Nise gel: description of the drug, instructions, contraindications

Most diseases of the musculoskeletal system are accompanied by pain. This significantly reduces a person's quality of life. In addition to general treatment, pain can be effectively relieved with the help of topical medications. One of these is Nise gel. This product has proven itself well among specialists and patients and has been popular in the pharmacological market for many years.

Pharmacological properties of the drug Nise gel

Nise gel contains nimesulide, a selective COX-2 inhibitor. It has an analgesic and anti-inflammatory effect due to the inhibition of COX-2, which leads to inhibition of the synthesis of prostaglandins, which are involved in the formation of edema and pain during inflammation. Nimesulide inhibits platelet activation factor, tumor necrosis factor alpha, and the release of proteinases and histamine. Methyl salicylate, a derivative of salicylic acid, has a local irritating and distracting effect. Menthol has an analgesic effect, accompanied by a feeling of cold. The analgesic effect of menthol is associated with stimulation of cold receptors, stabilization of calcium ion flows through the channels of neuronal membranes. Capsaicin has a local irritant effect, causes a local increase in blood flow and tissue hyperemia at the site of application, and promotes the release of endogenous biologically active substances. Nise gel is characterized by high safety of use (virtually no side effects are noted). When applied externally, the gel is gradually absorbed through the skin into the underlying muscle or synovial fluid. Equilibrium concentrations between skin and muscle or synovial fluid are achieved quickly. With local application of Nise gel, systemic absorption is insignificant, since the levels of nimesulide in the blood plasma remained below the detection limit of high-performance liquid chromatography and only after 5 hours very low concentrations (100 μg/l) of hydroxynimesulide in the blood plasma were detected.

Indications for use

Nise (orally or externally) is prescribed for symptomatic treatment, reduction of pain and inflammation in the following diseases:

• Rheumatoid and psoriatic arthritis;
• Arthralgia;
• Articular syndrome with exacerbation of gout and rheumatism;
• Ankylosing spondylitis;
• Osteochondrosis with radicular syndrome;
• Osteoarthritis;
• Radiculitis;
• Lumbago;
• Sciatica;
• Arthritis of various etiologies;
• Bursitis, inflammation of tendons and ligaments;
• Myalgia of non-rheumatic and rheumatic origin;
• Post-traumatic inflammation of soft tissues and the musculoskeletal system (ruptures and damage to ligaments, bruises);
• Pain syndrome of various origins (including algodismenorrhea, toothache and headache, pain due to injuries, in the postoperative period);
• Fever of various origins (including those arising from infectious and inflammatory diseases).

Nise has no effect on the progression of the disease.

Special instructions for the use of the drug Nise gel

The drug is intended for external use. Elderly patients with significant impairment of liver and kidney function, patients with congestive heart failure should use the drug with caution. It is recommended to apply the gel only to intact areas of the skin, avoid contact with open wounds. Do not use the gel under airtight or tight bandages. Avoid getting the gel into the eyes and mucous membranes. Wash your hands thoroughly before and after using the gel. Indications for use of the gel in children and dosage have not been established.

Description and characteristics

Nise gel belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs). Belongs to the class of sulfonanilides. This drug is intended to reduce the intensity of inflammatory processes, as well as to relieve pain.

The active substance is nimesulide, which has a blocking effect on cyclooxygenase-2.

This drug is available in aluminum tubes of 20, 50 and 100 g. Transparent gel of uniform consistency, yellow or light yellow in color, without foreign particles.

Note that this drug is not able to influence the root cause of pain. Nise gel is intended for symptomatic treatment as a complex therapy.

Release form and composition

The drug is produced in the form of a suspension, tablets, dispersible tablets, 1% gel.

1 g of gel 1% contains 10 mg of nimesulide. The auxiliary components of the gel include N-methyl-2-pyrrolidone, propylene glycol, macrogol, isopropanol, purified water, carbomer 940, butylated hydroxyanisole, thiomersal, potassium dihydrogen phosphate, flavor (Narcissus-938).

Nise, tablets 100 mg, 20 pcs.

Manufacturer

Dr. Reddy's, India

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.

pharmachologic effect

Pharmacotherapeutic group: non-steroidal anti-inflammatory drug (NSAID).
CodeATX:M01AX17. Pharmacological properties Pharmacodynamics

Non-steroidal anti-inflammatory drug (NSAID) from the sulfonanilide class. It 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). It has anti-inflammatory, analgesic and pronounced antipyretic effects.

Pharmacokinetics

Absorption when taken orally is high (food intake reduces the rate of absorption without affecting its degree). Time to reach maximum concentration (Tmax) - 1.5-2.5 hours. Communication with plasma proteins - 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acidic alpha 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%), is 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.

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, and does not affect the progression of the disease.

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's age up to 12 years.

Carefully

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 serotonin reuptake inhibitors (for example, 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 messages.

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 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.

