Nimesulide tablets: instructions, reviews and prices. Dosage and administration Nimesulide in the form of granules. Action and therapeutic effects

Nemulex is known as an analgesic, anti-inflammatory and antipyretic agent.

Available in packs of 10 or 30 sachets. Inside contains granules that are used to prepare a suspension for oral administration.

One dose contains 100 mg of nimesulide. The solution, like the powder itself, has a light yellow tint, and is packaged in packs of 2-4-6-10-20-30 bags.

The composition of the product

Nemulex contains:

100 mg nimesulide;
100 mg macrogol cetostearate (auxiliary);
19 mg citric acid;
sucrose 1721 mg;
40 mg colloidal silicon dioxide;
20 mg orange flavor.

Pharmacological action of the drug

The drug affects the body in several planes:

anti-inflammatory;
antipyretic;
painkiller;
antiaggregatory.

Pharmacokinetics means

When taking the medicine inside, there is a high absorption of the drug. When eating, it decreases.

In the blood, the drug in high concentration is up to 2.5 hours.

It binds best to plasma proteins, and to a very small extent to erythrocytes.

It penetrates well into the focus of inflammation, on average this figure is up to 40%.

It is excreted from the body with the help of the liver, kidneys and bile.

Mechanism of action

Nemulex has an inhibitory effect on prostaglandins at the site of inflammation. The drug is used for symptomatic treatment.

It blocks various pain sensations and inhibits the inflammatory process, but all this happens only for the duration of the drug. The drug has no effect on the progress of the disease.

To whom is the medicine prescribed?

Indications for use:

The drug does not have a therapeutic effect, it relieves only pain and inflammation of an episodic nature.

ulcer 12 of the duodenum and stomach;
polyps, bronchial asthma and aspirin intolerance in history;
bleeding of the gastrointestinal tract and its inflammation in the acute phase;
cardiac and hepatic dysfunction;
hemophilia;
alcohol addiction;
drug addiction;
kidney problems;
condition after coronary artery bypass grafting;
hyperkalemia;
intolerance to the components of the drug;
children under 12 years of age;
pregnancy and lactation;
co-administration of other hepatoxic drugs.

With caution, it is necessary to take the elderly with coronary artery disease, heart failure, patients with diabetes mellitus.

How to take medicine?

It is necessary to dissolve the contents of the package in half a glass of water. For adults and children over 14, the dosage will be no more than 100 mg - 2 times a day.

Reception must be carried out after a meal. In renal failure, no more than 100 mg per day. To minimize side effects, the drug should be prescribed in small doses. The period of use of funds is not more than 2 weeks.

The choice of dosage according to the patient's condition

This drug is recommended to take no more than 200 mg per day, regardless of the nature of the pain.

For toothache and headache, as well as menstrual pain, no more than 1 packet per day. With an increase in temperature and a flu-like condition, the medicine should be discontinued.

In postoperative and post-traumatic situations, you can take 100 mg twice a day, morning and evening, to relieve paroxysmal pain.

For arthrosis and myalgia, the drug should be taken as prescribed by a doctor, but not more than 200 mg per day. The same applies to chronic diseases for which this remedy is prescribed.

In the presence of renal failure, the dosage is reduced to 100 mg per day.

The total duration of admission is not more than 15 days. With a longer intake, it is necessary to monitor the condition of the liver. The drug affects fertility, so it is not practiced if pregnancy is planned.

Cases of overdose

Signs of an overdose of the drug are:

nausea;
vomit;
drowsiness;
increase in pressure;
respiratory depression;
bleeding from the gastrointestinal tract;
apathy.

First aid for overdose

There is no antidote for this drug. It is necessary to do a gastric lavage and drink a laxative, in addition, activated charcoal is prescribed.

The state of the liver and kidneys is monitored.

special instructions

With vomiting, flatulence, abdominal pain, symptomatic assistance is necessary.

In the presence of allergic reactions, rashes, urticaria and other reactions of the body, it is necessary to take antihistamines in order to prevent anaphylactic shock.

For other side effects, first aid is provided depending on the manifestation of symptoms.

If the functions of the liver and kidneys are impaired, the drug is not prescribed.

During pregnancy and lactation is not prescribed. Children are allowed to receive from the age of 14.

Taking with other medicines

Nemulex enhances the effect of Cyclosporine. Reduces the effectiveness of salicylic acid, Furosemide and some drugs.

It is not recommended to take it together with diuretics, as well as glucocorticosteroids and serotonin reuptake blockers. Since in the first case, the kidneys suffer, and in the second, bleeding of the gastrointestinal tract is possible.

Expert opinion

In their reviews, doctors generally speak positively about Nemulex.

From the practice of application

Patients' opinion.

Patient Admission Tips:

should not be taken on an empty stomach;
do not need to be taken by those who have problems with the gastrointestinal tract (ulcers, colitis);
dilute the product in water, do not pour the powder into your mouth, drowsiness may occur;
do not mix with juices or other drinks, only water.

Pros and cons of the tool

efficiency;
quickly absorbed due to dissolution in water;
relieves several symptoms at once.

must be dissolved in water before taking;
many side effects, not suitable for everyone.

Buying and storing medicine

The price of 10 packages of Nemulex is an average of 182 rubles. The cost depends on the number of bags in the package.

Shelf life 4 years. Store at room temperature in a dark, dry place. The release is by prescription.

How to replace the drug?

Nemulex has a large number of analogues:

Nemulex and Nimesil: two drug brothers

Since the dose of nimesulide in the preparations is absolutely the same, then choose the drug that is cheaper.

The effect of using the tool is similar. They can differ only in taste, due to flavors. Any of these drugs should be prescribed by a doctor. The difference in drugs is only in price.

Just like that, without a doctor's prescription, it is not accepted, so each time the specialist evaluates the severity of the disease and the benefits of the drug in a particular case.

It is most often used as a strong analgesic and anti-inflammatory agent, since the effect occurs very quickly, in just a few minutes.

Nimid is a non-steroidal anti-inflammatory drug. Its active ingredient is nimesulide. Such a tool is able to eliminate inflammation, temperature and moderate pain. It is recommended for inflammation of the joints and tissues around them (osteoarthritis, rheumatism), gynecological and inflammatory diseases. In addition, the drug helps to avoid the process of cartilage tissue destruction due to the property of suppressing the synthesis of interleukin-6 and urokinase. And by reducing the level of toxins in inflammatory tissues, the agent is able to have an antioxidant effect.

Composition and forms of release

Instructions for use of the drug indicates the variety of means:

Powders, granules. Active agent: in 2 g of powder - 100 mg of nimesulide. The package contains 30 sachets of 2 g.
Tablets. 1 tablet contains 100 mg of nimesulide. The package contains 1-10 plates (10 tablets each).
Tablets with enhanced formula Nimid Forte. Contains 100 mg nimesulide, tizanidine hydrochloride (2 mg tizanidine). The package contains 1 plate of 10 tablets.
Gel. 1 g of gel contains 10 mg of nimesulide.

pharmachologic effect

The active substance nimesulide is a non-steroidal anti-inflammatory drug from the group of sulfonanilides. It reduces fever, reduces pain, relieves inflammation. The effectiveness of this drug is associated with the action of the arachidonic acid cascade, which reduces the biosynthesis of prostaglandins.

