Nise tablets 100mg, No. 20

• rheumatoid arthritis;

• articular syndrome with exacerbation of gout;

• psoriatic arthritis;

• ankylosing spondylitis;

• osteochondrosis with radicular syndrome;

• osteoarthritis;

• myalgia of rheumatic and non-rheumatic genesis;

• inflammation of ligaments, tendons, bursitis, incl. post-traumatic inflammation of soft tissues;

• pain syndrome of various origins (including in the postoperative period, with injuries, algomenorrhea, toothache, headache, arthralgia, lumboishalgia).

• The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.

The drug should be used in the minimum effective dose for the smallest possible short course. The tablets are taken with sufficient water, preferably after meals. In the presence of gastrointestinal diseases, it is advisable to take the drug at the end of a meal or after a meal.

Adults and children over 12 years old - inside 1 tab. 2 times / day

The maximum daily dose for adults is 200 mg. Patients with chronic renal failure require a daily dose reduction of up to 100 mg.

Tablets are white with a yellowish tinge, round, biconvex, with a smooth surface.

1 tab.

nimesulide 100 mg

Excipients: calcium hydrogen phosphate - 75 mg, microcrystalline cellulose (type 114) - 40 mg, corn starch - 54 mg, sodium carboxymethyl starch - 35 mg, magnesium stearate - 3 mg, colloidal silicon dioxide - 2 mg, talc - 1 mg.

• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including 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 blood clotting disorders;

• decompensated heart failure;

• liver failure or any active liver disease;

• a history of indications of the development of hepatotoxic reactions when using nimesulide preparations; concomitant use of potentially hepatotoxic substances;

• alcoholism, drug addiction;

• severe renal failure (CC <30 ml / min);

• progressive kidney disease;

• confirmed hyperkalemia;

• period after coronary artery bypass grafting;

• pregnancy;

• lactation period (breastfeeding);

• children under 12 years of age;

• hypersensitivity to the active substance or auxiliary components of the drug.

• With caution: coronary artery disease, cerebrovascular diseases, congestive heart failure, arterial hypertension, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, CC <60 ml / min, history of the development of gastrointestinal ulcers, the presence of Helicobacter pylori infection, severe somatic diseases , concomitant therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral corticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline), long-term use of paroxetine, sertraline), elderly age, smoking, frequent alcohol consumption.

pharmachologic effect

NSAIDs from the sulfonanilide class. It is a selective competitive inhibitor of COX-2, inhibits the synthesis of prostaglandins in the focus of inflammation. The depressing effect on COX-1 is less pronounced (less often it causes side effects associated with inhibition of prostaglandin synthesis in healthy tissues). It has anti-inflammatory, analgesic and pronounced antipyretic effects.

Pharmacokinetics

Suction

After oral administration, nimesulide is well absorbed from the gastrointestinal tract. Food intake reduces the rate of absorption without affecting its extent. Cmax of nimesulide is 3.5-6.5 mg / l.

Distribution

Plasma protein binding is 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acidic ? 1-glycoproteins - 1%. The dose of the drug does not affect the degree of binding to blood proteins. Vd is 0.19-0.35 l / kg. Penetrates into the tissues of the female genital organs, where after a single dose, the concentration of nimesulide 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 histohematogenous barriers.

Metabolism

Nimesulide is metabolized in the liver by tissue monooxygenases. The main metabolite, 4-hydroxynimesulide (25%), has a similar pharmacological activity, but due to a decrease in the size of the molecules, it is able to quickly diffuse along the hydrophobic channel of COX-2 to the active binding site of the methyl group. 4-hydroxynimesulide is a water-soluble compound that does not require glutathione and phase II metabolism conjugation reactions (sulfation, glucuronidation, etc.) to be eliminated. Excretion T1 / 2 of nimesulide is 1.56-4.95 hours, T1 / 2 of 4-hydroxynimesulide - 2.89-4.78 hours. The metabolite is excreted by the kidneys (65%) and bile (35%), undergoes enetrohepatic recirculation. Pharmacokinetics in special clinical cases In patients with renal insufficiency (CC 30-80 ml / min),as well as in children and the elderly, the pharmacokinetic profile of nimesulide does not change significantly.

