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Active ingredients
Nimesulide
Release form
Gel
Composition
Each tablet contains: Active ingredient: Nimesulide 100 mg. Excipients: calcium hydrophosphate 75 mg, cellulose microcrystalline (type 114) 40 mg, corn starch 54 mg, sodium carboxymethyl starch 35 mg, magnesium stearate 3 mg, colloidal silicon dioxide 2 mg, talc 1 mg.
Pharmacological effect
1. Nimesulide is a nonsteroidal anti-inflammatory agent (NSAID) from the sulfonanilide class, it has analgesic, anti-inflammatory and antipyretic effects. The effect is due to the selective blocking of cyclooxygenase-2, as well as a number of other mechanisms, such as: suppressing the synthesis of platelet activating factor, reducing the production of superoxide anion stimulated by polymorphonuclear leukocytes by suppressing type IV protein kinase and phosphodiesterase IV. Prevention of bradykinin and cytokine-induced hyperalgesia by inhibiting the release of tumor necrosis factor a. , Neutralization of hypochlorous acid, Prevention of inactivation of α-proteinase inhibitors, Inhibition of proteases (including ellastase, collagenases), Inhibition of histamine release from basophils and mast cells, Slowing degradation of cartilage matrix by inhibiting the synthesis of metalloproteases. 2. Menthol has a local irritant, analgesic, distracting, antipruritic, antiseptic, soothing effect. The effect is mainly due to reflex reactions associated with the stimulation of sensitive nerve endings: stimulation of the receptors of the skin or mucous membranes stimulates the formation and release of endogenous biologically active substances (enkephalins, endorphins, peptides, kinins) involved in the regulation of pain, vascular permeability and other processes , providing anesthetic, distracting and antipruritic action. Antiseptic activity is manifested indiscriminate lesion of microbial cells. Irritant (distracting) effect helps to reduce pain. Local action is accompanied by a narrowing of blood vessels, a feeling of cold, turning into a feeling of light burning and pricking.Skin-visceral reflexes (reflex arc does not affect the brain) improve tissue trophism (according to the zones of innervation). Reflexively changes the tone of blood vessels, both superficial and deeply located in the tissues and internal organs. 3. Capsaicin has an effect by reducing the content of substance P, which is a neurotransmitter, which conducts reactions of pain and itching from receptors of the peripheral nervous system to the central one. Capsaicin blocks the synthesis and transfer of substance P through the neuron, which leads to a decrease in the intensity of the pain impulse. 4. Methyl salicylate is a derivative of salicylic acid. When local application quickly penetrates into the deeper layers of the skin, is absorbed, hydrolyzed and converted into the anion of salicylic acid. Non-selectively inhibits cyclooxygenase, reduces the synthesis of prostaglandins responsible for inflammation, pain, fever. Normalizes the increased permeability of capillaries, improves microcirculation processes, reduces swelling and infiltration of inflamed tissues, causes a decrease in pain in the pathology of joints, muscles and soft tissues. It has a local irritant effect on the skin, which helps to reduce pain.
Pharmacokinetics
Nimesulide: according to international studies, the maximum concentration of nimesulide in the blood plasma after a single topical application at a dose of 200 mg is observed 24 hours after application and reaches 9. 77 ng / ml. Metabolized in the liver. No traces of the main metabolite of nimesulide, 4-hydroxynimesulide, were detected in plasma. With prolonged use, the concentration of nimesulide on day 8 was 37. 25 + 13. 25 ng / ml, which is 100 times less than when taken orally in an average daily dose (200 mg / day). Due to insignificant systemic absorption, there are no data on the pharmacokinetics of the other active ingredients when applied topically.
Indications
Rheumatoid arthritis, rheumatoid arthritis and psoriasis; inflammation of soft tissues and musculoskeletal system (injuries and tears of ligaments, bruises), pain syndrome of various origins (in t, h, in the postoperative period, with injuries, shift, toothache, headache).