The drug is well absorbed when taken orally. The maximum dose after application is reached in 1.5-2 hours. Eating reduces the rate of absorption of the drug, but this does not affect the therapeutic effect. Nimesulide is displayed:

with urine - about 50%;
with feces about 29%;
1-3% is excreted unchanged.

When the drug is prescribed

Indications for use:

with sore teeth;
joint pain;
bruises;
dislocations;
osteoporosis;
rheumatism;
pain in the muscles, back;
radiculitis;
during a headache.

It helps to reduce pain during sprains, with injured tendons and muscles. Doctors recommend using it in cases of fever, if the patient is diagnosed with inflammation of the ear, nose, throat. The ointment is used for inflammation and degenerative changes in the musculoskeletal system.

Contraindications for use

Like other drugs, Nimid has its own contraindications:

It should not be taken if a person has a stomach disease, an ulcer (during an exacerbation).
Liver disorders.
The medication is contraindicated in the presence of an allergy to the components included in the composition, as well as with urticaria.
In the form of a gel, it is contraindicated in patients with severe sensitivity to irritants, with infections, violation of the integrity of the skin.
Prohibited medication for asthma patients.
Pregnant women and while breastfeeding.
Do not take the remedy for cerebrovascular bleeding.
Alcoholism and drug addiction are also contraindications.

Rules for taking the drug

Instructions for use indicate that Nimid tablets are consumed after meals. Wash them down with a little water. The medicine is not chewed.

In the form of tablets, Nimid Forte is prescribed only for adults.

The drug in granules is drunk after meals. To do this, Nimid powder is poured into a glass, poured with water, preferably warm. Dissolve the powder immediately before use.

Nimid gel is prescribed topically. To do this, it is applied to painful areas. Spread with a thin layer. The ointment is not rubbed into the skin, left until completely absorbed. The place to which it is applied must first be cleaned for better absorption. Apply 3-4 times a day.

Elderly people and children from 12 years of age do not need dose adjustment. The duration of therapy is determined individually. The maximum course of treatment is 15 days. The dosage and duration of therapy are prescribed by the doctor.

Adverse reactions and overdose

Tolerability of the drug is good, but side effects that are associated with different body systems are possible:

There may be dizziness, headache.
Often there is diarrhea or constipation, vomiting, nausea, pain in the abdomen.
Some patients are diagnosed with skin rashes, itching, increased sweating.
There are side effects associated with the nervous system: nervousness, nightmares, anxiety.
There may be an increase in pressure, shortness of breath, blurred vision.

There are special instructions that must be taken into account when using Nimid in order to avoid side effects.

If you use the medication according to the instructions, not exceeding the allowable and recommended doses, observing the multiplicity, then all side effects will be minimized or not appear.

If the patient takes the drug and does not see the effectiveness, you need to stop treatment. If flu symptoms occur at the time of taking the medicine, stop taking the medicine.

During the use of additional drugs, attention should be paid to their interaction with the components of Nimid. This will help avoid any unwanted consequences. The drug is taken with caution simultaneously with such drugs: Aspirin, Warfarin, Furosemide, Theophylline, Digoxin, Glibenclamide. In the case of the use of Methotrexate, a break between doses of drugs should be taken at 24 hours. Nimid can increase the concentration of the active substance in the blood, which will cause an increase in toxicity.

In cases of overdose, the following symptoms may occur:

nausea;
vomit;
pain in the stomach;
drowsiness;
apathy.

If an overdose is detected in the first 4 hours, the patient may induce vomiting, take a laxative and activated charcoal. If the measures taken are ineffective, you should go to the hospital.

Analogues and patient reviews

Nimid is an imported drug. The manufacturer is Kusum Helthker (India).

It has analogues:

Nimesulide-Darnitsa (Ukraine).
Nise (India).
Nimesil (Italy).
Nimegezik (India).
Nimulid (India).

The price of the product in comparison with analogues is average. The tool is not cheap, but almost every patient can afford to buy it.

NSAIDs. Selective COX-2 inhibitor

Active substance

Release form, composition and packaging

Granules for suspension for oral administration in the form of a light yellow granular powder with an orange smell.

Excipients: ketomacrogol 1000, sucrose, maltodextrin, anhydrous citric acid, orange flavor.

2 g - laminated paper bags (9) - packs of cardboard.
2 g - paper bags laminated (15) - packs of cardboard.
2 g - paper bags laminated (30) - packs of cardboard.

pharmachologic effect

Non-steroidal anti-inflammatory drug from the class of sulfonamides. It has anti-inflammatory, analgesic and antipyretic effects. Nimesulide acts as an inhibitor of the cyclooxygenase enzyme responsible for the synthesis of prostaglandins and inhibits mainly cyclooxygenase-2.

Pharmacokinetics

After oral administration, the drug is well absorbed from the gastrointestinal tract, reaching C max in the blood after 2-3 hours. Plasma protein binding is 97.5%. T 1/2 is 3.2-6 hours. Easily penetrates through histohematic barriers.

It is metabolized in the liver by cytochrome P450 (CYP) 2C9 isoenzyme. The main metabolite is the pharmacologically active parahydroxy derivative of nimesulide, hydroxynimesulide. Hydroxynimesulide is excreted in the bile in a metabolized form (found exclusively in the form of glucuronate - about 29%).

Nimesulide is excreted from the body, mainly by the kidneys (about 50% of the dose taken). The pharmacokinetic profile of nimesulide in the elderly does not change when prescribing single and multiple / repeated doses.

According to a pilot study conducted with the participation of patients with mild to moderate renal insufficiency (CC 30-80 ml / min) and healthy volunteers, Cmax of nimesulide and its metabolite in the plasma of patients did not exceed the concentration of nimesulide in healthy volunteers. AUC and T 1/2 in patients with renal insufficiency were higher by 50%, but within the pharmacokinetic values. With repeated administration of the drug, cumulation is not observed.

Indications

- treatment of acute pain (pain in the back, lower back; pain in the musculoskeletal system, including injuries, sprains and dislocations of the joints, tendinitis, bursitis; toothache);

- symptomatic treatment of osteoarthritis with pain syndrome;

- algomenorrhea.

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use.

