Nimesulide gel 1%, 20g

Composition

Per 100 g:

Active ingredient:

nimesulide – 1.00 g;

Auxiliary substances:

methylpyrrolidone-25.00 g,

isopropanol-10.00 g,

propylene glycol-10.00 g,

carbomer-1.20 g,

macrogol-400-31.55 g,

lavender oil-0.25 g,

trometamol-0.09 g,

water-up to 100.00 g.

* Note. If necessary, to achieve the optimal pH of the gel, it is allowed to change the trometamol content in the range from 0.02 g to 0.15 g per 100 g.

Pharmacological action

Pharmacotherapy group:  NSAID Code ATX: M01axPharmacodynamics :

Nimesulide Gel is a non-steroidal anti-inflammatory drug (NSAID) It has a local analgesic and anti-inflammatory effect.

Nimesulide is a selective competitive reversible cyclooxygenase type II (endoperoxide-prostaglandin-H2 synthetase) inhibitor. Reduces the concentration of short-lived prostaglandin H 2, a substrate for kinin-stimulated prostaglandin E 2 synthesis in the inflammatory focus. Reducing the concentration of prostaglandin E2 (a mediator of inflammation and pain) reduces the activation of prostanoid EP-type receptors, which is manifested by analgesic and anti-inflammatory effects.

When applied topically, it relieves or disappears pain at the site of application of the gel, including joint pain at rest and during movement, reduces morning stiffness and swelling of the joints. Helps to increase the volume of movement.

Pharmacokinetics:

When applying the gel, the concentration of the Active ingredient in the systemic circulation is extremely low. The maximum concentration after a single application is noted by the end of the first day, its value is more than 300 times lower than that for oral dosage forms of nimesulide. No traces of the main metabolite of nimesulide,4 – hydroxynimesulide, were found in the blood.

Indications

Local symptomatic treatment of inflammatory and degenerative diseases of the musculoskeletal system (osteoarthritis osteochondrosis with radicular syndrome sciatica inflammatory tendon ligament damage bursitis sciatica lumbago).

Muscle pain of rheumatic and non-rheumatic origin.

Post-traumatic inflammation of the soft tissues and musculoskeletal system (injuries and torn ligaments bruises).

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

Use during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Contraindications

Hypersensitivity to nimesulide and its components.

Complete or incomplete combination of bronchial asthma angioedema or urticaria recurrent nasal and paranasal sinus polyposis and intolerance to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs (including in the anamnesis).

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

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

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

Pregnancy and breast-feeding period children under 12 years of age.

With caution:

Hepatic insufficiency; renal insufficiency (creatinine clearance 30-60 ml/min); erosive and ulcerative lesions of the gastrointestinal tract in the anamnesis (including peptic ulcer of the stomach and duodenum 12); blood clotting disorders (including hemophilia prolongation of bleeding time tendency to bleed) bleeding from the gastrointestinal tract in the anamnesis; severe heart failure arterial hypertension; diabetes mellitus 2 type; elderly and children’s 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 common (> 1/10) (>>1/100 >><1/10) (>1/1000 <1/10) (><1/100) (>1/10000 <1/100) (><1/1000) (

Skin and subcutaneous tissue disorders: infrequently-pruritus; very rarely-urticaria peeling transient skin discoloration (not requiring discontinuation of the drug).

If you experience any adverse reactions, you should stop using the drug and consult your doctor.

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

Interaction

Pharmacokinetic interaction with drugs competing for binding to plasma proteins is not excluded.

Caution should be exercised when nimesulide is co administered with digoxin phenytoin lithium preparations diuretics cyclosporine methotrexate other NSAIDs antihypertensive and antidiabetic agents.

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

How to take, course of use and dosage

Externally. Before applying the gel, wash and dry the skin surface.

For adults and children over 12 years of age, apply a uniform thin layer of gel approximately 3 cm long to the area of maximum soreness without rubbing 3-4 times a day.

Do not rub the gel intensively or use it under an occlusal dressing.

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

Overdose

Cases of overdose of the drug are not described. However, when applying large amounts of gel (exceeding 50 g) to large areas of the skin, overdose is not excluded. There is no specific antidote. You should consult a doctor.

Description

Light yellow or yellow transparent gel with a specific smell.

Special instructions

Do not apply the gel to the mucous membranes of the eye damaged and infected skin areas affected by skin diseases areas and open wounds.

When applying the drug, there may be an intense burning sensation that disappears within a few days. During the application of the drug and before cleaning your hands, do not touch sensitive areas of the skin. If the gel accidentally gets on the mucous membranes or sensitive areas of the skin, wash these areas with plenty of water.

The gel should be used with caution in patients with an increased risk of adverse reactions caused by salicylates.

Do not use the drug under an occlusive dressing.

Influence on the ability to drive vehicles and mechanisms:

The drug does not affect the ability to drive a car or other mechanical means.

Form of production

Gel for external use 1%.

Storage conditions

Store in a dark place at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf

life is 2 years.

Do not use after the expiration date.

Active ingredient

Nimesulide

Dosage form

gel for external use