Diclac^® Lipogel (Gel) Instructions for Use

Marketing Authorization Holder

Sandoz, d.d. (Slovenia)

Manufactured By

Salutas Pharma, GmbH (Germany)

ATC Code

M02AA15 (Diclofenac)

Active Substance

Diclofenac (Rec.INN registered by WHO)

Dosage Form

Diclac® Lipogel

Gel for external use 1%: tubes 50 g or 100 g

Dosage Form, Packaging, and Composition

50 g – aluminum tubes (1) – cardboard boxes.
100 g – aluminum tubes (1) – cardboard boxes.

Clinical-Pharmacological Group

NSAIDs for external use

Pharmacotherapeutic Group

NSAID

Pharmacological Action

NSAID for external use, a derivative of phenylacetic acid. It has anti-inflammatory and analgesic effects.

The mechanism of action is due to the inhibition of COX-1 and COX-2 activity, which leads to disruption of arachidonic acid metabolism and the synthesis of prostaglandins, which are a key component in the development of inflammation.

When applied externally, it leads to the disappearance or reduction of pain at the site of application, reduces joint pain at rest and during movement, as well as morning stiffness and joint swelling.

It helps to increase the range of motion in the affected joints.

Pharmacokinetics

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 applied drug and on the degree of skin hydration.

The binding of diclofenac to plasma proteins is 99.7%, mainly to albumin (99.4%). Diclofenac is predominantly distributed and retained deep in tissues subject to inflammation, such as joints, where its concentration is 20 times higher than in plasma.

The metabolism of diclofenac occurs partially by glucuronidation of the unchanged molecule, but predominantly through single and multiple hydroxylation, leading to the formation of several phenolic metabolites, most of which are converted into glucuronide conjugates.

Two phenolic metabolites are biologically active, but to a much lesser extent than Diclofenac.

The total systemic plasma clearance of diclofenac is 263±56 ml/min.

The terminal T_1/2 is 1-2 hours. The 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 T_1/2, but this metabolite is completely inactive.

Most of diclofenac and its metabolites are excreted in the urine.

Indications

Back pain in inflammatory and degenerative diseases of the spine (radiculitis, osteoarthritis, lumbago, sciatica); joint pain (including finger joints, knees) in rheumatoid arthritis, osteoarthritis; muscle pain (due to sprains, overexertion, bruises, injuries); inflammation and swelling of soft tissues and joints due to injuries and in rheumatic diseases (tenosynovitis, bursitis, lesions of periarticular tissues).

ICD codes

Dosage Regimen

For external use, the amount of the drug depends on the size of the painful area.

The single dose depends on the dosage form used and the age of the patient.

Gel, ointment, spray for external use

Adults and children over 12 years of age should apply the drug to the skin over the area of inflammation 3-4 times/day, Children aged 6 to 12 years – up to 2 times/day.

The duration of use depends on the indications and the effectiveness of the treatment. After 2 weeks of using the drug, the patient should consult a doctor.

Transdermal patch

Apply as applications to the skin.

Adults, elderly patients, and adolescents over 15 years of age should apply the patch to the skin over the painful area for 24 hours. Only 1 patch may be used within 24 hours.

For the treatment of soft tissue injuries, the patch should be used for no more than 14 days, and for the treatment of muscle and joint diseases – no more than 21 days, unless otherwise recommended by a doctor.

If there is no improvement after 7 days or if the condition worsens, it is necessary to consult a doctor.

Adverse Reactions

Definition of adverse reaction frequency: very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥1/10 000, <1/1000) and very rare (<10 000), frequency unknown (frequency cannot be estimated from the available data).

Infections and infestations: very rare – pustular rash.

Immune system disorders: very rare – generalized skin rash, allergic reactions (urticaria, hypersensitivity: angioedema).

Respiratory, thoracic and mediastinal disorders: very rare – asthma attacks, bronchospastic reactions.

Skin and subcutaneous tissue disorders: common – erythema, dermatitis, including contact dermatitis (symptoms: eczema, itching, swelling of the treated skin area, rash, papules, vesicles, peeling); rare – bullous dermatitis; very rare – photosensitivity reactions.

Contraindications

“Aspirin triad” (attacks of bronchial asthma, urticaria and acute rhinitis when taking acetylsalicylic acid or other NSAIDs); impaired skin integrity at the site of application of the drug; III trimester of pregnancy; lactation period (breastfeeding); children under 6 years of age and older, depending on the drug used; hypersensitivity to diclofenac, other NSAIDs or to any of the excipients of the drug used.

With caution: hepatic porphyria (in the acute phase); erosive and ulcerative lesions of the gastrointestinal tract; severe impairment of liver and kidney function; chronic heart failure; bronchial asthma; blood clotting disorders (including hemophilia, prolonged bleeding time, tendency to bleed); I and II trimesters of pregnancy; elderly patients.

Use in Pregnancy and Lactation

Contraindicated in the III trimester of pregnancy due to the possibility of reducing uterine tone and/or premature closure of the fetal arterial duct.

Use in the I and II trimesters of pregnancy is possible in cases where the potential benefit to the mother outweighs the potential risk to the fetus or infant.

Use during lactation (breastfeeding) is contraindicated.

Use in Hepatic Impairment

Use with particular caution in patients with a history of liver disease.

Use in Renal Impairment

Use with particular caution in patients with a history of kidney disease.

Pediatric Use

Not recommended for use in children under 6 years of age.

Geriatric Use

Use with particular caution in elderly patients.

Special Precautions

Apply only to intact skin areas.

Avoid contact of the drug with eyes, mucous membranes, or open wounds.

Should not be used under airtight (occlusive) dressings.

Caution is required when applying large amounts of the drug to large areas of sensitive skin for a prolonged period. When used with other dosage forms of diclofenac, the total maximum daily dose should be considered.

Avoid prolonged exposure to sunlight during use.

Drug Interactions

Drugs that cause photosensitization – enhanced effect of drugs capable of causing photosensitization.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

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.