Instructions for use Nimelgan granules for oral suspension 100 mg sachet No. 30
Composition
active ingredient: nimesulide;
1 sachet of 2 g of granules contains nimesulide 100 mg;
excipients: macrogol cetostearyl ether, sucrose, maltodextrin, anhydrous citric acid, orange flavoring.
Dosage form
Granules for oral suspension.
Main physicochemical properties: light yellow granular powder with an orange odor, after partial dissolution the color of the suspension is white or light yellow.
Pharmacotherapeutic group
Non-selective non-steroidal anti-inflammatory drugs. ATC code M01A X17.
Pharmacological properties
Pharmacodynamics
Nimesulide is a nonsteroidal anti-inflammatory drug (NSAID) of the methanesulfonanilide group, which has anti-inflammatory, analgesic and antipyretic effects. The therapeutic effect of nimesulide is due to the fact that it interacts with the arachidonic acid cascade and reduces prostaglandin biosynthesis by inhibiting cyclooxygenase.
Pharmacokinetics
In humans, nimesulide is well absorbed after oral administration, reaching a maximum concentration in blood plasma after 2-3 hours. Up to 97.5% of nimesulide binds to blood plasma proteins. Nimesulide is actively metabolized in the liver with the participation of CYP2C9, an isoenzyme of cytochrome P450. The main metabolite is a parahydroxy derivative, which also has pharmacological activity. The half-life is from 3.2 to 6 hours. Nimesulide is excreted from the body with urine - approximately 50% of the dose taken. About 29% of the dose taken is excreted with feces in a metabolized form. Only 1-3% is excreted from the body unchanged. The pharmacokinetic profile in elderly patients does not change.
Indication
Treatment of acute pain, primary dysmenorrhea. Nimesulide should only be used as a second-line drug. The decision to prescribe nimesulide should be made based on an assessment of all the risks for the individual patient.
Contraindication
Hypersensitivity to nimesulide or to any component of the drug. History of hypersensitivity reactions (bronchospasm, rhinitis, urticaria) associated with the use of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs. History of hepatotoxic reactions to nimesulide. Concomitant use of other substances with potential hepatotoxicity. Alcoholism and drug addiction. History of gastrointestinal bleeding or perforation associated with previous use of non-steroidal anti-inflammatory drugs. Gastric or duodenal ulcer in the acute phase, history of ulcer, perforation or bleeding in the digestive tract. History of cerebrovascular bleeding or other hemorrhages, as well as diseases accompanied by bleeding. Severe blood clotting disorders. Severe heart failure. Severe renal dysfunction. Liver dysfunction. Increased body temperature and/or flu-like symptoms. 3rd trimester of pregnancy or breastfeeding. Children under 12 years of age.
Interaction with other medicinal products and other types of interactions
Pharmacodynamic interactions.
Corticosteroids: Increased risk of gastrointestinal ulceration or bleeding. Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs). Increased risk of gastrointestinal bleeding.
Anticoagulants: NSAIDs may enhance the effect of anticoagulants such as warfarin or acetylsalicylic acid, which is why this combination is contraindicated in patients with severe coagulation disorders. If such combination therapy cannot be avoided, careful monitoring of blood coagulation parameters is necessary.
Diuretics, angiotensin-converting enzyme (ACE) inhibitors, and angiotensin II antagonists.
NSAIDs may reduce the effect of diuretics and other antihypertensive drugs. In some patients with impaired renal function (e.g. dehydrated patients or elderly patients), the concomitant use of ACE inhibitors, angiotensin II antagonists or agents that inhibit the cyclooxygenase system may lead to further deterioration of renal function and the development of acute renal failure, which is usually reversible. These interactions should be taken into account when the patient is taking nimesulide together with ACE inhibitors or angiotensin II antagonists. Great caution should be exercised when using this combination, especially in elderly patients. Patients should be adequately hydrated and renal function should be closely monitored after the start of this combination. Nimesulide temporarily reduces the effect of furosemide on sodium excretion and, to a lesser extent, potassium excretion, and also reduces the diuretic effect. The combined use of furosemide and nimesulide in patients with impaired renal or cardiac function requires caution.
