Pharmacological properties
NSAIDs, a derivative of propionic acid. It has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is associated with inhibition of prostaglandin synthesis at the level of cyclooxygenase. In addition, ketoprofen inhibits lipoxygenase, has anti-bradykinin activity, stabilizes lysosomal membranes, and inhibits the release of enzymes involved in the inflammatory process.
Ketoprofen does not adversely affect articular cartilage.
Pharmacokinetics
When applied topically, ketoprofen is absorbed slowly and practically does not accumulate in the body. Bioavailability is 5%. Ketoprofen penetrates well into the subcutaneous tissue, ligaments and muscles, synovial fluid and reaches therapeutic concentrations there. The concentration of the drug in blood plasma is extremely low. Ketoprofen is metabolized in the liver to form conjugates, which are mainly excreted in the urine.
Ketoprofen metabolism does not depend on age, the presence of severe renal failure or cirrhosis.
Indications for use
Symptomatic therapy of painful and inflammatory processes of various origins, including:
- Rheumatoid arthritis and periarthritis;
- Ankylosing spondylitis (Bekhterev dicease);
- Psoriatic arthritis;
- Reactive arthritis (Reuters syndrome);
- Osteoarthrosis of various localization;
- Tendinitis, bursitis;
- Myalgia;
- Neuralgia;
- Sciatica;
- Injuries of the musculoskeletal system (including sports), bruises of muscles and ligaments and tendons of muscles.
Dosage and administration
A small amount of gel (3-5 cm) is applied in a thin layer on the skin over the lesion 1-2 times / day, gently rubbing into the skin. The dose depends on the area of the lesion, 5 cm of the gel corresponds to 100 mg of ketoprofen, 10 cm of the gel corresponds to 200 mg of ketoprofen.
The gel can be used in combination with other dosage forms (capsules, tablets, suppositories). The total maximum daily dose, regardless of dosage form, should not exceed 200 mg.
The duration of treatment without consulting a doctor is not more than 14 days.
The use of occlusive dressings is not recommended.
Side effects
Dermatological reactions: in 3% of cases, erythema, pruritus, mild transient dermatitis; rarely – photosensitivity. One case of severe contact dermatitis due to poor hygiene and sun exposure and 1 case of severe generalized dermatitis are described.
From the respiratory system: very rarely – asthmatic attacks (as an option for an allergic reaction).
From the urinary system: one case of impaired renal function in a patient with chronic renal failure after application of the gel has been described; in isolated cases, interstitial nephritis.
Contraindications
- A history of bronchospasm, urticaria, and rhinitis caused by NSAIDs and salicylates.
- Violation of the integrity of the skin (eczema, weeping dermatitis, open or infected wound);
- III trimester of pregnancy;
- Lactation period;
- Children’s age up to 12 years;
- Hypersensitivity to ketoprofen or other components of the drug, acetylsalicylic acid or other NSAIDs;
With caution: the drug should be prescribed in case of impaired liver and / or kidney function, erosive and ulcerative lesions of the gastrointestinal tract, blood diseases, bronchial asthma, chronic heart failure.
Use in the I and II trimesters is possible in cases where the expected benefit of therapy for the mother outweighs the potential risk to the fetus.
Drug interactions
Since the concentration of the drug in plasma is extremely low, manifestations of symptoms of interaction with other drugs (similar to symptoms with systemic use) are possible only with frequent and prolonged use.
The simultaneous use of other dosage forms (ointments, gels) containing ketoprofen or other NSAIDs is not recommended.
The simultaneous administration of acetylsalicylic acid reduces the degree of binding of ketoprofen to plasma proteins.
Ketoprofen reduces the excretion of methotrexate and contributes to an increase in its toxicity.
Interactions with other drugs and the effect on their elimination are not significant. When prescribing the drug to patients receiving coumarins, medical monitoring is recommended.
Special instructions
When applying the gel, avoid getting the drug on the mucous membranes of the eye and the skin around the eyes.
If side effects occur, discontinue use of the drug.
The total daily dose, regardless of dosage form, should not exceed 200 mg. During therapy and for 2 weeks after discontinuation of therapy, direct sunlight and ultraviolet radiation should be avoided. After applying the gel, wash your hands thoroughly.
If skin irritation occurs, therapy should be temporarily discontinued. With severe irritation, continued therapy is not recommended.
The drug should be stored out of the reach of children and not used after the expiration date.
Overdose
Symptoms: an overdose of ketoprofen in dosage forms for external use is not registered. Skin reactions are possible – irritation, erythema, itching.
Treatment: drug withdrawal; when applying the gel, thoroughly rinse the skin with running water. If necessary, carry out symptomatic therapy.
Release form
Gel for external use 2.5% for 15 g, 25 g, 30 g and 50 g in tubes. Tubes, along with instructions for use, are placed in a cardboard case.
Storage conditions
Store in a dry, dark place at a temperature of no higher than 25°C.
Shelf life
3 years.
Pharmacy sales terms
Without recipe.
