Diclofenac-zdorovya

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT DICKLOFENAC-ZDOROV'YA (DICLOFENAC-ZDOROVYE)

Composition:

Active ingredient: diclofenac;

1 g of gel contains 10 mg of sodium diclofenac;

Excipients: carbomer, concentrated ammonia solution, propylene glycol, glycerol, 96% ethanol, methylparaben (E 218), purified water.

Pharmaceutical form. Gel.

Main physicochemical properties: white homogeneous gel with a mild specific odor.

Pharmacotherapeutic group. Topical preparations used for joint and muscular pain. Topical non-steroidal anti-inflammatory drugs. 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. Its main mechanism of action is the inhibition of prostaglandin biosynthesis.

In inflammation caused by injuries or rheumatic diseases, the drug reduces pain, tissue swelling, and shortens the recovery period of impaired functions of injured joints, ligaments, tendons, and muscles. The drug reduces acute pain within 1 hour after the initial application. Relief of pain and functional impairments is achieved after 4 days of treatment with the drug. Due to its water-alcohol base, the drug 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 of the drug applied and the degree of skin hydration. After topical application of 2.5 g of the drug to a skin surface area of 500 cm², the extent of diclofenac absorption is approximately 6%. Application of an occlusive dressing for 10 hours results in a threefold increase in diclofenac absorption.

After application of the drug to the skin over hand and knee joints, diclofenac appears in blood plasma (where its maximum concentration is approximately 100 times lower than after oral administration), synovial membrane, and synovial fluid. Diclofenac binding to plasma proteins 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 enters 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, although to a much lesser extent than diclofenac.

Diclofenac and its metabolites are primarily excreted in urine. The total systemic plasma clearance of diclofenac is 263 ± 56 ml/min, and the terminal half-life is on average 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 product. History of asthma attacks, 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 after local application of the product is very low, the occurrence of interactions is unlikely.

Special precautions for use

The product should only be applied to intact skin areas, avoiding contact with inflamed, damaged or infected skin. Contact with eyes and mucous membranes should be avoided. The product must not be swallowed.

Use with caution in combination with oral NSAIDs. The likelihood of systemic adverse effects with topical application of diclofenac is low compared to oral formulations; however, it cannot be excluded when the product is used over relatively large skin areas for prolonged periods.

If any skin rash develops, treatment with the product should be discontinued.

The product should not be used under airtight occlusive dressings; however, application under non-occlusive dressings is acceptable. If ligaments are strained, the affected area may be bandaged with a bandage.

The product contains propylene glycol, which may cause skin irritation.

Methylparaben (E 218) contained in the medicinal product may cause allergic reactions (possibly delayed).

Use during pregnancy or breastfeeding. There are no clinical data on the use of diclofenac during pregnancy. Even though systemic exposure is lower than with 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, parturition, or postnatal development of offspring has been observed.

It is unknown whether diclofenac penetrates into breast milk following topical application; therefore, use of the product is not recommended during breastfeeding. However, if there are strong clinical reasons for using the product during breastfeeding, the product should not be applied to the mammary glands or large skin areas, and should not be used for prolonged periods.

Data on the effect of topically applied diclofenac on human fertility are lacking.

Ability to affect the speed of reactions while driving or operating machinery. No effect has been observed.|established|

Method of Administration and Dosage

For adults and children aged 14 years and older, 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, 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 when the hands themselves are the treated area.

The duration of treatment depends on the nature of the condition and the treatment response. The medication should not be used for longer than 14 consecutive days in cases of injuries or soft tissue rheumatism, or longer than 21 days in cases of arthritic joint pain, unless otherwise directed by a physician.

Consult a physician if symptoms do not improve or worsen after 7 days of treatment.

Elderly patients do not require dose adjustment.

Children. The medication is not recommended for use in children under 14 years of age. If the medication is used in children aged 14 years and older for longer than 7 days, or if symptoms worsen, consult a physician.

Overdose. Overdose is unlikely due to the low systemic absorption of diclofenac following topical application. However, in case of accidental ingestion, systemic adverse reactions may occur.

In case of accidental ingestion, empty the stomach immediately and administer an adsorbent. Symptomatic treatment should be administered, applying therapeutic measures appropriate for NSAID poisoning.

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, angioneurotic edema.

Respiratory system disorders: bronchial asthma.

Skin and connective tissue disorders: rash, urticaria, eczema, erythema, dermatitis (including contact, bullous), photosensitivity reactions, skin 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. 30 g or 50 g in a tube in a carton.

Supply category. Over-the-counter.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROV'YA".

Manufacturer's address and place of business. 22 Shevchenka Street, Kharkiv, Kharkiv Oblast, 61013, Ukraine.