Nimesil granules for the preparation of suspensions 100 mg pack 2 g N9
Condition: New product
995 Items
More info
Active ingredients
Pharmacological effect
Nimesulide is an NSAID from the sulfonamide class. It has anti-inflammatory, analgesic and antipyretic effects. Nimesulide acts as an inhibitor of the COX enzyme, which is responsible for the synthesis of PG and inhibits mainly COX-2.
Pharmacokinetics
After ingestion, the drug is well absorbed from the gastrointestinal tract, reaching Cmax in the blood plasma in 2–3 hours; communication with plasma proteins - 97.5%; T1 / 2 is 3.2–6 h. Easily penetrates histohematogenous barriers.
Metabolized in the liver by the cytochrome P450CYP 2C9 isoenzyme. The main metabolite is a pharmacologically active parahydroxy derivative of nimesulide - hydroxynimesulide. Hydroxynimesulide is excreted in the bile in a metabolized form (it is found only in the form of glucuronate - about 29%).
Nimesulide is eliminated from the body, mainly by the kidneys (about 50% of the dose taken).
The pharmacokinetic profile of nimesulide in the elderly does not change with the appointment of single and multiple / repeated doses.
According to an experimental study conducted with patients with mild and moderate renal failure (Cl creatinine 30–80 ml / min) and healthy volunteers, the Cmax of nimesulide and its metabolite in the plasma of patients did not exceed the concentration of nimesulide in healthy volunteers. AUC and T1 / 2 in patients with renal insufficiency were 50% higher, but within the range of pharmacokinetic parameters. When re-taking the drug cumulation is not observed.
Indications
treatment of acute pain (pain in the back, lower back; pain in the pathology of the musculoskeletal system, including injuries, sprains and dislocations of the joints; tendinitis, bursitis);
toothache;
symptomatic treatment of osteoarthritis with pain;
disalgomenorrhea.
The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use.
Contraindications
hypersensitivity to nimesulide or to one of the components of the drug;
hyperergic reactions (in history), for example, bronchospasm, rhinitis, urticaria, associated with the intake of acetylsalicylic acid or other NSAIDs, including nimesulide;
hepatotoxic reactions to nimesulide (in history);
concomitant (simultaneous) administration of drugs with potential hepatotoxicity, for example, paracetamol or other analgesics or NSAIDs;
inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase;
the period after coronary artery bypass surgery;
febrile syndrome for colds and acute respiratory viral infections;
complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses with intolerance to acetylsalicylic acid and other NSAIDs (including in history);
gastric ulcer or duodenal ulcer in the acute phase, history of ulcers, perforation or bleeding in the gastrointestinal tract;
history of cerebrovascular hemorrhage or other bleeding, as well as diseases involving bleeding;
severe coagulation disorders;
severe heart failure;
severe renal insufficiency (Cl creatinine <30 ml / min), confirmed hyperkalemia;
liver failure or any active liver disease;
pregnancy and lactation;
alcoholism, drug addiction;
children under the age of 12 years.
Carefully: severe forms of arterial hypertension, type 2 diabetes, heart failure, coronary heart disease, cerebrovascular diseases, dyslipidemia / hyperlipidemia, peripheral artery disease, smoking, Cl creatinine less than 60 ml / min.
Anamnestic data on the presence of gastrointestinal ulcers, infections caused byHelicobacter pylori; elderly age; prolonged prior use of NSAIDs; severe somatic diseases.
Concomitant therapy with the following drugs: anticoagulants (for example, warfarin), antiplatelet agents (for example acetylsalicylic acid, clopidogrel), oral GCS (for example, prednisolone), SSRIs (for example, citalopram, fluoxetine, paroxetine, sertralin).
The decision on the appointment of the drug Nimesil should be based on an individual assessment of the risks and benefits of taking the drug.
Use during pregnancy and lactation
Like other NSAIDs class drugs that inhibit GHG synthesis, nimesulide may adversely affect the course of pregnancy and / or the development of the embryo and lead to premature closure of the ductus arteriosus,hypertension in the pulmonary artery system, impaired renal function, which can turn into renal failure with oligohydramnios, increase the risk of bleeding, reduce uterine contractility, the appearance of peripheral edema.
In this regard, nimesulide is contraindicated during pregnancy and lactation.
The use of the drug Nimesil® may adversely affect female fertility and is not recommended for women planning a pregnancy. When planning a pregnancy, consultation with your doctor is necessary.
Dosage and administration
Inside after meal. 1 pack (100 mg Nimesulide) 2 times a day. The contents of the bag poured into a glass and dissolved in about 100 ml of water. The prepared solution is not subject to storage.
