Diclofenac-Akrikhin (Gel) Instructions for Use

Marketing Authorization Holder

Akrikhin Chemical and Pharmaceutical Plant, JSC (Russia)

Contact Information

AKRIKHIN JSC (Russia)

ATC Code

M02AA15 (Diclofenac)

Active Substance

Diclofenac (Rec.INN registered by WHO)

Dosage Forms

	Diclofenac-Akrikhin	Gel for external use 1%: tubes 40 g or 50 g
		Ointment for external use 1%: tube 30 g

Dosage Form, Packaging, and Composition

Ointment for external use from white to white with a grayish or yellowish tint, with a faint specific odor; the presence of pearlescent streaks is allowed.

* calculated as 100% substance

Excipients: dimethyl sulfoxide (dimexide), macrogol (polyethylene oxide 1500), macrogol (polyethylene oxide 400), propylene glycol, succinic acid.

30 g – aluminum tubes (1) – cardboard packs.

Gel for external use from white to white with a yellowish or grayish tint, with a specific odor.

Excipients: ethanol (rectified ethyl alcohol) – 25 g, propylene glycol – 5 g, carbomer 940 (carbopol 980) – 0.9 g, diethanolamine – 1 g, liquid paraffin (vaseline oil) – 2.5 g, cocoyl caprylocaprate – 2.5 g, macrogol cetostearyl ether (macrogol 20 cetostearyl ether) – 2 g, lavender oil – 0.05 g, orange flower oil (neroli oil) – 0.05 g, purified water – up to 100 g.

40 g – aluminum tubes (1) – cardboard packs.
50 g – aluminum tubes (1) – cardboard packs.

Clinical-Pharmacological Group

NSAIDs for external use

Pharmacotherapeutic Group

NSAID

Pharmacological Action

The active component Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) with pronounced analgesic and anti-inflammatory properties. By non-selectively inhibiting COX-1 and COX-2, it disrupts the metabolism of arachidonic acid and the synthesis of prostaglandins, which are the main link in the development of inflammation.

Diclofenac-Akrikhin is used to relieve pain and reduce swelling associated with the inflammatory process. When applied topically, it causes a reduction or disappearance of joint pain at rest and during movement. It reduces morning stiffness and joint swelling, and helps increase the range of motion.

In post-operative and traumatic injuries, it quickly suppresses pain and inflammatory phenomena in the area of application of the drug and promotes the resorption of post-traumatic hematoma.

The drug in the form of a gel, due to its water-ethanol base, additionally has a local anesthetic effect.

Pharmacokinetics

Absorption and Distribution

When applied externally, Diclofenac penetrates the skin well, concentrating mainly in the focus of inflammation and synovial fluid. The amount of diclofenac absorbed through the skin is proportional to the contact time of the drug with the skin and the area of its application, depends on the total dose of the drug and the degree of skin hydration. With the recommended method of application, no more than 6% of diclofenac is absorbed. The use of an occlusive dressing for 10 hours leads to a 3-fold increase in the resorption of diclofenac.

Binding to plasma proteins (mainly albumin) is 99%.

Metabolism and Excretion

It is metabolized in the liver, mainly by hydroxylation, forming several derivatives, two of which are pharmacologically active, but to a lesser extent than Diclofenac.

It is excreted by the kidneys (about 65%) and with bile (about 35%) in the form of inactive compounds with glucuronic and sulfuric acids; less than 1% is excreted unchanged. The total systemic plasma clearance of diclofenac averages 263 ml/min, the terminal T_1/2 is 1-2 hours.

Indications

• Inflammatory diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic arthritis, juvenile chronic arthritis, ankylosing spondylitis);
• Rheumatic diseases of soft tissues (tenosynovitis, bursitis, lesions of periarticular tissues);
• Degenerative diseases of the musculoskeletal system (osteoarthritis deformans, osteochondrosis);
• Post-traumatic inflammation of soft tissues and joints, for example, resulting from sprains, strains, and contusions;
• Pain syndrome and swelling associated with diseases of muscles and joints (rheumatoid arthritis, osteoarthritis, radiculitis, lumbago, sciatica, muscle pain of rheumatic and non-rheumatic origin).

ICD codes

Dosage Regimen

Externally.

For adults and children over 12 years of age, the drug is applied in a thin layer over the focus of inflammation 3-4 times/day and gently rubbed in. The required amount of the drug depends on the size of the painful area. A single dose of the drug is 2-4 g (comparable in volume to the size of a large cherry or a walnut). For children aged 6 to 12 years, use no more than 2 times/day, a single dose of the drug is up to 2 g.

After applying the drug, it is necessary to wash hands if this area is not being treated.

The duration of treatment depends on the indications and the observed effect. After 2 weeks of using the drug, you should consult a doctor.

Adverse Reactions

Local reactions: eczema, photosensitivity, contact dermatitis (itching, redness, swelling of the treated skin area, papules, vesicles, peeling).

Systemic reactions: generalized skin rash, allergic reactions (urticaria, angioedema, bronchospasm).

Contraindications

• History of bronchospasm attack, rhinitis, urticaria after taking acetylsalicylic acid or another NSAID;
• Erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase);
• III trimester of pregnancy;
• Lactation period;
• Children under 6 years of age;
• Impaired integrity of the skin;
• Hypersensitivity to diclofenac or other components of the drug, to acetylsalicylic acid or other NSAIDs.

Use with caution in patients with hepatic porphyria (exacerbation), erosive and ulcerative lesions of the gastrointestinal tract, severe impairment of liver and kidney function, chronic heart failure, bronchial asthma, in the I and II trimesters of pregnancy, and in elderly patients.

Use in Pregnancy and Lactation

The use of the drug is contraindicated in the III trimester of pregnancy. The use of the drug in the I and II trimesters is possible only after consultation with a doctor.

There is no experience with the use of the drug during lactation.

Use in Hepatic Impairment

The drug should be used with caution in severe liver dysfunction.

Use in Renal Impairment

The drug should be used with caution in severe renal dysfunction.

Pediatric Use

The use of the drug is contraindicated in children under 6 years of age.

Geriatric Use

The drug should be used with caution in elderly patients.

Special Precautions

The drug should be applied only to intact skin, avoiding contact with open wounds.

After application, an occlusive dressing should not be applied.

Avoid getting the drug into the eyes and mucous membranes.

When using the drug in conjunction with other dosage forms of diclofenac, the maximum daily dose should be taken into account.

When applied to large areas of the skin for a long time, the risk of developing systemic side effects characteristic of NSAIDs increases.

Before using the drug, patients with gastric and duodenal ulcers, bronchial asthma, rhinitis, polyps of the nasal mucosa, impaired liver, kidney, or hematopoietic system function, as well as when using other NSAIDs simultaneously, should consult a doctor.

Effect on the ability to drive vehicles and operate machinery

No effect.

Overdose

The extremely low systemic absorption of the active components of the drug during external use makes overdose practically impossible.

Drug Interactions

The drug may enhance the effect of drugs that cause photosensitivity.

No clinically significant interaction with other drugs has been described.

Storage Conditions

The ointment should be stored out of the reach of children at a temperature not exceeding 15°C (59°F); shelf life – 4 years.

The gel should be stored out of the reach of children at a temperature from 15°C (59°F) to 25°C (77°F); shelf life – 3 years.

Dispensing Status

The drug is approved for use as an over-the-counter product.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.