Instructions for use of Nimesil powder

Use of Nimesil powder: indications and contraindications

The medicine is used to suppress pain, inflammation, and associated symptomatic manifestations. In the instructions for use, the manufacturer recommends taking Nimesil for the following indicators:

• for pain accompanying osteoarthritis;
• painful sensations arising from injuries, inflammation in the joint capsule and tendons;
• algodismenorrhea.

The list of contraindications for the use of Nimesil is presented:

• bronchospasm, rhinitis, symptoms of urticaria that occur in response to taking NSAIDs or aspirin;
• performed coronary artery bypass surgery, therapy with hepatotoxic medications;
• inflammatory pathologies of the intestinal tract;
• elevated temperature due to inflammatory and infectious pathologies;
• transition to the acute phase of the ulcer, spontaneous hemorrhages in the gastrointestinal tract;
• a combination of allergies to NSAIDs, nasal polyps and chronic inflammation of the respiratory tract;
• local hemorrhages;
• decompensated kidney or heart failure;
• disorders of blood clotting rate;
• potassium deficiency, liver pathologies;
• alcoholism, drug addiction;
• period of pregnancy or breastfeeding;
• children under twelve years of age.

Particular caution when taking is necessary for patients:

• with severe form of non-insulin-dependent diabetes;
• hypertension or ischemia;
• AHF, dyslipidemia;
• lesions of peripheral arteries;
• ulcers, somatic diseases in the period of decompensation.

The medication requires medical supervision with prolonged use of NSAIDs, oral glucocorticosteroids, and antiplatelet agents. Problems with therapy can be caused by smoking and simultaneous treatment with drugs that slow down the rate of blood clotting.

NIMESAN TABLETS 100MG N20

Pharmacotherapeutic group: Non-steroidal anti-inflammatory drug (NSAID) ATC code: M01AX17 Pharmacological action Non-steroidal anti-inflammatory drug (NSAID) from the sulfonanilide class. It is a selective competitive inhibitor of cyclooxygenase-2 (COX-2), an enzyme involved in the synthesis of prostaglandins, mediators of edema, inflammation and pain. It has anti-inflammatory, analgesic and antipyretic effects. Reversibly inhibits the formation of prostaglandin E2, both at the site of inflammation and in the ascending pathways of the nociceptive system, including the pathways of pain impulses in the spinal cord. Reduces the concentration of short-lived prostaglandin H2, from which prostaglandin E2 is formed under the action of prostaglandin isomerase. A decrease in the concentration of prostaglandin E2 leads to a decrease in the degree of activation of EP type prostanoid receptors, which is expressed in analgesic and anti-inflammatory effects. It has a slight effect on COX-1, practically without interfering with the formation of prostaglandin E2 from arachidonic acid under physiological conditions, thereby reducing the number of side effects of the drug. The drug also suppresses platelet aggregation by inhibiting the synthesis of endoperoxides and thromboxane A2, inhibits the synthesis of platelet aggregation factor, and inhibits plasminogen activation by increasing the concentration of inhibitor-1. Suppresses the release of histamine and also reduces the degree of bronchospasm caused by exposure to histamine and acetaldehyde. Inhibits the release of tumor necrosis factor a, which causes the formation of cytokinins. It has been shown that nimesulide is able to suppress the synthesis of interleukin-6 and urokinase, thereby preventing the destruction of cartilage tissue. Inhibits the synthesis of metalloproteases (elastase, collagenase), preventing the destruction of proteoglycans and collagen of cartilage tissue. It has antioxidant properties and inhibits the formation of toxic oxygen breakdown products by reducing the activity of myeloperoxidase. Interacts with glucocorticoid receptors, activating them through phosphorylation, which also enhances the anti-inflammatory effect of the drug. Pharmacokinetics Absorption when taken orally is high. Eating reduces the rate of absorption without affecting its extent. The time to reach the maximum concentration of the active substance in the blood plasma is 1.5-2.5 hours. The connection with plasma proteins is 95%, with erythrocytes 2%, with lipoproteins 1%, with acidic alpha1-glycoproteins 1%. The dose of the drug does not affect the degree of its binding to blood proteins. The maximum concentration of nimesulide in blood plasma reaches 3.5-6.5 mg/l. Volume of distribution 0.19-0.35 l/kg. Penetrates into the tissues of the female genital organs, where after a single dose its concentration is about 40% of the concentration in plasma. Penetrates well into the acidic environment of the inflammation site (40%) and synovial fluid (43%). Easily penetrates histo-hematological barriers. Metabolized in the liver by tissue monooxygenases. The main metabolite 4-hydroxynimesulide (25%) has similar pharmacological activity. The half-life of nimesulide is 1.56-4.95 hours, 4-hydroxynimesulide 2.89-4.78 hours. 4-hydroxynimesulide is excreted by the kidneys (65%) and bile (35%). In patients with renal failure (creatinine clearance 1.8-4.8 l/h or 30-80 ml/min), as well as in children and the elderly, the pharmacokinetic profile of nimesulide does not change significantly.

Possible adverse reactions to Nimesil and overdose

Non-standard effects during treatment appear:

• allergies - with increased sweating, rashes, itching, erythema, urticaria, dermatitis, Lyell and Stevens-Johnson syndrome, Quincke's edema;
• problems with the hematopoietic system - anemic conditions, insufficient levels of platelets, leukocytes, red blood cells, hemorrhagic syndrome, thrombocytopenic purpura, increased number of eosinophils;
• visual and nervous disorders - panic attacks, vestibular dysfunction, cephalalgia, poor sleep with nightmares, non-inflammatory brain damage, unreasonable anxiety, drowsiness, decreased visual acuity;
• dysfunction of the circulatory system - rapid heartbeat, arterial hypertension, hot flashes, changes in blood pressure;
• pathologies of the digestive tract - dyspeptic disorders, gastritis, increased gas formation, painful sensations in the epigastric region, ulcers and perforation of the gastrointestinal tract, hepatitis, icteric discoloration of the skin, an increase in the number of liver enzymes.

