Diclac® gel

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT DICLAC® GEL

Composition:

Active substance: diclofenac;

1 g of gel contains 50 mg of sodium diclofenac;

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

Pharmaceutical form. Gel.

Main physicochemical properties: colorless or slightly yellowish transparent gel with a characteristic odor of isopropanol, free from air bubbles.

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.

Diclac® Gel is a non-steroidal anti-inflammatory agent for topical use, belonging to the group of phenylacetic acid derivatives. The drug exerts pronounced local anti-rheumatic, analgesic, and anti-inflammatory effects, which are due to inhibition of prostaglandin synthesis – mediators of pain and inflammation.

In inflammation caused by injuries or rheumatic diseases, Diclac® 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 both on the total applied dose of the drug and on the degree of skin hydration. Maximum plasma concentration is observed 6–9 hours after application. After oral administration, maximum plasma concentration is reached approximately within 1–2 hours. The mean duration of the active substance in systemic circulation is about 9 hours, which is significantly longer compared to 1–2 hours after oral administration.

Diclofenac accumulates in the skin, which acts as a reservoir, allowing gradual release of the substance into adjacent tissues. From there, diclofenac predominantly reaches deeper inflamed tissues, such as joints, where it continues to act and is found in concentrations up to 20 times higher than in plasma.

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

Metabolism and elimination of diclofenac are not altered in renal or hepatic insufficiency.

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 of the excipients of the medicinal product. History of asthma attacks, urticaria, acute rhinitis, nasal polyps, or angioedema induced by acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs. Last trimester of pregnancy. Childhood age.

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 co-administering with oral nonsteroidal anti-inflammatory drugs (NSAIDs).

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

Diclac® Gel should only be applied to intact skin, avoiding contact with inflamed, damaged, or infected skin. Contact with eyes and mucous membranes should be avoided. The product must not be taken orally.

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

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

Diclac® Gel contains isopropyl alcohol, which may cause mild localized skin irritation.

Due to the potential for 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 nonsteroidal anti-inflammatory drugs, the drug is contraindicated during the third trimester of pregnancy due to the risk of impaired uterine contractility, prolonged bleeding time, fetal renal dysfunction leading to oligohydramnios, and/or development of cardiovascular toxicity, including premature closure of the ductus arteriosus and pulmonary hypertension. Use during the first two trimesters of pregnancy is permitted only if the expected benefit outweighs the potential risk to the fetus. Women who are planning pregnancy and those in the first two trimesters of pregnancy should use the lowest effective dose for the shortest possible duration.

Risk of impaired fetal renal function leading to oligohydramnios has been observed with NSAIDs (including diclofenac) starting from the 20th week of pregnancy.

It is unknown whether diclofenac is excreted in breast milk following topical application. Therefore, use of Diclac® Gel during breastfeeding is only permitted 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 topical diclofenac on human fertility.

Ability to affect reaction speed when driving or operating machinery.

No effect.

Method of Administration and Dosage.

Apply Diclac® Gel 3–4 times daily, gently rubbing it into the skin. The amount of the product 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 applying the product, hands should be washed unless the hands themselves are the treated area.

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

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

If the product is used without prior medical prescription, consult a physician if the patient's condition does not improve or worsens after 7 days of treatment.

Elderly patients (over 65 years of age). There is no reason to believe that elderly patients require a special dose adjustment or are at increased risk of adverse reactions different from those in other patients.

Patients with renal impairment. There is no reason to believe that patients with renal impairment require a special dose adjustment.

Patients with hepatic impairment. There is no reason to believe that patients with hepatic impairment require a special dose adjustment.

Children.

Dosage recommendations and therapeutic indications for the use of Diclac® Gel in children are not available.

Overdose.

Overdose is unlikely due to the low systemic absorption of diclofenac following topical application. However, in case of accidental ingestion, note that one 100-g tube 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 should be implemented, applying therapeutic measures commonly used in poisoning with nonsteroidal anti-inflammatory drugs.

Adverse reactions.

Diclac® 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 categorized by 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, erythema, burning sensation, swelling and vesicle formation, papules, pustules, skin desquamation and dryness, dermatitis (including contact dermatitis); rare – bullous dermatitis; very rare – photosensitivity reactions, generalized skin rashes, sensation of skin burning.

Immune system disorders: very rare – hypersensitivity reactions (including urticaria), angioneurotic edema of the face, dyspnea.

Respiratory system disorders: very rare – bronchial asthma.

Gastrointestinal system: adverse reactions occur very rarely following 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 cannot be excluded, as well as hypersensitivity reactions in the form of angioedema, dyspnea.

Shelf life. 3 years.

Storage conditions.

Store at temperatures not exceeding 25 °C.

Keep out of reach of children.

Packaging.

50 g, 100 g or 150 g of gel in a tube; 1 tube in a cardboard box.

Prescription status. Over-the-counter.

Manufacturer.

SALUTAS Pharma GmbH.

Manufacturer's address and location of manufacturing site.

Production unit in Osterweddingen, Lange Herren 3, Sülzetal, OT Osterweddingen, Saxony-Anhalt, 39171, Germany.