Instructions for use Ultrafastin gel for external use 2.5% tube 30 g
Composition
active ingredient: ketoprofen;
1 g of gel contains 25 mg of ketoprofen lysine salt;
excipients: polyethylene glycol 200, methyl parahydroxybenzoate (E 218), propyl parahydroxybenzoate (E 216), carbomer, triethanolamine, purified water.
Dosage form
Gel.
Main physicochemical properties: transparent or opalescent gel from colorless to light yellowish.
Pharmacotherapeutic group
Nonsteroidal anti-inflammatory drugs for topical use. ATC code M02A A10.
Pharmacological properties
Pharmacodynamics.
Ketoprofen has anti-inflammatory and analgesic effects.
Ketoprofen inhibits the activity of cyclooxygenase-1 and cyclooxygenase-2, resulting in a decrease in the synthesis of prostaglandins, which play a major role in the pathogenesis of inflammation and pain. The mechanism of anti-inflammatory action of ketoprofen is not fully understood. It reduces oxygen metabolism of neutrophils and the release of lysosomal enzymes, inhibits macrophage migration and exhibits antibradykinin activity. Properties of this type allow to shorten the second phase of the inflammatory reaction by reducing the migration of macrophages and granulocytes into the synovial membrane and the formation of cellular filtrates.
Pharmacokinetics.
Ketoprofen penetrates well through the skin and exhibits local anti-inflammatory and analgesic effects. Absorption and distribution depend on the thickness of the skin, subcutaneous tissue and its blood supply, as well as on the prevalence of inflammatory infiltrates. After topical application, the concentration of ketoprofen at the site of application is similar to that after internal administration, and the concentration in blood plasma shows a 60-fold decrease. The bioavailability of the gel is about 5%. About 99% of the absorbed ketoprofen binds to blood plasma proteins. The drug is metabolized in the liver. About 80% of the dose is excreted in the urine as metabolites, less than 10% is excreted unchanged. It does not accumulate in the body.
Indication
Post-traumatic pain in muscles and joints, tendon inflammation.
Contraindication
Any history of photosensitivity reactions;
known hypersensitivity reactions, such as symptoms of bronchial asthma, allergic rhinitis or urticaria, that occurred when using ketoprofen, fenofibrate, tiaprofenic acid, acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (NSAIDs);
history of skin allergy to ketoprofen, tiaprofenic acid, fenofibrate, ultraviolet (UV) blockers, or perfumes;
exposure to sunlight (even diffused light) or UV radiation in a solarium during treatment with the gel and for 2 weeks after its cessation;
hypersensitivity to any components of the drug;
Do not use the gel if there are pathological changes on the skin, such as weeping dermatoses, skin damage, rashes, skin injuries, burns, eczema or acne, or skin infections and open wounds;
3rd trimester of pregnancy;
childhood.
Interaction with other medicinal products and other types of interactions
Systemic absorption of ketoprofen when applied topically is very low and no reports of interactions with other drugs have been received during treatment with the drug, but the following interactions have been identified with the use of oral forms of ketoprofen or other NSAIDs.
Ketoprofen may inhibit the excretion of methotrexate and lithium salts and reduce the effectiveness of some diuretics, such as thiazides and furosemide. Concomitant use with high doses of methotrexate is not recommended due to a decrease in the excretion of methotrexate, which significantly increases its toxicity.
Concomitant use with acetylsalicylic acid or other non-steroidal anti-inflammatory drugs may enhance their effects and the adverse reactions caused by them.
Concomitant use of probenecid and ketoprofen leads to a decrease in the plasma clearance of ketoprofen and the degree of its protein binding.
The use of the drug simultaneously with anticoagulants, antithrombotic agents, and glucocorticosteroids enhances their effect.
With the simultaneous use of cardiac glycosides and cyclosporine with ketoprofen, their toxicity increases due to reduced excretion.
Ketoprofen may reduce the effect of diuretics and antihypertensive drugs, increase the effectiveness of oral hypoglycemic drugs - sulfonylurea derivatives, as well as some anticonvulsants (phenytoin).
Ketoprofen may reduce the effect of mifepristone, therefore at least 8 days should elapse between the course of mifepristone treatment and the start of ketoprofen therapy.
It is recommended to conduct regular examinations of patients taking coumarin drugs.
Application features
Despite the fact that systemic side effects of ketoprofen with topical application are practically absent, the gel should be used with caution in patients with impaired renal, cardiac or hepatic function, with a history of peptic ulcer or intestinal inflammation, cerebrovascular bleeding or hemorrhagic diathesis.
