Doloxene strong

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT DOLOXEN STRONG (DOLOXEN STRONG)

Composition:

Active substance: diclofenac sodium;

1 g of gel contains sodium diclofenac – 50 mg;

Excipients: ethanol 96%, glycerol, mineral oil, carbomer, hydrogenated polyethoxylated castor oil, methyl parahydroxybenzoate (E 218), propyl parahydroxybenzoate (E 216), ammonia solution 15%, propylene glycol, purified water.

Pharmaceutical form. Gel.

Main physicochemical properties: white or slightly yellowish-white gel of homogeneous consistency.

Pharmacotherapeutic group.

Agents used locally for joint and muscular pain. Topical non-steroidal anti-inflammatory agents. Diclofenac. ATC code M02A A15.

Pharmacological properties.

Pharmacodynamics.

Doloxen Strong is a non-steroidal anti-inflammatory agent with pronounced anti-rheumatic, analgesic, and anti-inflammatory properties. Its main mechanism of action is the inhibition of prostaglandin biosynthesis—mediators of pain and inflammation.

In inflammation caused by injuries or rheumatic diseases, Doloxen Strong reduces pain, tissue swelling, and shortens the recovery period of functions in damaged joints, ligaments, tendons, and muscles.

Pharmacokinetics.

Sodium diclofenac is slowly and partially absorbed through the skin surface. The amount of diclofenac absorbed through the skin is proportional to the application area and depends both on the total applied dose of the drug and on the degree of skin hydration. Maximum plasma concentration is observed within 6–9 hours. After oral administration, peak plasma concentration is reached approximately within 1–2 hours. The average duration of retention of the active substance in systemic circulation is about 9 hours, which is significantly longer compared to 1–2 hours after oral administration.

Diclofenac accumulates in the skin, which acts as a reservoir, allowing gradual release of the substance into adjacent tissues. From there, diclofenac primarily penetrates into deeper inflamed tissues, such as joints, where it continues to act and is found at concentrations up to 20 times higher than in plasma.

Metabolism and elimination of the drug after topical application are similar to those after systemic administration. Diclofenac and its metabolites are primarily excreted via urine. Total systemic plasma clearance of diclofenac is 263 ± 56 mL/min, and the terminal half-life averages 1–3 hours. Diclofenac is 99% bound to plasma proteins. Following rapid hepatic metabolism (hydroxylation and conjugation with glucuronic acid), approximately two-thirds of the substance is excreted by the kidneys and one-third via bile.

In renal or hepatic insufficiency, the metabolism and elimination of diclofenac from the body remain unchanged.

Clinical characteristics.

Indications.

Local treatment of pain and inflammation of joints, muscles, ligaments, and tendons of rheumatic or traumatic origin.

Contraindications.

Hypersensitivity to diclofenac, other nonsteroidal anti-inflammatory drugs (NSAIDs), or any other components of the medicinal product. History of attacks of bronchial asthma, urticaria, acute rhinitis, nasal polyps, or angioedema induced by acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs. Open wounds, inflamed or infected skin areas, eczema. Application to mucous membranes is contraindicated. Third trimester of pregnancy. Childhood.

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 occurrence of interactions is unlikely.

Special precautions for use.

The drug should be used with caution in combination with oral nonsteroidal anti-inflammatory agents.

The likelihood of developing systemic adverse effects with topical application of diclofenac is low compared to oral forms; however, it cannot be excluded when the drug is applied over relatively large skin areas for prolonged periods.

Doloxene Strong should be applied only to intact skin areas, avoiding contact with inflamed, damaged, or infected skin. Contact of the drug with eyes and mucous membranes should be avoided. The drug must not be used internally.

If any skin rashes occur, treatment with the drug should be discontinued.

Application under an occlusive, air-impermeable dressing is not recommended; however, use under a non-occlusive dressing is acceptable. In case of ligament sprain, the affected area may be bandaged with a bandage.

Patients should be warned about the need for caution when smoking or being near open flames, as there is a risk of sustaining severe burns.

Do not apply to open wounds or infected skin, or to skin areas affected by eczema, or to mucous membranes.

The medicinal product contains: propylene glycol, which may cause mild localized skin irritation; polyoxyl hydrogenated castor oil, which may cause skin reactions; methylparahydroxybenzoate (E 218) and propylparahydroxybenzoate (E 216), which may cause allergic reactions (possibly delayed).

Due to the possible development of photosensitivity, exposure to direct sunlight and visits to solariums should be avoided during treatment and for 2 weeks after discontinuation of treatment.

Use during pregnancy or breastfeeding.

Systemic concentrations of diclofenac after topical application are lower than after oral administration.

Based on experience with systemic nonsteroidal anti-inflammatory drugs (NSAIDs), the following recommendations can be provided.

Pregnancy

Inhibition of prostaglandin synthesis may have adverse effects on pregnancy and/or embryonic/fetal development. Therefore, women planning pregnancy should reduce the dosage to the minimum possible level and shorten the duration of treatment.

