Nemulex granules d / prig. solution inside 100mg, No. 10

• Rheumatoid arthritis;

• osteoarthritis;

• arthritis of various etiologies;

• arthralgia;

• myalgia;

• postoperative and post-traumatic pain;

• bursitis;

• tendinitis;

• algodismenorrhea;

• toothache and headache.

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

Inside. The contents of 1 sachet 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 a 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 daily dose reduction of up to 100 mg.

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

Oral suspension granules

1 sachet

active substance: nimesulide 100 mg

excipients: macrogol cetostearate (Cremophor A25) - 100 mg; anhydrous citric acid - 19 mg; colloidal silicon dioxide (aerosil) - 40 mg; sucrose - 1721 mg; orange flavor - 20 mg

• Hypersensitivity;

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

• erosive and ulcerative lesions of the mucous membrane of the stomach and duodenum;

• active gastrointestinal bleeding;

• bleeding, incl. cerebrovascular;

• inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase;

• hemophilia and other blood clotting disorders;

• decompensated chronic heart failure;

• liver failure or any active liver disease;

• hepatotoxic reactions when using nimesulide in history;

• alcoholism;

• addiction;

• severe chronic renal failure (Cl creatinine <30 ml / min);

• progressive kidney disease;

• confirmed hyperkalemia;

• period after coronary artery bypass grafting;

• concomitant use of other hepatotoxic drugs;

• pregnancy;

• breastfeeding period;

• age up to 12 years.

With care: coronary heart disease, cerebrovascular disease, chronic heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, renal failure (Cl creatinine <30-60 ml / min), anamnestic data on the development of gastrointestinal ulcers, presence Helicobacter pylori infections, advanced age, prolonged use of NSAIDs, severe somatic diseases, concomitant use of anticoagulants (including warfarin), antiplatelet agents (including ASA, clopidogrel), oral corticosteroids, SSRIs (including citalopram , fluoxetine, paroxetine, sertraline).

pharmachologic effect

NSAIDs. It has anti-inflammatory, analgesic, antipyretic and antiplatelet effects. Unlike other NSAIDs, it selectively suppresses COX-2, inhibits the synthesis of prostaglandins in the focus of inflammation; has a less pronounced inhibitory effect on COX-1 (less often causes side effects associated with inhibition of prostaglandin synthesis in healthy tissues).

Pharmacokinetics

Suction

Oral absorption is high. Food intake reduces the rate of absorption without affecting its extent. Tmax in blood plasma is 1.5-2.5 hours. Cmax in blood plasma is 3.5-6.5 mg / l.

Distribution

Plasma protein binding - 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acid alpha1-glycoprotein 1%. Dose variation does not affect the degree of binding. Vd - 0.19-0.35 l / kg. It penetrates well into the acidic environment of the focus of inflammation (40%), synovial fluid (43%). Easily penetrates histohematogenous barriers.

Metabolism

It 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 metabolic conjugation reactions (including sulfation, glucuronidation) to be eliminated. 4-hydroxynimesulide undergoes enterohepatic recirculation.

Withdrawal

T1 / 2 of nimesulide - 1.56-4.95 hours, 4-hydroxynimesulide - 2.89-4.78 hours. 4-hydroxynimesulide is excreted by the kidneys (65%) and with bile (35%).

Side effect

From the digestive system: diarrhea, nausea, vomiting, constipation, flatulence, gastritis, abdominal pain, stomatitis, tarry stools, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenum, increased liver transaminases, hepatitis, fulminant hepatitis, jaundice, cholestasis.

Allergic reactions: hypersensitivity reactions, anaphylactoid reactions.

From the side of the central nervous system: dizziness, fear, nervousness, nightmares, headache, drowsiness, encephalopathy (Reye's syndrome).

On the part of the skin: itching, skin rash, increased sweating, erythema, dermatitis, urticaria, angioedema, facial swelling, exudative erythema multiforme, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

From the urinary system: edema, dysuria, hematuria, urinary retention, hyperkalemia, renal failure, oliguria, interstitial nephritis.

From the hematopoietic system: anemia, eosinophilia, thrombocytopenia, pancytopenia, purpura, prolonged bleeding time.

