Remesulide

Remesulide is a medicine with antirheumatic medicinal effect. It belongs to the group of NSAIDs and has the following therapeutic properties - antipyretic, anti-inflammatory, and analgesic.

The active ingredient of the drug is the substance nimesulide. This component selectively slows down the activity of the element COX-2, and at the same time suppresses the processes of binding of PG substances inside the zone affected by inflammation.

Indications Remesulide

It is used as a substance that eliminates acute pain. It is prescribed for the treatment of signs of osteoarthritis, accompanied by pain. At the same time, it is used in women for the treatment of primary dysmenorrhea.

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Release form

The component is released in tablets - 10 pieces in a plate. In a box - 1 or 3 plates.

Pharmacodynamics

Nimesulide slows the release of the enzyme myeloperoxidase, and at the same time suppresses the formation of free oxygen radicals, while not affecting chemotaxis with phagocytosis.

The drug also suppresses the formation of tumor necrosis factor and other inflammatory agents.

Pharmacokinetics

After oral administration, nimesulide is absorbed at high speed inside the gastrointestinal tract. The values of intraplasmic Cmax are recorded after 2-3 hours. Synthesis of the substance with intraplasmic blood protein is 97.5%.

The drug is involved in intrahepatic metabolic processes; its main metabolic element is the medicinally active substance hydroxynimesulide.

Approximately 65% of the used dose of the drug is excreted in the urine, and the remaining 35% is excreted in the feces.

Dosing and administration

Remesulide should be taken orally, after meals, with some liquid. The medicine should be taken 1 tablet 2 times a day - in the morning and in the evening.

The maximum duration of use of the medication is 15 days.

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Use Remesulide during pregnancy

Remesulide should not be administered to pregnant or breastfeeding patients.

Contraindications

Main contraindications:

• use in case of intolerance associated with the drug or other NSAIDs;
• an aggravated ulcer affecting the gastrointestinal tract;
• severe disorders of blood clotting processes;
• bleeding inside the digestive system;
• severe heart failure;
• history of gastrointestinal bleeding;
• liver or kidney failure (severe);
• the presence of suspicion of the presence of a surgical disease of an acute nature;
• combination with drugs that, in theory, can provoke the development of hepatotoxic symptoms.

Side effects Remesulide

Side effects include:

• nervousness, asthma attacks, abdominal pain, dizziness, dyspnea and blurred vision;
• various signs of intolerance, anemia, malaise, nausea, asthenia, tachycardia and vomiting, as well as headaches and increased blood pressure;
• nightmares, hyperkalemia, thrombocytopenia or pancytopenia, drowsiness, constipation and diarrhea;
• purpura, swelling, itching and hypothermia, as well as fear, bloating and renal failure;
• rash on the epidermis, hyperhidrosis and hot flashes;
• jaundice, gastritis, bronchial spasm, erythema, dyspepsia and tubulointerstitial nephritis;
• stomatitis, urticaria and dermatitis, as well as bleeding within the digestive system and Quincke's edema;
• hematuria or oliguria, as well as perforation or ulcer in the gastrointestinal tract;
• facial edema, erythema multiforme, dysuria and hepatitis;
• urinary retention, cholestasis and SSc.

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Overdose

Poisoning with the drug may cause symptoms such as apathy, vomiting, drowsiness, lethargy, nausea, abdominal pain and increased blood pressure. In addition, bleeding within the digestive system, acute renal failure, respiratory depression and coma may occur.

The medicine has no antidote. In case of intoxication, gastric lavage is required in the first 4 hours and enterosorbents are prescribed to the patient. After that, supportive and symptomatic measures are taken. At the same time, the work of the kidneys and liver must be closely monitored.

Interactions with other drugs

Drug interactions.

Corticosteroids.

The risk of developing ulcers or bleeding within the digestive system increases.

SSRIs and antiplatelet agents.

The likelihood of bleeding within the digestive system increases.

Anticoagulants.

NSAIDs can potentiate the activity of anticoagulants, such as aspirin or warfarin. In this regard, such combinations are prohibited for use in people with severe forms of coagulation disorders. If it is impossible to refuse such a combination, it is necessary to very carefully monitor the blood coagulation values.

ACE inhibitors, diuretics and angiotensin-2 component antagonists.

NSAIDs can reduce the activity of antihypertensive drugs and diuretics. In some patients with renal dysfunction (e.g., the elderly or dehydrated), the combined use of ACE inhibitors, angiotensin-2 antagonists, or agents that suppress the COX system may result in further deterioration of renal function and development of acute renal failure (which is usually treatable).

Such interactions should be taken into account in situations where the patient uses nimesulide together with ACE inhibitors or angiotensin-2 antagonists. Extreme caution is required, especially in the elderly. After starting to use this combination, renal function should be closely monitored. Patients should also drink enough fluids.

The drug temporarily reduces the effect of furosemide on the excretion of Na, and also (less intensively) – K. At the same time, it weakens the diuretic effect. The use of furosemide with nimesulide in people with heart or kidney disorders should be done with caution.

In volunteers, the use of nimesulide caused a rapid weakening of the effect of furosemide, which promoted the excretion of Na, as well as K (but less pronounced), and in addition, reduced the diuretic effect. The combination of these drugs causes a decrease in AUC values (by approximately 20%), as well as a weakening of the cumulative excretion of furosemide, without changing the indicators of its intrarenal clearance.

Pharmacokinetic effects when combined with other drugs.

There is information confirming that NSAIDs can reduce lithium clearance, which causes an increase in its plasma values and toxicity. In case of using Remesulide in people using lithium agents, it is necessary to regularly monitor plasma lithium values.

It has no clinically significant interaction with theophylline, cimetidine and glibenclamide, and also with digoxin, warfarin and antacids (combination of magnesium and aluminum hydroxide) when used in vivo.

The drug inhibits the activity of the enzyme CYP2C9. Use together with medications that are substrates of this enzyme may lead to an increase in their plasma indices. It is necessary to use nimesulide very carefully less than 24 hours before or after using methotrexate, because this can increase the values of the latter in the blood serum and enhance its toxic properties.

Due to the effect that substances that inhibit synthetase (including nimesulide) have on renal PG, the nephrotoxic activity of cyclosporines may increase.

The effect that other drugs have in relation to nimesulide.

In vitro testing has shown that valproic and salicylic acids, as well as tolbutamide, are capable of displacing nimesulide from the synthesis sites. However, although these effects were detected in blood plasma, they were not observed during clinical use of the drug.

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Storage conditions

Remesulide must be stored in dark places at temperatures below 25°C.

Shelf life

Remesulide can be used within a 5-year period from the date of sale of the drug.

Application for children

Not for use in pediatrics – under 12 years of age.

Analogues

The analogs of the drug are Nimid, Aponil, Nimesil, Affida Fort and Nimesulide, as well as Nise, Nimegesic with Nimesin and Toro-Sanovel.

Reviews

Remesulide is considered a very effective medicine - according to reviews, it copes with its task as well as other well-known drugs, but its cost is much lower.