Ibument

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT IBUMENT (IBUMENT)

Composition:

Active substances: ibuprofen, levomenthol;

1 g of gel contains ibuprofen 50 mg, levomenthol 30 mg;

Excipients: carbomer, ethanol (96%), propylene glycol, diethylamine, purified water.

Pharmaceutical form. Gel.

Main physicochemical properties: colorless, transparent or almost transparent gel with a characteristic odor. Opalescence and a yellowish tint may be present.

Pharmacotherapeutic group.

Topical preparations used for joint and muscle pain.

ATC code M02AX10.

Pharmacological properties.

Pharmacodynamics.

Ibument is a combined topical preparation containing ibuprofen and naturally derived menthol. Ibuprofen, a derivative of phenylpropionic acid, belongs to the group of nonsteroidal anti-inflammatory drugs (NSAIDs) and exerts analgesic and anti-inflammatory effects due to inhibition of prostaglandin synthetase. The action of levomenthol, the optical isomer of menthol, is mediated by reflex responses associated with stimulation of sensitive nerve endings in the skin. Menthol stimulates skin nociceptors, resulting in the release of peptides that produce vasodilatory effects. The preparation exerts a counterirritant, stimulating effect and relieves pain.

Pharmacokinetics.

When applied topically, ibuprofen is well and rapidly absorbed through the skin. Only a very small amount reaches the systemic circulation. Maximum plasma concentration of ibuprofen is achieved 2 hours after application and amounts to 0.6 μg/mL. The extent of ibuprofen absorption following topical administration is approximately 5% of that observed after oral administration.

Levomenthol absorbed through the skin is transported to the liver. Some Phase I metabolism may occur in the skin, but the majority takes place in the liver. Menthol undergoes hydroxylation, followed by conjugation with glucuronic acid, prior to circulation to the kidneys for urinary excretion.

Clinical characteristics.

Indications.

The medicinal product Ibument is recommended for relief of pain and reduction of inflammation in rheumatic, muscular and joint pain, in back pain, as well as in pain and swelling due to injury, ligament sprains and sports injuries.

Contraindications.

The medicinal product is contraindicated:

• in case of hypersensitivity to ibuprofen, levomenthol, acetylsalicylic acid or to any component of the product or to other NSAIDs (including oral administration);
• in asthma or in patients with a history of bronchial asthma attacks, urticaria, Quincke's edema, or acute rhinitis induced by acetylsalicylic acid or other NSAIDs;
• for application on damaged or denuded (epithelium-free) skin;
• for application on open wounds, inflammatory and infectious skin diseases such as weeping eczema, and for application on mucous membranes;
• in dermatoses;
• in presence of local infection;
• for simultaneous application on the same area with other topical medicinal products;
• in peptic ulceration of the gastrointestinal tract;
• during the third trimester of pregnancy.

Interaction with other medicinal products and other forms of interaction.

When used concomitantly with acetylsalicylic acid or other NSAIDs, the risk of adverse reactions increases. Nonsteroidal anti-inflammatory drugs may interact with antihypertensive agents, may reduce the diuretic effect of furosemide, and may enhance the effect of anticoagulants, although such likelihood is very low for topical preparations.

Special precautions for use.

The product contains propylene glycol, which may cause skin irritation; therefore, prior to first use, the patient's sensitivity to the medicinal product Ibument should be tested on a small area of skin.

Severe skin adverse reactions have been reported with the use of ibuprofen, including exfoliative dermatitis, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms (DRESS syndrome), and acute generalized exanthematous pustulosis, which may be life-threatening or lead to fatal outcomes (see section "Adverse reactions"). Most such reactions occurred within the first month of treatment.

If signs or symptoms indicating these reactions occur, ibuprofen should be discontinued immediately and alternative therapy should be considered (if necessary).

It is known that oral ibuprofen may exacerbate renal insufficiency or aggravate active peptic ulcer disease. Patients with impaired renal function, asthma, active peptic ulcer disease of the stomach or duodenum in medical history, and patients undergoing treatment with oral nonsteroidal anti-inflammatory drugs should consult a physician before using the product.

The gel must not be applied to mucous membranes, near mucous membranes, on lips, nostrils, around the eyes, genital areas, or the anal opening, nor on damaged, inflamed, or irritated skin. If the gel comes into contact with any of these areas, it should be immediately washed off with large amounts of clean water.

After applying Ibument gel, hands must always be washed unless they are the site of treatment.

If the product is ingested, the patient should immediately seek medical advice or go to the nearest emergency unit.

Airtight dressings must not be applied over the area where the gel has been applied.

The use of the medicinal product should be discontinued if rash or irritation occurs, and medical advice should be sought.

Adverse reactions may be minimized by using the lowest effective dose for the shortest possible duration.

If any adverse effects occur, or if there is no improvement or worsening of the condition, the patient should consult a physician.

The use of the medicinal product Ibument, like other drugs that inhibit cyclooxygenase/prostaglandin synthesis, may impair fertility, although this likelihood is lower with topically applied nonsteroidal anti-inflammatory drugs compared to oral formulations. For women who have difficulty conceiving or who are undergoing fertility investigations, discontinuation of Ibument may be considered.

