Nimesil granules for susp. 100mg 2g pack. 9 pc

Description

Composition
Active substance:
1 sachet contains: 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.
Description:
Light yellow granular powder with an orange flavor.
Product form:
Granules for oral suspension, 100 mg.
2 g of granules in a three-layer bag [paper / aluminum foil / polyethylene].
At 9.15 and 30 bags with instructions for use in a cardboard package.
Contraindications
Hypersensitivity to nimesulide or other components of the formulation; hyperergic reaction history (bronchoconstriction, rhinitis, urticaria), associated with the use of aspirin or other NSAIDs, including nimesulide; complete or partial combination of asthma, recurrent nasal polyposis or paranasal sinuses intolerant of aspirin and other NSAIDs (including history); hepatotoxic reactions to nimesulide (history); simultaneous use with other drugs with potential hepatotoxicity (e.g., other NSAIDs); chronic inflammatory bowel disease (Crohn’s disease, ulcerative colitis) in acute phase; since the aortocoronary bypass surgery; febrile syndrome colds and acute respiratory viral infections; suspected acute surgical pathology; gastric ulcer or duodenal ulcer in the acute phase; erosive and ulcerative lesions of the gastrointestinal tract; perforation or gastrointestinal bleeding in history; cerebrovascular bleeding history or other diseases associated with excessive bleeding; severe blood coagulation disorders; severe heart failure; severe renal failure (creatinine clearance
Carefully
Arterial hypertension, diabetes, compensated heart failure, ischemic heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, peripheral arterial disease, hemorrhagic diathesis, smoking and creatinine clearance of 30-60 ml / min.
Ulcerative lesions of the gastrointestinal tract in history; infection caused by infection with Helicobacter pylori history; elderly age; long previous use of NSAIDs; severe somatic disease.
The simultaneous use of the following drugs: anticoagulant (e.g., warfarin), antiplatelet agents (e.g., aspirin, clopidogrel), oral corticosteroids (e.g., prednisone), selective serotonin reuptake inhibitor (such as citalopram, fluoxetine, paroxetine, sertraline).
Dosage
100 mg
Indications
Acute pain (pain in the back, waist, pain in the musculoskeletal system, including contusions, sprains, and dislocations of the joints, tendinitis, bursitis, toothache); imptomaticheskoe treatment of osteoarthritis (osteoarthritis), pain syndrome; Primary algomenorrhea.
The drug is intended for the symptomatic therapy reduce pain and inflammation at the time of use; nimesulide recommended for therapy as a second-line drug.
Interaction with other drugs
Corticosteroids increase the risk of gastrointestinal ulcers or bleeding.
Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs), e.g., fluoxetine, increases the risk of gastrointestinal bleeding.
NSAIDs can enhance the effect of anticoagulants, such as warfarin. Due to the increased risk of bleeding, such a combination is not recommended and is contraindicated in patients with severe coagulation disorders. If combination therapy still can not be avoided, it is necessary to carry out careful monitoring of blood coagulability.
diuretics
NSAIDs may reduce the effect of diuretics.
In healthy volunteers nimesulide temporarily reduces the excretion of sodium by the action of furosemide, to a lesser extent – potassium excretion, and actually reduces the diuretic effect.
The simultaneous use of nimesulide and furosemide results in a decrease (about 20%) of the area under the curve “concentration – time” (AUC) and the reduction of cumulative excretion of unchanged furosemide renal clearance of furosemide.
Concomitant use of Furosemide and nimesulide requires caution in patients with renal or heart failure.
ACE inhibitors and angiotensin-II receptor
NSAIDs can reduce the effect of antihypertensive drugs. In patients with renal insufficiency mild to moderate (creatinine clearance of 30-80 ml / min) while the use of ACE inhibitors, angiotensin II receptor antagonists and agents that suppress cyclooxygenase system (NSAIDs, antiplatelet agents) may further deterioration of kidney function and the occurrence of acute renal failure, which usually is 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 undertaken with caution, especially in elderly patients. Patients should receive adequate amounts of fluids, and renal function should be closely monitored after the start of the simultaneous application.
mifepristone
It is theoretically possible reduction in effectiveness of mifepristone and prostaglandin analogues while the use of NSAIDs (including acetylsalicylic acid) due to the action antiprostaglandinovogo latter. Limited data indicate that NSAIDs daily application of a prostaglandin analog has no adverse effect on the action of mifepristone or prostaglandin analogue in the cervix, uterine contractility and does not reduce the clinical efficacy of medical termination of pregnancy.
