Nimesil granules d / prig. solution 100mg, No. 30

• Treatment of acute pain (back pain, lower back pain; pain syndrome in the musculoskeletal system, including injuries, sprains and dislocations of joints, tendenitis, bursitis; toothache);

• symptomatic treatment of osteoarthritis with pain syndrome; algodismenorrhea.

• The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use.

Nimesil is taken orally, 1 sachet (100 mg of nimesulide) 2 times / day. The drug is recommended to be taken after meals. The contents of the sachet are poured into a glass and dissolved in about 100 ml of water. The prepared solution cannot be stored.

Nimesil is used only for the treatment of patients over 12 years old. Adolescents (aged 12 to 18 years): Based on the pharmacokinetic profile and pharmacodynamic characteristics of nimesulide, there is no need for dose adjustment in adolescents.

Patients with impaired renal function: based on pharmacokinetic data, there is no need to adjust the dose in patients with mild to moderate renal failure (CC 30-80 ml / min). Elderly patients: when treating elderly patients, the need to adjust the daily dose is determined by the doctor based on the possibility of interaction with other drugs.

The maximum duration of treatment with nimesulide is 15 days. To reduce the risk of unwanted side effects, the minimum effective dose should be used in a minimally short course.

Granules for the preparation of oral suspension in the form of a light yellow granular powder with an orange scent.

1 pack. (2 g)

nimesulide 100 mg

Excipients: ketomacrogol 1000, sucrose, maltodextrin, anhydrous citric acid, orange flavor.

• A history of hyperergic reactions, for example, bronchospasm, rhinitis, urticaria, associated with the intake of acetylsalicylic acid or other NSAIDs, incl. nimesulide;

• history of hepatotoxic reactions to nimesulide;

• concomitant (simultaneous) use of drugs with potential hepatotoxicity, for example, paracetamol or other analgesic or non-steroidal anti-inflammatory drugs;

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

• period after coronary artery bypass grafting;

• fever in infectious and inflammatory diseases;

• full or partial combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses with intolerance to acetylsalicylic acid and other NSAIDs (including a history);

• peptic ulcer of the stomach and duodenum in the acute phase, a history of ulcers, perforation or bleeding in the gastrointestinal tract;

• a history of cerebrovascular bleeding or other bleeding, as well as diseases accompanied by bleeding;

• severe blood clotting disorders;

• severe heart failure;

• severe renal failure (CC <30 ml / min), confirmed hyperkalemia;

• liver failure or any active liver disease;

• children under 12 years of age;

• pregnancy and the period of breastfeeding;

• alcoholism, drug addiction;

• hypersensitivity to the components of the drug.

  With care: severe forms of arterial hypertension, type 2 diabetes mellitus, heart failure, coronary heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, peripheral arterial disease, smoking, CC <60 ml / min, history of gastrointestinal ulceration, infection, caused by Helicobacter pylori; elderly age; long-term previous use of NSAIDs; severe somatic diseases; concomitant therapy with the following drugs: anticoagulants (eg warfarin), antiplatelet agents (eg acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (eg prednisolone), selective serotonin reuptake inhibitors (eg citalopram, fluoxetine), sertraline. The decision to prescribe the drug Nimesil should be based on an individual assessment 'risk-benefit 'when taking the drug.

pharmachologic effect

Non-steroidal anti-inflammatory drug from the sulfonamide class. It has anti-inflammatory, analgesic and antipyretic effects. Nimesulide acts as an inhibitor of the enzyme cyclooxygenase, which is responsible for the synthesis of prostaglandins, and inhibits mainly cyclooxygenase-2.

Pharmacokinetics

After oral administration, the drug is well absorbed from the gastrointestinal tract, reaching Cmax in blood plasma after 2-3 hours. Plasma protein binding is 97.5%. T1 / 2 is 3.2-6 hours. Easily penetrates the histohematogenous barriers. 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. Hydroxynimesulide is excreted in the bile in a metabolized form (found exclusively in the form of glucuronate - about 29%). Nimesulide is excreted from the body, mainly by the kidneys (about 50% of the dose taken). The pharmacokinetic profile of nimesulide in the elderly does not change with the appointment of single and multiple / repeated doses. According to a pilot study,conducted with the participation of patients with mild to moderate renal failure (CC 30-80 ml / min) and healthy volunteers, Cmax of nimesulide and its metabolite in the plasma of patients did not exceed the concentration of nimesulide in healthy volunteers. AUC and T1 / 2 in patients with renal insufficiency were 50% higher, but within the pharmacokinetic values. With repeated administration of the drug, cumulation is not observed.

Side effect

From the side of the hematopoietic system: rarely - anemia, eosinophilia, hemorrhagic syndrome; very rarely - thrombocytopenia, patitopenia, thrombocytopenic purpura.