Pharmacokinetic interactions with other drugs.
There have been reports that NSAIDs reduce lithium clearance, leading to increased plasma lithium levels and lithium toxicity. When prescribing nimesulide to patients receiving lithium therapy, frequent monitoring of plasma lithium levels should be performed.
There is no clinically significant interaction with glibenclamide, theophylline, warfarin, digoxin, cimetidine and antacids (aluminum and magnesium hydroxide combination) in vivo. Nimesulide inhibits the activity of the CYP2C9 enzyme. When drugs that are substrates of this enzyme are used simultaneously with nimesulide, their plasma concentrations may increase. Caution is required if nimesulide is administered less than 24 hours before or less than 24 hours after taking methotrexate, since an increase in the serum level of the latter and an increase in its toxicity is possible.
Due to their effect on renal prostaglandins, synthetase inhibitors, to which nimesulide belongs, may increase the nephrotoxicity of cyclosporines.
The effect of other drugs on nimesulide.
In vitro studies have shown that nimesulide is displaced from binding sites by tolbutamide, salicylic acid and valproic acid. Although these interactions have been identified in plasma, these effects have not been observed during clinical use of the drug.
Application features
Undesirable side effects can be minimized by using the lowest effective dose for the shortest period of time necessary to control symptoms.
If the treatment is ineffective (reduction in symptoms of the disease), therapy with the drug should be discontinued.
During treatment with nimesulide, it is recommended to avoid the simultaneous use of hepatotoxic drugs, as well as to refrain from drinking alcohol. The use of NSAIDs may mask an increase in body temperature associated with a background bacterial infection. In the event of an increase in body temperature or the appearance of flu-like symptoms in patients using nimesulide, the drug should be discontinued.
Serious hepatic reactions, including fatalities, have been reported during treatment with nimesulide. Patients who experience symptoms suggestive of liver damage, such as anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine, or patients whose liver function tests are abnormal, should discontinue the drug. Re-administration of nimesulide to such patients is contraindicated. During treatment with nimesulide, the patient should refrain from taking other analgesics. Concomitant use of other NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided.
Patients taking nimesulide who develop flu-like symptoms should discontinue its use.
Elderly patients have an increased frequency of adverse reactions to NSAIDs, especially possible bleeding and perforation in the digestive tract, which can be fatal.
Ulceration, bleeding or perforation in the digestive tract can be life-threatening, especially if there is a history of similar events in the patient when using any other NSAIDs (without a prescription). The risk of such events increases with increasing NSAID dose in patients with a history of gastrointestinal ulcer, especially complicated by bleeding or perforation, and in elderly patients. In such patients, treatment should be started with the lowest possible effective dose. For these patients, as well as for those taking concomitant low doses of acetylsalicylic acid or other drugs that increase the risk of gastrointestinal complications, the possibility of using combination therapy with protective agents, such as misoprostol or proton pump inhibitors, should be considered.
Patients with toxic lesions of the digestive tract, especially elderly patients, should report any unusual symptoms that occur in the digestive tract, especially bleeding. This is especially important in the initial stages of treatment. Patients taking concomitant medications that may increase the risk of ulceration or bleeding, such as corticosteroids, anticoagulants, SSRIs, antiplatelet agents (acetylsalicylic acid), should be informed of the need to exercise caution when using nimesulide.
If a patient receiving nimesulide experiences bleeding or ulcers in the digestive tract, treatment with the drug should be discontinued.
NSAIDs should be prescribed with caution to patients with a history of Crohn's disease or nonspecific ulcerative colitis, as nimesulide may lead to their exacerbation.
Concomitant use of nimesulide with other drugs, such as oral contraceptives, anticoagulants, antiplatelet agents, may cause exacerbation of Crohn's disease and other diseases of the digestive tract.
