Nonsteroidal anti-inflammatory and anti-rheumatic preparations.
Treatment of acute pain. symptomatic treatment of osteoarthritis with pain. primary dysmenorrhea.
Known hypersensitivity to nimesulide or to any component of the preparation. hyperergic reactions that have occurred in the past (bronchospasm, rhinitis, urticaria) due to the use of acetylsalicylic acid or other nonsteroidal anti-inflammatory preparations; hepatotoxic reactions to nimesulide that have occurred in the past; gastric and duodenal ulcers in the acute phase, recurrent ulcers or bleeding in the digestive tract, cerebrovascular bleeding or other lesions accompanied by bleeding; severe coagulation disorders; severe heart failure; severe renal or hepatic failure; fever and flu-like symptoms, suspicion of acute surgical pathology. do not use concomitantly with other preparations that could potentially cause hepatotoxic reactions. alcoholism and preparation addiction.
excipients: lactose, monohydrate; potato starch; microcrystalline cellulose; colloidal anhydrous silica; calcium stearate.
Nimesulide is prescribed after a careful benefit / risk assessment. apply the minimum effective dose for the shortest time. the maximum duration of nimesulide treatment is 15 days.
Adults and the elderly: 1 tablet (100 mg) 2 times a day (daily dose - 200 mg).
Children older than 12 years: no dose adjustment is required.
Patients with renal impairment: no dose adjustment is required for patients with mild or moderate renal impairment (creatinine clearance 30-80 ml / min). Take the preparation orally after a meal and drink plenty of fluids.
Adverse reactions.
The frequency of adverse events is classified as follows: very common (1/10), common (1/100, 1/1000, 1 / 10,000,
From the blood system: rarely - anemia, eosinophilia; very seldom - thrombocytopenia, pancytopenia, purpura.
From the immune system: rarely - hypersensitivity; very rarely - anaphylaxis.
Metabolic disorders: rarely - hyperkalemia.
From the psyche: rarely - a feeling of fear, nervousness, nightmares.
From the nervous system: sometimes - dizziness; very rarely - headache, drowsiness, encephalopathy (Reye's syndrome).
From the organs of vision: rarely - blurred vision.
From the hearing organs: very rarely - vertigo (dizziness).
From the cardiovascular system: rarely - tachycardia, hemorrhage, lability of blood pressure, hot flashes; sometimes - arterial hypertension.
From the respiratory system: sometimes - shortness of breath; very rarely - asthma, bronchospasm.
From the digestive tract: often - diarrhea, nausea, vomiting; sometimes - constipation, flatulence, gastritis; very rarely - abdominal pain, dyspepsia, stomatitis, black stools, bleeding in the digestive tract, ulcers and perforation of the duodenum / stomach.
From the hepatobiliary system: very rarely - hepatitis, lightning-fast (fulminant) hepatitis with fatal outcome, jaundice, cholestasis.
From the skin: sometimes - itching, skin rashes, sweating; rarely - erythema, dermatitis; very rarely - urticaria, angioneurotic edema, facial edema, erythema polyp, Stevens-Johnson syndrome, toxic epidermal necrolysis.
From the urinary system: rarely - dysuria, hematuria, urinary retention; very rarely - renal failure, oliguria, interstitial nephritis.
General disorders: sometimes - edema; rarely - malaise, asthenia; very rarely - hypothermia.
Laboratory indicators: often - increase in level of liver enzymes.
Overdose.
Symptoms of acute overdose with nonsteroidal anti-inflammatory preparations (NSAIDs) are usually limited to the following manifestations: apathy, drowsiness, nausea, vomiting, epigastric pain. these symptoms are usually reversible with maintenance therapy. possible occurrence of gastrointestinal bleeding, hypertension, acute renal failure, respiratory depression, coma, but such phenomena are rare. Anaphylactoid reactions have been reported with therapeutic doses of NSAIDs and overdose. there is no specific antidote. treatment of overdose - symptomatic and supportive. There are no data on the excretion of nimesulide by hemodialysis, but if we take into account the high degree of binding of nimesulide to plasma proteins (up to 97.5%), it is unlikely that dialysis will be effective. in the presence of symptoms of overdose or after administration of a large dose of the preparation for 4 hours after taking it, patients may be prescribed: artificial induction of vomiting, and / or activated charcoal (60-100 g for adults) and / or osmotic laxative. forced diuresis, increased urinary alkalinity, hemodialysis and hemoperfusion may be ineffective due to the high degree of binding of nimesulide to plasma proteins. kidney and liver function should be monitored.
