Nimesil granules for the preparation of suspensions 2 g 30 pcs
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Active ingredients
Nimesulide
Release form
Granules
Composition
In 1 bag (2 g): Active ingredient: nimesulide - 100 mg; Excipients: macrogol cetostearyl ether - 8.0 mg, sucrose - 1805.05 mg, maltodextrin - 15.0 mg, anhydrous citric acid - 30.0 mg , orange flavoring - 42.0 mg.
Pharmacological effect
Nonsteroidal anti-inflammatory drug from the class of sulfonamides. 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
Nimesulide is well absorbed from the gastrointestinal tract (GIT). The maximum plasma concentration (Cmax) after oral administration of a single dose of nimesulide, 100 mg, reaches an average of 2 to 3 hours and is 3-4 mg / l. The area under the curve "concentration - time" (AUC) - 20-35 mg h / l. Communication with plasma proteins - 97.5%. Metabolized in the liver with the help of 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 eliminated from the body, mainly with urine (about 50% of the dose taken), about 29% is excreted in the metabolized form of feces. The half-life (T1 / 2) is 3.2-6 hours. The pharmacokinetic profile of nimesulide in elderly patients and in patients with mild to moderate renal insufficiency does not change with the administration of single and multiple / repeated doses. A study conducted in patients with mild to moderate renal insufficiency (creatinine clearance 30-80 ml / min), Сmax of nimesulide and its main metabolite were not higher than in healthy volunteers. AUC and T1 / 2 observed were 50% higher, but were within the limits of AUC and T1 / 2 values observed in healthy volunteers with nimesulide. Repeated use did not lead to cumulation of nimesulide.
Indications
- acute pain (pain in the back, lower back; pain in the musculoskeletal system, including bruises, sprains and dislocations of the joints; tendenitis,bursitis; toothache); - symptomatic treatment of osteoarthritis (osteoarthritis) with pain; - primary algomenorrhea. The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use; nimesulide recommends for therapy as a second-line drug.
Contraindications
- a history of hyperergic reactions, for example, bronchospasm, rhinitis, urticaria, associated with the intake of acetylsalicylic acid or other NSAIDs, including nimesulide; - hepatotoxic reactions to nimesulide in history; - concomitant (simultaneous) medication with potential hepatotoxicity, for example, paracetamol or other analgesic or nonsteroidal anti-inflammatory drugs; - inflammatory bowel disease (Crohn's disease, nonspecific ulcerative colitis); period after coronary artery bypass surgery; - fever in infectious and inflammatory diseases; - full or partial combination of bronchial asthma, etsidiviruyuschego nasal polyposis or paranasal sinuses intolerant of aspirin and other NSAIDs (including history) - gastric ulcer and duodenal ulcer in an exacerbation phase, the presence of a history of ulcers, perforation or bleeding in the gastrointestinal tract; - Presence a history of cerebro vascular bleeding or other bleeding, as well as bleeding disorders; severe coagulation disorders; severe heart failure; severe renal failure (CC <30 m / Min) and confirmed hyperkalemia; - hepatic failure or any active liver disease; - children up to 12 years - during pregnancy and breastfeeding - alcoholism, drug addiction; - hypersensitivity to the drug.
Precautionary measures
Severe forms of arterial hypertension, type 2 diabetes, heart failure, coronary heart disease, cerebrovascular diseases, dyslipidemia / hyperlipidemia, peripheral artery disease, smoking, CC <60 ml / min, anamnestic data on the presence of ulcerative lesions of the gastrointestinal tract, infectionscaused by Helicobacter pylori; elderly age; prolonged prior use of NSAIDs; severe somatic diseases; concomitant therapy 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, fluoxetine, sertraline). should be based on an individual assessment of the risk-benefit when taking the drug. The drug is contraindicated in liver failure or any active liver disease. In patients with renal insufficiency, Nimesil should be used with caution, as renal function may deteriorate. In case of deterioration, treatment with Nimesil must be stopped. The drug is contraindicated in severe renal failure (CC <30 ml / min). In patients with mild and moderate forms of renal failure (CC 30-80 ml / min), there is no need to adjust the dose. The drug is prescribed with caution in elderly patients. Elderly patients are particularly susceptible to adverse reactions to NSAIDs, including the occurrence of gastrointestinal bleeding and perforations that threaten the patient’s life, deterioration of kidney, liver and heart function. When taking the drug Nimesil for this category of patients, proper clinical monitoring is necessary. When treating elderly patients, the need for adjusting the daily dose is determined by the doctor based on the possibility of interaction with other drugs.
