Nise, gel 1%, 20g

Composition

1 g of gel contains: Active ingredient: Nimesulide 10 mg; Excipients: N-methyl-2-pyrrolidone 250 mg;Propylene glycol 100 mg;Macrogol of 315.5 mg;Isopropanol 100 mg;purified Water 200 mg;Karbomer-940 20 mg;0.2 mg Butylhydroxyanisole;Thiomersal 0.1 mg;Potassium dihydrogen phosphate 0.2 mg;Flavoring (Narcissus-938) 4 mg.

drugs, the

drugs, the analgesic, antipyretic, anti-inflammatory.

Pharmacodynamics

of NSAIDs from the class of sulfonanilides. It is a selective competitive inhibitor of COX-2, inhibits synthesis PG in the focus of inflammation. The inhibitory effect on COX-1 is less pronounced (it is less likely to cause side effects associated with inhibition of PG synthesis in healthy tissues). It has anti-inflammatory, analgesic and antipyretic effects.

Pharmacokinetics

Absorption by mouth is high. Food intake reduces the rate of absorption without affecting its degree. Tmax — 1.5-2.5 h. Plasma protein binding — 95%, erythrocyte binding — 2%, lipoprotein binding — 1%, and acidic alpha_-1-glycoproteins binding-1%. Changing the dose does not affect the degree of binding. _Cmax-3.5-6.5 mg /_l. vd-0.19-0.35 l / kg. Penetrates into the tissues of the female genital organs, where after a single dose, its concentration is about 40% of the plasma concentration. It penetrates well into the acidic environment of the inflammatory focus (40%), synovial fluid (43%). Easily penetrates through histohematic barriers.

It is metabolized in the liver by tissue monooxygenases. The main metabolite,4-hydroxynimesulide (25%), has similar pharmacological activity, but due to a decrease in the size of molecules, it can quickly diffuse along the hydrophobic COX — 2 channel to the active site of the methyl group binding. 4-hydroxynimesulide is a water-soluble compound that does not require glutathione and phase II conjugation reactions (including sulfation, glucuronidation).

T_1/2 of nimesulide is 1.56-4.95 hours,4-hydroxynimesulide is 2.89 — 4.78 hours. 4-hydroxynimesulide is excreted by the kidneys (65%) and with bile (35%), undergoes enterohepatic recirculation.

In patients with renal insufficiency (creatinine clearance 1.8–4.8 l/h or 30-80 ml/min), as well as in children and the elderly, the pharmacokinetic profile of nimesulide does not change significantly.

Indications

• Local symptomatic treatment of inflammatory and degenerative diseases of the musculoskeletal system (for example, osteoarthritis, osteochondrosis with radicular syndrome, sciatica, inflammatory damage to ligaments, tendons, bursitis, sciatica, lumbago).
• Muscle pain of rheumatic and non-rheumatic origin.
• Post-traumatic inflammation of the soft tissues and musculoskeletal system (injuries and ruptures of ligaments, bruises).

Use during pregnancy and lactation

Niaz is contraindicated during pregnancy and lactation.

Contraindications

• Hypersensitivity to nimesulide and components of the drug;
• Erosive and ulcerative lesions of the gastrointestinal tract in the acute stage, bleeding from the gastrointestinal tract, dermatosis, damage to the epidermis and skin infections in the field of application;
• Severe renal (creatinine clearance less than 30 ml / min) or hepatic insufficiency, a history of bronchospasm associated with the use of acetylsalicylic acid or other NSAIDs;
• Pregnancy and lactation;
• Children under 7 years of age.

With caution:

• Liver failure;
• Kidney failure;
• Severe heart failure;
• Arterial hypertension;
• Type 2 diabetes mellitus;
• Elderly and children’s age.

Side effects

Local reactions: pruritus, urticaria, flaking, transient discoloration of the skin (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 “liver” transaminases; headache, dizziness; fluid retention, hematuria; allergic reactions (anaphylactic shock, skin rash); thrombocytopenia, leukopenia, anemia, agranulocytosis, prolongation of bleeding time.

Interaction

With caution, it is used simultaneously with diuretics, blood pressure medications, other painkillers, anti-inflammatory, antidiabetic drugs.

How to take, course of use and dosage

Externally. Before applying the gel, wash and dry the skin surface. Apply a uniform thin layer of gel about 3 cm long to the area of maximum soreness, without rubbing,3-4 times a day. The amount of gel and the frequency of its application (no more than 4 times a day) may vary depending on the size of the treated area and the patient’s reaction. Do not use the gel for more than 10 days without consulting a doctor.

Overdose

Symptoms:  apathy, drowsiness, nausea, vomiting. They are usually reversible with supportive care. It is possible to develop gastrointestinal bleeding, arterial hypertension, acute renal failure, respiratory depression.

Treatment:  symptomatic, supportive care of the patient; if overdose has occurred within the last 4 hours — induction of vomiting, use of activated charcoal (60-100 g per adult), osmotic laxatives. Forced diuresis and hemodialysis are ineffective due to the high level of protein binding. There is no specific antidote to the drug.

Special instructions

The drug is recommended to be applied only to undamaged areas of the skin, avoiding contact with open wounds. Avoid contact with the gel in the eyes and other mucous membranes. Do not use the gel under airtight bandages. After applying the gel, wash your hands with soap and water. Close the tube tightly after using the gel.

Form of production

Gel for external use.

Storage conditions

At a temperature not exceeding 25 ° C. Do not freeze it. Keep out of reach of children!

Shelf

life is 2 years.

Active ingredient

Nimesulide

Dosage form

gel for external use

Description

Children over 7 years of age, For adults, Children as prescribed by a doctor

Indications

Tendon Inflammation, Osteoarthritis, Bursitis, Lumbago, Dislocations and Sprains, Osteochondrosis, Sciatica, Rheumatoid Arthritis, Sciatica, Gout, Arthritis, Myositis, Bruises