Instructions Nimedar granules for oral suspension 100 mg/2 g single-dose package No. 30
Composition
active ingredient: nimesulide;
1 single-dose packet of 2 g of granules contains nimesulide 100 mg;
excipients: polyethylene glycol cetostearyl ether, maltodextrin, anhydrous citric acid, orange flavoring, crystalline sugar.
Dosage form
Granules for oral suspension.
Main physicochemical properties: granules from light yellow to yellow.
Pharmacotherapeutic group
Non-selective non-steroidal anti-inflammatory drugs. ATC code M01A X17.
Pharmacological properties
Pharmacodynamics
Nimedar is a nonsteroidal anti-inflammatory drug of the methanesulfonanilide group, which exhibits anti-inflammatory, analgesic and antipyretic effects. The therapeutic effect of Nimedar is due to the fact that it interacts with the arachidonic acid cascade and reduces prostaglandin biosynthesis by inhibiting cyclooxygenase.
Pharmacokinetics
In the human body, Nimedar is well absorbed after oral administration, reaching a maximum plasma concentration after 2–3 hours. Up to 97.5% of nimesulide binds to plasma proteins. Nimesulide is actively metabolized in the liver with the participation of CYP2C9, an isoenzyme of cytochrome P 450. 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 - about 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 based on an assessment of all the risks for the individual patient.
Contraindication
Hypersensitivity to nimesulide or any component of the drug. History of hypersensitivity reactions (bronchospasm, rhinitis, urticaria) associated with the use of acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs.
History of hepatotoxic reactions to nimesulide.
Concomitant use of other substances with potential hepatotoxicity.
History of gastrointestinal bleeding or perforation associated with previous use of nonsteroidal anti-inflammatory drugs (NSAIDs).
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.
The patient has an elevated body temperature and/or flu-like symptoms.
Alcoholism and drug addiction.
Children under 12 years old.
Third trimester of pregnancy and breastfeeding.
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: 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.
In healthy volunteers, nimesulide rapidly reduces the sodium-excreting and, to a lesser extent, potassium-excreting effects of furosemide, and also reduces the diuretic effect. Simultaneous 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 changes in the renal clearance of furosemide.
Pharmacokinetic interactions with other drugs.
NSAIDs have been reported to reduce lithium clearance, leading to increased plasma lithium levels and lithium toxicity. When Nimedar is prescribed 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 Nimedar, their plasma concentration may increase. Caution is required when nimesulide is administered less than 24 hours before or less than 24 hours after taking methotrexate, since it is possible to increase the level of the latter in the blood serum and increase its toxicity.
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 its 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 treatment is ineffective, drug therapy 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 nonsteroidal anti-inflammatory drugs 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.
There have been reports of serious liver reactions during treatment, including fatalities, with nimesulide. Patients who experience symptoms suggestive of liver damage, such as anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine, and patients whose liver function tests are abnormal should discontinue the drug. Re-administration of nimesulide to such patients is contraindicated. During treatment with Nimedar, the patient should refrain from taking other analgesics. Concomitant use of other NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided.
Patients taking nimesulide should discontinue use if flu-like symptoms occur.
Elderly patients have an increased frequency of adverse reactions to NSAIDs, especially gastrointestinal bleeding and perforation, 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 who are taking 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 increase the risk of ulceration or bleeding, such as corticosteroids, anticoagulants, selective serotonin reuptake inhibitors, antiplatelet agents (acetylsalicylic acid), should be informed of the need to exercise caution when using nimesulide.
If a patient receiving Nimedar experiences bleeding or ulcers in the digestive tract, treatment with the drug should be discontinued.
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.
Patients with a history of hypertension and/or heart failure, as well as patients with fluid retention and edema due to the use of NSAIDs, require appropriate monitoring of their condition and consultation with a doctor.
Clinical studies and epidemiological data suggest that some NSAIDs, especially at high doses and with prolonged use, may cause 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, ischemic heart disease, peripheral arterial disease and/or cerebrovascular disease should be prescribed nimesulide after careful assessment of the condition. This also applies to patients with risk factors for cardiovascular disease, such as: hypertension, hyperlipidemia, diabetes mellitus, smoking.
