To alleviate the patient's condition - eliminate pain, swelling of soft tissues, relieve fever and other symptoms of inflammation, doctors prescribe various non-steroidal anti-inflammatory drugs. Nise is a representative of this group of drugs. Made on the basis of Nimesulide - a synthetic drug belonging to the class of sulfonanilides. Unlike many other NSAIDs, the use of which causes the development of serious side effects, Nise is characterized by high therapeutic activity with guaranteed safety. This explains the popularity of the drug. As an integral part of complex therapy, Nise is widely used in the treatment of articular pathologies and other diseases accompanied by an inflammatory process and severe pain of various localization. The instructions for the drug will tell you about the properties, the mechanism of action of Nise, the rules of admission and the existing contraindications.

Pharmacological properties of the drug

The medicinal properties of Nise listed in the instructions are due to the compound included in its composition - Nimesulide. It is the first in the world, synthesized back in 1985, a selective selective cyclooxygenase-2 isoenzyme inhibitor. Nimesulide has no significant effect on COX-1. It is the 2nd form of the enzyme that is more responsible for the onset of pain. It is synthesized in peripheral tissues and the central nervous system as a response to damage and, by participating in the synthesis of prostaglandins (cellular mediators of inflammation), contributes to the development of the pathological process.

COX-1 is constantly present in a certain amount in the human body everywhere - mainly in the stomach, kidneys, blood vessels. Non-selective NSAIDs, suppressing the activity of the useful, important for the regulation of physiological processes, COX-1 cause ulcers, bleeding and other complications from the gastrointestinal tract. As a selective inhibitor,

Nise has many useful properties, it has:

• antipyretic effect - eliminates fever, hot flashes, reduces high temperature caused by the shift of the set point of thermal homeostasis from the normal value for a person (36.5-37 degrees) to an increased level;

• chondroprotective - prevents thinning and destruction of hyaline cartilage;

• antioxidant - inhibits the rate of oxidative reactions, the formation and accumulation of a large number of toxic products of cellular metabolism (free oxygen radicals);

• antiplatelet - prevents the aggregation of blood corpuscles (erythrocytes, platelets), preventing the formation of blood clots;

• antihistamine effect - reduces the phenomenon of bronchospasm (impaired bronchial patency), blocking the release of histamine and suppressing acetaldehyde, which enhances the synthesis of histamine;

• anti-inflammatory effect - combats the main clinical signs of inflammation, swelling of tissue elements, increased blood circulation, irritation and squeezing of receptors and nerve fibers. As a result, Nise eliminates skin redness, itching, local hyperthermia, pronounced swelling of damaged tissues. Relieves pain, restores the impaired function of the inflamed organ;

• analgesic effect - relieves pain, a reflex change in functions caused by the body's action aimed at protecting and getting rid of the painful pain factor.

Forms of release and composition

Nise is distributed in several forms, which allows you to choose a dosage form that is convenient for use and achieve the desired therapeutic effect. Pharmacies receive a medicine that differs in the method of application, concentration of the active ingredient and composition, these are:

• Gel for local action, 1% - uniform consistency, transparent, pale yellow. Packaged in 20 or 50 g aluminum tube. Instructions are included in the package. Additional ingredients: n-methyl-2-pyrrolidone, propylene and polyethylene glycols - solvents of substances used in the synthesis process, gel base; isopropyl alcohol - as a solvent and disinfectant; carbopol - base, gives viscosity; butylhydroxyanisole is a wax-like substance, an antioxidant. The composition also includes purified water, flavoring, monosubstituted potassium phosphate to create an acidic environment, thiomersal - an antiseptic, bactericidal, fungicidal component of the gel.

• Enteral administration (through the digestive tract):

• tablets are yellowish-white in color, with a smooth surface, convex on both sides. 10 pcs. in a blister. 2 blisters are included in a cardboard box. Besides 100 mg. Nimesulide in the composition of the tablet includes excipients: calcium hydrogen phosphate, corn starch - fillers that impart mass and ensure the completeness of absorption; sodium salt of carboxymethyl starch - thickener; microcrystalline cellulose - a disintegrant that breaks the tablet on contact with water; magnesium stearate - improves flowability, reduces the adhesion of the tableted mass; colloidal particles of silicon dioxide - adsorbent intestinal preparation.

• sachets for preparation 100 ml. suspensions - granules mixed with light yellow powder. The mixture has a citrus aroma - the smell of orange, packaged in 2 g. Content of Nimesulide - 100 mg. The paper box contains 9 such bags and instructions. The constituent components of the drug: sucrose - used to impart mass and as a corrective agent that corrects the taste of the prepared solution, orange flavor - for the smell, maltodextrin - for sweetening; anhydrous citric acid - provides gas formation and destruction of granules in a liquid medium; crospovidone - for disintegration, rapid swelling in water and disintegration of granules.

How Nise works

During clinical trials, it has been proven that due to its high selectivity to the cyclooxygenase-2 enzyme and a low effect on the form 1 isoenzyme, Nise is a highly safe drug. Side effects from the gastrointestinal tract are recorded 2.1 times less than when using, 2 - Diclofenac, 1.8 -.

The analgesic and anti-inflammatory effect manifests itself quickly - according to the instructions, pain relief occurs after 15 minutes. The medication is effective for inflammatory processes of any type and localization.