Epidemiological data suggest that use of prostaglandin synthesis inhibitors in early pregnancy is associated with an increased risk of miscarriage, congenital heart defects, and gastroschisis. The absolute risk of cardiac malformations increases from less than 1% to approximately 1.5%. This risk is considered to increase proportionally with dose and duration of treatment. Animal studies have shown that prostaglandin synthesis inhibitors increase the risk of pre-implantation and post-implantation embryonic/fetal loss. In addition, in animals, an increased risk of various developmental abnormalities (including cardiovascular defects) has been observed.

Clinical data on the use of diclofenac during pregnancy are lacking. Even though systemic exposure is lower compared to oral administration, it is unknown whether the systemic effects of diclofenac achieved after topical application may be harmful to the embryo/fetus. Diclofenac should not be used during the first and second trimesters of pregnancy 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").

Impaired fetal renal function leading to oligohydramnios has been observed with the use of NSAIDs (including diclofenac) from the 20th week of pregnancy.

Breastfeeding

Diclofenac passes into breast milk in small amounts. Therefore, the use of Doloxene Strong during breastfeeding is permitted only if the expected benefit, in the physician's opinion, outweighs the potential risk to the infant. If there are strong medical reasons for using the drug during breastfeeding, the gel should not be applied to the mammary glands or large skin areas, and should not be used in larger amounts or for longer than recommended.

Fertility.

There are no available data on the effect of topically applied diclofenac on human fertility.

Ability to affect reaction speed when driving or operating machinery.

No effect.

Method of Administration and Dosage

Doloxene Strong should be applied 3–4 times daily, gently rubbed into the skin. The amount of the drug used depends on the size of the affected area (for example, 2–4 g of gel, corresponding in volume to the size of a cherry or a walnut, is sufficient for application to an area of 400–800 cm²).

After application, hands should be washed, except when the hands themselves are the area being treated.

The duration of therapy depends on the nature of the disease and the effectiveness of treatment.

The drug should not be used for more than 14 consecutive days.

If the drug is used without a doctor's prescription and there is no improvement or if the patient's condition worsens after 7 days of treatment, medical advice should be sought.

Elderly patients (aged 65 years and older). There is no reason to believe that elderly patients require special dose adjustment or are more likely to experience adverse reactions different from those in other patients.

Patients with renal impairment. There is no reason to believe that patients with renal impairment require special dose adjustment.

Patients with hepatic impairment. There is no reason to believe that patients with hepatic impairment require special dose adjustment.

Children.

Dosage recommendations and therapeutic indications for the use of Doloxene Strong in children are not available.

Overdose.

Overdose is unlikely due to the low systemic absorption of diclofenac following topical application. In case of significant overdose, the gel should be wiped off the skin with a paper towel. The paper towel should be disposed of with household waste to prevent unused medication from entering the aquatic environment.

In case of accidental ingestion, note that one 100 g tube contains the equivalent of 5 g of sodium diclofenac, which may lead to systemic adverse reactions.

In case of accidental ingestion, the stomach should be emptied immediately, and an adsorbent should be administered. Symptomatic treatment should be provided, applying therapeutic measures commonly used in poisoning with nonsteroidal anti-inflammatory drugs.

Side effects.

Doloxen Strong is generally well tolerated. Adverse reactions include mild transient skin reactions at the site of application. Allergic reactions may occur rarely.

The assessment of adverse reactions is presented according to the frequency of occurrence: very common (≥ 1/10), common (≥ 1/100, < 1/10), uncommon (≥ 1/1000, < 1/100), rare (≥ 1/10,000, < 1/1000), very rare (< 1/10,000).

Infections and infestations: very rare – pustular rashes.

Skin and subcutaneous tissue disorders: common – dermatitis (including contact dermatitis), rash, pruritus, eczema, erythema; uncommon – redness, exanthema, burning sensation, development of swelling and vesicles, papules, pustules, skin peeling and dryness; rare – bullous dermatitis; very rare – photosensitivity reactions, generalized skin rashes, sensation of skin burning.

Immune system disorders: very rare – hypersensitivity reactions (including urticaria), angioneurotic edema of the face, dyspnea.

Respiratory system disorders: very rare – bronchial asthma.

Gastrointestinal system: adverse reactions occur very rarely after topical application of preparations containing diclofenac.

When the gel is used in high doses or applied over large areas of skin, the possibility of systemic adverse reactions cannot be excluded (e.g., adverse reactions affecting the kidneys, liver, or gastrointestinal tract, as well as hypersensitivity reactions such as angioedema, dyspnea).

Shelf life. 2 years.

Do not use after the expiry date stated on the packaging.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging.

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

100 g of gel in a laminated tube; 1 tube in a cardboard box.

Supply category. Over-the-counter.

Manufacturer.

PJSC “CHEMICAL PHARMACEUTICAL PLANT “CHERVONA ZIRKA”.

Manufacturer's address and place of business.

Ukraine, 61010, Kharkiv region, Kharkiv, Gordeyevskaya Street, 1.