Nise tablets: instructions for use. The drug "Nise" (tablets): composition, properties and indications for use of Nise in injections instructions for use

Dr. REDDY's Laboratories Dr. Reddy with Laboratories Ltd. Canonpharma Production, CJSC

Country of origin

India Russia

Product group

Anti-inflammatory drugs (NSAIDs)

Non-steroidal anti-inflammatory drug (NSAID).

Release forms

• 10 - blisters (1) - cardboard packs. 10 - blisters (2) - cardboard packs. 10 - blisters (10) - cardboard packs 10 - blisters (2) - cardboard boxes. 20 g - aluminum (1) - cardboard packs. 50 g - aluminum (1) - cardboard packs. 10 tablets are placed in a blister pack made of polyvinyl chloride film and aluminum foil.

Description of the dosage form

• Gel for external use 1% White with a yellowish tint, round biconvex tablets with a smooth surface. Gel for external use 1% is transparent, light yellow or yellow in color, free of foreign particles. Capsule-shaped tablets, film-coated, white to almost white in color, with a characteristic odor. Dispersible tablets

pharmachologic effect

Amtolmetin guacil is a non-steroidal anti-inflammatory drug (NSAID), a non-selective cyclooxygenase (COX) inhibitor. Amtolmetin guacil is a precursor to tolmetin. It has anti-inflammatory, analgesic, antipyretic, desensitizing effects, and has a gastroprotective effect. Suppresses pro-inflammatory factors, reduces platelet aggregation; inhibits COX-1 and COX-2, disrupts the metabolism of arachidonic acid, reduces the formation of prostaglandins (including at the site of inflammation), suppresses the exudative and proliferative phases of inflammation. Reduces capillary permeability; stabilizes lysosomal membranes; inhibits the synthesis or inactivates inflammatory mediators (prostaglandins, histamine, bradykinins, cytokines, complement factors). Blocks the interaction of bradykinin with tissue receptors, restores impaired microcirculation and reduces pain sensitivity at the site of inflammation. Affects the thalamic centers of pain sensitivity; reduces the concentration of biogenic amines with algogenic properties; increases the pain sensitivity threshold of the receptor apparatus. Eliminates or reduces the intensity of pain, reduces morning stiffness and swelling, increases the range of motion in the affected joints after 4 days of treatment. The protective effect of amtolmetin guacil on the gastric mucosa is realized by stimulating capsaicin receptors (also called vanilloid receptors) present in the walls of the gastrointestinal tract. Due to the presence of a vanillin group in amtolmetin guacil, it can stimulate capsaitin receptors, which in turn causes the release of calcitonin gene-encoded peptide (CAGP) and a subsequent increase in nitric oxide (NO) production. Both of these actions counterbalance the negative effect caused by the decrease in prostaglandins due to COX inhibition. Amtolmetin guacil was well tolerated by patients with long-term use (for 6 months).

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%), subject to enterohepatic recycling. 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 conditions

Since Nise® is partially excreted by the kidneys, its dose should be reduced in patients with impaired renal function, 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. 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.

Compound

• Each tablet contains: Active substance: nimesulide 100 mg. Excipients: calcium hydrogen phosphate 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. Each film-coated tablet contains: Active substance: amtolmetin guacil 600 mg; Excipients: lactose monohydrate 40.1 mg, hypromellose (15 cps) 6.0 mg, lactose monohydrate (Flowlac 100) 120.3 mg, colloidal silicon dioxide 1.6 mg, sodium carboxymethyl starch (type-A) 24.0 mg , magnesium stearate 8.0 mg; Film coating: hypromellose (5 pps) 12.5 mg, titanium dioxide 6.25 mg, macrogol-400 1.25 mg. nimesulide 10 mg Excipients: N-methyl-2-pyrrolidone, propylene glycol, macrogol, isopropanol, carbomer 940, butylated hydroxyanisole, thimerosal, potassium phosphate, water, flavor. nimesulide 10 mg; excipients: N-methyl-2-pyrrolidone 250 mg, propylene glycol 100 mg, macrogol 315.5 mg, isopropanol 100 mg, purified water 200 mg, carbomer-940 20 mg, butylated hydroxyanisole 0.2 mg, thiomersal 0.1 mg, potassium dihydrogen phosphate 0.2 mg, flavor (Narcissus-938) 4 mg. nimesulide 50 mg Excipients: microcrystalline cellulose, calcium phosphate, corn starch, sodium carboxymethyl starch, magnesium stearate, talc, colloidal silicon dioxide, aspartame, pineapple flavoring

