Rapten gel

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT RAPTEN GEL (RAPTEN GEL)

Composition:

Active substance: diclofenac diethylamine;

1 g of gel contains 11.6 mg of diclofenac diethylamine (equivalent to 10 mg of sodium diclofenac);

Excipients: isopropyl alcohol, benzyl alcohol, sodium metabisulfite (E 223), carbomer 940, polysorbate 80, sorbitol solution (non-crystallizing), triethanolamine, purified water.

Pharmaceutical form. Gel.

Main physicochemical properties: transparent, colorless, homogeneous gel.

Pharmacotherapeutic group. Agents used locally for joint and muscular pain. Topical non-steroidal anti-inflammatory drugs. Diclofenac.

ATC code M02A A15.

Pharmacological Properties

Pharmacodynamics

Diclofenac is a highly effective non-steroidal anti-inflammatory agent with pronounced anti-rheumatic, analgesic, anti-inflammatory, and antipyretic effects. The main mechanism of diclofenac's therapeutic action is the inhibition of prostaglandin biosynthesis via cyclooxygenase-2 (COX-2).

In inflammation caused by injuries or rheumatic diseases, Rapten gel reduces pain and tissue swelling.

It has been reported that in inflammatory and traumatic or rheumatic pain, topical application of diclofenac reduces the recovery time of functions in affected organs and decreases acute pain and pain during movement.

Due to its water-alcohol base, the preparation also provides 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 applied and the degree of skin hydration. After topical application of 2.5 g of Rapten gel 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 Rapten gel to the skin over the wrist and knee joints, diclofenac is detected in blood plasma (where its maximum concentration is approximately 100 times lower than after oral administration), as well as in the synovial membrane and synovial fluid. Protein binding of diclofenac 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, rather than into blood plasma. There, it continues to act and is found in concentrations up to 20 times higher than in blood plasma.

Diclofenac is metabolized mainly by mono- or multi-stage hydroxylation followed by glucuronidation, or by glucuronidation of the intact molecule.

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 in plasma is 1–2 hours. Four metabolites, including two active ones, have short half-lives of 1–3 hours, while one has a slightly longer half-life but is almost inactive.

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 medicinal product;

• History of bronchial asthma attacks, angioedema, urticaria, or acute rhinitis induced by acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs;
• Third trimester of pregnancy.

Interaction with other medicinal products and other forms of interaction.

Since systemic absorption of diclofenac following topical application of the product is very low, the likelihood of interactions is very slight.

Special precautions for use.

The possibility of developing systemic adverse effects (which occur with systemic forms of diclofenac) should be considered when using the product on larger areas of skin or for longer periods than recommended.

Rapten gel should be applied only to intact, undamaged skin areas, avoiding contact with inflamed, wounded, or infected skin. Contact of the product with eyes and mucous membranes should be avoided. The product must not be swallowed.

If any skin rash occurs, treatment with the product should be discontinued. Rapten gel should not be used under occlusive, air-impermeable dressings, but its use under non-occlusive dressings is permitted.

Use during pregnancy or breastfeeding.

Pregnancy.

There are no clinical data on the use of Rapten gel during pregnancy. Even though systemic effects may be lower compared to oral administration, it is unknown whether the systemic exposure to Rapten gel following topical application could be harmful to the embryo/fetus. During the first and second trimesters of pregnancy, Rapten gel 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 Rapten gel, may cause cardiovascular 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, Rapten gel is contraindicated during the last trimester of pregnancy (see section "Contraindications").

It is unknown whether diclofenac is excreted in breast milk following topical application. Therefore, the use of Rapten gel during breastfeeding is permitted only if the expected benefit outweighs the potential risk to the infant. If there are strong reasons for using the product during breastfeeding, it should not be applied to the breasts or large skin areas, and should not be used in larger amounts or for longer periods than recommended.

There are no data on the effect of topical diclofenac on human fertility.

Ability to affect reaction speed when driving or operating machinery.

Diclofenac has no effect when applied topically.

Dosage and Administration

The product is intended for external use only.

For adults and children aged 14 years and older, Raptan gel should be applied 3–4 times daily, gently rubbed into the skin. The amount of product used depends on the size of the affected area (for example, 2–4 g of gel, corresponding in size to a cherry or a walnut, is sufficient for application to a skin area of 400–800 cm²).

After application, hands should be washed, 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 product should not be used for longer than 14 consecutive days for injuries or soft tissue rheumatism, or for longer than 21 days for arthritic pain, unless otherwise directed by a physician.

Children.

Raptan gel is not recommended for use in children under 14 years of age. When used in children over 14 years of age for longer than 7 days, or if disease symptoms worsen, medical advice should be sought.

Overdose.

Overdose is unlikely due to the low systemic absorption of diclofenac following topical application. However, adverse effects similar to those observed with overdose of diclofenac-containing tablets may occur following accidental ingestion of the product.

In case of accidental ingestion, gastric lavage should be performed immediately and an adsorbent agent administered. Symptomatic treatment is indicated, using therapeutic measures appropriate for poisoning with nonsteroidal anti-inflammatory drugs.

Side effects

Rapten gel is usually well tolerated. Adverse reactions include mild, transient skin reactions at the application site. In rare cases, allergic reactions may occur.

Infections and infestations:

Pustular rashes.

Immune system disorders:

Hypersensitivity reactions (including urticaria), angioneurotic edema.

Respiratory system disorders:

Bronchial asthma.

Skin and subcutaneous tissue disorders:

Rash, pruritus, eczema, erythema, dermatitis, including contact dermatitis; bullous dermatitis; photosensitivity reactions.

Shelf life. 3 years.

Storage conditions.

Store at a temperature not exceeding 25 °C.

Keep out of reach of children.

After first opening, store the preparation in the closed tube and use within 6 months.

Packaging. 40 g of gel in a tube; 1 tube in a cardboard box.

Supply category. Over-the-counter.

Manufacturer.

«Hemofarm» AD.

«Hemofarm» AD.

Manufacturer's address and place of business.

Beogradski put bb, 26300, Vrsac, Serbia.