Nimesil® is used only for the treatment of patients over 12 years old.
Teenagers (from 12 to 18 years). Based on the pharmacokinetic profile and pharmacodynamic characteristics of nimesulide, adolescents do not need to adjust the dose.
Patients with impaired renal function. Based on pharmacokinetic data, there is no need for dose adjustment in patients with mild or moderate forms of renal failure (Cl creatinine 30–80 ml / min).
Elderly patients. In the treatment of elderly patients, the need to adjust the daily dose is determined by the doctor based on the possibility of interaction with other drugs.
The maximum duration of treatment with nimesulide is 15 days.
To reduce the risk of unwanted side effects, use the minimum effective dose of the minimum short course.
Side effects
The frequency is classified by category, depending on the occurrence of the case: very often (> 10), often (> 100– <10); infrequently (> 1000– <100), rarely (> 10,000– <1000), very rarely (<10,000).
Violations of the circulatory and lymphatic systems: rarely - anemia, eosinophilia, hemorrhage; very rarely - thrombocytopenia, pancytopenia, thrombocytopenic purpura.
Allergic reactions: infrequently - itching, rash, excessive sweating; rarely, hypersensitivity reactions, erythema, dermatitis; very rarely - anaphylactoid reactions, urticaria, angioedema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).
Violations by the central nervous system: infrequently - dizziness; rarely, fear, nervousness, nightmare; very rarely - headache, drowsiness, encephalopathy (Reye's syndrome).
Violations of the senses: rarely - blurry vision.
Violations by the CCC:infrequently - arterial hypertension, tachycardia, blood pressure lability, hot flashes.
Respiratory disorders: infrequently - shortness of breath; very rarely - exacerbation of asthma, bronchospasm.
Violations of the gastrointestinal tract: often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, dyspepsia, stomatitis, tarry stools, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenum.
Liver and biliary system disorders: very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis, increased liver enzymes.
Kidney and urinary system disorders: rarely - dysuria, hematuria, urinary retention; very rarely - renal failure, oliguria, interstitial nephritis.
General violations: rarely - malaise, asthenia; very rarely - hypothermia.
Other: rarely - hyperkalemia.
Overdose
Symptoms: apathy, drowsiness, nausea, vomiting, epigastric pain. With the maintenance therapy of gastropathy, these symptoms are usually reversible. Gastrointestinal bleeding may occur. In rare cases, it may increase blood pressure, acute renal failure, respiratory depression and coma, anaphylactoid reactions.
Treatment: symptomatic. There is no specific antidote. If overdose occurred during the last 4 hours, induction of vomiting and / or administration of activated carbon (from 60 to 100 g per adult) and / or osmotic laxative. Forced diuresis, hemodialysis are ineffective due to the high association of the drug with proteins (up to 97.5%). Control of kidney and liver function is shown.
Interaction with other drugs
Pharmacodynamic Interactions
GKS. Increase the risk of gastrointestinal ulcers or bleeding.
Antiplatelet agents and SSRIs such as fluoxetine. Increase the risk of gastrointestinal bleeding.
Anticoagulants. NSAIDs may enhance the action of anticoagulants, such as warfarin. 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, it is necessary to carefully monitor blood clotting rates.
Diuretics. NSAIDs can reduce the effect of diuretics.
In healthy volunteers, nimesulide temporarily reduces the excretion of sodium under the action of furosemide, to a lesser extent - the excretion of potassium and reduces the actual diuretic effect.
The combined use of nimesulide and furosemide leads to a decrease (by approximately 20%) of AUC and a reduction in the cumulative excretion of furosemide without altering the renal clearance of furosemide.
The joint appointment of furosemide and nimesulide requires caution in patients with impaired renal or cardiac functions.
ACE inhibitors and angiotensin II receptor antagonists. NSAIDs can reduce the effect of antihypertensive drugs. In patients with mild and moderate renal failure (Clcreatin 30–80 ml / min) with the joint appointment of ACE inhibitors, angiotensin II receptor antagonists or substances that suppress the COX system (NSAIDs, antiplatelet agents), the kidney failure may be further worsened and acute renal failure may occur which is usually reversible. These interactions should be considered in patients taking Nimesil® in combination with ACE inhibitors or angiotensin II receptor antagonists. Therefore, the joint intake of these drugs should be prescribed with caution, especially for elderly patients. Patients should receive a sufficient amount of fluid, and renal function should be carefully monitored after the start of joint therapy.
