Name:
Nise tab 100mg №20
Description:
Pills color from almost white to yellow, round, with a smooth convex surface on both sides. The main active ingredient Nimesulide Release form 10 tablets in a blister pack. 2 blister packs, together with instructions for medical use, are placed in a cardboard pack. Dosage 100mg №20 Pharmacodynamics Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties, which 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 joint use of nimesulide with drugs 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 to detection of this metabolite in the circulating blood is short (0.8 hours), but the amount of its formation is small and much 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 is 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 displayed unchanged. Hydroxynimesulide? the main metabolite is found exclusively in the form of glucuronate. Approximately 29% of the dose taken is excreted in the metabolized form in the feces. The pharmacokinetic profile of nimesulide in the elderly does not change when prescribing single and multiple / repeated doses. In a short-term experimental study conducted in patients with mild to moderate renal insufficiency (creatinine clearance 30–80 ml/min) and healthy volunteers, the maximum concentration of nimesulide and its main metabolite in the plasma of patients was not greater than the concentration in healthy volunteers. The area under the curve “Concentration ? time “(AUC) and half-life (t1 / 2 beta) in patients with renal insufficiency were 50% higher, but were always in the range of pharmacokinetic values observed in healthy volunteers taking nimesulide. Repeated administration of the drug did not lead to accumulation. Nimesulide is contraindicated in patients with hepatic impairment. Indications for use? Acute pain treatment? Primary dysmenorrhea? Nimesulide 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. Route of administration and doses In order to minimize unwanted side effects, the minimum effective dose should be taken with the shortest duration of treatment. The maximum duration of treatment with nimesulide is 15 days. Adult patients: 100 mg of nimesulide twice 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. Adolescents (12 to 18 years of age): based on the pharmacokinetic profile 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 for dose adjustment in patients with mild to moderate renal insufficiency (creatinine clearance 30–80 ml / min), while in patients with severe renal insufficiency (creatinine clearance < 30 ml / min) the appointment of Nise is contraindicated. Patients with hepatic impairment: Nise is contraindicated in patients with hepatic impairment. Undesirable effects of therapy can be reduced by prescribing the lowest effective dose of the drug for the shortest possible time required to treat the relevant disease. Use during pregnancy and lactation In the third trimester of pregnancy, the use of Nise is contraindicated. Pregnancy Suppression of prostaglandin synthesis may adversely affect pregnancy and/or fetal development. Data obtained from epidemiological studies suggest that the use of drugs that inhibit prostaglandin synthesis in early pregnancy may increase the risk of spontaneous abortion, fetal heart disease and gastroschisis. The absolute risk of an abnormal cardiovascular system increased from less than 1% to about 1.5%. It is believed that the risk increases with increasing dose and duration of use. In animals, administration of a prostaglandin synthesis inhibitor resulted in increased pre- and post-implantation loss and increased fetal mortality. In addition, data were obtained that in animals treated with a prostaglandin synthesis inhibitor during organogenesis, the incidence of various fetal malformations, including those of the cardiovascular system, increased. Do not take nimesulide during the first and second trimester of pregnancy unless absolutely necessary. In the case of the use of 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: 1) can lead to the development in the fetus: pneumocardial toxic damage (with premature closure of the arterial ducts and hypertension in the pulmonary artery system); ? kidney dysfunction, which can progress to renal failure with the development of oligohydramnios; 2) in the mother and fetus at the end of pregnancy is possible: ? an increase in bleeding time, an antiplatelet effect that can occur even when using very low doses of the drug; ? suppression of the contractile activity of the uterus, which can lead to a delay or lengthening of the period of childbirth. Therefore, nimesulide is contraindicated in the third trimester of pregnancy. Lactation. At the moment, it is not known whether nimesulide is excreted in breast milk. Nise is contraindicated for use in nursing mothers. Fertility. Like other NSAIDs, drugs containing nimesulide are not recommended for women planning pregnancy. Precautions Unwanted side effects can be minimized by using the lowest effective dose for the shortest duration necessary to control the symptoms of the disease. In the absence of improvement in symptoms, drug therapy should be discontinued. In elderly patients, the frequency of adverse reactions to NSAIDs is increased, especially the frequency of gastrointestinal bleeding and perforation (in some cases even fatal), as well as impaired renal, hepatic and cardiac function. Therefore, appropriate clinical observation is recommended. Liver disorders Rare cases of serious liver reactions, including very rare cases of death, have been reported associated with the use of nimesulide-containing medicinal products. Patients who experience symptoms similar to those of liver damage during treatment