Diclac® lipogel

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT DICLAC® LIPOGEL (DICLAC® LIPOGEL)

Composition:

Active substance: sodium diclofenac;

1 g of gel contains sodium diclofenac 10 mg;

Excipients: RRR-α-tocopherol, carbomer, decyl oleate, octyldodecanol, lecithin, ammonia solution 10%, disodium edetate, flavoring agent – "Vert de Creme - lilial free" oil, isopropyl alcohol, purified water.

Pharmaceutical form. Gel.

Main physicochemical properties: slightly yellowish homogeneous gel with a characteristic isopropanol odor, free from agglomerates, lumps, and foreign particles.

Pharmacotherapeutic group.

Agents used locally for joint and muscular pain. Non-steroidal anti-inflammatory drugs for topical use. Diclofenac.

ATC code M02A A15.

Pharmacological properties.

Pharmacodynamics.

Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) for topical use, belonging to the phenylacetic acid derivatives group. The drug has pronounced local anti-rheumatic, analgesic, and anti-inflammatory properties due to inhibition of prostaglandin synthesis—mediators of pain and inflammation. In inflammation caused by injuries or rheumatic diseases, Diclac® Lipogel reduces pain, tissue swelling, and shortens the recovery period of functions in damaged joints, ligaments, tendons, and muscles. Due to its water-alcohol base, the preparation also exerts a local anesthetic and cooling effect.

Pharmacokinetics.

The amount of diclofenac absorbed through the skin is proportional to the application area and depends both on the total applied dose of the drug and on the degree of skin hydration. The extent of diclofenac absorption is approximately 6% of the dose after topical application of 2.5 g of diclofenac gel to 500 cm² of skin, as determined relative to total renal elimination compared with diclofenac tablets. Occlusion for 10 hours leads to a threefold increase in the amount of diclofenac absorbed.

After topical administration of the gel to areas of the arms and knees, diclofenac concentration can be measured in blood plasma, synovial tissue, and synovial fluid. Maximum plasma concentration of diclofenac after topical application is approximately 100 times lower than after oral administration of tablets. 99.7% of diclofenac is bound to plasma proteins, primarily to albumin (99.4%). Diclofenac accumulates in the skin, which acts as a reservoir, from which the substance is gradually released into adjacent tissues. From there, diclofenac predominantly penetrates into deeper inflamed tissues, such as joints, where it continues to act and reaches concentrations up to 20 times higher than in blood plasma.

Diclofenac metabolism involves partial glucuronidation of intact molecules, but primarily hydroxylation, forming several phenolic metabolites. Two of these phenolic metabolites are biologically active, although to a much lesser extent than diclofenac.

Total systemic plasma clearance of diclofenac is 263 ± 56 mL/min (mean value ± SD). The elimination half-life ranges from 1 to 2 hours. Four of the metabolites, including two active ones, also have short elimination half-lives ranging from 1 to 3 hours. One metabolite, 3'-hydroxy-4'-methoxy-diclofenac, has a longer plasma half-life but is practically inactive. Diclofenac and its metabolites are primarily excreted in urine.

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 nonsteroidal anti-inflammatory drugs, to isopropyl alcohol, or to any other components of the product. History of asthma attacks, urticaria, acute rhinitis, nasal polyps, angioedema induced by acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs. Third trimester of pregnancy.

Interaction with other medicinal products and other forms of interaction.

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

Special precautions for use.

Use with caution in combination with oral nonsteroidal anti-inflammatory drugs.

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

Diklak® Lipogel should be applied only to intact skin areas, avoiding application on inflamed, wounded, 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. Use of an occlusive dressing is not recommended. In cases of ligament sprains, the affected area may be wrapped with a bandage.

In conditions associated with joint redness or swelling, acute lower back pain radiating to the lower limbs and/or accompanied by neurological disturbances (such as numbness or tingling sensations), medical advice should be sought.

The gel may be used under a non-occlusive dressing, but must not be applied under air-impermeable occlusive dressings.

Use during pregnancy or breastfeeding.

There are no clinical data on the use of Diklak® Lipogel during pregnancy. Although systemic exposure to diclofenac is lower with topical administration than with oral use, it is unknown whether the systemic exposure achieved after topical application of Diklak® Lipogel could be harmful to the embryo/fetus. During the first and second trimesters of pregnancy, Diklak® Lipogel 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, Diklak® Lipogel is contraindicated during the last trimester of pregnancy (see section "Contraindications").

Sodium diclofenac passes into breast milk in small amounts. Therefore, if there are strong clinical reasons for using the gel during breastfeeding, it should not be applied to the breasts or to large skin areas, nor used for prolonged periods.

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

Ability to influence reaction rate when driving or operating machinery.

No effect.

Method of Administration and Dosage

For adults and children aged 14 years and older, Diclac® Lipogel should be applied 3–4 times daily. The amount of medication used depends on the size of the affected area (e.g., 2–4 g, corresponding in size to a cherry or walnut, is sufficient for application to an area of 400–800 cm²). The gel should be applied in a thin layer and gently rubbed into the skin. Do not use under occlusive, air-impermeable dressings.

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

The duration of treatment depends on the indication and therapeutic response.

The medication should not be used for longer than 14 consecutive days in cases of injuries or soft tissue rheumatism, or for longer than 21 days in cases of arthritic joint pain, unless otherwise directed by a physician.

Medical advice should be sought if symptoms do not improve or worsen after 7 days of treatment.

Children.

This medication should not be used in children under 14 years of age. When used in children aged 14 years and older for longer than 7 days, or if 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, the stomach should be emptied immediately and an adsorbent agent administered. Symptomatic treatment should be provided, employing therapeutic measures used for poisoning with nonsteroidal anti-inflammatory drugs.

Side effects.

The assessment of adverse reactions is based on their 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).

Skin reactions: uncommon – itching, redness, exanthema, burning sensation, development of edema and vesicles, papules, pustules, skin peeling and dryness, dermatitis (including contact dermatitis); rare – bullous dermatitis; very rare – photosensitivity reactions, pustular rashes, eczema.

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

Respiratory system: very rare – bronchial asthma.

Gastrointestinal tract: 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 occurrence of systemic adverse reactions, as well as hypersensitivity reactions in the form of angioedema and dyspnea, cannot be excluded.

Shelf life. 3 years.

Storage conditions.

Store at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging.

50 g of gel in a tube; 1 tube per cardboard box.

Prescription status.

Over-the-counter.

Manufacturer.

Salutas Pharma GmbH, Germany.

Manufacturer's address and place of business.

Production site in Osterweddingen, Lange Goehren 3, Suelzetal, OT Osterweddingen, Saxony-Anhalt, 39171, Germany.