Artrokol

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

Composition:

Active substance: ketoprofen;

1 g of gel contains ketoprofen 25 mg;

Excipients: carbomer 980, triethanolamine, 96% ethanol, methylparaben (E 218), purified water.

Pharmaceutical form. Gel.

Main physicochemical properties: clear, colorless, homogeneous gel with a faint odor of alcohol.

Pharmacotherapeutic group.

Non-steroidal anti-inflammatory drugs for topical use. ATC code M02A A10.

Pharmacological properties.

Pharmacodynamics.

Ketoprofen belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs), derivatives of arylpropionic acid. Its mechanism of action is associated with inhibition of prostaglandin synthesis. It exerts local analgesic, anti-inflammatory, and anti-exudative effects.

Pharmacokinetics.

Plasma and tissue levels of ketoprofen were measured in 24 patients undergoing knee surgery. After repeated topical application of ketoprofen in gel form, its plasma concentration was approximately 60 times lower (9–39 ng/g) compared to a single oral dose of ketoprofen (490–3300 ng/g). The tissue concentration of ketoprofen at the site of application was within a similar concentration range for both the gel and oral formulations; however, the gel showed significantly higher inter-individual variability.

The bioavailability of ketoprofen after topical application is approximately 5% of that after oral administration (based on urinary excretion data).

The extent of plasma protein binding is approximately 99%. Ketoprofen is primarily excreted by the kidneys in the form of a glucuronide conjugate.

Clinical characteristics.

Indications.

• Relief of acute painful conditions of the musculoskeletal system caused by injury, such as sports injuries, dislocations, sprains, and contusions.
• Pain associated with mild arthritis.

Contraindications.

• Known hypersensitivity reactions, such as bronchial asthma symptoms or allergic rhinitis, occurring after use of ketoprofen, fenofibrate, tiaprofenic acid, acetylsalicylic acid, or other NSAIDs.
• Hypersensitivity to other components of the medicinal product.
• History of photosensitization reactions.
• History of skin allergic reactions upon exposure to dexketoprofen, ketoprofen, tiaprofenic acid, fenofibrate, ultraviolet (UV) light blockers, or perfumes.
• Exposure to sunlight (even diffused light) or UV irradiation in solarium during treatment and within 2 weeks after discontinuation of the medicinal product.
• Use in the presence of skin pathological conditions such as eczema or acne.
• Application to infected skin, open wounds, mucous membranes, anal or genital areas, eyes, or under occlusive dressings.
• Use during the third trimester of pregnancy.

Interaction with other medicinal products and other forms of interaction.

Systemic absorption of ketoprofen following topical application is very low; therefore, drug interactions are unlikely.

There have been no reports of interactions with other medicinal products; however, the following interactions have been observed with oral formulations of ketoprofen or other NSAIDs.

Serious interactions have been reported when NSAIDs, including ketoprofen, are used concomitantly with methotrexate.

Special precautions for use

The medicinal product should be used with caution in patients with cardiac, hepatic, or renal impairment. There have been reports of isolated cases of systemic adverse reactions related to kidney injury.

Topical application of large amounts of ketoprofen may lead to systemic effects such as hypersensitivity and bronchial asthma. Patients with bronchial asthma in combination with chronic rhinitis, chronic sinusitis, and/or nasal polyps have a higher risk of developing allergy to acetylsalicylic acid and/or NSAIDs than the general population.

Serious skin reactions, including Stevens–Johnson syndrome, have been reported in association with the use of NSAIDs, including ketoprofen gel. Patients using the medicinal product should be informed about the signs and symptoms of serious skin reactions. At the first appearance of skin rash, mucosal lesions, or any other signs of hypersensitivity, use of the medicinal product should be discontinued immediately.

The recommended duration of treatment should not be exceeded, as the risk of developing contact dermatitis and photosensitization reactions increases over time.

In addition, the following precautionary measures should be observed during use of the medicinal product:

• Hands should be thoroughly washed after each application of the gel;
• If any skin reactions occur, including those associated with concomitant use of medicinal products containing octocrylene (some cosmetic or hygiene products), use should be stopped immediately;
• The gel should not be applied under occlusive dressings;
• The gel must not be applied to mucous membranes or into the eyes;
• The gel should not be applied near open flames, as it contains alcohol;
• The gel must not be diluted.