Contraindications

- a history of hyperergic reactions, for example, bronchospasm, rhinitis, urticaria associated with taking or other NSAIDs, incl. nimesulide;

- hepatotoxic reactions to nimesulide in history;

- concomitant (simultaneous) use of drugs with potential hepatotoxicity, for example, or other analgesic or non-steroidal anti-inflammatory drugs;

- inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase;

- the period after coronary artery bypass grafting;

- fever in infectious and inflammatory diseases;

- full or partial combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses with intolerance to acetylsalicylic acid and other NSAIDs (including history);

- peptic ulcer of the stomach and duodenum in the acute phase, the presence of an ulcer in history, perforation or bleeding in the gastrointestinal tract;

- a history of cerebrovascular bleeding or other bleeding, as well as diseases accompanied by bleeding;

- severe blood clotting disorders;

- severe insufficiency;

- severe renal insufficiency< 30 мл/мин), подтвержденная гиперкалиемия;

- liver failure or any active liver disease;

- children's age up to 12 years;

- pregnancy and breastfeeding period;

- alcoholism, drug addiction;

- Hypersensitivity to the components of the drug.

Carefully: severe arterial hypertension, type 2 diabetes mellitus, heart failure, coronary heart disease, cerebrovascular disease, dyslipidemia/hyperlipidemia, peripheral arterial disease, smoking, CC< 60 мл/мин, анамнестические данные о наличии язвенного поражения ЖКТ, инфекции, вызванной Helicobacter pylori; пожилой возраст; длительное предшествующее использование НПВП; тяжелые соматические заболевания; сопустствующая терапия следующими препаратами: антикоагулянты (например, варфарин), антиагреганты (например, ацетилсалициловая кислота, клопидогрел), пероральные глюкокортикостероиды (например, преднизолон), селективные ингибиторы обратного захвата серотонина (например, циталопрам, флуоксетин, сертралин).

The decision to prescribe the drug Nimesil should be based on an individual risk-benefit assessment when taking the drug.

Dosage

Nimesil is taken orally, 1 sachet (100 mg of nimesulide) 2 times / day. The drug is recommended to be taken after meals. The contents of the sachet are poured into a glass and dissolved in about 100 ml of water. The prepared solution cannot be stored.

Nimesil is used only for the treatment of patients older than 12 years.

Patients with impaired renal function: based on pharmacokinetic data, there is no need to adjust the dose in patients with mild to moderate renal insufficiency (CC 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, the minimum effective dose should be used for the shortest possible course.

Side effects

From the side of the hematopoietic system: rarely - anemia, eosinophilia, hemorrhagic syndrome; very rarely - thrombocytopenia, pacitopenia, 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).

From the CNS: infrequently - dizziness; rarely - a feeling of fear, nervousness, nightmares; very rarely - headache, drowsiness, encephalopathy (Reye's syndrome).

From the organ of vision: rarely - blurred vision.

From the side of the cardiovascular system: infrequently - arterial hypertension, tachycardia, arterial pressure lability, hot flashes.

From the respiratory system: infrequently - shortness of breath; very rarely - exacerbation of bronchial asthma, bronchospasm.

From the digestive system: often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, dyspepsia, stomatitis, tarry stools, gastrointestinal bleeding, ulcers and / or perforation of the stomach or duodenum; very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis, increased activity of liver enzymes.

From the urinary system: 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, pain in the epigastric region. With maintenance therapy for gastropathy, 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.

Treatment: carry out symptomatic therapy. There is no specific antidote. If an overdose has occurred within the last 4 hours, it is necessary to induce vomiting and / or provide activated charcoal (adults from 60 to 100 g) and / or an osmotic laxative. Forced diuresis, hemodialysis are ineffective due to the high connection of the drug with proteins (up to 97.5%). Control of function of kidneys and a liver is shown.

drug interaction

Pharmacodynamic interactions:

When combined with glucocorticosteroids, the risk of gastrointestinal ulcers or bleeding increases.

When combined with antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs), such as fluoxetine, the risk of gastrointestinal bleeding increases.

NSAIDs may increase the effect of anticoagulants such as warfarin. 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.

Diuretics:

NSAIDs can weaken the effect of diuretics.

In healthy volunteers, nimesulide temporarily reduces sodium excretion under the action of furosemide, to a lesser extent, potassium excretion, and reduces the actual diuretic effect.

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 furomeside.

The co-administration of furosemide and nimesulide requires caution in patients with impaired renal and cardiac function.

ACE inhibitors and angiotensin II receptor antagonists:

NSAIDs may reduce the effect. In patients with mild to moderate renal insufficiency (CC 30-80 ml / min), with the joint appointment of ACE inhibitors, angiotensin II receptor antagonists or substances that suppress the cyclooxygenase system (NSAIDs, antiplatelet agents), further deterioration of renal function and the occurrence of acute renal failure are possible. 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 combined use of these drugs should be prescribed with caution, especially for elderly patients. Patients should be adequately hydrated and renal function should be closely monitored after initiation of concomitant therapy.

Pharmacokinetic interactions with other drugs:

There is evidence that NSAIDs reduce the clearance of lithium, which leads to an increase in the concentration of lithium in the blood plasma and its toxicity. When prescribing nimesulide to patients receiving lithium therapy, regular monitoring of plasma lithium concentrations should be carried out.

Clinically significant interactions with glibenclamide, theophylline, digoxin, cimetidine and antacids (for example, a combination of aluminum and magnesium hydroxides) were not observed.

Nimesulide inhibits the activity of the CYP2C9 isoenzyme. While taking drugs that are substrates of this enzyme with nimesulide, the concentration of these drugs in plasma may increase.

In connection with the action on renal prostaglandins, prostaglandin synthetase inhibitors, such as nimesulide, may increase the nephrotoxicity of cyclosporins.

Interaction of other drugs with nimesulide:

In vitro studies have shown that nimesulide is displaced from the binding sites by tolbutamide 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.

special instructions

Unwanted side effects can be minimized by using the lowest effective dose of the drug for the shortest possible course.

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

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 complicated by bleeding or perforation, as well as in elderly patients, so treatment should be started with the lowest possible dose. Patients receiving drugs that reduce blood clotting or inhibit platelet aggregation also increase the risk of gastrointestinal bleeding. In the event of gastrointestinal bleeding or ulcers in patients taking Nimesil, treatment with the drug should be discontinued.

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 (skin itching, yellowing of the skin, nausea, vomiting, abdominal pain, dark urine, increased activity of "liver" transaminases), you should stop taking the drug and consult your doctor.

Despite the rarity of visual impairment in patients taking nimesulide simultaneously with other NSAIDs, treatment should be stopped immediately. If any visual disturbance occurs, the patient should be examined by an ophthalmologist.

The drug can cause fluid retention in the tissues, so patients with high blood pressure and cardiac disorders should use Nimesil 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 discontinued.

Clinical studies and epidemiological data suggest that NSAIDs, especially at high doses and with long-term use, may lead to a small risk of myocardial infarction or stroke. There are not enough data to exclude the risk of such events when using nimesulide.

