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

Nimesulide refers to NSAIDs whose mechanism of action is associated with selective inhibition of cyclooxygenase-2 (COX-2) and effects on a number of other factors: suppression of the platelet activation factor, tumor necrosis factor alpha, inhibition of proteinases and histamine. Selectively inhibiting COX-2, decreases the biosynthesis of prostaglandins in the inflammatory focus, has a less pronounced inhibitory effect on COX-1 (less often causes side effects associated with the inhibition of prostaglandin synthesis in healthy tissues).

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.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 origin,

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

- pain syndrome of various genesis (including in the postoperative period, with trauma, algodismenorea, toothache, headache, arthralgia, lumbar ligation).

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:

- erosive and ulcerative changes in the gastric and duodenum mucosa;

- inflammatory bowel disease in the phase of exacerbation;

- active gastrointestinal bleeding;

- expressed violations of the liver and / or kidney function, severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease;

- severe hepatic impairment or active liver disease;

- pregnancy and lactation;

- children's age till 12 years;

- hypersensitivity to nimesulide and drug components;

- severe heart failure;

- severe blood clotting disorders;

- confirmed hyperkalemia;

- period after aortocoronary shunting;

- anamnestic data on an attack of bronchial obstruction, rhinitis, urticaria after taking acetylsalicylic acid or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome - rhinosinusitis, urticaria, polyps nasal mucosa, asthma).

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 inside (body weight over 40 kg) appoint 1 tablet 2 times a day.

Tablets are taken after meals with enough water. Maximum

daily dose of 5 mg / kg.

Patients with chronic renal failure require a reduction in the daily dose to 100 mg.

Course of treatment: as directed by a doctor.

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 stools, gastroepithelial 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 - bronchospasm; possibly exacerbation of bronchial asthma.

The cardiovascular system: infrequently - arterial hypertension; rarely - tachycardia, hemorrhages, "hot flashes".

Sense organs: rarely - blurred vision.

Skin and mucous membranes: infrequently - itching, rash, increased sweating; rarely: erythema, dermatitis.

Liver and biliary system: often - increased activity of "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.

Hematopoiesis: rarely - anemia, eosinophilia; very rarely - thrombocytopenia, pancytopenia, purpura, prolonged bleeding time.

Allergic reactions: rarely - hypersensitivity reactions; very rarely - anaphylactoid reactions, urticaria, angioedema, edema of the face, multiform exudative erythema, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome)

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. Gastrointestinal can occur bleeding, arterial hypertension, acute renal failure, respiratory depression.

Treatment: requires symptomatic treatment 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 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 increases the onset of side effects while taking methotrexate.

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

Nimesulide can enhance the nephrotoxic effect of cyclosporin on the kidneys. Use with glucocorticosteroids, serotonin reuptake inhibitors increases the risk of developing bleeding in the gastrointestinal tract.

Special instructions:

Nimulide should be used with caution in patients who have a tendency to bleed, patients with upper gastrointestinal disease or patients receiving anticoagulants. Since Nimulid partially excreted by the kidneys, its dosage for patients with impaired renal function should be reduced, depending on the creatinine clearance values.

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.

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.

Effect on the ability to drive transp. cf. and fur:Patients who have side effects: dizziness, drowsiness, blurred vision,care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets of 100 mg.

For 10 tablets in a blister of PVC / aluminum foil.

For 3 or 10 blisters in a cardboard box along with instructions for use.

Packaging:(10) - packings cellular planimetric (10) - packs cardboard
(10) - packings, cellular, outline (3) - packs, cardboard

Storage conditions:

Store at temperature 15-25 ° C, in a dry and protected from light place. Keep out of the reach of children.

Shelf life:5 years. Do not use the drug with expired shelf life.

Terms of leave from pharmacies:On prescription

Registration number:П N011525 / 02

Date of registration:09.06.2009

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)