Nimulide suspension for oral administration 50mg / 5ml, 60ml

• Acute pain (back pain, lower back pain; pain in the musculoskeletal system, including bruises, sprains and dislocations of the joints; tendinitis, bursitis; toothache);

• symptomatic treatment of osteoarthritis (osteoarthritis) with pain syndrome;

• primary algomenorrhea.

Inside adults 100-200 mg 2, children 1.5 mg / kg 2-3

Maximum dose: for children - 5 mg / kg / 2-3 divided doses.

5 ml

nimesulide 50 mg

excipients: xanthan gum; sorbitol solution 70% uncrystallized; glycerol; sucrose; macrogol glyceryl hydroxystearate (Cremophor RH-40); sodium methyl parahydroxybenzoate; sodium propyl parahydroxybenzoate; sodium benzoate; colloidal silicon dioxide; sodium disulfite; citric acid monohydrate; hydrochloric acid (conc.); flavoring additive - vanilla; flavoring additive - mango; dye quinoline yellow; purified water

• Peptic ulcer of the stomach and duodenum in the acute phase,

• acute bleeding from the gastrointestinal tract,

• moderate to severe hepatic impairment

• , renal failure (CC less than 30 ml / min),

• pregnancy, lactation;

• hypersensitivity to nimesulide and other NSAIDs (including acetylsalicylic acid).

pharmachologic effect

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

Reduces the concentration of short-lived prostaglandin H2, a substrate for kinin-stimulated synthesis of prostaglandin E2, in the focus of inflammation and in the ascending pathways of pain impulses in the spinal cord. A decrease in the concentration of prostaglandin E2 (a mediator of inflammation and pain) reduces the activation of prostanoid receptors of the EP type, which manifests itself in analgesic and anti-inflammatory effects.

Pharmacokinetics

After oral administration, nimesulide is well absorbed from the gastrointestinal tract, Cmax in blood plasma is achieved on average after 2-3 hours and is 3-4 mg / l. AUC is 20-35 mg h / l. Plasma protein binding is 97.5%. After oral administration of a single dose of 100 mg, nimesulide is present in the tissues of the female genital organs at a concentration of 40% of the plasma concentration. It is metabolized in the liver with the participation of the CYP2C9 isoenzyme. The main metabolite is the pharmacologically active parahydroxy derivative of nimesulide - hydroxynimesulide, which is found exclusively in the form of glucuronate. Nimesulide is excreted from the body mainly in the urine (about 50% of the dose taken), in the form of metabolites, about 29% is excreted in the feces. T1 / 2 is 3.2-6 hours.

Side effect

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.

On the part of the skin and subcutaneous tissues: infrequently - itching, skin rash, excessive sweating; rarely - erythema, dermatitis; very rarely - urticaria, facial edema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

From the nervous system: infrequently - dizziness; very rarely - headache, drowsiness, encephalopathy (Reye's syndrome).

Mental disorder: rarely - a feeling of fear, nervousness, nightmares.

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

On the part of the organ of hearing and labyrinthine disorders: very rarely - vertigo.

From the side of the cardiovascular system: infrequently - increased blood pressure; rarely - tachycardia, blood pressure lability, flushes of blood to the skin of the face, palpitations.

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, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenum; very rarely - abdominal pain, dyspepsia, stomatitis, tarry stools.

From the liver and biliary tract: often - increased activity of 'liver' enzymes; very rarely - hepatitis, fulminant (fulminant) hepatitis (including deaths), 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.

Others: rarely - malaise, asthenia.

Application during pregnancy and lactation

Nimesulide is contraindicated for use during pregnancy and during breastfeeding.

Application for violations of liver function

Contraindicated in moderate to severe hepatic impairment.

Application for impaired renal function

Contraindicated in renal failure (CC less than 30 ml / min).

Use in elderly patients

When applied externally, a doctor's control over the condition of elderly patients with impaired renal function, liver function, and congestive heart failure is required.

special instructions

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

Reported reactions from the liver, which in most cases are reversible, 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).

With caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn's disease), since an exacerbation of these diseases is possible. 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, therefore, treatment should be started with the lowest possible dose. For such patients, as well as for patients who require the simultaneous use of low doses of acetylsalicylic acid or other drugs that increase the risk of complications from the gastrointestinal tract, it is recommended to additionally prescribe the intake of gastroprotective agents (misoprostol or proton pump blockers). Patients with a history of gastrointestinal diseases,especially elderly patients, should inform the doctor about new symptoms from the gastrointestinal tract (especially about symptoms that may indicate possible gastrointestinal bleeding).

In the event of gastrointestinal bleeding or ulcerative lesions of the gastrointestinal tract in patients taking nimesulide, it should be canceled.

Given the reports of visual impairment in patients taking other NSAIDs, if any visual impairment occurs, the use of nimesulide should be stopped immediately and an ophthalmological examination should be performed.

Nimesulide can cause fluid retention, therefore, in patients with arterial hypertension, with 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, can lead to a small risk of myocardial infarction or stroke. There is insufficient data to exclude the risk of such events when using nimesulide.

If signs of a cold or ARVI occur during the use of nimesulide, it should be canceled immediately.

Nimesulide can change the properties of platelets, therefore, care must be taken when using it in persons with hemorrhagic diathesis, however, nimesulide does not replace the prophylactic action of acetylsalicylic acid in cardiovascular diseases.

Elderly patients are especially susceptible to adverse reactions to NSAIDs, incl. the risk of gastrointestinal bleeding and perforation, life-threatening the patient, decreased kidney, liver and heart function. When taking nimesulide for this category of patients, proper clinical supervision is required.

At the first manifestations of a skin rash, damage to the mucous membranes or other signs of an allergic reaction, nimesulide should be discontinued immediately.

Influence on the ability to drive vehicles and other mechanisms

During the period of nimesulide use, care should be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Drug interactions

GCS increase the risk of gastrointestinal ulcers or bleeding.

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

NSAIDs can enhance 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 the combination therapy still cannot be avoided, it is necessary to carefully monitor the blood clotting parameters.

NSAIDs can reduce the effect of diuretics. In healthy volunteers, nimesulide temporarily reduces the excretion of sodium by furosemide, to a lesser extent - excretion of potassium and reduces the actual diuretic effect.
The simultaneous use of nimesulide and furosemide leads to a decrease (by approximately 20%) AUC and a decrease in the cumulative excretion of furosemide without changing the renal clearance of furosemide. The simultaneous use of furosemide and nimesulide requires caution in patients with renal or heart failure.

NSAIDs can reduce the effect of antihypertensive drugs. In patients with mild to moderate renal failure (CC 30-80 ml / min), with the simultaneous use of ACE inhibitors, angiotensin II receptor antagonists and agents that suppress the COX 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 in combination with ACE inhibitors or angiotensin II receptor antagonists. Therefore, the simultaneous use of these drugs should be carried out with caution, especially in elderly patients. Patients should receive an adequate amount of fluid, and renal function should be closely monitored after the start of concomitant use.

It is theoretically possible to reduce the effectiveness of mifepristone and prostaglandin analogues when used simultaneously with NSAIDs (including acetylsalicylic acid) due to the antiprostaglandin action of the latter. Limited data show that the use of NSAIDs on the day of administration 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 efficacy 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 the blood plasma and its toxicity. When using nimesulide in patients on therapy with lithium preparations, regular monitoring of the concentration of lithium in the blood plasma should be carried out.

Nimesulide inhibits the activity of the CYP2C9 isoenzyme. With the simultaneous use of drugs that are substrates of this enzyme with nimesulide, the concentration of the latter in plasma may increase.

When using nimesulide less than 24 hours before or after using methotrexate, caution is required, because in such cases, the concentration of methotrexate in the blood plasma and, accordingly, the toxic effects may increase.

In connection with the effect on renal prostaglandins, inhibitors of prostaglandin synthetases, which include nimesulide, can increase the nephrotoxicity of cyclosporins.