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 can be fatal, such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis. If such reactions occur within the first month of a previously prescribed course of treatment, the risk of their occurrence in patients is significantly increased. Nimedar should be discontinued at the first signs of skin rash, mucosal lesions, or other allergic manifestations.
The use of nimesulide may impair female fertility and is not recommended for women planning to become pregnant. Women who have difficulty conceiving or who are
During an examination for infertility, it is not recommended to prescribe nimesulide.
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. Epidemiological data suggest that use of prostaglandin synthesis inhibitors in early pregnancy increases the risk of spontaneous abortion, fetal heart defects and gastroschisis. The absolute risk of cardiovascular malformations increases 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 prescribed to 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 cause the development of:
pneumocardiac toxic lesion (with premature closure of the ductus arteriosus and hypertension in the pulmonary artery system); renal dysfunction, which may 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; suppression of uterine contractile activity, which may lead to delayed or prolonged labor.
Therefore, nimesulide is contraindicated in the third trimester of pregnancy.
Since NSAIDs 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 is evidence of renal failure in infants whose mothers used nimesulide at the end of pregnancy. Animal studies have shown atypical reproductive toxicity of the drug, but there are no reliable data on the use of nimesulide in pregnant women.
Since it is not known whether nimesulide passes into breast milk, its use is contraindicated during breastfeeding.
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 take after meals.
The maximum duration of treatment with Nimedar is 15 days.
Adults: 100 mg nimesulide (1 single-dose packet) 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: No dose adjustment is required for patients with mild or moderate renal impairment (creatinine clearance 30–80 ml/min), while severe renal impairment (creatinine clearance < 30 ml/h) is a contraindication to the use of Nimedar.
The contents of the packet are poured into a glass, dissolved in water and taken orally.
Children
The drug Nimedar is contraindicated in children under 12 years of age.
Overdose
Symptoms of acute overdose with nonsteroidal anti-inflammatory drugs (NSAIDs) are usually limited to the following: apathy, drowsiness, nausea, vomiting, epigastric pain. These symptoms are usually reversible with supportive therapy. Gastrointestinal bleeding, arterial hypertension, acute renal failure, respiratory depression, coma are possible, but such phenomena are rare. There have been reports of anaphylactoid reactions when using therapeutic doses of NSAIDs and in case of their overdose. There is no specific antidote. Treatment of overdose is symptomatic and supportive. There is no data on the removal of nimesulide by hemodialysis, but if we take into account the high degree of binding of nimesulide to plasma proteins (up to 97.5%), then dialysis is unlikely to 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), an osmotic laxative. Forced diuresis, increasing urine alkalinity, hemodialysis and hemoperfusion may be ineffective due to the high degree of binding of nimesulide to plasma proteins. Kidney and liver function should be monitored.
Adverse reactions
From the side of the circulatory and lymphatic system: anemia, eosinophilia, thrombocytopenia, pancytopenia, purpura.
Immune system disorders: hypersensitivity, anaphylaxis.
Metabolic: hyperkalemia.
From the perspective of the psyche: feelings 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 auditory organs: vertigo (dizziness).
Cardiovascular system: tachycardia, hypertension, hemorrhage, blood pressure lability, hot flashes.
From the respiratory system and mediastinal organs: shortness of breath, asthma, bronchospasm.
Gastrointestinal: dyspepsia, diarrhea, nausea, vomiting, constipation, flatulence, gastritis, gastrointestinal bleeding, gastric or duodenal ulcer and perforation, abdominal pain, stomatitis, black stools, bloody vomiting, ulcerative stomatitis, exacerbation of colitis and Crohn's disease.
From the liver and biliary system: increased liver enzymes, hepatitis, fulminant hepatitis, with fatal outcome, including jaundice, cholestasis.
Skin and subcutaneous tissue disorders: pruritus, rash, erythema, dermatitis, blistering, urticaria, angioedema, facial edema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, increased sweating.
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 the use of nonsteroidal anti-inflammatory drugs (NSAIDs) are gastrointestinal.
Clinical and epidemiological studies suggest that some NSAIDs, especially at high doses and with prolonged use, may lead to arterial thrombotic complications, such as myocardial infarction or stroke.
Expiration date
2 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
2 g of granules in a single-dose packet, 30 packets in a box.
Vacation category
According to the recipe.
Producer
Location of the manufacturer and its business address
Ukraine, 02093, Kyiv, Boryspilska St., 13.