Nise indications for use

• - rheumatoid arthritis; - articular syndrome with rheumatism and exacerbation of gout; - psoriatic arthritis; - ankylosing spondylitis; - osteochondrosis with radicular syndrome; - radiculitis; - sciatica; - lumbago; - osteoarthritis; - arthritis of various etiologies; - arthralgia; - myalgia of rheumatic and non-rheumatic origin; - inflammation of ligaments, tendons, bursitis; - post-traumatic inflammation of soft tissues and the musculoskeletal system (damage and rupture of ligaments, bruises); - pain syndrome of various origins (including in the postoperative period, with injuries, algodismenorrhea, toothache, headache); - fever of various origins (including infectious and inflammatory diseases).

Nise contraindications

• - erosive and ulcerative lesions of the gastrointestinal tract in the acute phase; - bleeding from the gastrointestinal tract; - “aspirin triad”; - liver dysfunction; - severe renal failure (CR

Nise dosage

• 1% 100 mg 50 mg 50 mg/5 ml 600 mg

Nise side effects

• The frequency of side effects is classified depending on the frequency of occurrence: often (1-10%), uncommon (0.1-1%), rare (0.01-0.1%), very rare (less than 0.01%) , including individual messages. From the digestive system: often – nausea; uncommon – dyspepsia, discomfort in the stomach and intestines, bloating; rarely – abdominal pain, diarrhea, vomiting, constipation, gastritis; very rarely - peptic ulcer, liver dysfunction. From the urinary system: increased urea nitrogen in the blood, urinary tract infections From the senses: rarely - tinnitus, visual impairment. From the respiratory system: rarely - bronchospasm, shortness of breath, rhinitis, laryngeal edema. From the central nervous system: often – dizziness, headache, drowsiness; rarely – depression. From the cardiovascular system: often - increased blood pressure. From the hematopoietic organs: rarely - anemia, thrombocytopenia, agranulocytosis, leukopenia. From the skin: uncommon – skin rash (including maculopapular rash), purpura, rare – exfoliative dermatitis (fever with or without chills, redness, thickening or peeling of the skin, swelling and/or tenderness of the tonsils), urticaria, Stevens-Johnson syndrome , Lyell's syndrome. Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, itching of the skin, tachypnea or dyspnea, swelling of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing). Other: often ¬ – weakness; uncommon – swelling (face, legs, ankles, fingers, feet, weight gain); rarely – increased sweating, fever, lymphadenopathy; very rarely - swelling of the tongue. Symptoms of overdose, measures to assist in case of overdose Symptoms: abdominal pain, nausea, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, impaired renal function, metabolic acidosis. Treatment: gastric lavage, administration of adsorbents (activated carbon) and symptomatic therapy (maintaining vital body functions). There is no specific antidote.

Drug interactions

Inducers of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites. Reduces the effectiveness of uricosuric, antihypertensive drugs and diuretics. Enhances the hypoglycemic effect of sulfonylurea derivatives, the effect of anticoagulants, antiplatelet agents, fibrinolytics, side effects of estrogens, glucocorticosteroids and mineralcorticoids. Antacids and cholestyramine reduce absorption. Increases the concentration of lithium and methotrexate in the blood. In some patients with impaired renal function, co-administration of NSAIDs and angiotensin-converting enzyme (ACE) inhibitors may result in further deterioration of renal function. Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.

Overdose

Currently, no cases of overdose of Nise have been reported. When applying more than 50 g of gel to large areas of the skin, an overdose may develop (systemic adverse reactions). There is no specific antidote. You should immediately consult a doctor.

Storage conditions

• keep away from children

Information provided

Nise is a drug that has two properties at once: anti-inflammatory and analgesic (local). The main active ingredient is nimesulide, which in turn belongs to the selective reversible inhibitors of the COX-2 type (endoperoxid-PGN2 synthesis). Nise's action is aimed at reducing the concentration of short-acting PGN2, a substrate that is the result of kinin-stimulated PGE2 synthesis, directly at the site of the inflammatory process or in the ascending pathways that conduct pain impulses along the spinal cord.

Composition and release form

Release form

• Pills.
• Gel.
• Suspension.

Composition of the medicine

Nise is available in two versions of tablets: for oral administration and dispersible (to take, they must first be dissolved in a small amount of water).

1 tablet contains 100 mg of nimesulide, the main active ingredient. Additional components of the drug are microcrystalline cellulose, corn starch, magnesium stearate, talc, colloidal silicon anhydrate, sodium glycogen, calcium hydrogen phosphate.