The composition of the drug includes sucrose, this should be taken into account for patients with diabetes mellitus (0.15-0.18 XE per 100 mg of the drug) and people on a low-calorie diet. Nimesil is not recommended for patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltose deficiency.

If there are signs of a "cold" or an acute respiratory viral infection during treatment with Nimesil, the drug should be discontinued.

Nimesil should not be used 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 preventive effect of acetylsalicylic acid in cardiovascular diseases.

Elderly patients are particularly susceptible to adverse reactions to NSAIDs, including life-threatening gastrointestinal bleeding and perforations, deterioration of kidney, liver and heart function. When taking the drug Nimesil for this category of patients, proper clinical monitoring is necessary.

Like other NSAIDs that inhibit prostaglandin synthesis, nimesulide may adversely affect pregnancy and/or fetal development and may lead to premature closure of the ductus arteriosus, hypertension in the pulmonary artery system, impaired renal function, which may progress to renal failure. with oligodyramnia, to an increased risk of bleeding, a decrease in uterine contractility, the occurrence of peripheral edema. In this regard, nimesulide is contraindicated during pregnancy and lactation. The use of the drug Nimesil can adversely affect female fertility and is not recommended for women planning a pregnancy. When planning pregnancy, consultation with your doctor is necessary.

There is evidence of the occurrence in rare cases of skin reactions (such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) to nimesulide as well as to other NSAIDs. At the first sign of a skin rash, mucosal lesions or other signs of an allergic reaction, Nimesil should be discontinued.

The 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 period of treatment with Nimesil, care should be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Pregnancy and lactation

Like other NSAIDs that inhibit prostaglandin synthesis, nimesulide may adversely affect pregnancy and/or fetal development and may lead to premature closure of the ductus arteriosus, hypertension in the pulmonary artery system, impaired renal function, which may progress to renal failure. with oligodyramnia, to an increased risk of bleeding, a decrease in uterine contractility, the occurrence of peripheral edema. In this regard, the drug is contraindicated during pregnancy and during breastfeeding.

Application in childhood

The drug is contraindicated in children under the age of 12 years.

Teenagers (ages 12 to 18): based on the pharmacokinetic profile and pharmacodynamic characteristics of nimesulide, there is no need for dose adjustment in adolescents.

For impaired renal function

In patients with renal insufficiency, Nimesil should be used with caution, as renal function may deteriorate. If the condition worsens, treatment with Nimesil should be discontinued. The drug is contraindicated in severe renal insufficiency (CC< 30 мл/мин).

In patients with mild to moderate renal insufficiency (CC 30-80 ml / min), there is no need to adjust the dose.

For impaired liver function

The drug is contraindicated in liver failure or any active liver disease.

Use in the elderly

The drug is prescribed with caution to elderly patients. Elderly patients are particularly susceptible to adverse reactions to NSAIDs, including life-threatening gastrointestinal bleeding and perforations, deterioration of kidney, liver and heart function. When taking the drug Nimesil for this category of patients, proper clinical monitoring is necessary.

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.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

Storage conditions:

List B. Store in a dry, dark place and out of the reach of children at a temperature not exceeding 25 ° C.

Best before date:

Do not use after the expiry date stated on the packaging.

Trade name of the drug: Nimesil ®

International Nonproprietary Name (MIN): nimesulide

Dosage form: granules for suspension for oral administration.

Compound:

1 package contains:
Active substance: nimesulide 100 mg;
Excipients: ketomacrogol 1000, sucrose, maltodextrin, anhydrous citric acid, orange flavor.

Description: light yellow granular powder with an orange smell.

Pharmacotherapeutic group:

non-steroidal anti-inflammatory drugs (NSAIDs).

ATC Code: M01AX17

Pharmacological properties

Pharmacodynamics Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) from the sulfonamide class. It has anti-inflammatory, analgesic and antipyretic effects. Nimesulide acts as an inhibitor of the cyclooxygenase enzyme responsible for the synthesis of prostaglandins and inhibits mainly cyclooxygenase 2.

Pharmacokinetics After oral administration, the drug is well absorbed from the gastrointestinal tract, reaching a maximum plasma concentration in 2-3 hours; connection with plasma proteins - 97.5%; the half-life is 3.2-6 hours. Easily penetrates through histohematic barriers.
It is metabolized in the liver by cytochrome P450 (CYP) 2C9 isoenzyme. The main metabolite is the pharmacologically active parahydroxy derivative of nimesulide, hydroxynimesulide. Hydroxynimesulide is excreted in the bile in a metabolized form (found exclusively in the form of glucuronate - about 29%). Nimesulide is excreted from the body, mainly by the kidneys (about 50% of the dose taken). The pharmacokinetic profile of nimesulide in the elderly does not change when prescribing single and multiple / repeated doses.
According to a pilot 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 metabolite in the plasma of patients did not exceed the concentration of nimesulide in healthy volunteers. The area under the concentration-time curve (AUC) and half-life in patients with renal insufficiency were higher by 50%, but within the pharmacokinetic values. With repeated administration of the drug, cumulation is not observed.

Indications for use

Treatment of acute pain (pain in the back, lower back; pain in the musculoskeletal system, including injuries, sprains and dislocations of the joints; tendonitis, bursitis; toothache);
Symptomatic treatment of osteoarthritis with pain syndrome;
Algodysmenorrhea.

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 use of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs, including nimesulide. Hepatotoxic reactions to nimesulide (history).
Concomitant (simultaneous) use of drugs with potential hepatotoxicity, for example, paracetamol or other analgesic or non-steroidal anti-inflammatory drugs.
Inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase. The period after coronary artery bypass grafting.
Feverish syndrome with colds and acute respiratory viral infections.
Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses with intolerance to acetylsalicylic acid and other NSAIDs (including history);
Peptic ulcer of the stomach or duodenum in the acute phase, a history of ulcers, perforations or bleeding in the gastrointestinal tract.
A history of cerebrovascular bleeding or other bleeding, as well as diseases accompanied by bleeding.
Severe bleeding disorders.
Severe heart failure.
Severe renal failure (creatinine clearance<30 мл/мин), подтвержденная гиперкалиемия.
Liver failure or any active liver disease.
Children under the age of 12.
Pregnancy and lactation.
Alcoholism, drug addiction.

Carefully: severe arterial hypertension, type 2 diabetes mellitus, heart failure, coronary heart disease, cerebrovascular disease, dyslipidemia/hyperlipidemia, peripheral arterial disease, smoking, creatinine clearance less than 60 ml/min.

Anamnestic data on the presence of ulcerative lesions of the gastrointestinal tract, infection caused by Helicobacter pylori; elderly age; long-term prior use of NSAIDs; severe somatic diseases.

Concomitant therapy with the following drugs: anticoagulants (eg, warfarin), antiplatelet agents (eg, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (eg, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline). The decision to prescribe the drug Nimesil ® should be based on an individual risk-benefit assessment when taking the drug.

