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: articular syndrome, including exacerbation of gout, rheumatic diseases, psoriasis, osteoarthritis; osteochondrosis with radicular syndrome; radiculitis, inflammatory damage to ligaments, tendons; bursitis; sciatica; lumbago.

Muscle pain of rheumatic and non-rheumatic origin.

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

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.

Pharmacological effect

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

ATX code: M01AX17

Pharmacological properties

Pharmacodynamics

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

Nimesulide is a selective competitive reversible inhibitor of cyclooxygenase type II (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) at the site of inflammation. A decrease in the concentration of prostaglandin E2 is manifested by an analgesic and anti-inflammatory effect.

It also inhibits the synthesis of metalloproteases (elastase, collagenase), thereby preventing the destruction of proteoglycans and collagen of 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. Helps increase range of motion in joints.

Pharmacokinetics

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

After a single application to the skin, Cmax of nimesulide in the blood plasma is observed at 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.

Special instructions

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

When applying Nise® ActiveGel to the skin, a burning sensation may occur, which goes away on its own and does not require discontinuation of the drug.

While using the drug and before cleansing your hands, you should not touch sensitive areas of the skin. If the gel accidentally gets on 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 adverse reactions caused by salicylates.

Close the tube tightly after use.

Impact on the ability to drive vehicles and machinery

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

Active ingredient

Nimesulide

Composition

1 g of gel contains:

active ingredient:

nimesulide 10 mg;

excipients: dimethyl sulfoxide, diethylene glycol monoethyl ether, propylene glycol, citric acid monohydrate, Sepineo R 600 (sodium acrylamide/acryloyl dimethyl taurate copolymer, isohexadecane, polysorbate 80), Calm Valley flavoring, purified water.

Pregnancy

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

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, damage to the epidermis and skin infections in the area of ​​application.

Severe renal (creatinine clearance less than 30 ml/min) or liver failure.

Pregnancy and breastfeeding period.

Children’s age up to 12 years.

With caution

Liver failure; renal failure (creatinine clearance higher
30-60 ml/min); history of erosive and ulcerative lesions of the gastrointestinal tract (including peptic ulcer of the stomach and duodenum); bleeding disorders (including hemophilia, prolongation of bleeding time, tendency to bleed), history of bleeding from the gastrointestinal tract; severe heart failure; arterial hypertension; diabetes mellitus; childhood; old age.

Side Effects

When used externally, the drug is usually well tolerated.

The adverse events presented below are listed depending on the anatomical and physiological classification and frequency of occurrence. The frequency of side effects is determined by 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.

Disorders 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 cannot be excluded: heartburn, nausea, vomiting, diarrhea, gastralgia, ulceration of the gastrointestinal mucosa, increased activity of “liver” transaminases; headache, dizziness; fluid retention, hematuria; allergic reactions (anaphylactic shock, skin rash); thrombocytopenia, leukopenia, anemia, agranulocytosis, prolongation of bleeding time.

If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.

Interaction

It is possible that nimesulide may interact pharmacokinetically with drugs that compete for binding to plasma proteins.

Caution should be exercised when using nimesulide simultaneously with digoxin, phenytoin, lithium preparations, diuretics, cyclosporine, methotrexate, other NSAIDs, antihypertensive and hypoglycemic agents.

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

Overdose

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

Storage conditions

At a temperature not exceeding 25 °C. Do not freeze.

Keep out of the reach of children!

Shelf life

2 years. Do not use after expiration date.

Manufacturer

Dr. Reddy’s Laboratories Ltd, India