In terms of the strength of the effects, Nise is not inferior to the widely used NSAIDs - Naproxen, Diclofenac, Ibuprofen. Its antipyretic effect is more powerful than Aspirin, Paracetamol, Indomethacin. The combined use of oral and external agents allows for greater therapeutic efficacy with a lower dosage of tablets. Practically without exerting a systemic effect, the components of the gel quickly and deeply penetrate into the inflamed muscle tissue, the articular region. The clinical effect of the application comes quickly, the progression of Nise's disease does not affect.

The pharmacological action of Nise is carried out at the molecular level, based on chemical reactions in the body. They are all listed in the instructions. The clinical effect is due to the following mechanisms:

• regulation of the production of prostaglandins - a decrease in the concentration of prostaglandins H2 synthesized from arachidonic acid, which are precursors of prostaglandins E2. This substance serves as a trigger for the development of an inflammatory reaction, febrile conditions, increased pain sensitivity, bone resorption and calcium release from bones;

• suppression of the formation of endoperoxides responsible for the production of thromboxanes in platelets, which cause vasoconstriction, increased pressure, stimulate the activation and aggregation of new platelets;

• inhibition of the synthesis of metalloprotease enzymes that have a destructive effect on the components of the extracellular structure of the tissue - the main protein of the connective tissue collagen, core proteins of proteoglycans;

• blocking the effect on the regulatory centers of the hypothalamus of endogenous pyrogenic substances - inflammatory mediators of interleukins-1, -6, extracellular protein, tumor necrosis factor;

• inactivation of alpha-1-antitrypsin, which is deposited in liver cells and destroys them;

• a decrease in the activity of myeloperoxidase, an enzyme of neutrophil lysosomes that can damage tissues;

• activation of glucocorticoid receptors, important for the regulation of the immune system, capable of eliminating inflammatory stimuli.

Nise has a high absorption from the gastrointestinal tract, food intake does not affect the completeness of absorption, but reduces the rate of the process.

To achieve the maximum concentration of Nimesulide in the blood, according to the instructions, it takes 1.5-2.5 hours. The degree of binding to blood proteins does not depend on the dosage and is:

• 95% - plasma proteins;

• 2% - erythrocytes;

• 1% - lipoproteins;

• 1% is acidic alpha-1 glycoprotein.

The drug freely overcomes the histohematological barriers separating blood and tissue fluid. It is characterized by good penetrating ability: up to 40% enters the genital tissues of women and the acidic environment, characteristic of the focus of inflammation, 43% - synovial fluid. Metabolic processes take place in the liver, the transformation product exhibits similar activity. It does not accumulate in the body - it is excreted mainly with urine or bile through the liver. Due to enterohepatic recirculation, the therapeutic effect lasts for a longer time: the half-life is 1.5-5 hours, and the COX-2 blocking action lasts 8 hours, in the synovial fluid - 12 hours.

Reception Nise

The gel is dispensed without a prescription. In accordance with the instructions, it is used for local treatment, has a pronounced pain relief. It absorbs well, ensuring maximum penetration of the components. Application rules:

• the area of ​​the skin on which the gel will be applied should be washed and dried beforehand;

• squeeze out of the tube the amount necessary to cover the area of ​​maximum lesion - usually a column of gel 3 cm long is enough;

• spread over the painful surface evenly, in a thin layer, do not rub;

• let it absorb, leaving it alone for a couple of minutes, then you can cover it with a gauze bandage;

• apply regularly - 2-4 rubles per day, do not exceed the safe daily dose - a maximum of 30 g;

Means for oral administration are prescribed by a doctor. He sets the dosage, methodology and duration of treatment based on the principle of the lowest effective dose Nise and the shortest possible time.

The instruction prescribes taking Nise in the form of tablets and suspensions in accordance with the following scheme:

• it is desirable to combine with a meal or immediately after a meal. Drink the tablets with a sufficient volume of liquid, do not grind, swallow whole. Prepare a suspension from a bag with granules. To do this, pour the contents into a glass and pour 100 ml of clean water;

• the dosage for the elderly and children from 12 years old is similar to the standard adult dose, in the presence of chronic renal failure, halve;

• with pain, fever, severe symptoms of inflammation, 100 mg of Nimesulide (1 tab. or 1 sachet), with painful menstruation - 50 mg. Reception 2 p / day, interval - 12 hours. In severe cases, it is allowed to reduce the interval to 6 hours, but not more than 400 mg / day;

Indications for use

Nise is indicated for the symptomatic treatment of joint diseases, relief of various types of pain, infectious diseases accompanied by fever, inflammation. Relevant for:

• various types of arthritis, incl. rheumatoid, psoriatic;

• tendinitis, tenosynovitis - inflammation of the tendon tissue;

• lumbago - lumbago in the lower back;

• acute pain syndrome with injuries, sprains;

• postoperative, dental, menstrual, headache.

Contraindications, side effects

In addition to the standard requirement to prohibit admission in the presence of nasal polyps, bronchial asthma, individual intolerance to NSAIDs, the instruction prohibits taking Nise in case of:

• erosion, ulcers, gastrointestinal bleeding, other types of blood flow;

Nise is a drug from the group of non-steroidal anti-inflammatory drugs, inhibitors of COX-2.

Release form
Pharmacological effects
Indications and contraindications
Adverse Reactions
Interaction with other medications
Price and reviews

Release form, composition

The active ingredient of the drug is nimesulide. Microcrystalline cellulose, starch, magnesium stearate, silicon dioxide are used as auxiliary components.

