Remesulid

General characteristics. Structure:

Active ingredient: nimesulide;

1 tablet contains Nimesulide in terms of 100% substance of 100 mg;

excipients: lactoses monohydrate, potato starch, gipromelloz, silicon dioxide colloid anhydrous, кросповидон, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Nimesulide – the active agent having antiinflammatory, analgesic and febrifugal properties. Nimesulide selectively inhibits TsOG II (cyclooxygenase II) and synthesis of prostaglandins in the inflammation center oppresses.

Nimesulide inhibits myeloperoxidase enzyme release, and also education of free radicals of oxygen oppresses, without influencing processes of phagocytosis and a chemotaxis, formation of a factor of a necrosis of tumors and other mediators of an inflammation oppresses.

Pharmacokinetics.

At intake Nimesulide is quickly soaked up in digestive tract. The maximum concentration in a blood plasma is reached in 2-3 hours. Linkng of Nimesulide with proteins of a blood plasma reaches 97,5%.

Drug is metabolized in a liver, a key product of metabolism is hydroxynimesulide – pharmacological active agent.

About 65% of the accepted dose of Nimesulide are allocated with urine, other 35% – with a stake.

Pharmaceutical characteristics

Main physical and chemical properties: tablets of yellowish or yellowish-greenish color with a biconvex surface. On a surface of tablets the mramornost is allowed.

Indications to use:

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

Route of administration and doses:

For the purpose of prevention of emergence and for weakening of manifestations of side reactions drug should be accepted throughout the smallest time and in minimum effective dose. It is necessary to appoint drug only after careful assessment of a ratio risk/advantage.

To accept drug inside after food and to wash down with enough liquid.

For adults and children 12 years – on 1 tablet (100 mg) 2 times a day – in the morning and are more senior in the evening.

The maximum duration of treatment – 15 days.

For patients of advanced age the specified scheme of dosing does not need correction.

For patients with easy or moderate degree of a renal failure (clearance of creatinine of 30-80 ml/min.) it is not necessary to adjust a dose.

Features of use:

It is necessary to apply minimum effective dose to decrease in risk of development of side effects with the smallest duration of a course of treatment. If the condition of the patient does not improve, treatment needs to be stopped.

In case of increase in levels of liver enzymes or identification of signs of injury of a liver (for example anorexia, nausea, vomiting, an abdominal pain, feeling of fatigue, urine of dark color) drug needs to be cancelled. Such patients and are forbidden to appoint further Nimesulide.

During treatment by Remesulid it is recommended to avoid simultaneous use of hepatotoxic drugs, analgetik, other non-steroidal anti-inflammatory drugs, and also to refrain from alcohol intake.

Gastrointestinal bleeding or ulcer/perforation can develop at any time at use of drug with the warning symptoms or without them both at gastrointestinal complications in the anamnesis, and without them. When developing gastrointestinal bleeding or ulcer drug should be cancelled.

For the patients having in the anamnesis the ulcer in a digestive tract which is especially complicated by bleeding or perforation and also at patients of advanced age and also for those which accept at the same time low doses of acetylsalicylic acid or other drugs increasing risk of emergence of complications from a digestive tract it is necessary to consider the possibility of use of a combination therapy using such drugs as мисопростол or inhibitors of a proton pomp.

The patients accepting the accompanying drugs which can increase risk of developing of an ulcer or bleeding such as corticosteroids, anticoagulants, selective serotonin reuptake inhibitors, antithrombocytic means (acetylsalicylic acid), it is necessary to inform on need to adhere to care at Nimesulide use.

With care patients should appoint Nimesulide with gastrointestinal disturbances, ulcer colitis or disease Krone in the anamnesis.

