Nimulide, 50mg/5ml suspension, 60ml

Composition

5 ml of suspension contains:

Active ingredient:  

nimesulide Br. F. 50.00 mg;

Auxiliary substances:  

xanthan gum,

70% sorbitol solution,

uncrystallized. glycerin (glycerol),

sucrose,

macrogol glycerylhydroxystearate (Cremophor RH 40),

sodium methyl parahydroxybenzoate,

sodium propyl parahydroxybenzoate,

sodium benzoate,

colloidal silicon dioxide,

sodium disulfite,

citric acid monohydrate,

hydrochloric acid (conc. ),

vanilla flavor

, mango flavor,

dye quinoline yellow,

purified water.

Pharmacological action

Clinical and pharmacological group: NSAIDs. Selective COX-2 inhibitor Pharmacological action

of NSAIDs from the class of sulfonanilides, a selective competitive reversible COX-2 inhibitor. It has anti-inflammatory, analgesic and antipyretic effects. It has a less pronounced depressing effect on COX-1.

Reduces the concentration of short-lived prostaglandin H₂, a substrate for kinin-stimulated prostaglandin E_{2 synthesis}, in the focus of inflammation and in the ascending pathways of pain impulses in the spinal cord. Reducing the concentration_{of prostaglandin E2} (a mediator of inflammation and pain) reduces the activation of EP-type prostanoid receptors, which is manifested by analgesic and anti-inflammatory effects.

Pharmacokineticsafter oral use, nimesulide is well absorbed from the gastrointestinal tract, _cmax in blood plasma is reached on average in 2-3 hours and is 3-4 mg/l. AUC is 20-35 mg×h / l. Binding to plasma proteins is 97.5%. After oral use of a single dose of 100 mg, nimesulide is present in the tissues of the female genital organs in a concentration of 40% of the plasma concentration. It is metabolized in the liver with the participation of the SUR2C9 isoenzyme. The main metabolite is the pharmacologically active parahydroxy derivative of nimesulide-hydroxynimesulide, which is found exclusively in the form of glucuronate. Nimesulide is mainly excreted in the urine (about 50% of the dose taken), and about 29% is excreted as metabolites in the faeces. T_1/2 is 3.2-6 hours.

Indications

Acute pain (back pain, low back pain; musculoskeletal pain, including bruises, sprains and dislocations of joints; tendinitis, bursitis; toothache); symptomatic treatment of osteoarthritis (osteoarthritis) with pain syndrome; primary algodismenorrhea.

Use during pregnancy and lactation

Nimesulide is contraindicated for use during pregnancy and lactation.

Contraindications

• Hypersensivity to the nimesulide;
• hyperergic reactions in anamnesis (bronchospasm, rhinitis, urticaria) associated with the use of acetylsalicylic acid or other NSAIDs, including nimesulide;
• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses with intolerance to acetylsalicylic acid and other NSAIDs (including in the anamnesis);
• hepatotoxic reactions to nimesulide in history;
• the simultaneous use with other drugs with potential hepatotoxicity (e. g., other NSAIDs);
• chronic inflammatory bowel disease (Crohn’s disease, ulcerative colitis) in the acute phase;
• after the coronary artery bypass surgery;
• febrile syndrome and SARS;
• suspected acute surgical pathology;
• peptic ulcer of the stomach or duodenum in the acute phase;
• erosive-ulcerative lesions in the gastrointestinal tract;
• perforation or gastrointestinal bleeding in history;
• cerebrovascular bleeding or history of other diseases, accompanied by an increased risk of bleeding;
• severe violations of coagulability of blood;
• severe heart failure;
• severe renal insufficiency (CC<30 ml/min), confirmed hyperkalemia;
• children up to age 12 years;
• pregnancy, lactation;
• alcoholism, drug addiction;
• hepatic failure, active liver disease.

With caution

Arterial hypertension, diabetes mellitus, compensated heart failure, IHD, cerebrovascular diseases, dyslipidemia/hyperlipidemia, peripheral arterial diseases, hemorrhagic diathesis, smoking, creatinine clearance 30-60 ml / min.