Dosage and administration

Nimesil is taken orally, 1 sachet (100 mg nimesulide) twice a day. The drug is recommended to be taken after meals. The contents of the sachet are poured into a glass and dissolved in about 100 ml of water. The prepared solution cannot be stored.

Nimesil ® is used only for the treatment of patients older than 12 years.

Teenagers (from 12 to 18 years old): based on the pharmacokinetic profile and pharmacodynamic characteristics of nimesulide, there is no need for dose adjustment in adolescents.

Patients with impaired renal function: based on pharmacokinetic data, there is no need to adjust the dose in patients with mild to moderate renal insufficiency (creatinine clearance 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, the minimum effective dose should be used for the shortest possible course.

Side effects

The frequency is classified into rubrics, depending on the occurrence of the case: very often (> 10), often (<10-<100), нечасто (<100-<1000), редко (<1000-<10000), очень редко (<10000).

Disorders of the circulatory and lymphatic systems: rarely - anemia, eosinophilia, hemorrhages; 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).

Central nervous system disorders: infrequently - dizziness; rarely - a feeling of fear, nervousness, nightmares; very rarely - headache, drowsiness, encephalopathy (Reye's syndrome).

Sensory disturbances: rarely - blurred vision.

Cardiovascular disorders: infrequently - arterial hypertension, tachycardia, arterial pressure lability, hot flashes.

Respiratory system disorders: infrequently - shortness of breath; very rarely - exacerbation of bronchial asthma, bronchospasm.

Gastrointestinal disorders: often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, dyspepsia, stomatitis, tarry stools, gastrointestinal bleeding, ulcers and / or perforation of the stomach or duodenum.

Liver and biliary disorders: very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis, increased activity of liver enzymes.

Renal and urinary disorders: rarely - dysuria, hematuria, urinary retention; very rarely - renal failure, oliguria, interstitial nephritis.

General violations: rarely - malaise, asthenia; very rarely - hypothermia.

Others: rarely - hyperkalemia.

Overdose

Symptoms: apathy, drowsiness, nausea, vomiting, pain in the epigastric region. With maintenance therapy for gastropathy, 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.

Treatment: Symptomatic. There is no specific antidote. If an overdose has occurred within the last 4 hours, it is necessary to induce vomiting and / or provide activated charcoal (60 to 100 g per adult) and / or an osmotic laxative. Forced diuresis, hemodialysis are ineffective due to the high connection of the drug with proteins (up to 97.5%). Control of function of kidneys and a liver is shown.

Interaction with other drugs

Pharmacodynamic interactions:

Glucocorticosteroids: increase the risk of gastrointestinal ulcers or bleeding.

Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs), such as fluoxetine: increase the risk of gastrointestinal bleeding.

Anticoagulants: NSAIDs may increase the effect 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 still cannot be avoided, careful monitoring of blood coagulation parameters should be carried out.

Diuretics

NSAIDs may reduce the effect of diuretics.

In healthy volunteers, nimesulide temporarily reduces sodium excretion under the action of furosemide, to a lesser extent, potassium excretion, and reduces the actual diuretic effect.

The co-administration of furosemide and nimesulide requires caution in patients with impaired renal or cardiac function.

ACE inhibitors and angiotensin-II receptor antagonists

NSAIDs may reduce the effect of antihypertensive drugs. In patients with mild to moderate renal insufficiency (creatinine clearance 30-80 ml / min), with the joint appointment of ACE inhibitors, angiotensin II receptor antagonists or substances that suppress the cyclooxygenase system (NSAIDs, antiplatelet agents), further deterioration of kidney function and the occurrence of acute renal failure, 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 combined use of these drugs should be prescribed with caution, especially for elderly patients. Patients should be adequately hydrated and renal function should be closely monitored after initiation of concomitant therapy.

Pharmacokinetic interactions with other drugs:

Clinically significant interactions with glibenclamide, theophylline, digoxin, cimetidine and antacids (for example, a combination of aluminum and magnesium hydroxides) were not observed.

Nimesulide inhibits the activity of the CYP2C9 isoenzyme. While taking drugs that are substrates of this enzyme with nimesulide, the concentration of these drugs in plasma may increase.

When prescribing nimesulide less than 24 hours before or after taking methotrexate, caution is required, 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, prostaglandin synthetase inhibitors, such as nimesulide, may increase the nephrotoxicity of cyclosporins.

Interaction of other drugs with 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.

special instructions

Unwanted side effects can be minimized by using the lowest effective dose of the drug for the shortest possible course. Nimesil ® should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn's disease), since exacerbation of these diseases is possible.

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 signs of liver damage appear (skin itching, yellowing of the skin, nausea, vomiting, abdominal pain, darkening of urine, increased activity of "liver" transaminases), you should stop taking the drug and consult your doctor. Despite the rarity of visual impairment in patients taking nimesulide simultaneously with other NSAIDs, treatment should be stopped immediately. If any visual disturbance occurs, the patient should be examined by an ophthalmologist. The drug can cause fluid retention in the tissues, so patients with high blood pressure and cardiac disorders 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 discontinued. Clinical studies and epidemiological data suggest that NSAIDs, especially at high doses and with long-term use, may lead to a small risk of myocardial infarction or stroke. There are not enough data to exclude the risk of such events when using nimesulide. The composition of the drug includes sucrose, this should be taken into account for patients with diabetes mellitus (0.15-0.18 XE per 100 mg of the drug) and people on a low-calorie diet. Nimesil is not recommended for use in patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltose deficiency.

If there are signs of a "cold" or an acute respiratory viral infection during treatment with Nimesil ®, the drug should be discontinued. Do not use Nimesil ® simultaneously with other NSAIDs.

Elderly patients are particularly susceptible to adverse reactions to NSAIDs, including the risk of life-threatening gastrointestinal bleeding and perforation, deterioration of kidney, liver and heart function. When taking the drug Nimesil ® for this category of patients, proper clinical monitoring is necessary.

Like other NSAIDs that inhibit prostaglandin synthesis, nimesulide may adversely affect pregnancy and/or fetal development and may lead to premature closure of the ductus arteriosus, hypertension in the pulmonary artery system, impaired renal function, which may progress to renal failure. with oligohydramnia, to an increased risk of bleeding, a decrease in uterine contractility, the occurrence 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 pregnancy. When planning pregnancy, consultation with your doctor is necessary.

The effect of the drug on the ability to drive vehicles and control mechanisms

The effect of the drug Nimesil ® on the ability to drive vehicles and control mechanisms has not been studied, therefore, during the period of treatment with Nimesil ®, care should be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Release form

Granules for suspension for oral administration, 100 mg.

2 g of granulate in three-layer bags (paper / aluminum / polyethylene).

9.15 or 30 bags with instructions for use in a cardboard box.

Storage conditions

List B.

Store in a dry, dark place at a temperature not exceeding 25°C. Keep out of the reach of children!

Best before date

Do not use after the expiry date stated on the packaging.

