Naisulid powder for suspension for oral administration 100mg in 2.0g bags №10

Name:
Naisulid por.dprig.susp.dn.approx.100mg in pack.2.0g in pack No. 10
Description:
White or white with a yellowish tint powder with a specific odor. When 100 ml of carbon dioxide-free water (freshly boiled and cooled water) is added to the contents of the sachet, a white or light yellow suspension with a characteristic orange odor is obtained. The main active substance Nimesulide Form of release powder Dosage 100 mg Special instructions and precautions Undesirable effects can be minimized by using the lowest effective dose for the minimum time necessary to eliminate symptoms. If the patient’s condition does not improve, treatment should be discontinued. Elderly patients Elderly patients have an increased incidence of adverse reactions with NSAIDs, especially gastrointestinal bleeding and perforation (sometimes fatal), as well as an increased incidence of renal, hepatic and cardiac dysfunction. Therefore, appropriate close clinical monitoring is recommended. Concomitant therapy When using the drug Naisulid®, the simultaneous use of other NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided. You should refrain from taking other analgesics at the same time (see also the section “Interaction with other drugs and other forms of interaction”). Influence on the liver In rare cases, there may be serious reactions from the liver associated with the use of nimesulide-containing drugs, including in very rare cases with a fatal outcome. If symptoms or signs appear in patients taking nimesulide that may indicate liver damage and impaired liver function (for example, anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine, abnormal laboratory parameters characterizing liver function ), treatment with nimesulide should be discontinued. Such patients are not recommended to take nimesulide in the future. With a short-term use of the drug Naisulid®, liver damage is usually reversible. Patients who develop an increase in body temperature and / or other symptoms similar to the flu or a cold during the use of nimesulide should immediately stop using nimesulide. Gastrointestinal disorders Gastrointestinal bleeding, ulceration, or ulcer perforation may occur with any NSAID at various stages of treatment, regardless of the presence of warning symptoms or a history of gastrointestinal disease. Patients with any history of gastrointestinal involvement, especially elderly patients, should report any gastrointestinal symptoms. This is especially important in the early stages of treatment. With the development of ulcers, bleeding or other complications, nimesulide should be canceled. Gastrointestinal bleeding, ulceration and perforation of the ulcer that occur during the use of nimesulide can threaten the patient’s life, especially if a history (regardless of the elapsed time) shows the occurrence of such conditions during treatment with any NSAID with or without the presence of dangerous symptoms, or in the anamnesis there are indications of other serious violations of the gastrointestinal tract. The risk of gastrointestinal bleeding, ulcers, ulcer perforation is increased when taking high doses of nimesulide, as well as in patients with a history of ulcers, especially those complicated by bleeding or perforation, in the elderly. These patients should start treatment at the lowest dose. For these patients, as well as patients who are taking concomitantly low doses of aspirin or other drugs that increase the risk of gastrointestinal disease, consideration should be given to adding agents that protect the gastrointestinal mucosa from damage to the treatment regimen (for example, misoprostol or a proton pump inhibitor). Naisulid® should be used with caution in patients with gastrointestinal pathology, including peptic ulcer, history of gastrointestinal bleeding, ulcerative colitis and Crohn’s disease, due to the risk of exacerbation of these conditions. Also, it should be used with caution in patients taking other drugs that may increase the risk of ulceration or bleeding (eg, oral corticosteroids, anticoagulants (warfarin), selective serotonin reuptake inhibitors, antiplatelet agents (aspirin); see also the section “Interaction with other drugs means and other forms of interaction”). Skin reactions Very rare cases of severe skin reactions have been reported with NSAIDs (including exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis); such reactions can lead to death. Patients appear to be most at risk of developing skin reactions during the initial period of therapy. Naisulid should be discontinued at the first sign of skin