Nemux - instructions for use, dose, side effects, contraindications

Composition:Composition: 1 sachet contains: active substance: nimesulide 100 mg; Excipients: macrogol cetostearate (Cremophor A25) - 100 mg, citric acid anhydrous - 19 mg, silicon dioxide colloid (aerosil) - 40 mg, sucrose - 1721 mg, flavoring orange - 20 mg.

Description:

The granules are yellowish in color. The resulting suspension is light yellow.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug.

ATX: & nbsp

M.01.A.X Other non-steroidal anti-inflammatory drugs

M.01.A.X.17 Nimesulide

Pharmacodynamics:

Nonsteroidal anti-inflammatory drug (NSAID), has anti-inflammatory, analgesic, antipyretic and antiplatelet effect.In contrast to other NSAIDs, it selectively inhibits cyclooxygenase-2 (COX-2), inhibits the synthesis of prostaglandins (Pg) in the hearth of inflammation; has a less pronounced inhibitory effect on cyclooxygenase-1 (COX-1) (rarely causes side effects associated with inhibition of synthesis Pg in healthy tissues).

Pharmacokinetics:

Absorption when ingested - high (eating intake reduces the rate of absorption, without affecting its degree). The time to reach the maximum concentration in the blood plasma (TCam) is 1.5-2.5 hours. The connection with plasma proteins is 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acid alpha 1-glycoprotein-1%. Changenore doses does not affect the degree of binding. The maximum concentration (Cmax) is 3.5-6.5 mg / l. The volume of distribution is 0.19-0.35 l / kg. It penetrates into the acidic environment of the inflammatory focus (40%), synovial fluid (43%). Easily penetrates through the histohematological barriers. Metabolized in the liver by tissue monooxygenases. The main metabolite is 4-hydroxynimidesulide (25%), has similar pharmacological activity, but due to the reduction in the size of the molecules it is able to diffuse quickly through the hydrophobic channel of COX-2 to the active binding site of the methyl group. 4-Hydroxyimidesulide is a water-soluble compound, for the elimination of which is not required glutathione and the conjugation reaction of the second phase of metabolism (sulfation, glucuronidation, etc.). The half-life of Nimesulide (T1 / 2) is 1.56-4.95 hours, 4-hydroxynimidesulide is 2.89-4.78 hours. 4-Hydroxynimidesulide is excreted by the kidneys (65%) and with bile (35%), is enterohepatic recycling.

Indications:

- Rheumatoid arthritis;

- Osteoarthritis;

- Arthritis of various etiologies;

- Arthralgia;

- Myalgia;

- Postoperative and post-traumatic pain;

- Bursitis;

- Tendonitis;

- Algodismenorea;

- Toothache and headache.

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

Contraindications:

Hypersensitivity, complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid (ASA) and other NSAIDs (including in history), erosive and ulcerative lesions of 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 phase of exacerbation,hemophilia and other disorders of blood clotting, decompensated chronic heart failure (CHF), hepatic insufficiency or any active liver disease, hepatotoxic reactions with nimesulide in history, alcoholism, drug addiction, severe chronic renal failure (CRF) (CC less than 30 ml / min) , progressive kidney disease, confirmed hyperkalemia, the period after aortocoronary bypass grafting, simultaneous use of other hepatotoxic drugs ( LS), children under 12 years of age, pregnancy, the period of breastfeeding.

Carefully:Coronary heart disease (CHD), cerebrovascular disease, CHF, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, kidney failure (QC less than 30-60 ml / min), anamnestic data on the development of gastrointestinal ulcer ), the presence of infection Helicobacter pylori, old age, long-term use of NSAIDs, severe somatic diseases, simultaneous reception of anticoagulants (incl. warfarin), anti-regents (including ASK, clopidogrel), oral glucocorticosteroids (SCS), selective serotonin reuptake inhibitors (incl. citalopram, fluoxetan, paroxetine, sertraline).

Pregnancy and lactation:The use of nimesulide may adversely affect female fertility and is not recommended for women planning a pregnancy.

Dosing and Administration:

Inside.

The contents of 1 packet of granules 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 reduction in the daily dose to 100 mg.

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

Side effects:

Allergic reactions: hypersensitivity reactions, anaphylactoid reactions.

From the central nervous system ', dizziness, a sense of fear, nervousness, nightmarish dreams, headache, drowsiness, encephalopathy (Reye's syndrome).

From the skin: itching, skin rash, increased sweating, erythema, dermatitis, urticaria, angioedema, facial swelling, multiform exudative erythema, including 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 gastrointestinal tract: diarrhea, nausea, vomiting, constipation, flatulence, gastritis, abdominal pain, stomatitis, tarry stool, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenum.

From the liver and bile excretory system: an increase in "hepatic" tranceam-naz, hepatitis, fulminant hepatitis, jaundice, cholestasis.

From the hematopoiesis: anemia, eosinophilia, thrombocytopenia, pancytopenia, purpura, prolongation of bleeding time.

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

From the sense organs: blurred vision.

From the cardiovascular system: Arterial hypertension, tachycardia, hemorrhages, "hot flashes".

Other: general weakness, hypothermia.

Overdose:

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

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

Interaction:

There is evidence that nimesulide can reduce the bioavailability of furosemide, compete with the binding of plasma proteins to fenofibrate, salicylic acid, tolbutamide."Nimelide" can replace salicylic acid and furosemide (but not warfarin) in plasma proteins. It has no effect on drugs affecting the concentration of glucose and glucose tolerance in diabetic patients treated with various drugs containing sulfonylureas. It is not recommended to take nimesulide concomitantly with diuretics, which have a damaging effect on renal hemodynamics.

The physiological concentrations of unsaturated fatty acids do not affect the binding of nimesulide to serum albumin. In therapeutic concentrations, the binding of nimesulide was not affected warfarin, furosemide, glibenclamide, digitoxin. In the presence of nimesulide, free fractions of methotrexate can increase significantly. Taking nimesulide in therapeutic doses orally for a short period does not change the serum digoxin profile in patients with mild heart failure.

The concentration of lithium in plasma increases with simultaneous intake of lithium and nimesulide preparations. Nimesulide can enhance the action of cyclosporin on the kidneys.Use with glucocorticosteroids, serotonin reuptake inhibitors increasedthe risk of developing gastrointestinal bleeding.

Special instructions:

To reduce the risk of side effects, it is necessary to apply the drug at the lowest effective dose with the shortest duration. If the patient's condition does not improve, treatment should be stopped.

It is necessary to stop taking the drug in case of fever or development on the background of its intake of influenza-like symptoms.

When appearing in patients receiving Nimesulide, symptoms indicative of liver damage (eg, anorexia, nausea, vomiting, abdominal pain, increased fatigue, dark urine), or increased levels of "liver" transaminases, the drug should be discontinued. It is not recommended to appoint such patients Nimesulide and in the future.

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 expressed symptoms (including pain syndrome). If there is a gastrointestinal bleeding or ulcers, the drug should be discarded.

If the kidney function worsens, the drug should be discarded.

In the case of using the drug for more than 2 weeks, monitoring of liver function parameters is necessary.

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

In elderly patients, the most common side effects when taking the drug, including gastrointestinal bleeding, perforation, impaired heart, kidney and liver function. Therefore, regular clinical monitoring of the patient's condition is recommended.

Effect on the ability to drive transp. cf. and fur:In case when using the drug there are undesirable phenomena from the central nervous system and sensory organs, it is necessary to refrain from driving by car and to engage in activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Granules for the preparation of a suspension for Ingestion 100 mg.

2 grams of granules in a laminated bag from a three-layer foil (polyethylene, aluminum, paper).

By 2,4,6,10, 20 or 30 bags together with instructions for use in a pack of cardboard.

Packaging:2) - laminated bags of three-layer foil (10) / 2 grams of granules in laminated bags of three-layer foil. For 10 bags with instructions for use in a pack of cardboard / - Pack of cardboard
(2) - laminated bags of three-layer foil (2) / 2 grams of granules in laminated bags of three-layer foil. 2 packs with instructions for use in a pack of cardboard / - Pack of cardboard
(2) - laminated bags of three-layer foil (20) / 2 grams of granules in laminated bags of three-layer foil. For 20 bags with instructions for use in a pack of cardboard / - A pack of cardboard
(2) - laminated bags of three-layer foil (30) / 2 grams of granules in laminated bags of three-layer foil. 30 packs with instructions for use in a pack of cardboard / - A pack of cardboard
(2) - laminated bags of three-layer foil (4) / 2 grams of granules in laminated bags of three-layer foil. For 4 bags with instructions for use in a pack of cardboard / - Pack of cardboard
(2) - laminated bags of three-layer foil (6) / 2 grams of granules in laminated bags of three-layer foil. 6 packs with instructions for use in a pack of cardboard / - A pack of cardboard
(2) - laminated bags of three-layer foil / "In bulk". 2 grams of granules in a laminated bag of three-layer foil. For 880 sachets per box of cardboard. / - carton box

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006686/10

Date of registration:15.07.2010

The owner of the registration certificate:FarmSirma Soteks, ZAO FarmSirma Soteks, ZAO Russia

Manufacturer: & nbsp

FarmSirma Soteks, ZAO Russia

Information update date: & nbsp14.08.2015

Illustrated instructions

Instructions

Nemux® (Nemuleks®)