Nysulide dispersible tablets 100mg, No. 20

• Acute pain (pain in the back, lower back; pain in the musculoskeletal system, including bruises, sprains and dislocations of the joints; tendinitis, bursitis; toothache);

• symptomatic treatment of osteoarthritis (osteoarthritis) with pain syndrome;

• primary algomenorrhea.

• The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use; Nimesulide is recommended for therapy as a second-line drug.

For oral administration. Place the tablet on your tongue, the tablet will dissolve quickly and you can swallow it without water.

Adults and children over 12 years of age inside (body weight over 40 kg) are prescribed 100 mg 2 times a day.

It is taken after meals. If necessary, the tablet can be taken with a sufficient amount of water. The maximum daily dose for adults and children over 12 years of age is 200 mg.

Elderly patients: When treating elderly patients, the daily dose adjustment is not required.

Patients with renal impairment:

In patients with mild to moderate renal insufficiency (creatinine clearance 30-60 ml / min), dose adjustment is not required, in patients with severe renal insufficiency (creatinine clearance less than 30 ml / min) nimesulide is contraindicated.

Patients with hepatic impairment:

The use of nimesulide in patients with hepatic impairment is contraindicated. Treatment course: as prescribed by a doctor. To reduce the likelihood of side effects, it is recommended to take the minimum effective dose for the shortest possible time. The maximum duration of the course of treatment with nimesulide is 15 days.

1 tablet contains:

active substance: nimesulide 100 mg;

excipients: microcrystalline cellulose, corn starch, pregelatinized corn starch, colloidal silicon dioxide (aerosil), citric acid monohydrate, sodium carboxymethyl starch, type A, aspartame, talc, magnesium stearate, pineapple flavor.

• Hypersensitivity to nimesulide or other components of the drug;

• a history of hyperergic reactions (bronchospasm, rhinitis, urticaria) associated with the use of acetylsalicylic acid or other NSAIDs, including nimesulide;

• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses with intolerance to acetylsalicylic acid and other NSAIDs (including a history); - history of hepatotoxic reactions to nimesulide;

• simultaneous use with other drugs with potential hepatotoxicity (for example, other NSAIDs);

• chronic inflammatory bowel diseases (Crohn's disease, ulcerative colitis) in the acute phase;

• period after coronary artery bypass grafting;

• febrile syndrome with colds and acute respiratory viral infections;

• suspicion of acute surgical pathology;

• peptic ulcer of the stomach or duodenum in the acute phase;

• erosive and ulcerative lesions of the gastrointestinal tract; a history of perforation or gastrointestinal bleeding;

• history of cerebrovascular bleeding or other diseases accompanied by increased bleeding;

• severe bleeding disorders;

• severe heart failure;

• severe renal impairment (creatinine clearance <30 ml / min), confirmed hyperkalemia;

• children under 12 years of age;

• pregnancy and the period of breastfeeding;

• alcoholism, drug addiction;

• liver failure, active liver disease.

  Carefully

• Arterial hypertension, diabetes mellitus, compensated heart failure, ischemic heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, peripheral arterial disease, hemorrhagic diathesis, smoking, creatinine clearance 30-60 ml / min. History of ulcerative lesions of the gastrointestinal tract; a history of Helicobacter pylori infection; elderly age; long-term previous use of NSAIDs; severe somatic diseases. Simultaneous use with the following drugs: anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, fluoxinetine, serotraline).

Pharmacodynamics

Nimesulide is a non-steroidal anti-inflammatory drug from the sulfonamide class. It has anti-inflammatory, analgesic and antipyretic effects. Unlike non-selective NSAIDs, nimesulide mainly inhibits cyclooxygenase-2 (COX-2), inhibits the synthesis of prostaglandins in the inflammation focus; has a less pronounced inhibitory effect on cyclooxygenase-1 (COX-1).