rash, mucosal lesions and/or other hypersensitivity reactions. Impaired renal function In patients with renal or heart failure, nimesulide should be used with caution, since nimesulide may impair renal function. If the condition worsens, treatment should be discontinued. Cardiovascular and cerebrovascular effects It is necessary to monitor the condition of patients with arterial hypertension and / or with mild to moderate heart failure in history, since cases of fluid retention and edema have been reported during treatment with NSAIDs. Clinical studies and epidemiological data suggest that some NSAIDs, especially at high doses and with long-term use, may lead to a slight increase in the risk of pathological conditions associated with arterial thrombosis (for example, myocardial infarction or stroke). There are not enough data to exclude the risk of such conditions when using nimesulide. Patients with uncontrolled arterial hypertension, congestive heart failure, established coronary heart disease, peripheral arterial disease and / or cerebrovascular disease should be prescribed nimesulide after a thorough assessment of the condition and the benefit / risk ratio. Also, a thorough assessment of the condition and the benefit / risk ratio should be performed before starting long-term treatment in patients with risk factors for the development of cardiovascular disease (for example, arterial hypertension, hyperlipidemia, diabetes mellitus, smoking). Since nimesulide can affect platelet function, it should be used with caution in patients with hemorrhagic diathesis. Naisulid® cannot serve as a substitute for acetylsalicylic acid in the prevention of cardiovascular diseases. Influence on fertility The use of nimesulide can reduce female fertility, so it is not recommended to prescribe it to women planning a pregnancy. In women who have problems conceiving or who are being examined for infertility, the possibility of discontinuing nimesulide should be considered. Excipients Naisulid® contains sucrose (white crystalline sugar). This medicinal product should not be used in patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency. Due to the content of sucrose, the drug may have a negative effect on tooth enamel. Pharmacological properties Nimesulide is a non-steroidal anti-inflammatory drug with analgesic and antipyretic properties, which acts by inhibiting the cyclooxygenase enzyme involved in the synthesis of prostaglandins. When taken orally, it is well absorbed. Nimesulide is actively metabolized in the liver in various ways, including with the help of cytochrome P450 CYP2C9, the activity of which decreases, which can lead to an increase in plasma concentrations of drugs taken simultaneously with nimesulide and being, like nimesulide, a substrate of this isoenzyme. The main metabolite is the para-hydroxy form, which has pharmacological activity. Hydroxynimesulide is the only metabolite that can be found in plasma and is almost entirely in the conjugated state. Nimesulide is excreted mainly in the urine (approximately 50% of the administered dose). Only 1-3% is excreted unchanged. Approximately 29% of the administered substance is excreted after biotransformation with feces. The kinetic profile of nimesulide does not change in elderly patients with single and repeated injections. In an experimental study with mild to moderate renal impairment (creatinine clearance 30–80 ml/min), Cmax of nimesulide and its metabolites did not exceed the level in healthy volunteers. AUC and T1 / 2 were 50% higher, but always within the values observed with the use of nimesulide in healthy volunteers. Repeated use of the drug does not lead to cumulation. Contraindicated in patients with hepatic insufficiency. Indications for use Treatment of acute pain. Primary dysmenorrhea. Naisulid® can only be prescribed as a second-line therapy. The decision to prescribe nimesulide should be based on an overall risk assessment for each patient. Dosage and administration The drug is intended for oral administration. Before use, it is necessary to prepare a suspension. To do this, the contents of the package are dissolved in 100 ml of freshly boiled drinking water cooled to room temperature and shaken vigorously. After that, the suspension is ready for use; it must be taken immediately after preparation. Undesirable effects of therapy can be minimized by prescribing the lowest effective dose of the drug for the shortest possible period of time required to treat the disease in question. The maximum duration of taking nimesulide should not exceed 15 days. Adult patients: 1 sachet (100 mg nimesulide) 2 times a day after meals. Elderly