Fort-gel

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT FORT-GEL (FORT-GEL)

Composition:

Active substance: 1 g of gel contains 0.025 g of ketoprofen;

Excipients: ethanol 96%, carbomer, triethanolamine, lavender oil, purified water.

Pharmaceutical form. 2.5% gel.

Main physicochemical properties: colorless, almost transparent gel of homogeneous consistency, with a fragrant odor.

Pharmacotherapeutic group.

Non-steroidal anti-inflammatory drugs for topical use. Ketoprofen.

ATC code M02A A10.

Pharmacological properties.

Pharmacodynamics.

Ketoprofen belongs to nonsteroidal anti-inflammatory drugs (NSAIDs), propionic acid derivatives. It exerts analgesic and anti-inflammatory effects by inhibiting the activity of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), suppressing bradykinin activity, stabilizing lysosomal membranes, and inhibiting macrophage migration. Ketoprofen provides analgesic and anti-inflammatory effects at both the early stage (vascular phase) and late stage (cellular phase) of the inflammatory response. Ketoprofen also inhibits platelet aggregation.

Pharmacokinetics.

When applied topically, ketoprofen gel is absorbed through the skin and penetrates locally into inflamed tissues. Systemic absorption is very low (only about 5% of the applied dose).

The medicinal product applied to the skin rapidly penetrates into the affected area and maintains a therapeutic concentration locally. In contrast, absorption into the systemic circulation occurs slowly. After application of a gel containing 50 to 150 mg of ketoprofen, the plasma concentration of the active substance reaches no more than 0.08–0.15 mcg/mL within 5–8 hours, which produces almost no clinically significant systemic effects.

Clinical characteristics.

Indications.

Post-traumatic pain in muscles and joints, tendovaginitis.

Contraindications.

Hypersensitivity to ketoprofen or to any other excipients of the drug, salicylates, or other NSAIDs.

Known hypersensitivity reactions, such as bronchial asthma, allergic rhinitis, or urticaria following administration of ketoprofen, other NSAIDs, acetylsalicylic acid, fenofibrate, or tiaprofenic acid. Exacerbation of gastric or duodenal ulcer. History of gastrointestinal bleeding. Chronic dyspepsia (discomfort and pain in the upper abdomen). Severe renal insufficiency. Skin damage and disorders, skin injuries, irritation, pruritus, acne, burns (rash, eczema, skin infections). The gel must not be applied to damaged skin (dermatoses, open or infected wounds). Do not use occlusive dressings.

Any history of photosensitization reactions. History of skin allergic reactions induced by ketoprofen, other excipients of the drug, fenofibrate, tiaprofenic acid, ultraviolet (UV) blockers, or perfumes. Exposure to sunlight (even on cloudy days), including indirect sunlight and UV radiation in solariums, during the entire treatment period and for 2 weeks after discontinuation of the drug.

Third trimester of pregnancy, breastfeeding period.

Interaction with other medicinal products and other forms of interaction.

Monitoring is recommended for patients taking coumarins.

Concomitant use of other topical medicinal forms containing ketoprofen or other NSAIDs is not recommended, as it may enhance their effects as well as the adverse reactions they cause. Concurrent use of acetylsalicylic acid and ketoprofen reduces the plasma protein binding of ketoprofen. Simultaneous administration of probenecid and ketoprofen leads to reduced plasma clearance of ketoprofen and decreased extent of its protein binding. Ketoprofen, like other NSAIDs, reduces methotrexate excretion, thereby increasing its toxicity. Despite the low degree of ketoprofen absorption through the skin, its concomitant use with high doses of methotrexate is not recommended due to reduced methotrexate excretion, which significantly increases its toxicity.

Due to the increased risk of bleeding when ketoprofen is used concomitantly with oral anticoagulants or corticosteroids, the patient should be under continuous medical supervision. With anticoagulants, antiplatelet agents, acetylsalicylic acid or other NSAIDs, glucocorticoids – enhanced effects of the aforementioned drugs.