From the respiratory system: shortness of breath, exacerbation of bronchial asthma, bronchospasm.

From the senses: blurred vision.

From the side of the cardiovascular system: arterial hypertension, tachycardia, hemorrhages, hot flashes.

Others: general weakness, hypothermia.

Application during pregnancy and lactation

Use during pregnancy and lactation (breastfeeding) is contraindicated.

The use of nimesulide 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.

Application for impaired renal function

Use is contraindicated in severe chronic renal failure (CC <30 ml / min).

Application in children

Contraindicated in children under 12 years of age.

Use in elderly patients

Elderly patients do not need dose reduction.

special instructions

To reduce the risk of side effects, it is necessary to use the drug in the minimum effective dose with the shortest duration. If the patient's condition does not improve, treatment must be discontinued.

It is necessary to stop taking the drug if the temperature rises or develops against the background of taking flu-like symptoms.

If patients taking NemulexЃ develop symptoms indicating liver damage (for example, anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine), or an increase in the activity of hepatic transaminases, the drug should be discontinued. It is not recommended for such patients to prescribe NemulexЃ in the future.

Gastrointestinal bleeding or ulcer / perforation of the stomach or duodenum can develop at any time during the use of the drug and not be accompanied by clinically pronounced symptoms (including pain syndrome). If gastrointestinal bleeding or ulcers occur, the drug should be discontinued.

In case of deterioration of renal function, the drug should be canceled.

If the drug is used for more than 2 weeks, it is necessary to monitor liver function indicators.

In patients with cirrhosis of the liver or with renal failure with hypoalbuminemia or hyperbilirubinemia, the binding of nimesulide is reduced.

Elderly patients most often develop side effects when taking the drug, incl. gastrointestinal bleeding, perforation, dysfunction of the heart, kidneys and liver. Therefore, regular clinical monitoring of the patient's condition is recommended.

Influence on the ability to drive vehicles and mechanisms

If during the use of the drug there are undesirable effects on the part of the central nervous system and sensory organs, then patients should refrain from driving vehicles and engaging in activities that require increased concentration of attention and speed of psychomotor reactions.

Overdose

Symptoms: nausea, vomiting, drowsiness, apathy, gastrointestinal bleeding, increased blood pressure, acute renal failure, respiratory depression.

Treatment: symptomatic and supportive treatment is recommended. There is no specific antidote. Patients admitted to the hospital with symptoms of an overdose of the drug (within 4 hours after taking it or after taking a high dose) are recommended to wash the stomach, take activated carbon (for adults - 60-100 mg) and / or an osmotic-type laxative. Regular monitoring of liver and kidney function is required. There are no data on the possibility of removing nimesulide by hemodialysis. Forced diuresis, hemodialysis are ineffective due to the high degree of binding of the drug to proteins.

Drug interactions

There is evidence that nimesulide is able to reduce the bioavailability of furosemide, compete for binding to plasma proteins of fenofibrate, salicylic acid, tolbutamides. NemulexЃ can replace salicylic acid and furosemide (but not warfarin) in plasma proteins.

NemulexЃ has no effect on drugs that affect the concentration of glucose in the blood and glucose tolerance in patients with diabetes mellitus treated with sulfonylurea derivatives.

Physiological concentrations of unsaturated fatty acids do not affect the binding of nimesulide to serum albumin.

At therapeutic concentrations, the binding of nimesulide was not affected by warfarin, furosemide, glibenclamide, digitoxin.

It is not recommended to take NemulexЃ simultaneously with diuretics, which have a damaging effect on renal hemodynamics.

Taking NemulexЃ in therapeutic doses by mouth for a short period does not change the serum profile of digoxin in patients with mild heart failure.

In the presence of nimesulide, the free fractions of methotrexate can increase significantly.

The concentration of lithium in plasma increases with the simultaneous administration of lithium preparations and NemulexЃ.

NemulexЃ can enhance the effect of cyclosporine on the kidneys.

With the simultaneous use of the drug NemulexЃ with GCS, serotonin reuptake inhibitors, the risk of gastrointestinal bleeding increases.