Nise is available in the form of tablets (including soluble) for oral administration, suspension, and gel for external application.

Pharmacological effects

Nise is a selective inhibitor of an enzyme that is involved in the formation of prostaglanid, a mediator of inflammation, pain and edema. This drug has a pronounced anti-inflammatory, analgesic, antipyretic effect. The use of nimesulide also contributes to the suppression of platelet aggregation, the release of histamine, and a decrease in the degree of bronchospasm.

Nimesulide also prevents the development of the process of destruction of cartilage tissue, has an antioxidant effect and is involved in the production of elastase and collagenase.

When applied topically, Nise eliminates pain in the area of ​​application of the gel, including joint pain that occurs at rest or when moving, helps to eliminate morning stiffness and eliminates joint swelling.

The drug is excreted through the kidneys and bile.

Indications for use

Before starting to use Nise in any dosage form, the patient should be informed that this drug is used only for symptomatic treatment.

This medication has no effect on the systemic course of the disease.

Indications for the use of Nise in the form of a gel are:

• local symptomatic therapy of the inflammatory process and pain in the joint area;
• complex therapy of arthritis: rheumatoid, psoriatic;
• osteoarthritis and osteochondrosis;
• radiculitis;
• sprains;
• bursitis;
• muscle pains of a rheumatic and non-rheumatic nature;
• soft tissue damage - tears, bruises.

Nise in the form of tablets for oral administration is indicated for use in the following conditions:

• with rheumatoid arthritis;
• articular syndrome;
• with exacerbation of gout;
• with osteochondrosis and osteoarthritis;
• myalgia and spondyloarthritis;
• with inflammation of ligaments and tendons;
• to eliminate pain of various origins (including dental, headache).

In the treatment of diseases of the spine, you can combine the use of drugs in the form of tablets for oral administration and in the form of a gel.

Contraindications

Nise in the form of tablets is contraindicated for use when:

• incomplete combination of polyposis of the nasal sinuses and nose, bronchial asthma and individual intolerance to aspirin (as well as other drugs from the group of non-steroidal anti-inflammatory drugs);
• in the presence of ulcerative lesions of the stomach and duodenum;
• with the development of gastric bleeding;
• with inflammatory diseases of the gastrointestinal tract;
• with diseases of the hematopoietic system;
• in case of development of heart failure;
• with serious violations of the normal functioning of the kidneys and liver;
• under the age of 12.

The drug in the form of tablets with extreme caution is prescribed for ischemic heart disease, angina pectoris, diabetes mellitus, peptic ulcer disease, in old age, and also if the patient is a smoker.

Caution is also required in cases where the patient additionally takes drugs from the group of anticoagulants, corticosteroids, antiplatelet agents.

Application during pregnancy

The use of the drug Nise is contraindicated during the period of bearing a child. In the event that the use of this medication is required during lactation, it is necessary to consider stopping breastfeeding.

Adverse Reactions

The drug Nise, intended for oral administration, can provoke the development of undesirable side reactions:

• heartburn, nausea, vomiting, pain in the intestinal region, the development of ulcerative lesions and other side effects from the gastrointestinal tract;
• headache and dizziness;
• the development of thrombocytopenia, anemia, leukopenia;
• allergic manifestations: itching, urticaria, redness of the skin;
• fluid retention;
• the drug may increase the duration of bleeding.

Nise gel can cause the development of allergic manifestations at the site of application of the drug: itching, urticaria, peeling, discoloration of the skin.

In the event that the patient applies the gel to large areas of the skin, the risk of developing systemic side effects increases.

Interaction with other groups of drugs

The drug Nise can interact with drugs that include digoxin, lithium, with drugs from the group of hypoglycemic agents, diuretics and non-steroidal anti-inflammatory drugs, anticoagulants, antibacterial drugs (cyclosporins), as well as methotrexate.

Mode of application

Nise in the form of a suspension is recommended for use before the main meal. However, in the event that the patient develops discomfort or pain in the abdomen, the drug can be taken after eating.

The drug in the form of tablets for oral administration is recommended to be used after the main meal (including for patients with gastrointestinal diseases), drinking plenty of water. In case of violations of the normal functioning of the kidneys, the maximum daily dosage should not exceed 100 mg. For other categories of patients, the maximum daily dose is 200 mg of the drug.

Nise gel must be applied to a dry, clean skin surface. The drug is applied in a thin layer to the area with the maximum manifestation of pain. You do not need to rub in the drug. Frequency rate of application - up to 4 times a day.

Nise gel can be used for no more than 10 days.

What to do in case of overdose?

To date, there has been no information on cases of overdose with Nise. In case of an accidental overdose, such reactions of the body may develop as an increase in blood pressure, disruption of the normal functioning of the gastrointestinal tract and kidneys, the development of seizures and respiratory depression. In this case, it is recommended to immediately flush the stomach and carry out symptomatic treatment. There is no specific antidote.

Nise is prescribed with caution to patients with a history of impaired renal function and vision problems.

With prolonged use of this medication, systematic monitoring of the condition of the liver and kidneys is required.

In the event that the use of this medication is required in patients of older age groups, then there is no need to adjust the dosage.

Since the use of Nise can contribute to the development of dizziness, then patients whose activities require an increased concentration of attention and a quick psychomotor reaction should be especially careful.

