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

Excipients: microcrystalline cellulose 58 mg, corn pregelatinized corn starch 15 mg, low-substituted giprolose 20 mg, croscarmellose sodium 4 mg, sodium lauryl sulfate 1 mg, silicon dioxide colloid 1 mg, magnesium stearate 1 mg.

Description:Tablets of light yellow or yellow color, round, flat-cylindrical with a bevel.

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:

Nonsteroidal anti-inflammatory drug (NSAID), has anti-inflammatory, analgesic, antipyretic and antiplatelet effect.Selectively inhibits cyclooxygenase-2 (COX2), which inhibits the synthesis of prostaglandins in the focus of inflammation and in the hypothalamus; has a less pronounced inhibitory effect on cyclooxygenase-1 (COX1) (rarely causes side effects associated with the inhibition of prostaglandin (SG) synthesis in healthy tissues); suppresses the release of histamine, inhibits the synthesis of interleukin-6 and urokinase. The drug suppresses the aggregation of platelets and has antioxidant properties.

Pharmacokinetics:

Suction

Absorption when ingested - high (eating intake reduces the rate of absorption, without affecting its degree). The dose change does not affect the degree of binding. The maximum concentration in the blood plasma is reached after 1.5-2.5 h.

Distribution

The connection with plasma proteins is 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acid alpha 1-glycoproteids - 1%. The maximum concentration in the blood plasma is 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.

Metabolism

Metabolized in the liver by tissue monooxygenases. The main metabolite is 4-hydroxynimidesulide (25%), has similar pharmacological activity, but due to the decrease in the size of the molecules it is able to rapidly diffuse along the hydrophobic channel of COX2 to the active binding site of the methyl group.

Excretion

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, etc.).

The half-life of Nimesulide (T1 / 2) is about 1.56-4.95 hours, 4-hydroxynimidesulide is 2.89-4.78 hours. 4-Hydroxynimidesulide is excreted by the kidneys (65%) and bile (35%), is enterohepatic recycling.

Indications:

- rheumatoid arthritis;

- articular syndrome in rheumatic diseases and gout;

- ankylosing spondylitis (Bekhterev's disease);

- osteoarthrosis, synovitis, tendonitis, tendovaginitis, bursitis;

- pain syndrome of various genesis (headache, algodismenorea, post-traumatic pains);

pain in the spine, neuralgia, myalgia, traumatic inflammation of soft tissues and the musculoskeletal system.

It is intended for symptomatic therapy, reducing pain and inflammation at the time of use.

Contraindications:

- hypersensitivity to nimesulide and other NSAIDs;

complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs;

erosive and ulcerative lesions of the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding, cerebrovascular or other bleeding, inflammatory bowel disease (Crohn's disease, ulcerative colitis) during the exacerbation phase;

hemophilia and other disorders of blood coagulability;

- decompensated chronic heart failure; period after aortocoronary bypass surgery,

- hepatic insufficiency or any active liver disease, hepatotoxic reactions when using nimesulide in a history, concomitant use of potentially hepatotoxic substances;

- severe chronic renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia;

- pregnancy,

- lactation period,

- children under 12 years.

Carefully:

Coronary heart disease, cerebrovascular diseases, chronic heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, kidney failure (creatinine clearance 30-60 ml / min), anamnestic data on the development of gastrointestinal ulcer, infection Helicobacter pylori, old age, prolonged use of NSAIDs, alcoholism, severe somatic diseases, concomitant therapy with the following drugs: anticoagulants (incl. warfarin), antiplatelet agents (incl. acetylsalicylic acid, clopidogrel), oral glucocorticosteroids, selective serotonin reuptake inhibitors (incl. citalopram, fluoxetine, paroxetine, sertraline).

Pregnancy and lactation:

The drug is contraindicated in pregnancy.

If you need to take the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

The dosage regimen is selected individually, taking into account the severity of the condition.

For adults, take 1 tablet 2 times a day. The maximum daily intake for adults is 200 mg.

Tablets are taken orally after a meal with enough water.

For children over the age of 12 years (with a body weight of more than 40 kg), the drug is prescribed in a single dose at a rate of 1.5 mg / kg body weight, but not more than 200 mg / day (100 mg 2 times / day).

A minimum effective dose should be used with the minimum possible short course.

Side effects:

The incidence of adverse reactions listed below was determined according to the following (World Health Organization classification): very often more than 1/10; often from more than 1/100 to less than 1/10; infrequently - from more than 1/1000 to less than 1/100; rarely from more than 1/10000 to less than 1/1000; very rarely - less than 1/10000, including individual messages.

From the gastrointestinal tract: often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, stomatitis, tarry stool, gastrointestinal bleeding, ulceration of the mucous membrane of the stomach or duodenum.

From the side of the central nervous system: infrequently - dizziness; rarely - a sense of fear, nervousness, nightmarish dreams; very rarely - headache, drowsiness, encephalopathy (Rein's syndrome).