Concomitant use of ketoprofen with cardiac glycosides, lithium preparations, and cyclosporine increases their toxicity due to reduced excretion. Ketoprofen may reduce the effect of diuretics and antihypertensive drugs, enhance the efficacy of oral hypoglycemic agents – sulfonylurea derivatives, and some anticonvulsants (phenytoin). Concurrent use of ketoprofen with diuretics or angiotensin-converting enzyme inhibitors increases the risk of impaired renal function.

Ketoprofen may reduce the effect of mifepristone; therefore, at least 8 days must elapse between the end of mifepristone treatment and the initiation of ketoprofen therapy.

Special precautions for use.

The product should be used externally only. If a dose of the gel is missed, do not double the dose at the next application.

Although systemic adverse effects of ketoprofen with topical application are practically absent, the gel should be used with caution in patients with impaired kidney, heart, or liver function, with a history of peptic ulcer or intestinal inflammation, cerebrovascular hemorrhage, or hemorrhagic diathesis. Isolated cases of systemic adverse reactions related to kidney injury have been reported.

Do not apply the gel to the anal or genital area.

The gel should not be used concomitantly with other topical agents on the same skin areas. Topical application of large amounts of gel may provoke systemic effects, including bronchial asthma attacks and hypersensitivity reactions such as contact dermatitis, urticaria, and bronchospasm.

Do not exceed the recommended amount of gel or duration of treatment, as the risk of developing contact dermatitis and photosensitization reactions increases over time.

The gel should not be applied to damaged skin surfaces (e.g., eczema, open or infected wounds, dermatitis in the exudative phase). Avoid contact of the gel with mucous membranes, eyes, and the skin around the eyes. Do not use under occlusive dressings, over large skin areas, in amounts greater than necessary, or more frequently than required, and avoid open flames (since the product contains ethanol).

Octocrylene is an ingredient in some cosmetic and hygiene products such as shampoos, after-shave gels, shower gels, creams, lipsticks, anti-aging creams, makeup removers, and hair sprays, used to prevent their photodegradation.

If skin changes occur, treatment should be temporarily discontinued. Treatment should not be continued in the presence of pronounced irritation. Hands should be thoroughly washed after each application of the gel. Surgical gloves should be used if prolonged rubbing of Fort-gel is required.

Areas of skin treated with the product should be protected from sunlight (including UV radiation in solariums) during treatment and for 2 weeks after treatment to minimize any risk of photosensitization; discontinue treatment immediately if any skin reactions occur, including skin reactions following concomitant use with products containing octocrylene (some cosmetic and hygiene products).

Direct sunlight and UV radiation, including exposure in solariums, should be avoided during treatment and for 2 weeks after its completion.

The product should be prescribed with caution to patients taking anticoagulants, diuretics, or lithium salts. Regular monitoring is recommended for patients undergoing treatment with coumarin derivatives.

Topical application of large amounts of gel may provoke systemic effects, including bronchial asthma attacks and hypersensitivity reactions such as contact dermatitis, urticaria, and bronchospasm.

Elderly patients are more prone to adverse reactions when using NSAIDs.

Use during pregnancy or breastfeeding.

There are no clinical data on the use of Fort-gel during pregnancy. Even though systemic exposure to ketoprofen following topical application is lower than with oral administration, it is unknown whether it could be harmful to the embryo/fetus. Fort-gel should not be used during the first and second trimesters of pregnancy except in cases of extreme necessity. 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 synthetase inhibitors, including Fort-gel, may cause cardiopulmonary and renal toxicity in the fetus. Prolonged bleeding may occur in both mother and child near the end of pregnancy, and labor may be prolonged. Therefore, Fort-gel is contraindicated during the last trimester of pregnancy (see section "Contraindications").

Following systemic administration (oral, rectal, parenteral), traces of ketoprofen are found in breast milk. Ketoprofen should not be used during breastfeeding.

Ability to influence the speed of reactions when driving or operating machinery.

There are no data on the effect of Fort-gel on the ability to drive or operate machinery.

Method of Administration and Dosage.

Topical gel. Apply the preparation as a thin layer (3-5 cm of gel), gently rubbing it in until completely absorbed, twice daily. The duration of treatment is determined individually by a physician, but the use of the drug is recommended for no more than 10 days.