Pharmacokinetic interactions with other drugs
Lithium preparations. There is evidence that NSAIDs reduce lithium clearance, which leads to an increase in plasma concentration of lithium and its toxicity. In the appointment of nimesulide to patients receiving therapy with lithium drugs, should regularly monitor the concentration of lithium in the plasma.
There were no clinically significant interactions with glibenclamide, theophylline, digoxin, cimetidine and antacid drugs (for example, a combination of aluminum and magnesium hydroxides).
Nimesulide inhibits the activity of CYP2C9 isoenzyme. At the same time taking drugs with nimesulide, which are the substrates of this enzyme, the concentration of these drugs in the plasma may increase.
When prescribing nimesulide less than 24 hours before or after taking methotrexate, caution is required because in such cases, the level of methotrexate in the plasma and, accordingly, the toxic effects of this drug may increase.
Due to the effect on renal GHGs, COX inhibitors, such as nimesulide, can increase the nephrotoxicity of cyclosporins.
The interaction of other drugs with nimesulide
Researchin vitro showed that nimesulide is displaced from the binding sites of tolbutamide, salicylic acid and valproic acid, but these effects were not observed during the clinical use of the drug.
special instructions
Undesirable side effects can be minimized by using the minimum effective dose of the drug with the shortest possible short course.
Nimesil® should be used with caution in patients with gastrointestinal diseases in history (ulcerative colitis, Crohn's disease), since exacerbation of these diseases is possible.
The risk of gastrointestinal bleeding, ulcer or perforation of the ulcer increases with an increase in the dose of NSAIDs in patients with an ulcer history, especially complicated by bleeding or perforation, as well as in elderly patients, so treatment should begin with the lowest possible dose. Patients receiving drugs that reduce blood clotting or suppress platelet aggregation also increases the risk of gastrointestinal bleeding. In the event of gastrointestinal bleeding or ulcers in patients taking Nimesil®, treatment with the drug should be canceled.
Since Nimesil® is partially excreted by the kidneys, its dosage for patients with impaired renal function should be reduced depending on the level of urination.
There is evidence of the occurrence of rare cases of reactions from the liver. If there are signs of liver damage (itching, yellowing of the skin, nausea, vomiting, abdominal pain, dark urine, increased activity of hepatic transaminases), you should stop taking the drug and contact your doctor.
Despite the rare occurrence of visual impairment in patients who took nimesulide simultaneously with other NSAIDs, treatment should be immediately discontinued.If any visual impairment occurs, the patient should be examined by an optometrist.
The drug can cause fluid retention in the tissues, so patients with high blood pressure and cardiac abnormalities Nimesil should be used with extreme caution.
In patients with renal or heart failure, Nimesil® should be used with caution, as renal function may deteriorate. If the condition worsens, treatment with Nimesil® should be stopped.
Clinical studies and epidemiological data suggest that NSAIDs, especially in high doses and with prolonged use, may lead to a slight risk of myocardial infarction or stroke. To eliminate the risk of such events when using nimesulide data is not enough.
The preparation contains sucrose, this should be taken into account for patients with diabetes mellitus (0.15–0.18 XE per 100 mg of the drug) and persons who are on a low-calorie diet. Nimesil® is not recommended for patients with fructose intolerance, glucose-galactose malabsorption, or sucrose-isomaltose deficiency.
In the event of a cold or acute respiratory viral infection in the course of treatment with Nimesil®, the drug should be discontinued.
Do not use Nimesil® simultaneously with other NSAIDs.
Nimesulide can change the properties of platelets, so care must be taken when using the drug in people with hemorrhagic diathesis, but the drug does not replace the prophylactic effect of acetylsalicylic acid in cardiovascular diseases.
Elderly patients are particularly susceptible to adverse reactions to NSAIDs, including risk of gastrointestinal bleeding and perforations that threaten the patient’s life, deterioration of kidney, liver and heart function. At reception of the drug Nimesil® for this category of patients appropriate clinical control is necessary.
There is evidence of the occurrence in rare cases of skin reactions (such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) on nimesulide as well as on other NSAIDs.At the first signs of skin rash, mucosal lesions or other signs of an allergic reaction, Nimesil® should be stopped.
Effect of the drug on the ability to drive vehicles and control mechanisms. The effect of Nimesil® on the ability to drive vehicles and control mechanisms has not been studied, therefore, during the treatment with Nimesil®, care should be taken when driving vehicles and practicing potentially hazardous activities requiring increased concentration and psychomotor speed.
Storage conditions
In a dry, dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.
2 years.
Do not use after the expiration date printed on the package.