Instruction for use: Sulidin

Active substance Nimesulide

ATX code M02AA Non-steroidal anti-inflammatory drugs for topical use

Pharmacological group

Other non-narcotic analgesics, including non-steroidal and other anti-inflammatory drugs

Composition

Gel for external use 1 g

active substance:

nimesulide 10 mg

auxiliary substances: diethylene glycol monoethyl ether - 687.5 mg; glyceryl monooleate - 290 mg; giprolose - 12.5 mg

Description of dosage form

Homogeneous gel of light yellow color with a characteristic smell.

pharmachologic effect

Pharmacological action - anti-inflammatory, analgesic.

Pharmacodynamics

Nimesulide - N- (4-nitro-2-phenoxyphenyl) methanesulfonamide - NSAID-class sulfanilides, selective inhibitor of COX-2. Virtually does not block the activity of COX-1.

Has a pronounced anti-inflammatory, analgesic and antipyretic effect. It is comparable in effectiveness to indomethacin, diclofenac, ibuprofen and piroxicam, but it is much less likely to cause side effects. In addition, it inhibits the formation of superoxide radicals by stimulated polymorphonuclear leukocytes, binds free radicals, inhibits activation of integrin, inhibits the synthesis of platelet activation factor, prevents the stimulation of nerve endings with bradykinin, inhibits the release of TNF-α, releases histamine from mast cells, inhibits protease activity (elastase , collagenase), prevents damage to the cartilage matrix by inhibiting the synthesis of metalloproteases.

Pharmacokinetics

The gel is quickly absorbed into the underlying tissues, enters the synovial fluid.

After a single external application in a dose of 200 mg of Cmax, nimesulide in plasma reaches 9.77 ng / ml of blood and is observed after 24 hours.

With prolonged external application, the concentration of nimesulide on the 8th day in blood plasma is (37.25 ± 13.25) ng / ml, which is 100 times less than when ingested at an average daily dose (200 mg / day).

Five hours after the application of the gel, the concentration of the main active metabolite (4-hydroxynimidesulide) in the blood plasma does not exceed 100 μg / l.

Indications

Local therapy for conditions characterized by pain, inflammation and muscle or joint rigidity:

osteoarthritis;

periarthritis;

tendonitis;

tenosynovitis;

bursitis;

lumbago;

stretching of muscles, ligaments and other post-traumatic states of the musculoskeletal system.

Contraindications

hypersensitivity to any component of the drug or to other NSAIDs;

Patients in whom acetylsalicylic acid preparations or other inhibitors of PG synthesis cause allergic reactions such as rhinitis, urticaria, or bronchospasm;

damage to the skin or signs of local infection at the site of the intended application;

simultaneous use of other topical drugs;

children's age is less than 12 years.

With caution: bleeding from the gastrointestinal tract in an anamnesis, erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, severe renal / hepatic insufficiency, severe disorders of the blood coagulation system, uncontrolled chronic heart failure.

pregnancy and lactation

Nimesulide is not used in pregnancy and breastfeeding. Studies of the safety and efficacy of the drug during pregnancy and during breastfeeding have not been conducted.

There are no data on the effect on fetal development.

Side effects

With external use, nimesulide is usually well tolerated.

Local reactions: moderate or severe skin irritation, hyperemia, rash, desquamation, itching.

Systemic reactions (with prolonged use or use in large areas): heartburn, nausea, vomiting, diarrhea, gastralgia, ulceration of the mucous membrane of the gastrointestinal tract, headache, dizziness; fluid retention, allergic reactions (skin rash, anaphylactic shock); Thrombocytopenia, leukopenia, anemia, agranulocytosis; increased activity of hepatic transaminases; prolonged bleeding time; hematuria.

In case of adverse reactions, discontinue use of the drug and prescribe appropriate treatment.

Interaction

With external use, nimesulide does not cause clinically significant effects on the metabolism of other drugs.

Dosing and Administration

Outwardly.

Approximately 3 cm of the gel is applied a thin layer on a clean and dry patch of skin over the painful area 3-4 times a day.

Do not rub the gel intensively or use under occlusive dressings. It is recommended that you avoid wearing crushing clothing. Wash hands before and after the procedure.

The duration of therapy is determined individually and averages 7-15 days.

Use in children under 12 years. Recommendations and indications for the use of the drug in pediatric practice in children under 12 years are not established.

Overdose

Cases of drug overdose with external application have not been described.

special instructions

Do not apply gel on mucous membranes, eyes, damaged and infected skin areas affected by skin diseases of the area and open wounds.

When applying the product, an intense burning sensation can occur, which disappears for several days. During the application of the drug and before cleaning hands should not touch sensitive areas of the skin. If you accidentally hit the gel on the mucous membranes or sensitive areas of the skin, you should rinse these areas with plenty of water.

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

The mutagenic effect of nimesulide was not revealed in experimental studies, nor were the data on the influence of nimesulide on the chromosome of lymphocytes in vitro and on the interaction with H-thymidine of cultured human lymphocytes.

Impact on the ability to drive and work with machinery. Does not affect.

Form of issue

Gel for external use 1%. 30 g of gel in laminated tubes, sealed with a membrane and sealed with a screw-on white propylene cap. One tube is put in a cardboard box.

Conditions of leave from pharmacies

On prescription.

storage Conditions

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life

2 years.

Do not use after the expiry date printed on the package.