Nimesulide

Nimesulide is a non-steroidal anti-inflammatory drug that belongs to sulfonanilides, has an anti-inflammatory, analgesic and antipyretic effect.

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

The drug helps to get rid of the pain that occurs after surgical interventions or traumatic injuries. Nimesulide is often prescribed to patients suffering from rheumatism, arthralgia, algodismenosis and a number of other pathologies, which are accompanied by strong pain sensations of different locations.

Clinical and pharmacological group

NSAIDs. Selective inhibitor of COX-2.

Conditions of leave from pharmacies

Released without a doctor's prescription.

Price list

How much does Nimesulide cost in pharmacies? The average price is at the level of50 rubles.

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Form of issue and composition

Nimesulide is available in the following forms:

Tablets (10 pcs. Each) in the blister; , or 3 blisters in the package);
Suspension for oral administration (60 ml per vial);
Gel 0.1%: homogeneous, transparent or almost transparent, yellow (30 g in a tube, 1 tube in a cardboard bundle);
Powder for the preparation of a suspension: from white to white with a yellowish hue of color, dissolving forms a suspension white or light yellow color with a characteristic lemon scent (2 g in a bag, 9 or 30 packs in a package).

Active ingredient: nimesulide (100 mg in 1 tablet, 50 mg in 1 g of powder, 10 mg in 1 ml of suspension, 10 mg in 1 g of gel).

Auxiliary components:

Tablets: lactose monohydrate, microcrystalline cellulose, magnesium stearate, croscarmellose sodium, calcium hydrophosphate dihydrate, sodium lauryl sulfate, talc, hydroxypropylcellulose, aerosil;
Gel: Macrogol 400, Carbomer, Dimexide, Propylene Glycol, Ethyl Alcohol.

Pharmacological effect

Imesulide has a pronounced anti-inflammatory, and also, moderate analgesic and weak antipyretic effect. The drug is a selective inhibitor of cyclooxygenase-2.

Thus, the mechanism of the anti-inflammatory effect of the drug is based on inhibiting the synthesis of prostaglandins: the active substance of the drug inhibits predominantly cyclooxygenase-2, due to which the synthesis of prostaglandins is suppressed mainly in the area of inflammation and, to a lesser extent, in the kidneys and mucous membrane of the stomach.

The maximum concentration of the drug in the blood plasma is reached one to two hours after ingestion of a suspension or tablets of Nimesulide. From the body, the drug is almost completely removed within 24 hours. With prolonged use of Nimesulide, cumulation (accumulation) of the drug is not observed.

Indications for use

A non-steroidal anti-inflammatory drug is a great way to quickly get rid of pain, swelling within the body. It is important to understand that a medicine with nimesulide will relieve you of the symptoms of the disease, but it will not eliminate the ailment itself. According to the instructions for use, the substance has three main areas of work:

anti-inflammatory effect;
elimination of heat;
anesthesia.

The medicine received a large number of positive reviews and is actively used in medicine. If you do not know what helps nimesulid, check out this list:

osteochondrosis;
inflammation of the tendons;
rheumatism;
problems of the musculoskeletal system;
pain in the muscles.

Contraindications

According to the instructions to Nimesulid, it can not be taken in such cases:

Pregnancy;
Lactation;
Children up to 12 years;
Bleeding, including cerebrovascular;
Active gastrointestinal bleeding;
Confirmed hyperkalemia;
Severe chronic renal failure (creatinine clearance <30 mL / minute);
Alcoholism or drug addiction;
Simultaneous administration of other hepatotoxic drugs;
Hepatotoxic reactions with nimesulide in history;
Erosive-ulcerative lesions of the mucous membrane of the stomach and duodenum;
Exacerbation of inflammatory bowel disease (Crohn's disease or ulcerative colitis);
Decompensated chronic heart failure;
Period after aortocoronary bypass surgery;
Any active or progressive liver disease, liver failure;
Blood clotting disorders, incl. hemophilia;
Hypersensitivity to the drug;
Complete or incomplete combination of bronchial asthma and recurrent polyposis of the nose / paranasal sinuses with intolerance to acetylsalicylic acid or other NSAIDs (in history including).

Relative contraindications:

Dyslipidemia and hyperlipidemia;
Creatinine clearance <30-60 ml / minute;
Smoking;
Presence of Helicobacter pylori infection;
Ulcerative lesions of the gastrointestinal tract in the anamnesis;
Chronic heart failure;
Cerebrovascular diseases;
Cardiac ischemia;
Diseases of peripheral arteries;
Diabetes;
Severe somatic diseases;
Elderly age;

Simultaneous use of the following drugs: anticoagulants (including warfarin), antiaggregants (including acetylsalicylic acid and clopidogrel), oral glucocorticosteroids, selective serotonin reuptake inhibitors (including paroxetine, citalopram, sertraline, fluoxetine).

