Nice pills 100mg, 30pcs

Composition

Each tablet contains: Active ingredient: nimesulide 100 mg. Auxiliary substances: calcium hydrophosphate 75 mg, microcrystalline cellulose (type 114) 40 mg, corn starch 54 mg, sodium carboxymethyl starch 35 mg, magnesium stearate 3 mg, colloidal silicon dioxide 2 mg, talc 1 mg

Pharmacological action

Pharmacotherapy group: nonsteroidal anti-inflammatory drug (NSAID).

KodATH: M 01 AH 17.

Pharmacological properties

Pharmacodynamics

Nonsteroidal anti-inflammatory drug (NSAID) from the class of sulfonanilides. It is a selective competitive inhibitor of cyclooxygenase-2( COX-2), inhibits the synthesis of prostaglandins in the inflammatory focus. The inhibitory effect on COX-1 is less pronounced (less often causes side effects associated with inhibition of prostaglandin synthesis in healthy tissues). It has an anti-inflammatory, analgesic and pronounced antipyretic effect.

Pharmacokinetics

Oral absorption is high (food intake reduces the rate of absorption without affecting its degree). Time to reach maximum concentration (Tmax) -1.5 – 2.5 h. The relationship with plasma proteins is 95%, with red blood cells-2%, with lipoproteins-1%, with acidic alpha-glycoproteins-1%. Changing the dose does not affect the degree of binding. The maximum concentration (Cmax) is 3.5-6.5 mg/l. The volume of distribution is 0.19-0.35 l / kg. Penetrates into the tissues of the female genital organs, where after a single dose, its concentration is about 40% of the plasma concentration. It penetrates well into the acidic environment of the inflammatory focus (40%), synovial fluid (43%). Easily penetrates through histohematic barriers.

It is metabolized in the liver by tissue monooxygenases. The main metabolite,4-hydroxynimesulide (25%), has similar pharmacological activity, but due to a decrease in the size of molecules, it is able to quickly diffuse through the COX-2 hydrophobic channel to the active site of the methyl group binding. 4-hydroxynimesulide is a water-soluble compound that does not require glutathione and phase II conjugation reactions (sulfation, glucuronidation, etc. ) for its elimination.

The half-life (T 1/2) of nimesulide is 1.56-4.95 hours,4-hydroxynimesulide is 2.89 – 4.78 hours. 4-hydroxynimesulide is excreted by the kidneys (65%) and with bile (35%), undergoes enterohepatic recirculation.

In patients with renal insufficiency (creatinine clearance 1.8-4.8 l/h or 30-80 ml/min), as well as in children and the elderly, the pharmacokinetic profile of nimesulide does not change significantly.

Indications

rheumatoid arthritis; articular syndrome with exacerbation of gout;- psoriatic arthritis

– ankylosing spondylitis;

– osteochondrosis with radicular syndrome;

– osteoarthrosis;

– myalgia, rheumatic and non-rheumatic origin;

– inflammation of the ligaments, tendons, bursitis, including post-traumatic inflammation of soft tissue;

pain syndrome of different Genesis (including in the postoperative period for injuries, algomenorrhea, toothache, headache, arthralgia, lumboischialgia).

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

Contraindications

• Hypersensitivity to the Active ingredient or auxiliary components;
• 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);
• erosive and ulcerative changes in the mucous membrane of the stomach and duodenum (duodenum), active gastrointestinal bleeding, cerebrovascular or other bleeding;
• inflammatory bowel disease (Crohn’s disease, ulcerative colitis) in the acute phase;
• hemophilia and other blood clotting disorder;
• decompensated heart failure;
• liver failure or any active liver disease;
• anamnestic information about the development of hepatotoxic reactions using drugs nimesulide;
• concomitant use of potentially hepatotoxic substances;
• alcohol and drug abuse;
• severe renal insufficiency (creatinine clearance less than 30 ml/min), progressive kidney diseases, confirmed hyperkalemia;
• the period following the coronary artery bypass surgery;
• pregnancy, lactation;
• children’s age up to 12 years.

With caution

Coronary heart disease, cerebrovascular diseases, congestive heart failure, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral artery disease, smoking, creatinine clearance less than 60 ml / min. Medical history of gastrointestinal ulceration, presence of Helicobacter pylori infection, advanced age, long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases, concomitant therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisone), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).

Side effects

The frequency of side effects is classified according to the frequency of occurrence of the case: often (1-10%), sometimes (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%), including individual reports.

