Naisulide pills 100mg, 20pcs

Composition

1 tablet contains:

Active ingredient:  nimesulide 100 mg;

excipients:  microcrystalline cellulose, lactose monohydrate, potato starch, povidone K-30, sodium carboxymethyl starch (sodium starch glycolate), talc, magnesium stearate.

Pharmacological action

Pharmacotherapeutic group

NSAIDs

ATX Code: M01AX

Pharmacodynamics :

Nimesulide is a nonsteroidal anti-inflammatory drug (NSAID) from the class of sulfonamides. It has anti-inflammatory analgesic and antipyretic effects. Nimesulide belongs to a new generation of NSAIDs, the mechanism of action of which is associated with selective inhibition of cyclooxygenase II and the effect on a number of other factors: suppression of platelet activation factor, tumor necrosis factor alpha, suppression of proteinases and histamine.

Pharmacokinetics:

Suction

After oral use, it is well absorbed from the gastrointestinal tract (GIT). The maximum concentration in blood plasma (Cmax) after oral use is reached on average in 2-3 hours.

Distribution

The relationship with plasma proteins is 95% with red blood cells-2% with lipoproteins-1% with acidic alpha-1-glycoproteins-1%. Penetrates into the tissues of the female genital organs, where after a single dose, its concentration is about 40% of the concentration in blood plasma. It penetrates well into the acidic environment of the inflammatory focus (40%) and synovial fluid (43%). Easily penetrates through histohematic barriers.

Metabolism

It is metabolized in the liver by the cytochrome P 450 (CYP)isoenzyme2 From 9. The main metabolite is the pharmacologically active parahydroxy derivative of nimesulide-hydroxynimesulide.

Deduction

The half-life of nimesulide (T 1/2) is about 156-495 hours of hydroxynemesulide-289-478 hours.

Nimesulide is excreted mainly through the kidneys (about 50% of the dose taken) hydroxynimesulide is excreted through the kidneys (65%) and with bile (35%) undergoes enterohepatic recirculation.

Pharmacokinetics in special patient groups

In patients with mild to moderate renal insufficiency (creatinine clearance 30-80 ml/min), as well as in children and the elderly, the pharmacokinetic profile of nimesulide does not change significantly.

Repeated use does not lead to accumulation of the drug.

Indications

Rheumatoid arthritis joint syndrome with exacerbation of gout; psoriatic arthritis; ankylosing spondylitis; osteochondrosis with radicular syndrome; osteoarthritis; myalgia of rheumatic and non-rheumatic origin; inflammation of tendon ligaments bursitis including post-traumatic soft tissue inflammation; pain syndrome of various origins (including in the postoperative period for injuries algodismenorrhea toothache headache arthralgia lumboishalgia).

The drug is intended for symptomatic therapy of reducing pain and inflammation at the time of use, it does not affect the progression of the disease.

Use during pregnancy and lactation

The use of nimesulide during pregnancy and lactation is contraindicated.

If it is necessary to use nimesulide during breastfeeding, breastfeeding should be discontinued.

The use of nimesulide may negatively affect female fertility and is not recommended for women planning pregnancy. When planning a pregnancy, you should consult your doctor.

Contraindications

– Hypersensitivity to nimesulide or other components of the drug;

– complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance of acetylsalicylic acid and other NSAIDs (including in the anamnesis);

anamnestic information about the development of hepatotoxic reactions using drugs nimesulide;

– simultaneous use with other drugs with potential hepatotoxicity;

– inflammatory bowel disease (Crohn’s disease ulcerative colitis) in the acute phase;

– the period after the coronary artery bypass surgery;

– erosive and ulcerative changes in the mucous membrane of the stomach and duodenal ulcers, active gastrointestinal bleeding;

– cerebrovascular bleeding in history;

– hemophilia and other blood clotting disorder;

decompensated heart failure;

– severe renal insufficiency (creatinine clearance <30 ml/min), progressive kidney diseases, confirmed hyperkalemia;

– liver failure or any active liver disease;

alcohol addiction;

– deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;

– pregnancy and the period of breastfeeding;

– children’s age up to 12 years.

With caution:

Arterial hypertension diabetes mellitus compensated heart failure ischemic heart disease cerebrovascular diseases dyslipidemia / hyperlipidemia peripheral arterial diseases smoking frequent alcohol consumption renal failure (creatinine clearance 30-60 ml / min).

A history of ulcerative lesions of the gastrointestinal tract; the presence of Helicobacter pylori; elderly age; long-term previous use of NSAIDs; severe somatic diseases.

Concomitant therapy with the following medications: anticoagulants (e. g. warfarin) antiplatelet agents (e. g. acetylsalicylic acid clopidogrel) oral glucocorticosteroids (e. g. prednisone) selective serotonin reuptake inhibitors (e. g. citalopram fluoxetine paroxetine sertraline).