patients: in the treatment of elderly patients, there is no need to reduce the daily dose. Children and adolescents Children (under 12 years of age): for this category of patients, the appointment of nimesulide-containing drugs is contraindicated (see section “Contraindications”). Adolescents (12 to 18 years): given the pharmacokinetic profile of nimesulide in adults and the pharmacodynamic characteristics of nimesulide, there is no need to adjust the dose 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 impairment (creatinine clearance 30 × 80 ml / min); in severe renal insufficiency (creatinine clearance < 30 ml / min), the drug is contraindicated (see section "Contraindications"), Patients with hepatic insufficiency: the drug is contraindicated in patients with hepatic insufficiency (see section "Contraindications"). If you have taken an overdose of the drug, immediately seek advice from your doctor or a doctor at the nearest medical institution (for example, a polyclinic or a hospital emergency department); at the same time, if possible, take with you the package with the drug and the leaflet for medical use (see section "Overdose"). Do not take a double dose to make up for a missed dose! Use during pregnancy and lactation Fertility Like other NSAIDs, nimesulide is not recommended for women planning a pregnancy (see also section "Special Instructions and Precautions"). Pregnancy Inhibition of prostaglandin synthesis can adversely affect the course of pregnancy, the development of the embryo / fetus, and the course of childbirth. Nimesulide, which inhibits prostaglandin synthetase, can lead to premature closure of the ductus arteriosus in the fetus, pulmonary hypertension, kidney dysfunction (which can progress to renal failure with oligohydramnios), and can also prolong bleeding time, inhibit uterine contractions. Data from epidemiological studies show an increased risk of miscarriage and heart disease following the use of prostaglandin synthesis inhibitors early in pregnancy. The risk is expected to increase with dose and duration of treatment. In animals, the use of inhibitors of prostaglandin synthesis led to an increase in pre- and post-implantation losses and fetal/embryo mortality. In addition, in animals after the introduction of prostaglandin synthesis inhibitors during organogenesis, an increased incidence of various malformations, including cardiovascular ones, was observed. Tests in rabbits have shown atypical reproductive toxicity. There are no data on the use of nimesulide in pregnant women. Therefore, the potential risk to humans cannot be reliably assessed and the use of nimesulide during pregnancy is contraindicated. Lactation It is not known whether nimesulide is excreted in breast milk. Therefore, its use is contraindicated during breastfeeding. Interaction with other drugs Pharmacodynamic interactions Other non-steroidal anti-inflammatory drugs (NSAIDs) The combined use of drugs containing nimesulide and other non-steroidal anti-inflammatory drugs, including acetylsalicylic acid in anti-inflammatory doses (? 1 g once or ? 3 g as a total daily dose), is not recommended . Corticosteroids Corticosteroids increase the risk of gastrointestinal ulcers or bleeding. Anticoagulants NSAIDs may increase the effect of anticoagulant agents such as warfarin. Due to the increased risk of bleeding, this combination is not recommended for patients receiving warfarin, acetylsalicylic acid, or other anticoagulant agents. This combination is contraindicated in patients with severe bleeding disorders. If combination therapy still cannot be avoided, careful monitoring of blood coagulation parameters should be carried out. Antiplatelet agents and selective serotonin reuptake inhibitors Antiplatelet agents and selective serotonin reuptake inhibitors increase the risk of gastrointestinal bleeding. Diuretics, angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor antagonists NSAIDs may reduce the effectiveness of diuretics and other antihypertensive drugs. In some patients with impaired renal function (for example, in patients with dehydration or in elderly patients), the co-administration of ACE inhibitors or angiotensin II receptor antagonists, as well as substances that suppress the cyclooxygenase system, can cause a further decrease in kidney function (up to acute renal failure). ), which is usually reversible. This interaction should be taken into account in patients taking Naisulid in conjunction with ACE inhibitors or angiotensin II receptor antagonists. When prescribing this combination, caution should be exercised, especially in elderly patients. Patients should be adequately hydrated