Arterial hypertension;
• Heart and renal failure;
• Diabetes mellitus 2 types;
• Hemorrhagic diathesis;
• The expressed metabolism disturbances;
• Astenisation (exhaustion, increased fatigue);
• Dehydration;
• Advanced age.

Route of administration and dosage

Nimesulide is accepted inside, it is more preferable – after food, washing down with enough water.

The recommended dosing modes:

• Adults: 2 times a day on 1 tablet (100 mg); as much as possible – 400 mg a day;
• Children of 12 years with body weight it is more than 40 kg: 2 times a day on 1 tablet (100 mg); as much as possible – 200 mg a day;
• Children of 12 years with body weight it is less than 40 kg: a single dose – 1,5 mg/kg of body weight, frequency rate of reception – 2-3 times a day; the maximum daily dose – 5 mg/kg.

It is necessary to accept the smallest effective dose of Nimesulide. Duration of therapy should not exceed 15 days.

Dose adjustment is not required to elderly patients.

Side effects

During use of Nimesulide the disturbances from some systems of an organism which are shown with various frequency can be observed (≥1/10 – it is very frequent;> 1/100, <1/10 – it is frequent;> 1/1000, <1/100 – infrequently;> 1/10 000, <1/1000 – it is rare; <1/10 000, including separate messages – it is very rare):

• Nervous system: infrequently – dizziness; seldom – irritability, frustration of a dream, concern; very seldom – encephalopathy, a headache, a syndrome to Reyna, drowsiness;
• Cardiovascular system: infrequently – hypertensia; seldom – heartbeat, tachycardia;
• Digestive tract: often – heartburn, vomiting, nausea, diarrhea; infrequently – abdominal distention, a lock, gastritis; very seldom – an ulceration of a mucous membrane of digestive tract, a stomach ache, a melena, a tar-like chair, increase in activity of hepatic transaminases, toxic hepatitis (including with a lethal outcome);
• Kidneys and urinary tract: seldom – a hamaturia, a dysuria, a liquid delay; very seldom – a renal failure, an oliguria, intersticial nephrite;
• Blood and lymphatic system: seldom – an eosinophilia, anemia, lengthening of a bleeding time; very seldom – an agranulocytosis, thrombocytopenia, a purpura, a pancytopenia;
• Allergic reactions: infrequently – skin rash and an itch; seldom – a dieback, an erythema; very seldom – the heavy skin phenomena, including a toxic epidermal necrolysis (Lyell's disease), Stephens-Johnson's syndrome, an acute anaphylaxis, a bronchospasm;
• Others: infrequently – hypostases; seldom – a hyperpotassemia, an adynamy, вертиго, vision disorders, an indisposition; very seldom – a hypothermia.

At development of any of the described side effects, and also in cases of emergence of other disturbances it is necessary to consult with the doctor.

Special instructions

At development during therapy of the symptoms indicating injury of a liver (in the form of anorexia, nausea, vomiting, abdominal pains, increased fatigue, urine darkening), or at abnormal results of functional hepatic trials it is necessary to cancel Nimesulide. Such patients are not recommended to accept drug and further.

Gastrointestinal bleedings or perforation/ulcer during therapy can arise at any time, with the advent of the warning signs and existence of gastrointestinal complications in the anamnesis or without them. At development of an ulcer or gastrointestinal bleeding administration of drug needs to be cancelled.

During treatment Nimesulide recommends to avoid the ethanol use, and also simultaneous use with hepatotoxic drugs, analgetics, other non-steroidal anti-inflammatory drugs.

At deterioration in a functional condition of kidneys treatment needs to be interrupted.

Patients with hemorrhagic diathesis need to apply Nimesulide under constant control.

Most often development of side effects (including perforation, gastrointestinal bleedings, dysfunctions of heart, liver and kidneys) is observed at elderly patients therefore patients of this age category need regular clinical control of a state.

During use of Nimesulide it is necessary to be careful at control of motor transport, service of moving mechanisms and performance of other potentially dangerous types of the works requiring special attention and bystry psychomotor reactions that is connected with probability of development of side effects in the form of dizziness and drowsiness.

Medicinal interaction

At simultaneous use of Nimesulide with some medicines there can be following effects:

• The drugs which are metabolized with CYP2C9 enzyme participation: increase in their concentration in a blood plasma;
• Cyclosporine: increase in nephrotoxicity;
• Antiepileptic (valproic acid), antifungal (кетоконазол), antitubercular drugs (isoniazid), Amiodaronum, methotrexate, Methyldopum, amoxicillin: development of the additive hepatotoxic effect;
• Warfarin, similar anticoagulants, acetylsalicylic acid: increase in risk of development of bleeding (the combination is not recommended, at heavy disturbances of a blood coagulation – it is contraindicated; in need of simultaneous use of these drugs it is necessary to control effect of anticoagulants);
• Furosemide: decrease in its efficiency (it is necessary to be careful against the background of functional disturbances of heart and kidneys);
• Lithium drugs: increase in concentration of lithium in a blood plasma and its toxicity (regular control of its concentration is necessary).

Terms and storage conditions

To store in protected from light, the place, dry, unavailable to children, at a temperature up to 25 °C.

Period of validity – 2 years.