There is evidence that some NSAIDs, especially at high doses and with prolonged use, may carry a small risk of arterial thrombotic events, such as myocardial infarction and stroke. There is insufficient data to exclude a risk of such events with nimesulide.
Patients with uncontrolled hypertension, acute heart failure, established ischemic heart disease, peripheral arterial disease and/or cerebrovascular disease should be prescribed nimesulide after a careful assessment of the condition. The same applies to patients with risk factors for cardiovascular disease, such as hypertension, hyperlipidemia, diabetes mellitus, smoking, before prescribing the drug.
Patients with impaired renal function or heart failure should be prescribed the drug with caution due to the possibility of worsening renal function. In case of deterioration of the patient's condition, treatment should be discontinued.
Elderly patients should be carefully monitored for the possibility of bleeding and perforation of the gastrointestinal tract, deterioration of renal, hepatic or cardiac function. Since nimesulide may affect platelet function, it should be prescribed with caution to patients with hemorrhagic diathesis. However, nimesulide does not replace acetylsalicylic acid in the prevention of cardiovascular diseases.
There have been rare reports of severe skin reactions with NSAIDs, some of which may be fatal, such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis. In most cases, if these reactions occurred during the first month of previously prescribed treatment, the risk of their occurrence in patients is significantly increased. Nimesulide should be discontinued at the first signs of skin rash, mucosal lesions and other allergic manifestations.
The use of nimesulide may impair female fertility and is not recommended for women attempting to conceive. Nimesulide is not recommended for women who are unable to conceive or who are undergoing investigation for infertility.
Nimesulide contains sucrose, so it should not be prescribed to patients with hereditary fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency.
Ability to influence reaction speed when driving vehicles or other mechanisms
Studies on the effect of nimesulide on the ability to drive or use machines have not been conducted, but if patients experience headache, dizziness, or drowsiness while taking nimesulide, they should refrain from driving or operating machinery.
Use during pregnancy or breastfeeding
Inhibition of prostaglandin synthesis may adversely affect pregnancy and/or fetal development. The data obtained during the studies allow us to conclude that the use of drugs that inhibit prostaglandin synthesis in early pregnancy may increase the risk of spontaneous abortion, fetal heart defects and gastroschisis. The absolute risk of developing a cardiovascular anomaly has increased from less than 1% to approximately 1.5%. The risk is believed to increase with increasing dose and duration of use.
Nimesulide should not be taken during the first and second trimesters of pregnancy unless clearly necessary. If the drug is used in women attempting to conceive or during the first and second trimesters of pregnancy, the lowest possible dose and the shortest possible duration of treatment should be used.
In the third trimester of pregnancy, all prostaglandin synthesis inhibitors can lead to the development of the following in the fetus:
pneumocardiac toxic lesion (with premature closure of the ductus arteriosus 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:
increased bleeding time, anti-aggregation effect, which may occur even when using very low doses of the drug; inhibition of uterine contractile activity, which may lead to a delay or prolongation of the period of labor.
Therefore, nimesulide is contraindicated in the third trimester of pregnancy.
Like NSAIDs that inhibit prostaglandin synthesis, nimesulide can cause premature closure of the ductus arteriosus, pulmonary hypertension, oliguria, oligohydramnios. The risk of bleeding, labor weakness, and peripheral edema increases. There are isolated reports of renal failure in infants whose mothers used nimesulide late in pregnancy.
Nimesulide may impair female fertility and is therefore not recommended for use in women attempting to conceive. Women who are unable to conceive or who are undergoing investigation of infertility should consider discontinuing nimesulide. If pregnancy occurs during treatment with nimesulide, the physician should be informed.
Method of administration and doses
To minimize possible unwanted side effects, the minimum effective dose should be used for the shortest possible time. It is recommended to use after meals.
The maximum duration of treatment with Nimelgan is 15 days.
Adults: 100 mg nimesulide (1 sachet) 2 times a day after meals.
Elderly patients: no dose adjustment is required.