Use in pregnancy and lactation

Nimesulide should not be taken during pregnancy. The greatest danger is its use in the third trimester of pregnancy due to possible atony of the uterus in a woman and premature closure of the ductal duct in the child.

During the lactation period, the drug can be prescribed only if, during the period of treatment, breastfeeding is discontinued.

Dosage and route of administration

The instructions for use indicate that Nimesulide is taken internally.

The frequency of administration of nimesulide preparations, the duration of the course of treatment, and also the dosages are determined by the severity of the symptoms pathology, general condition of a person, concomitant diseases, age and form of release of a medicinal product.

Powder

The contents of 1 packet of granules are dissolved in 80-100 ml of water. The recommended dose for adults and adolescents aged 12-18 years is 100 mg (1 sachet) 2 times / day after meals. The maximum daily dose for adults and adolescents aged 12-18 years is 200 mg.

No dose reduction is required for elderly patients.

Patients with chronic renal failure require a reduction in the daily dose to 100 mg.

The minimum effective dose should be given for as short a period of time as possible in order to minimize the risk of adverse reactions. The maximum duration of the drug should not exceed 15 days.

Pills

Tablets Nimesulid intended for admission to adults and adolescents over 12 years. It is desirable to take them after meals, wholly, without chewing and washing down with a sufficient amount of water.

The average recommended therapeutic dosage is 1 tablet 2 times a day. The maximum daily dosage should not exceed 200 mg.

The recommended duration of therapy should not exceed 10 days. If necessary, the dosage and duration of taking Nimesulide tablets is determined individually by the attending physician.

Suspension

In 1 ml of suspension or syrup Nimesulide contains 10 mg of active substance. Based on this, the dosage is calculated. Suspension or syrup is intended for use in children under 12 years of age.

Dosages for children are calculated by body weight: 1.5-3 mg per 1 kg of body weight. This means that a child weighing 10 kg should take nimesulide at a dose of 1.5 * 10 = 15 mg per day, which corresponds to 1.5 ml of syrup or suspension. This amount is divided into 2 - 3 doses per day. To set the appropriate amount of suspension in the package with the drug is enclosed a special measuring syringe. The maximum allowable syrup dosing of Nimesulide syrup for children corresponds to 5 mg per 1 kg. If the weight of the child exceeds 40 kg, then the calculation of the dose is not used, but is applied 100 mg twice a day, as in adults.

A continuous course of application of nimesulide in the form of a syrup or suspension is a maximum of 15 days. It is better to take the drug for a shorter period, stopping use immediately after eliminating symptoms and normalizing the condition.

Side effects

During the application of Nimesulide, there may be abnormalities on the part of certain body systems that manifest themselves at different frequencies (≥1 / 10 - very often; > 1/100, <1/10 - often; > 1/1000, <1/100 - infrequently; > 1/10 000, <1/1000 - rarely; <1/10 000, including individual messages - very rarely):

Cardiovascular system: infrequently - hypertension; rarely - palpitation, tachycardia;
Allergic reactions: infrequent - skin rash and itching; rarely - exanthema, erythema; very rarely - severe skin conditions, including toxic epidermal necrolysis (Lyell's syndrome), Stevens-Johnson syndrome, anaphylactic shock, bronchospasm;
Gastrointestinal tract: often - heartburn, vomiting, nausea, diarrhea; infrequently - bloating, constipation, gastritis; very rarely - ulceration of the mucous membrane of the gastrointestinal tract, stomach pain, melena, tarry stool, increased activity of hepatic transaminases, toxic hepatitis (including fatal);
Nervous system: infrequently - dizziness; rarely - irritability, sleep disorder, anxiety; very rarely - encephalopathy, headache, Rhine syndrome, drowsiness;
Blood and lymphatic system: rarely - eosinophilia, anemia, prolonged bleeding time; very rarely - agranulocytosis, thrombocytopenia, purpura, pancytopenia;
Kidneys and urinary tract: rarely - hematuria, dysuria, fluid retention; very rarely - renal failure, oliguria, interstitial nephritis;
Other: infrequently - swelling; rarely - hyperkalemia, asthenia, vertigo, visual impairment, malaise; very rarely - hypothermia.

With the development of any of the described side effects, as well as in cases of other disorders, it is necessary to consult a doctor.

