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

Excipients: docusate sodium 1.8 mg, giprolose 2 mg, povidone 8 mg, lactose monohydrate 122 mg, cellulose microcrystalline 144 mg, castor oil hydrogenated 1.2 mg, magnesium stearate 1 mg, carboxymethyl sodium starch 20 mg.

Description:Tablets are pale yellow or yellowish in color, flat-cylindrical with a facet and a risk.

Pharmacotherapeutic group:nonsteroidal anti-inflammatory drug.

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 sulfonanilides.It is a selective competitive inhibitor of cyclooxygenase-2 (COX-2), inhibits the synthesis of prostaglandins in the inflammatory focus. The inhibitory effect on COX-1 is less pronounced (it rarely causes side effects associated with the inhibition of prostaglandin synthesis in healthy tissues). Has anti-inflammatory, analgesic and pronounced antipyretic effect.

Pharmacokinetics:

Absorption when ingested - high (eating intake reduces the rate of absorption, without affecting its degree). Communication with plasma proteins 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acid alpha 1-glycoproteids - 1%. The dose change does not affect the degree of binding. Cmax - 3,5-6,5 mg / l. The volume of distribution is 0.19-0.35 l / kg. Penetrates into the tissue 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 histohematological barriers. Metabolized in the liver by tissue monooxygenases. The main metabolite is 4-hydroxynimidesulide (25%), has a similar pharmacological activity, but due to the decrease 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-hydroxynimidesulide 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 and others).

T1/2 nimesulide - about 1.56-4.95 h, 4-hydroxynimidesulide - 2.89-4.78 h. 4-hydroxynimidesulide is excreted by the kidneys (65%) and bile (35%), is subjected to enterohepatic recirculation.

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

Indications:

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, including post-inflammatory soft tissue inflammation, pain syndrome of various origins (including number in the postoperative period, with trauma, algodismenorea, toothache, headache, arthralgia, lumboeishalgia), febrile syndrome with infectious inflammatory diseases.

Contraindications:Hypersensitivity to the drug components, erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), bleeding from the gastrointestinal tract; a history of bronchospasm, urticaria, or acute rhinitis associated with the use of acetylsalicylic acid, NSAIDs; liver failure; renal failure (creatinine clearance less than 30 ml / min, confirmed hyperkalemia), severe heart failure, severe blood clotting disorders, post-coronary artery bypass grafting, pregnancy, lactation, children under 12 years.

Carefully:

Ischemic heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance less than 60 ml / min.

Anamnestic data on the development of gastrointestinal lesions, the presence of infection Helicobacter pylori, old age, prolonged use of NSAIDs, frequent alcohol use, severe physical illness, concomitant therapy with the following drugs:

- Anticoagulants (for example, warfarin)

- antiaggregants (eg, acetylsalicylic acid, clopidogrel)

- oral glucocorticosteroids (for example, prednisolone)

- selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline)

Dosing and Administration:

Adults and children over 12 years of age (body weight over 40 kg) are prescribed tablets of 1 tablet 2 times a day.

Tablets are taken after meals with enough water. The maximum daily dose is 200 mg.

Side effects:

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

Gastrointestinal tract: often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, stomatitis, tarry stool, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenum.

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

Respiratory system-, infrequently - shortness of breath; very rarely - bronchial asthma, bronchospasm. The cardiovascular system: infrequently - arterial hypertension; rarely - tachycardia, hemorrhages, "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).

Liver and biliary system: often - increased "liver" transaminases; very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis.

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

Organs of hematopoiesis: rarely - anemia, eosinophilia; very rarely - thrombocytopenia, pancytopenia, purpura, prolonged bleeding time.

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

General Reagents: rarely - general weakness; very rarely - hypothermia.

In case of occurrence of other, not mentioned above, side effects or worsening of your state of health, please contact your doctor immediately.

Overdose:

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

Treatment: requires symptomatic treatment of the patient and maintenance of care for him. There is no specific antidote. In case an overdose has occurred within the last 4 hours, it is necessary to induce vomiting, to receive activated charcoal (60-100 g per adult), osmotic laxatives. Forced diuresis, hemodialysis are 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. Reduces the therapeutic effect of antihypertensive drugs. Nimesulide can increase the possibility of occurrence of side effects with simultaneous admissionmethotrexate.

The level of lithium in the plasma increases with simultaneous reception of lithium and nimesulide preparations. Because of the high degree of binding of nimesulide to plasma proteins, patients who are treated with hydantoin and sulfonamides at the same time should be under the supervision of a physician, passing the examination at short intervals.

Nimesulide can enhance the action of cyclosporin on the kidneys.

Use with glucocorticosteroids, serotonin reuptake inhibitors increases the risk of developing gastrointestinal bleeding.

Special instructions:

Nimesulide should be used with caution in patients with a tendency to bleed, patients with upper gastrointestinal tract diseases or patients receiving medications that reduce blood clotting, or drugs that inhibit platelet aggregation.

Because the Nimesulide partially excreted by the kidneys, dosage for patients with impaired renal function should be reduced, depending on the level of urination. Given reports of visual impairment in patients taking other NSAIDs, treatment should be stopped immediately if any visual impairment occurs and the oculist should examine the patient.

The drug can cause fluid retention in tissues, so patients with high blood pressure and with cardiac disorders Nimesulide should be used with extreme caution. Patients should undergo regular medical supervision if they take medications along with nimesulide, which are characterized by an effect on the gastrointestinal tract. Patients whose work requires concentration (constant attention) should be aware that the drug may cause drowsiness or dizziness.

To reduce the risk of developing adverse events on the part of the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

Form release / dosage:

Tablets of 100 mg. For 10 tablets in a blister, two blisters are placed in a cardboard box together with instructions for use.

Packaging:tablets, 100 mg (contour cell packaging) 10 x 2 (carton pack) Angro package: tablets, 100 mg (bag) 1000 x 1 (polypropylene container); tablets, 100 mg (contour pack) 10 x 1000 (carton box)

Storage conditions:AT protected from light at a temperature of no higher than 25 ° C. Keep out of the reach of children!

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-002222/08

Date of registration:31.03.2008

The owner of the registration certificate:REPLEK FARM Skopje, OOOREPLEK FARM Skopje, OOO Macedonia

Manufacturer: & nbsp

REPLEK FARM SCOPE, LLC Russia

Representation: & nbspREPLECK FARM LTD SCOPJEREPLECK FARM LTD SCOPJERussia

Information update date: & nbsp15.08.2015

Illustrated instructions

Instructions

Nimesulide (Nimesulid)