NIMESULIDE

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT NIMESULIDE (NIMESULIDE)

Composition:

Active substance: nimesulide;

1 g of gel contains 10 mg of nimesulide;

Excipients: benzalkonium chloride, propylene glycol, carbomer 980, disodium edetate, sodium hydroxide, purified water.

Pharmaceutical form. Topical gel.

Main physicochemical properties: opaque, homogeneous, light-yellow colored gel.

Pharmacotherapeutic group. Topical non-steroidal anti-inflammatory drugs.

ATC code M02A A26.

Pharmacological Properties

Pharmacodynamics. Nimesulide is a non-steroidal anti-inflammatory drug (NSAID), a selective inhibitor of cyclooxygenase-2. In equimolar concentrations, nimesulide is comparable in anti-inflammatory activity to indomethacin and piroxicam during the initial stages of inflammation. By inhibiting prostaglandin synthesis at the site of inflammation, nimesulide has virtually no effect on the synthesis of regulatory prostaglandins in the gastric mucosa and kidneys. It suppresses the activity of platelet-activating factor, tumor necrosis factor-α, proteases, histamine, and the formation of free oxygen radicals. When applied topically, it reduces or eliminates pain at the site of application, including joint pain, and decreases morning stiffness and joint swelling.

Pharmacokinetics. With topical application, there is a gradual transdermal absorption of nimesulide into subcutaneous tissues and joint synovial fluid. The drug practically does not penetrate into systemic circulation, which explains the absence of significant systemic effects.

Clinical Characteristics

Indications. For local treatment of pathological conditions of the musculoskeletal system characterized by pain, inflammation, and restricted mobility, such as osteoarthritis, periarthritis, post-traumatic tendinitis, tenosynovitis, muscle strains, and heavy physical stress on joints.

Contraindications. Hypersensitivity to nimesulide or to any other components of the medicinal product. Dermatitis and infectious skin diseases. Epidermal damage.

Do not use in patients in whom acetylsalicylic acid or other drugs that inhibit prostaglandin synthesis cause allergic reactions such as rhinitis, urticaria, or bronchospasm.

Do not use during the third trimester of pregnancy.

Interaction with other medicinal products and other forms of interaction. When applied topically, no interactions with other medicinal products have been established. However, it should be borne in mind that if systemic absorption occurs, nimesulide may enhance the efficacy and toxicity of many drugs due to displacement from plasma protein binding sites, thereby increasing their free fraction in the blood. Therefore, the medicinal product should be used with caution when administered concomitantly with anticoagulants, digoxin, phenytoin, lithium-containing drugs, diuretics, antihypertensive agents, other NSAIDs, cyclosporine, methotrexate, and oral hypoglycemic agents.

When several non-steroidal anti-inflammatory drugs are used simultaneously by topical application, local irritation may occur, manifesting as urticaria, erythema, and desquamation.

Glucocorticoids and antirheumatic agents (gold compounds, aminoquinolones) enhance the anti-inflammatory effect of nimesulide.

Special precautions.

Medical supervision is required when prescribing the drug to elderly patients with impaired kidney or liver function, or with congestive heart failure. The drug should also be used under medical supervision in patients with gastroduodenal bleeding, peptic ulcers in the acute stage, or severe blood coagulation disorders.

Do not use simultaneously with other locally applied medicinal products.

The gel should be applied only to intact skin areas, avoiding contact with open wounds. Care should be taken to prevent the gel from entering the eyes or mucous membranes. Do not apply the gel under occlusive dressings.

To minimize the risk of adverse reactions, the lowest effective dose for the shortest necessary duration of treatment should be used. If the patient's condition does not improve, medical advice must be sought immediately.

Do not use in patients with hypersensitivity to NSAIDs. If hypersensitivity reactions occur, treatment should be discontinued.

During treatment, photosensitivity reactions may occur. To reduce the risk of photosensitivity, patients should avoid exposure to UV radiation and avoid using sunbeds.

The medicinal product contains propylene glycol, which may cause skin irritation; and benzalkonium chloride, which may cause irritation and skin reactions.

Use during pregnancy or breastfeeding. Use during pregnancy or breastfeeding is not recommended.

There are no clinical data on the use of Nimesulide during pregnancy. Even though systemic exposure is lower compared to oral administration, it is unknown whether the systemic exposure to Nimesulide achieved after topical application could be harmful to the embryo/fetus. During the first and second trimesters of pregnancy, Nimesulide should not be used unless clearly necessary. If use is required, the dose should be as low as possible and the duration of treatment as short as possible.

During the third trimester of pregnancy, systemic use of prostaglandin synthetase inhibitors, including Nimesulide**, may cause cardiovascular and renal toxicity in the fetus. Prolonged bleeding may occur in both mother and child near the end of pregnancy, and labor may be prolonged. Therefore,** Nimesulide is contraindicated during the last trimester of pregnancy (see section "Contraindications").

Effect on ability to drive or operate machinery. No effect.

Method of Administration and Dosage

Apply externally to adults. Before applying the gel, wash and dry the skin surface. Apply a thin strip of gel approximately 3 cm in length as a thin layer to the affected painful areas and gently rub in. Frequency of application is 3–4 times daily.

The duration of treatment is determined individually depending on therapeutic efficacy and should not exceed 4 weeks.

Children. Do not use in children.

Overdose. Systemic adverse effects characteristic of nimesulide and other nonsteroidal anti-inflammatory drugs may occur when the gel is applied to large areas of skin or when recommended doses are exceeded: dyspepsia, headache, dizziness, epigastric pain.

Treatment: reduce dose or discontinue the drug. Symptomatic therapy.

Adverse Reactions

Skin-related: Local skin irritation of mild to moderate severity: erythema, rash, desquamation, pruritus, allergic reactions.

Immune system-related: Hypersensitivity reactions, including anaphylactic reactions such as angioedema, vasomotor rhinitis, urticaria, and bronchospasm.

Reporting suspected adverse reactions

Reporting of suspected adverse reactions after drug registration is of great importance. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, are encouraged to report all cases of suspected adverse reactions and lack of drug efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 2 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging. 30 g, 40 g, or 100 g in tubes.

One tube containing 30 g, 40 g, or 100 g, packed in a cardboard box.

Availability. Over-the-counter.

Manufacturer. JSC "Lubnipharm".

Manufacturer's address and location of business activity. 16 Barvinkova St., Lubny, Poltava Oblast, 37500, Ukraine.