A history of ulcerative lesions of the gastrointestinal tract; a history of infection caused by Helicobacter pylori; advanced age; long-term previous use of NSAIDs; severe somatic diseases.

Concomitant use with the following medications: anticoagulants (e. g., warfarin), antiplatelet agents (e. g., acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (e. g., prednisone), selective serotonin reuptake inhibitors (e. g., citalopram, fluoxetine, paroxetine, sertraline).

Side effects

From the hematopoietic system:  rarely-anemia, eosinophilia, hemorrhages; very rarely-thrombocytopenia, pancytopenia, thrombocytopenic purpura.

From the immune system:  rarely-hypersensitivity reactions; very rarely-anaphylactoid reactions, very urticaria, angioedema.

Skin and subcutaneous tissue disorders:  infrequently-pruritus, skin rash, excessive sweating; rarely-erythema, dermatitis; very rarely-urticaria, facial edema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome).

Nervous system disorders:  infrequently – dizziness; very rarely-headache, drowsiness, encephalopathy (Reye’s syndrome).

Mental disorder:  rarely – a feeling of fear, nervousness, nightmarish dreams.

From the side of the visual organ:  rarely – blurred vision; very rarely-visual impairment.

Hearing disorders and labyrinth disorders:  very rarely – vertigo.

From the cardiovascular system:  infrequently-increased blood pressure; rarely-tachycardia, lability of blood pressure, “flushes” of blood to the skin of the face, palpitation sensation.

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

From the digestive system:  often – diarrhea, nausea, vomiting; infrequently-constipation, flatulence, gastritis, gastrointestinal bleeding, ulceration and / or perforation of the stomach or duodenum; very rarely – abdominal pain, dyspepsia, stomatitis, tarry stools.

Liver and biliary tract disorders:  often-increased activity of “liver” enzymes; very rarely-hepatitis, fulminant hepatitis (including fatal outcomes), jaundice, cholestasis.

From the urinary system:  rarely-dysuria, hematuria, urinary retention; very rarely-renal failure, oliguria, interstitial nephritis.

From the side of metabolism:  rarely-hyperkalemia; infrequently-peripheral edema; very rarely – hypothermia.

Other services:  rarely-malaise, asthenia.

Composition

Corticosteroid interactions increase the risk of gastrointestinal ulcers or bleeding.

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

NSAIDs may enhance the effects 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 is still unavoidable, careful monitoring of blood clotting parameters is necessary. NSAIDs can reduce the effect of diuretics. In healthy volunteers, nimesulide temporarily reduces the excretion of sodium under the action of furosemide, to a lesser extent – the excretion of potassium and reduces the actual diuretic effect. Concomitant use of nimesulide and furosemide resulted in a decrease (approximately 20%) in AUC and a decrease in the cumulative excretion of furosemide without altering the renal clearance of furosemide. Concomitant use of furosemide and nimesulide requires caution in patients with renal or cardiac insufficiency.

NSAIDs can reduce the effect of antihypertensive drugs. In patients with mild to moderate renal insufficiency (creatinine clearance 30-80 ml / min), concomitant use of ACE inhibitors, angiotensin II receptor antagonists, and agents that suppress the COX system (NSAIDs, antiplatelet agents) may lead to 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 in combination with ACE inhibitors or angiotensin II receptor antagonists. Therefore, concomitant use of these drugs should be carried out with caution, especially in elderly patients. Patients should receive sufficient fluids, and renal function should be carefully monitored after starting concomitant use. Theoretically, it is possible to reduce the effectiveness of mifepristone and prostaglandin analogues when used simultaneously with NSAIDs (including acetylsalicylic acid) due to the antiprostaglandin effect of the latter. Limited data show that the use of NSAIDs on the day of use of a prostaglandin analog does not adversely affect the effect of mifepristone or a prostaglandin analog on cervical dilatation, uterine contractility, and does not reduce the clinical effectiveness of medical termination of pregnancy.