Contraindications
Erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, bleeding from the gastrointestinal tract, aspirin triad, abnormal liver function, severe renal failure, dermatosis, damage to the epidermis, skin infections in the area of application (for the gel), children up to 2 years. Hypersensitivity to nimesulide and other components of the drug, acetylsalicylic acid and other NSAIDs. Caution should be given to the drug for hypertension, heart failure, type 2 diabetes (insulin-independent).
Precautionary measures
If irritation occurs, use of the gel should be discontinued and appropriate treatment should be prescribed. Do not apply the gel on the eyes, mucous membranes, skin areas with open lesions, dermatosis or infectious lesions. During application, an intense burning sensation may occur, which disappears within a few days. Do not touch sensitive skin areas during the procedure and before cleansing the hands of the remnants of the drug. The gel should be used with caution in patients at risk of developing adverse reactions caused by salicylates.
Use during pregnancy and lactation
Nimesulide is not used in pregnant and lactating women. Studies confirming its effectiveness and safety during pregnancy and lactation have not been conducted. There is no data on the impact on the development of the fetus.
Dosage and administration
Before applying the gel, wash and dry the skin. A gel column with a length of about 3 cm is applied to the area of maximum pain, rubbing with a uniform thin layer (not rubbed) 3-4 times a day. The maximum dose - 5 mgkg mass Telasut. The duration of the drug is 10 days.
Side effects
Local reactions: itching, urticaria, peeling, transient discoloration of the skin (not requiring discontinuation of the drug). If any adverse reactions occur, discontinue use of the drug and consult a doctor. When applying the gel to large areas of skin or with prolonged use, the development of systemic adverse reactions is possible: heartburn, nausea, vomiting, diarrhea, gastralgia, ulceration of the gastrointestinal mucosa, increased activity of liver transaminases. headache, dizziness.fluid retention, hematuria. allergic reactions (anaphylactic shock, skin rash). thrombocytopenia, leukopenia, anemia, agranulocytosis, prolongation of bleeding time.
Overdose
Cases of overdose with local use have not been described. When applied more than 50 g on large areas of skin, overdose may develop (systemic adverse reactions). Recommended treatment to the doctor. There are no specific antidotes.
Interaction with other drugs
The effect of drugs that reduce blood clotting, increases with their simultaneous use with nimesulide. Nimesulide may reduce the effects of furosemide. Nimesulide may increase the possibility of side effects while taking methotrexate. The level of lithium in plasma increases while taking drugs of lithium and nimesulide. Nimesulide may enhance the effect of cyclosporine on the kidneys. Use with glucocorticosteroids, serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.
special instructions
Do not apply the gel around the eyes, on the mucous membranes, on healthy parts of the body, on the wound surfaces. Do not use with dermatitis. Do not touch the sensitive areas of the skin with your hands with the gel. Avoid using gel with air-tight dressings. After applying the gel, wash your hands with soap and water. After a complete rubbing of the drug can be observed redness, burning. These symptoms usually disappear within a few days after discontinuation of the drug. It should be used with caution in patients with an increased risk of side effects associated with taking salicylates. Pediatric use: Indications and recommendations for use in children are not known. Effect of use in drivers and workers associated with the mechanisms: Patients taking nimesulide orally should be warned about its side effect - dizziness. Use with caution while driving and working. No cases of dizziness after topical administration of nimesulide have been described. Mutagenicity and carcinogenicity: In various studies, nimesulide was not a mutagenic drug. There is also no data on the effect of the drug on the chromosomes of lymphocytes in vitro, and the interaction with H-thymidine of cultured human lymphocytes.Pediatric use: Indications and recommendations for use in children are not known. Effect of use in drivers and workers associated with the mechanisms: Patients taking nimesulide orally should be warned about its side effect - dizziness. Use with caution while driving and working. No cases of dizziness after topical administration of nimesulide have been described. Mutagenicity and carcinogenicity: In various studies, nimesulide was not a mutagenic drug. There is also no data on the effect of the drug on the chromosomes of lymphocytes in vitro, and the interaction with H-thymidine of cultured human lymphocytes.