More info
Active ingredients
Nimesulide
Release form
Pills
Composition
Active ingredient: Nimesulide (Nimesulidum) Concentration of the active substance (mg): 100
Pharmacological effect
Nimulid is a NSAID of the sulfonalide class. It has anti-inflammatory, analgesic and antipyretic effects. Nimesulide refers to NSAIDs, the mechanism of action of which is associated with selective inhibition of cyclooxygenase-2 (COX-2) and effects on a number of other factors: suppression of platelet activating factor, tumor necrosis factor alpha, suppression of proteinases and histamine. Selectively suppressing COX-2, reduces the biosynthesis of prostaglandins in the inflammation, has a less pronounced inhibitory effect on COX-1 (rarely causes side effects associated with inhibition of the synthesis of prostaglandins in healthy tissues).
Pharmacokinetics
Oral absorption is high (food intake decreases the rate of absorption without affecting its degree). Plasma protein binding - 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acid alpha1-glycoproteins - 1%. Changing the dose does not affect the degree of binding. Cmax - 3.5-6.5 mg / l. Vd - 0.19-0.35 l / kg. It penetrates the tissue of the female genital organs, where, after a single dose, its concentration is about 40% of the concentration in plasma. It penetrates well into the acidic environment of the focus of inflammation (40%), synovial fluid (43%). Easily penetrates histohematogenous barriers. Metabolized in the liver by tissue monooxygenases. The main metabolite, 4-hydroxynimesulide (25%), has similar pharmacological activity, but due to a decrease in the size of molecules, it is able to quickly diffuse through the hydrophobic channel of COX-2 to the active binding site of the methyl group. 4-hydroxynimesulide is a water-soluble compound, which does not require glutathione and conjugation reactions of the second phase of metabolism (sulfation, glucuronation, etc.) for nitride. T1 / 2 nimesulide - about 1.56–4.95 h, 4-hydroxyminesulide - 2.89–4.78 parts excreted by the kidneys (65%) and with bile (35%), undergoes 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 nimesulide profile does not change significantly.
Indications
- rheumatoid arthritis; - articular syndrome with exacerbation of gout; - psoriatic arthritis; - ankylosing spondyloarthritis, osteochondrosis with radicular syndrome; - osteoarthrosis; - pain syndrome of various genesis (including in the postoperative period, with injuries, algomenorrhea, toothache, headache, arthralgia, lumboischalgia); - symptomatic therapy to reduce pain and inflammation at the time of use. use, the progression of the disease is not affected.
Contraindications
- erosive and ulcerative changes of the mucous membrane of the stomach and duodenum, including inflammatory bowel disease in the acute phase; active gastrointestinal bleeding; severe liver and / or kidney dysfunction; severe renal failure (creatinine clearance less than 30 ml / min); progressive kidney disease; severe heart failure; severe clotting disorders blood; —confirmed hyperkalemia; —a period after coronary artery bypass surgery; —anamnestic data on an attack of broncho-obstruction, rhinitis, urticaria, after taking acetylsalicylic acid or otherwise NSAIDs (complete or incomplete intolerance to acetylsalicylic acid - rhinosinusitis, urticaria, nasal mucous polyps, asthma); severe hepatic insufficiency or active liver disease; pregnancy; lactation; components of the drug.
Precautionary measures
Do not exceed recommended doses. With caution: coronary heart disease, cerebrovascular diseases, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral artery disease, smoking, creatinine clearance less than 60 ml / min, anamnestic data on the development of gastric ulcer, infection Helicobacter pylori, old age, long-term use of NSAIDs, frequent use of alcohol, severe somatic diseases, concomitant therapy with the following drugs: - anticoagulants (for example, warfarin); - antiplatelet agents (for example, acetylsalicylic acid, clopidogrel); - oral GCS (for example, prednisolone); - selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).
Use during pregnancy and lactation
The drug is contraindicated in pregnancy and lactation.
Dosage and administration
Adults and children over 12 years old (body weight more than 40 kg) are prescribed 1 tab. 2 times / day. Tablets are taken after a meal with a sufficient amount of water. The maximum daily dose is 5 mg / kg. Patients with chronic renal failure require a reduction in the daily dose to 100 mg. Treatment course: prescribed by a doctor.
Side effects
On the part of the digestive system: often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, stomatitis, tarry stools, gastrointestinal bleeding, ulcers and / or perforation of the stomach or duodenum. On the CNS side: infrequently - dizziness; rarely - a feeling of fear, nervousness, nightmares; very rarely - headache, drowsiness, encephalopathy (Reye's syndrome). On the part of the respiratory system: infrequently - shortness of breath; very rarely - bronchospasm; possible exacerbation of bronchial asthma. From the side of the cardiovascular system: rarely - arterial hypertension; rarely - tachycardia, hemorrhages, hot flushes. Sensory organs: rarely - blurred vision. From the skin and mucous membranes: rarely - itching, rash, increased sweating; rarely - erythema, dermatitis. From the side of the liver and biliary system: often - increased activity of hepatic transaminases; very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis. On the urinary system: rarely - edema; rarely - dysuria, hematuria, urinary retention, hyperkalemia; very rarely - renal failure, oliguria, interstitial nephritis. On the side of the hematopoietic system: rarely - anemia, eosinophilia; very rarely, thrombocytopenia, pancytopenia, purpura, prolongation of bleeding time. Allergic reactions: rarely - hypersensitivity reactions; very rarely - anaphylachidic reactions, urticaria, angioedema, swelling of the face, erythema multiforme, including exudative erythema. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome). General reactions: rarely - general weakness; hypothermia is very rare. In the case of other side effects not mentioned above or deterioration of your health, please contact your doctor immediately.
Overdose
Symptoms: apathy, drowsiness, nausea, vomiting.Gastrointestinal bleeding may occur, arterial hypertension, acute renal failure, respiratory depression. Treatment: symptomatic treatment of the patient is required, there is no specific antidote. If an overdose occurred during the last 4 hours, it is necessary to induce vomiting, to receive activated carbon (60-100 g per adult), osmotic laxatives. Forced diuresis, hemodialysis are ineffective due to the high association of the drug with proteins.
Interaction with other drugs
The effect of drugs that reduce blood clotting, increases with their simultaneous use with nimesulide. Nimesulide may reduce the effect of furosemide. Reduces the therapeutic effect of antihypertensive drugs. Nimesulide increases the onset of side effects while taking methotrexate. The level of lithium in plasma increases while taking drugs of lithium and nimesulide. Nimesulide may enhance the nephrotoxic effect of cyclosporine on the kidneys. Use with glucocorticosteroids, serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.
special instructions
Nimulid should be used with caution in patients who have a tendency to bleed, patients with diseases of the upper gastrointestinal tract or patients receiving anticoagulants. Considering reports of visual impairment in patients taking other NSAIDs, treatment should be immediately stopped if any visual impairment occurs and the patient should examine the oculist. The drug can cause fluid retention in the tissues, so patients with high blood pressure and cardiac disorders Nimulid should be used with extreme caution. To reduce the risk of adverse events from the gastrointestinal tract, you should use the minimum effective dose of the minimum possible short course. Influence on ability to drive motor transport and control mechanismsPatients who have side effects: dizziness, drowsiness, blurred vision , care must be taken when driving motor vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.