Side effect

Determination of the frequency of side effects: often (1-10%), infrequently (0.1-1%), rarely (0.01-0.1%), very rarely (<0.01%), including individual messages. Allergic reactions: rarely - hypersensitivity reactions; very rarely - urticaria, angioedema, anaphylactoid reactions. From the side of the central nervous system: infrequently - dizziness; rarely - a feeling of fear, nervousness, nightmares; very rarely - headache, drowsiness, encephalopathy (Reye's syndrome). From the side of the skin: infrequently - itching, rash, increased sweating; rarely - erythema, dermatitis; very rarely - swelling of the face, erythema multiforme exudative, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome). From the urinary system: infrequently - edema; rarely - dysuria, hematuria, urinary retention, hyperkalemia;very rarely - renal failure, oliguria, interstitial nephritis. From the digestive system: often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, stomatitis, tarry stools, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenum. From the liver and biliary system: often - increased hepatic transaminases; very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis. From the side of hematopoiesis: rarely - anemia, eosinophilia; very rarely - thrombocytopenia, pancytopenia, purpura, prolonged bleeding time. From the respiratory system: infrequently - shortness of breath; very rarely - exacerbation of bronchial asthma, bronchospasm. From the senses: rarely - blurred vision. On the part of the cardiovascular system:infrequently - arterial hypertension; rarely - tachycardia, hemorrhages, hot flashes. Others: rarely - general weakness; very rarely - hypothermia.

Application during pregnancy and lactation

The use of NiseЃ during pregnancy and lactation (breastfeeding) is contraindicated. The use of the drug may adversely affect female fertility and is not recommended for women planning a pregnancy.

Application for violations of liver function

Contraindicated in liver failure or any active liver disease, a history of the development of hepatotoxic reactions with the use of nimesulide preparations, the concomitant use of potentially hepatotoxic substances.

Application for impaired renal function

Contraindicated in severe renal failure (CC <30 ml / min), in progressive kidney disease. Patients with chronic renal failure require a daily dose reduction of up to 100 mg.

Application in children

The use of tablets (100 mg) is contraindicated in children under 12 years of age, dispersible tablets (50 mg) in children under 7 years of age.

Use in elderly patients

The drug should be used with caution in elderly patients.

special instructions

Since nimesulide is partially excreted by the kidneys, its dose for patients with impaired renal function should be reduced, depending on the CC value. Given the reports of visual impairment in patients taking other NSAIDs, treatment should be stopped immediately if any visual impairment occurs, and the patient should be examined by an ophthalmologist. The drug can cause fluid retention in the tissues, therefore NiseЃ should be used with extreme caution in patients with high blood pressure and cardiac disorders. Regular medical supervision is required if the patient, along with nimesulide, is taking medications that have an effect on the gastrointestinal tract. When signs of liver damage appear (itching, yellowness of the skin, nausea, vomiting, abdominal pain, darkening of urine,increased activity of hepatic transaminases), you should stop taking the drug and consult your doctor. The drug should not be used concomitantly with other NSAIDs. The drug can change the properties of platelets, but does not replace the prophylactic effect of acetylsalicylic acid in cardiovascular diseases. After 2 weeks of using the drug, it is necessary to monitor the biochemical parameters of liver function. Use in pediatrics The drug is contraindicated in children under 12 years of age.After 2 weeks of using the drug, it is necessary to monitor the biochemical parameters of liver function. Use in pediatrics The drug is contraindicated in children under 12 years of age.After 2 weeks of using the drug, it is necessary to monitor the biochemical parameters of liver function. Use in pediatrics The drug is contraindicated in children under 12 years of age.

Influence on the ability to drive vehicles and use mechanisms

The drug can cause drowsiness, dizziness and blurred vision, therefore, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Overdose

Symptoms: apathy, drowsiness, nausea, vomiting, gastrointestinal bleeding, increased blood pressure, acute renal failure, respiratory depression are also possible. Treatment: symptomatic and supportive therapy. There is no specific antidote. If an overdose has occurred within the last 4 hours, it is necessary to induce vomiting, ensure the intake of activated carbon (60-100 g per adult), osmotic laxatives. Forced diuresis, hemodialysis are ineffective due to the high degree of binding of the drug to plasma proteins.

Drug interactions

The effect of drugs that reduce blood clotting is enhanced by their simultaneous use with nimesulide. Nimesulide is able to reduce the effect of furosemide. Nimesulide may increase the possibility of developing adverse reactions while taking methotrexate. The concentration of lithium in plasma increases with the simultaneous administration of lithium and nimesulide preparations. Due to the high degree of binding of nimesulide to plasma proteins, patients who are simultaneously treated with hydantoin and sulfonamides should be under medical supervision, undergoing examination at short intervals. Nimesulide may increase the effect of cyclosporine on the kidneys. When used simultaneously with GCS, serotonin reuptake inhibitors, it increases the risk of gastrointestinal bleeding.