There is evidence that NSAIDs reduce the clearance of lithium, resulting in increased concentration of lithium in blood plasma and its toxicity. In the application of nimesulide in patients on lithium therapy treatment should regularly monitor the concentration of lithium in blood plasma.
Clinically significant interactions with glibenclamide, theophylline, digoxin, cimetidine, and antacids (such as aluminum and a combination of magnesium hydroxide) was observed.
Nimesulide inhibits isozyme CYP2C9. While the use of nimesulide drugs that are substrates of this enzyme in the plasma concentration of the latter can be increased.
When assigning nimesulide in less than 24 hours before or after requires careful methotrexate, since in such cases the MTX level in blood plasma and, accordingly, the toxic effects may increase.
In connection with the effect on renal prostaglandin, prostaglandin synthetase inhibitors, nimesulide relates to any, may enhance the nephrotoxicity of cyclosporin.
Overdose
Symptoms: lethargy, drowsiness, nausea, vomiting, epigastric pain. These symptoms are usually reversible during the symptomatic and supportive therapy. You may experience gastrointestinal bleeding. May increase the blood pressure, the occurrence of gastrointestinal bleeding, acute renal failure, respiratory depression, coma, anaphylactoid reactions.
Treatment: Symptomatic and supportive therapy. No specific antidote. If overdose has occurred during the last 4 hours necessary to cause emesis and / or ensure the reception of activated charcoal (60 to 100 g for an adult) and / or the osmotic laxative. Forced diuresis, hemodialysis, hemoperfusion, urinary alkalization inefficient due to the high degree of binding to proteins of nimesulide (to 97.5%). Necessary to monitor the state of the kidneys and liver.
pharmachologic effect
Pharmacological group:
Nonsteroidal anti-inflammatory drugs (NSAIDs).
Pharmacodynamics:
Nimesulide is a non-steroidal anti-inflammatory agent from the class of sulfonamides. It has anti-inflammatory, analgesic and antipyretic effect. In contrast, non-selective NSAIDs, nimesulide mainly inhibits cyclooxygenase-2 (COX-2) inhibits the synthesis of prostaglandins in inflammation; It has a less pronounced inhibitory effects on cyclooxygenase-1 (COX-1).
Pharmacokinetics:
Nimesulide is well absorbed from the gastrointestinal tract (GIT).
The maximum plasma concentration (Cmax) after oral administration of a single dose of nimesulide of 100 mg, on average reached after 2 – 3 hours, and at 3-4 mg / l. The area under the curve “concentration – time» (AUC) – 20-35 mg h / L. Communication with the plasma protein – 97.5%.
It is metabolized in the liver using isoenzyme of cytochrome P450 (CYP) 2C9. The major metabolite is pharmacologically active paragidroksiproizvodnoe nimesulide – hydroxynimesulide, which is found exclusively in the form of a glucuronate.
Nimesulide is excreted mainly in urine (about 50% of the dose) in the faeces metabolise the form displayed around 29%. The half-life (T1 / 2) is 3,2-6 hours.
The pharmacokinetic profile of Nimesulide in the elderly and in patients with renal insufficiency mild to moderate in severity individual does not change when assignment single and multiple / repeated doses.
From a study conducted in patients with mild and moderate renal severity of failure (creatinine clearance of 30-80 ml / min), Cmax nimesulide and its main metabolite were not higher than in healthy volunteers. AUC and T1 / 2 observed were 50% higher, but were in the range of values ​​of AUC and T1 / 2 observed in healthy volunteers during treatment with nimesulide. Repeated application did not lead to accumulation of nimesulide.
Pregnancy and breast-feeding
As with other drugs in the class of NSAIDs, which inhibit prostaglandin synthesis, nimesulide could adversely affect the course of pregnancy and / or embryo development, and may result in the premature closure of the ductus arteriosus, hypertension in the pulmonary fetal artery, renal dysfunction, which can move in renal failure with oliuriey the fetus to increased risk of bleeding, reduction in uterine contractility, peripheral edema in the mother.
