Artejа®-d gel

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ARTEJА®-D GEL

Composition:

Active substance: diclofenac;

1 g of gel contains 50 mg of sodium dicloenac;

Excipients: isopropyl alcohol, macrogol-7-glyceryl cocoate, hypromellose, purified water.

Pharmaceutical form. 5% gel.

Main physicochemical characteristics: transparent, colorless or slightly yellowish gel with a characteristic odor of isopropyl alcohol.

Pharmacotherapeutic group.

Agents used locally for joint and muscular pain. Non-steroidal anti-inflammatory agents for topical use. Diclofenac. ATC code M02A A15.

Pharmacological properties.

Pharmacodynamics.

Arteja®-D gel is a non-steroidal anti-inflammatory drug (NSAID) for topical use from the phenylacetic acid derivatives group. The drug has pronounced local anti-rheumatic, analgesic, and anti-inflammatory properties, which are due to inhibition of prostaglandin synthesis – mediators of pain and inflammation.

In inflammation caused by injuries or rheumatic diseases, Arteja®-D gel reduces pain, tissue swelling, and shortens the recovery period of functions in damaged joints, ligaments, tendons, and muscles.

Pharmacokinetics.

Sodium diclofenac is slowly and partially absorbed through the skin surface. The amount of diclofenac absorbed through the skin is proportional to the application area and depends on both the total applied dose of the drug and the degree of skin hydration. Maximum plasma concentration is observed within 6–9 hours. After oral administration, maximum plasma concentration is reached approximately within 1–2 hours. The average duration of the active substance in systemic circulation is approximately 9 hours, which is significantly longer compared to 1–2 hours after oral administration.

Diclofenac accumulates in the skin, which acts as a reservoir, from where the substance is gradually released into adjacent tissues. From there, diclofenac predominantly enters deeper inflamed tissues, such as joints, where it continues to exert its effect and is found at concentrations up to 20 times higher than in plasma.

Metabolism and elimination of the drug after topical application are similar to those after systemic administration. Diclofenac and its metabolites are primarily excreted in urine. Total systemic plasma clearance of diclofenac is 263 ± 56 ml/min, and the terminal half-life averages 1–3 hours. Diclofenac is 99% bound to plasma proteins. After rapid hepatic metabolism (hydroxylation and conjugation with glucuronic acid), about two-thirds of the substance is excreted by the kidneys and one-third via bile.

In renal or hepatic insufficiency, metabolism and elimination of diclofenac from the body remain unchanged.

Clinical characteristics.

Indications.

Local treatment of pain and inflammation of joints, muscles, ligaments, and tendons of rheumatic or traumatic origin.

Contraindications.

Hypersensitivity to diclofenac or to other NSAIDs, to isopropyl alcohol or to any of the excipients of the medicinal product. History of asthma attacks, urticaria, acute rhinitis, nasal polyps, angioedema induced by acetylsalicylic acid or other non-steroidal anti-inflammatory drugs. Third trimester of pregnancy. Childhood.

Interaction with other medicinal products and other forms of interaction.

Since systemic absorption of diclofenac following topical application of the product is very low, the occurrence of interactions is unlikely.

Special precautions for use.

Use with caution when combining the drug with oral NSAIDs.

The likelihood of developing systemic adverse effects with topical application of diclofenac is low compared to oral forms; however, systemic effects cannot be excluded when the drug is applied over relatively large skin areas for prolonged periods.

Artezia®-D gel should be applied only to intact skin areas, avoiding contact with inflamed, injured, or infected skin. Contact of the drug with eyes and mucous membranes should be avoided. The drug must not be used internally.

If any skin rash occurs, treatment with the drug should be discontinued. Use under an occlusive, air-tight dressing is not recommended; however, application under a non-occlusive dressing is permitted. In case of ligament sprains, the affected area may be bandaged with a bandage.

Do not apply to open wounds or infected skin, or to areas affected by eczema, or to mucous membranes.

Artezia®-D gel contains isopropyl alcohol, which may cause mild localized skin irritation.

Due to the possibility of photosensitivity, exposure to direct sunlight and visits to solariums should be avoided during treatment and for 2 weeks after discontinuation of treatment.

Use during pregnancy or breastfeeding.

