Nimika dispersible tablets 100 mg No. 10x2
Name
Nimika.
Release form
Dispersible tablets.
Dosage
100 mg. Quantity per package: 20 pcs.
Manufacturer
Ipka Laboratories Ltd.
INN
Nimesulide.
FTG
Npvp.
Compound
Each 100 mg dispersible tablet contains: Active substance: nimesulide 100.00 mg Excipients: corn starch 73.10 mg, microcrystalline cellulose 124.40 mg, colloidal anhydrous silica 4.00 mg, pregelatinized starch 12.00 mg, citric acid monohydrate 3.00 mg, talc 5.00 mg, sodium starch glycolate type A 3.00 mg, aspartame 10.00 mg, magnesium stearate 2.50 mg, fruit flavor 10.00 mg.
Description
Round, flat, beveled tablets, light yellow to yellow in color, scored on one side.
Pharmacotherapeutic group
Other nonsteroidal anti-inflammatory and antirheumatic drugs. ATS code: M01AX17.
Pharmacological properties
Pharmacodynamics Nimesulide is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties that acts as an inhibitor of the cyclooxygenase enzyme responsible for the synthesis of prostaglandins. Pharmacokinetics Nimesulide is well absorbed when taken orally. After taking a single dose of 100 mg of nimesulide, in adults the maximum plasma concentration is reached after 2-3 hours and is 3-4 mg/l. The area under the curve (AUC) is 20-35 mg h/l. When taking nimesulide at a dose of 100 mg once or twice a day for 7 days, no differences in pharmacokinetic properties were noted. Up to 97.5% of nimesulide binds to plasma proteins. Nimesulide is actively metabolized in the liver in various ways with the participation of the cytochrome P450 (CYP)2C9 isoenzyme. Therefore, in cases of combined use of nimesulide with medications that are metabolized with the participation of this isoenzyme, the possible occurrence of drug interactions should be taken into account. The main metabolite is the pharmacologically active parahydroxy derivative of nimesulide. The time until this metabolite is detected in the circulating blood is short (0.8 hours), but the amount of its formation is small and significantly less than the amount of absorption of nimesulide. Hydroxynimesulide is the only metabolite found in plasma. This metabolite is almost completely present in bound form. The half-life ranges from 3.2 to 6 hours. Nimesulide is excreted from the body mainly in the urine (about 50% of the dose taken). Only 1-3% is excreted unchanged. Hydroxynimesulide is the main metabolite, found exclusively in the form of glucuronate. Approximately 29% of the dose taken is excreted in metabolized form in the feces. The pharmacokinetic profile of nimesulide in elderly people does not change when single and multiple/repeated doses are prescribed. In a short-term experimental study involving patients with mild to moderate forms of renal failure (creatinine clearance 30-80 ml/min) and healthy volunteers, the maximum concentration of nimesulide and its main metabolite in the plasma of patients was no greater than the concentration in healthy volunteers. The area under the concentration-time curve (AUC) and half-life (t1/2 beta) in patients with renal impairment were 50% higher, but were always within the pharmacokinetic range observed in healthy volunteers taking nimesulide. Repeated administration of the drug did not lead to accumulation. Nimesulide is contraindicated in patients with liver failure.
Indications for use
Treatment of acute pain Primary dysmenorrhea Nimesulide can be prescribed only as a treatment and second line. The decision to prescribe nimesulide should be based on an overall risk assessment for each patient.
Contraindications
known hypersensitivity to nimesulide or one of the excipients. hyperergic reactions that have occurred in the past (bronchospasm, rhinitis, urticaria) in connection with taking acetylsalicylic acid or other NSAIDs. past hepatotoxic reactions to nimesulide. concomitant use of other substances with potential hepatotoxicity. alcoholism, drug addiction. Previous gastrointestinal bleeding or perforation associated with previous NSAID therapy. gastric or duodenal ulcer in the acute phase, a history of ulcers, perforation or bleeding in the gastrointestinal tract. a history of cerebrovascular bleeding or other hemorrhages, as well as diseases accompanied by bleeding. severe blood clotting disorders. severe heart failure. severe renal failure. liver failure. patients with cold or flu symptoms. age up to 12 years. The use of the drug is contraindicated in the third trimester of pregnancy and during breastfeeding.