Exposure to sunlight (even on cloudy days) or ultraviolet (UV) radiation in sunbeds during topical application of ketoprofen may cause potentially serious skin reactions (photosensitization). To prevent photosensitization reactions, clothing should be used to cover the areas of skin to which the gel has been applied during treatment and for 2 weeks after discontinuation of treatment. Sunbeds should also be avoided during treatment and for 2 weeks after stopping the gel.

The product contains ethanol; however, no special precautions related to the dose or route of administration of ethanol are required.

The medicinal product contains methylparaben (E 218), which may cause allergic reactions (possibly delayed).

Use during pregnancy or breastfeeding

First and second trimesters of pregnancy

No embryotoxic effects have been observed in animals. There are no clinical data on the use of topical forms of ketoprofen during pregnancy. Even though systemic exposure is lower than with oral administration, it is unknown whether the systemic exposure to ketoprofen achieved after topical application could be harmful to the embryo/fetus. During the first and second trimesters of pregnancy, the medicinal product should not be used except in cases of extreme necessity. If used, the dose should be as low as possible and the duration of treatment as short as possible.

Third trimester of pregnancy

During the third trimester of pregnancy, systemic use of prostaglandin synthetase inhibitors, including ketoprofen, may cause cardiopulmonary and renal toxicity in the fetus. Prolonged bleeding may occur in both mother and child towards the end of pregnancy, and labor may be prolonged. Therefore, the use of this medicinal product is contraindicated during the third trimester of pregnancy (see section "Contraindications").

Period of breastfeeding

Ketoprofen passes into breast milk in minimal amounts. The medicinal product should not be used during breastfeeding.

Ability to affect reaction speed when driving or operating machinery

There are no data on the effect of topical ketoprofen on the ability to drive or operate machinery.

Method of Administration and Dosage

The medicinal product is intended for topical application (on the skin).

Apply the gel as a thin layer to the affected area of skin 2–4 times daily and gently rub in until completely absorbed. The usual recommended dose is 15 g (14 cm of gel corresponds to 7.5 g). The duration of treatment is 7 days.

Elderly Patients

There are no specific dosage recommendations for elderly patients.

Children

The medicinal product must not be used in children.

Overdose

Overdose is unlikely with topical (cutaneous) application.

In case of accidental ingestion of the gel, systemic adverse reactions may occur depending on the amount ingested. If such reactions develop, supportive and symptomatic treatment should be administered.

Adverse Reactions

Adverse reactions are classified by organ systems and frequency of occurrence: very common (≥ 1/10), common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥1/10,000, <1/1000), very rare (<1/10,000), frequency not known (frequency cannot be estimated from the available data).

Immune system disorders:

Frequency not known – hypersensitivity reactions, including anaphylactic shock, angioedema.

Skin and subcutaneous tissue disorders:

Uncommon – local skin reactions such as erythema, eczema, pruritus, burning sensation; rare – photosensitization reactions, urticaria; very rare – bullous and flebotic eczema, which may spread and become generalized; frequency not known – Stevens-Johnson syndrome.

Renal and urinary disorders:

Very rare – worsening of pre-existing renal impairment.

Reporting of suspected adverse reactions

Reporting of suspected adverse reactions after medicinal product registration is important. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals should report any suspected adverse reactions via the national pharmacovigilance system.

Shelf life

3 years.

Storage conditions

Store at a temperature not exceeding 25 °C, in a place inaccessible to children.

Packaging

45 g in a tube, 1 tube per cardboard box.

Prescription status

Prescription only.

Manufacturer

UORLDMEDITSIN ILACH SAN. VE TICJ. A.S. /
WORLD MEDICINE ILAC SAN. VE TIC. A.S.

Manufacturer's address and location of business operations

COSB G.O.Pasa Mah. 6. Cad. No:30, Cerkezkoy/Tekirdag, Turkey.

Marketing Authorization Holder

LLC "WORLD MEDICINE", Ukraine /
WORLD MEDICINE, LLC, Ukraine