Use during pregnancy and lactation
Like other NSAID drugs that inhibit prostaglandin synthesis, nimesulide can adversely affect pregnancy and / or embryo development and can lead to premature closure of the ductus arteriosus, hypertension in the pulmonary artery system, impaired kidney function, which can develop renal failure with oliuria in the fetus, to increase the risk of bleeding, reduce uterine contractility, the occurrence of peripheral edema in the mother. The data obtained during epidemiological studies investigations indicate a possible increase in the risk of spontaneous abortion, the risk of heart disease and gastroschisis when using agents that block prostaglandin synthesis in early pregnancy.The absolute risk of developing an abnormality of the cardiovascular system increases from about 1% to 1.5%. It is believed that the risk increases with increasing dose and duration of use. There is no data on the penetration of nimesulide into breast milk. The use of Nimesil during pregnancy and during breastfeeding is contraindicated. The use of nimesulide may adversely affect female fertility and is not recommended for women planning pregnancy. When planning a pregnancy, consultation with your doctor is necessary.
Dosage and administration
Inside The contents of the bag are poured into a glass and dissolved in approximately 100 ml of water at room temperature (a suspension of white or light yellow color is formed). The prepared solution cannot be stored. The Nimesil preparation is used only for treating patients over 12 years old. Adults and children over 12 years old: by 1 sachet twice a day, after meals. Elderly patients: when treating older patients, the need for adjusting the daily dose is determined by the doctor based on the possibility of interaction with other drugs. Patients with renal insufficiency: Patients with mild to moderate severity (creatinine clearance 30-60ml / min) do not need dose adjustment, while Nimesil is contraindicated in patients with severe renal insufficiency (creatinine clearance <30 ml / min) Patients with liver failure: The use of the drug Nimesil in patients with liver failure is contraindicated. To reduce the likelihood of side effects, it is recommended to take the minimum effective dose for min. Imno short time. The maximum daily dose for adults and children over 12 years old is 200 mg. The maximum duration of the course of treatment is 15 days.
Side effects
The frequency is classified by category in accordance with the recommendations of the World Health Organization, depending on the occurrence of the case: very often (≥ 1/10), often (≥ 1/100, <1/10), infrequently (≥ 1/1000, <1 / 100), rarely (≥ 1/10000, <1/1000), very rarely (<1/10000), including individual messages. Disorders of the blood and lymphatic system Rare: anemia, eosinophilia, hemorrhage; Very rare: thrombocytopenia, pancytopenia,thrombocytopenic purpura. Immune system disorders. Rarely: hypersensitivity reactions; Very rare: anaphylactoid reactions. Disorders of the skin and subcutaneous tissues. Not often: itching, skin rash, excessive sweating; Rarely: erythema, dermatitis; Very rare: rash, excessive sweating; Rarely: erythema, dermatitis; , erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome). Nervous system disorders. Often: dizziness; Very rare: headache, drowsiness, encephalopathy (syn Rei's rum). Psychiatric DisordersRadko: feeling of fear, nervousness, nightly "nightmarish" dreams. Disorders of the organ of visionRedko: blurred vision; Very rare: visual impairment. Disorders of the organ of hearing and labyrinth disordersVery rare: vertigo. Disorders of the heart vascular system Infrequently: high blood pressure; Rarely: tachycardia, blood pressure lability, blood flushes to the skin of the face, feeling of heartbeat. Disorders of the respiratory system Frequently: shortness of breath; Very rare: exacerbation of b ronchial asthma, bronchospasm. Disorders of the gastrointestinal tract Frequently: diarrhea, nausea, vomiting; Infrequently: constipation, flatulence, gastritis, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenal ulcer; Very rare: pain in the stomach, discomfort, or stomach or duodenum perforation; Very rare: pain in the stomach, discomfort, or stomach or duodenum perforation; Very rare: pain in the stomach, discomfort, or stomach or duodenum perforation; Very