Cost, analogues

The cost of the drug Nise for the period of May 2015 is formed as follows:

• Gel 1%, 20 grams - 160-180 rubles.
• Gel 1%, 50 grams - 260-290 rubles.
• Tablets 10 grams, No. 20 - 200-220 rubles.

Analogs of the drug Nise are the following drugs: Nimica, Nimulid, Nimesil, Aponil.

If replacement is necessary, a preliminary consultation with the attending physician is required.

Reviews

The use of Nise for relieving pain in the lower back has proven to be effective. A pronounced therapeutic effect is observed by the 10th day of taking the drug. In comparison with other drugs from the group of non-steroidal anti-inflammatory drugs, the active component of Nise (nimesulide) completely relieves pain and restores posture with fewer side effects (according to research results - 13 to 21).

Patients with a history of osteoarthritis took this drug and noted a decrease in radicular symptoms and an increase in the volume of active movements. The functional state of the spine also improves, according to the Schober test. The result is a high analgesic and anti-inflammatory activity. All this makes it possible to use Nise in the complex treatment of diseases of the spine with other groups of drugs to eliminate the main symptoms of the disease.

Vera Nikolaevna, doctor

The doctor prescribed oral administration and topical use of the drug to relieve back pain. I am very pleased with this tool. I noted this feature - the local application of the gel allows you to reduce the dosage of tablets and reduces the risk of side effects. The pain syndrome disappears within 10 minutes after applying the drug. If you take another pill, the pain does not make itself felt throughout the day. I use it together with muscle relaxants and nootropic drugs.

Victoria

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Injections and tablets Artrosan - complete instructions for use

Artrozan is an anti-inflammatory, non-steroidal drug. Has a pronounced antipyretic and analgesic effect.

Meloxicam is the active ingredient of the drug.

The effect occurs due to inhibition of the activity of cyclooxygenase-2 (COX-2), less effect on COX-1, which is involved in the synthesis of prostaglandins (PG).

Pharmacokinetics of the drug

The bioavailability of the active ingredient Artrosan is 89%. When taken simultaneously with food, the percentage of absorption does not change. Well absorbed in the gastrointestinal tract.

The maximum concentration is reached in 4-5 hours. The half-life is 12-14 hours.

99% of meloxicam binds to blood plasma proteins.

The difference between the maximum and basal concentration in the body is small and amounts to a ratio (2.5: 1).

Nominal distribution space is 11 liters. The desired plasma concentration at steady state is reached after 3-5 days.

It is excreted equally in urine and feces.

Indications for use

As follows from the instructions, the drug is prescribed for degenerative diseases of the joints, in particular, for the relief of acute and chronic pain.

Suitable for arthritis, ankylosing spondyloarthritis, osteoarthritis.

Contraindications

There is also a fairly large number of contraindications:

• individual hypersensitivity to the components of the drug;
• children under 15;
• renal or hepatic impairment;
• peptic ulcer of the duodenum or stomach, postponed erosive and ulcerative lesions of the gastrointestinal tract;
• aspirin asthma;
• pregnancy, lactation;
• heart failure.

Medication dosage

Instructions for use for injections and tablets Artrozan indicates that the drug can be used orally, rectally, intramuscularly, depending on the form of release.

The dosage is selected individually, the minimum effective dose is found:

• the initial dose is 7.5;
• taken once a day (7.5 - 15 mg) with meals, without chewing;
• rectally - 1 suppository per day;
• when taking tablets and intramuscular injections together, the daily dosage should not exceed 15 mg;

Release form

Tablets are available in this form:

• 10 tablets in a blister, 1/2/3/5 blisters per pack;
• 15 tablets in a blister, 1/2/3 blisters in a package.

Injections: 2.5 ml ampoules 3/5/10 pieces per package.

Suppositories: 7.5-15 mg of active substance in a 25/50/100 mg candle.

The package contains 10 suppositories.

Ointment: 5% ointment in tubes of 30/50 g.

Overdose and additional instructions

In case of an overdose, nausea, bleeding in the gastrointestinal tract, vomiting, asystole, renal and hepatic failure, loss of consciousness, epigastric pain are observed.

Hemodialysis, forced diuresis and alkalization of urine are ineffective in case of an overdose of Artrosan, since it has a high binding capacity with blood proteins.

Side effects

Often (1 in 100) the following side effects occur:

• dyspepsia, nausea, vomiting;
• skin rash, itching;
• dizziness, drowsiness;
• belching;
• anemia.

Sometimes (1 case in 500):

• ulcers of the stomach and duodenum;
• gastrointestinal bleeding;
• noise in ears;
• the formation of an abscess with intramuscular injection;
• palpitations, increased blood pressure;
• exacerbation of bronchial asthma, cough.

Rarely (1 case in 5000):

• photosensitivity;
• erythema multiforme;
• toxic epidermal necrolysis;
• renal medullary necrosis;
• bullous reactions;
• disorientation.

Very rare (1 in 10,000):

• hyperbilrubinemia;
• hyperemia of the face;
• leukopenia;
• esophagitis;
• conjunctivitis.

special instructions

It is undesirable to take Artrosan for smokers, patients with alcohol dependence and drug addiction.

The drug is prescribed with caution in patients with diabetes mellitus, with peripheral arterial pathology.

The medicine reduces blood clotting.

Interaction with alcohol

Serious, unforeseen conditions are possible after taking, in particular, large doses of alcohol, which can be fatal.

