Ultrafastin

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

Composition:

active substance: ketoprofen;

1 g of gel contains 25 mg of ketoprofen lysine salt;

excipients: polyethylene glycol 200, methylparaben (E 218), propylparaben (E 216), carbomer, triethanolamine, purified water.

Pharmaceutical form. Gel.

Main physico-chemical properties: transparent or opalescent gel, colorless to slightly yellowish.

Pharmacotherapeutic group. Topical non-steroidal anti-inflammatory drugs. ATC code M02A A10.

Pharmacological properties.

Pharmacodynamics.

Ketoprofen exerts anti-inflammatory and analgesic effects.

Ketoprofen inhibits the activity of cyclooxygenase-1 and cyclooxygenase-2, thereby reducing the synthesis of prostaglandins, which play a key role in the pathogenesis of inflammation and pain. The mechanism of ketoprofen's anti-inflammatory action is not completely understood. It reduces oxygen metabolism in neutrophils and the release of lysosomal enzymes, inhibits macrophage migration, and exhibits anti-bradykinin activity. These properties help reduce the second phase of the inflammatory response by decreasing the migration of macrophages and granulocytes into the synovial membrane and the formation of cellular exudates.

Pharmacokinetics.

Ketoprofen penetrates well through the skin and exerts local anti-inflammatory and analgesic effects. Absorption and distribution depend on skin thickness, subcutaneous tissue, blood supply, and the extent of inflammatory infiltrates. After topical application, the concentration of ketoprofen at the site of application is similar to that achieved with oral administration, while plasma concentrations are reduced approximately 60-fold. The bioavailability of the gel is about 5%. Approximately 99% of absorbed ketoprofen is protein-bound in plasma. The drug is metabolized in the liver. About 80% of the dose is excreted in urine as metabolites, less than 10% is excreted unchanged. It does not accumulate in the body.

Clinical characteristics.

Indications.

Post-traumatic pain in muscles and joints, tendon inflammation.

Contraindications.

• Any history of photosensitivity reactions;
• known hypersensitivity reactions, such as bronchial asthma symptoms, allergic rhinitis, or urticaria, occurring during use of ketoprofen, fenofibrate, tiaprofenic acid, acetylsalicylic acid, or other nonsteroidal anti-inflammatory drugs (NSAIDs);
• history of skin allergic reactions to ketoprofen, tiaprofenic acid, fenofibrate, ultraviolet (UV) light blockers, or perfumed products;
• exposure to sunlight (even diffused light) or UV irradiation in solarium during treatment with the gel and within 2 weeks after discontinuation of therapy;
• hypersensitivity to any component of the drug;
• the gel should not be applied in the presence of pathological skin conditions, such as weeping dermatoses, skin lesions, rashes, skin trauma, burns, eczema or acne, or skin infections and open wounds;
• third trimester of pregnancy;
• pediatric age.

Interaction with other medicinal products and other types of interactions.

Systemic absorption of ketoprofen after topical application is very low, and there have been no reports of interactions with other medicinal products during treatment with this drug. However, the following interactions have been observed with oral forms of ketoprofen or other NSAIDs.

Ketoprofen may inhibit the elimination of methotrexate and lithium salts and reduce the efficacy of certain diuretics, such as thiazides and furosemide. Concomitant use with high-dose methotrexate is not recommended due to reduced methotrexate excretion, which significantly increases its toxicity.

Concomitant use of ketoprofen with acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs may enhance their effects and increase the risk of adverse reactions.

Concomitant use of probenecid and ketoprofen leads to decreased plasma clearance of ketoprofen and reduced protein binding.

Concomitant use of the drug with anticoagulants, antiplatelet agents, and glucocorticoids enhances their effects.

Concomitant use of ketoprofen with cardiac glycosides or cyclosporine increases their toxicity due to reduced excretion.

Ketoprofen may reduce the effect of diuretics and antihypertensive agents, increase the effect of oral hypoglycemic agents—sulfonylurea derivatives—and some anticonvulsants (e.g., phenytoin).

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

Regular monitoring is recommended for patients taking coumarin derivatives.

Special precautions for use

The product is intended for topical use 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 use are practically absent, the gel should be used with caution in patients with impaired renal, cardiac, or hepatic function, a history of peptic ulcer or intestinal inflammation, cerebrovascular hemorrhage, or hemorrhagic diathesis.

Caution is necessary in patients with chronic bronchial asthma associated with chronic rhinitis, sinusitis, and/or nasal polyps. Patients in this group have an increased risk of developing allergic reactions to acetylsalicylic acid and/or other NSAIDs compared to the general population.