rare: pain in the stomach, discomfort, or stomach or duodenum perforation; Very rare: pain in the stomach, discomfort, / or stomach or duodenum perforation; Very rare: pain in the stomach, discomfort, or stomach or duodenum perforation; Very rare: pain in the stomach, discomfort, / or perforation of the stomach or duodenum , stomatitis, tarry stools. Disorders of the liver and biliary system. Frequently: increased activity of “liver” enzymes; Very rarely: hepatitis, fulminant (fulminant) hepatitis (including deaths), jaundice, cholestasis. Disorders of the kidneys and m chevyvodyaschey sistemyRedko: dysuria, hematuria, urinary retention; Very rarely, renal failure, oliguria, interstitial nefrit.Narusheniya with the water-electrolyte obmenaRedko: giperkaliemiya.ProchieNechasto: peripheral edema; Rare: malaise, asthenia; Very rarely hypothermia.
Overdose
Symptoms: apathy, drowsiness, nausea, vomiting, pain in the epigastric region. With the maintenance therapy of gastropathy, these symptoms are usually reversible. Gastrointestinal bleeding may occur.In rare cases, there may be an increase in blood pressure, acute renal failure, respiratory depression and coma, anaphylactoid reactions. Treatment: symptomatic therapy is carried out. There is no specific antidote. In the event that an overdose occurred within the last 4 hours, it is necessary to induce vomiting and / or ensure the intake of activated charcoal (adults 60 to 100 g) and / or osmotic laxative. Forced diuresis, hemodialysis are ineffective due to the high association of the drug with proteins (up to 97.5%). Control of kidney and liver function is shown.
Interaction with other drugs
Pharmacodynamic interactions: When used together with glucocorticosteroids, the risk of gastrointestinal ulcers or bleeding increases. When used in conjunction with anti-platelet agents and selective serotonin reuptake inhibitors (SSRIs), for example, fluoxetine increases the risk of gastrointestinal bleeding. 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 combination therapy cannot be avoided, careful monitoring of blood clotting parameters is necessary. ingestion of nimesulide and furosemide results in a decrease (approximately by 20%) of the area under the concentration-time curve (AUC) and a decrease in the cumulative excretion of furosemide without changing renal clearance furomesida.Sovmestnoe nimesulide administration of furosemide and requires caution in patients with impaired renal function and serdtsa.Ingibitory ACE and angiotensin II receptor antagonists: NSAIDs can reduce the effect of antihypertensive agents. In patients with mild and 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), further deterioration of renal function and the occurrence 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 intake of these drugs should be prescribed with caution, especially for elderly patients. Patients should receive a sufficient amount of fluid, and renal function should be carefully monitored after initiating joint therapy. Pharmacokinetic interactions with other drugs: There is evidence that NSAIDs reduce lithium clearance, which leads to an increase in plasma lithium concentration and toxicity. When nimesulide is prescribed to patients receiving lithium therapy, they should regularly monitor plasma lithium concentrations. Clinically significant interactions with glibenclamide, theophylline, digoxin, cimetidine, and antiacid drugs (for example, a combination of aluminum and magnesium hydroxides) were not observed. None inhibit activity . While taking drugs with nimesulide, which are the substrates of this enzyme, the concentration of these drugs in plasma may increase. When prescribing nimesulide less than 24 hours before or after taking methotrexate, be careful, because in such cases the level of methotrexate in plasma and, accordingly, The toxic effects of this drug may increase. Due to the effect on renal prostaglandins, prostaglandin synthetase inhibitors, such as nimesulide, may increase nephrotoxicity of cyclo porinov.Vzaimodeystvie nimesulide with other drugs: studies in vitro demonstrated that nimesulide is displaced from binding sites tolbutamide, salicylic acid and valproic acid. Despite the fact that these interactions were identified in the blood plasma, these effects were not observed during the clinical use of the drug.