Caution should be exercised in patients with chronic bronchial asthma in combination with chronic rhinitis, sinusitis and/or polypous rhinitis. 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 drug should not be applied to mucous membranes, anal or genital area, as well as to large areas of skin, under airtight dressings, on the skin around the eyes. Prevent the gel from getting into the eyes. Do not exceed the recommended dosage and do not use the gel together with other topical products containing ketoprofen or other NSAIDs on the same areas of skin.
It is necessary to protect the treated skin areas from the sun (including UV rays in solariums) during treatment and for 2 weeks after treatment to reduce any risk of photosensitization. During treatment and for 2 weeks after its end, exposure to sunlight and solariums should be avoided.
The drug should be discontinued immediately if any skin reactions occur, including skin reactions after simultaneous use with products containing octocrylene (octocrylene is added to some cosmetic and hygiene products, such as shampoos, aftershave gels, shower gels, lipsticks, creams, including anti-aging creams, makeup removers, hairsprays, to delay their photodegradation).
The prescribed duration of treatment should not be exceeded due to the increased risk of developing contact dermatitis and hypersensitivity reactions with long-term use.
Hands should be washed after each application, unless the hands are the area to be treated. Protective gloves should be worn if prolonged rubbing into the skin is required.
Use during pregnancy or breastfeeding
I and II trimesters of pregnancy. Since safety studies of ketoprofen in pregnant women have not been conducted, its use should be avoided in the I and II trimesters of pregnancy. In the I and II trimesters, the use of the gel is possible only as prescribed by a doctor if 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 if the systemic exposure to ketoprofen achieved after topical application is lower compared to oral administration, it is not known whether Ultrafastin, gel, can be harmful to the embryo/fetus. During the first and second trimester of pregnancy, Ultrafastin, 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 synthetase inhibitors, including ketoprofen, may cause cardiopulmonary and renal toxicity in the fetus. At the end of pregnancy, prolonged bleeding may occur in both the mother and the child, and labor may be delayed. Therefore, Ultrafastin, gel, is contraindicated during the last trimester of pregnancy (see section "Contraindications").
After 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 using other mechanisms
Data is missing.
Method of administration and doses
For external use.
2-3 times a day, apply a small amount of gel (3-5 cm) in a thin layer to the skin of the affected area and rub in lightly. The duration of treatment is determined by the doctor individually. The amount of gel depends on the size of the injured area: 5 cm of gel corresponds to 100 mg of ketoprofen, 10 cm – 200 mg of ketoprofen.
There is no need to apply a dry bandage, because the gel is well absorbed through the skin, has no odor, does not contain dyes, does not leave greasy stains, and does not stain clothes.
Hands should be washed after applying the gel, except when applying the gel directly to the hands. If prolonged rubbing into the skin is necessary, protective gloves should be used.
Children
Do not use in children under 15 years of age.
Overdose
There is no specific antidote for ketoprofen overdose, symptomatic treatment is recommended along with maintaining vital body functions. Gastric lavage and administration of activated charcoal (the first dose should be administered together with sorbitol) are recommended if no more than 1 hour has passed since the overdose.
Side effects
Classification of side effects by organ system and frequency of occurrence: very common (≥ 1/10), common (≥ 1/100 and < 1/10), uncommon (≥ 1/1000 and < 1/100), rare (≥ 1/10,000 and < 1/1000), very rare < 1/10,000, including isolated reports, frequency unknown (cannot be estimated from the available data).
Immune system disorders: frequency unknown - angioedema and anaphylaxis, hypersensitivity reaction.
Skin and subcutaneous tissue disorders: infrequently - itching, erythema, vesicular eczema, burning sensation,
Rare: photosensitivity, urticaria. Severe reactions such as bullous rash or weeping eczema, which may be widespread or generalized.
On the part of the urinary system: very rarely - deterioration of renal function in a patient with chronic renal failure after topical application of ketoprofen.
Other effects (effects on the gastrointestinal tract, kidneys) arise as a result of penetration of the active substance through the skin, therefore they depend on the amount of gel used, the treated skin surface, the degree of absorption through the skin, the duration of treatment, and the presence or absence of a bandage.
Patients with hypersensitivity to acetylsalicylic acid and other NSAIDs may experience an attack of bronchial asthma.
Expiration date
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. 1 tube in a cardboard box.
Vacation category
According to the recipe.
Producer
Pharmaceutical Works POLPHARMA SA
Location
Medana Branch in Sieradz, 10, Wladyslawa Lokietka Str., 98-200 Sieradz, Poland / Medana Branch in Sieradz, 10, Wladyslawa Lokietka Str., 98-200 Sieradz, Poland