and consideration should be given to monitoring renal function at the start of combination therapy and periodically thereafter. Pharmacokinetic interactions: effects of nimesulide on the pharmacokinetics of other drugs Furosemide In healthy volunteers, nimesulide temporarily reduced the effect of furosemide in terms of sodium excretion, to a lesser extent, in terms of potassium excretion, and also reduced the diuretic effect. Co-administration of nimesulide and furosemide leads to a decrease (approximately 20%) in the area under the concentration-time curve (AUC) and to a decrease in the cumulative excretion of furosemide without changing the renal clearance of furosemide. The co-administration of furosemide and drugs containing nimesulide requires caution in patients with impaired renal and / or cardiac function. Lithium There is evidence that NSAIDs reduce the clearance of lithium, which leads to an increase in the level of lithium in the blood plasma and, thus, to an increase in the likelihood of lithium toxicity. When prescribing the drug Nisulid® to patients receiving therapy with lithium-based drugs, frequent monitoring of the level of lithium in the blood plasma should be carried out. Methotrexate When prescribing nimesulide less than 24 hours before or less than 24 hours after taking methotrexate, care must be taken, since in such cases the plasma level of methotrexate and, accordingly, the toxic effects of this agent may increase. Cyclosporine In connection with the action on renal prostaglandins, prostaglandin synthetase inhibitors, which include nimesulide, may increase the nephrotoxicity of cyclosporine. Other agents In vivo studies have been conducted to identify possible pharmacokinetic interactions with glibenclamide, theophylline, warfarin, digoxin, cimetidine, and antacids (eg, a combination of aluminum hydroxide and magnesium hydroxide). No clinically significant interactions were observed. Nimesulide inhibits the activity of the CYP2C9 enzyme. With the simultaneous use of nimesulide and drugs that are substrates of this enzyme, the concentration of these drugs in the blood plasma may increase. Pharmacokinetic interactions: effects of other drugs on the pharmacokinetics of nimesulide In vitro studies have shown that nimesulide is displaced from the binding sites by tolbutamide, salicylic acid and valproic acid. Other than a possible effect on plasma levels, this interaction should not be of any clinical significance. Contraindications Known individual hypersensitivity to nimesulide and / or other components of the drug. History? hypersensitivity (for example, bronchospasm, rhinitis, urticaria, etc.) to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs. History? hepatotoxic reactions to nimesulide. Simultaneous use with other potentially hepatotoxic drugs. Liver failure. Severe renal impairment (creatinine clearance < 30 ml / min). Gastric or duodenal ulcer in the acute phase, recurrent ulcers or bleeding in the gastrointestinal tract in history, cerebral hemorrhages or other disorders accompanied by bleeding. Severe blood clotting disorders. Severe heart failure. Pregnancy and breastfeeding. Children under 12 years of age. Alcoholism, drug addiction. Fever and / or flu-like symptoms. Composition 2.0 g of powder contains 100 mg of nimesulide as an active ingredient. Excipients: maltodextrin, anhydrous citric acid, flavor Orange PX 1488, white crystalline sugar. Overdose Acute overdose of nimesulide can be manifested by lethargy, drowsiness, nausea and vomiting, pain in the epigastric region, which decrease with symptomatic treatment. Overdose can lead to gastrointestinal bleeding, rarely? to hypertension, acute renal failure, decreased respiratory activity and coma. In case of an overdose of nimesulide, symptomatic and supportive therapy is indicated. There is no specific antidote for nimesulide. There is no information on the excretion of nimesulide during hemodialysis, but since nimesulide is characterized by a high degree of binding to plasma proteins (97.5%), hemodialysis in the treatment of overdose is most likely useless. Due to the strong binding to plasma proteins, neither forced diuresis, urinary alkalinization, nor hemoperfusion are likely to be effective. If an overdose has occurred within the last 4 hours or an overdose of very high doses is observed, then vomiting should be induced and/or activated charcoal (60 x 100 g for adults) and/or an osmotic laxative should be taken. In case of overdose, the functions of the kidneys and liver should be carefully monitored. Side effectsAccording to the results of clinical studies and epidemiological data, the use of some