How to take, course of administration and dosage

The minimum effective dose should be used for the shortest possible short course. The tablets are taken with enough water, preferably after meals. Adults and children over 12 years of age, take 1 tablet orally 2 times a day. 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. The maximum daily dose for adults is 200 mg. Patients with chronic renal failure require a reduction in 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 requires symptomatic treatment and supportive care. There is no specific antidote. If an overdose occurs 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.

Special instructions

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, 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, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration 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 the reach of children!

Best before date

3 years

Active substance

Nimesulide

Conditions for dispensing from pharmacies

On prescription

Dosage form

pills

Purpose

For adults as prescribed by a doctor, Children over 12 years old, Children as prescribed by a doctor

Indications

Migraine, Radiculitis, Bursitis, Arthritis, Gout, Dislocations and sprains, Tendon inflammation, Myositis, Osteochondrosis, Rheumatoid arthritis, Sciatica, Arthrosis, Lumbago

Barcode and weight

Barcode: 8901148052031, 8901148005836, 8901148236608, 0118901148005 Weight: 0.013 kg

Contraindications

• A combination of intolerance to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs with bronchial asthma (complete or incomplete) and recurrent polyposis of the nose or paranasal sinuses (including a history);
• Erosive and ulcerative changes in the mucous membrane of the stomach and duodenum;
• Active gastrointestinal bleeding;
• Severe renal failure (with creatinine clearance less than 30 ml per minute);
• Liver failure or any active liver disease;
• Damage to the epidermis, dermatosis and skin infections in the area of ​​application (gel for external use);
• Pregnancy and lactation;
• Age up to 2 years for suspension, 3 years for dispersible tablets, 7 years for gel for external use and 12 years for tablets;
• Hypersensitivity to the components of the drug.

Additional contraindications to the use of Nise in tablet form are:

• Inflammatory bowel diseases (including ulcerative colitis, Crohn's disease) in the acute phase;
• Cerebrovascular or other bleeding;
• Hemophilia and other bleeding disorders;
• Hepatotoxic reactions when using nimesulide preparations (if there are indications in the anamnesis);
• Decompensated heart failure;
• Confirmed hyperkalemia;
• Progressive kidney diseases;
• Simultaneous use with potentially hepatotoxic substances;
• Drug addiction, alcoholism;
• The period after coronary artery bypass surgery.

Nise in tablet form should be taken with caution if you have the following diseases/conditions:

• Cardiac ischemia;
• Diseases of the brain caused by pathological changes in cerebral vessels with impaired cerebral circulation (cerebrovascular diseases);
• Congestive heart failure;
• Arterial hypertension;
• Hyperlipidemia/dyslipidemia;
• Diabetes;
• Peripheral artery disease;
• Renal failure with creatinine clearance less than 60 ml per minute;
• Ulcerative lesions of the gastrointestinal tract (indications in the anamnesis);
• Presence of Helicobacter pylori infection;
• Somatic diseases with severe course;
• Concomitant use with anticoagulants (for example, warfarin), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone);
• Long-term use of non-steroidal anti-inflammatory drugs;
• Elderly age;
• Frequent drinking of alcohol, smoking.

Dispersible tablets are recommended to be taken under medical supervision for the following diseases:

• Arterial hypertension;
• Heart failure;
• Diabetes mellitus type 2 (non-insulin dependent).

Nise should be used externally with caution in the presence of diseases/conditions such as:

• Hepatic, renal and severe heart failure;
• Diabetes mellitus type 2;
• Arterial hypertension;
• Elderly and children's age.

Flux treatment methods

Treatment should be started as early as possible. If an abscess on the gum opens spontaneously, there is a risk of infection entering the bloodstream. With such an infection, blood poisoning develops, and such a complication can lead to serious consequences, including the death of the patient.

Flux treatment is always complex. The treatment program depends on the degree of tooth decay and the spread of infection.

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Drug interactions

Nimesulide enhances the effect of drugs that reduce blood clotting, reduces the effect of furosemide, and increases the risk of adverse reactions of methotrexate.

When taken simultaneously with lithium, nimesulide increases its plasma concentrations.

Nimesulide has a high degree of binding to plasma proteins; therefore, patients who are being simultaneously treated with hydantoin and sulfonamides should be under regular medical supervision.

Nimesulide enhances the effect of cyclosporine on the kidneys.

In combination with GCS, serotonin reuptake inhibitors, nimesulide increases the risk of bleeding in the gastrointestinal tract.