Patients with arterial hypertension and/or with heart failure in the anamnesis, and also patients with a liquid delay in an organism and hypostases owing to use of NPVS demand the corresponding control of a state and consultation of the doctor. Clinical trials and epidemiological data allow to draw a conclusion that some NPVS, especially in high doses and at prolonged use, can result in insignificant risk of emergence of arterial trombotichesky episodes, for example, to a myocardial infarction and a stroke. For an exception of risk of emergence of such phenomena at use of Nimesulide of data it is not enough. Patients with not controlled arterial hypertension, the acute heart failure established by coronary heart disease, diseases of peripheral arteries and/or cerebrovascular diseases Nimesulide should appoint after careful assessment of a state. Before purpose of drug it is also necessary to estimate carefully a condition of patients with risk factors of development of cardiovascular diseases, for example, at arterial hypertension, a lipidemia, a diabetes mellitus, when smoking.

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

At patients of advanced age side effects owing to administration of drug, including gastrointestinal bleedings, perforation, dysfunction of heart, kidneys and a liver therefore regular clinical control of a condition of the patient is recommended develop more often.

As Nimesulide can break function of thrombocytes at patients with hemorrhagic diathesis, it needs to be applied with care, under constant control.

Use of non-steroidal anti-inflammatory drugs can mask the fervescence connected with a background bacterial infection. At fervescence or emergence of grippopodobny symptoms it is necessary to stop administration of drug.

Drug contains lactose therefore patients with rare hereditary forms of intolerance of a galactose, insufficiency of Lapp-lactase or a syndrome of glyukozo-galaktozny malabsorption should not use drug.

Ability to influence speed of response at control of motor transport or work with other mechanisms

Influence of Nimesulide on ability to drive the car and to perform the works requiring special attention were not studied. However patients who after use of Nimesulide feel dizziness or drowsiness should refrain from driving and performance of the work requiring special attention.

Side effects:

From system of blood: anemia, eosinophilia, thrombocytopenia, pancytopenia, purpura.

From immune system: hypersensitivity, anaphylaxis.

Metabolic disturbances: hyperpotassemia.

From mentality: feeling of fear, nervousness, nightmares.

From a nervous system: dizziness, headache, drowsiness, encephalopathy (syndrome to Reja).

From organs of sight: sight illegibility.

From acoustic organs: вертиго (dizziness).

From cardiovascular system: tachycardia, hemorrhage, lability of arterial pressure, inflows, arterial hypertension.

From respiratory system: short wind, asthma, bronchospasm.

From a digestive tract: diarrhea, nausea, vomiting, a lock, a meteorism, gastritis, an abdominal pain, dyspepsia, stomatitis, excrements of black color, bleeding in a digestive tract, an ulcer and perforation of a duodenal gut / stomach.

From gepatobiliarny system: hepatitis, fulminant (fulminantny) hepatitis with a lethal outcome, jaundice, a cholestasia.

From skin: an itch, skin rashes, the increased perspiration, an erythema, dermatitis, urticaria, a Quincke's disease, a face edema, a poliformny erythema, Stephens-Johnson's syndrome, a toxic epidermal necrolysis.

From an urinary system: dysuria, hamaturia, urination delay, renal failure, oliguria, intersticial nephrite.

General disturbances: hypostases, indisposition, adynamy, hypothermia.

Laboratory indicators: increase in level of liver enzymes.

Interaction with other medicines:

Pharmakodinamichesky interactions.

Corticosteroids: the risk of developing of an ulcer of a digestive tract or bleeding increases.

Antithrombocytic means and the selection inhibitors of repeated serotonin reuptake: the risk of developing of bleedings in a digestive tract increases.

Anticoagulants: NPVS can strengthen effect of anticoagulants, such as warfarin or acetylsalicylic acid therefore such combination is not recommended or is contraindicated to patients with heavy disorders of coagulation. If such combination therapy cannot be avoided, it is necessary to carry out careful control of indicators of a blood coagulation.