According to the instructions, 1 dispersible tablet contains 50 mg of nimesulide. In addition, the drug contains microcrystalline cellulose, corn starch, magnesium stearate, talc, pineapple flavor, sodium carboxymethyl starch, calcium phosphate, silicon dioxide, aspartame.

Composition of Nise gel

Excipients are: methyl salicylate, diethyl phthalate, propylene glycol, sodium benzoate, diethylene glycol monoethyl ether, polyoxyl 40 from castor oil, carbomer 940, disodium edetate, purified water, butylated hydroxytoluene, capsaicin, menthol, trometamol.

Composition of the Nise suspension

Nimesulide is the main active ingredient.

Additional substances of Nise suspension are sucrose, sorbitol, methylparaben, propylparaben, pineapple flavor, yellow dye, xanthan gum, polysorbate 80, citric acid, glycerin, purified water. Unlike other forms of the drug, Nise suspension is recommended to be used before meals. However, if the child feels discomfort in the stomach, it is better to move the time of administration to the end of the meal.

Storage conditions

List B: dry, dark place, temperature no higher than 25 degrees.

pharmachologic effect

A decrease in the concentration of PGE2, which is a mediator of the inflammatory process or pain syndrome, leads to a decrease in the activation of prostanoid receptors of the EP type. This action gives an analgesic effect in combination with an anti-inflammatory one.

When Nise is used as a local anesthetic, it causes a reduction in pain or its complete elimination in the area where the gel was applied, in particular this applies to pain in the joints at rest and during movement, reduces stiffness in the morning, as well as swelling in the area of ​​the joints. In addition, the use of the drug can increase the range of movements.

The main difference between the drug Nise and other NSAIDs is that only it is capable of selectively, that is, selectively, suppressing COX-2, inhibiting the production of prostaglandins directly at the site of inflammation.

Nise extremely rarely causes various side effects. This is due to the possibility of inhibiting prostaglandin production in healthy tissues.

If the medicine is used in tablets for oral administration, we can talk about good absorption from the stomach and intestines. The time it takes to reach maximum concentration is about 2.5 hours. The half-life of the drug is 3 hours. Nise is biotransformed in liver cells. The process of elimination from the body is carried out by the kidneys. Does not accumulate during long-term use.

Indications for use of Nise

• diseases of the musculoskeletal system of inflammatory and degenerative origin (rheumatoid arthritis, osteoarthritis, osteochondrosis with radicular syndrome, radiculitis, bursitis, inflammation of ligaments and tendons, sciatica, lumbago);
• pain in muscle fibers;
• inflammation in the post-traumatic period (as a result of damage to ligaments, bruises);
• elevated temperature.

Contraindications

• ulcer;
• individual intolerance;
• renal and liver failure;
• “aspirin” asthma;
• lactation period;
• pregnancy.

For diabetes mellitus, arterial hypertension and heart failure, Nise should be taken with extreme caution.

Side effects

• gastralgia;
• diarrhea;
• nausea;
• dizziness;
• heartburn;
• allergy;
• fluid retention in the body, swelling;
• headache;
• anemia;
• hematuria;
• skin rash, itching, flaking.

Instructions for use

Method and dosage of tablets

Tablets for oral administration are called Nise 100.

Nise tablets should be taken immediately after meals. It should not be bitten or crushed in any other way. It is enough to swallow it and wash it down with a small amount of water. It is not advisable to take Nise before meals. This may lead to irritation or other stomach discomfort.

Standard doses of Nise are prescribed to patients over 12 years of age. People over 65 years of age should not reduce the standard recommended dose. In addition, the dose of the drug should not be adjusted downwards in patients who have been diagnosed with renal failure with a creatinine clearance level, which was determined using the Rehberg test, up to 30 ml/min. If this indicator is above 30 ml/min, then taking Nise is contraindicated.

Dosage

The instructions indicate the following regimen for taking Nise to relieve pain, eliminate fever and reduce inflammation: 1 tablet of the drug, the equivalent of 100 mg of the active substance, twice a day, with equal intervals between doses.

The total daily dose of Nise can be increased only as prescribed by a doctor in case of emergency, up to 4 tablets per day with a dosing interval of 6 hours. The maximum dose of the drug, regardless of the severity of the pain syndrome, is 400 mg. Ignoring this rule risks overdose.

This type of Nise should be taken either directly during a meal or immediately after it. It is not recommended to take it before meals, as side effects from the digestive system may develop. To take one tablet, dissolve in 1 tsp. water. There is no need to take additional water or other drink.

