Nise Active gel for external use 1%, 50g

• Local symptomatic treatment of diseases of the musculoskeletal system: articular syndrome, including exacerbation of gout, rheumatic diseases, psoriasis, osteoarthritis: osteochondrosis with radicular syndrome; sciatica, inflammation of the ligaments, tendons; bursitis; sciatica: lumbago.

• Muscle pains of rheumatic and non-rheumatic origin.

• Post-traumatic inflammation of soft tissues and musculoskeletal system (damage and rupture of ligaments, bruises).

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

Outwardly. Apply only to cleansed and dry skin.

Apply a column of gel, approximately 3 cm long, in an even thin layer on the area of ??maximum pain without rubbing. Apply 3-4 times a day.

Do not rub the gel intensively or apply it under an occlusive dressing.

Do not use the drug for more than 10 days without consulting a doctor.

If after treatment there is no improvement or new symptoms appear, you should consult your doctor. Use the drug only according to the method of administration and in the doses indicated in the instructions.

1 g of gel contains:

active substance: nimesulide 10 mg;

excipients: dimethyl sulfoxide, diethylene glycol monoethyl ether, propylene glycol, citric acid monohydrate, Sepineo P 600 (copolymer of acrylamide / acryloyyl dimethyl taurate sodium, isohexadecane, polysorbate 80). aromatizer 'Kalm Valley', purified water.

• Hypersensitivity to nimesulide and other components of the drug.

• Complete or incomplete combination of bronchial asthma, angioedema or urticaria, recurrent polyposis of the nose and paranasal sinuses, and intolerance to acetylsalicylic acid and other NSAIDs (including a history).

• Erosive and ulcerative lesions of the gastrointestinal tract in the acute stage, bleeding from the gastrointestinal tract.

• Dermatoses, epidermal damage and skin infections in the area of ??application. Severe renal (creatinine clearance less than 30 ml / min) or hepatic impairment.

• Pregnancy and the period of breastfeeding.

• Children under 12 years of age.

Carefully

Liver failure: renal failure (creatinine clearance above 30-60 ml / min); history of erosive and ulcerative lesions of the gastrointestinal tract (including gastric ulcer and 12 duodenal ulcer); bleeding disorders (including hemophilia, prolongation of bleeding time, tendency to bleeding), history of bleeding from the gastrointestinal tract: severe heart failure: arterial hypertension: diabetes mellitus: childhood; elderly age.

Trade name:

NiseЃ Activegel

International non-proprietary name:

nimesulide

Dosage form:

gel for external use

Composition

1 g of gel contains:

active substance: nimesulide 10 mg;

excipients: dimethyl sulfoxide, diethylene glycol monoethyl ether, propylene glycol, citric acid monohydrate, Sepineo P 600 (copolymer of acrylamide / acryloyyl dimethyl taurate sodium, isohexadecane, polysorbate 80). aromatizer 'Kalm Valley', purified water.

Description

Homogeneous transparent gel from colorless to pale yellow in color with a characteristic odor.

Pharmacotherapeutic group:

non-steroidal anti-inflammatory drug (NSAID)

ATX code:

M01AX17

Pharmacological properties

Pharmacodynamics
Contains nimesulide, a non-steroidal anti-inflammatory agent that has a local analgesic and anti-inflammatory effect.

Nimesulide is a selective competitive reversible type II cyclooxygenase inhibitor (endoperoxide prostaglandin H2 synthetase). Reduces the concentration of short-lived prostaglandin H2, a substrate for kinin-stimulated synthesis of prostaglandin E2 (a mediator of inflammation and pain) in the inflammation focus. A decrease in the concentration of prostaglandin E2 is manifested by analgesic and anti-inflammatory effects.

It also inhibits the synthesis of metalloproteases (elastase, collagenase), thereby preventing the destruction of proteoglycans and collagen in cartilage tissue.

When applied externally, it causes a weakening or disappearance of pain at the site of application, including pain in the joints at rest and during movement, reduces morning stiffness and swelling of the joints. Promotes increased range of motion in the joints.

Pharmacokinetics
After a single application to the skin surface with an area of ??28 cm2 of NiseЃ Activegel, gel for external use 1%, at a dose of 40 mg (according to nimesulide), the maximum concentration of the active substance in plasma (Cmax) is 14.83 ng / ml, the time to reach maximum concentration (Tcmax) -11h and the area under the plasma concentration-time curve (AUC) - 195.46 ngh / ml, significantly differed from similar pharmacokinetic parameters (5.35 ng / ml, 16.34 h and 71.07 ngh / ml respectively) of the drug NiseЃ, gel for external use 1%. which indicates a faster absorption and better relative bioavailability of nimesulide when using NiseЃ Activegel.

After a single application to the skin, Cmax of nimesulide in blood plasma is noted by the end of the first day and is significantly (more than 300 times) lower than the same indicator for oral forms of nimesulide.

No traces of the main metabolite of nimesulide, 4-hydroxynimesulide, are found in the blood.

