Instructions Ketonal cream 5% tube 30 g
Composition
active ingredient: ketoprofen;
1 g of cream contains ketoprofen 50 mg;
Excipients: methylparaben (methyl parahydroxybenzoate) (E 218), propylparaben (propyl parahydroxybenzoate) (E 216), propylene glycol, isopropyl myristate, white soft paraffin, polyethylene glycol 45 and dodecyl glycol copolymer, glycerol sorbitan oleostearate, magnesium sulfate heptahydrate, purified water.
Dosage form
Cream.
Main physicochemical properties: white or almost white homogeneous cream.
Pharmacotherapeutic group
Topical agents for joint and muscle pain. Nonsteroidal anti-inflammatory drugs for topical use. ATX code M02A A10.
Pharmacological properties
Pharmacodynamics
Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and anti-inflammatory effects. Ketoprofen inhibits the activity of cyclooxygenase-1 and cyclooxygenase-2, which reduces 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 anti-bradykinin 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
With topical application, the absorption of ketoprofen is insignificant, which determines the local nature of the drug's action and the absence of systemic effects. The bioavailability of ketoprofen in the form of a cream is about 5%. The degree of binding to blood proteins is 99%. The active substance is found in synovial fluid in therapeutic concentrations; the concentration in blood plasma is insignificant.
With three-time application of 70-80 mg of ketoprofen in the form of a cream to the knee surface, the maximum concentration in blood plasma (0.0182 ± 0.118 μg/ml) is noted 6 hours after application of the drug. 12 hours after the last application of the cream to the skin of the knee, the following concentrations of ketoprofen are reproduced in the articular tissues: adipose tissue - 4.7 ± 3.87 μg/g, joint membrane - 2.35 ± 2.41 μg/g, synovial fluid - 1.31 ± 0.89 μg/g.
Ketoprofen is metabolized in the liver to form conjugates that are slowly excreted mainly in the urine. The metabolism of ketoprofen is not altered in elderly patients, with severe renal failure or cirrhosis of the liver.
Indication
Post-traumatic pain in muscles and joints, tendon inflammation.
Contraindication
Hypersensitivity to ketoprofen or other excipients of the drug, salicylates and other nonsteroidal anti-inflammatory drugs. Known hypersensitivity reactions, for example, symptoms of bronchial asthma, allergic rhinitis or urticaria after using ketoprofen, other NSAIDs, acetylsalicylic acid, fenofibrate, tiaprofenic acid. Any photosensitivity reactions in history. History of skin allergy manifestations that occurred when using ketoprofen, other excipients of the drug, fenofibrate, tiaprofenic acid, ultraviolet (UV) blockers or perfumes. Exposure to sunlight (even on a foggy day), including indirect sunlight and UV radiation in a solarium during the entire period of treatment and for 2 weeks after stopping treatment with the drug. Exacerbation of gastric or duodenal ulcer; history of gastrointestinal bleeding, chronic dyspepsia (discomfort and pain in the upper abdomen), severe renal failure. Skin damage, rashes, skin injuries, irritation, itching, skin infections, acne, burns. The cream should not be applied to damaged skin (eczema, dermatoses, open and infected wounds). Do not use airtight dressings.
Interaction with other medicinal products and other types of interactions
The simultaneous use of other topical medications containing ketoprofen or other NSAIDs is not recommended, as this may enhance their effects as well as the adverse reactions caused by them.
Despite the low degree of absorption of ketoprofen through the skin, its simultaneous use with high doses of methotrexate is not recommended due to a decrease in the excretion of methotrexate, resulting in a significant increase in methotrexate toxicity. Ketoprofen may slightly inhibit the excretion of methotrexate and lithium salts and reduce the effect of some diuretics, such as thiazides and furosemide.
Since the concentration of the drug in blood plasma is extremely low, manifestations of interaction with other drugs (as well as symptoms with systemic use) are possible only with frequent and prolonged use:
– with methotrexate, cardiac glycosides, lithium salts, cyclosporine – increased toxicity due to decreased excretion;
– enhancing the effect of the above-mentioned drugs; simultaneous use of the drug with other topical forms (ointments, gels) containing ketoprofen or other NSAIDs is not recommended;
– with antihypertensives, diuretics, mifepristone – weakening of the effect of the above-mentioned drugs. 8 days should elapse between the course of treatment with mifepristone and the start of therapy with ketoprofen.
With simultaneous use of acetylsalicylic acid and ketoprofen, the binding of ketoprofen to blood plasma proteins decreases.
Concomitant use of probenecid and ketoprofen leads to a decrease in the plasma clearance of ketoprofen and the degree of its binding to blood proteins.
Monitoring of patients taking coumarin is recommended.
Application features
The drug should be used externally only. If you miss the time to apply the cream, do not double the dose when applying the drug again.
Despite the fact that systemic side effects of ketoprofen with topical application are practically absent, the cream 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. Isolated cases of systemic adverse reactions associated with renal damage have been reported.
Do not apply the cream to mucous membranes, the anal or genital area, as well as to large areas of skin, under occlusive dressings, or on the skin around the eyes. Prevent the cream from getting into the eyes.
Do not use on damaged areas of skin (e.g. eczema, acne, infections or open wounds).