Reception scheme

• For patients over 12 years of age, the drug is prescribed in the amount of two tablets per day (total daily dose of 100 mg of nimesulide);
• for children aged 3 to 12 years, the maximum permissible dose of Naise is calculated taking into account body weight: 3-5 mg of the main substance per 1 kg of weight (for example, for a child weighing 20 kg, the daily dose ranges from 3*20=60 mg to 5*20 = 100 mg, that is, 60-100 mg should be taken per day), and the resulting dose should be divided into several doses throughout the day at equal intervals.

If the child’s weight exceeds 40 kg, but his age is less than 12 years, then the patient is prescribed the norm for an adult.

Method and dosage of the gel

This form of Nise is intended for local anesthesia.

According to the instructions, you need to apply Nise gel to an area of ​​skin that has previously been thoroughly washed and dried. If the drug is used to anesthetize an unopened wound, warm water and soap are suitable for washing, and a towel will help to dry. If the skin is damaged, Nise gel cannot be used.

For one use, about 3 ml of gel should be squeezed onto the skin area, which should be distributed over the affected area without rubbing. Ignoring this rule can lead to the formation of a burn, which, although it goes away on its own, still causes some discomfort. Leave the drug Nise for 2 minutes so that it is absorbed. Next, the treated area must be covered with a gauze bandage; airtight bandages cannot be applied.

Reception regimen:

The number of procedures per day is no more than 4, otherwise side effects are possible. The maximum permissible daily dose is 30 g of gel or 1.5 tubes. The duration of treatment using Nise gel is calculated purely individually, taking into account the speed of pain relief, but no more than 10 days.

If irritation occurs in the area of ​​use of the drug Nise, its use should be stopped. The gel contains capsaicin, which can cause burning and redness of the skin. In some cases, this effect develops into increased sensitivity. This reaction is considered normal.

When taking Nise gel, you need to be extremely careful and prevent the product from getting into the eyes, mucous membranes of the nose, mouth and other organs. After use, the tube of product must be carefully closed and your hands washed.

Method and dosage of suspension

Before each use, shake the bottle with the suspension, and only then pour the product into a measuring cup. The suspension can be used to treat children older than two months according to certain regimens:

• for children under two years of age: 1.5 mg of the drug per 1 kg of the patient’s weight (if the child’s weight is 10 kg, then the daily dose is 1.5 * 10 = 15 mg, which must be divided into 3 doses);
• for children under 5 years of age: single dose - 2.5 ml three times a day;
• for children under 12 years of age: 5 ml three times a day;
• for children over 12 years of age: adult dose, which corresponds to 10 ml of suspension twice a day.

This form of the drug can be used not only for children, but also for adults for whom taking tablets is contraindicated. However, people with diabetes should not take it.

During pregnancy and lactation

During pregnancy, as well as during lactation, the use of the drug Nise is contraindicated.

Overdose

Symptoms of overdose are apathy, drowsiness, nausea and vomiting. With a quick response, you can get rid of them. If the overdose is significant, then the development of bleeding of the gastrointestinal tract, renal failure, and depression of respiratory function is possible.

Treatment consists of eliminating a specific symptom. Activated carbon and an osmotic laxative are prescribed.

Interaction with other drugs

Due to the fact that both alcohol and the drug Nise have a toxic effect on the liver, it is undesirable to take them at the same time. The drug can increase both the effectiveness and toxicity of other drugs: it reduces the effect of furosemide and increases the risk of side effects when used together with methotrexate.

Domestic and foreign analogues

The most popular analogues are:

Analogue of Nise - Nimesulide

It has antipyretic, proinflammatory and analgesic effects. This drug will relieve the symptoms of the disease, not the disease itself.

Analogue of Nise - Artrum

Available in gel form and is a non-steroidal anti-inflammatory drug. The main active ingredient is ketoprofen. Cannot be used by patients under 15 years of age.

Diclofenac - analogue

Available in ampoules and tablets. The main effect is the elimination of pain. When using the drug in injections, the maximum daily dose is 1 injection. The duration of treatment is no more than two days.

Price in pharmacies

The price of Nise in different pharmacies can vary significantly. This is due to the use of cheaper components and the pricing policy of the pharmacy chain.

Read the official information about the drug Nise, the instructions for use of which include general information and a treatment regimen. The text is provided for informational purposes only and cannot serve as a substitute for medical advice.

INSTRUCTIONS

on medical use of the drug

NIZE®

Registration number: P No. 012824/03

Tradename: Nise®

International Nonproprietary Name (INN): nimesulide

Chemical formula: 4"-nitro-2"-phenoxy-methane sulfonanilide (CAS 51803-78-2).