The medicinal product must not be applied to mucous membranes, the anal or genital areas, large areas of skin, under occlusive dressings, or to the skin around the eyes. Avoid contact of the gel with the eyes. Do not exceed the recommended dosage, and do not use the gel concurrently with other topical products containing ketoprofen or other NSAIDs on the same skin areas.

Areas of skin treated with the product must be protected from sunlight (including UV radiation in tanning beds) during treatment and for 2 weeks after treatment to minimize the risk of photosensitization. Exposure to sunlight and use of tanning beds should be avoided during treatment and for 2 weeks after its completion.

The product must be discontinued immediately if any skin reactions occur, including skin reactions following concomitant use with products containing octocrylene (octocrylene is added to certain cosmetic and hygiene products such as shampoos, shaving gels, shower gels, lipsticks, creams—including anti-aging creams, makeup removers, hair lacquers—to prevent their photodegradation).

The prescribed duration of treatment should not be exceeded due to the increasing risk of contact dermatitis and hypersensitivity reactions with prolonged use.

Hands should be washed immediately after each application, except when the hands themselves are the area being treated. If prolonged skin rubbing is required, protective gloves should be used.

Use during pregnancy or breastfeeding

First and second trimesters of pregnancy. Since safety studies of ketoprofen use in pregnant women have not been conducted, its use should be avoided during the first and second trimesters of pregnancy. Use of the gel during the first and second trimesters is possible only under medical supervision when the expected benefit to the mother outweighs the potential risk to the fetus.

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

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

Ability to influence reaction speed when driving or operating machinery

Data are lacking.

Method of Administration and Dosage

For external use only.

Apply a small amount of gel (3-5 cm) 2-3 times daily to the affected area of skin as a thin layer and gently rub in. The duration of treatment is determined individually by a physician. The amount of gel used depends on the size of the injured area: 5 cm of gel corresponds to 100 mg of ketoprofen, 10 cm corresponds to 200 mg of ketoprofen.

There is no need to apply a dry dressing, as the gel is well absorbed through the skin, is odorless, contains no dyes, does not leave greasy stains, and does not soil clothing.

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

Do not use in children under 15 years of age.

Overdose

Overdose with ketoprofen in gel form is unlikely. If excessive amounts of gel have been applied to the skin, wash the area with water. In case of accidental oral ingestion, ketoprofen may cause drowsiness, nausea, and vomiting, with severity depending on the amount ingested. High doses of ketoprofen with systemic administration may lead to respiratory depression, coma, convulsions, gastrointestinal bleeding, acute renal failure, and increased or decreased arterial blood pressure.

There is no specific antidote for ketoprofen overdose. Symptomatic treatment together with supportive measures to maintain vital functions is recommended. Gastric lavage and administration of activated charcoal (the first dose should be given with sorbitol) are recommended if less than 1 hour has passed since the overdose.

Side effects.

Classification of adverse effects by organ systems and frequency of occurrence: very common (≥ 1/10), common (≥ 1/100 and < 1/10), uncommon (≥ 1/1000 and < 1/100), rare (≥ 1/10000 and < 1/1000), very rare < 1/10000, including isolated reports, frequency unknown (cannot be estimated from available data).

Immune system disorders: frequency unknown – angioneurotic edema and anaphylaxis, hypersensitivity reaction.

Skin and subcutaneous tissue disorders: uncommon – pruritus, erythema, vesicular eczema, burning sensation;

rare – photosensitivity, urticaria. Severe reactions such as bullous rash or weeping eczema, which may spread or become generalized.

Renal and urinary disorders: very rare – worsening of renal function in patients with chronic kidney failure following topical application of ketoprofen.

Other effects (gastrointestinal tract, kidneys) occur due to systemic absorption of the active substance through the skin and therefore depend on the amount of gel used, the size of the treated skin area, the degree of skin absorption, duration of treatment, and the presence or absence of an occlusive dressing.

In patients with hypersensitivity to acetylsalicylic acid and other NSAIDs, bronchial asthma attacks may occur.

Shelf life. 3 years.

Storage conditions.

Store at a temperature not exceeding 25 °C, in a place protected from light.

Keep out of reach of children.

Packaging.

Tubes of 30 g or 50 g. One tube per cardboard box.

Prescription status. Prescription only.

Manufacturer.

Pharmaceutical Works POLPHARMA S.A.

Address:

Medana Branch in Sieradz, 10, Wladyslawa Lokietka Str., 98-200 Sieradz, Poland