Reception for dysfunction of the kidneys and liver

The exacerbation of any kidney or liver disease should be considered when planning the use of the drug. And it is possible only with hemodialysis.

Interaction with other drugs

Drugs of the SSRI group, fibrinolytics, vitamin K antagonists, Heparin increase the risk of bleeding.

It is necessary to take intrauterine contraceptives with caution, as Artrosan can reduce the contraceptive effect.

Artrosan reduces the effectiveness of antihypertensive drugs.

When taken simultaneously with diuretics and cyclosporine, acute renal failure may develop.

Taking Kolestyramine accelerates the elimination of meloxicam from the body.

NSAID drugs increase the risk of gastrointestinal ulceration.

Reception during pregnancy and lactation

TO It is categorically forbidden to take pregnant and lactating women, meloxicam negatively affects the fetus, provokes internal bleeding in the digestive tract, and disrupts the normal functioning of the kidneys.

It is not advisable to take the drug for women planning pregnancy, as they reduce female fertility.

How doctors and patients respond to the drug

We offer to study the feedback of doctors and patients who have used injections or Artrozan tablets.

What patients say

Opinion of doctors

In general, Artrozan is popular among the prescribed anti-inflammatory nonsteroidal drugs for the treatment of arthritis and similar diseases with doctors.

Neurologists highly appreciate the drug in its ability to localize and suppress acute pain.

The dosage should be adjusted or the medication should be canceled only upon prior consultation with a doctor.

It is undesirable to drive a car, or work on site with the necessary increased care.

Pros and cons of the medication

The downside is the shortage in pharmacies of such a form of Artrosan as gel and suppositories, even with their effectiveness, they occupy a very small niche among anti-inflammatory drugs.

Pills almost white with a yellowish tinge, round, biconvex, with a smooth surface.

Excipients: microcrystalline cellulose, corn starch, calcium hydrogen phosphate, sodium starch glycolate, purified talc, magnesium stearate, colloidal anhydrous silicon.

10 pieces. - blisters (1) - cardboard boxes.
10 pieces. - blisters (2) - cardboard boxes.
10 pieces. - blisters (10) - cardboard boxes.

Clinical and pharmacological group

NSAIDs. Selective COX-2 inhibitor

pharmachologic effect

NSAIDs from the sulfonanilide class. Selective inhibitor of COX-2 - an enzyme involved in the synthesis of prostaglandins - mediators of edema, inflammation and pain. The drug has anti-inflammatory, analgesic and antipyretic effects.

Reversibly inhibits the formation of prostaglandin E 2, both in the focus of inflammation and in the ascending pathways of the nociceptive system, including the pathways for conducting pain impulses in the spinal cord.

Reduces the concentration of short-lived prostaglandin H 2, from which prostaglandin E 2 is formed under the action of prostaglandin isomerase. A decrease in the concentration of prostaglandin E 2 leads to a decrease in the degree of activation of prostanoid receptors of the EP type, which is expressed in analgesic and anti-inflammatory effects.

It has a slight effect on COX-1, practically does not interfere with the formation of prostaglandin E 2 from arachidonic acid under physiological conditions, thereby reducing the number of side effects of the drug.

The drug inhibits platelet aggregation by inhibiting the synthesis of endoperoxides and thromboxane A2, inhibits the synthesis of platelet aggregation factor, inhibits the activation of plasminogen 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.

The drug also inhibits the release of tumor necrosis factor alpha, which is responsible for the formation of cytokines.

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 in cartilage tissue.

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

Pharmacokinetics

Suction

After oral administration, nimesulide is well absorbed from the gastrointestinal tract. Food intake reduces the rate of absorption without affecting its extent. C max of nimesulide in blood plasma is reached 1.5-2.5 hours after administration and is 3.5-6.5 mg / l. Undergoes a "first pass" effect through the liver.

Distribution

Plasma protein binding is 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acidic α 1 -glycoproteins - 1%. The dose of the drug does not affect the degree of binding to blood proteins.

V d is 0.19-0.35 l / kg. Penetrates into the tissues of the female genital organs, where after a single dose, the concentration of nimesulide is about 40% of the plasma concentration. It penetrates well into the acidic environment of the inflammation focus (40%), synovial fluid (43%). Easily penetrates the histo-hematological barriers.

Metabolism

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

Withdrawal

T 1/2 - 1.56-4.95 hours, T 1/2 of 4-hydroxynimesulide - 2.89-4.78 hours. The metabolite is excreted by the kidneys (65%) and bile (35%).

Pharmacokinetics in special clinical situations

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

Indications for the use of the drug

- rheumatoid arthritis;

- osteoarthritis;

- arthritis of various etiologies;

- arthralgia;

- myalgia;

- postoperative and post-traumatic pain;

- bursitis;

- tendinitis;

- algodismenorrhea,

- toothache,

- headache.

Dosage regimen

Inside adults appoint 100 mg 2 times / day. The maximum daily dose is 400 mg.

The tablets should be taken with sufficient water, preferably before meals. In the presence of gastrointestinal diseases, it is advisable to take the drug at the end of a meal or after a meal.

Children over 12 years old the drug is prescribed in a single dose of 1.5 mg / kg of the child's body weight 2-3 times / day. The maximum dose is 5 mg / kg / day. Teenagers weighing more than 40 kg the drug is prescribed at 100 mg no more than 2 times / day.