The data obtained in epidemiological studies indicate a possible increase in risk of spontaneous abortion, the risk of heart disease and gastroschisis when applied early in pregnancy means that block the synthesis of prostaglandins. The absolute risk for cardiovascular abnormalities increases with about 1% to 1.5%. It is believed that the risk increases with the dose and duration of application.
Data on the penetration of nimesulide in breast milk is not available.
Use of the drug Nimesil® during pregnancy and lactation is contraindicated.
The use of nimesulide may negatively affect female fertility and is not recommended for women planning pregnancy. When planning a pregnancy should consult with a physician.
Conditions of supply of pharmacies
On prescription.
side effects
The frequency is classified by category in accordance with the recommendations of the World Health Organization, in the case of occurrence: very common (> 1/10), common (> 1/100, 1/1000, 1/10000,
Blood disorders and lymphatic system
Rare: anemia, eosinophilia, hemorrhage;
Very rare: thrombocytopenia, pancytopenia, thrombocytopenic purpura.
Violations by the immune system
Rarely: hypersensitivity reactions;
Very rare: anaphylactoid reactions.
Violations of the skin and subcutaneous tissue
Uncommon: pruritus, skin rash, excessive sweating;
Rare: erythema, dermatitis;
Very rarely, urticaria, angioedema, swelling of face, poliformnaya erythema, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome).
Disorders of the nervous system
Uncommon: dizziness;
Very rare: headache, somnolence, encephalopathy (Reye’s syndrome).
mental disorders
Rare: anxiety, nervousness, night “nightmarish” dream.
Violations by the organ of vision
Rare: blurred vision;
Very rare: blurred vision.
Violations by the organ of hearing and labyrinth disorders
Very rare: vertigo.
Violations of the cardiovascular system
Uncommon: increase in blood pressure;
Rare: tachycardia, labile blood pressure, “tides” of blood to the facial skin, palpitations.
Violations of the respiratory system
Uncommon: shortness of breath;
Very rare: aggravation of asthma, bronchospasm.
Disorders of the gastrointestinal tract
Common: diarrhea, nausea, vomiting;
Uncommon: constipation, flatulence, gastritis, gastrointestinal bleeding, ulcers and / or perforation of the stomach or duodenum;
Very rare: abdominal pain, dyspepsia, stomatitis, tarry stools.
Violations of the liver and biliary system
Often: increased activity of “liver” enzymes;
Very rare: hepatitis, fulminant (fulminant) hepatitis (including fatal outcomes), jaundice, cholestasis.
Violations of the kidneys and urinary system
Rare: dysuria, hematuria, urinary retention;
Very rare: renal insufficiency, oliguria, interstitial nephritis.
Violations by the water-electrolyte metabolism
Rare: hyperkalemia.
other
Uncommon: peripheral edema;
Rare: malaise, asthenia;
Very rare: hypothermia.
special instructions
The undesirable side effects can be minimized by applying the drug in the minimal effective dose with a minimum duration of application required for the relief of pain.
There is evidence of very rare cases, severe reactions on the part of the liver, including fatal cases associated with the use of drugs nimesulidosoderzhaschih. If you have symptoms that are similar to the symptoms of liver disease (anorexia, pruritus, yellowing of the skin, nausea, vomiting, abdominal pain, dark urine, increased activity of “liver” transaminases) should immediately stop using Nimesil® drug and consult a doctor. Repeated use of the drug Nimesil® contraindicated in these patients.
The reactions reported by the liver, with most of the reversible, short-term use at preparation.
During the drug Nimesil® patient should refrain from receiving other analgesics, including NSAIDs (including selective COX-2 inhibitors).
Nimesil® The drug should be used with caution in patients with gastrointestinal diseases in history (ulcerative colitis, Crohn’s disease), since it is possible aggravation of these diseases.
The risk of gastrointestinal bleeding, peptic ulcer / perforation of the stomach or duodenum is increased in patients with the presence of ulcerative lesions gastrointestinal (ulcerative colitis, Crohn’s disease), history, as well as in elderly patients, with increasing doses of NSAIDs, so treatment should begin with the lowest possible dose. These patients as well as patients who required the simultaneous use of low-dose acetylsalicylic acid or other agents which increase the risk of complications in the gastrointestinal tract, it is recommended to appoint further reception gastroprotectives (misoprostol or proton pump blockers). Patients with diseases of the gastrointestinal tract in history, especially elderly patients, should be reported to your doctor about the newly emerging symptoms of the gastrointestinal tract (especially about the symptoms, which may indicate possible gastrointestinal bleeding).