When adverse reactions occur in the respiratory department, shortness of breath is observed. In other cases, there is a decrease in body temperature, hematuria, problems with urination, and asthenic syndrome.

Symptoms of an overdose of Nimesil include vomiting, apathy, nausea and drowsiness. In difficult cases, spontaneous bleeding develops in the gastrointestinal tract, sometimes there is an increase in blood pressure, acute kidney dysfunction, breathing problems, anaphylaxis, and coma.

To relieve the clinical manifestations of an overdose, symptomatic treatment is used, with gastric lavage, taking activated charcoal (1 tablet per 10 kg of weight), and an osmotic laxative. It is imperative to monitor the functionality of the liver and kidneys.

Methods and dosages in the instructions for use of Nimesil

The granular product is diluted in half a glass of water, the finished substance should be used immediately. The drug is taken orally, 1 sachet after meals, twice a day. Therapeutic manipulations should not exceed 2 weeks. To prevent the development of adverse reactions, the medication is prescribed in minimal effective dosages.

The instructions for use of Nimesil do not contain any special instructions for the treatment of children - in the period from 12 to 18 years, therapy is carried out at adult dosages. If the patient has a history of kidney disease, then the standard amount and frequency of use of the solution remains unchanged.

In old age, the characteristics of the body are taken into account; all changes in the therapy recommended by the manufacturer are carried out on the recommendation of a doctor. The specialist is based on the compatibility of the drug with other medications.

Doctors do not recommend using Nemisil for minor attacks of headache or without a prescription from a local physician. The drug is not suitable for continuous use and can cause serious adverse reactions, including anaphylactic shock and coma. The appearance of unusual clinical signs requires immediate contact with a local physician.

Instructions for use NIMESIL

Undesirable side effects can be minimized by using the lowest effective dose for the shortest duration necessary to control disease symptoms, as well as gastrointestinal and cardiovascular risks, below).

If there is no improvement in symptoms, drug therapy should be discontinued.

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 Nimesil® (for example, anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine) or patients whose laboratory tests of liver function deviate from normal values, 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.

During treatment with Nimesil®, the patient should refrain from taking other analgesics. The concomitant use of Nimesil® and other NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided.

Patients receiving nimesulide who develop flu-like or cold-like symptoms should discontinue treatment with the drug.

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, which can be fatal to the patient.

Gastrointestinal bleeding, ulcer and ulcer perforation:

Gastrointestinal bleeding, ulceration and ulcer perforation may be life-threatening if the patient's medical history shows similar problems occurring when taking any non-steroidal anti-inflammatory drugs during treatment (regardless of the elapsed time), with or without the presence of dangerous symptoms, or the presence of history of serious gastrointestinal disorders.

The risk of gastrointestinal bleeding, ulceration, or perforation of an ulcer increases with increasing doses of nonsteroidal anti-inflammatory drugs, 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 gastrointestinal toxicity, especially the elderly, should report any unusual gastrointestinal symptoms (especially gastrointestinal 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 oral corticosteroids, anticoagulants such as warfarin, selective serotonin reuptake inhibitors, or antiplatelet agents such as aspirin, should be advised to use the drug with caution.

If gastrointestinal bleeding or ulcers occur in patients receiving Nimesil®, treatment with the drug should be discontinued.

NSAIDs should be prescribed with caution to patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn's disease), since exacerbation of these diseases is possible.

Disorders of the cardiovascular and cerebrovascular systems:

Patients with arterial hypertension and/or a history of 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 of their condition and consultation with a physician.

Clinical studies and epidemiological data suggest that some nonsteroidal anti-inflammatory drugs, especially at high doses and when used for long periods of time, 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, acute heart failure, established coronary artery disease, peripheral arterial disease and/or cerebrovascular disease, nimesulide should be prescribed after careful evaluation. An equally careful consideration of the condition should be performed before initiating long-term treatment in patients with risk factors for cardiovascular disease (eg, hypertension, hyperlipidemia, diabetes mellitus, smoking).

In patients with renal or heart failure, Nimesil® should be used with caution, as the drug may worsen renal function. If the condition worsens, treatment should be discontinued.

Elderly patients are particularly susceptible to adverse reactions to NSAIDs, including gastrointestinal bleeding and perforation, and deterioration of renal, hepatic, and cardiac function. Therefore, appropriate clinical monitoring is advisable.

Since nimesulide can affect platelet function, it should be prescribed with caution to patients with bleeding diathesis. However, Nimesil® does not replace acetylsalicylic acid in the prevention of cardiovascular diseases.

There are very rare reports of serious skin reactions to non-steroidal anti-inflammatory drugs, some of which can be fatal. Including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis. Patients are at very high risk of such reactions if, with a previously prescribed course of treatment, the onset of the reaction in most cases occurred during the first month of treatment. Nimesil® should be discontinued at the first signs of a skin rash, damage to the mucous membranes and other signs of an allergic reaction.

Nimesil® contains sucrose. This drug should not be prescribed to patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption, or sucrase-isomaltase deficiency.

Impact on the ability to drive vehicles and operate machinery

Studies on the effects of nimesulide-containing drugs on the ability to drive vehicles and operate machines and mechanisms have not been conducted. Despite this, patients experiencing headache, dizziness or drowsiness after taking Nimesil® should not drive a vehicle, machinery or machinery.