Directions for use and doses
The minimum effective dose should be administered for the shortest possible period of time in order to minimize the risk of adverse reactions. The maximum duration of taking nimesulide should not exceed 15 days. Before use, the tablet should be dissolved in 5 ml (1 teaspoon) of water. Adult patients: 1 tablet (100 mg nimesulide) twice a day after meals. Elderly patients When treating 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 use of nimesulide-containing medications is contraindicated. Adolescents (12 to 18 years): Based on the pharmacokinetic profile in adults and the pharmacodynamic characteristics of nimesulide, no dose adjustment is necessary in adolescents. Patients with impaired renal function Based on pharmacokinetic data, there is no need for dose adjustment in patients with mild to moderate forms of renal failure (creatinine clearance 30-80 ml/min), while in patients with severe renal failure (creatinine clearance
Adverse reactions
Clinical studies and epidemiological data suggest that the use of some NSAIDs, especially in high doses over a long period of time, may be associated with a slight increase in the risk of arterial thrombosis (eg, myocardial infarction or stroke). Edema, increased blood pressure and heart failure have also been reported during treatment with NSAIDs. When using NSAIDs, there is evidence of very rare cases of bullous reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis. When treated with NSAIDs, the most common adverse events were gastrointestinal events. Peptic ulcers, perforation or gastrointestinal bleeding may develop, sometimes with fatal consequences, especially in elderly patients. There is information about the appearance of nausea, vomiting, diarrhea, flatulence, constipation, dyspepsia, abdominal pain, tarry stools, vomiting blood, ulcerative stomatitis, exacerbation of colitis and Crohn's disease after taking the drug. Gastritis is less common. The frequency of cases is classified as follows: very common (≥ 1/10), common (≥ 1/100,
Interaction with other drugs
Pharmacodynamic interactions Other NSAIDs: the combined use of nimesulide preparations 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: Increase the risk of gastrointestinal ulcers or bleeding. Anticoagulants: NSAIDs may enhance the effect of anticoagulants such as warfarin or acetylsalicylic acid. 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. Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs): This group of drugs increases the risk of gastrointestinal bleeding. Diuretics, angiotensin-converting enzyme inhibitors (ACEIs), angiotensin II receptor antagonists (AIIA) and 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), co-administration of ACE inhibitors or angiotensin II antagonists, as well as substances that suppress the COX system, can cause a further decrease in renal function up to acute renal failure, which is, as a rule, reversible in nature. This interaction should be taken into account in patients taking nimesulide together with an ACE inhibitor or AIIA. Therefore, caution should be exercised when prescribing this combination of drugs, especially in elderly patients. Patients should be kept adequately hydrated and the need to monitor renal function should be considered upon initiation of combination therapy and periodically thereafter. Effect of nimesulide on the pharmacokinetics of other drugs Furosemide: in healthy volunteers, nimesulide temporarily reduced the effect of furosemide on sodium excretion, to a lesser extent on potassium excretion, and also reduced the diuretic response. 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 furosemide. Co-administration of furosemide and nimesulide requires caution in patients with impaired renal or cardiac function. Lithium: There is evidence that NSAIDs reduce the clearance of lithium, resulting in increased plasma lithium levels and lithium toxicity. When prescribing nimesulide to patients receiving lithium therapy, plasma lithium levels should be monitored. In vivo studies were conducted to identify possible pharmacokinetic interactions with glibenclamide, theophylline, warfarin, digoxin, cimetidine and antacids (for example, combinations of aluminum and magnesium hydroxide). No clinically significant interactions were observed. Nimesudide inhibits the activity of the CYP2C9 enzyme. When taking 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 less than 24 hours after taking methotrexate, caution should be exercised, since in such cases the plasma level of methotrexate and, accordingly, the toxic effects of this drug may increase. Due to their effect on renal prostaglandins, inhibitors of prostaglandin synthesis, which include nimesulide, may increase the nephrotoxicity of cyclosporines. Influence of other substances on the pharmacokinetics of nimesulide In vitro studies have shown that nimesulide is displaced from binding sites by tolbutamide, salicylic acid and valproic acid. Although these interactions were determined in blood plasma, these effects were not observed during clinical use of the drug.