Allergic reactions: infrequently - itching, rash, excessive sweating; rarely - hypersensitivity reactions, erythema, dermatitis; very rarely - anaphylactoid reactions, urticaria, angioedema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

From the side of the central nervous system: infrequently - dizziness; rarely - a feeling of fear, nervousness, nightmares; very rarely - headache, drowsiness, encephalopathy (Reye's syndrome).

From the side of the organ of vision: rarely - blurry vision.

From the side of the cardiovascular system: infrequently - arterial hypertension, tachycardia, lability of blood pressure, 'hot flashes'.

From the respiratory system: infrequently - shortness of breath; very rarely - exacerbation of bronchial asthma, bronchospasm.

From the digestive system: often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, dyspepsia, stomatitis, tarry stools, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenum; very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis, increased activity of liver enzymes.

From the urinary system: rarely - dysuria, hematuria, urinary retention; very rarely - renal failure, oliguria, interstitial nephritis.

General disorders: rarely - malaise, asthenia; very rarely - hypothermia. Others: rarely - hyperkalemia.

Application during pregnancy and lactation

Like other drugs of the NSAID class that inhibit the synthesis of prostaglandins, nimesulide can adversely affect the course of pregnancy and / or the development of the embryo and can lead to premature closure of the ductus arteriosus, hypertension in the pulmonary artery system, impaired renal function, which can turn into renal failure with oligodynamia, to an increased risk of bleeding, a decrease in uterine contractility, the occurrence of peripheral edema. In this regard, the drug is contraindicated during pregnancy and during breastfeeding.

Application for violations of liver function

The drug is contraindicated in liver failure or any active liver disease.

Application for impaired renal function

In patients with renal insufficiency, Nimesil should be used with caution, since renal function may deteriorate. If the condition worsens, treatment with Nimesil should be discontinued. The drug is contraindicated in severe renal failure (CC <30 ml / min). In patients with mild to moderate forms of renal failure (CC 30-80 ml / min), there is no need to adjust the dose.

Application in children

The drug is contraindicated in children under 12 years of age. Adolescents (aged 12 to 18 years): Based on the pharmacokinetic profile and pharmacodynamic characteristics of nimesulide, there is no need for dose adjustment in adolescents.

Use in elderly patients

The drug is prescribed with caution to elderly patients. Elderly patients are particularly susceptible to adverse reactions to NSAIDs, including the occurrence of gastrointestinal bleeding and life-threatening performances, and deterioration of kidney, liver and heart function. When taking the drug Nimesil for this category of patients, proper clinical control is required. When treating elderly patients, the need to adjust the daily dose is determined by the doctor based on the possibility of interaction with other drugs.

special instructions

Undesirable side effects can be minimized by using the minimum effective dose of the drug in the smallest possible short course. Nimesil should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn's disease), since an exacerbation of these diseases is possible. The risk of gastrointestinal bleeding, ulcers or perforation of the ulcer increases with an increase in the dose of NSAIDs in patients with a history of ulcers, especially complicated by bleeding or perforation, as well as in elderly patients, so treatment should be started with the lowest possible dose. Patients receiving drugs that reduce blood clotting or inhibit platelet aggregation also have an increased risk of gastrointestinal bleeding.In the event of gastrointestinal bleeding or ulcers in patients taking Nimesil, drug treatment should be canceled. Since Nimesil is partially excreted by the kidneys, its dosage for patients with impaired renal function should be reduced, depending on the level of urination. There is evidence of rare cases of liver reactions. If signs of liver damage appear (skin itching, yellowing of the skin, nausea, vomiting, abdominal pain, dark urine, increased activity of 'hepatic' transaminases), stop taking the drug and consult your doctor. Despite the rarity of visual impairment in patients taking nimesulide concurrently with other NSAIDs, treatment should be stopped immediately. If any visual impairment occurs,the patient should be examined by an ophthalmologist. The drug can cause fluid retention in the tissues, therefore, patients with high blood pressure and cardiac disorders should use Nimesil with extreme caution. In patients with renal or heart failure, Nimesil should be used with caution, since renal function may deteriorate. If the condition worsens, treatment with Nimesil should be discontinued. Clinical studies and epidemiological data suggest that NSAIDs, especially in high doses and with prolonged use, can lead to a small risk of myocardial infarction or stroke. There is insufficient data to exclude the risk of such events when using nimesulide. The composition of the drug includes sucrose, this should be taken into account by patients,suffering from diabetes mellitus (0.15-0.18 XE per 100 mg of the drug) and persons following a low-calorie diet. Nimesil is not recommended for patients with rare hereditary diseases of fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltose deficiency. If signs of a 'cold' or acute respiratory viral infection occur during treatment with Nimesil, the drug should be discontinued. Do not use Nimesil concomitantly with other NSAIDs. 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 particularly prone to adverse reactions to NSAIDs,including the occurrence of gastrointestinal bleeding and performations that threaten the patient's life, deterioration in the function of the kidneys, liver and heart. When taking the drug Nimesil for this category of patients, proper clinical control is required. Like other drugs of the NSAID class that inhibit the synthesis of prostaglandins, nimesulide can adversely affect the course of pregnancy and / or the development of the embryo and can lead to premature closure of the ductus arteriosus, hypertension in the pulmonary artery system, impaired renal function, which can turn into renal failure with oligodynamia, to an increased risk of bleeding, a decrease in uterine contractility, the occurrence of peripheral edema. In this regard, nimesulide is contraindicated during pregnancy and lactation.The use of the drug Nimesil can adversely affect female fertility and is not recommended for women planning pregnancy. When planning a pregnancy, it is necessary to consult with your doctor. There is evidence of the occurrence in rare cases of skin reactions (such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) to nimesulide as well as to other NSAIDs. At the first signs of a skin rash, damage to the mucous membranes or other signs of an allergic reaction, the use of Nimesil should be discontinued.toxic epidermal necrolysis) on nimesulide as well as on other NSAIDs. At the first signs of a skin rash, damage to the mucous membranes or other signs of an allergic reaction, the use of Nimesil should be discontinued.toxic epidermal necrolysis) on nimesulide as well as on other NSAIDs. At the first signs of a skin rash, damage to the mucous membranes or other signs of an allergic reaction, the use of Nimesil should be discontinued.

