Naiz Activgel, gel 1% 50 g

Pharmacotherapeutic group: nonsteroidal anti-inflammatory drug (NSAID)

ATX code: M01AX17

Pharmacological properties

Pharmacodynamics

Contains nimesulide, a nonsteroidal anti-inflammatory drug with local analgesic and anti-inflammatory effect.

Nimesulide is a selective competitive reversible inhibitor of cyclooxygenase type II (endoperoxide-prostaglandin-N₂ synthetase). Reduces the concentration of short-lived prostaglandin H₂, a substrate for kinin-stimulated synthesis of prostaglandin E₂ (mediator of inflammation and pain) in the focus of inflammation. Reducing the concentration of prostaglandin E₂ manifests analgesic and anti-inflammatory effects.

Inhibits also the synthesis of metalloproteases (elastase, collagenase), thus preventing the destruction of proteoglycans and collagen of cartilage tissue.

When applied externally, it relieves or eliminates pain at the site of application, including joint pain at rest and on movement, reduces morning stiffness and joint swelling. Helps increase the amount of movement in the joints.

Pharmacokinetics

After a single application of 28 cm² of Nais^® on the skin surfaceActivgel, gel for external use 1%, at a dose of 40 mg (by nimesulide), the maximum concentration of the active substance in plasma (C_max) was 14.83 ng/ml, the time to reach maximum concentration (T_Cmax) – 11 h and the area under the curve “plasma concentration – time” (AUC) – 195.46 ng*h/ml, were significantly different from the analogous pharmacokinetic parameters (5.35 ng/ml, 16.34 h and 71.07 ng*h/ml, respectively) of the preparation Naïsesup>®, gel for external use 1%, which indicates faster absorption and better relative bioavailability of nimesulide when using the drug Naise^® Activgel.

After a single application on the skin the C_max of nimesulide in plasma is noted by the end of the first day and is significantly (more than 300 times) lower than that of oral forms of nimesulide.

Indications

Local symptomatic treatment of diseases of the musculoskeletal system: joint syndrome, including exacerbation of gout, rheumatic diseases, psoriasis, osteoarthritis; osteochondrosis with radicular syndrome; radiculitis, inflammatory ligament, tendonitis; bursitis; sciatica; lumbago.

Muscular pain of rheumatic and non-rheumatic origin.

Post-traumatic inflammation of soft tissues and musculoskeletal system (ligament injuries and tears, contusions).

The drug is intended as symptomatic therapy, to reduce pain and inflammation at the time of use, has no effect on the progression of the disease.

Active ingredient

Nimesulide

Composition

1 g of the gel contains:

the active ingredient:

nimesulide 10 mg;

excipients: dimethyl sulfoxide, diethylene glycol monoethyl ether, propylene glycol, citric acid monohydrate, Sepineo P 600 (acrylamide/acryloyldimethyl taurate sodium copolymer, isohexadecane, polysorbate 80), “Calm valley” flavoring, purified water.

How to take, the dosage

Externally. Apply only to clean and dry skin.

A column of gel about 3 cm long, apply in an even, thin layer to the area of maximum soreness, without rubbing. Apply 3-4 times a day.

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

Do not use more than 10 days without consulting a physician.

If there is no improvement or new symptoms after treatment, you should talk to your doctor. Use only in the way and with the dose directed.

Interaction

Possible pharmacokinetic interaction of nimesulide with drugs that compete for binding to blood plasma proteins.

Cautious use of nimesulide with digoxin, phenytoin, lithium preparations, diuretics, cyclosporine, methotrexate, other NSAIDs, hypotensive and hypoglycemic agents should be observed.

Before using the gel, consult a physician if you are already using the above drugs or are under a physician’s care.

Special Instructions

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

The application of Naise^® ActiveGel on the skin may cause a burning sensation, which disappears on its own and does not require withdrawal of the drug.

At the time of application and before cleansing the hands, do not touch sensitive areas of the skin. If the gel accidentally comes into contact with mucous membranes or sensitive skin, rinse thoroughly with water. The drug should be used with caution in patients with an increased risk of adverse reactions caused by salicylates.

Close the tube tightly after use.

Impact on ability to drive, operate machinery

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

Synopsis

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

Contraindications

Hypersensitivity to nimesulide and other components of the drug.

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

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

Dermatoses, epidermal lesions and skin infections in the area of application.

Developed renal (creatinine clearance less than 30 ml/min) or hepatic insufficiency.

Pregnancy and breastfeeding.

Children under 12 years of age.

With caution

Hepatic impairment; renal impairment (creatinine clearance above
30-60 ml/min); gastrointestinal erosive ulcers in history (including peptic ulcer and 12 duodenal ulcer); blood clotting disorders (including hemophilia, prolongation of bleeding time, susceptibility to bleeding), bleeding from the gastrointestinal tract in the history; severe heart failure; arterial hypertension; diabetes; childhood age; old age.

Side effects

The drug is generally well tolerated when used externally.

The undesired phenomena presented below are listed according to anatomico-physiological classification and frequency of occurrence. The frequency of adverse events is determined by WHO and is graded as follows: very common (≥1/10), common (≥1/100 and < 1/10), infrequent (≥1/1000 and < 1/100), rare (≥1/10000 and < 1/1000), very rare (< 1/10000, including individual cases), not established.

Skin and subcutaneous tissue disorders: infrequent – itching, very rare – urticaria, peeling; when using topical forms of nimesulide transient changes in skin color are possible (not requiring withdrawal of the drug).

When applying the drug to large areas of the skin or with prolonged use, the development of systemic adverse reactions typical for nimesulide is not excluded: heartburn, nausea, vomiting, diarrhea, gastralgia, gastrointestinal mucosa ulceration, increased activity of “liver” transaminases; headache, dizziness; fluid retention, hematuria; allergic reactions (anaphylactic shock, skin rash); plateletopenia, leukopenia, anemia, agranulocytosis, prolonged bleeding time.

If any of the side effects listed in the instructions worsen, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

Cases of overdose of the drug have not been described. In case of violation of the dosage regimen and application of large amounts of the drug (more than 50 g) on large skin areas, overdose can not be excluded. There is no specific antidote. It is necessary to consult a physician.

Pregnancy use

The drug is contraindicated in pregnancy and during breast-feeding.

Similarities

Naiz, Nimesil, Nimesulide, Nemulex, Nimesulide-TEVA, Nimulide, Nimesan tablets 100 mg 20 pcs, Naisulide, Mialais