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

Nimesulide suppresses the activity of the SUR2-C9 isoenzyme. When drugs that are substrates of this enzyme are used simultaneously with nimesulide, the concentration of the latter in plasma may increase.

Caution should be exercised when using nimesulide less than 24 hours before or after the use of methotrexate, as in such cases, the concentration of methotrexate in the blood plasma and, accordingly, toxic effects may increase.

Due to the effect on renal prostaglandins, prostaglandin synthetase inhibitors, such as nimesulide, may increase the nephrotoxicity of cyclosporins.

How to take, course of use and dosage

Inside, preferably before a meal; in case of impaired stomach function – at the end or after a meal. Adults-100 mg 2 times a day; children-1.5 mg / kg 2-3 times a day.

The maximum dose for children is no more than 5 mg / kg / day in 2-3 divided doses. When prescribing to elderly patients, no dose adjustment is required.

Special instructions

If you experience symptoms similar to those of liver damage (anorexia, pruritus, yellowing of the skin, nausea, vomiting, abdominal pain, darkening of the urine, increased activity of hepatic transaminases), you should immediately stop using nimxulide and consult a doctor. Repeated use of nimesulide in such patients is contraindicated.

Hepatic reactions, which in most cases are reversible, have been reported with short-term use of nimesulide.

During the use of nimasulide, the patient should refrain from taking other analgesics, including NSAIDs (including selective COX-2 inhibitors).

Use caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn’s disease), as these diseases may worsen. The risk of gastrointestinal bleeding, peptic ulcer/perforation of the stomach or duodenum increases in patients with a history of gastrointestinal ulceration (ulcerative colitis, Crohn’s disease), as well as in elderly patients, with an increase in the dose of NSAIDs, so treatment should begin with the lowest possible dose. Such patients, as well as patients who require concomitant use of low doses of acetylsalicylic acid or other agents that increase the risk of gastrointestinal complications, are recommended to additionally prescribe gastroprotectors (misoprostol or proton pump blockers). Patients with a history of gastrointestinal diseases, especially elderly patients, should inform the doctor about new gastrointestinal symptoms (especially those that may indicate possible gastrointestinal bleeding).

If gastrointestinal bleeding or ulcerative lesions of the gastrointestinal tract occur in patients taking nimesulide, it should be discontinued.

Given reports of visual impairment in patients taking other NSAIDs, if any visual impairment occurs, nimesulide should be discontinued immediately and an eye examination should be performed.

Nimesulide can cause fluid retention, so in patients with arterial hypertension, renal and/or heart failure, it should be used with extreme caution. If the condition worsens, treatment with nimesulide should be discontinued.

Clinical studies and epidemiological data suggest that NSAIDs, especially in high doses and with prolonged use, may lead to a low risk of myocardial infarction or stroke. To exclude the risk of such events when using nimesulide, data are not sufficient.

If signs of a cold or acute respiratory viral infection occur during the use of nimesulide, it should be immediately discontinued.

Nimesulide can alter the properties of platelets, so caution should be exercised when using it in people with hemorrhagic diathesis, but nimesulide does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.

Elderly patients are particularly susceptible to adverse reactions to NSAIDs, including the risk of gastrointestinal bleeding and perforation, which threatens the patient’s life, reduced kidney, liver and heart function. When taking nimesulide for this category of patients, proper clinical monitoring is necessary.

At the first appearance of skin rash, mucosal lesions, or other signs of an allergic reaction, nimesulide should be discontinued immediately.

Influence on the ability to drive vehicles and other mechanisms

During the use of nimesulide, caution should be exercised when driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

List B. : In a dry place, protected from light, at a temperature of 15-25 °C.

See expiration date. on the packaging.

Active ingredient

Nimesulide

Conditions of release from pharmacies

By prescription

Dosage form

suspension for oral use

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor, Children over 2 years of age

Indications

Sprains and Sprains, Rheumatoid Arthritis, Bursitis, Myositis, Tendon Inflammation, Migraines, Lumbago, Colds, Sciatica, Osteochondrosis, Sciatica, Gout