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

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

Overdose

Symptoms: apathy, drowsiness, nausea, vomiting, epigastric pain. These symptoms are usually reversible with maintenance therapy for gastropathy. Gastrointestinal bleeding is possible. In rare cases, an increase in blood pressure, acute renal failure, respiratory depression and coma, anaphylactoid reactions are possible. Treatment: symptomatic therapy is performed. There is no specific antidote. In the event that an overdose has occurred within the last 4 hours, it is necessary to induce vomiting and / or provide an intake of activated charcoal (adults from 60 to 100 g) and / or an osmotic laxative. Forced diuresis, hemodialysis are ineffective due to the high connection of the drug with proteins (up to 97.5%). Control of kidney and liver function is shown.

Drug interactions

Pharmacodynamic interactions: When used together with glucocorticosteroids, the risk of gastrointestinal ulcers or bleeding increases. When used together with antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs), for example, fluoxetine, the risk of gastrointestinal bleeding increases. 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 weaken the effect of diuretics. In healthy volunteers, nimesulide temporarily reduces sodium excretion by furosemide,to a lesser extent - excretion of potassium, and reduces the actual diuretic effect. Co-administration of nimesulide and furosemide leads to a decrease (by approximately 20%) in the area under the concentration-time curve (AUC) and a decrease in the cumulative excretion of furosemide without changing the renal clearance of furomeside. The joint appointment of furosemide and nimesulide requires caution in patients with impaired renal and cardiac function. ACE inhibitors and angiotensin II receptor antagonists: NSAIDs can reduce the effect of antihypertensive drugs. In patients with mild to moderate renal failure (CC 30-80 ml / min), with the joint appointment of ACE inhibitors, angiotensin II receptor antagonists or substances that suppress the cycloxygenase system (NSAIDs, antiplatelet agents),possible further deterioration of renal function and the emergence of acute renal failure, which is usually reversible. These interactions should be considered in patients taking Nimesil in combination with ACE inhibitors or angiotensin II receptor antagonists. Therefore, the joint administration of these drugs should be prescribed with caution, especially for elderly patients. Patients should receive adequate fluid intake, and renal function should be closely monitored after starting concomitant therapy. Pharmacokinetic interactions with other drugs: 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 nimesulide is prescribed to patients receiving lithium therapy,plasma lithium concentrations should be monitored regularly. Clinically significant interactions with glibenclamide, theophylline, digoxin, cimetidine and antacids (for example, a combination of aluminum and magnesium hydroxides) were not observed. Nimesulide inhibits the activity of the isoenzyme CYP2C9. With the simultaneous administration of drugs that are substrates of this enzyme with nimesulide, the concentration of these drugs in plasma may increase. When prescribing nimesulide less than 24 hours before or after taking methotrexate, caution is required, since in such cases, the plasma level of methotrexate and, accordingly, the toxic effects of this drug may increase. Due to the effect on renal prostaglandins, inhibitors of prostaglandin synthetases, which include nimesulide, can increase the nephrotoxicity of cyclosporins.Interaction of other drugs with nimesulide: In vitro studies have shown that nimesulide is displaced from the binding sites by tolbutamide, salicylic acid and valproic acid. Despite the fact that these interactions were determined in blood plasma, these effects were not observed during the clinical use of the drug.