Clinical experience with the use of diclofenac in pregnant women is limited. Like other NSAIDs, the drug is contraindicated during the third trimester of pregnancy due to the risk of uterine inertia, prolonged bleeding time, fetal renal dysfunction leading to oligohydramnios, and/or development of cardiovascular and pulmonary toxicity, including premature closure of the arterial duct and pulmonary hypertension. Systemic use of prostaglandin synthesis inhibitors, including the medicinal product Artezia®-D gel, during the third trimester of pregnancy may cause cardiovascular, pulmonary, and renal toxicity in the fetus. In late pregnancy, prolonged bleeding may occur in both mother and child, and labor may be delayed. Therefore, the medicinal product Artezia®-D gel is contraindicated during the last trimester of pregnancy (see section "Contraindications"). Impaired fetal renal function leading to oligohydramnios has been observed with the use of NSAIDs (including diclofenac) starting from the 20th week of pregnancy. Use of the drug during the first two trimesters of pregnancy is permitted only if the expected benefit outweighs the potential risk to the fetus. Even though the systemic effect of diclofenac after topical application is lower than with oral administration, it is unknown whether the systemic exposure to the medicinal product Artezia®-D gel achieved after topical use could be harmful to the embryo/fetus. During the first and second trimesters of pregnancy, Artezia®-D gel should not be used unless clearly necessary. Women who are planning pregnancy, as well as those in the first two trimesters of pregnancy, should use the lowest effective dose for the shortest possible duration.

It is unknown whether diclofenac penetrates into breast milk after topical application. Therefore, use of the medicinal product Artezia®-D gel during breastfeeding is permitted only if, in the physician’s opinion, the expected benefit outweighs the potential risk to the infant. If there are strong medical reasons for using the drug during breastfeeding, the gel should not be applied to the breasts or large skin areas, and should not be used in larger amounts or for longer than recommended.

Fertility. There are no available data on the effect of topically applied diclofenac on human fertility.

Ability to affect reaction speed when driving or operating machinery. No effect.

Method of Administration and Dosage

Apply Artedzha®-D gel 3–4 times daily, gently rubbing it into the skin. The amount of the preparation used depends on the size of the affected area (for example, 2–4 g of gel, corresponding in volume to the size of a cherry or a walnut, is sufficient for application to an area of 400–800 cm²).

After application, hands should be washed unless the hands themselves are the area being treated.

The duration of therapy depends on the nature of the disease and the treatment response.

The preparation should not be used for longer than 14 consecutive days.

If the patient does not experience improvement or if symptoms worsen after 7 days of treatment, medical advice should be sought, especially if the product is being used without prior medical consultation.

Elderly patients (aged 65 years and older). There is no evidence suggesting that elderly patients require a specific dosage adjustment or are more likely to experience adverse reactions different from those in other patients.

Patients with renal impairment. There is no evidence suggesting that patients with renal impairment require a specific dosage adjustment.

Patients with hepatic impairment. There is no evidence suggesting that patients with hepatic impairment require a specific dosage adjustment.

Children.

Dosage recommendations and therapeutic indications for the use of Artedzha®-D gel in children have not been established.

Overdose.

Overdose is unlikely due to the low systemic absorption of diclofenac following topical application. However, in case of accidental ingestion, it should be noted that one 100 g tube contains 5 g of sodium diclofenac, which may lead to the development of systemic adverse reactions.

In case of accidental ingestion, gastric lavage should be performed immediately and an adsorbent administered. Symptomatic treatment, employing therapeutic measures appropriate for NSAID poisoning, is indicated.

Adverse reactions.

Artezia®-D gel is generally well tolerated. Adverse reactions include mild transient skin reactions at the site of application. Allergic reactions may occur rarely.

The assessment of adverse reactions is presented according to the frequency of occurrence: very common (≥ 1/10), common (≥ 1/100, < 1/10), uncommon (≥ 1/1,000, < 1/100), rare (≥ 1/10,000, < 1/1,000), very rare (< 1/10,000).

Infections and infestations: very rare – pustular rashes.

Skin and subcutaneous tissue disorders: uncommon – rash, pruritus, erythema, eczema, exanthema, burning sensation, edema, vesicles, papules, pustules, desquamation, dry skin, dermatitis (including contact dermatitis); rare – bullous dermatitis; very rare – photosensitivity reactions, generalized skin rashes, skin burning sensation.

Immune system disorders: very rare – hypersensitivity reactions (including urticaria), facial angioedema, dyspnea.

Respiratory system disorders: very rare – bronchial asthma.

Gastrointestinal disorders: adverse reactions occur very rarely after topical application of preparations containing diclofenac.

When the gel is used in high doses or applied to large areas of skin, the possibility of systemic adverse reactions as well as hypersensitivity reactions such as angioedema and dyspnea cannot be excluded.

Shelf life. 2 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Do not freeze.

Keep out of reach of children.

Packaging.

50 g or 100 g of gel in a tube; 1 tube per carton.

Availability. Over-the-counter (without prescription).

Manufacturer. JSC «FITOFARM».

Manufacturer's address and location of business activity.

17 Chumatska Street, Boryspil, Kyiv Oblast, 08303, Ukraine.

Marketing Authorization Holder. Delta Medical Promotions AG

Address of the Marketing Authorization Holder.

26 Oetenbachgasse, Zurich CH-8001, Switzerland