Use during pregnancy or breastfeeding.
The use of nimesulide may increase female fertility and is not recommended for women who are planning to become pregnant. Nimesulide is not recommended for women who have difficulty conceiving or are undergoing infertility testing.
The use of Nimesulide is contraindicated in the third trimester of pregnancy.
Like other NSAIDs, Nimesulide is not recommended for use in women who are planning to become pregnant.
Like other NSAIDs that inhibit prostaglandin synthesis, nimesulide can cause premature closure of the botal duct, pulmonary hypertension, oliguria, and dehydration. The risk of bleeding, weakness of labor and peripheral edema increases. There have been isolated reports of renal failure in neonates born to women who used nimesulide in late pregnancy.
In the first and second trimesters of pregnancy the preparation is not used.
As it is not known whether nimesulide is excreted in human milk, its use is not recommended during breast-feeding.
Where are you.
Nimesulide is not used in children under 12 years of age.
Features of application.
Nimesulide should be used only as a second-line preparation. the decision to prescribe nimesulide should be made based on an assessment of all risks to the individual patient.
Undesirable side effects can be minimized by taking the least effective dose for the shortest period of use required to control the symptoms of the disease. In the absence of effective treatment (reduction of symptoms), preparation therapy should be discontinued. Cases of severe hepatic reactions, including fatalities, have been reported with nimesulide. Patients who have experienced symptoms similar to those of hepatic impairment during treatment with Nimesulide, such as anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine, or patients who have abnormal liver function tests, should stop using the preparation. Re-administration of nimesulide to such patients is contraindicated. Other analgesics should be avoided during treatment with Nimesulide. Concomitant use of other NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided. Patients who have used nimesulide and who have symptoms similar to the flu or cold should discontinue it. Elderly patients have an increased incidence of adverse reactions to NSAIDs, especially with regard to possible bleeding and perforation in the digestive tract, which can be fatal for the patient. Ulcers, bleeding or perforation in the digestive tract can be life-threatening, especially if there is evidence that the patient has had similar symptoms with any other NSAIDs (without a statute of limitations). The risk of such phenomena increases with increasing dose of NSAIDs in patients with a history of gastrointestinal ulcers, especially complicated by bleeding or perforation, as well as in elderly patients. Such patients should start treatment with the lowest possible effective dose. For these patients, as well as those taking concomitant low doses of acetylsalicylic acid or other preparations that increase the risk of gastrointestinal complications, the use of combination therapy with preparations such as misoprostol or proton pump inhibitors should be considered. Patients with toxic gastrointestinal lesions, especially the elderly, should be informed of any unusual symptoms occurring in the gastrointestinal tract, especially bleeding. This is especially important in the early stages of treatment. Patients taking concomitant medications that may increase the risk of ulceration or bleeding, such as corticosteroids, anticoagulants, selective serotonin reuptake inhibitors, antiplatelet agents (acetylsalicylic acid), should be advised to use the product. In case of bleeding or gastrointestinal ulcers in patients receiving Nimesulide, treatment with the preparation should be discontinued. NSAIDs should be used with caution in patients with Crohn's disease or a history of nonspecific ulcerative colitis, as nimesulide may exacerbate them. Patients with a history of hypertension and / or heart failure, as well as patients with fluid retention and edema due to NSAIDs, require appropriate monitoring and consultation with a physician. Clinical studies and epidemiological data suggest that some NSAIDs, especially in high doses and with long-term use, may lead to a small risk of arterial thrombotic episodes, such as myocardial infarction and stroke. To exclude the risk of such phenomena when using nimesulide data are not enough. Nimesulide should be prescribed to patients with uncontrolled hypertension, acute heart failure, established coronary heart disease, peripheral arterial disease and / or cerebrovascular disease after careful assessment. It is also necessary to carefully assess the condition of patients with risk factors for cardiovascular disease, such as hypertension, hyperlipidemia, diabetes mellitus, smoking, before prescribing the preparation. Patients with renal or heart failure should be prescribed the preparation with caution due to possible deterioration of renal function. In case of deterioration, treatment should be discontinued. Careful clinical monitoring should be performed in the elderly due to the possible development of bleeding and perforation of the digestive tract, deterioration of renal, liver or heart function. Because nimesulide may affect platelet function, it should be used with caution in patients with hemorrhagic diathesis. However, nimesulide does not replace acetylsalicylic acid in the prevention of cardiovascular disease. Nimesulide should be discontinued at the first signs of skin rash, mucosal lesions and other allergic reactions.