Pharmokinetics

Nimesulide is well absorbed from the gastrointestinal tract (GIT). The maximum concentration in blood plasma (Cmax) after oral administration of a single dose of nimesulide, which is 100 mg, is reached on average after 2 to 3 hours and is 3-4 mg / l. The area under the concentration-time curve (AUC) is 20-35 mg h / l. Communication with blood plasma proteins - up to 97.5%. It is metabolized in the liver by the cytochrome P450 isoenzyme (CYP) 2C9. The main metabolite is the pharmacologically active parahydroxy derivative of nimesulide - hydroxynimesulide, which is found exclusively in the form of glucuronate. Nimesulide is excreted from the body mainly in the urine (about 50% of the dose taken); in the metabolized form, about 29% is excreted in the feces. The half-life (T1 / 2) is 3.2-6 hours.The pharmacokinetic profile of nimesulide in the elderly and in patients with mild to moderate renal insufficiency does not change with the use of single and multiple / repeated doses. In a study conducted in patients with mild to moderate renal insufficiency (creatinine clearance 30-80 ml / min), Cmax of nimesulide and its main metabolite were not higher than in healthy volunteers. AUC and T1 / 2 were 50% higher, but were within the AUC and T1 / 2 values ??observed in healthy volunteers while using nimesulide. Repeated use did not lead to cumulation of nimesulide.conducted in patients with renal insufficiency of mild and moderate severity (creatinine clearance 30-80 ml / min), Cmax of nimesulide and its main metabolite were not higher than in healthy volunteers. AUC and T1 / 2 were 50% higher, but were within the AUC and T1 / 2 values ??observed in healthy volunteers while using nimesulide. Repeated use did not lead to the cumulation of nimesulide.conducted in patients with mild and moderate renal failure (creatinine clearance 30-80 ml / min), the Cmax of nimesulide and its main metabolite were not higher than in healthy volunteers. AUC and T1 / 2 were 50% higher, but were within the AUC and T1 / 2 values ??observed in healthy volunteers while using nimesulide. Repeated use did not lead to cumulation of nimesulide.

Overdose

Symptoms: apathy, drowsiness, nausea, vomiting, epigastric pain. These symptoms are usually reversible with symptomatic and supportive therapy. Perhaps an increase in blood pressure, the occurrence of gastrointestinal bleeding, acute renal failure, respiratory depression, coma, anaphylactoid reactions. Treatment: symptomatic and supportive therapy. There is no specific antidote. In case an overdose has occurred within the last 4 hours, it is necessary to induce vomiting and / or provide the intake of activated charcoal (from 60 to 100 g per adult), and / or an osmotic laxative. Forced diuresis, hemodialysis, hemoperfusion, urine alkalization are ineffective due to the high degree of binding of nimesulide to blood plasma proteins (up to 97.5%). It is necessary to monitor the state of kidney and liver function.

Side effects

Blood and lymphatic system disorders

Rarely: anemia, eosinophilia, hemorrhages; Very rare: thrombocytopenia, pancytopenia, thrombocytopenic purpura.

Immune system disorders

Rarely: hypersensitivity reactions; Very rare: anaphylactoid reactions.

Skin and subcutaneous tissue disorders

Uncommon: itching, skin rash, excessive sweating; Rarely: erythema, dermatitis; Very rare: urticaria, angioedema, facial edema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

Nervous system disorders

Uncommon: dizziness; Very rare: headache, drowsiness, encephalopathy (Reye's syndrome). Disorder of the psyche Rarely: a feeling of fear, nervousness, nightmare 'nightmares'.

Violations of the organ of vision

Rarely: blurred vision; Very rare: visual impairment.

Hearing and labyrinth disorders

Very rare: vertigo. Cardiovascular system disorders Uncommon: increased blood pressure; Rarely: tachycardia, lability of blood pressure, 'flushes' of blood to the skin of the face, palpitations.

Respiratory system disorders

Uncommon: shortness of breath; Very rare: exacerbation of bronchial asthma, bronchospasm.

Disorders from the gastrointestinal tract Often: diarrhea, nausea, vomiting; Uncommon: constipation, flatulence, gastritis, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenum; Very rare: abdominal pain, dyspepsia, stomatitis, tarry stools.

Liver and biliary tract disorders

Often: increased activity of 'liver' enzymes; Very rare: hepatitis, fulminant (fulminant) hepatitis (including deaths), jaundice, cholestasis.

Renal and urinary tract disorders Rarely: dysuria, hematuria, urinary retention; Very rare: renal failure, oliguria, interstitial nephritis.

