Diclofenac-zdorovya ultra

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT DICLOFENAC-ZDOROVYE ULTRA (DICLOFENAC-ZDOROVYE ULTRA)

Composition:

Active substance: diclofenac;

1 g of gel contains sodium diclofenac 50 mg;

Excipients: methylparaben (E 218), peppermint oil, carbomer, glycerin, polyethylene glycol 400, ethanol 96 %, dimethyl sulfoxide, concentrated ammonia solution, purified water.

Pharmaceutical form. Gel.

Main physicochemical characteristics: white homogeneous gel with a characteristic odour.

Pharmacotherapeutic group. Topically applied agents for 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 drug (NSAID) with pronounced anti-rheumatic, analgesic, anti-inflammatory, and antipyretic effects. The main mechanism of action is inhibition of prostaglandin biosynthesis.

In inflammation caused by injuries or rheumatic diseases, the medicinal product reduces pain, tissue swelling, and accelerates restoration of functions in damaged joints, ligaments, tendons, and muscles. The drug reduces acute pain within 1 hour after the initial application. Due to its water-alcohol base, the medicinal product has 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 dose applied and on the degree of skin hydration. After topical application of 2.5 g of the medicinal product to a skin surface area of 500 cm², the extent of diclofenac absorption is approximately 6%. Application of an occlusive dressing for 10 hours increases diclofenac absorption threefold.

After application to the skin over wrist and knee joints, diclofenac is detected in blood plasma (where its maximum concentration is approximately 100 times lower than after oral administration), synovial membrane, and synovial fluid. Protein binding of diclofenac in blood 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 predominantly penetrates into deeper inflamed tissues, such as joints, where it continues to act and is found in concentrations up to 20 times higher than in blood plasma.

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

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.

In renal or hepatic insufficiency, metabolism and elimination of diclofenac from the body 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, other NSAIDs, or to any of the excipients. History of bronchial asthma attacks, angioedema, urticaria, or acute rhinitis induced by acetylsalicylic acid or other 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 drug is very low, the occurrence of interactions is unlikely.

Instructions for Use

The gel is recommended to be applied only to intact areas of skin, avoiding contact with inflamed, damaged, or infected skin. Contact of the drug with eyes and mucous membranes should be avoided. The gel must not be swallowed.

Use with caution in combination with oral NSAIDs. The likelihood of developing systemic adverse effects with topical application of diclofenac is low compared to oral forms, but it cannot be excluded when the drug is applied over relatively large skin areas for prolonged periods. In such cases, the medicinal product should be used cautiously in patients with hepatic, renal, or cardiac insufficiency, as well as in patients with active peptic ulcer disease.

If any skin rashes occur, treatment with the drug should be discontinued.

The medicinal product should not be used under occlusive, air-impermeable dressings; however, its use under non-occlusive dressings is acceptable. In case of ligament sprains, the affected area may be bandaged with a wrap.

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

Methylparaben (E 218) may cause allergic reactions (possibly delayed). Dimethyl sulfoxide may cause skin irritation.

Use during pregnancy or breastfeeding.

Clinical data on the use of diclofenac during pregnancy are lacking. Even though systemic effects are lower compared to oral administration, it is unknown whether the systemic exposure to diclofenac achieved after topical application could be harmful to the embryo/fetus. During the first and second trimesters of pregnancy, diclofenac should not be used unless clearly necessary. If used, the dose should be 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, diclofenac is contraindicated during the last trimester of pregnancy (see section "Contraindications").

In animal studies, no evidence of harmful effects of the drug on pregnancy, embryonic development, delivery, or postnatal development of offspring was observed.

It is unknown whether diclofenac is excreted in breast milk following topical application; therefore, use of the medicinal product during breastfeeding is permitted only when, in the physician’s opinion, the expected benefit outweighs the potential risk to the infant. If there are strong reasons for using the drug during breastfeeding, it should not be applied to the mammary glands or large areas of skin, nor should it be used for prolonged periods.

Data on the effect of topical diclofenac on human fertility are lacking.

Ability to influence reaction rate while driving or operating machinery.

No effect.

Method of administration and dosage.

For adults, apply 3–4 times daily, gently rubbing into the skin. The amount of medication used depends on the size of the affected area. Usually, 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 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. Dosage recommendations and therapeutic indications for use of the drug in children are not available.

Overdose.

Overdose is unlikely due to the low systemic absorption of diclofenac when applied topically. However, in case of accidental ingestion, the potential for systemic adverse reactions should be considered.

In case of accidental ingestion, the stomach should be emptied immediately and an adsorbent administered. Symptomatic treatment with therapeutic measures appropriate for poisoning with NSAIDs is indicated.

Adverse reactions.

The product is generally well tolerated. Adverse reactions include mild, transient skin reactions at the site of application. Allergic reactions may occur rarely.

Infections and infestations: pustular rashes.

Immune system disorders: hypersensitivity reactions (including urticaria), angioedema.

Respiratory system disorders: bronchial asthma.

Skin and connective tissue disorders: rash, erythema, eczema, exanthema, erythema, edema and vesicle formation, papules, pustules, desquamation and dryness of the skin, dermatitis (including contact dermatitis, bullous dermatitis), photosensitivity reactions, burning sensation, pruritus.

Shelf life. 3 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging. 50 g or 100 g in a tube in a carton.

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

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA".

Manufacturer's address and place of business.

Ukraine, 61013, Kharkiv, Kharkiv region, Shevchenka Street, 22.