with Nise (eg, anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine) or who have abnormal liver function laboratory tests should discontinue drug treatment. Re-appointment of nimesulide in such patients is contraindicated. Liver damage, in most cases reversible, has been reported after short-term exposure to the drug. During treatment with Nise, the patient should refrain from taking other analgesics. The concomitant use of Nise and other NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided. Patients treated with nimesulide and who develop flu-like or cold-like symptoms should discontinue treatment with the drug. Gastrointestinal disorders Gastrointestinal bleeding, ulcers, and perforation of the ulcer may be life-threatening if there is a history of such problems with any NSAID during treatment (regardless of time elapsed), with or without dangerous symptoms, or a history of serious disorders of the gastrointestinal tract. The risk of gastrointestinal bleeding, ulceration or perforation of the ulcer increases with increasing dose of NSAIDs in patients with a history of ulcers, especially those complicated by hemorrhage or perforation, as well as in elderly patients. For these patients, treatment should be initiated at the lowest possible dose. For these patients, as well as patients who are taking concomitant low doses of 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 gastrointestinal toxicity, especially the elderly, should report any unusual gastrointestinal symptoms (especially gastrointestinal bleeding). This is especially important in the early stages of treatment. Gastrointestinal bleeding, as well as the formation of ulcers or perforation, are noted for all NSAIDs at different stages of treatment, regardless of the presence of precursor symptoms or a history of gastrointestinal pathology. With the development of gastrointestinal bleeding or manifestations, nimesulide should be discontinued. Nimesulide should be used with caution in patients with gastrointestinal disorders, including peptic ulcer, history of gastrointestinal bleeding, ulcerative colitis, and Crohn's disease. Patients taking concomitant medications that may increase the risk of ulcers or bleeding, such as oral corticosteroids, anticoagulants such as warfarin, selective serotonin reuptake inhibitors, or antiplatelet agents such as aspirin, should be advised to take the drug with caution. funds. If gastrointestinal bleeding or ulcers occur in patients receiving Nise, treatment with the drug should be discontinued. NSAIDs should be used with caution in patients with a history of gastrointestinal disease (ulcerative colitis, Crohn's disease), as these diseases may worsen. Nise should be used with caution in patients with renal or cardiac insufficiency as the medicinal product may impair renal function. If the condition worsens, treatment should be discontinued. Skin reactions Very rare cases of severe skin reactions to NSAIDs have been reported, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis, some of which can be fatal. Patients appear to be most at risk of developing skin reactions during the initial period of therapy. Nise should be discontinued at the first sign of skin rash, mucosal lesions, and other signs of hypersensitivity. Renal disorders Care should be taken when prescribing the drug to patients with impaired renal or cardiac function, since the use of nimesulide may lead to deterioration of renal function. In case of deterioration, treatment should be interrupted. 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 undergoing examination for infertility, the possibility of discontinuing nimesulide should be considered. Disorders of the cardiovascular and cerebrovascular systems Patients with arterial hypertension and / or mild / moderate acute heart failure in history, as well as patients with the occurrence of fluid retention in the body and edema, as a reaction to the use of NSAID therapy, require appropriate monitoring and consultation doctor. Clinical studies and 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 are not enough data to exclude the risk of such events when using nimesulide. In patients with uncontrolled arterial hypertension, congestive heart failure, established ischemic heart disease, peripheral arterial disease and/or cerebrovascular disease, nimesulide should be prescribed after a thorough evaluation of the condition. An equally thorough assessment of the condition 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. However, Nise does not replace acetylsalicylic acid in the prevention of cardiovascular disease. Interaction with other drugs Other non-steroidal anti-inflammatory drugs (NSAIDs) The combined use of drugs containing nimesulide and other NSAIDs, 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 increase the effect of anticoagulants such as warfarin or acetylsalicylic acid. Due to the increased risk of bleeding, this combination is not recommended and contraindicated in patients with severe coagulation 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 (SSRIs): Increase the risk of gastrointestinal bleeding. Diuretics, angiotensin-converting enzyme inhibitors (ACE inhibitors), type 2 angiotensin receptor antagonists (AIIA): 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 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 considered in patients taking Nise concomitantly with an ACE inhibitor or an AIIA. Therefore, when prescribing this combination of drugs, care should be taken, especially in elderly patients. Patients should be adequately hydrated and monitoring of renal function should be considered after initiation 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 