The cream should not be used together with other topical agents on the same skin areas. The recommended amount of cream and duration of treatment should not be exceeded, as the risk of developing contact dermatitis and photosensitivity reactions increases over time.
It is necessary to protect the treated skin from the sun (including UV rays from solariums) during treatment and for 2 weeks after its end to reduce any risk of photosensitivity. Areas where the cream is applied should be protected from sunlight with clothing.
The drug should be discontinued immediately if any skin reactions occur, including skin reactions after simultaneous use with products containing octocrylene (octocrylene is included in some cosmetic and hygiene products, such as shampoos, aftershave gels, shower gels, creams, lipsticks, anti-aging creams, makeup removers, hairsprays, to delay their photodegradation).
Hands should be washed thoroughly after each application of the cream. If the cream needs to be rubbed into the skin for a long time, surgical gloves should be used.
Local application of large amounts of cream may cause systemic effects, including asthma attacks and hypersensitivity reactions such as contact dermatitis, urticaria, and bronchospasm.
The cream contains methylparaben (E 218) and propylparaben (E 216), which may cause immediate-type (urticaria, bronchospasm) or delayed-type (contact dermatitis) hypersensitivity reactions.
Use during pregnancy or breastfeeding
The use of the drug is contraindicated in the 3rd trimester of pregnancy, in the 1st and 2nd trimesters the use of the cream is possible only as prescribed by a doctor in the case when the expected benefit to the mother outweighs the potential risk to the fetus. All prostaglandin synthesis inhibitors, including ketoprofen, cause toxic damage to the cardiopulmonary system and kidneys of the fetus.
At the end of pregnancy, bleeding time may increase in both the mother and the baby.
NSAIDs can cause delayed labor, so the use of the drug is contraindicated in the third trimester of pregnancy.
Breastfeeding should be discontinued during treatment with ketoprofen.
Ability to influence reaction speed when driving vehicles or other mechanisms
Data is missing.
Method of administration and doses
For external use.
The cream should be applied to the skin of the affected area with a thin layer 2 times a day and rubbed in carefully. The amount of cream depends on the size of the affected area. The drug should be used, as a rule, for no more than 10 days. The cream can be used in combination with other dosage forms (capsules, tablets, suppositories). The total maximum daily dose should not exceed 200 mg of ketoprofen, regardless of the dosage form used.
The use of compressive and airtight bandages is not recommended. Hands should be washed after applying the drug, except when applying the cream directly to the hands.
Children
There is no data, so the drug should not be prescribed to this category of patients.
Overdose
Symptoms: irritation, erythema, itching or increased manifestations of other adverse reactions.
In case of accidental ingestion of ketoprofen, the drug may cause drowsiness, dizziness, nausea, vomiting, and epigastric pain. These symptoms usually resolve after appropriate symptomatic treatment. High doses of ketoprofen when administered systemically may cause bradypnea, coma, convulsions, gastrointestinal bleeding, acute renal failure, and increased or decreased blood pressure.
Treatment: There is no specific antidote, 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, especially in the first 4 hours after overdose or when using a dose 5-10 times higher than the recommended dose.
Adverse reactions
On the part of the immune system: hypersensitivity reactions, anaphylactic reactions, including angioedema, and anaphylaxis, observed with systemic and local use of ketoprofen, bronchospasm, attacks of bronchial asthma.
Skin and subcutaneous tissue disorders: skin irritation, allergic skin reactions, flushing, itching, rash, burning, swelling, erythema, eczema, including vesicular, bullous and phlyctenulosis, which can spread and become generalized; purpuric, bullous rash; increased sweating, urticaria, dermatitis (contact, exfoliative); photosensitivity, including serious skin reactions from exposure to the sun; purpura, erythema multiforme, lichen-like dermatitis, skin necrosis, Stevens-Johnson syndrome. There have been reports of local skin reactions that may subsequently extend beyond the site of application.
On the part of the digestive tract: heartburn, peptic ulcer, gastrointestinal bleeding, nausea, vomiting, diarrhea or constipation (with prolonged use).
Urinary system: a case of deterioration of renal function in a patient with chronic renal failure after topical application of ketoprofen has been described. In isolated cases, interstitial nephritis has occurred.
Depending on the penetrating ability of the active substance, the amount of cream applied, the area of the treated area, the integrity of the skin, the duration of use of the drug and the use of hermetic dressings, other adverse reactions of hypersensitivity, adverse reactions from the digestive tract and urinary system are possible. Elderly patients are more prone to adverse reactions when using non-steroidal anti-inflammatory drugs.
Ketoprofen may cause attacks of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid or its derivatives.
Expiration date
5 years.
Storage conditions
Store at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
30 g of cream in a tube, 1 tube in a cardboard box.
Vacation category
According to the recipe.
Producer
Salutas Pharma GmbH, Germany.
Location of the manufacturer and its business address
Lange Gohren 3, gemass den Lageplanen Nr. 1-5, 39171 Sulzetal, OT Osterweddingen, Saxony-Anhalt, Germany/Lange Gohren 3, gemass den Lageplanen Nr. 1-5, 39171 Sulzetal, OT Osterweddingen, Saxony-Anhalt, Germany.