Dosage form: pills

Compound: 1 tablet contains 100 mg of nimesulide as an active substance and excipients: microcrystalline cellulose, corn starch, calcium hydrogen phosphate, sodium starch glycolate, purified talc, magnesium stearate, anhydrous colloidal silicon.

Description: almost white with a yellowish tint, round, biconvex tablets with a smooth surface.

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

ATX Code: M01AX17

pharmachologic effect

Non-steroidal anti-inflammatory drug (NSAID) from the sulfone-anilide class. It is a selective competitive inhibitor of cyclooxygenase-2 (COX-2), an enzyme involved in the synthesis of prostaglandins - mediators of edema, inflammation and pain. It has anti-inflammatory, analgesic and antipyretic effects.

Reversibly inhibits the formation of prostaglandin E2, both at the site of inflammation and in the ascending pathways of the nociceptive system, including the pathways of pain impulses in the spinal cord.

Reduces the concentration of short-lived prostaglandin H2, from which prostaglandin E3 is formed under the action of prostaglandin isomerase. A decrease in the concentration of prostaglandin E2 leads to a decrease in the degree of activation of EP type prostanoid receptors, which is expressed in analgesic and anti-inflammatory effects.

It has a slight effect on COX-1, practically without interfering with the formation of prostaglandin E2 from arachidonic acid under physiological conditions, thereby reducing the number of side effects of the drug.

The drug also suppresses platelet aggregation by inhibiting the synthesis of endoperoxides and thromboxane Aj, inhibits the synthesis of platelet aggregation factor, and inhibits plasminogen activation by increasing the concentration of inhibitor-1. Suppresses the release of histamine and also reduces the degree of bronchospasm caused by exposure to histamine and acetaldehyde. Inhibits the release of tumor necrosis factor a, which causes the formation of cytokinins.

It has been shown that nimesulide is able to suppress the synthesis of interleukin-6 and urokinase, thereby preventing the destruction of cartilage tissue. Inhibits the synthesis of metalloproteases (elastase, collagenase), preventing the destruction of proteoglycans and collagen of cartilage tissue.

It has antioxidant properties and inhibits the formation of toxic oxygen breakdown products by reducing the activity of myeloperoxidase. Interacts with glucocorticoid receptors, activating them through phosphorylation, which also enhances the anti-inflammatory effect of the drug.

Pharmacokinetics

Absorption when taken orally is high. Eating reduces the rate of absorption without affecting its extent. The time to reach the maximum concentration of the active substance in the blood plasma is 1.5-2.5 hours. The connection with plasma proteins is 95%, with erythrocytes - 2%, with lipoproteins -1%, with acidic alpha1-glycoproteins -1%.

The dose of the drug does not affect the degree of its binding to blood proteins.

The maximum concentration of nimesulide in blood plasma reaches 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 histo-hematological barriers.

Metabolized in the liver by tissue monooxygenases. The main metabolite, 4-hydroxynimesulide (25%), has similar pharmacological activity.

The half-life of nimesulide is 1.56 - 4.95 hours, 4-hydroxynimesulide - 2.89-4.78 hours. 4-hydroxynimesulide is excreted by the kidneys (65%) and bile (35%).

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.

Indications

Rheumatoid arthritis, osteoarthritis, arthritis of various etiologies, arthralgia, myalgia, postoperative and post-traumatic pain, bursitis, tendonitis, algodismenorrhea, toothache and headache, fever of various origins.

Contraindications

Hypersensitivity, erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase), bleeding from the gastrointestinal tract, “aspirin” asthma, liver failure, renal failure (creatinine clearance - less than 30 ml/min), pregnancy, lactation, children age (up to 12 years).

Carefully arterial hypertension, heart failure, type 2 diabetes mellitus.

Directions for use and doses

Orally, 1 tablet (100 mg) 2 times a day. The maximum daily dose for adults is 400 mg. The tablets are taken with sufficient water, preferably before meals. If you have diseases of the gastrointestinal tract, it is advisable to take the drug at the end of a meal or after a meal.

Children over 12 years of age are prescribed a single dose of 1.5 mg/kg of the child’s body weight 2-3 times a day, the maximum daily dose of the drug is 5 mg/kg per day. For adolescents weighing over 40 kg, take 100 mg no more than 2 times a day.

Side effect

Heartburn, nausea, vomiting, diarrhea, gastralgia, ulceration of the gastrointestinal mucosa; headache, dizziness; fluid retention; allergic reactions (skin rash, anaphylactic shock); thrombocytopenia, leukopenia, anemia, agranulocytosis, prolongation of bleeding time; increased activity of “liver” transaminases, hematuria; bronchospasm.