Allergic reactions:  rarely-hypersensitivity reactions; very rarely-anaphylactoid reactions.

From the central nervous system:  infrequently – dizziness; rarely-a feeling of fear, nervousness, nightmares; very rarely-headache, drowsiness, encephalopathy (Reis syndrome).

From the side of the skin:  infrequently-pruritus, rash, increased sweating; rarely: erythema, dermatitis; very rarely: urticaria, angioedema, facial edema, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome).

From the urinary system:  infrequently-edema; rarely-dysuria, hematuria, urinary retention, hyperkalemia; very rarely-renal failure, oliguria, interstitial nephritis.

From the gastrointestinal tract:  often – diarrhea, nausea, vomiting; infrequently-constipation, flatulence, gastritis; very rarely-abdominal pain, stomatitis, tarry stools, gastrointestinal bleeding, ulceration and / or perforation of the stomach or duodenum.

From the liver and biliary system:  often-an increase in “hepatic” transaminases; very rarely-hepatitis, lightning hepatitis, jaundice, cholestasis.

From the side of hematopoietic organs:  rarely-anemia, eosinophilia; very rarely-thrombocytopenia, pancytopenia, purpura, prolongation of bleeding time.

Respiratory system disorders:  infrequently-shortness of breath; very rarely-exacerbation of bronchial asthma, bronchospasm.

From the side of the senses:  rarely – blurred vision.

From the cardiovascular system:  infrequently-arterial hypertension; rarely-tachycardia, hemorrhages, hot flashes. Other services:  rarely-general weakness; very rarely – hypothermia.

Interaction

The effect of medications that reduce blood clotting is enhanced when they are used simultaneously with nimesulide.

Nimesulide may reduce the effect of furosemide. Nimesulide may increase the possibility of side effects when taking methotrexate at the same time.

The level of lithium in plasma increases with simultaneous use of lithium and nimesulide preparations.

Nimesulide may increase the effect of cyclosporine on the kidneys.

Use with glucocorticosteroids, serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.

How to take, course of use and dosage

The minimum effective dose should be used in the shortest possible course. Tablets are taken with a sufficient amount of water, preferably after a meal. Adults and children over 12 years of age inside 1 tablet 2 times a day. In the presence of diseases of the gastrointestinal tract, it is advisable to take the drug at the end of a meal or after a meal. The maximum daily dose for adults is 200 mg. Patients with chronic renal failure need to reduce the daily dose to 100 mg.

Overdose

Symptoms:  apathy, drowsiness, nausea, vomiting. Gastrointestinal bleeding, increased blood pressure, acute renal failure, and respiratory depression may occur.

Treatment:  the patient needs symptomatic treatment and supportive care. There is no specific antidote. If an overdose has occurred within the last 4 hours, it is necessary to induce vomiting, provide activated charcoal (60-100 g per adult), osmotic laxatives. Forced diuresis and hemodialysis are ineffective due to the high binding of the drug to proteins.

Special instructions

Since Naiz® is partially excreted by the kidneys, its dose for patients with impaired renal function should be reduced, depending on the indicators of creatinine clearance. Given reports of visual impairment in patients taking other NSAIDs, treatment should be stopped immediately if any visual impairment occurs and the patient should be examined by an optometrist.

The drug may cause fluid retention in the tissues, so patients with high blood pressure and cardiac disorders should use Naiz® with extreme caution.

Patients should be monitored regularly if they are taking medications that have a significant effect on the gastrointestinal tract along with nimesulide.

If signs of liver damage appear (pruritus, yellowing of the skin, nausea, vomiting, abdominal pain, darkening of the urine, increased levels of “liver” transaminases), stop taking the drug and consult your doctor. Do not use the drug simultaneously with other NSAIDs.

The drug can change the properties of platelets, but it does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases. The use of the drug may negatively affect female fertility and is not recommended for women planning pregnancy.

After 2 weeks of using the drug, it is necessary to monitor the biochemical parameters of liver function.

This dosage form is contraindicated for children under 12 years of age, but if it is necessary to use nimesulide in children over 7 years of age,50 mg dispersible tablets and suspension can be used, in strict accordance with the instructions for medical use attached to them.

Since the drug can cause drowsiness, dizziness and blurred vision, caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

List B. In a dry place protected from light at a temperature not exceeding 25°C. Keep out of reach of children!

Shelf life

3 years

Active ingredient

Nimesulide

Conditions of release from pharmacies

By prescription

Dosage form

Tablets