In case of fever or flu-like symptoms in patients taking nimesulide, the preparation should be discontinued.
Ability to influence the speed of reaction when driving a car or working with other mechanisms.
The effect of nimesulide on the ability to drive and perform tasks requiring increased attention has not been studied. however, patients who experience dizziness or drowsiness after taking nimesulide should refrain from driving and performing work that requires special attention.
Interaction with other preparations and other types of interactions.
Pharmacodynamic interactions.
Corticosteroids: Increased risk of gastrointestinal ulceration or bleeding.
Antiplatelet agents and selective serotonin reuptake inhibitors (SSSRIs): Increases the risk of gastrointestinal bleeding.
Anticoagulants: NSAIDs may increase the effect of anticoagulants such as warfarin or acetylsalicylic acid, so this combination is not recommended or contraindicated in patients with severe coagulation disorders. If such combination therapy cannot be avoided, careful monitoring of blood coagulation should be performed.
Diuretics, angiotensin-converting enzyme inhibitors and angiotensin-II antagonists: NSAIDs may reduce the effects of diuretics and other antihypertensive preparations. In some patients with impaired renal function (eg, dehydrated or elderly patients), the general use of ACE inhibitors, angiotensin II antagonists, or cyclooxygenase inhibitors may further impair renal function and lead to acute renal failure, which usually reversible. These interactions should be considered when the patient is co-administering Nimesulide with ACE inhibitors or angiotensin II antagonists. You need to be very careful when using this combination, especially for the elderly. Patients should receive adequate fluid intake and renal function should be closely monitored after initiating such a combination. Nimesulide temporarily reduces the effect of furosemide on sodium excretion, to a lesser extent on potassium excretion and reduces the diuretic effect. Concomitant use of furosemide and nimesulide requires caution in patients with impaired renal or cardiac function.
Pharmacokinetic interactions with other preparations.
NSAIDs have been reported to reduce lithium clearance, leading to increased plasma lithium levels and lithium toxicity. When administering Nimesulide to patients receiving lithium therapy, plasma lithium levels should be monitored frequently.
There is no clinically significant interaction with glibenclamide, theophylline, warfarin, digoxin, cimetidine and antacids (combination of aluminum and magnesium hydroxide). Nimesulide inhibits the activity of the enzyme CYP2C9. When co-administered with Nimesulide preparations that are substrates of this enzyme, their concentration in plasma may increase. Caution should be exercised when nimesulide is administered less than 24 hours before or less than 24 hours after methotrexate administration, as there may be an increase in serum methotrexate and an increase in its toxicity.
Pharmacological properties.
Pharmacodynamics.
Nimesulide is a non-steroidal anti-inflammatory preparation of the methanesulfonanilide group, which has anti-inflammatory, analgesic and antipyretic effects. The therapeutic effect of Nimesulide is due to the fact that it interacts with the arachidonic acid cascade and reduces the biosynthesis of prostaglandins by inhibiting cyclooxygenase.
Pharmacokinetics.
In humans, nimesulide is well absorbed when taken orally, reaching maximum plasma concentrations in 2-3 hours. Up to 97.5% of nimesulide binds to plasma proteins. Nimesulide is actively metabolized in the liver by CYP2C9, an isoenzyme of cytochrome P450. The major metabolite is a parahydroxy derivative, which also has pharmacological activity. The half-life is from 3.2 to 6 hours.
Nimesulide is excreted in the urine - about 50% of the dose. About 29% of the dose is excreted in the feces in a metabolized form. Only 1-3% is excreted unchanged. The pharmacokinetic profile in the elderly does not change.
Pharmaceutical characteristics.
Basic physical and chemical properties: solid, round cylinders, the upper and lower surfaces of which are flat, the edges of the surfaces are beveled, without a dash for division, light yellow, marble is allowed on the surface.
Storage conditions.
Store in the original package at a temperature not exceeding 25 ° C.