Nimesulide is a non-steroidal anti-inflammatory drug, which belongs to the sulfonanilide, has anti-inflammatory, analgesic and antipyretic effect.
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).
The drug helps to get rid of pain arising after surgical interventions or traumatic injuries. Nimesulide is often prescribed to patients suffering from rheumatism, arthralgia, algomenorrhea and a number of other pathologies, which are accompanied by strong pain sensations of various locations.
Clinical and pharmacological group
NSAIDs. Selective inhibitor of TsOG-2.
Pharmacy sales terms
It is released without a prescription.
How much does Nimesulide in pharmacies? The average price is at 50 rubles.
Release form and composition
Nimesulide is available in the following forms:
- Tablets (10 pieces in a blister; 1,2 or 3 blisters per pack);
- Suspension for oral administration (60 ml vial);
- Gel 0.1%: homogeneous, transparent or almost transparent, yellow (30 g in a tube, 1 tube in a carton box);
- Powder for the preparation of suspensions: from white to white with a yellowish tinge, when dissolved forms a suspension of white or light yellow color with a characteristic lemon smell (2 g per bag; 9 or 30 bags per pack).
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).
- Tablets: lactose monohydrate, microcrystalline cellulose, magnesium stearate, sodium croscarmellose, calcium hydrogen phosphate dihydrate, sodium lauryl sulfate, talc, hydroxypropylcellulose, aerosil;
- Gel: macrogol 400, carbomer, dimexide, propylene glycol, ethyl alcohol.
imesulide has a pronounced anti-inflammatory, as well as moderate analgesic and mild antipyretic effect. The drug is a selective inhibitor of cyclooxygenase-2.
Thus, the mechanism of the anti-inflammatory action of the drug is based on the inhibition of prostaglandin synthesis: the active substance of the drug inhibits mainly cyclooxygenase-2, due to which prostaglandin synthesis is inhibited mainly in the area of inflammation and to a lesser extent in the kidneys and gastric mucosa.
The maximum concentration of the drug in the blood plasma is achieved one to two hours after ingestion of a suspension or tablets of Nimesulide. From the body the drug is almost completely excreted within 24 hours. With long-term use of Nimesulide accumulation (accumulation) of the drug is not observed.
Indications for use
Nonsteroid drug against inflammation is a great way to quickly get rid of pain, swelling inside the body. It is important to understand that the medicine with nimesulide will relieve you from 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;
The drug has received a large number of positive reviews and is actively used in medicine. If you do not know what helps nimesulide from, read this list:
- tendon inflammation;
- problems of the musculoskeletal system;
- muscle pain.
According to the instructions to Nimesulid, it should not be taken in such cases:
- Children's age 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;
- The simultaneous appointment of other hepatotoxic drugs;
- Hepatotoxic reactions in the application of nimesulide in history;
- Erosive and ulcerative lesions of the gastric mucosa and duodenum;
- Exacerbation of inflammatory bowel disease (Crohn's disease or ulcerative colitis);
- Decompensated chronic heart failure;
- The period after coronary artery bypass surgery;
- Any active or progressive liver disease, liver failure;
- Blood coagulation disorders, incl. hemophilia;
- Hypersensitivity to the drug;
- A complete or incomplete combination of bronchial asthma and recurrent nasal polyposis / paranasal sinuses with intolerance to acetylsalicylic acid or other NSAIDs (including a history of).
- Dyslipidemia and hyperlipidemia;
- Creatinine clearance <30-60 ml / minute;
- The presence of Helicobacter pylori infection;
- Ulcer lesion of the gastrointestinal tract in history;
- Chronic heart failure;
- Cerebrovascular diseases;
- Coronary heart disease;
- Peripheral artery diseases;
- Severe somatic diseases;
- Elderly age;
The simultaneous use of the following drugs: anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid and clopidogrel), oral glucocorticosteroids, selective serotonin reuptake inhibitors (including paroxetine, citalopram, sertralin, fluoxetine).
Use during pregnancy and lactation
Nimesulide should not be taken during pregnancy. Its use is most dangerous in the third trimester of pregnancy due to the possible atony of the uterus in a woman and the premature closure of the batal's duct in a child.
During the lactation period, the drug can be prescribed only if the breastfeeding is discontinued for the period of treatment.
Dosage and method of use
The instructions for use indicate that Nimesulide is taken orally.
The frequency of nimesulide medication, the duration of the course of treatment, and the dosage are determined by the severity of the symptoms of the pathology, the general condition of the person, concomitant diseases, age and the form of release of the drug.
- The contents of 1 sachet of granulate is 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.
Dose reduction is not 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 administered for as short a period as possible in order to minimize the risk of adverse reactions. The maximum duration of the drug should not exceed 15 days.
Nimesulide tablets are intended for ingestion in adults and adolescents over 12 years of age. It is advisable to take them after a meal, whole, without chewing and drinking plenty 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 the course of therapy should not exceed 10 days. If necessary, the dosage and duration of administration of Nimesulide tablets is determined by the attending physician individually.
1 ml of suspension or syrup Nimesulide contains 10 mg of the active substance. Based on this, and calculate the dosage. 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 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. For a set of the corresponding amount of suspension the special measured syringe is enclosed in packaging with a preparation. The maximum allowable waste dosage of Nimesulide Syrup for children is 5 mg per 1 kg. If the weight of the child exceeds 40 kg, then the dose calculation is not used, but used 100 mg 2 times a day, as in adults.
