Sulidin (Gel) Instructions for Use

Marketing Authorization Holder

Exeltis Healthcare, S.L. (Spain)

Manufactured By

Exeltis Ilac San. Ve Tic., A.S. (Turkey)

ATC Code

M02AA26 (Nimesulide)

Active Substance

Nimesulide (Rec.INN registered by WHO)

Dosage Form

Sulidin

Gel for external use 1%: tube 30 g

Dosage Form, Packaging, and Composition

30 g – laminated tubes (1) – cardboard packs.

Clinical-Pharmacological Group

NSAIDs for external use

Pharmacotherapeutic Group

NSAID

Pharmacological Action

Nimesulide N-(4-nitro-2-phenoxyphenyl) methanesulfonamide is a non-steroidal anti-inflammatory drug of the sulfanilide class, a selective inhibitor of cyclooxygenase type 2 (COX-2). It practically does not block the activity of COX-1. It has a pronounced anti-inflammatory, analgesic, and antipyretic effect.

In terms of efficacy, it is comparable to indomethacin, diclofenac, ibuprofen, and piroxicam, but causes side effects significantly less frequently. Furthermore, it inhibits the formation of superoxide radicals by stimulated polymorphonuclear leukocytes, binds free radicals, inhibits integrin activation, inhibits the synthesis of platelet-activating factor, prevents the stimulation of nerve endings by bradykinin, suppresses the release of tumor necrosis factor-alpha (TNF-α), the release of histamine from mast cells, suppresses the activity of proteases (elastase, collagenase), and prevents damage to the cartilage matrix by inhibiting the synthesis of metalloproteinase.

Pharmacokinetics

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

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

With prolonged external use, 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 taken orally at an average daily dose (200 mg/day).

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

Indications

Local therapy for conditions characterized by pain, inflammation, and muscular or joint rigidity, such as

• Osteoarthritis;
• Periarthritis;
• Tendinitis;
• Tenosynovitis;
• Bursitis;
• Lumbago;
• Muscle strain, ligament strain and other post-traumatic conditions of the musculoskeletal system.

ICD codes

Dosage Regimen

The drug is intended for external use only.

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

The gel should not be rubbed in intensively or used under occlusive dressings. It is recommended to avoid wearing tight clothing. Hands should be washed 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 for children under 12 years of age have not been established.

Adverse Reactions

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 on large areas): heartburn, nausea, vomiting, diarrhea, gastralgia, ulceration of the gastrointestinal mucosa, headache, dizziness; fluid retention, allergic reactions (skin rash, anaphylactic shock); thrombocytopenia, leukopenia, anemia, agranulocytosis; increased activity of “liver” transaminases; prolongation of bleeding time; hematuria.

In case of adverse reactions, it is necessary to discontinue the use of the drug and prescribe appropriate treatment.

Contraindications

The use of the drug Sulidin is contraindicated

• In case of hypersensitivity to any component of the drug or to other NSAIDs;
• In patients in whom acetylsalicylic acid preparations or other inhibitors of prostaglandin synthesis cause allergic reactions such as rhinitis, urticaria, or bronchospasm;
• In case of skin damage or presence of signs of local infection at the intended site of application;
• With simultaneous use of other topical medicines;
• In children under 12 years of age.

With caution. History of gastrointestinal bleeding, erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, severe renal/hepatic insufficiency, severe blood clotting disorders, uncontrolled chronic heart failure.

Use in Pregnancy and Lactation

Nimesulide is not used during pregnancy and breastfeeding.

Studies of the safety and efficacy of the drug use during pregnancy and breastfeeding have not been conducted. There are no data on the effect on fetal development.

Use in Hepatic Impairment

With caution: severe hepatic insufficiency.

Use in Renal Impairment

With caution: severe renal insufficiency.

Pediatric Use

Recommendations and indications for the use of the drug in pediatric practice for children under 12 years of age have not been established.

Special Precautions

The gel should not be applied to mucous membranes, eyes, damaged and infected skin areas, areas affected by skin diseases, and open wounds.

An intense burning sensation may occur when applying the drug, which disappears within a few days. During the application of the drug and until hands are cleaned, one should not touch sensitive areas of the skin. If the gel accidentally gets on mucous membranes or sensitive areas of the skin, these areas should be rinsed with plenty of water.

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

Experimental studies have not revealed a mutagenic effect of nimesulide, and no data were obtained on the effect of nimesulide on lymphocyte chromosomes in vitro and on interaction with H-thymidine of cultured human lymphocytes.

Effect on ability to drive vehicles and operate machinery. Taking Sulidin does not affect the ability to drive vehicles and operate machinery.

Overdose

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

Drug Interactions

With external use, Nimesulide does not cause a clinically significant effect on the metabolism of other drugs.

Storage Conditions

At a temperature not exceeding 25°C (77°F). Keep out of reach of children.

Shelf Life

Shelf life . 2 years. Do not use after the expiration date.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.