General treatment

Methods depend on the reasons that caused the flux. The only exception is periostitis, which develops against the background of periodontitis. In this case, immediately after opening the abscess, the doctor begins periodontal treatment. No medical manipulations with the tooth are required. In other cases of dental disease you need to treat:

• Pulpitis. First, the dentist drills out carious cavities and performs pulp removal. After this, endodontic canal treatment is performed.
• Periodontitis. Treatment depends on whether depulpation and canal filling have been previously performed. If periodontitis has developed for the first time, the doctor will remove the pulp, clean and fill the canals. If filling of the canals has already been performed previously, they need to be unfilled and treated again. Since it is very important that the pus comes out of the flux completely, when treating complicated pulpitis and periodontitis, a temporary filling is not placed.
• Tooth after restoration. At the first stage, the doctor is faced with the task of completely removing inflammation. After this, the damaged tissue of the root apex is removed. If the condition of the root allows, the tooth is restored again using a core tab or pin and an artificial crown. When the damage is very severe, it is more advisable to remove the tooth.

Directions for use and dosage

Nise should be used at the lowest effective dose for the shortest possible time.

The tablets should be taken with plenty of water.

Nise in the form of tablets and suspensions is preferable to take before meals, but if you feel discomfort in the stomach or have diseases of the gastrointestinal tract, you can take it at the end of a meal or after it. Dispersible tablets should be taken at the end or after a meal, first dissolving a single dose in 1 teaspoon (5 ml) of water.

For adults and children over 12 years of age, Nise is prescribed 100 mg (1 tablet) 2 times a day. The maximum dose is 2 tablets per day. In case of chronic renal failure, the daily dose should be reduced by 2 times.

Nise children are prescribed 2-3 times a day at 3-5 mg/kg body weight (maximum 5 mg/kg). For body weights greater than 40 kg, the drug is prescribed in an adult dose. When using the drug in children, you need to choose a dosage form according to age: suspension - from 2 years; dispersible tablets – from 3 years; tablets - from 12 years.

Nise in the form of a gel is used externally, applying (without rubbing) a thin, even layer to the area of ​​maximum pain. The surface of the skin should first be washed and dried. A single dose is about 3 cm of gel, the frequency of use is 3-4 times a day. The dosage regimen may vary depending on the area of ​​the treated surface and the response to therapy (but not more than 4 times a day).

You should not use Nise for longer than 10 days without medical advice.

Side effects

When using Nise in tablet form, the following side effects may develop:

• Cardiovascular system: uncommon – arterial hypertension; rarely – hemorrhages, tachycardia, hot flashes;
• Digestive system: often – nausea, diarrhea, vomiting; infrequently – flatulence, constipation, gastritis; very rarely - stomatitis, abdominal pain, gastrointestinal bleeding, tarry stools, ulcer and/or perforation of the stomach or duodenum;
• Respiratory system: infrequently - shortness of breath; very rarely - bronchospasm, exacerbation of bronchial asthma;
• Urinary system: infrequently - edema; rarely - dysuria, urinary retention, hematuria, hyperkalemia; very rarely - oliguria, renal failure, interstitial nephritis;
• Central nervous system: infrequently – dizziness; rarely – a feeling of fear, nightmares, nervousness; very rarely - drowsiness, headache, encephalopathy (Reye's syndrome);
• Skin: uncommon – itching, increased sweating, rash; rarely – dermatitis, erythema; very rarely - swelling of the face, exudative erythema multiforme, including Stevens-Johnson and Lyell syndrome;
• Liver and biliary system: often - increased liver transaminases; very rarely - fulminant hepatitis, hepatitis, jaundice, cholestasis;
• Sense organs: rarely – blurred vision;
• Hematopoietic organs: rarely – eosinophilia, anemia; very rarely - pancytopenia, thrombocytopenia, prolonged bleeding time, purpura;
• Allergic reactions: rarely – hypersensitivity reactions; very rarely - angioedema, urticaria, anaphylactoid reactions;
• Other: rarely – general weakness; very rarely - hypothermia.

When using Nise in the form of dispersible tablets, the following disorders may develop:

• Central nervous system: dizziness, headache;
• Digestive system: diarrhea, heartburn, vomiting, nausea, pain in the stomach, toxic hepatitis, erosive and ulcerative lesions of the gastrointestinal tract, increased activity of liver transaminases;
• Hematopoietic system: thrombocytopenia, anemia, leukopenia, agranulocytosis;
• Allergic reactions: skin rash, anaphylactic shock, bronchospasm;
• Other: fluid retention, prolongation of bleeding time, hematuria.

Nise in suspension form is usually well tolerated by patients. In some cases, the following may occur: nausea, stomach pain, vomiting, diarrhea, urticaria, itching, bronchospasm.

When using an external gel, local reactions may develop in the form of itching, peeling, urticaria, and transient changes in skin color (does not require discontinuation of the drug). With prolonged therapy or when used on large areas of the skin, systemic adverse reactions may occur, manifested as heartburn, nausea, diarrhea, vomiting, ulceration of the gastrointestinal mucosa, gastralgia, increased activity of liver transaminases, dizziness, headache, fluid retention, hematuria, allergic reactions, leukopenia, thrombocytopenia, agranulocytosis, anemia, prolongation of bleeding time.

If any side effects develop, you should interrupt treatment and consult a doctor.