Side effects

WHO classification of frequency of side effects:

Very common (≥1/10) common (≥1/100 < 1/10) uncommon (≥1/1000 <1/100) rare (≥1/10000<1/1000) very rare (

Disorders of the blood and lymphatic system

Rarely: anemia eosinophilia hemorrhages;

Very rare: thrombocytopenia agranulocytosis pancytopenia purpura thrombocytopenic prolongation of bleeding time.

Immune system disorders

Rare: hypersensitivity reactions.

Very rare: anaphylactoid reactions.

Skin and subcutaneous tissue disorders

Infrequently: skin pruritus skin rash increased sweating;

Rare: erythema dermatitis;

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

Nervous system disorders

Infrequently: dizziness.

Very rare: headache, drowsiness, encephalopathy (Reye’s syndrome).

Mental disorders

Rare: feeling of fear nervousness night “nightmare” dreams.

Sensory disorders

Rare: blurred vision.

Disorders of the cardiovascular system

Infrequently: increased blood pressure;

Rare: tachycardia lability of blood pressure “hot flashes” palpitation sensation.

Respiratory system disorders

Infrequently: shortness of breath.

Very rare: exacerbation of bronchial asthma bronchospasm.

Disorders of the gastrointestinal tract

Often: diarrhea nausea vomiting;

Infrequently: constipation flatulence gastritis;

Very rare: abdominal pain dyspepsia stomatitis tarry stools gastrointestinal bleeding ulceration and / or perforation of the stomach or duodenum.

Liver and biliary tract disorders

are common: increased activity of “liver” enzymes;

Very rare: hepatitis fulminant hepatitis jaundice cholestasis.

Kidney and urinary tract disorders

Rarely: dysuria hematuria urinary retention;

Very rare: renal failure oliguria interstitial nephritis.

Disorders of water and electrolyte metabolism

Rare: hyperkalemia.

Other services

Infrequently: peripheral edema.

Rarely: asthenia malaise;

Very rare: hypothermia.

Interaction

Glucocorticosteroids increase the risk of gastrointestinal ulcers or bleeding.

Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs) increase the risk of gastrointestinal bleeding.

Anticoagulants

NSAIDs may enhance the effects of anticoagulants such as warfarin. Due to the increased risk of bleeding, this combination is not recommended and is contraindicated in patients with severe coagulation disorders. If combination therapy is still unavoidable, careful monitoring of blood clotting parameters is necessary.

Diuretics

NSAIDs may reduce the effect of diuretics. In healthy volunteers, nimesulide temporarily reduces the excretion of sodium under the action of furosemide to a lesser extent-the excretion of potassium and reduces the actual diuretic effect. Concomitant use of nimesulide and furosemide results in a decrease (approximately 20%) in the area under the concentration – time curve (AUC) and a decrease in the cumulative excretion of furosemide without changing the renal clearance of furosemide. Concomitant use of furosemide and nimesulide requires caution in patients with renal or cardiac insufficiency.

ACE inhibitors and angiotensin-II receptor

antagonists NSAIDs may reduce the effect of antihypertensive drugs. In patients with mild to moderate renal insufficiency (creatinine clearance 30-80 ml / min), concomitant use of ACE inhibitors, angiotensin II receptor antagonists and cyclooxygenase inhibitors (NSAIDs, antiplatelet agents) may lead to further deterioration of renal function and the occurrence of acute renal failure, which is usually reversible.These interactions should be considered in patients taking nimesulide in combination with ACE inhibitors or angiotensin II receptor antagonists.

This combination of drugs should be administered with caution, especially in elderly patients. Patients should receive sufficient fluids and renal function should be carefully monitored after starting co-therapy.

Mifepristone

Theoretically, it is possible to reduce the effectiveness of mifepristone and prostaglandin analogues when used simultaneously with NSAIDs (including acetylsalicylic acid) due to the antiprostaglandin effect of the latter.

Limited data show that the use of NSAIDs on the day of use of a prostaglandin analog does not adversely affect the effect of mifepristone or a prostaglandin analog on cervical dilatation uterine contractility and does not reduce the clinical effectiveness of medical termination of pregnancy.

Concomitant use of nimesulide with salicylates or other nonsteroidal anti-inflammatory drugs is not recommended due to the increased risk of ulceration of the gastrointestinal tract. Nimesulide displaces salicylic acid when it binds to plasma receptors.

There is evidence that NSAIDs reduce the clearance of lithium, which leads to an increase in the concentration of lithium in blood plasma and its toxicity. When prescribing nimesulide to patients receiving lithium therapy, regular monitoring of the concentration of lithium in the blood plasma should be carried out.

There were no clinically significant interactions with glibenclamide theophylline digoxin cimetidine or antacids (for example, a combination of aluminum and magnesium hydroxides).