on sodium excretion, to a lesser extent, on potassium excretion, and reduced the diuretic response. Co-administration of nimesulide and furosemide leads to a decrease (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. The co-administration of furosemide and drugs containing 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 Nise to patients receiving therapy with lithium drugs, frequent monitoring of plasma lithium levels should be carried out. In vivo studies have been conducted to identify possible pharmacokinetic interactions with glibenclamide, theophylline, warfarin, digoxin, cimetidine, and antacid drugs (eg, a combination of aluminum and magnesium hydroxide). No clinically significant interactions were observed. Nimesulide inhibits the activity of the CYP2C9 enzyme. When drugs that are substrates of this enzyme are taken simultaneously with Nise, 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, care must be taken, since in such cases the plasma level of methotrexate and, accordingly, the toxic effects of this drug may increase. In connection with the action on renal prostaglandins, inhibitors of prostaglandin synthesis, which include nimesulide, may increase the nephrotoxicity of cyclosporins. 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. Despite the fact that these interactions were determined in blood plasma, these effects were not observed during the clinical use of the drug. Contraindications? Known hypersensitivity to nimesulide or to one of the excipients of the drug. ? Past hyperergic reactions (eg, bronchospasm, rhinitis, urticaria) in connection with the use of 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. ? An ulcer of the stomach or duodenum 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 bleeding disorders. ? Severe heart failure. ? Severe renal failure. ? Liver failure. ? Patients with cold or flu symptoms. ? Age up to 12 years. ? The appointment of the drug is contraindicated in the third trimester of pregnancy and during lactation. Composition Composition per 1 tablet: active substance: nimesulide? 100 mg; excipients: anhydrous calcium hydrogen phosphate, microcrystalline cellulose, corn starch, sodium starch glycolate (type A), magnesium stearate, anhydrous colloidal silicon dioxide, purified talc. Overdose Symptoms of acute H11BC overdose are usually limited to the following: apathy, drowsiness, nausea, vomiting and pain in the epigastric region. With maintenance therapy, these symptoms are usually reversible. Gastrointestinal bleeding may occur. In rare cases, it is possible to increase blood pressure, acute renal failure, respiratory depression and coma. Anaphylactoid reactions have been reported with therapeutic doses of NSAIDs and with overdose of such drugs. In case of NSAID overdose, treatment is symptomatic and supportive. There is no specific antidote. There are no data on the elimination of nimesulide by hemodialysis, however, based on the high level of plasma protein binding (up to 97.5%), it can be concluded that dialysis is ineffective in case of drug overdose. If symptoms of an overdose are present or after taking a large dose of the drug within 4 hours after ingestion, patients may be prescribed: inducing vomiting and / or taking activated charcoal (60 × 100 grams for adults) and / or taking an osmotic laxative. Forced diuresis, alkalinization of urine, hemodialysis or hemoperfusion may be ineffective due to the high level of drug binding to blood proteins. The functions of the kidneys and liver should be monitored. Side effect Determination of the frequency of side effects: often (1-10%), infrequently (0.1-1%), rarely (0.01-0.1%), very rarely (<0.01%), including individual messages. Allergic reactions: rarely - hypersensitivity reactions; very rarely - urticaria, angioedema, anaphylactoid reactions. 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). On the part of the skin: infrequently - itching, rash, increased sweating; rarely - erythema, dermatitis; very rarely - puffiness of the face, erythema multiforme exudative, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome). From the urinary system: infrequently - edema; rarely - dysuria, hematuria, urinary retention, hyperkalemia; very rarely - renal failure, oliguria, interstitial nephritis. From the digestive system: often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, stomatitis, tarry stools, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenum. From the side of the liver and biliary system: often - an increase in hepatic transaminases; very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis. On the part of the hematopoietic organs: rarely - anemia, eosinophilia; very rarely - thrombocytopenia, pancytopenia, purpura, prolongation of bleeding time. From the respiratory system: infrequently - shortness of breath; very rarely - exacerbation of bronchial asthma, bronchospasm. From the senses: rarely - blurred vision. From the side of the cardiovascular system: infrequently - arterial hypertension; rarely - tachycardia, hemorrhages, hot flashes. Others: rarely - general weakness; very rarely - hypothermia. Storage conditions Store at a temperature not exceeding 25 ° C in a place protected from light and moisture. Keep out of the reach of children. Best before date ? 3 years. Do not use after the expiration date indicated on the package. Buy Nise tablets 100mg No. 10x2 Price for Nise tablets 100mg No. 10x2 Instructions for use for Nise tablets 100mg No. 10x2
INN | NIMESULID |
---|---|
The code | 90 801 |
Barcode | 4 810 147 009 196 |
Dosage | 100mg |
Active substance | Nimesulide |
Manufacturer | Dr. Reddis, pack. Nesvizh ZMP, Belarus |
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