If any adverse reactions occur, you should stop taking the drug and consult your doctor.

Overdose

Cases of drug overdose have not been described. There is no specific antidote.

Interaction with other drugs

Caution should be exercised when using nimesulide simultaneously with the following drugs (due to the drugs competing for binding to plasma proteins): digoxin; phenytoin and lithium preparations; diuretics and antihypertensive drugs; other NSAIDs; cyclosporine; methotrexate and antidiabetic agents.

Nise

Compound

The chemical composition of Nise in tablets and dispersible tablets is the same.
The main active substance is nimesulide. Auxiliary elements: calcium phosphate, microcrystalline cellulose, corn starch, magnesium stearate, sodium glycolate, colloidal silicon dioxide, talc, aspartame, flavoring.

The chemical composition of Nise in the form of an oral suspension differs from the drug in tablet form. Nimesulide is the main active substance. Excipients: sorbitol, sucrose, propylparaben, methylparaben, citric acid monohydrate, xanthan gum, polysorbate 80, choline yellow WS, pineapple flavor #1 and purified water.

The chemical composition of the gel is as follows. Nimesulide is the main active element. Excipients: propylene glycol, N-methyl-2-pyrrolidone, PEG-400, isopropanol, butylated hydroxyanisole, carbomer-940, thimserosal, potassium phosphate, flavoring, water.

pharmachologic effect

The drug has antipyretic, anti-inflammatory, analgesic and antiplatelet effects. Suppresses the formation of prostaglandin at the site of inflammation, selectively inhibits COX2. Rarely may cause side effects due to inhibition of prostaglandin synthesis in healthy tissues. Slows down lipid peroxidation and has no effect on phagocytosis and hemostasis. When taken orally, it is absorbed quite well from the gastrointestinal tract. The maximum concentration of the drug is achieved 1.5–2.5 hours after administration. Its half-life is 3 hours. The main metabolite in its composition is the active hydroxynimesulide. This drug is biotransformed in the liver. Excretion is carried out mainly by the kidneys. Does not accumulate with prolonged use.

The drug in the form of a gel has a local anti-inflammatory analgesic effect. With its help, pain in the joints weakens or disappears during movement and rest. Swelling and morning stiffness of the joints are neutralized.

Indications for use

This drug is prescribed for the following diseases: osteoarthritis, osteoarthritis, bursitis, tendovaginitis, tendinitis, rheumatism, ankylosing spondylitis, muscle pain, post-traumatic pain, spinal pain, infectious diseases, all kinds of inflammatory processes, febrile syndrome, myalgia and neuralgia.

Nise in the form of a gel is used for degenerative and inflammatory diseases of the musculoskeletal system, such as rheumatoid and psoriatic arthritis, articular syndrome with exacerbation of gout and rheumatism, radiculitis, osteochondrosis with radicular syndrome, osteoarthritis, lumbago, bursitis, sciatica, inflammatory damage to tendons and ligaments .

Mode of application

The drug is taken orally. For adults, two doses per day of 100 mg are prescribed. If necessary, the daily dose can be increased to a maximum of 400 mg.
Experts recommend taking the suspension or tablets before meals, but if you experience discomfort in the stomach, you can take the drug after meals.

Nise, available in the form of dispersible tablets, should be dissolved in water (one tablet per teaspoon) and taken after meals.
For children over two years of age, the medicine is prescribed in the form of a suspension, for children over three years of age - in the form of a suspension or dispersible tablets. Older children (12 years and older) can take the tablets. The optimal dose for them should be calculated based on body weight: 3-5 mg per kg. Adolescents who have reached a weight of 40 kg can take the medicine at an adult dose - 100 mg twice a day.

Nise in the form of a gel is applied to the skin. Before this, the desired area of ​​skin should be thoroughly washed and dried. A column of gel, 3 cm long, is applied to the most painful area and rubbed to a thin, uniform layer. This procedure should be carried out 3-4 times a day.

The drug can be used for 10 days.

Side effects

When using this medication, the following side effects have been noted: headache, drowsiness, dizziness, nausea, diarrhea, vomiting, heartburn, gastralgia, stomach pain, tarry stools, toxic hepatitis, ulceration of the mucous membrane of the gastrointestinal tract, petechiae, melena; purpura, oliguria, fluid retention, anemia, leukopenia, thrombocytopenia, agranulocytosis, hematuria, high activity of “liver” transaminases. Various allergic reactions such as anaphylactic shock or skin rash also occur.