Nimesulide inhibits the activity of the CYP2C9 isoenzyme. When drugs that are metabolized with the participation of this enzyme are used simultaneously with nimesulide, the concentration of the latter in blood plasma may increase.

When used concomitantly with antiepileptic drugs (valproic acid) antifungal drugs (ketoconazole) antituberculous drugs (isoniazid) amiodarone methotrexate methyldopa amoxicillin in combination with clavulanic acid, an additive hepatotoxic effect is possible.

Caution should be exercised when prescribing nimesulide less than 24 hours before or after taking methotrexate, as in such cases the concentration of methotrexate in the blood plasma and, accordingly, the toxic effects of this drug may increase.

Due to the effect on renal prostaglandins, prostaglandin synthetase inhibitors such as nimesulide may increase the nephrotoxicity of cyclosporine.

In vitro studies have shown that nimesulide is displaced from the binding sites of tolbutamide by salicylic acid. Despite the fact that these interactions were determined in blood plasma, these effects were not observed during the clinical use of the drug.

How to take, course of use and dosage

For oral use. The minimum effective dose of the drug should be used in the shortest possible course.

Tablets are taken with a sufficient amount of liquid, preferably after a meal. In the presence of diseases of the gastrointestinal tract, the drug is recommended to be taken at the end of a meal or after a meal.

Adults: 100 mg 2 times a day. The maximum daily dose for adults is 200 mg.

Children over 12 years of age: 100 mg up to twice a day.

The duration of the course of treatment is not more than 15 days.

No dose adjustment is required in patients with mild or moderate chronic renal failure (creatinine clearance 30-60 ml / min).

Overdose

Symptoms: apathy drowsiness nausea vomiting epigastric pain. These symptoms are usually reversible with symptomatic and supportive care. Gastrointestinal bleeding may occur. In rare cases, it is possible to increase blood pressure the occurrence of gastrointestinal bleeding acute renal failure respiratory depression coma anaphylactoid reactions.

Treatment:

Symptomatic and supportive care. There is no specific antidote. If an overdose has occurred within the last 4 hours, it is necessary to induce vomiting and/or provide activated charcoal (from 60 to 100 g for an adult) and / or an osmotic laxative. Forced diuresis and hemodialysis are ineffective due to the high degree of binding of nimesulide to plasma proteins. It is necessary to monitor the state of kidney and liver function.

Special instructions

The drug should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn’s disease), as these diseases may worsen.

The risk of gastrointestinal bleeding ulceration/perforation of the stomach or duodenum increases with increasing NSAID dose in patients with a history of gastric or duodenal ulcers particularly complicated by bleeding or perforation, as well as in elderly patients, so treatment should begin with the lowest possible dose.

Patients receiving medications that reduce blood clotting or inhibit platelet aggregation also have an increased risk of gastrointestinal bleeding. If gastrointestinal bleeding or stomach ulcers occur in patients taking Nisulide, treatment should be discontinued.

If you experience symptoms similar to those of liver damage (anorexia pruritus yellowing of the skin nausea vomiting abdominal pain darkening of the urine increased activity of “liver” transaminases), you should immediately stop using the drug and consult a doctor.

Patients with arterial hypertension cardiac disorders cerebrovascular diseases the drug should be used with caution. If the condition worsens, treatment with the drug should be discontinued.

Since nimesulide is partially excreted by the kidneys, its dose for patients with impaired renal function should be reduced depending on creatinine clearance indicators. In case of deterioration of renal function, the drug should be discontinued.

Nimesulide can alter the properties of platelets, so caution should be exercised when using the drug in people with hemorrhagic diathesis, but the drug does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.

During treatment with Nisulide®, it is recommended to avoid the simultaneous use of hepatotoxic drugs, analgesics, other NSAIDs (with the exception of low doses of acetylsalicylic acid used in antiplatelet doses) and the use of ethanol.

In patients taking nimesulide together with cardiological doses of acetylsalicylic acid, combination therapy with gastroprotectors (proton pump inhibitors or misoprostol) should be used.

Elderly patients are particularly susceptible to adverse reactions to NSAIDs, including the risk of gastrointestinal bleeding and perforation, and life-threatening renal, liver, and heart failure. When taking the drug for this category of patients, proper clinical monitoring of the condition of these patients is necessary.

Taking into account reports of visual impairment in patients taking other NSAIDs, if any visual impairment occurs, the use of Naisulide® should be stopped immediately and an ophthalmological examination should be performed.

Influence on the ability to drive vehicles and mechanisms:

The effect of the drug on the ability to drive vehicles and mechanisms has not been studied, so during the period of use of the drug, caution should be exercised when driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

Store at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Nimesulide

Conditions of release from pharmacies

By prescription

Dosage form

Tablets