Overdose

Overdose can include nausea and vomiting, epigastric pain and gastrointestinal bleeding, drowsiness and lethargy, arterial hypertension and acute renal failure, respiratory depression and anaphylactic reactions up to shock and coma.

There is no specific antidote. In case of an overdose of Nimesulide, the victims are prescribed only symptomatic treatment: gastric lavage and taking activated charcoal or other adsorbents during the first four hours. Hemodialysis is not performed because it is not effective.

special instructions

Before you start using the drug, read the special instructions:

If the kidney function worsens, the drug should be discarded.
It is necessary to stop taking the drug in case of fever or development on the background of its intake of influenza-like symptoms.
In the case of using the drug for more than 2 weeks, monitoring of liver function parameters is necessary.
To reduce the risk of side effects, it is necessary to apply the drug at the lowest effective dose with the shortest duration. If the patient's condition does not improve, treatment should be stopped.
Gastrointestinal bleeding or ulcer / perforation of the stomach or duodenum may develop at any time when using the drug, which may not be accompanied by clinically expressed symptoms (including pain syndrome). If there is a gastrointestinal bleeding or ulcers, the drug should be discarded.
In patients with cirrhosis of the liver or with renal insufficiency with hypoalbuminemia or hyperbilirubinemia, the binding of nimesulide is reduced.
When symptoms appear in patients taking Nimesulide that indicate liver damage (eg, anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine), or elevated liver transaminases, the drug should be discontinued. It is not recommended for such patients to appoint Nimesulide in the future.
In elderly patients, the most common side effects when taking the drug, including gastrointestinal bleeding, perforation, impaired heart, kidney and liver function. Therefore, regular clinical monitoring of the patient's condition is recommended.
The use of nimesulide may adversely affect female fertility and is not recommended for women planning a pregnancy.

Drug Interactions

When using the drug, it is necessary to take into account the interaction with other drugs:

Nimelide can replace salicylic acid and furosemide (but not warfarin) in plasma proteins.
There is evidence that nimesulide may reduce the bioavailability of furosemide, compete with plasma fusion with fenofibrate, salicylic acid, tolbutamide.
It is not recommended to take nimesulide concomitantly with diuretics, which have a damaging effect on renal hemodynamics.
The physiological concentrations of unsaturated fatty acids do not affect the binding of nimesulide to serum albumin.
Taking nimesulide in therapeutic doses orally for a short period does not change the serum digoxin profile in patients with mild heart failure.
In therapeutic concentrations, the binding of nimesulide was not affected by warfarin, furosemide, glibenclamide, digitoxin.
In the presence of nimesulide, free fractions of methotrexate can increase significantly.
The concentration of lithium in plasma increases with simultaneous intake of lithium and nimesulide preparations. Nimesulide can enhance the action of cyclosporin on the kidneys.
It has no effect on drugs affecting blood glucose concentration and glucose tolerance in patients with diabetes mellitus, treated with various drugs containing sulfonylureas.
Use with SCS, serotonin reuptake inhibitors increases the risk of developing gastrointestinal bleeding.

Reviews

We picked up some reviews of people who used the drug Nimesulide:

Katerina. Nimesulide is an anesthetic and anti-inflammatory drug to help, it needs to be taken more than once, and for some time-if radiculitis (I have three hernias) - after 2-3 days of nimesulide treatment, the effect comes, a toothache - depending on what severity: after tooth extraction and Implantation to me nimesulid helped to partially relieve the pain immediately after the operation and completely removed the pain a week after the operation. Headache - someone like, and looking at what kind of pain (spasm of muscle-tension headache-will help in an hour and a half, if the headache is caused by something else, it can not help, another drug is needed). Therefore, it is important to know what you are treating, and what particular drug it is treating, and everything will be cured in the end. Also do not write, that does not help - still as helps!
Olga. Excellent medicine "from everything." I think that it should be in the first aid kit. We use it with the whole family for a couple of years. Perfectly suitable for pain or fever. When I'm sick, I dissolve 1 packet of powder in a half-glass of water, drink at night, sweat properly under a warm blanket, and the morning the temperature drops, and the headache goes away. I also use Nimesulide for headaches. I take in tablets or in a powdery state. One of the big advantages is that this drug is universal and is inexpensive, so it can be used for different symptoms.
Nastya. I used to buy Naise, but then I chose the domestic analogue - nimesulide. It also helps very well, but costs 3 times cheaper. Great after surgery. Sutures do not hurt at all. All night you can sleep peacefully. It's a pity that the drug has many contraindications, so you need to follow instructions for use clearly.