On the part of the respiratory system: infrequently - shortness of breath, very rarely - bronchial asthma, bronchospasm.

From the side of the cardiovascular system: infrequently - arterial hypertension; rarely - tachycardia, hemorrhages, "hot flashes".

From the senses: rarely - blurred vision, very rarely - dizziness. Skin and mucous membranes: infrequently - itching, rash, increased sweating; rarely - erythema, dermatitis; very rarely: urticaria, angioedema, facial swelling, multi-form exudative erythema, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

Liver and bile excretory system: often - increased hepatic transaminases, very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis.

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

From the hemopoietic system: rarely - anemia, eosinophilia; very rarely - thrombocytopenia, pancytopenia, purpura, lengthening of hematopoiesis.

Allergic reactions: rarely - hypersensitivity reactions; very rarely anaphyllactoid reactions

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

Overdose:

In case of an overdose, it is possible to disturb kidney function, increase blood pressure, develop hepatotoxicity (skin itch, yellowing of the skin, nausea, vomiting).

Treatment: should stop taking the drug, carry out symptomatic therapy with gastric lavage and the use of activated charcoal.

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.

The efficacy and toxicity of many drugs can be increased with concomitant administration with nimesulide, due to the competitive displacement of nimesulide from the sites of binding to plasma proteins and the increase of their free fraction in the blood (pharmacokinetic interaction).

Nimesulide may increase the possibility of side effects while taking with methotrexate.

The level of lithium in the blood plasma increases with simultaneous reception of lithium and nimesulide preparations.

Because of the high degree of binding of nimesulide to plasma proteins,simultaneously taking hydantoin and sulfonamides, should be under the supervision of a doctor, passing the examination at short intervals.

Nimesulide can enhance the action of cyclosporin on the kidneys.

The use of nimesulide in conjunction with glucocorticoids, serotonin reuptake inhibitors increases the risk of developing gastrointestinal bleeding.

Special instructions:

Caution should be given to patients with ischemic heart disease, high blood pressure, cerebrovascular disease.

Nimesulide should be taken with caution to patients who have a tendency to bleeding, patients with diseases of the upper gastrointestinal tract 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 urinary excretion.

With prolonged use, it is necessary to monitor the function of the kidneys, when using the drug for more than two weeks, it is necessary to monitor the indicators of liver function (hepatic transaminases).

If there are signs of hepatotoxicity (itchy skin, yellowing of the skin, nausea, vomiting, abdominal pain, darkening of urine, increased activity of "liver" transaminases), stop taking the drug.

Do not take nimesulide concurrently with other NSAIDs.

Nimesulide can alter the properties of platelets, but does not replace the preventive effect of acetylsalicylic acid in diseases of the cardiovascular system. The use of nimesulide may adversely affect female fertility and is not recommended for women planning a pregnancy.

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

Effect on the ability to drive transp. cf. and fur:As nimesulide when ingested may cause drowsiness and dizziness, the drug should be administered with caution to patients with activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets of 100 mg.

10 tablets per contour cell package; by 1,2 or 3 contour squares with instructions for medical use in a pack of cardboard.

For 30 or 100 tablets in a can of polymer with a lid. Each bank, together with instructions for medical use, is placed in a cardboard pack.

Packaging:(1) / 10 tablets per contour mesh package, 1 circuit cell pack together with instructions for the medical use of the preparation in a pack of cardboard / - A pack of cardboard (10) - a contour mesh box made of polyvinylchloride film and foil of aluminum printed lacquered
(10) - a contoured cell pack of a polyvinylchloride film and foil of aluminum printed lacquered (2) / 10 tablets per contour cell package, 2 circuit packs together with instructions for medical use of the drug in a pack of cardboard / - A pack of cardboard
(10) - a contoured cellular package made of polyvinylchloride film and foil of aluminum printed lacquered (3) / 10 tablets per contour cell package, 3 contiguous cellular packs along with instructions for medical use of the preparation in a pack of cardboard / - A pack of cardboard
(100) - a can of polymeric materials with a lid for packaging medicines (1) / 100 tablets per can of polymeric materials,1 jar along with instructions for medical use of the drug in a pack of cardboard / - A pack of cardboard
(30) - a can of polymeric materials with a lid for packaging medicines (1) / 30 tablets per can of polymeric materials, 1 jar along with instructions for medical use of the drug in a pack of cardboard / - A pack of cardboard

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children!

Shelf life:

2 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-001620

Date of registration:02.04.2012

The owner of the registration certificate:Berezovsky Pharmaceutical Plant, ZAO Berezovsky Pharmaceutical Plant, ZAO Russia

Manufacturer: & nbsp

Berezovsky Pharmaceutical Plant, ZAO Russia

Information update date: & nbsp14.08.2015

Illustrated instructions

Instructions

Nimesulide (Nimesulid)