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

sodium methylparahydroxybenzoate, sodium propylparahydroxybenzoate, potassium sorbate, croscarmellose sodium, silicon dioxide colloid, magnesium stearate, orange flavor.

Description:Round, biconvex tablets are pale yellow.

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:

Nimulide is a non-steroidal anti-inflammatory drug (NSAID) from the sulfonanilide class.

Nimesulide belongs to a new generation of NSAIDs whose mechanism of action is related to the selective inhibition of cyclooxygenase-2 (COX-2), an enzyme involved in the synthesis of prostaglandins, mediators of edema, inflammation and pain, and an impact on a number of other factors: suppression of the platelet activation factor, tumors alpha, suppression of proteinases and histamine. 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. FROM_max - 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. Well penetrates into acid environment of the inflammation 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 (sulphation, 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%), 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 origin,

- inflammation of ligaments, tendons, bursitis, including post-matmatic inflammation of soft tissues,

pain syndrome of various genesis (including in the postoperative period, with trauma, algodismenorea, toothache, headache, arthralgia, lumboeishalgia),

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 to the active substance or ancillary components;

- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including in the anamnesis);

- erosive and ulcerative changes in the mucosa of the stomach or duodenum, active gastrointestinal bleeding; cerebrovascular or other bleeding;

- inflammatory bowel disease (ulcerative colitis, Crohn's disease) in the phase of exacerbation;

- hemophilia and other bleeding disorders;

-decompensated heart failure,

-hepatic insufficiency or any active liver disease,marked renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia;

-period after aortocoronary shunting;

-Birth, the period of breastfeeding,

-Children under 12 years of age;

- anamnestic data on the development of hepatotoxic reactions with the use of nimesulide preparations;

- concomitant use of potentially hepatotoxic substances;

alcoholism, drug addiction.

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)

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

Dosing and Administration:

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

Adults and children over 12 years of age (body weight over 40 kg): Nimulide is usually given orally at a dose of 100 mg (1 tablet) 2 times a day at the end or after meals. The tablet should be put on the tongue, where it immediately begins to dissolve. Swallow the saliva in which the tablet dissolved.

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, heartburn; 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, swelling titti multi-form 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, leukopenia, eosinophilia; very rarely - thrombocytopenia, pancytopenia, purpura, prolonged bleeding time.

Allergic reactions: 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 clotting 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:

Nimulide should be used with caution in patients who have a tendency to bleeding, 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 the tissues, so patients with high blood pressure and with cardiac abnormalities Nimulide should be used with extreme caution. Patients should undergo regular medical supervision if they take medication along with nimesulide, which are characterized by an effect on the gastrointestinal tract.

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.

If there are signs of liver damage (skin itching, yellowing of the skin, nausea, vomiting, abdominal pain, darkening of urine, increased level of "liver" transaminases), stop taking the drug and consult a doctor. Do not use the drug simultaneously with other NSAIDs. The drug can alter the properties of platelets, but does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.After 2 weeks of using the drug, it is necessary to monitor the indicators of liver function ("transaminase").

Effect on the ability to drive transp. cf. and fur:Patients whose work activity requires concentration (constant attention), should be aware that the drug may cause drowsiness or dizziness.

Form release / dosage:

Tablets for resorption 100 mg.

For 10 tablets in a blister made of polyvinylchloride and aluminum foil. For 1 or 2 blisters in a cardboard box together with instructions for use.

Packaging:(10) - blisters (1) - packs of cardboard
(10) - blisters (2) - packs cardboard

Storage conditions:Store at a temperature not exceeding 25 ⁰ C, in a dry, dark place. Keep out of the reach of children.

Shelf life:3 years. Do not use the product after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011525 / 03

Date of registration:08.04.2009

The owner of the registration certificate:Panacea Biotech Co., Ltd.Panacea Biotech Co., Ltd. India

Manufacturer: & nbsp

PANACEA BIOTEC, Ltd. India

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

Information update date: & nbsp15.08.2015

Illustrated instructions

Instructions

Nimoolid (Nimulid)