Children over 12 years of age: no dose adjustment is required.
Patients with renal impairment: For patients with mild or moderate renal impairment (creatinine clearance 30-80 ml/min), no dose adjustment is required, while severe renal impairment (creatinine clearance < 30 ml/h) is a contraindication for the use of Nimesulide.
Pour the contents of the packet into a glass, dissolve in water and take orally.
Children
Nimesulide is contraindicated in children under 12 years of age.
Overdose
Symptoms: apathy, drowsiness, nausea, vomiting, epigastric pain. These symptoms are usually reversible with supportive therapy. Gastrointestinal bleeding, hypertension, acute renal failure, respiratory depression, coma may occur, but these events are rare. Anaphylactoid reactions have been reported with therapeutic doses of NSAIDs and with their overdose.
Treatment: symptomatic and supportive therapy. There is no data on the removal of nimesulide by hemodialysis, but taking into account the high degree of binding of nimesulide to blood plasma proteins (up to 97.5%), it is unlikely that dialysis will be effective. In the presence of symptoms of overdose or after the use of a large dose of the drug within 4 hours after its administration, patients can be prescribed artificial vomiting and/or taking activated charcoal (60-100 g for adults), and/or taking an osmotic laxative. Forced diuresis, increasing the alkalinity of the urine, hemodialysis and hemoperfusion may be ineffective due to the high degree of binding of nimesulide to blood plasma proteins. Kidney and liver function should be monitored.
There is no specific antidote.
Adverse reactions
From the blood system: anemia, eosinophilia, thrombocytopenia, pancytopenia, purpura.
Immune system disorders: hypersensitivity, anaphylaxis.
Metabolic: hyperkalemia.
On the part of the psyche: feeling of fear, nervousness, night terrors.
From the nervous system: dizziness, headache, drowsiness, encephalopathy (Reye's syndrome).
From the organs of vision: blurred vision, visual disturbances.
On the part of the organs of hearing: vertigo.
Cardiovascular system: tachycardia, hypertension, hemorrhage, blood pressure lability, hot flashes.
From the respiratory system: shortness of breath, bronchial asthma, bronchospasm.
On the part of the digestive tract: diarrhea, nausea, vomiting, constipation, flatulence, gastritis, bleeding in the digestive tract, ulcer and perforation of the duodenum or stomach, abdominal pain, dyspepsia, stomatitis, black stools.
Hepatobiliary system: increased liver enzyme levels; hepatitis; fulminant hepatitis with fatal outcome, including jaundice, cholestasis.
Skin: itching, rash, increased sweating, erythema, dermatitis, urticaria, angioedema, facial edema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
From the urinary system: dysuria, hematuria, urinary retention, renal failure, oliguria, interstitial nephritis.
General disorders: edema, malaise, asthenia, hypothermia.
The most common adverse reactions observed with NSAIDs are gastrointestinal. Peptic ulcers, perforations or bleeding in the digestive tract, which can sometimes be life-threatening, especially in elderly patients, may occur. The following adverse reactions have been reported after the use of this group of drugs: nausea, vomiting, diarrhea, bloating, constipation, dyspepsia, abdominal pain, black stools, bloody vomiting, ulcerative stomatitis, exacerbation of colitis and Crohn's disease. Gastritis has been observed less frequently.
There have been reports of edema, hypertension, and heart failure as reactions to the use of NSAIDs.
Very rarely, skin reactions such as blistering, Stevens-Johnson syndrome and toxic epidermal necrolysis may occur with the use of NSAIDs.
Research data suggest that some NSAIDs, especially at high doses and with long-term use, may lead to a small increased risk of arterial thrombotic complications, such as myocardial infarction or stroke.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
30 sachets in a cardboard box.
Vacation category
According to the recipe.
Producer
ASTRAPHARM LLC, Ukraine.
Location of the manufacturer and its business address
08132, Kyiv region, Kyiv-Svyatoshynskyi district, Vyshneve town, Kyivska st., 6.
