Actasulide - instructions for use, analogs, testimonials and release forms (100 mg tablets) of the drug for the treatment of headache and toothache, arthrosis, arthritis, menstrual pain in adults, children and pregnancy. Composition and alcohol

In this article, you can read the instructions for using the drugAktasulid. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Actasulide in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Actasulide in the presence of existing structural analogues.The use for the treatment of headache, toothache, arthritis, arthritis, menstrual pain in adults and children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

Actasulide - Non-steroidal anti-inflammatory drug (NSAID) from the class of sulfon-anilides. It is a selective competitive inhibitor of cyclooxygenase-2 (COX-2) - an enzyme involved in synthesis of prostaglandins - mediators edema, inflammation and pain. Has anti-inflammatory, analgesic and pronounced antipyretic effect.

To a small extent it acts on COX 1, practically preventing the formation of PGE2 from arachidonic acid under physiological conditions, thereby reducing side effects of the drug. It demonstrated that Nimesulide (active drug substance Aktasulid) able to inhibit the synthesis of IL-6 and urokinase, thereby preventing the destruction of cartilage. 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.

Composition

Nimesulide + excipients.

Pharmacokinetics

Absorption when ingested is high. Eating lowers the absorption rate without affecting its degree. The maximum concentration in the blood plasma is achieved after 1.5-2.5 hours. Binding to plasma proteins - 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. 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. In patients with renal insufficiency, as well as in children and the elderly, the pharmacokinetic profile of nimesulide does not change significantly.

Indications

• rheumatoid arthritis;
• osteoarthritis;
• arthritis of various etiologies;
• arthralgia;
• myalgia;
• postoperative and post-traumatic pain;
• bursitis;
• tendonitis;
• algodismenorea;
• toothache and headache.

Forms of release

Tablets of 100 mg.

Instructions for use and dosing regimen

Inside, 1 tablet (100 mg) 2 times a day. Tablets are taken with a sufficient amount of water, preferably before meals. If there are diseases of the digestive tract, it is advisable to take the drug at the end of the meal or after eating.

Children over 12 years are prescribed from the calculation of a single dose of 1.5 mg per kilogram 2-3 times a day, the maximum daily dose of the drug - 5 mg per kilogram. Adolescents with a body weight above 40 kg - 100 mg not more than 2 times a day.

Side effect

• diarrhea;
• nausea, vomiting;
• constipation;
• flatulence;
• gastritis (inflammation of the gastric mucosa);
• stomach ache;
• stomatitis (inflammation of the oral mucosa);
• gastrointestinal bleeding;
• ulcer or perforation of the stomach, duodenum;
• dizziness;
• a sense of fear;
• nervousness;
• headache;
• drowsiness;
• dyspnea;
• bronchial asthma;
• bronchospasm;
• arterial hypertension;
• tachycardia (increased heart rate);
• hemorrhage (hemorrhage);
• blurred vision;
• itching;
• rash;
• increased sweating;
• edema;
• retention of urine;
• impaired kidney function;
• anemia;
• eosinophilia (absolute or relative increase in the number of eosinophils);
• hypersensitivity reactions;
• general weakness;
• low temperature.

Contraindications

• hypersensitivity;
• erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation);
• bleeding from the digestive tract;
• intracranial hemorrhages;
• "aspirin" asthma;
• liver failure;
• renal failure (QC less than 30 ml / min);
• severe heart failure;
• pregnancy;
• lactation period;
• children's age (up to 12 years).

Carefully:

• arterial hypertension;
• heart failure;
• diabetes mellitus type 2.

Application in pregnancy and lactation

Actasulide is contraindicated during pregnancy and lactation.

Use in children

Actasulide is contraindicated in children under 12 years of age.

special instructions

Actasulide should be used with caution in patients with a tendency to bleeding, patients with upper gastrointestinal disorders or patients receiving medications that reduce blood clotting, or drugs that inhibit platelet aggregation.

Since Aktasulid is partially excreted by the kidneys, the dose 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 Actasulide should be used with extreme caution. Patients should undergo regular medical supervision if they take drugs alongside with Actasulide that affect the gastrointestinal tract.

It is not recommended to use the drug Aktasulid together with alcohol because of the increased risk of developing bleeding in the gastrointestinal tract.

Impact on the ability to drive vehicles and manage mechanisms

Patients whose work requires concentration (constant attention) should be aware that the drug may cause drowsiness or dizziness.

Drug Interactions

The effect of drugs that reduce blood coagulability, increases with their simultaneous use with nimesulide.

Actasulide may reduce the action of furosemide.

Nimesulide may increase the chance of side effects while taking 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.

Analogues of the drug Actasulide

Structural analogs for the active substance:

• Amoeolin;
• Aponil;
• Aulin;
• Mesulide;
• Nyz;
• Nysulid;
• Nemux;
• Nimegesic;
• Nimesan;
• Nimesil;
• Nimesulide;
• Nimika;
• Nimulid;
• Novolide;
• Prolid;
• Sulaydine;
• Fllolid.

Analogues for the pharmacological group (other non-narcotic analgesics, including non-steroidal and other anti-inflammatory drugs):

• Arthro-Active;
• Arthrodarin;
• Артрокер;
• Arthrofoon;
• Askalcin;
• Broxinac;
• Bronflex;
• Wobenzym;
• Galavit;
• Diartrin;
• Diaflex;
• Iflubene;
• Catadolone;
• Naqvan;
• Neurodolone;
• Nifluryl;
• Nolodates;
• Oxadol;
• Oralcept;
• Pirabutol;
• Relaphene;
• Remidon;
• Reopyrin;
• Tantum;
• Tysol;
• Falimint;
• Phlogenzyme;
• Flugesic;
• Citralgin.

Response of a therapist

Aktasulid is an effective medicament, which allows you to quickly remove pain from arthrosis and arthritis, algodismenore (painful periods). The drug helps to ease the condition of postoperative patients, as well as people with post-traumatic pain. Excellent removes headache and toothache. The peculiarity of Actasulide is that it belongs to selective non-steroidal anti-inflammatory drugs, in comparison with non-selective, its negative effect on the gastrointestinal tract is minimal, and therefore the side effects from taking the drug are significantly less.

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