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

Lactose monohydrate 50.00 mg, corn starch 216.39 mg, methyl parahydroxybenzoate 0.60 mg, propyl parahydroxybenzoate 0.010 mg, crospovidone (collidone C1) 13.00 mg, talc 4.00 mg, magnesium stearate 1.00 mg.

Description:Flat triangular shaped tablets with beveled edges of light yellow color with a risk on one side.

Pharmacotherapeutic group:Non-steroidal 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 sulfonanilides.It is a selective competitive inhibitor of cyclooxygenase-2 (COE-2), an enzyme involved in the synthesis of prostaglandins, mediators of edema, inflammation and pain. Has anti-inflammatory, analgesic and antipyretic effect.

Reversibly inhibits the formation of prostaglandin E2, both in the focus of inflammation, and in the ascending pathways of the nociceptive system, including ways of carrying painful spinal cord impulses.

Reduces the concentration of short-lived prostaglandin H2, from which prostaglandin isomerase produces prostaglandin E2. A decrease in the concentration of prostaglandin E2 leads to a decrease in the degree of activation of prostanoid EP receptors, which is manifested in analgesic and anti-inflammatory effects.

Has little effect on COX-1, practically without interfering with the formation of prostaglandin E2 from arachidonic acid under physiological conditions, thereby reducing the side effects of the drug.

The drug also suppresses platelet aggregation by inhibiting the synthesis of endoperoxides and thromboxane A2, inhibits the synthesis of platelet aggregation factor, inhibits the activation of plasminogen by increasing the concentration of inhibitor-1.Suppresses the release of histamine, and also reduces the degree of bronchospasm caused by the action of histamine and acetaldehyde. Inhibits the release of tumor necrosis factor a, which causes the formation of cytokinins.

Shown, that nimesulide is able to suppress the synthesis of interleukin-6 and urokinase, thereby preventing the destruction of cartilaginous tissue. Inhibits the synthesis of metalloproteases (elastase, collagenase), preventing the destruction of proteoglycans and cartilaginous collagen.

It has antioxidant properties, inhibits the formation of toxic products of oxygen decay due to a decrease in the activity of myeloperoxidase. Interacts with glucocorticoid receptors, activating them by phosphorylation, which also enhances the anti-inflammatory effect of the drug.

Pharmacokinetics:

Absorption when ingested - high. Eating lowers the absorption rate without affecting its degree. 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-glycoproteids - 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 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 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-hydroxynimidesulide is excreted by the kidneys (65%) and with bile (35%).

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, osteoarthritis, arthritis of various etiology, arthralgia, myalgia, postoperative and post-traumatic pains, bursitis, tendenitis, algodismenorea, dental and headache.

Contraindications:

Hypersensitivity, complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid, etc.nonsteroidal antiinflammatory drugs (including history), erosive and ulcerated gastric mucosal lesions and 12 duodenal ulcer, active gastrointestinal bleeding, cerebrovascular or other bleeding, inflammatory bowel disease (Crohn's disease, ulcerative colitis) in acute phase , hemophilia and others. coagulation disorders, asthma, chronic heart failure, liver failure or any active liver disease, hepatotoxic reactions using nimesil lida a history of alcoholism, drug abuse, severe chronic renal failure (creatinine clearance less than 30 mL / min), progressive renal disease, confirmed hyperkalemia, since the aortocoronary bypass, simultaneous al. hepatotoxic drugs, pregnancy, lactation, infancy up to 12 years.

Carefully:

ischemic heart disease, cerebrovascular disease, chronic heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus,diseases of peripheral arteries, smoking, kidney 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, simultaneous administration of anticoagulants (incl. warfarin), antiplatelet agents (incl. acetylsalicylic acid, clopidogrel), oral glucocorticosteroids, selective serotonin reuptake inhibitors (incl. citalopram, fluoxetine, paroxetine, sertraline).

Dosing and Administration:

Inside, after a meal, 50-100 mg 2 times a day.

In patients with chronic liver failure, the daily dose is 100 mg. A minimum effective dose should be used with the minimum possible short course.

Children over 12 years of age are prescribed from the calculation of a single dose of 1.5 mg / kg of the child's body weight, the maximum daily dose of the drug is 5 mg / kg per day (not more than 200 mg / day).

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".

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

General reactions: 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 side effects with the simultaneous administration of methotrexate.

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:

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.It is necessary to control laboratory indicators of hepatic transaminase activity at least once a week.

Effect on the ability to drive transp. cf. and fur:Care must be taken when driving vehicles and other activities. potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets of 100 mg.

For 10, 15, 20 tablets in a blister of PVC / aluminum foil. By 1,2, 3, 4, 5, 6 or 10 blisters are placed in a cardboard box together with an instruction for use.

Packaging:(10) - packings, cellular, outline (1) - packs, cardboard
(10) - packings cellular planimetric (10) - packs cardboard
(10) - packings, cellular, outline (2) - packs, cardboard
(10) - packings, cellular, outline (3) - packs, cardboard
(10) - packings, cellular, outline (4) - packs, cardboard
(10) - packings, cellular planimetric (5) - packs cardboard
(10) - packings, cell planimetric (6) - packs cardboard
(15) - packings, cellular, planimetric (1) - packs cardboard
(15) - packings cellular planimetric (10) - packs cardboard
(15) - packings, cellular, outline (2) - packs, cardboard
(15) - packings, cellular planimetric (3) - packs cardboard
(15) - packings cellular planimetric (4) - packs cardboard
(15) - packings, cellular planimetric (5) - packs cardboard
(15) - packings, cellular, outline (6) - packs, cardboard
(20) - packings, cell planimetric (1) - packs cardboard
(20) - packings, cellular planimetric (10) - packs cardboard
(20) - packings, cellular, outline (2) - packs, cardboard
(20) - packings, cellular, outline (3) - packs, cardboard
(20) - packings cellular planimetric (4) - packs cardboard
(20) - packings, cellular planimetric (5) - packs cardboard
(20) - packings, cellular planimetric (6) - packs cardboard

Storage conditions:

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 printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001985

Date of registration:28.01.2013

The owner of the registration certificate:Shraya Life Senses Pvt. Ltd.Shraya Life Senses Pvt. Ltd. India

Manufacturer: & nbsp

SHREYA LIFE SCIENCES, Pvt.Ltd. India

Representation: & nbspSHREYA LIFE SENENSIZ Pvt.Ltd. SHREYA LIFE SENENSIZ Pvt.Ltd. India

Information update date: & nbsp14.08.2015

Illustrated instructions

Instructions

Nimesan® (Nimesan)