Nimesil® drug should be used with caution in patients receiving drugs that increase the risk of bleeding or expressions (oral corticosteroids, anticoagulants such as warfarin, selective serotonin reuptake inhibitors or antiplatelet agents such as acetylsalicylic acid).
In case of gastrointestinal bleeding or gastrointestinal ulceration in patients taking the drug imesil®, drug treatment should be discontinued immediately.
Taking into account the reports of visual disturbances in patients treated with other NSAIDs, with the appearance of any violation of Nimesil® use of the drug should be immediately discontinued and an ophthalmologic examination performed.
The drug can cause fluid retention in the tissue, so patients with hypertension, renal and / or heart failure, ischemic heart disease, peripheral arterial disease and / or cerebrovascular disease, the presence of risk factors for cardiovascular disease (for example, hyperlipidemia, diabetes, smokers) Nimesil® drug should be used with extreme caution. In the case of deterioration, the treatment should be discontinued drug Nimesil®.
The preparation includes sucrose, it should be considered for patients suffering from diabetes (0.15-0.18 XE 100 mg of the drug) and persons who observe a low-calorie diet. Nimesil® drug is not recommended for patients with intolerance to fructose, sucrose-isomaltose deficiency or glucose-galactose syndrome malabsorption.
If there are signs of “cold” or acute respiratory viral infection during use of the drug Nimesil® the drug should be discontinued.
Nimesulide can change the properties of platelets, so care must be taken when using the drug in patients with hemorrhagic diathesis, however, the drug does not replace the prophylactic effect of aspirin in cardiovascular diseases.
Elderly patients are particularly susceptible to adverse reactions to NSAIDs, including the risk of gastrointestinal bleeding and perforation, threatening the patient’s life, reduced kidney function, liver and heart. Before the drug Nimesil® for this category of patients is needed proper clinical management.
Имеются данные о возникновении в редких случаях кожных реакций (таких как эксфолиативный дерматит, синдром Стивенса-Джонсона, токсический эпидермальный некролиз) при приеме НПВП, в том числе и нимесулида. При первых проявлениях кожной сыпи, поражении слизистых оболочек или других признаках аллергической реакции прием препарата Нимесил® следует немедленно прекратить.
Влияние препарата на способность к управлению транспортными средствами и другими механизмами
Влияние препарата Нимесил® на способность к управлению транспортными средствами и механизмами не изучалось, поэтому в период лечения препаратом Нимесил® следует соблюдать осторожность при вождении автотранспорта и занятиях потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций.
Storage conditions
Store at a temperature not higher than 25 C.
Keep out of the reach of children!.
Dosing and Administration
Inside. Содержимое пакетика высыпают в стакан и растворяют примерно в 100 мл воды комнатной температуры (образуется суспензия белого или светло – желтого цвета).
Приготовленный раствор хранению не подлежит.
Препарат Нимесил® применяется только для лечения пациентов старше 12 лет.
Взрослым и детям старше 12 лет: по 1 пакетику два раза в сутки, после еды.
Пациенты пожилого возраста: при лечении пожилых пациентов необходимость корректировки суточной дозы определяется врачом исходя из возможности взаимодействия с другими лекарственными средствами.
Пациенты с почечной недостаточностью: у пациентов с почечной недостаточностью легкой и умеренной степени тяжести (клиренс креатинина 30-60 мл/мин) кореекции дозы не требуется, в то время как пациентам с тяжелой почечной недостаточностью (клиренс креатинина
Patients with hepatic insufficiency:
Применение препарата Нимесил® у пациентов с печеночной недостаточностью противопоказано.
Для уменьшения вероятности развития побочных эффектов рекомендуется принимать минимальную эффективную дозу в течение минимально короткого времени.
Максимальная суточная доза для взрослых и детей старше 12 лет составляет 200 мг.
Максимальная продолжительность курса лечения – 15 дней.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist