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

non-crystallized 500.00 mg, glycerol (glycerol) 150.00 mg, sucrose 1000.00 mg, macrogol glyceryl hydroxy stearate (Cremophor RH 40) 10.00 mg, sodium methylparahydroxybenzoate 9.00 mg, sodium propyl parahydroxybenzoate 1.00 mg, sodium benzoate 10.00 mg, silicon colloidal dioxide 10.00 mg, sodium disulphite 2.50 mg, citric acid monohydrate 1.25 mg, hydrochloric acid (conc.) 0.009 ml, vanilla flavor additive 0.00218 ml, mango flavor additive 0.00405 ml, quinoline yellow color 0.275 mg, purified water q.s. up to 5 ml.

Description:a suspension of yellow color with a fragrant smell.

Pharmacotherapeutic group:nonsteroidal anti-inflammatory drug (NSAID).

ATX: & nbsp

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

M.01.A.X.17 Nimesulide

Pharmacodynamics:

Non-steroidal anti-inflammatory drug (NSAID) from the class of sulfonylides. Has the properties of a selective inhibitor of cyclooxygenase-2 (COX-2) - an enzyme involved in the synthesis of prostaglandins - mediators of edema, inflammation and pain; to a lesser extent inhibits the activity of COX-1. Has anti-inflammatory, analgesic and antipyretic effect.

Pharmacokinetics:

Absorption when ingested - high. Eating lowers the absorption rate without affecting its degree. Subjected to enterohepatic recirculation. The time to reach the maximum concentration of active substance in the blood plasma is 1.5-2.5 hours. The connection with plasma proteins is 95%, with erythrocytes 2%, with lipoproteins -1%, with acid alpha 1-glycoproteins 1%.

The dose of the drug does not affect the degree of its binding to blood proteins.

The maximum concentration of nimesulide in blood plasma is 3.5-6.5 mg / l. [The volume of distribution is 0,19 - 0,35 l / kg * Penetrates into the tissues of the female genital organs, where after a single intake its concentration is about 40% of the concentration in the plasma.It penetrates into the acidic environment of the inflammatory focus (40%), synovial fluid (43%). Easily penetrates through the histo-hematical barriers.

Metabolized in the liver by tissue monooxygenases. The main metabolite - 4-hydroxynimidesulide (25%) has similar pharmacological activity.

The half-life of nimesulide is 1.56-4.95 hours, 4-hydroxynimidesulide - 2.89-4.78 hours. 4-hydroxyynesulide is excreted by the kidneys (65%) and with bile (35%).

In patients with renal insufficiency (creatinine clearance 1.8 to 4.8 l / h or 30 to 80 ml / min), as well as in children and the elderly, the pharmacokinetic profile of nimesulide does not change significantly.

Indications:Rheumatoid arthritis, osteoarthritis, arthritis of various etiologies, arthralgia, myalgia, postoperative and post-traumatic pains, bursitis, tendonitis, algodismenorea, dental and headache, including with febrile syndrome.

Contraindications:

Hypersensitivity, erosive-ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), bleeding from the gastrointestinal tract, complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acids and other non-steroidal anti-inflammatory drugs (including history), any violations of the liver function, renal failure (creatinine clearance less than 30 ml / min), cerebrovascular bleeding, inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the phase of exacerbation, hemophilia and other coagulation disorders blood, decompensated chronic heart failure, hepatotoxic reactions with nimesulide in history, alcoholism, drug addiction, progressive kidney disease, confirmed by hypercalcia a period after aortocoronary bypass surgery, simultaneous reception | other hepatotoxic drugs, pregnancy, lactation, children under 2 years.

Carefully:

Carefully: arterial hypertension, heart failure, type 2 diabetes, ischemic heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, peripheral arterial disease, smoking, renal failure (creatinine clearance 30-60 ml / min), anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of infection Helicobacter pylori, old age, long-term use of non-steroidal anti-inflammatory drugs, alcoholism, severe somatic diseases, concurrent | admission anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), oral glucocorticosteroids, selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).

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

Dosing and Administration:

Adults: inside, 100 mg (10 ml) 2 times a day. The maximum daily intake for adults is 200 mg (20 ml). In the presence of diseases of the gastrointestinal tract, the drug should be taken at the end of the meal or after eating.

Children from 2 years: inside, appoint at the rate of a single dose of 1.5 mg / kg body weight of the child 2-3 times a day, the maximum daily dose of the drug - 5 mg / kg per day. To adolescents with a body weight of more than 40 kg-100 mg (10 ml) not more than 2 times a day.

Side effects:

The frequency is classified according to the headings, depending on the occurrence of the event: very often (> 1/10), often (> 1/100), infrequently (> 1/1000), rarely (> 1/10000), very rarely (1/10000 ).

Central nervous system: infrequently - dizziness; rarely - a sense of fear, nervousness, "nightmarish dreams"; very rarely - headache, drowsiness, encephalopathy (Reye syndrome).

Gastrointestinal tract: often - diarrhea, nausea, vomiting, increase in "liver" transaminases; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, stomatitis, tarry stool, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenum, hepatitis, fulminant hepatitis, jaundice, cholestasis Respiratory system: infrequently - shortness of breath; very rarely - bronchial asthma, bronchospasm. The cardiovascular system: infrequently - arterial hypertension; rarely - tachycardia, "hot flashes".

Sense organs: rarely - blurred vision, very rarely - dizziness.

Skin and mucous membranes: infrequently - itching, rash, increased sweating ;, rarely: erythema, dermatitis; very rarely: urticaria, angioedema, facial swelling, multiform exudative erythema, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

Kidney and urinary system: infrequently - swelling; rarely - dysuria, hematuria, urinary retention, hyperkalemia; very rarely - renal failure, oliguria, interstitial nephritis.

Hematopoiesis: rarely - anemia, eosinophilia; very rarely - thrombocytopenia, pancytopenia, hemorrhage, purpura, prolongation of bleeding time.

Allergic reactions: rarely - hypersensitivity reactions; very rarely anaphylactoid reactions.

Other: rarely - general weakness; very rarely - hypothermia.

Overdose:

Symptoms: apathy, drowsiness, nausea, vomiting. Symptoms are reversible in the provision of supportive care for patients. There may be gastrointestinal bleeding, arterial hypertension, acute renal failure, respiratory depression.

Treatment: It requires symptomatic treatment of the patient and supporting care of the patient. There is no specific antidote. In case an overdose has occurred within the last 4 hours, it is necessary to induce vomiting, to ensure the reception of activated charcoal, (60-100 g per adult person), osmotic laxatives. Forced diuresis, hemodialysis - ineffective because of the high connection of the drug with proteins.

Interaction:

The effect of medications that reduce blood coagulability, increases with their simultaneous use with nimesulide.

Nimesulide may reduce the action of furosemide. Nimesulide can increase the possibility of side effects with the simultaneous administration of methotrexate. The level of lithium in the plasma increases with simultaneous reception 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 the supervision of a physician, undergoing inspection at short intervals, Nimesulide can enhance the action of cyclosporin on the kidneys.

Hepatotoxic drugs - increase the risk of hepatotoxic action. When used simultaneously with glucocorticosteroids, selective serotonin reuptake inhibitors, the risk of bleeding from the gastrointestinal tract increases.

Special instructions:

When prescribing the medication, elderly patients do not need to adjust the dosage regimen.

With prolonged use, systematic monitoring of liver and kidney function is necessary at least once every two weeks.

If there are signs of liver damage (pruritus, jaundice, nausea, vomiting, abdominal pain, darkening of urine, increased activity of "liver" transaminases), stop taking the drug immediately and consult a doctor.

Given reports of visual impairment in patients taking [other non-steroidal anti-inflammatory drugs, if any visual impairment occurs, treatment should be immediately discontinued and an ophthalmological examination performed.

The drug may cause fluid retention, so patients with high blood pressure and heart disease nimesulide should be used with extreme caution.

Patients should undergo regular medical supervision if they take medications along with nimesulide, for which the effect on the gastrointestinal tract is characteristic.

Do not use the drug simultaneously with other non-steroidal anti-inflammatory drugs.

Nimesulide may reduce platelet aggregation, but it does not replace the preventive effect of antiplatelet agents (including acetylsalicylic acid, clopidogrel, ticlopidine) in cardiovascular diseases.

Effect on the ability to drive transp. cf. and fur:

Care must be taken when driving vehicles and engaging in other potentially hazardous activities that require a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Suspension for oral administration 50 mg / 5 ml.

For 60 ml in bottles of brown glass or plastic with a screwed-on drip tray. Each bottle together with the instruction for use and the measuring cup is placed in a cardboard box.

Packaging:(60) - brown glass vials or plastic screw cap (1) / 60 ml vials of brown glass or plastic screw cap. Each vial together with instructions for use and a measured glass is placed in a cardboard box / -. The cardboard pack

Storage conditions:

Store in a dry, protected from light place at a temperature below 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011525 / 01

Date of registration:09.02.2012

The owner of the registration certificate:KORAL-MED, CJSC KORAL-MED, CJSC Russia

Manufacturer: & nbsp

PANACEA BIOTEC, Ltd. India

Representation: & nbspKORAL-MED, CJSCKORAL-MED, CJSC

Information update date: & nbsp14.08.2015

Illustrated instructions

Instructions

Nimoolid (Nimulid)