Disturbances from water and electrolyte metabolism Rarely: hyperkalemia. Other Uncommon: peripheral edema; Rarely: malaise, asthenia; Very rare: hypothermia.

Special conditions

Undesirable side effects can be minimized by using the drug in the minimum effective dose with the minimum duration of use necessary to relieve pain. There is evidence of very rare cases of serious liver reactions, including deaths associated with the use of nimesulide-containing drugs.

If symptoms similar to signs of liver damage appear (anorexia, pruritus, yellowing of the skin, nausea, vomiting, abdominal pain, dark urine, increased activity of 'hepatic' transaminases), you should immediately stop using NaisulidЃ and consult a doctor. Repeated use of NaisulidЃ in such patients is contraindicated. Reported reactions from the liver, which in most cases are reversible, with short-term use of nimesulide. During the use of NaisulidЃ, the patient should refrain from taking other analgesics, including NSAIDs (including selective COX-2 inhibitors). The drug NaisulidЃ should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn's disease), since these diseases may exacerbate.The risk of gastrointestinal bleeding, peptic ulcer / perforation of the stomach or duodenum increases in patients with a history of ulcerative gastrointestinal lesions (ulcerative colitis, Crohn's disease), as well as in elderly patients, with an increase in the dose of NSAIDs, therefore, treatment should be started with the lowest possible dose. For such patients, as well as patients who require the simultaneous use of low doses of acetylsalicylic acid or other drugs that increase the risk of complications from the gastrointestinal tract, it is recommended to additionally prescribe the use of gastroprotective agents (misoprostol or proton pump blockers).Crohn's disease) in history, as well as in elderly patients, with an increase in the dose of NSAIDs, therefore, treatment should be started with the lowest possible dose. Such patients, as well as patients who require the simultaneous use of low doses of acetylsalicylic acid or other drugs that increase the risk of complications from the gastrointestinal tract, are advised to additionally prescribe gastroprotective agents (misoprostol or proton pump blockers).Crohn's disease) in history, as well as in elderly patients, with an increase in the dose of NSAIDs, therefore, treatment should be started with the lowest possible dose. For such patients, as well as patients who require the simultaneous use of low doses of acetylsalicylic acid or other drugs that increase the risk of complications from the gastrointestinal tract, it is recommended to additionally prescribe the use of gastroprotective agents (misoprostol or proton pump blockers).it is recommended to additionally prescribe the intake of gastroprotective agents (misoprostol or proton pump blockers).it is recommended to additionally prescribe the intake of gastroprotective agents (misoprostol or proton pump blockers).

Patients with a history of gastrointestinal disease, especially elderly patients, should inform the doctor about new gastrointestinal symptoms (especially about symptoms that may indicate possible gastrointestinal bleeding). NaisulidЃ should be used with caution in patients taking drugs that increase the risk of ulceration or bleeding (oral corticosteroids, anticoagulants such as warfarin, selective serotonin reuptake inhibitors, or antiplatelet agents such as acetylsalicylic acid).

In the event of gastrointestinal bleeding or ulcerative lesions of the gastrointestinal tract in patients taking NaisulidЃ, treatment with the drug should be discontinued. Given the reports of visual impairment in patients taking other NSAIDs, if any visual impairment occurs, the use of NaisulidЃ should be immediately discontinued and an ophthalmological examination should be performed. The drug can cause fluid retention, therefore, in patients with arterial hypertension, with renal and / or heart failure, NaisulidЃ should be used with extreme caution. If the condition worsens, treatment with NaisulidЃ should be discontinued. Clinical studies and epidemiological data suggest that NSAIDs, especially in high doses and with prolonged use,can lead to a negligible risk of myocardial infarction or stroke. There is insufficient data to exclude the risk of such events when using nimesulide.