Side effect

From the digestive system: heartburn, nausea, vomiting, diarrhea, gastralgia, erosive and ulcerative lesions of the gastrointestinal tract, increased activity of hepatic transaminases.

From the side of the central nervous system: headache, dizziness.

From the hematopoietic system: thrombocytopenia, leukopenia, anemia, agranulocytosis.

Allergic reactions: skin rash, anaphylactic shock, bronchospasm.

Others: fluid retention, prolonged bleeding time, hematuria.

Contraindications to the use of the drug

- erosive and ulcerative lesions of the gastrointestinal tract in the acute phase;

- bleeding from the gastrointestinal tract;

- "" aspirin "" asthma;

- liver failure;

- severe renal failure (CC<30 мл/мин);

- pregnancy;

- lactation period (breastfeeding);

- children under 12 years old;

- hypersensitivity to the drug.

WITH caution the drug should be prescribed for arterial hypertension, heart failure, type 2 diabetes mellitus (non-insulin dependent).

Use of the drug during pregnancy and lactation

Nise is contraindicated for use during pregnancy.

If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Application for violations of liver function

Contraindicated in liver dysfunction.

Application for impaired renal function

The drug is contraindicated in severe renal failure (CC<30 мл/мин).

special instructions

With prolonged use, systematic monitoring of liver and kidney function is necessary.

When using the drug in elderly patients, correction of the dosage regimen is not required.

Overdose

Currently, cases of an overdose of Nise have not been described. There is no specific antidote.

Drug interactions

Possible manifestations of drug interactions (due to the competition of drugs for binding to proteins) while taking the drug Nise orally with digoxin, phenytoin, lithium drugs, diuretics, antihypertensive drugs, other NSAIDs, cyclosporine, methotrexate, oral hypoglycemic agents.

Conditions of dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

List B. The drug should be stored in a dry, dark place, out of reach of children, at a temperature not exceeding 25 ° C. Shelf life is 3 years.

"

The nonsteroidal anti-inflammatory drug Nise belongs to the sulfonalide class. The selective substance of the enzyme cyclooxygenase-2, which is involved in the synthesis of prostaglandins - neurotransmitters of edema, anti-inflammatory process and soreness. The drug has analgesic, antipyretic effects and stimulates processes aimed at relieving inflammation.

To understand what this drug helps from, you need to know its way of acting on the patient:

Pharmacokinetics

After consumption, it is perfectly absorbed from the gastrointestinal tract, to a greater extent from the intestines. Eating food decreases absorption, but does not affect absorption. It has a penetrating ability into the genitals of a woman's body, where after one use, the content of nimesulide is approximately 40% of that in the blood plasma. It also passes well into the acidic environment of the center of the inflammatory process, periarticular exudate and internal barriers.

The highest concentration in the circulatory system is observed after 2.5 hours, and the connection with protein molecules reaches 95%.

The metabolic process in the body of nimesulide is carried out in the liver. The half-life is about 5 hours. Metabolic products are excreted by the kidneys and with bile secretion.

Composition of the product

Nise composition contains the main active element - nimesulide 100 mg. As additional components are present:

• 75 mg calcium hydrogen phosphate;
• 40 mg MCC;
• 54 mg corn starch;
• 35 mg sodium carboxymethyl starch;
• 3 mg - stearic acid;
• 1 mg talc;
• 2 mg - pyrogenic silicon dioxide.

Methods of use and dosage

Based on the underlying disease, a specific form of this remedy is prescribed.

Pills

For adults, the drug in tablets is prescribed 100 mg 2 times throughout the day. The highest dosage per day is 400 mg. It is advisable to consume at the same hours, approximately 12 hours later in the morning and in the evening.

The suspension is applied before eating, but if there is an uncomfortable condition in the epigastric region, it can be used at the end of a meal or immediately after eating.

In the form of soluble tablets, the product must be consumed after a meal. 1 tablet must be dissolved in 5 ml of water (1 teaspoon).

Dissolved tablets should not be washed down with water or other liquids. If the aftertaste of the medicine is felt after taking, then you can drink a small sip of plain water.

Children from the age of two are recommended to use the medicine in the form of a suspension, from the age of three - in the form of soluble tablets or suspension, from the age of twelve - 100 mg twice a day. The dosage is 3-5 mg / kg of body 2-3 times during the day. The highest dose is 5 mg / kg for 24 hours, which is divided into 2-3 doses. Patients weighing 40 kg or more are recommended 100 mg twice a day.

The highest dosage of this agent is 5 mg / kg body weight in 24 hours. Duration of admission is 10 days.

Gel

Before applying, you need to wash and dry the surface of the skin at the site of application. Apply the gel evenly in a small amount with a strip of approximately 3 cm on the area of ​​severe pain - from 3 to 4 times (but not more) throughout the day, do not rub.

The amount and frequency of use of the gel depends on the area of ​​application on the skin and the patient's response.

The highest dosage is 5 mg / kg throughout the day, but not more than 30 mg. Duration of use - 10 days without consulting a specialist.

Capsaicin (included) can cause a burning sensation and redness of the skin. In isolated cases, the burning sensation does not go away, but it can turn into hypersensitivity of this area of ​​the skin. This is considered a normal reaction and does not require discontinuation of the drug.

When using the gel, you must not allow it to get into the eyes, as well as on the mucous membranes. After using it, you need to tightly close the tube and wash your hands with soap and water.

When rubbing in the gel, a burn may occur on the skin surface, which heals on its own for several days. If irritation occurs, it is necessary to stop using the drug.

