Diclosan

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

Composition:

Active substances: 1 g of gel contains sodium diclofenac (calculated as the dry substance) – 10 mg;

nicotinic acid – 10 mg;

Excipients: carbomer (carbopol 934 P or 974 NF), glycerin, isopropyl alcohol, 15% ammonia solution, formaldehyde solution (35%), purified water.

Pharmaceutical form. Gel.

Main physico-chemical properties: white or whitish-yellowish homogeneous gel of uniform consistency, with a faint specific odor.

Pharmacotherapeutic group. Agents used locally in joint and muscular pain. Topical non-steroidal anti-inflammatory agents. Diclofenac.

ATC code M02A A15.

Pharmacological Properties

Pharmacodynamics

Diclofenac is a non-steroidal anti-inflammatory agent with pronounced anti-rheumatic, analgesic, anti-inflammatory, and antipyretic effects. Its main mechanism of action is the inhibition of prostaglandin biosynthesis.

In inflammation caused by injuries or rheumatic diseases, Diclonsan reduces pain, tissue swelling, and shortens the recovery period of functions in damaged joints, ligaments, tendons, and muscles. Clinical data have demonstrated that Diclonsan reduces acute pain within 1 hour after initial application. 94% of patients responded to Diclonsan within 2 days of treatment, compared to 8% who responded to placebo. Relief from pain and functional impairments was achieved after 4 days of treatment with Diclonsan. Due to its water-alcohol base, the preparation also produces a local anesthetic and cooling effect.

Pharmacokinetics

The amount of diclofenac absorbed through the skin is proportional to the application area and depends on both the total dose applied and the degree of skin hydration. After topical application of 2.5 g of Diclonsan to a skin surface area of 500 cm², the absorption rate of diclofenac is approximately 6%. Application of an occlusive dressing for 10 hours results in a threefold increase in diclofenac absorption.

After application of Diclonsan to the skin over hand and knee joints, diclofenac is detected in blood plasma (where its maximum concentration is approximately 100 times lower than after oral administration), in the synovial membrane, and in synovial fluid. Protein binding of diclofenac is 99.7%.

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

Diclofenac is metabolized mainly via hydroxylation, forming several phenolic derivatives, two of which are pharmacologically active but to a significantly lesser extent than diclofenac itself.

Diclofenac and its metabolites are primarily excreted in urine. Total systemic plasma clearance of diclofenac is 263 ± 56 mL/min, and the terminal elimination half-life averages 1–3 hours.

In renal or hepatic insufficiency, the metabolism and elimination of diclofenac are not altered.

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 components of the medicinal product. History of asthma attacks, urticaria, or acute rhinitis induced by acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs (NSAIDs). Third trimester of pregnancy.

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 likelihood of interactions is very low.

Special precautions for use

Use with caution when administered concomitantly with oral NSAIDs.

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

Diklosan 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 product must not be ingested.

If any skin rash develops, treatment with the drug should be discontinued. Diklosan should not be used under airtight occlusive dressings; however, application under non-occlusive dressings is permitted. In case of ligament strain, the affected area may be bandaged with a wrap.

The medicinal product contains formaldehyde solution (35%), which may cause local skin reactions (e.g., contact dermatitis).

Use during pregnancy or breastfeeding

There are no clinical data on the use of Diklosan during pregnancy. Although the systemic effect of the drug is lower than with oral administration, it is unknown whether the systemic exposure to diclofenac achieved after topical application may be harmful to the embryo/fetus. During the first and second trimesters of pregnancy, Diklosan should not be used unless clearly necessary. If required, the dose should be kept as low as possible and the duration of treatment as short as possible.

During the third trimester of pregnancy, systemic use of prostaglandin synthesis inhibitors, including diclofenac, may cause cardiopulmonary and renal toxicity in the fetus. At late stages of pregnancy, prolonged bleeding may occur in both mother and child, and labor may be delayed. Therefore, Diklosan is contraindicated during the last trimester of pregnancy (see section "Contraindications").

If there is a strong medical justification for using Diklosan during breastfeeding, and the expected benefit outweighs the potential risk, as determined by the physician, the product should not be applied to the breasts or large skin areas, nor should it be used for prolonged periods.

Ability to affect reaction speed while driving or operating machinery

No effect.

Method of Administration and Dosage

For adults and children aged 14 years and older, Diklosan should be applied 3–4 times daily, gently rubbed into the skin. The amount of the drug used depends on the size of the affected area (for example, 2–4 g, corresponding in size to a cherry or a walnut, is sufficient for application to an area of 400–800 cm²).

After application, hands should be washed thoroughly, except in cases when the hands themselves are the treated area.

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

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

Children.

Diklosan is not recommended for use in children under 14 years of age. If the drug is used in children aged 14 years and older for longer than 7 days, or if disease symptoms worsen, medical advice should be sought.

Overdose.

Overdose is unlikely due to the low systemic absorption of diclofenac when applied topically. In case of accidental ingestion, note that one 100 g tube of the drug contains the equivalent of 1 g of sodium diclofenac; systemic adverse reactions may occur.

In case of accidental ingestion, the stomach should be emptied immediately and an adsorbent administered. Symptomatic treatment is indicated, using therapeutic measures appropriate for poisoning with nonsteroidal anti-inflammatory drugs (NSAIDs).

Adverse Reactions

Diclosan is generally well tolerated. Adverse reactions include mild, transient skin reactions at the application site. In rare cases, allergic reactions may occur.

Infections and infestations

Rare (<1/10,000): pustular rashes.

Immune system disorders

Rare (<1/10,000): hypersensitivity reactions (including urticaria), angioneurotic edema.

Respiratory system disorders

Rare (<1/10,000): bronchial asthma.

Skin and subcutaneous tissue disorders

Common (≥1/100; <1/10): rash, pruritus, eczema, erythema, dermatitis, including contact dermatitis.

Uncommon (≥1/10,000; <1/1,000): bullous dermatitis.

Rare (<1/10,000): photosensitivity reactions, skin burning sensation.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after medicine authorization is highly important. It allows continuous monitoring of the benefit-risk balance of the medicine. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy through 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. 40 g in a tube; 1 tube per carton.

Supply category. Over-the-counter.

Manufacturer: JSC "Lubnipharm".

Manufacturer's address and location of business activity.

16, Barvinkova Street, Lubny, Poltava region, Ukraine, 37500.