Indications for use

Local symptomatic treatment of diseases of the musculoskeletal system: articular syndrome, including exacerbation of gout, rheumatic diseases, psoriasis, osteoarthritis: osteochondrosis with radicular syndrome; sciatica, inflammation of the ligaments, tendons; bursitis; sciatica: lumbago.

Muscle pains of rheumatic and non-rheumatic origin.

Post-traumatic inflammation of soft tissues and musculoskeletal system (damage and rupture of ligaments, bruises).

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

Contraindications

Hypersensitivity to nimesulide and other components of the drug.

Complete or incomplete combination of bronchial asthma, angioedema or urticaria, recurrent polyposis of the nose and paranasal sinuses, and intolerance to acetylsalicylic acid and other NSAIDs (including a history).

Erosive and ulcerative lesions of the gastrointestinal tract in the acute stage, bleeding from the gastrointestinal tract.

Dermatoses, epidermal damage and skin infections in the area of ??application. Severe renal (creatinine clearance less than 30 ml / min) or hepatic impairment.

Pregnancy and the period of breastfeeding.

Children under 12 years of age.

Carefully

Liver failure: renal failure (creatinine clearance above 30-60 ml / min); history of erosive and ulcerative lesions of the gastrointestinal tract (including gastric ulcer and 12 duodenal ulcer); bleeding disorders (including hemophilia, prolongation of bleeding time, tendency to bleeding), history of bleeding from the gastrointestinal tract: severe heart failure: arterial hypertension: diabetes mellitus: childhood; elderly age.

Application during pregnancy and during breastfeeding

The use of the drug during pregnancy and during breastfeeding is contraindicated.

Method of administration and dosage

Outwardly. Apply only to cleansed and dry skin.

Apply a column of gel, approximately 3 cm long, in an even thin layer on the area of ??maximum pain without rubbing. Apply 3-4 times a day.

Do not rub the gel intensively or apply it under an occlusive dressing.

Do not use the drug for more than 10 days without consulting a doctor.

If after treatment there is no improvement or new symptoms appear, you should consult your doctor. Use the drug only according to the method of administration and in the doses indicated in the instructions.

Side effect

When used externally, the drug is usually well tolerated.

The adverse events presented below are listed depending on the anatomophysiological classification and frequency of occurrence. The incidence of side effects is determined by the WHO and has the following gradation: very often (1/10), often (1/100 and <1/10), infrequently (1/1000 and <1/100). rarely (1/10000 and <1/1000), very rarely (<1/10000, including isolated cases), not established.

Violations of the skin and subcutaneous tissues: infrequently - itching, very rarely - urticaria, peeling: when using local forms of nimesulide, a transient change in skin color is possible (not requiring discontinuation of the drug).

When applying the drug to large areas of the skin or with prolonged use, the development of systemic adverse reactions characteristic of nimesulide is not excluded: heartburn, nausea, vomiting, diarrhea, gastralgia. ulceration of the mucous membrane of the gastrointestinal tract. increased activity of 'hepatic' transaminases; headache, dizziness; fluid retention, hematuria: allergic reactions (anaphylactic shock, skin rash): thrombocytopenia, leukopenia, anemia, agranulocytosis, prolonged bleeding time.

If any of the side effects indicated in the instructions are aggravated, or you notice any other side effects that are not indicated in the instructions, inform your doctor.

Overdose

Cases of drug overdose have not been described. If the dosage regimen is violated and large amounts of the drug (exceeding 50 g) are applied to large areas of the skin, an overdose may develop. There is no specific antidote. You need to see a doctor.

Interaction with other medicinal products

The pharmacokinetic interaction of nimesulide with drugs competing for the connection with blood plasma proteins is not excluded.

Care should be taken with the simultaneous use of nimesulide with digoxin, phenytoin. lithium preparations. diuretics. cyclosporine, methotrexate, other NSAIDs, antihypertensive and hypoglycemic agents.

Before using the gel, you should consult with your doctor if you are already using these products or are under medical supervision.

special instructions

The preparation does not leave a visible trace after application. The gel should not be applied to the mucous membranes of the eyes, damaged and infected skin areas, areas affected by skin diseases and open wounds.

When NiseЃ Activegel is applied to the skin, a burning sensation may occur, which disappears on its own and does not require discontinuation of the drug.

During the use of the drug and before cleaning the hands, do not touch sensitive areas of the skin. In case of accidental contact of the gel on the mucous membranes or sensitive areas of the skin, rinse them thoroughly with water. The drug should be used with caution in patients with an increased risk of developing adverse reactions caused by salicylates.

Close the tube tightly after use.

Influence on the ability to drive vehicles, mechanisms

The drug does not affect the ability to drive vehicles or operate machinery.

Release form

Gel for external use 1%.
20 g, 50 g or 100 g in a laminated aluminum tube equipped with a membrane to control the first opening. Each tube, together with instructions for use, is placed in a cardboard box.

Storage conditions

At a temperature not higher than 25 ? C. Do not freeze.
Keep out of the reach of children!

Shelf life

2 years. Do not use after the expiration date.

Vacation conditions

Available without a prescription.