Naisulide, 100 mg 2 g 30 pcs

Pharmacotherapeutic group: Non-steroidal anti-inflammatory drug (NSAIDs)

CodeATX: M01AX17

Pharmacological properties.

Indications

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use; nimesulide is recommended for therapy as a second-line drug.

Active ingredient

Composition

1 sachet contains:

the active ingredient:

nimesulide 100 mg;

excipients:

sugar (sucrose),

maltodextrin,

cetomacrogol 1,000 (macrogol cetostearyl ether),

citric acid anhydrous,

“orange” flavoring.

How to take, the dosage

In the oral cavity, the contents of the sachet are dissolved in approximately 100 ml of water at room temperature (white or pale yellow suspension is formed).

The prepared solution should not be stored.

The drug Naisulide is used only for the treatment of patients over 12 years of age.

Adults and children over 12 years of age: 1 sachet twice daily, after meals.

Patients in the elderly: When treating elderly patients, the need to adjust the daily dose is determined by the physician with regard to possible interactions with other medications.

Patients with renal impairment: In patients with mild to moderate renal impairment (creatinine clearance 30-60 ml/min) no dose adjustment is necessary, whereas in patients with severe renal impairment (creatinine clearance <30 ml/min) Naisulide is contraindicated.

Patients with hepatic impairment:

The use of Naisulide* in patients with hepatic impairment is contraindicated.

In order to reduce the likelihood of side effects, it is recommended that the minimum effective dose be taken for the shortest possible time.

The maximum daily dose for adults and children over 12 years of age is 200 mg.

The maximum duration of treatment is 15 days.

Interaction

Glucocorticosteroids increase the risk of gastrointestinal ulceration or bleeding.

Antithrombiotics and selective serotonin reuptake inhibitors (SSRls)*, such as fluoxetine, increase the risk of gastrointestinal bleeding.

NSAIDs can increase the effect of anticoagulants, such as warfarin. Because of the increased risk of bleeding, this combination is not recommended and is contraindicated in patients with severe coagulation disorders. If combination therapy still cannot be avoided, careful monitoring of blood clotting parameters is necessary.

NSAIDs may decrease the effect of diuretics. In healthy volunteers, nimesulide temporarily reduces sodium excretion under the effect of furosemide, to a lesser extent – potassium excretion and reduces the diuretic effect itself.

The concomitant use of nimesulide and furosemide leads to a decrease (approximately 20%) in the area of the concentration-time curve (AUC) and a decrease in the cumulative excretion of furosemide without changing the renal clearance of furosemide.

The concomitant use of furosemide and nimesulide requires caution in patients with renal or heart failure.

ACE inhibitors and angiotheisin-II reuptake antagonists

NSAIDs may decrease the effect of hypotensive drugs. In patients with mild to moderate renal insufficiency (creatine clearance and 30-80 ml/min) when concomitant use of ACE inhibitors, angiotensin II receptor antagonists and agents inhibiting cyclooxygenase system (NSAIDs, antiaggregants), further worsening of renal function and occurrence of acute renal failure is possible, which is usually reversible. These interactions should be considered in patients taking nimesulide in combination with ACE inhibitors or angiotensin II receptor antagonists. Therefore, concomitant use of these drugs should be performed with caution, especially in elderly patients. Patients should receive sufficient fluids, and renal function should be carefully monitored after starting concomitant use.

Mifepristone

Theoretically, the efficacy of mifepristone and prostaglandin analogues may be reduced when used concomitantly with NSAIDs (including acetylsalicylic acid) through the antiprostaglandin effect of the latter. Limited data show that the use of NSAIDs on the day of use of a prostaglandin analog has no adverse effect on the effect of mifepristone or a prostaglandin analog on cervical dilation and uterine contractility and does not reduce the clinical effectiveness of medical termination of pregnancy.

There is evidence that NSAIDs decrease lithium clearance, which leads to increased plasma lithium concentrations and toxicity. When using nimesulide in patients on therapy with lithium drugs, regular monitoring of plasma lithium concentration should be performed.

Nimesulide inhibits the activity of CYP2C9 isoenzyme. When concomitant use of drugs that are substrates of this enzyme with nimesulide, plasma concentrations of the latter may increase.

When nimesulide is administered less than 24 hours before or after methotrexate administration, caution is required, because in these cases the plasma concentrations of methotrexate and, correspondingly, the toxic effects may increase.

Inhibitors of prostaglandin synthetases, such as nimesulide, may increase nephrotoxicity of cyclosporines because of their effect on renal prostaglandins.

Special Instructions

Unwanted side effects can be minimized by using the drug at the lowest effective dose with the shortest duration of use necessary to control the pain syndrome.

There have been reports of very rare cases of serious liver reactions, including death, associated with the use of nondrugs. If you experience symptoms similar to those of liver damage (anorexia, itching of the skin, yellowing of the skin, nausea, vomiting, abdominal pain, darkened urine, increased liver transaminase activity and name), you should immediately stop using Naisulide and consult a physician. Repeated use of Naisulide in such patients is contraindicated.

Hepatic reactions, which in most cases are reversible, have been reported with short-term use.

Patients should refrain from taking other analgesics, including NSAIDs (including COX-2 selective inhibitors) during the use of Naisulide.

The drug Naisulide should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn’s disease) due to the possible exacerbation of these diseases.