Patients with bronchial asthma, hay fever, chronic lung disease, or hypersensitivity to analgesics and anti-rheumatic drugs have a higher risk of developing asthma attacks, mucosal swelling (angioedema, Quincke's edema), or urticaria compared to other patients. Systemic absorption of ibuprofen after topical application is lower than after oral administration; therefore, the aforementioned complications may occur only rarely. The use of the product in such patients should be performed under medical supervision.

Care should be taken to ensure that children do not come into contact with skin areas treated with the product.

Skin areas treated with the product should not be exposed to prolonged sunlight to avoid photosensitivity.

Use during pregnancy or breastfeeding.

Pregnancy

Inhibition of prostaglandin synthesis may adversely affect pregnancy and/or embryonic/fetal development. Epidemiological data indicate an increased risk of miscarriage, congenital heart defects, and gastroschisis following the use of prostaglandin synthesis inhibitors during early pregnancy. The absolute risk of cardiovascular malformation increased from less than 1% to approximately 1.5%. The risk is considered to increase with higher doses and longer duration of therapy. Animal studies have shown that administration of prostaglandin synthesis inhibitors leads to increased pre- and post-implantation loss and embryofetal mortality. In addition, an increased incidence of various developmental abnormalities, including cardiovascular defects, has been reported in animals treated with prostaglandin synthesis inhibitors during the organogenesis period. If ibuprofen is used by a woman attempting to conceive, the dose should be as low as possible and the duration of treatment as short as possible.

There are no clinical data on the topical use of the medicinal product Ibument during pregnancy. Even though systemic exposure is lower compared to oral administration, it is unknown whether systemic exposure to Ibument achieved after topical application could be harmful to the embryo/fetus. Ibument 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.

Systemic use of prostaglandin synthetase inhibitors, including the medicinal product Ibument, during the third trimester of pregnancy may cause cardiopulmonary and renal toxicity in the fetus. Prolonged bleeding may occur in both mother and child towards the end of pregnancy, and labor may be delayed. Therefore, Ibument is contraindicated during the last trimester of pregnancy (see section "Contraindications").

Breastfeeding period

Ibuprofen is excreted in breast milk in minimal amounts, and its effect on the breastfed infant is not expected. Topically applied ibuprofen as a monotherapy may be used during breastfeeding. However, there is insufficient information regarding the excretion of levomenthol and its metabolites into breast milk. In the absence of sufficient data, the use of the medicinal product Ibument during breastfeeding is not recommended.

Ability to affect reaction speed when driving or operating machinery.

Not established.

Dosage and Administration

For external use only.

Pierce the sealed opening of the tube with the spike located on the upper outer part of the cap.

Apply a 1–4 cm strip of gel from the tube with each application.

Apply the gel to the affected area and gently rub in until completely absorbed. May be used up to 3 times daily, but no more frequently than every 4 hours. If there is no improvement after two weeks, consult a physician.

Do not cover the area where the gel has been applied with a bandage.

Children

Ibument is contraindicated in children under 12 years of age.

Overdose

The likelihood of overdose when using ibuprofen in the form of a topical gel is low. However, in case of overdose, adverse effects associated with systemic use of ibuprofen may occur (dyspeptic symptoms: nausea, heartburn, vomiting, flatulence; skin allergic reactions; headache, drowsiness, dizziness; arterial hypotension). If symptoms of overdose occur, discontinue use of the medication and consult a physician.

In case of exceeding the recommended dose, wash the gel off with water. There is no known specific antidote. Correction of the electrolyte balance is indicated.

Side effects.

Skin and subcutaneous tissue disorders: Hypersensitivity reactions may manifest as skin purpura, Quincke edema; skin redness, skin irritation. Severe skin reactions (e.g., erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis) — very rare. Photosensitivity reaction, drug reaction with eosinophilia and systemic symptoms (DRESS syndrome), acute generalized exanthematous pustulosis — frequency unknown. Most commonly observed skin disorders include rash, urticaria, pruritus, dry skin, burning sensation, contact dermatitis.

Respiratory system, thoracic organs and mediastinum disorders: Hypersensitivity reactions such as asthma attacks or worsening of asthma, dyspnea, dyspnoea, and bronchospasm may occur in patients with a history of asthma attacks or allergic diseases.

Gastrointestinal disorders: Depending on the amount of gel applied, the application area, skin integrity, duration of treatment, and use of occlusive dressing, abdominal pain and dyspepsia are possible, although unlikely.

Renal and urinary disorders: Impaired renal function in patients with a history of kidney disease.

Immune system disorders: Hypersensitivity reactions, including anaphylactic shock, angioneurotic edema, and non-specific allergic reactions.

Other systemic adverse reactions to NSAIDs depend on the amount of gel applied, the surface area of application, skin integrity, duration of treatment, and use of an occlusive dressing.

Reporting of adverse reactions after drug registration is of great importance. It enables continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals and pharmacists, as well as patients or their legal representatives, are encouraged to report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at: https://aisf.dec.gov.ua.

Shelf life. 3 years.

Do not use after the expiry date.

Storage conditions.

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

Keep out of reach of children.

Incompatibility.

Do not use with other topical medicinal products.

Packaging.

50 g in a tube, 1 tube per carton.

Prescription status.

Over-the-counter.

Manufacturer.

JSC “CHEMICAL PHARMACEUTICAL PLANT “CHERVONA ZIRKA”

Manufacturer’s name and address of the place of business.

1 Gordienkovska Street, Kharkiv, Kharkiv region, 61010, Ukraine