When using the gel, local adverse reactions may occur: urticaria, itching, peeling of the skin. If there is a transient change in skin color, then discontinuation of the medication is not required. When applying the gel to large areas of the skin, one cannot exclude systemic side effects that are typical when taking tablets and are listed above.

If any side effects are noticed, you should stop taking the medication and consult a doctor for advice.

Contraindications

The drug is contraindicated in case of peptic ulcer of the gastrointestinal tract in the acute stage, hypersensitivity to the components of the drug, liver failure, “aspirin” asthma, renal failure. Also, the drug should not be used for congestive heart failure, type 2 diabetes mellitus, arterial hypertension, pregnancy, or lactation. The drug in tablet form is contraindicated for children under 12 years of age; children under two years of age should not take this medicine in any form.

There are additional contraindications for the use of Nise gel: damage to the epidermis, dermatoses and various skin infections in the area of ​​application.

Pregnancy

During pregnancy and lactation, the use of this drug is prohibited. If there is an urgent need to use Nise, then breastfeeding should be stopped.

Drug interactions

The drug may increase the effectiveness and toxicity of some drugs due to competition between drugs for binding to plasma proteins. Nise interacts with phenytoin, digoxin, antihypertensive drugs, lithium drugs, diuretics, other NSAIDs, cyclosporine, methotrexate, anticoagulants, and oral hypoglycemic agents.

Overdose

Symptoms of overdose are an increase in the severity of adverse reactions. As a rule, this is impaired renal function, liver failure, irritation of the gastrointestinal tract, convulsions, respiratory depression, and increased blood pressure.

If any of these symptoms appear, you should immediately stop taking the drug and provide treatment: first of all, rinse the stomach, take activated charcoal and carry out symptomatic therapy. There is no clearly defined antidote. Hemodialysis and forced diuresis do not bring the desired results.

Release form

The drug is distributed in the form of 100 mg tablets, 50 mg dispersible tablets, 50 mg/5 ml oral suspension, and also as a 1% gel.

Storage conditions

Nise, presented in the form of regular and dispersible tablets, should be stored in a dry place, protected from light. Storage temperature should not exceed 25°C. The maximum shelf life is 3 years.

Nise gel is stored at a temperature not exceeding 25°C; freezing is prohibited. The shelf life of the drug is 2 years.

Nise in the form of a suspension or tablets of the regular and dispersible type is dispensed from pharmacies with a doctor’s prescription. Nise gel is an over-the-counter medicine.

Additionally

Long-term use of this drug requires constant monitoring of kidney function. Elderly people with cardiovascular and other diseases should take Nise with caution.

Avoid getting the gel on damaged skin, open wounds, eyes and other mucous membranes of the body. After using the gel, hands should be washed thoroughly.

Since the drug can cause drowsiness and dizziness, it should be prescribed with caution to patients whose activities require reaction time and increased attention, such as drivers.
Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.

I tried Nice and Pentalgin and Nurofen for migraines - all in one place. My head was still pounding. Then my daughter advised me to take Nalgesin. I had little faith in this drug, I thought it was just another useless NSAID, but I was wrong. During the next attack, I appreciated Nalgesin. Already after taking 1 tablet the pain... I tried Nice and Pentalgin and Nurofen for migraines - all in one place. My head was still pounding. Then my daughter advised me to take Nalgesin. I had little faith in this drug, I thought it was just another useless NSAID, but I was wrong. During the next attack, I appreciated Nalgesin. After taking 1 tablet, the pain went away and did not return for a long time.

I keep Nimesan for emergencies, for example, when cervical osteochondrosis does not allow me to even raise my arm or even turn my head to look around. We must pay tribute to this drug - it works instantly. I keep Nimesan for emergencies, for example, when cervical osteochondrosis does not allow me to even raise my arm or even turn my head to look around. We must pay tribute to this drug - it works instantly.

Nimesan is an excellent drug. My wrist hurt after playing tennis. It’s so strong that it’s impossible to tolerate. took a pill. It started working within a minute. But my wrist turned out to be dislocated; then I went to get it treated. Nimesan is an excellent drug. My wrist hurt after playing tennis. It’s so strong that it’s impossible to tolerate. took a pill. It started working within a minute. But my wrist turned out to be dislocated; then I went to get it treated.