special instructions
Undesirable side effects can be minimized by using the minimum effective dose of the drug for the shortest possible course. Nimesil should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn's disease),since exacerbation of these diseases is possible. The risk of gastrointestinal bleeding, ulcer or perforation of the ulcer increases with an increase in the NSAID dose in patients with a history of ulcer, especially complicated by bleeding or perforation, as well as in elderly patients, so treatment should be started with the lowest doses. Patients receiving drugs that reduce blood clotting or inhibit platelet aggregation also increase the risk of gastrointestinal bleeding. In the event of gastrointestinal bleeding or ulcers in patients taking Nimesil, treatment with the drug should be discontinued. Because Nimesil is partially excreted by the kidneys, its dosage for patients with impaired renal function should be reduced, depending on the level of urination. from the liver. If there are signs of liver damage (itching, yellowing of the skin, nausea, vomiting, abdominal pain, dark urine, increased activity of hepatic transaminases), you should stop taking the drug and contact your doctor. Despite the rarity of visual impairment in patients taking Nimesulide simultaneously with other NSAIDs, treatment should be immediately discontinued. If any visual impairment occurs, the patient should be examined by an optometrist. The drug may cause fluid retention in the tissues, so Nimesil should be used with extreme caution in patients with high blood pressure and cardiac activity. Nimesil should be used in patients with renal or heart failure with caution, since there may be a deterioration in kidney function. In case of deterioration, treatment with Nimesil must be discontinued. Clinical studies and epidemiological data suggest that NSAIDs, especially in high doses and with prolonged use, can lead to a slight risk of myocardial infarction or stroke. To exclude the risk of such events when using nimesulide, there is not enough data. The preparation contains sucrose, this should be taken into account for patients with diabetes mellitus (0.15-0.18 XE per 100 mg of the drug) and people on a low-calorie diet.Nimesil is not recommended for patients with rare hereditary diseases of fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltose insufficiency. If symptoms of a cold or acute respiratory viral infection occur during treatment with Nimesil, the drug should be discontinued. NSAIDs. Nimesulide may alter the properties of platelets, so care must be taken when using the drug in people with hemorrhagic However, the drug does not replace the prophylactic effect of acetylsalicylic acid in cardiovascular diseases. Older patients are particularly susceptible to adverse reactions to NSAIDs, including the occurrence of gastrointestinal bleeding and performations that threaten the patient’s life, deterioration of renal function, liver and heart. When taking the drug Nimesil for this category of patients, proper clinical control is required. Like other NSAID drugs that inhibit prostaglandin synthesis, nimesulide can adversely affect pregnancy and / or embryo development and can lead to premature closure of the arterial duct, hypertension in the system pulmonary artery, impaired renal function, which can turn into renal failure with oligodiramine, increase the risk of bleeding, reduce contractility of ma ki, the emergence of peripheral edema. In this regard, nimesulide is contraindicated during pregnancy and lactation. The use of the drug Nimesil may adversely affect female fertility and is not recommended for women planning a pregnancy. When planning a pregnancy, consultation with your doctor is necessary. There are data on the occurrence in rare cases of skin reactions (such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) on nimesulide as well as on other NSAIDs. At the first signs of skin rash, mucous membranes or other signs of an allergic reaction, Nimesil should be stopped. 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 treatment with the drug Nimesil should be careful when driving motor vehicles and pursuing potentially hazardous activities,requiring increased concentration and speed of psychomotor reactions.