Overdose
Symptoms of acute overdose of NSAIDs are usually limited to the following: apathy, drowsiness, nausea, vomiting, pain in the epigastric region. These symptoms are usually reversible with supportive care. Gastrointestinal bleeding may occur. In rare cases, increased blood pressure, acute renal failure, respiratory depression and coma may occur. Anaphylactoid reactions have been reported when taking therapeutic doses of NSAIDs and when overdosing on such drugs. In case of NSAID overdose, treatment is symptomatic and supportive. There is no specific antidote. There is no data regarding the elimination of nimesulide by hemodialysis, however, based on the high level of binding to plasma proteins (up to 97.5%), it can be concluded that dialysis is ineffective in case of drug overdose. If there are symptoms of overdose or after taking a large dose of the drug, within 4 hours after administration, patients may be prescribed: inducing vomiting and/or taking activated charcoal (60-100 grams for adults) and/or taking an osmotic laxative. Forced diuresis, urine alkalinization, hemodialysis or hemoperfusion may be ineffective due to the high level of nimesulide binding to blood proteins. Kidney and liver function should be monitored.
Precautionary measures
Undesirable side effects can be minimized by using the lowest effective dose for the shortest duration necessary to control symptoms of the disease. If there is no improvement in symptoms, drug therapy should be discontinued. While taking nimesulide, concomitant use of other painkillers and NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided. Liver disorders Rare cases of serious liver reactions, including very rare cases of death, have been reported in association with the use of nimesulide-containing medicinal products. Patients who experience symptoms similar to those of liver damage (eg, anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine) while using the drug or patients whose liver function laboratory tests are abnormal, should discontinue treatment with the drug. Repeated administration of nimesulide is contraindicated in such patients. Liver damage, most reversible, has been reported after short-term exposure to the drug. Gastrointestinal Disorders As with other NSAIDs, potentially fatal gastrointestinal bleeding, ulceration, or perforation may occur at any time during treatment, with or without prior symptoms or a history of serious gastrointestinal disease. The risk of gastrointestinal bleeding, ulceration, or perforation of an ulcer increases with increasing doses of NSAIDs in patients with a history of ulcers, especially those complicated by hemorrhage or perforation, and in elderly patients. For these patients, treatment should be started with the lowest possible dose. For these patients, as well as patients taking concomitant low-dose aspirin or other drugs that increase the risk of gastrointestinal disease, combination therapy with protective agents (eg, misoprostol or proton pump inhibitors) should be considered. Patients with a history of gastrointestinal toxicity, especially the elderly, should report any unusual gastrointestinal symptoms (especially gastrointestinal bleeding), especially during the initial stages of treatment. Gastrointestinal bleeding, as well as the formation of ulcers or perforations, are observed for all NSAIDs at different stages of treatment, regardless of the presence of warning symptoms or a history of gastrointestinal pathology. If gastrointestinal bleeding or ulceration develops, nimesulide should be discontinued. Nimesulide should be administered with caution to patients with gastrointestinal diseases, including peptic ulcers, a history of gastrointestinal bleeding, ulcerative colitis and Crohn's disease. Patients taking concomitant medications that may increase the risk of ulceration or bleeding, such as oral corticosteroids, anticoagulants such as warfarin, selective serotonin reuptake inhibitors, or antiplatelet agents such as aspirin, should be advised to exercise caution when taking the drug facilities. If gastrointestinal bleeding or ulceration occurs in patients taking the drug, treatment should be discontinued. Elderly Patients Elderly patients have an increased incidence of adverse reactions to non-steroidal anti-inflammatory drugs, especially the incidence of gastrointestinal bleeding and perforation (even fatal in some cases), as well as impaired cardiac, renal and hepatic function. Therefore, appropriate clinical observation is recommended. Cardiovascular disorders and cerebrovascular effects Patients with a history of arterial hypertension and/or mild/moderate acute heart failure, as well as patients with fluid retention and edema as a reaction to the use of NSAID therapy, require appropriate monitoring and consultation. doctor Clinical studies or epidemiological data suggest that