Diuretic means, inhibitors of an angiotensin-converting enzyme and antagonists of angiotensin - ІІ: NPVS can reduce effect of diuretics and other anti-hypertensive drugs. At some patients with the worsened function of kidneys (for example at patients with dehydration or elderly people) combined use of APF inhibitors, antagonists of angiotensin ІІ or the substances oppressing system of cyclooxygenase, perhaps further deterioration in function of kidneys and developing of an acute renal failure which, as a rule, happens reversible. These interactions need to be considered when the patient applies Nimesulide together with APF inhibitors or antagonists of angiotensin ІІ. It is necessary to be very careful, applying such combination, especially to elderly people. Patients need to receive enough liquid, and renal function should be controlled carefully after the beginning of use of such combination. Nimesulide temporarily reduces effect of furosemide on sodium removal, to a lesser extent – on removal of potassium and reduces diuretic effect. Simultaneous use of furosemide and Nimesulide demands care from patients with disturbance of renal or cordial function.

Pharmacokinetic interactions with other medicines.

There were messages that NPVS reduce clearance of lithium that leads to increase in level of lithium in plasma and toxicity of lithium. At purpose of Nimesulide the patients receiving therapy by lithium drugs need to carry out often control of level of lithium in a blood plasma.

There is no clinically significant interaction with glibenclamide, theophylline, warfarin, digoxin, Cimetidinum and antiacid drugs (a combination of aluminum and magnesium of hydroxide). Nimesulide oppresses activity of CYP2C9 enzyme. At simultaneous use with Nimesulide of the drugs which are substrates of this enzyme, their concentration in a blood plasma can increase. Care is necessary in case Nimesulide is appointed less than in 24 hours to or less than in 24 hours after reception of a methotrexate as increase in level of the last in blood serum and increase in its toxicity is possible.

Tolbutamidum, salitsilov acid and valproic acid force out Nimesulide from binding sites. However, despite possible influence on drug level in a blood plasma, these interactions are not considered as clinically significant.

Contraindications:

The known hypersensitivity to Nimesulide or to any component of drug. The Giperergichesky reactions taking place in the past (a bronchospasm, rhinitis, urticaria) in connection with use of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs; the hepatotoxic reactions to Nimesulide taking place in the past; stomach ulcer and a duodenum in an aggravation phase, recurrent ulcers or bleedings in a digestive tract, gastrointestinal bleeding in the anamnesis, cerebrovascular bleedings or bleedings the accompanying other diseases; heavy disturbances of a blood coagulation; heavy heart failure; heavy renal failure (clearance of creatinine <30 ml/min.); liver failure; the increased body temperature and grippopodobny symptoms, suspicion of acute surgical pathology. Not to apply along with other drugs which can potentially be the cause of hepatotoxic reactions. Alcoholism and drug addiction.

Overdose:

Symptoms. At overdose apathy, drowsiness, a lethargy, nausea, vomiting, pain in epigastric area is observed, there can also be gastrointestinal bleeding, arterial hypertension, an acute renal failure, respiratory depression, anaphylactoid reactions and a coma.

Treatment. There is no specific antidote. In case of overdose it is necessary to carry out a symptomatic and maintenance therapy. Patients for 4 hours need to wash out a stomach, to accept absorbent carbon (60-100 g for adults) and an osmotic purgative. The artificial diuresis, increase in alkalinity of urine, a hemodialysis and hemoperfusion can be inefficient because of high extent of linkng of Nimesulide with proteins of a blood plasma. Careful control of function of kidneys and a liver is necessary.

Use during pregnancy or feeding by a breast

 

Pregnancy. Use of drug is contraindicated in the III trimester of pregnancy.

Use of Nimesulide can break female fertility, it is not recommended to be applied to the women planning pregnancy. As well as other non-steroidal anti-inflammatory drugs oppressing synthesis of prostaglandins, Remesulid can cause premature closing of a botalovy channel, pulmonary hypertensia, an oliguria, an oligoamnios. The risk of development of bleeding, an atony of a uterus and peripheral hypostases increases. Considering also lack of data on drug use to pregnant women, Remesulid in I and II trimesters of pregnancy is not recommended to appoint.

Feeding by a breast. As it is unknown whether Nimesulide gets into breast milk, its use is contraindicated during feeding by a breast.

Children

Drug протипоказан to children up to 12 years.

Storage conditions:

Term godnosti.5 years. Not to use drug after the termination of the period of validity specified on packaging. To store in the place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister. On 1 or 3 blisters in a pack.