Nais, tablets 100 mg 20 pcs

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

CodeATX:M01AX17.

Indications

rheumatoid arthritis;
articular syndrome during exacerbation of gout;
psoriatic arthritis;
ankylosing spondylitis;
osteochondrosis with radicular syndrome;
osteoarthritis;
myalgia of rheumatic and non-rheumatic origin;
inflammation of ligaments, tendons, bursitis, including post-traumatic inflammation of soft tissues;
pain syndrome of various origins (including in the postoperative period, with injuries, algodismenorrhea, toothache, headache, arthralgia, lumbar ischialgia).
The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.

Pharmacological effect

Pharmacotherapeutic group: non-steroidal anti-inflammatory drug (NSAID).

ATX code: M01AX17.

Pharmacological properties

Pharmacodynamics

Non-steroidal anti-inflammatory drug (NSAID) from the sulfonanilide class. Is

a selective competitive inhibitor of cyclooxygenase-2 (COX-2), inhibits the synthesis of prostaglandins at the site of inflammation. The inhibitory effect on COX-1 is less pronounced (less likely to cause side effects associated with inhibition of prostaglandin synthesis in healthy tissues). Has anti-inflammatory, analgesic and pronounced antipyretic

action.

Pharmacokinetics

Absorption when taken orally is high (food intake reduces the rate of absorption without affecting its degree). Time to reach maximum concentration (TCmax) – 1.5-2.5 hours. Communication with plasma proteins – 95%, with erythrocytes – 2%, with lipoproteins – 1%, with acidic alpha1-glycoproteins – 1%. Changing the dose does not affect the degree of binding. The maximum concentration value (Cmax) is 3.5-6.5 mg/l. Volume of distribution – 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 concentration in plasma. Penetrates well into the acidic environment of the inflammation site (40%) and synovial fluid (43%). Easily penetrates histohematic barriers.

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

The half-life (T1/2) 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 bile (35%), and undergoes enterohepatic recirculation.

In patients with renal failure (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.

Special instructions

Since Nise® is partially excreted by the kidneys, its dose for patients with impaired renal function should be reduced, depending on creatinine clearance.
Given reports of visual disturbances in patients taking other NSAIDs, treatment should be stopped immediately if any visual disturbance occurs and the patient should be examined by an ophthalmologist.
The drug can cause fluid retention in tissues, so patients with high blood pressure and cardiac problems should use Nise® with extreme caution.
Patients should undergo regular medical monitoring if they, along with nimesulide, take medications that are characterized by an effect on the gastrointestinal tract.
If signs of liver damage appear (itching, yellowing of the skin, nausea, vomiting, abdominal pain, dark urine, increased levels of liver transaminases), you should stop taking the drug and consult your doctor.
The drug should not be used simultaneously with other NSAIDs.
The drug can change the properties of platelets, but does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.
The use of the drug may adversely affect female fertility and is not recommended for women planning pregnancy.
After 2 weeks of using the drug, monitoring of biochemical indicators of liver function is necessary.
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, dispersible tablets 50 mg 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, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Nimesulide

Composition

Each tablet contains:
Active ingredient: nimesulide 100 mg.
Excipients: calcium hydrogen phosphate, microcrystalline cellulose (type 114), corn starch, sodium carboxymethyl starch, magnesium stearate, colloidal silicon dioxide, talc.

Contraindications

Hypersensitivity to the active substance or auxiliary components; complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including a history); erosive and ulcerative changes in the mucous membrane of the stomach and duodenum (duodenum), active gastrointestinal bleeding, cerebrovascular or other bleeding; inflammatory bowel diseases (Crohn’s disease, ulcerative colitis) in the acute phase; hemophilia and other bleeding disorders; decompensated heart failure; liver failure or any active liver disease; anamnestic data on the development of hepatotoxic reactions when using nimesulide preparations; concomitant use of potentially hepatotoxic substances; alcoholism, drug addiction; severe renal failure (creatinine clearance less than 30 ml/min), progressive kidney disease, confirmed hyperkalemia; period after coronary artery bypass surgery; pregnancy, lactation period; children under 12 years of age (for this dosage form, see the “Special Instructions” section).

With caution
Coronary heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance less than 60 ml/min. Anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, old 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, prednisolone), selective reuptake inhibitors serotonin (eg, citalopram, fluoxetine, paroxetine, sertraline).

Side Effects

The frequency of side effects is classified depending on the frequency of occurrence: 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 (Reye’s syndrome).

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

From the urinary system: infrequently – swelling; 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, ulcer and/or perforation of the stomach or duodenum.

From the liver and biliary system: often – increased “liver” transaminases; very rarely – hepatitis, fulminant hepatitis, jaundice, cholestasis.

From the hematopoietic organs: rarely – anemia, eosinophilia; very rarely – thrombocytopenia, pancytopenia, purpura, prolonged bleeding time.

From the respiratory system: infrequently – shortness of breath; very rarely – exacerbation of bronchial asthma, bronchospasm.

From the senses: rarely – blurred vision.

From the cardiovascular system: infrequently – arterial hypertension; rarely – tachycardia, hemorrhages, “hot flashes”.

Other: rarely – general weakness; very rarely – hypothermia.

Interaction

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

Nimesulide may reduce the effect of furosemide. Nimesulide may increase the possibility of side effects while taking methotrexate.

Plasma lithium levels increase when lithium and nimesulide are taken simultaneously.

Nimesulide may enhance the effect of cyclosporine on the kidneys.

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

Overdose

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

Treatment: The patient requires 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, take activated carbon (60–100 g per adult), and osmotic laxatives. Forced diuresis and hemodialysis are ineffective due to the high binding of the drug to proteins.

Storage conditions

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

Shelf life

3 years.
Do not use after the expiration date stated on the package.

Manufacturer

Dr. Reddy’s Laboratories Ltd, India