The risk of gastrointestinal bleeding, peptic ulcer/perforation of the stomach or duodenum is increased in patients with a history of gastrointestinal ulcers (ulcerative colitis, Crohn’s disease), as well as in older patients, with increasing doses of NSAIDs, so treatment should be started with the lowest possible dose. Such patients, as well as patients who require simultaneous use of low doses of acetylsalicylic acid or other drugs that increase the risk of gastrointestinal complications, it is recommended to administer additional gastroprotectors (misoprostol or proton pump blockers).

Patients with a history of GI disease, especially elderly patients, should inform their physician about any new GI symptoms (especially symptoms that may indicate possible gastrointestinal bleeding).

The drug Naisulide® should be prescribed with caution in patients taking drugs that increase the risk of ulceration or bleeding (oral

corticosteroids, anticoagulants such as warfarin, selective serotonin reuptake inhibitors, or antiplatelet agents such as acetylsalicylic acid).

In case of gastrointestinal bleeding or gastrointestinal ulcers in patients taking Naisulide, treatment with the drug should be discontinued.

Given the reports of visual disturbances in patients taking other NSAIDs, if any visual disturbance occurs, the use of Naisulide should be stopped immediately and an ophthalmologic examination should be performed.

The drug may cause fluid retention; therefore, Naisulide should be used with extreme caution in patients with arterial hypertension, renal and/or heart failure. If the condition worsens, treatment with the drug Naisulide should be stopped.

Clinical studies and epidemiological data suggest that NSAIDs, especially in high doses and with long-term use, may lead to a small risk of myocardial infarction or stroke. There are not enough data to exclude the risk of such events when using nimesulide. The drug contains sucrose; this should be considered in patients with diabetes mellitus (0.15-0.18 units per 100 mg of the drug) and those who follow a low-calorie diet. Naisulide is not recommended for patients with fructose intolerance, sucrose-isomaltose deficiency or glucose-galactose malabsorption syndrome. If there are signs of a “cold” or acute respiratory viral infection during the use of Naisulide, the drug should be discontinued. Nimesulide may alter the properties of platelets, so caution should be exercised when using the drug in persons with hemorrhagic diathesis, but the drug does not replace the preventive action of acetylsalicylic acid in cardiovascular diseases. Elderly patients are particularly susceptible to adverse reactions to NSAIDs, including the risk of gastrointestinal bleeding and perforations, life-threatening patient, decreased kidney, liver, and heart function. Adequate clinical monitoring is required when taking Naisulide Prepagate for this patient population.

There are data on the occurrence of rare cases of skin reactions (such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) when taking NSAIDs, including nimesulide. At the first signs of skin rash, lesions of mucous membranes or other signs of allergic reactions the drug Naisulide should be immediately discontinued.

The effect of the drug on driving and other mechanisms

The effect of the drug Naisulide on driving and mechanisms has not been studied, therefore during the period of using Naisulide preparation one should be careful when driving vehicles and engaging in potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

Side effects

Frequency is classified according to the recommendations of the World Health Organization, according to the occurrence of the case: Very common ≥), common (≥1/100, < 1/10), infrequent (≥1/1000, < 1/100), rare (≥1/10000, < 1/1000), very rare, including individual reports

Rare: Anemia, eosinophilia, hemorrhages;

Very rare: thrombocytopenia, pancytopenia, thrombocytopenic purpura.

Immune system disorders

Rare: hypersensitivity reactions;

Very rare: anaphylactoid reactions.

Skin and subcutaneous tissue disorders

Infrequent: itching, skin rash, increased sweating;

Rare: erythema, dermatitis;

Very rare: Urticaria, angioedema, facial edema, polyform erythema, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome).

Nervous system disorders

Infrequent: dizziness;

very rarely: headache, somnolence, encephalopathy (Reye’s syndrome).

Mental disorders

Rarely: feelings of fear, nervousness, nighttime “nightmares” dreams.

Visual disturbances

Rare: blurred vision;

Very rare: visual disturbances.

Hearing and labyrinth disorders

Very rare: vertigo.

Cardiovascular system disorders

Infrequent: increased blood pressure;

Rarely: tachycardia, blood pressure lability, “rushes” of blood to the face, palpitations.

Respiratory system disorders

Infrequent: shortness of breath;

Very rare: exacerbation of bronchial asthma, bronchospasm.

Gastrointestinal tract disorders

Often: diarrhea, nausea, vomiting;

Infrequently: constipation, flatulence, gastritis, gastrointestinal bleeding, gastric or duodenal ulcer and/or perforation;

Liver and biliary tract disorders

Frequently: Increased activity of “liver” enzymes;

Very rare: hepatitis, fulminant (fulminant) hepatitis (including fatal outcomes), jaundice, cholestasis.

Rarely: dysuria, hematuria, urinary retention;

very rarely: renal failure, oliguria, interstitial nephritis.

Disorders of water-electrolyte metabolism

Rarely: hyperkalemia.

Other

Infrequent: peripheral edema;

Rare: malaise, asthenia;

Very rare: hypothermia.

Overdose

Symptoms: apathy, drowsiness, nausea, vomiting, epigastric pain. These symptoms are usually reversible with symptomatic and supportive therapy.

High blood pressure, gastrointestinal bleeding, acute renal failure, respiratory depression, coma, and anaphylactoid reactions may occur.

Treatment: symptomatic and supportive therapy. There is no specific antidote. If overdose occurred within the last 4 hours, it is necessary to induce vomiting and. or ensure intake of activated charcoal (60 to 100 g per adult) and/or osmotic laxative. Forced diuresis, hemodialysis, hemoperfusion, urine alkalinization are ineffective due to the high degree of nimesulide binding to blood plasma proteins (up to 97.5%). It is necessary to monitor the state of renal and hepatic function.

Similarities