NSAIDs, especially at high doses and for a long time, may be accompanied by a slight increase in the risk of developing pathologies caused by arterial thrombosis (for example, myocardial infarction or stroke). Edema, increased blood pressure, and heart failure have also been reported with NSAIDs. Very rare cases of severe skin reactions (including Steven-Jones syndrome and toxic epidermal necrolysis) have been reported with NSAIDs. In the treatment of NSAIDs, the most common adverse events were those of the gastrointestinal tract. Peptic ulcer, perforation, or gastrointestinal bleeding may develop, sometimes fatal, especially in elderly patients. There are reports of nausea, vomiting, diarrhea, flatulence, constipation, dyspepsia, abdominal pain, tarry stools, vomiting of blood, ulcerative stomatitis, exacerbation of colitis and Crohn's disease after taking the drug. Rarely observed gastritis. The following list of adverse reactions is based on the results of controlled clinical trials* (involving approximately 7800 people) and post-marketing experience. Reactions are distributed by type and by frequency of occurrence. The frequency of occurrence of possible adverse reactions is indicated as: very often (? 1/10); often (from? 1/100 to <1/10); infrequently (from? 1/1000 to <1/100); rarely (from? 1/10000 to <1/1000); very rare (< 1/10000), not known (frequency cannot be estimated from the available data). Blood and lymphatic system disorders: rare anemia*, eosinophilia*; very rarely ? thrombocytopenia, pancytopenia, purpura. Immune system disorders: rare ? hypersensitivity*; very rarely ? anaphylaxis. Metabolic and nutritional disorders: rare ? hyperkalemia*. Psychiatric disorders: rare? anxiety*, nervousness*, nightmares*. Nervous system disorders: Uncommon dizziness*, very rare ? headache, drowsiness, encephalopathy (Reye's syndrome). On the part of the organ of vision: rarely? blurred vision*; very rarely ? visual impairment. Hearing disorders and labyrinth disorders: very rarely? vertigo. Cardiac disorders: rare tachycardia*. Vascular disorders: infrequently? hypertension*, rare ? bleeding*, blood pressure lability*, hot flashes*. Respiratory, thoracic and mediastinal disorders: Uncommon dyspnea*; very rarely ? asthma, bronchospasm. Disorders from the gastrointestinal tract: often? diarrhea*, nausea*, vomiting*; infrequently ? constipation*, flatulence*, gastrointestinal bleeding, duodenal ulcer and perforation, gastric ulcer and its perforation; very rarely ? gastritis*, abdominal pain, dyspepsia, stomatitis, tarry stools (melena). Liver and biliary tract disorders: often? increased levels of liver enzymes*; very rarely ? hepatitis, fulminant (fulminant) hepatitis (including fatal cases), jaundice, cholestasis. Skin and subcutaneous tissue disorders: Uncommon itching*, rash*, increased sweating*; rarely ? erythema*, dermatitis*; very rarely ? urticaria, angioedema, facial edema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. Renal and urinary tract disorders: rare dysuria*, hematuria*; very rarely ? urinary retention*, renal failure, oliguria, interstitial nephritis. General disorders and disorders at the injection site: infrequently? edema*; rarely ? malaise*, asthenia*; very rarely ? hypothermia. *? the frequency is based on the results of clinical trials. Reporting adverse reactions If you experience any adverse reactions, it is recommended that you consult your doctor. This recommendation applies to any possible adverse reactions, including those not listed in the package insert for the use of the medicinal product. You can report adverse reactions directly to the Adverse Drug Reactions Information Database; you can also report the ineffectiveness of the drug. By reporting adverse reactions, you help to get more information about the safety of the medicine. Contraindications Known individual hypersensitivity to nimesulide and / or other components of the drug. History? hypersensitivity (for example, bronchospasm, rhinitis, urticaria, etc.) to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs. History? hepatotoxic reactions to nimesulide. Simultaneous use with other potentially hepatotoxic drugs. Liver failure. Severe renal impairment (creatinine clearance < 30 ml / min). Gastric or duodenal ulcer in the acute phase, recurrent ulcers or bleeding in the gastrointestinal tract in history, cerebral hemorrhages or other bleeding disorders. Severe blood clotting disorders. Severe heart failure. Pregnancy and breastfeeding. Children under 12 years old. light place at a temperature not exceeding 25 °C. Keep out of the reach of children. for oral administration 100mg in sachets 2.0g №10