I have been suffering from osteochondrosis for several years now. It starts with a pain in the neck and develops into a headache that makes you feel sick. I tried Nise, it didn’t help. Friends suggested trying Nimesan. I suffered so much that I would have agreed to an axe. But surprisingly, Nimesan turned out to be very effective. An hour later I only had slight discomfort... I have been suffering from osteochondrosis for several years now. It starts with a pain in the neck and develops into a headache that makes you feel sick. I tried Nise, it didn’t help. Friends suggested trying Nimesan. I suffered so much that I would have agreed to an axe. But surprisingly, Nimesan turned out to be very effective. An hour later I only had slight discomfort in my neck. I no longer have wild pains and sleepless nights.

At work it was necessary to move a lot, including stairs. So the pain in my knee was just killing me. I went to the doctor and he recommended Nimesan. An excellent drug. Now I can run all day and not worry about pain. Thanks to the doctor for the good recipe. At work it was necessary to move a lot, including stairs. So the pain in my knee was just killing me. I went to the doctor and he recommended Nimesan. An excellent drug. Now I can run all day and not worry about pain. Thanks to the doctor for the good recipe.

At work I usually sit haphazardly. And now I’ve finished it. It hurt my lower back. I thought he would let me go quickly. But no, it hurt so much that I could barely walk. On the way, I went to the pharmacy and bought Nimesan - I’ve known it for a long time, it helps a lot. By the time I got home, the pain had already passed. The product is good, but you need to do something about your sedentary... At work I usually sit haphazardly. And now I’ve finished it. It hurt my lower back. I thought he would let me go quickly. But no, it hurt so much that I could barely walk. On the way, I went to the pharmacy and bought Nimesan - I’ve known it for a long time, it helps a lot. By the time I got home, the pain had already passed. The product is good, but you need to do something about your sedentary lifestyle.

A couple of years ago, my sister and I were walking down the street and she felt pain in her back. She went into the pharmacy all in tears and asked for at least something to help with the pain. They gave me Nimesan. But I didn’t expect such an effect. After a couple of minutes she felt better. And after half an hour she practically forgot about... A couple of years ago, my sister and I were walking down the street and she felt pain in her back. She went into the pharmacy all in tears and asked for at least something to help with the pain. They gave me Nimesan. But I didn’t expect such an effect. After a couple of minutes she felt better. And after half an hour she practically forgot about the pain. Of course, you can’t neglect your back and you need to go to a doctor and get examined. But in such an emergency it was the right option.

I am only 32 years old, but I suffer from constant neck pain. The doctors all say their own things as usual. I got hooked on painkillers and, of course, tried almost everything that was available in pharmacies. So I’m sharing my expert experience: “Nimesan” is “numero uno” for me at the moment. It always works effectively, helps a lot, and the price... I am only 32 years old, but I suffer from constant neck pain. The doctors all say their own things as usual. I got hooked on painkillers and, of course, tried almost everything that was available in pharmacies. So I’m sharing my expert experience: “Nimesan” is “numero uno” for me at the moment. It always works effectively, helps a lot, and the price is several times lower than its analogues. What do you say: who has what experience?

Got into a car accident. No big deal, it just flew into the driver's door. He himself is unharmed, only the blow landed in his leg. In general, the leg caused some inconvenience later. Until my sister almost forcefully pushed Nimesan into me. At first I didn’t want to - I thought it was triangular bullshit, some kind of dietary supplement. It turned out that it helps. I took it until it went away... Got into a car accident. No big deal, it just flew into the driver's door. He himself is unharmed, only the blow landed in his leg. In general, the leg caused some inconvenience later. Until my sister almost forcefully pushed Nimesan into me. At first I didn’t want to - I thought it was triangular bullshit, some kind of dietary supplement. It turned out that it helps. I took it until my leg healed and I felt good.

Just recently, if something hurts, I put up with it until it goes away. My brother always drank Nimesan for pain. And recently I read an article that pain cannot be tolerated. Now I’m just starting to treat myself with Nimesan. Works great and is not expensive. Has anyone taken it? Just recently, if something hurts, I put up with it until it goes away. My brother always drank Nimesan for pain. And recently I read an article that pain cannot be tolerated. Now I’m just starting to treat myself with Nimesan. Works great and is not expensive. Has anyone taken it?

I advise everyone to take Nimesan. He injured his elbow while playing badminton in the yard. It seems that the elbow was treated, but for some reason inflammation began. My elbow hurt incredibly. The doctor prescribed Nimesan. I drank it and there was no pain at all. Plus I took antibiotics, so soon the elbow went away. I advise everyone to take Nimesan. He injured his elbow while playing badminton in the yard. It seems that the elbow was treated, but for some reason inflammation began. My elbow hurt incredibly. The doctor prescribed Nimesan. I drank it and there was no pain at all. Plus I took antibiotics, so soon the elbow went away.