During the use of tablets or gel, you must follow the recommendations of a specialist.

Indications for appointment

There are a number of situations where the drug can be used:

The drug is used to combat the symptoms of various diseases. It helps to relieve pain and inflammation, but it does not affect the development of the disease itself.

Contraindications

• bronchial status, chronic nasal or sinus polyposis, allergy to acetylsalicylic acid;
• the presence of ulcers and bleeding in the gastrointestinal tract;
• active diseases of the stomach or intestines;
• poor blood clotting ability;
• heart and kidney failure;
• changes in kidney performance;
• the use of some other drugs;
• excessive consumption of alcohol and drugs;
• the state of bearing the fetus;
• age less than 12 years.

All these factors will interfere with the adequate effect of the drug and can lead to a negative treatment result.

In addition, there are a number of factors that require the drug to be taken with caution:

• pathology in the cardiovascular system;
• diabetes;
• smoking;
• lack of creatinine;
• presumptive data on the presence of gastric and duodenal ulcers;
• abuse of alcohol-containing products;
• concurrent administration of blood clotting drugs.

Side effect

The drug can cause undesirable consequences in the patient, which are manifested due to the use of the drug. These effects include:

Medication overdose

With excessive use of the drug, the patient will have a number of negative factors that indicate an overdose. These effects include: drowsiness, complete indifference and indifference, nausea and vomiting. The formation of bleeding in the stomach, an increase in blood pressure indicators, renal failure and difficulty in breathing are possible.

You need to get rid of these symptoms. It is necessary to deal with the manifestation factors and monitor the patient's condition. No antidote is provided for today. If you notice symptoms of an overdose in the first 4 hours after taking the medicine, then you need to induce a gag reflex to cleanse the stomach, take activated charcoal and laxatives.

Combination with other medicines

If you take a remedy with drugs that worsen blood clotting, then this effect will be more pronounced. Nimesulide is capable of negatively affecting the efficacy of furosemide. Concomitant use with Methotrexate will increase its side effects.

Treatment with this drug together with antidepressants increases the likelihood of ulcers and bleeding in the stomach.

Special instructions

The medication is excreted from the body through the kidneys. Therefore, patients who have impaired function of these organs need to take a reduced dosage. The choice of the exact dose should be made by the doctor.

• If during the course the patient begins to complain of decreased vision, then therapy should be discontinued, and an ophthalmologist should conduct an examination.
• The tool has the ability to retain fluid in the tissues, therefore, those who have hypertension or impaired performance of the cardiovascular system should regularly monitor their condition and, if negative changes are detected, contact a specialist.
• Patients need to regularly consult a doctor if, simultaneously with this remedy, a course of medicines that have an effect on the gastrointestinal tract is carried out.
• If, during the use of Nise, the patient experiences symptoms of impaired liver function, the drug should be discontinued and the healthcare professional should be consulted. It is forbidden to use the medicine at the same time as other non-steroidal anti-inflammatory drugs.
• The drug has the ability to alter the functioning of platelets, but it is not an aspirin replacement therapy for cardiovascular ailments. The course negatively affects the female ability to produce offspring. It should be ruled out if pregnancy is planned.
• When drug treatment lasts more than 14 days, it is necessary to monitor the biochemical parameters of the liver.
• Niza tablets should not be used by children under 12 years of age. However, if there is a special need, children over 7 years old can take other forms of nimesulide.
• Care must be taken in handling complex equipment: the drug causes drowsiness, dizziness and blurry vision.

Release types

• The tablets are sold in a cardboard box. Inside there are 1, 2 or 10 plates, each containing 10 tablets. One tablet weighs 100 mg. Each package of Nise contains instructions for using the drug.
• Soluble tablets contain 50 mg of the main component; they are sold in a pharmacy in 10 pieces in a blister pack.
• The suspension contains 50 mg of the main substance per 5 ml of suspension. Available in 60 ml vials with a cap with a dose scale.
• Gel 1%. 1 mg contains 10 mg of the main component. Produced in 20 gram aluminum tubes.

Conditions of detention and shelf life

This drug belongs to list B. It is required to store Nise in a place protected from sunlight and humidity with a temperature below 25 degrees. Keep out of reach of children.

The shelf life is 3 years from the date of manufacture. Do not use after the expiration date.

Terms of sale

Sold in a retail pharmacy with a prescription.

Nise (NISE, Nice, Nimesulide, Nimesil) is a non-steroidal anti-inflammatory drug (NSAID) of the second generation of inhibitors used to relieve pain syndromes of various etiologies.

Pharmacological action of Nise

The active component of Nise is a specific or highly selective isoform of the enzyme cyclooxygenase (COX) - COX-2, a class of bellows-anilines. The drug has anti-inflammatory, analgesic and antipyretic effects, while it has an improved gastrointestinal safety profile.

According to the instructions, Nise reversibly inhibits (restrains):

• The formation of prostaglandin E2 in the focus of inflammation and in the structures of the central and peripheral nervous system - a decrease in the concentration of E2 inhibits the activity of prostanoid receptors of the EP-type, which gives an anti-inflammatory and analgesic effect;
• Synthesis of endoperoxides and thromboxane A2 - suppresses thrombus formation;
• Release of histamine - reduces the degree of bronchial spasms;
• Synthesis of interleukin-6, urokinase, metalloproteases (collagenase, elastase) - prevents the destruction of proteoglycans and, as a result, the destruction of collagen in cartilage tissue;
• Myeloperoxidase activity - inhibits the formation of oxygen decomposition toxins, gives an antioxidant effect.