A continuous course of use of nimesulide in the form of a syrup or suspension is a maximum of 15 days. It is better to take the drug less time, stopping use immediately after the elimination of symptoms and the normalization of the state.
During the use of Nimesulide, disturbances are observed on the part of some body systems that manifest themselves with different frequencies (≥1 / 10 - very often;> 1/100, 1/1000, 1/10 000, <1/1000 - rarely; <1 / 10,000, including individual messages - very rarely):
- Cardiovascular system: infrequently - hypertension; rarely - palpitations, tachycardia;
- Allergic reactions: rarely - skin rash and itching; rarely - rash, erythema; very rarely - severe skin events, including toxic epidermal necrolysis (Lyell's syndrome), Stevens-Johnson syndrome, anaphylactic shock, bronchospasm;
- Gastrointestinal tract: often - heartburn, vomiting, nausea, diarrhea; infrequently - abdominal distension, constipation, gastritis; very rarely - ulceration of the gastrointestinal mucosa, stomach pain, melena, tarry stools, increased activity of hepatic transaminases, toxic hepatitis (including fatal outcome);
- Nervous system: infrequently - dizziness; rarely - irritability, sleep disturbance, anxiety; very rarely - encephalopathy, headache, Reine 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: Infrequent - 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 violations, it is necessary to consult a doctor.
Overdose can cause 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 overdose of Nimesulide, victims are prescribed exclusively symptomatic treatment: gastric lavage and taking activated carbon or other adsorbents for the first four hours. Hemodialysis is not performed because it is not effective.
Before you start using the drug, read the specific instructions:
- In case of deterioration in renal function, the drug should be discontinued.
- It is necessary to stop taking the drug in case of fever or the development of flu-like symptoms on the background of his reception.
- If the drug is used for more than 2 weeks, monitoring of liver function indicators is necessary.
- To reduce the risk of side effects, it is necessary to use the drug in the lowest effective dose with the shortest duration. If the patient’s condition does not improve, treatment should be stopped.
- Gastrointestinal bleeding or an ulcer / perforation of the stomach or duodenum may develop at any time with the use of the drug, which may not be accompanied by clinically pronounced symptoms (including pain syndrome). If gastrointestinal bleeding or ulceration occurs, the drug should be withdrawn.
- In patients with cirrhosis of the liver or with renal insufficiency with hypoalbuminemia or hyperbilirubinemia, the binding of nimesulide is reduced.
- When patients taking Nimesulide, symptoms that indicate liver damage (for example, anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine), or increased liver transaminases, should be discontinued. It is not recommended to appoint Nimesulide in such patients in the future.
- Elderly patients most often develop side effects when taking the drug, including gastrointestinal bleeding, perforation, impaired function of the heart, kidneys and liver. 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.
When using the drug, you must consider 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, to compete in the binding of plasma proteins with fenofibrate, salicylic acid, tolbutamide.
- It is not recommended to take nimesulide simultaneously with diuretics, which have a damaging effect on renal hemodynamics.
- 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 profile of digoxin in patients with mild heart failure.
- At therapeutic concentrations, the binding of nimesulide was not affected by warfarin, furosemide, glibenclamide, digitoxin.
- In the presence of nimesulide, the free fractions of methotrexate can significantly increase.
- The concentration of lithium in the plasma increases while taking drugs of lithium and nimesulide. Nimesulide may enhance the effect of cyclosporine on the kidneys.
- It has no effect on drugs that affect blood glucose concentration and glucose tolerance in diabetic patients treated with various drugs containing sulfonylureas.
- Use with GCS, serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.
We picked up some reviews of people using the drug Nimesulide:
- Katerina. Nimesulide is an anesthetic and anti-inflammatory drug, so that it helps, you need to take it not once, but for some time — if sciatica (I have three hernias) - after 2-3 days of nimesulide, the effect comes, toothache - depending on what of severity: after the removal of the tooth and implantation, I was able to partially relieve pain immediately after surgery and completely relieve pain a week after surgery. A headache - to whom how, and despite what kind of pain (muscle spasm — tension headache — will help in an hour and a half, if the headache is caused by something else, it may not help, you need another drug). Therefore, it is important to know what you are treating, and what specific drug it heals, and everything will be cured in the end. And do not write that does not help - even as it helps!
- Olga Excellent medicine "from everything". I think that should be in the first aid kit. We use it with the whole family for a couple of years. Perfect for pain or at temperature. When I'm sick, I dissolve 1 pack of powder in a half-glass of water, drink it overnight, sweat well under a warm blanket, and the temperature drops in the morning, and the headache goes away. I also use “Nimesulide” for headaches.I accept in tablets or in a powdery state. I think one of the big advantages is that this medicine is universal and inexpensive, so it can be used for different symptoms.
- Nastya. I used to buy Nise, but then I chose a domestic analogue, Nimesulide, for reviews. It also helps very well, but it costs 3 times cheaper. Excellent after surgery. Stitches do not hurt at all. All night you can sleep peacefully. It is a pity that the drug has many contraindications, so you need to strictly follow the instructions for use.
Structural analogues of the active substance:
- Nimesulide Pharmaplant;
Before using analogues consult your doctor.
Storage conditions and shelf life
Store in a dark, dry place inaccessible to children at temperature up to 25 ° C.
Shelf life - 2 years.