Vacation from pharmacies

By prescription.

Applicant/manufacturer:

"Laboratory Guidotti S.P.A.", Italy, produced by "Laboratory Menarini S.A.", Spain
Distributor: Berlin - Chemi/Menarini Pharma GmbH Glieniker Weg 125, 12489 Berlin, Germany
Address for filing claims: 115162, Moscow, st. Shabolovka, house 31, building B

Minimum age from.	12 years old
Mode of application	oral
Amount in a package	30 pcs
Best before date	24 months
Maximum allowable storage temperature, °С	25°C
Storage conditions	in a dry place In a place protected from the sun Keep away from children
Release form	Granules
Manufacturer country	Russia
Vacation order	On prescription
Active substance	Nimesulide (Nimesulide)
Pharmacological group	M01AX17 Nimesulide

Instructions for use

Active ingredients

Release form

Compound

1 package contains: active substance: nimesulide 100 mg; ; excipients: orange flavor 5 mg, crospovidone 140 mg, anhydrous citric acid 25 mg, maltodextrin 15 mg, sucrose 1715 mg.

Pharmacological effect

NSAIDs, has anti-inflammatory, analgesic, antipyretic and antiplatelet effects. Unlike other NSAIDs, it selectively inhibits cyclooxygenase-2 (COX-2), inhibits the synthesis of prostaglandins (Pg) in the focus of inflammation; has a less pronounced inhibitory effect on cyclooxygenase-1 (COX-1) (rarely causes side effects associated with inhibition of Pg synthesis in healthy tissues).

Pharmacokinetics

Absorption: After oral administration, the drug is well absorbed from the gastrointestinal tract (GIT), reaching a maximum concentration (Cmax) in blood plasma after 2-3 hours. Distribution: Communication with plasma proteins - 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acidic alpha1-glycoproteins - 1%. It penetrates into the tissues of the female genital organs, where, after a single dose, its concentration is about 40% of the plasma concentration. It penetrates well into the acidic environment of the focus of inflammation (40%), synovial fluid (43%). Easily penetrates through histohematic barriers. Metabolism. It is metabolized in the liver by cytochrome P450 (CYP) 2C9 isoenzyme. The main metabolite is the pharmacologically active parahydroxy derivative of nimesulide, hydroxynimesulide. Withdrawal: The half-life (T1 / 2) of nimesulide is about 1.56-4.95 hours, hydroxynimesulide is 2.89-4.78 hours. Nimesulide is excreted from the body, mainly by the kidneys (about 50% of the dose taken). Hydroxynimesulide is excreted by the kidneys (65%) and bile (35%), undergoes enterohepatic recirculation. ; The pharmacokinetic profile of nimesulide in the elderly does not change when prescribing single and multiple / repeated doses. According to a pilot 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 metabolite in the plasma of patients did not exceed the concentration of nimesulide in healthy volunteers. The area under the concentration-time curve (AUC) and half-life in patients with renal insufficiency were higher by 50%, but within the pharmacokinetic values. With repeated administration of the drug, cumulation is not observed.

Indications

Treatment of acute pain (pain in the back, lower back; pain in the musculoskeletal system, including injuries, sprains and dislocations of the joints; tendonitis, bursitis; toothache) .; Symptomatic treatment of osteoarthritis with pain syndrome.; Algodismenorrhea.; The drug is intended for symptomatic therapy, reducing pain and inflammation; does not affect the progression of the disease.

Contraindications

Hypersensitivity to nimesulide or any auxiliary component of the drug .; Sucrase / isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption (Nimesulide Canon contains sucrose).; Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including a history) .; Erosive and ulcerative changes in the mucous membrane of the stomach and duodenum, active gastrointestinal bleeding, cerebrovascular or other bleeding .; Inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase .; Hemophilia and other bleeding disorders .; Decompensated heart failure .; Liver failure or any active liver disease.; Anamnestic data on the development of hepatotoxic reactions when using nimesulide preparations .; Alcoholism, drug addiction.; Severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia .; The period after coronary artery bypass grafting.; Simultaneous use of other hepatotoxic drugs .; Pregnancy and lactation.; Children's age up to 12 years.;

Use during pregnancy and lactation

The use of the drug Nimesulide Canon during pregnancy and during breastfeeding is contraindicated. If necessary, the use of the drug during breastfeeding, breastfeeding should be discontinued .; The use of nimesulide can adversely affect female fertility and is not recommended for women planning a pregnancy. When planning pregnancy, consultation with your doctor is necessary.

Dosage and administration

The drug Nimesulide Canon is taken orally, 1 sachet (100 mg nimesulide) twice a day. The drug Nimesulide Canon is recommended to be taken after meals. The contents of the sachet are poured into a glass and dissolved in about 100 ml of water (a suspension from white to light yellow is formed). The prepared solution is not subject to storage.; The drug Nimesulide Canon is used only for the treatment of patients older than 12 years.; Adolescents (from 12 to 18 years): based on the pharmacokinetic profile and 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 to adjust the dose in patients with mild to moderate renal insufficiency (creatinine clearance; 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, the minimum effective dose should be used for the shortest possible course.

Side effects

WHO classification of the incidence of side effects: very often - ≥1 / 10 appointments (more than 10%); often - from ≥1 / 100 to less than 1/10 appointments (more than 1% and less than 10%); infrequently - from ≥1 / 1000 to less than 1 / 100 appointments (more than 0.1% and less than 1%); rarely - from ≥1/10000 to less than 1/1000 appointments (more than 0.01% and less than 0.1%); very rarely - less than 1/10,000 appointments (less than 0.01%); the frequency is unknown - according to the available data, it is not possible to establish the frequency of occurrence .; Blood and lymphatic system disorders: Rarely - anemia, eosinophilia, hemorrhages; very rarely - thrombocytopenia, agranulocytosis, pancytopenia, thrombocytopenic purpura .; Allergic reactions: Rarely - hypersensitivity reactions; very rarely - anaphylactoid reactions .; Skin and subcutaneous tissue disorders: Infrequently - itching, rash, increased sweating; rarely - erythema, dermatitis; very rarely - urticaria, angioedema, swelling of the face, erythema multiforme exudative, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome) .; From the side of the central nervous system: infrequently - dizziness; rarely - a feeling of fear, nervousness, "nightmare" dreams; very rarely - headache, drowsiness, encephalopathy (Reye's syndrome) .; Sensory disorders: Rarely - blurred vision .; Cardiovascular disorders: Infrequently - increased blood pressure; rarely - tachycardia, lability of blood pressure, "hot flashes", a feeling of palpitations .; Respiratory system disorders: Infrequently - shortness of breath; very rarely - exacerbation of bronchial asthma, bronchospasm .; Gastrointestinal disorders: Often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, dyspepsia, stomatitis, tarry stools, gastrointestinal bleeding, ulceration of the mucous membrane and / or perforation of the stomach or duodenum .; Liver and biliary tract disorders: Often - increased "liver" transaminases; very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis .; Renal and urinary disorders: Rarely - dysuria, hematuria, urinary retention, hyperkalemia; very rarely - renal failure, oliguria, interstitial nephritis .; General disorders: Infrequently - edema; rarely - malaise, asthenia; very rarely - hypothermia.