The slight effect of Nise on the natural formation of prostaglandin E2 from arachidonic acid allows to reduce the number of side effects. By phosphorylation, Nise activates glucocorticoid receptors. This enhances the anti-inflammatory effect of the drug.

Nise is characterized by a high degree of absorption, while food intake, without affecting the degree of absorption, reduces its speed. The maximum concentration of the drug in the blood plasma is recorded after 1.5-2 hours from admission.

Nise release form

The undoubted advantage of the drug is the various forms of release. This significantly expands the circle of people using the drug and increases the list of painful conditions in which Nise brings relief.

Release forms:

• Nise tablets. Contains 100 mg of nimesulide. In a blister there are 10 pieces;
• Dispersible tablets Nise. Contains 50 mg of nimesulide. In a blister there are 10 pieces;
• Nise oral suspension. Contains 50 mg of nimesulide in 5 ml. 60 ml bottle, special dosing cap;
• Gel Nise 1% for external use. Contains 10 mg of nimesulide in 1 g. Tube 20 g and 50 g.

Nise tablets are recommended for adults in case of pain syndromes of various origins. Suspension Nise is convenient for relieving pain in children. When topical NSAIDs are needed, Nise gel is an excellent choice. The gel does not contain warming components, therefore it is recommended to use it during exacerbations of osteochondrosis, osteoarthritis, radiculitis. According to reviews, Nise gel helps well with inflammation of ligaments and tendons, post-traumatic inflammation of soft tissues, bursitis and bruises.

Indications for use of Nise

Nise, according to the instructions, is indicated for use in the treatment of:

• Arthritis of various etiologies - rheumatoid, psoriatic and ankylosing spondylitis, gout;
• Arthralgia;
• Joint syndrome with exacerbation of gout or rheumatism;
• Myalgia of rheumatic and non-rheumatic origin;
• Bursitis, inflammation of the tendons and ligaments;
• Osteoarthritis, osteochondrosis, radiculopathy;
• Radiculitis, lumbago, sciatica;
• Post-traumatic bruises and inflammations of the musculoskeletal system and soft tissues, tears and sprains of the ligaments;
• Pain syndromes of various origins - traumatic, postoperative, as well as headache and toothache, algodismenorrhea;
• Fevers;
• Infectious and inflammatory diseases.

Contraindications for use

Contraindications to the use of Nise, according to the instructions, are:

• Peptic ulcer of the gastrointestinal tract in the acute phase;
• Liver failure;
• Renal failure;
• Aspirin triad;
• Congestive heart failure;
• Type 2 diabetes mellitus;
• Hypersensitivity to drug components;
• Arterial hypertension;
• Pregnancy, lactation.

The use of the drug in any form is categorically contraindicated in children under the age of 2 years. Children under 12 years old should not take Nise in tablets, but only in the form of a suspension.

It is necessary to use Nise gel only on skin areas with intact epidermis, without dermatoses and various skin infections in the area of ​​application.

Method of application and dosage of Nise

Depending on age, there are various schemes for using Nise:

• Children over 2 years old - suspension at the rate of 3-5 mg per kg of body weight 2-3 times a day, duration of admission - 5 days;
• Children over 3 years old - suspension or dispersible tablets at the rate of 3-5 mg per kg of body weight 2-3 times a day, duration of administration - 5 days;
• Children over 12 years old or weighing more than 40 kg - adult dosage;
• Adults - Nise tablets or dispersible tablets, 100 mg twice a day, maximum (in case of severe pain) - no more than 400 mg per day, duration of administration - 5-10 days.

Suspension and Nise tablets should be taken before meals, if you feel discomfort in the stomach, they can be taken according to the dispersible scheme. Dispersible tablets - dissolve one tablet in a teaspoon (5 ml) of warm water, take at the end of a meal or immediately after a meal.

The surface of the skin should be washed and dried thoroughly before applying the gel. A column of gel about 3 cm is applied to the area of ​​pain, evenly spreading over the surface, but not rubbing. Use 3-4 times a day, the maximum dose is 5 mg per 1 kg of body weight, the duration of use is 10 days.

Side effects of Nise

Nise, according to reviews, can cause various violations:

• Digestive system - nausea, vomiting, heartburn, diarrhea, ulcerative and erosive lesions of the gastrointestinal tract;
• Central nervous system - dizziness, headaches;
• Hematopoietic system - thrombocytopenia, agranulocytosis, anemia;
• Allergic manifestations - bronchospasm, skin rashes, anaphylactic shock.

In places where the gel is applied, local skin reactions are possible (urticaria, itching, redness). Cancellation of the drug is optional.

An overdose of Nise can cause impaired renal function, liver failure, increased blood pressure, respiratory depression, convulsions.

In case of taking other drugs, before taking Nise, you should consult with your doctor. The drug can increase both the effectiveness of other drugs and their toxicity. Nimesulide interacts in the body with digoxin, phenytoin, antihypertensive drugs, diuretics, anticoagulants, other non-steroidal anti-inflammatory drugs, lithium drugs, hypoglycemic agents.

According to reviews, Nise has become very widespread. Many people prefer this drug because it relieves various types of pain and lowers the temperature for a long time. With short-term use, side effects are practically not manifested.