Diclofarm gel for external use 1%, 50g

Composition

Per 1 g of the drug:

Active ingredient:  

diclofenac sodium – 10 mg;

excipients:  

carbomer-15 mg,

ethanol (96%) – 150 mg,

isopropanol-150 mg,

trollamine-30 mg,

methyl parahydroxybenzoate-1 mg,

water-644 mg

Pharmacological action

Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid, which has a pronounced anti-inflammatory, analgesic and antipyretic effect.

Indiscriminately inhibiting cyclooxygenase 1 (COX 1) and cyclooxygenase 2 (COX 2), it disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the focus of inflammation, which are the main link in the development of inflammation.

It is used to eliminate pain and inflammation in joints, muscles and ligaments of traumatic or rheumatic origin, helping to reduce pain and swelling associated with the inflammatory process, increasing joint mobility.

Pharmacokinetics:

Suction

The amount of diclofenac absorbed through the skin is proportional to the area of the treated surface and depends both on the total dose of the drug applied and on the degree of hydration of the skin.

On day 7, the relative bioavailability of the drug (AUC ratio) is 4.5% (for an equivalent dose of diclofenac sodium salt). When wearing a moisture-permeable bandage, the absorption did not change.

The concentration of diclofenac in plasma, synovial membrane and synovial fluid was measured when the drug was applied to the affected joint area: the maximum concentration (Cmax) in plasma was approximately 100 times lower than after oral use of the same amount of diclofenac.

Distribution

99.7% of diclofenac binds to plasma proteins, mainly albumins (99.4%). Diclofenac is mainly distributed and retained in tissues susceptible to inflammation, such as joints, where its concentration is 20 times higher than in plasma.

Metabolism

The metabolism of diclofenac is carried out partly by glucuronidation of the unchanged molecule, but mainly by single and multiple hydroxylation, which leads to the formation of several phenolic metabolites, most of which are converted to glucuronide conjugates. Two phenolic metabolites are biologically active, but to a much lesser extent than diclofenac.

Deduction

The total systemic plasma clearance of diclofenac is 263±56 ml/min. Most of diclofenac and its metabolites are excreted by the kidneys. The final half-life (T 1/2) is 1-2 hours. T 1/2 of metabolites, including two pharmacologically active ones, is also short and is 1-3 hours. One of the metabolites (3′-hydroxy-4′-methoxydiclofenac) has a longer half-life, but this metabolite is inactive.

Indications

– back Pain in inflammatory and degenerative diseases of the spine (sciatica, osteoarthritis, lumbago, sciatica);

– pain in the joints (joints of the fingers, knee, etc. ) in osteoarthritis;

pain in muscles (due to sprain, strain, bruises, and injuries);

– inflammation and swelling of the soft tissues and joints due to injuries and rheumatic disease (tenosynovitis, bursitis, lesions of periarticular tissues, wrist syndrome).

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use. It does not affect the progression of the disease.

Recommendations for use

The gel is applied externally.

For adults and children over 12 years of age, the drug is applied in a thin layer to the skin above the focus of inflammation/injury 2-3 times a day, lightly rubbing into the skin.

The required amount of the drug depends on the size of the painful area.

A single dose of the drug – 2-4 g (which is comparable in volume to the size of a cherry or walnut, respectively) is sufficient to treat an area of 400-800 cm 2. If the hands are not a zone of pain localization, then after applying the drug they must be washed.

The duration of treatment depends on the indications and the observed effect. The drug should not be used for more than 14 days without a doctor’s recommendation. If after 7 days of use the therapeutic effect is not observed or the condition worsens, you should consult a doctor.

The drug Diclofarm should be used in the minimum effective doses with the shortest course.

Contraindications

– Hypersensitivity to diclofenac or other components of the drug;

– the tendency to the occurrence of asthma attacks, skin rashes or acute rhinitis to acetylsalicylic acid or other NSAIDs;

– violation of the integrity of the skin at the intended site of application;

– pregnancy (III trimester);

– the period of breastfeeding;

– children’s age (under 12 years).

With caution:

Hepatic porphyria (exacerbation); erosive and ulcerative lesions of the gastrointestinal tract; severe liver and kidney function disorders; blood clotting disorders (including hemophilia, prolongation of bleeding time, tendency to bleed); chronic heart failure; bronchial asthma; elderly age; pregnancy (I and II trimester).

Side effects

Adverse reactions are mainly characterized by moderate and passing skin manifestations at the site of application of the gel. In very rare cases, allergic reactions may occur.

The frequency of adverse reactions is determined in accordance with the World Health Organization classifications: very often-more than 1/10; often-more than 1/100, but less than 1/10; infrequently-more than 1/1000, but less than 1/100; rarely-more than 1/10000, but less than 1/1000; very rarely-less than 1/10000.

From the immune system

Very rarely – hypersensitivity reactions (including urticaria), angioedema.

Respiratory, thoracic and mediastinal disorders

Very rarely-suffocation attacks, bronchospasm.

From the skin and subcutaneous tissues

Often-erythema, dermatitis (including contact dermatitis), eczema, skin rash, pruritus;

rarely:  bullous dermatitis;

very rarely – photosensitization reactions, pustular rashes.

Interaction

Diclofenac may increase the effect of medications that cause photosensitization.

No clinically significant interactions with other drugs have been described.

Overdose

Due to the low systemic absorption, overdose is unlikely with topical application of the gel.

Symptoms: Accidental ingestion may cause systemic adverse reactions.

Treatment: gastric lavage, induction of vomiting, use of activated charcoal, symptomatic therapy. Hemodialysis is ineffective due to the high degree of binding of diclofenac to plasma proteins (about 99%).

Special instructions

Diclofarm should only be applied to undamaged skin, avoiding contact with open wounds. Do not allow the drug to enter the mouth, eyes and mucous membranes. After applying the drug, a bandage may be applied, but airtight occlusive dressings should not be applied.

If a skin rash develops after applying the drug, its use should be discontinued.

Influence on the ability to drive vehicles and mechanisms:

It does not affect the ability to drive vehicles, mechanisms, or engage in other activities that require increased concentration of attention.

Active ingredient

Diclofenac

Dosage form

gel for external use