If signs of a 'cold' or acute respiratory viral infection occur during the use of NaisulidЃ, the drug should be discontinued. Nimesulide can change the properties of platelets, therefore, care must be taken when using the drug in persons with hemorrhagic diathesis, however, the drug does not replace the prophylactic action of acetylsalicylic acid in cardiovascular diseases. Elderly patients are especially susceptible to adverse reactions to NSAIDs, including the risk of gastrointestinal bleeding and perforation, life-threatening the patient, and decreased kidney, liver and heart function. When taking NaisulidЃ for this category of patients, proper clinical control is required. There is evidence of rare cases of skin reactions (such as exfoliative dermatitis,Stevens-Johnson syndrome, toxic epidermal necrolysis) when taking NSAIDs, including nimesulide. At the first manifestations of a skin rash, mucosal lesions or other signs of an allergic reaction, NaisulidЃ should be discontinued immediately.

The effect of the drug on the ability to drive vehicles and other mechanisms

The effect of NaisulidЃ on the ability to drive vehicles and mechanisms has not been studied, therefore, during the period of using NaisulidЃ, care should be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Drug interactions

Glucocorticosteroids increase the risk of gastrointestinal ulcers or bleeding. Antiplatelet agents and selective serotonin reuptake inhibitors (SSRls), such as fluoxetine, increase the risk of gastrointestinal bleeding. NSAIDs can enhance the effects of anticoagulants such as warfarin. Due to the increased risk of bleeding, this combination is not recommended and is contraindicated in patients with severe coagulation disorders. If the combination therapy still cannot be avoided, it is necessary to carefully monitor the blood clotting parameters. Diuretics NSAIDs can reduce the effect of diuretics. In healthy volunteers, nimesulide temporarily reduces the excretion of sodium by furosemide, to a lesser extent - excretion of potassium and reduces the actual diuretic effect.The simultaneous use of nimesulide and furosemide leads to a decrease (by approximately 20%) in the area of ??the concentration-time curve (AUC) and a decrease in the cumulative excretion of furosemide without changing the renal clearance of furosemide. The simultaneous use of furosemide and nimesulide requires caution in patients with renal or heart failure. ACE inhibitors and angiotensin II receptor antagonists NSAIDs can reduce the effect of antihypertensive drugs. In patients with renal insufficiency of mild to moderate severity (creatinine clearance 30-80 ml / min) with the simultaneous use of ACE inhibitors, angiotensin II receptor antagonists and agents that suppress the cyclooxygenase system (NSAIDs, antiplatelet agents), further deterioration of renal function and the occurrence of acute kidney failure, which is usuallyis reversible. These interactions should be considered in patients taking nimesulide in combination with ACE inhibitors or angiotensin II receptor antagonists. Therefore, the simultaneous use of these drugs should be carried out with caution, especially in elderly patients. Patients should receive an adequate amount of fluid, and renal function should be closely monitored after the start of concomitant use. Mifepristone It is theoretically possible to reduce the effectiveness of mifepristone and prostaglandin analogs when used simultaneously with NSAIDs (including acetylsalicylic acid) due to the antiprostaglandin action of the latter. Limited data showthat the use of NSAIDs on the day of administration of a prostaglandin analog does not adversely affect the effect of mifepristone or a prostaglandin analog on cervical dilatation, uterine contractility, and does not reduce the clinical efficacy of medical abortion. There is evidence that NSAIDs reduce the clearance of lithium, which leads to an increase in the concentration of lithium in the blood plasma and its toxicity. When using nimesulide in patients on therapy with lithium preparations, regular monitoring of the concentration of lithium in the blood plasma should be carried out. Clinically significant interactions with glibenclamide, theophylline, digogsin, cimetidine and antacids (for example, a combination of aluminum and magnesium hydroxides) were not observed. Nimesulide inhibits the activity of the isoenzyme CYP2C9. With simultaneous use of drugs with nimesulide,being substrates of this enzyme, the concentration of the latter in plasma may increase. When prescribing nimesulide less than 24 hours before or after using methotrexate, caution is required, since in such cases, the concentration of methotrexate in the blood plasma and, accordingly, the toxic effects may increase. Due to the effect on renal prostaglandins, inhibitors of prostaglandin synthetases, which include nimesulide, can increase the nephrotoxicity of cyclosporins.Due to the effect on renal prostaglandins, inhibitors of prostaglandin synthetases, which include nimesulide, can increase the nephrotoxicity of cyclosporins.Due to the effect on renal prostaglandins, inhibitors of prostaglandin synthetases, which include nimesulide, can increase the nephrotoxicity of cyclosporins.