Fort-gel may be used in combination with other dosage forms of ketoprofen (capsules, tablets, rectal suppositories). The total maximum daily dose of ketoprofen should not exceed 200 mg, regardless of the dosage form used.

After applying the gel, hands should be washed, except when the gel is applied directly to the hands. If prolonged rubbing into the skin is required, protective gloves should be used.

Children.

The safety and efficacy of this medicinal product in this age group have not been established.

Overdose.

Accidental oral administration of ketoprofen may cause drowsiness, dizziness, nausea, vomiting, and epigastric pain. These symptoms usually resolve with appropriate symptomatic treatment. High doses of ketoprofen administered systemically may lead to bradypnea, coma, seizures, gastrointestinal bleeding, acute renal failure, and increased or decreased arterial blood pressure.

Systemic adverse effects may occur with prolonged use of Fort-gel, use in high doses, or application over large areas of skin.

Symptoms: skin irritation, erythema, and pruritus, or worsening of other adverse reactions.

Since the amount of ketoprofen penetrating through the skin into the blood plasma is low, overdose is unlikely. However, systemic adverse reactions are possible with prolonged application, high doses, or application over large skin areas. If excessive gel has been applied, the skin should be washed with water.

Possible adverse effects typical of NSAIDs: heartburn, nausea, epigastric discomfort, headache, dizziness.

Treatment: there is no specific antidote; symptomatic treatment with supportive care for vital functions is recommended. Gastric lavage and administration of activated charcoal (the first dose should be given with sorbitol) are recommended, especially within the first 4 hours after overdose or after ingestion of a dose 5–10 times higher than recommended. In case of irritation, erythema, or itching, the skin surface should be thoroughly rinsed with running water.

Adverse reactions.

Skin and subcutaneous tissue disorders: skin irritation, allergic skin reactions, hyperemia, erythema, burning sensation, pruritus, edema, urticaria, contact dermatitis, rash, eczema including vesicular, bullous, and phlyctenular forms, which may spread and become generalized, bullous dermatitis, exfoliative dermatitis, Stevens-Johnson syndrome, increased sweating; photosensitivity, including serious skin reactions following sun exposure (photosensitization); purpura, erythema multiforme, lichenoid dermatitis, skin necrosis. Very rarely, systemic adverse reactions may occur after prolonged use of the drug at high doses or application over large skin areas. There have been reports of local skin reactions that could subsequently extend beyond the application site.

Immune system disorders: hypersensitivity reactions, anaphylactic reactions, including angioneurotic edema, anaphylaxis, observed with both systemic and topical use of ketoprofen, bronchospasm, bronchial asthma attacks.

Respiratory system disorders: asthmatic attacks.

Urinary system disorders: worsening of kidney function; interstitial nephritis has been reported in isolated cases.

Gastrointestinal disorders: vomiting, dyspepsia, nausea, constipation, diarrhea, heartburn, peptic ulcers, gastrointestinal bleeding or perforation.

Nervous system disorders: headache, dizziness, vertigo, mood changes, somnolence or insomnia.

Depending on the permeability of the active substance, the amount of gel applied, the size of the treated area, the integrity of the skin, duration of treatment, and use of occlusive dressings, other hypersensitivity reactions, as well as adverse effects involving the gastrointestinal and urinary systems, are possible.

Elderly patients are more prone to adverse reactions when using NSAIDs. Ketoprofen may provoke bronchial asthma attacks in patients with hypersensitivity to acetylsalicylic acid or its derivatives.

The use of the drug should be discontinued if skin lesions or any other adverse reactions occur at the site of gel application.

Reporting of adverse reactions after drug registration is highly important. It enables ongoing monitoring of the benefit-risk balance of the medicinal product. Medical and pharmaceutical professionals, 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.

Storage conditions.

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

Keep out of reach of children.

Packaging.

30 g or 50 g in tubes, pack of 1.

Prescription status.

Prescription only.

Manufacturer/Applicant.

LLC "Ternopharm".

Manufacturer's/ Applicant's address and location of business activity.

4 Fabrychna Street, Ternopil, 46010, Ukraine.

Tel./Fax: (0352) 521-444, www.ternopharm.com.ua