Overdose

Symptoms: nausea, vomiting, drowsiness, apathy, gastrointestinal bleeding, increased blood pressure, acute renal failure, respiratory depression; ;Treatment: symptomatic and supportive treatment is recommended. There is no specific antidote for Nimesulide. Patients admitted to the hospital with symptoms of an overdose of the drug (within 4 hours after taking it or after taking a high dose) are recommended gastric lavage, activated charcoal (adults - 60-100 mg) and / or osmotic laxatives. Regular monitoring of liver and kidney function is necessary. There are no data on the possibility of removing nimesulide by hemodialysis. Formed diuresis, hemodialysis are ineffective due to the high connection of the drug with proteins .;

Interaction with other drugs

Glucocorticosteroids: increase the risk of gastrointestinal ulcers or bleeding .; Antiplatelet agents and selective serotonin reuptake inhibitors: increase the risk of gastrointestinal bleeding .; Anticoagulants: NSAIDs may increase the effect 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 still cannot be avoided, it is necessary to carefully monitor blood clotting parameters .; Diuretics: NSAIDs may reduce the effect of diuretics. In healthy volunteers, nimesulide temporarily reduces sodium excretion under the action of furosemide, to a lesser extent, potassium excretion, and reduces the actual diuretic effect. 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 nimesulide requires caution in patients with impaired renal or cardiac function .; ACE inhibitors and angiotensin-II receptor antagonists: NSAIDs may reduce the effect of antihypertensive drugs. In patients with mild to moderate renal insufficiency (creatinine clearance 30-80 ml / min), with the joint appointment of ACE inhibitors, angiotensin II receptor antagonists or substances that suppress the cyclooxygenase system (NSAIDs, antiplatelet agents), further deterioration of renal function and the occurrence of acute renal failure, which is usually reversible. These interactions should be considered in patients taking nimesulide Canon in combination with ACE inhibitors or angiotensin II receptor antagonists. Therefore, the combined use of these drugs should be prescribed with caution, especially for elderly patients. Patients should receive sufficient fluids, and renal function should be carefully monitored after the start of joint therapy .; There is evidence that NSAIDs reduce the clearance of lithium, which leads to an increase in the concentration of lithium in the blood plasma and its toxicity. When prescribing nimesulide to patients receiving lithium therapy, regular monitoring of plasma lithium concentrations should be carried out .; Clinically significant interactions with glibenclamide, theophylline, digoxin, cimetidine and antacids (for example, a combination of aluminum and magnesium hydroxides) were not observed. ; Nimesulide inhibits the activity of the CYP2C9 isoenzyme. While taking drugs metabolized with the participation of this isoenzyme with nimesulide, the concentration of these drugs in plasma may increase .; With simultaneous use with antiepileptic drugs (valproic acid), antifungal drugs (ketoconazole), anti-tuberculosis drugs (isoniazid), amiodarone, methotrexate, methyldopa, amoxicillin in combination with clavulanic acid, an additive hepatotoxic effect is possible .; Due to the high degree of binding of nimesulide to plasma proteins, patients taking sulfonamides at the same time should be under the supervision of a physician, undergoing examination at short intervals .; When prescribing nimesulide less than 24 hours before or after taking methotrexate, caution is required, since in such cases the plasma concentration of methotrexate and, accordingly, the toxic effects of this drug may increase. In connection with the action on renal prostaglandins, prostaglandin synthetase inhibitors, which include nimesulide, can increase the nephrotoxicity of cyclosporins .; In vitro studies have shown that nimesulide is displaced from the binding sites by tolbutamide, salicylic acid. Despite the fact that these interactions were determined in blood plasma, these effects were not observed during the clinical use of the drug.

special instructions

To reduce the risk of side effects, it is necessary to use the drug in the minimum effective dose with the shortest duration. If the patient's condition does not improve, treatment should be discontinued.; It is necessary to stop taking the drug in case of fever or development of flu-like symptoms while taking it.; If symptoms appear in patients taking Nimesulide that indicate liver damage (eg, anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine), or an increase in the level of hepatic transaminases, the drug should be discontinued. Such patients are not recommended to prescribe Nimesulide in the future.; Gastrointestinal bleeding or ulcer / perforation of the stomach or duodenum may develop at any time during the use of the drug, which may not be accompanied by clinically significant symptoms (including pain syndrome). If gastrointestinal bleeding or ulcers occur, the drug should be discontinued .; In case of deterioration of kidney function, the drug should be discontinued .; In the case of using the drug for more than 2 weeks, monitoring of liver function indicators is necessary .; In patients with cirrhosis of the liver or with renal insufficiency with hypoalbuminemia or hyperbilirubinemia, the binding of nimesulide is reduced .; Elderly patients most often develop side effects when taking the drug, including gastrointestinal bleeding, perforation, dysfunction of the heart, kidneys and liver. Therefore, regular clinical monitoring of the patient's condition is recommended .; The use of nimesulide can adversely affect female fertility and is not recommended for women planning pregnancy .; Influence on the ability to drive vehicles and control mechanisms; If, when using the drug, adverse effects occur on the part of the central nervous system and sensory organs, it is necessary to refrain from driving vehicles and engaging in activities that require increased concentration of attention and speed of psychomotor reactions .;

The composition of the medicinal product

active substance: 1 g of powder contains 50 mg of nimesulide;

Excipients: xanthan gum, colloidal silicon dioxide, calcium stearate, citric acid, aspartame (E 951), lemon oil, sucrose.

Dosage form

Powder for oral suspension.

Pharmacological group

Non-steroidal anti-inflammatory drugs.

ATC code M01A X17.

Indications

Sharp pain. Symptomatic treatment of osteoarthritis with pain syndrome. primary dysmenorrhea.

Contraindications

Hypersensitivity to Nimesulide or other components of the drug, as well as hypersensitivity reactions to other NSAIDs in history
severe liver dysfunction (liver failure) and hepatotoxic reactions to the drug in history, simultaneous use with potentially hepatotoxic drugs;
peptic ulcer of the stomach and duodenum in the acute stage;
severe renal dysfunction (creatinine clearance less than 30 ml/min);
severe blood clotting disorders;
severe heart failure
pregnancy (III trimester) and breastfeeding period
age up to 12 years;
alcoholism,
drug addiction;
elevated body temperature
flu-like conditions;
suspicion of acute surgical pathology.

Dosage and administration

With Nimesulide, which is in the form of a powder, it is necessary to prepare a ready-to-use suspension before using the drug. To do this, the contents of the package are dissolved in 100 ml of freshly boiled and cooled to room temperature drinking water and shaken thoroughly. After that, the suspension is ready for use.