some NSAIDs, especially at high doses and with long-term use, may lead to a small risk of arterial thrombotic events (eg, myocardial infarction or stroke). There is insufficient data to exclude the risk of such events when using nimesulide. In patients with uncontrolled hypertension, congestive heart failure, established coronary artery disease, peripheral arterial disease and/or cerebrovascular disease, nimesulide should be prescribed after careful evaluation. An equally thorough assessment of the condition should be performed before starting long-term treatment in patients with risk factors for cardiovascular disease (for example, arterial hypertension, hyperlipidemia, diabetes mellitus, smoking). Since nimesulide can affect platelet function, it should be prescribed with caution to patients with bleeding diathesis. However, nimesulide does not replace acetylsalicylic acid in the prevention of cardiovascular diseases. Renal disorders Caution should be exercised when prescribing the drug to patients with impaired renal or cardiac function, since the use of nimesulide may lead to deterioration of renal function. If worsening occurs, treatment should be discontinued. Skin reactions There have been reports of very rare cases of severe skin reactions to NSAIDs, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis, some of which can be fatal. Patients appear to be at greatest risk of developing skin reactions during the initial period of therapy. The drug should be discontinued at the first manifestations of skin rash, damage to the mucous membranes and other signs of hypersensitivity. Effect on fertility The use of nimesulide can reduce female fertility, so it is not recommended for women planning pregnancy. In women who have problems conceiving or are undergoing examination for infertility, discontinuation of nimesulide should be considered. This medicine contains the phenylalanine source aspartame, which may be harmful to people with phenylketonuria.
Pregnancy and lactation
Inhibition of prostaglandin synthesis may adversely affect pregnancy and/or fetal development. Data obtained from epidemiological studies suggest that in early pregnancy, the use of drugs that suppress prostaglandin synthesis may increase the risk of spontaneous abortion, fetal heart disease and gastroschisis. The absolute risk of cardiovascular abnormality increased from less than 1% to approximately 1.5%. The risk is believed to increase with increasing dose and duration of use. In animals, administration of a prostaglandin synthesis inhibitor resulted in increased pre- and postimplantation losses and increased embryonic mortality. In addition, evidence was obtained that in animals receiving a prostaglandin synthesis inhibitor during the period of organogenesis, the incidence of various fetal malformations, including the cardiovascular system, increased. You should not take nimesulide during the first and second trimester of pregnancy unless absolutely necessary. When using the drug by women trying to become pregnant, or in the first and second trimester of pregnancy, the lowest possible dose and the shortest possible duration of treatment should be chosen. In the third trimester of pregnancy, all inhibitors of prostaglandin synthesis: can lead to the development in the fetus of: pneumocardial toxic damage (with premature closure of the arterial ducts and hypertension in the pulmonary artery system); renal dysfunction, which can progress to renal failure with the development of oligohydramnios; in the mother and fetus at the end of pregnancy it is possible: an increase in bleeding time, an antiaggregation effect that can occur even when using very low doses of the drug; suppression of contractile activity of the uterus, which can lead to a delay or prolongation of the period of labor. Therefore, nimesulide is contraindicated in the third trimester of pregnancy. Since it is unknown whether nimesulide is excreted into breast milk, use is contraindicated during breastfeeding. Features of use in children The use of nimesulide in children under 12 years of age is contraindicated
Impact on the ability to drive vehicles and operate machinery
Due to the fact that, when taken orally, nimesulide can cause dizziness and drowsiness in some patients, they should refrain from engaging in potentially hazardous activities that require increased concentration.
Release form
Dispersible tablets 100 mg 10 tablets per blister Aluminum/Aluminium. 2 blisters along with instructions for use are placed in a cardboard pack.
Storage conditions
Store in a place protected from moisture and light at temperatures below 25°C. Keep out of the reach of children.
Best before date
3 years. Do not use the drug after the expiration date indicated on the package.
Release from pharmacies
By doctor's prescription.
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