Remesulid

Remesulid is a drug with antirheumatic drug effect. It is included in the group of NSAID drugs and has the following therapeutic properties - antipyretic, anti-inflammatory, and also painkillers.

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

Indications Remulsulide

It is used as a substance to eliminate acute pain. It is prescribed for the treatment of signs of osteoarthritis, accompanied by pain. However, it is used in women for the treatment of primary dysmenorrhea.

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Release form

The release of the component is implemented in tablets - 10 pieces inside the plate. In the box - 1 or 3 records.

Pharmacodynamics

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

Also, the drug inhibits the formation of tumor necrosis factor and other inflammatory conductors.

Pharmacokinetics

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

The drug is involved in intrahepatic metabolic processes; its main metabolic element is a substance with a medicinal activity hydroxynimesulide.

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

Dosing and administration

Remesulid is required to be taken orally, after eating, with some liquid. It is necessary to apply medicine on the 1st tablet 2 times a day - in the morning, and also in the evening.

The maximum duration of use of the drug - 15 days.

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Use Remulsulide during pregnancy

Remesulid should not be prescribed to pregnant or lactating patients.

Contraindications

The main contraindications:

• use in case of intolerance associated with the drug or the rest of NSAIDs;
• aggravated ulcers affecting the gastrointestinal tract;
• disorders of blood coagulation in the severe stage;
• bleeding within the digestive system;
• CH heavy character;
• history of bleeding inside the gastrointestinal tract;
• failure of the liver or kidneys (severe);
• the presence of a suspected surgical illness that is acute;
• combination with drugs, in theory capable of provoking the development of hepatotoxic symptoms.

Side effects Remulsulide

Among the side effects are:

• nervousness, asthma attacks, pain in the abdominal area, dizziness, dyspnea, and visual impairment;
• various signs of intolerance, anemia, malaise, nausea, asthenia, tachycardia and vomiting, and in addition to this headaches and increased blood pressure;
• nightmares, hyperkalemia, thrombocyte or pancytopenia, drowsiness, constipation and diarrhea;
• purpura, puffiness, itching and hypothermia, and beyond that fear, swelling and insufficiency of the kidneys;
• 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 inside the digestive system and angioedema;
• hematuria or oliguria, as well as perforation or an ulcer in the gastrointestinal tract;
• facial puffiness, erythema multiforme, dysuria, and hepatitis;
• urinary retention, cholestasis and SSD.

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Overdose

Due to drug poisoning, the development of such manifestations as apathy, vomiting, drowsiness, lethargy, nausea, pain in the abdominal area and an increase in blood pressure values. In addition, there may be bleeding within the digestive system, ARF, respiratory depression and a coma.

The medicine has no antidote. When intoxication in the first 4 hours is required to hold gastric lavage and appoint the patient chelators. After that, supporting and symptomatic measures are performed. However, you need to carefully monitor the work of the kidneys with the liver.

Interactions with other drugs

Drug interactions.

Corticosteroids.

Increases the likelihood of developing an ulcer or bleeding inside the digestive system.

SSRIs and anti-platelet agents.

Increases the likelihood of bleeding within the digestive system.

Anticoagulants.

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

ACEI substances, diuretic drugs and angiotensin-2 component antagonists.

NSAIDs can reduce the activity of antihypertensive drugs and diuretic substances. In some patients with kidney disorders (for example, in the elderly or those with dehydration), the joint use of an ACE inhibitor, antagonists of the angiotensin-2 component, or means that suppress the COX system, may experience a further decrease in renal function and the development of ARF (it is usually treatable).

Such interactions should be taken into account in situations where the patient uses nimesulide together with an ACE inhibitor or antagonists of the element angiotensin-2. Extreme care must be taken, in particular for older people. After you start using this combination, you must carefully monitor the work of the kidneys. Also, patients should consume a sufficient amount of fluid.

The drug for some time reduces the effect of furosemide on the excretion of Na, and in addition (less intense) - K. At the same time, it weakens the diuretic effect. The use of furosemide with nimesulide in people with disorders of the heart or kidney should be carried out carefully.

In volunteers, the use of nimesulide caused a rapid weakening of the effect of furosemide, which contributed to 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 (approximately 20%), as well as a weakening of the cumulative elimination of furosemide, without changing the indices of its intrarenal clearance.

Pharmacokinetic effects when combined with other drugs.

There is information confirming that NSAIDs are able to reduce the clearance of lithium, which causes an increase in its plasma values and toxicity. If Remesulida is used in persons using lithium products, it is necessary to regularly monitor plasma lithium values.

It does not have a clinically significant interaction with theophylline, cimetidine and glibenclamide, and in addition with digoxin, warfarin and antacids (a combination of hydroxide Mg and Al) when used in vivo.

The drug inhibits the activity of the enzyme CYP2С9. Use together with drugs that are substrates of this enzyme, can lead to an increase in their plasma parameters. It is required to use nimusulide very carefully less than 24 hours before or after using methotrexate, because it can increase the values of the latter inside the blood serum and enhance its toxic properties.

In connection with the effects that have relatively renal GHG substances that slow down synthetase (among them nimesulide), the nephrotoxic activity of cyclosporins may increase.

The effect that other drugs have on nimesulide.

In vitro testing has demonstrated that valproic and salicylic acids, as well as tolbutamide, are able to displace nimesulide from the areas of synthesis. But, despite the fact that these effects were found inside the blood plasma, they were not observed during the clinical use of the drug.

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Storage conditions

Remesulid must be kept in dark places, with a temperature of less than 25 ° C.

Shelf life

Remesulid can be used within a 5-year term from the time the medication is sold.

Application for children

Not used in pediatrics - younger than 12 years of age.

Analogs

Analogues of the drug are the substances Nimid, Aponil, Nimesil, Affida Fort and Nimesulid, and besides, Neise, Nimesic with Nimesin and Toro-Sanovel.

Reviews

Remesulid 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.