The suspension is taken orally after a meal.

Adults the drug is prescribed in a single dose of 100 mg (1 sachet of powder). The maximum daily dose is 200 mg (2 sachets).

For patients aged 12 to 18 years and elderly patients, the specified dosing regimen does not need correction.

In order to prevent the occurrence and to reduce the manifestation of adverse reactions, the drug must be taken for a short time and in the minimum effective dose. The drug should be prescribed only after a thorough assessment of the risk/benefit ratio. With mild and moderate forms of renal failure (creatinine clearance 30-80 ml / min), the dose does not need to be adjusted. In severe renal failure (creatinine clearance less than 30 ml / min), the use of the drug is not indicated.

The maximum duration of Nimesulide use should not exceed 15 days.

Adverse reactions

Frequency of manifestations very often - in more than one patient out of 10;

often - in more than one patient out of 100;

infrequently - in more than one patient in 1000;

rarely - in more than one patient in 10,000;

single - in more than one patient out of 100,000.

When using the drug, the following adverse reactions may occur, mainly during the first week of treatment:

from the cardiovascular system: infrequently - arterial hypertension; rarely - bleeding, hot flashes, fluctuations in blood pressure, tachycardia

From the blood system: rarely - anemia, eosinophilia, bleeding, isolated cases of pancytopenia, purpura and thrombocytopenia;

from the skin side: infrequently - there are rashes, itching, increased sweating, erythema, dermatitis single - angioedema, swelling of the face, erythema multiforme, urticaria, Stevens-Johnson syndrome and toxic epidermal necrolysis

from the digestive tract: often - diarrhea, nausea, vomiting; not often - constipation, flatulence, gastritis; single - abdominal pain, stomatitis, melena, gastric or duodenal ulcer, ulcer perforation or gastrointestinal bleeding;

from the side of the kidneys: rarely - dysuria, edema, hematuria, urinary retention; single - oliguria, interstitial nephritis and renal failure

from the liver: rarely - jaundice, cholestasis, increased levels of hepatic transaminases; sometimes there are cases of acute hepatitis, even fatal;

from the respiratory organs: infrequently - shortness of breath; single - asthma, bronchospasm, especially in patients with hypersensitivity to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs;

from the immune system: hypersensitivity reactions, anaphylaxis;

from the nervous systems: infrequently - dizziness; rarely - anxiety, nervousness, sleep disturbance, single - drowsiness, headache, encephalopathy (Reye's syndrome), nightmares;

other: and also while taking the drug, visual disturbances are possible. Asthenia, vertio, hypothermia, hyperkalemia.

Overdose

Symptoms. In case of overdose, lethargy, lethargy, drowsiness, nausea, vomiting, pain in the epigastric region are observed, gastrointestinal bleeding, arterial hypertension, acute renal failure, respiratory depression, anaphylactoid reactions and coma may also occur.

Treatment. There is no specific antidote. In case of overdose, symptomatic therapy should be carried out. Patients should be given gastric lavage for the first 4 hours and given activated charcoal (60-100 g for adults), an emetic, or an osmotic laxative. Hemodialysis is not effective. Careful monitoring of renal function is necessary.

Use during pregnancy or lactation

pregnancy

The use of Nimesulide is contraindicated in the last trimester of pregnancy. The use of Nimesulide can interfere with female fertility and is not recommended for women planning a pregnancy. Like other NSAIDs that inhibit prostaglandin synthesis, Nimesulide can cause premature closure of the ductus arteriosus, pulmonary hypertension, oliguria, and oligohydramnios. Risk of bleeding, uterine atony and peripheral edema. Considering also the lack of data on the use of the drug for pregnant women, it is not recommended to prescribe Nimesulide in the I and II trimesters of pregnancy.

lactation

Since it is not known whether Nimesulide passes into breast milk, the use of this drug is contraindicated during lactation.

Children

The drug is contraindicated in children under 12 years of age. Dosage for children over 12 years of age is the same as for adults.

Application features

To reduce the risk of adverse reactions, it is necessary to use the minimum effective dose with the shortest duration of treatment. If the patient's condition does not improve, treatment should be discontinued.

In the event of an increase in liver enzymes or signs of liver damage (eg anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine), the drug should be discontinued. Such patients are prohibited from prescribing Nimesulide in the future. Most cases of liver damage are reversed when Nimesulide is used for a short period.

Gastrointestinal bleeding or ulcer/perforation may develop at any time during the use of the drug, with or without warning symptoms, with or without a history of gastrointestinal complications. If gastrointestinal bleeding or ulcers occur, the drug should be discontinued.

With caution, Nimesulide should be prescribed to patients with gastrointestinal disorders, ulcerative colitis or Crohn's disease in history.

With caution, the drug should be prescribed to patients with renal or heart failure, since its use can lead to deterioration in renal function. In case of deterioration of kidney function, the drug should be discontinued.

Elderly patients are especially sensitive to non-steroidal anti-inflammatory drugs (NSAIDs). They most often develop adverse reactions due to taking the drug, including gastrointestinal bleeding, perforation, dysfunction of the heart, kidneys and liver. Therefore, regular clinical monitoring of the patient's condition is recommended.

Since Nimesulide can disrupt platelet function in patients with hemorrhagic diathesis, the drug should be used with caution, under constant medical supervision. The use of NSAIDs may mask an increase in body temperature associated with an underlying bacterial infection. In the event of an increase in body temperature or the appearance of flu-like symptoms, it is necessary to stop taking the drug.

The composition of the drug includes sugar, which must be borne in mind when treating patients with diabetes mellitus.

The ability to influence the reaction rate when driving vehicles or operating other mechanisms

During treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Interaction with other medicinal products and other forms of interaction

With simultaneous use with warfarin and similar anticoagulants, acetylsalicylic acid, there is an increased risk of bleeding.

Simultaneous use of Nimesulide with diuretics may adversely affect renal hemodynamics. The usual concentrations of unsaturated fatty acids do not affect the relationship of Nimesulide with albumin. In patients with reduced synthetic liver function or severe renal insufficiency, the communication of Nimesulide with plasma proteins (as well as other NSAIDs) is significantly reduced, leading to a vinification of the free fraction of the drug, which can subside the frequency and severity.

The simultaneous use of Nimesulide and furosemide requires caution in the treatment of patients with impaired renal and cardiac function.

Non-steroidal anti-inflammatory drugs reduce the clearance of lithium, which leads to an increase in the concentration of lithium in plasma and an increase in its toxicity. Therefore, with the simultaneous use of Nimesulide and lithium, it is necessary to carefully monitor the concentration of lithium in the plasma.

With the simultaneous use of Nimesulide with digoxin, theophylline, glibenclamide, ranitidine, antacids, no clinically significant interaction was noted.