Ketoprofen gel for external use 2.5% 30g
Compound
Active substance: ketoprofen 2.5 g.
Excipients: carbomer - 1.5 g, ethanol 95% - 32 g, trolamine - 2.9 g, lavender oil - 0.1 g, water - up to 100 g.
Pharmacokinetics
Ketoprofen is absorbed very slowly and practically does not accumulate in the body. Bioavailability is 5%. Ketoprofen penetrates into the subcutaneous tissue, ligaments and muscles, synovial fluid and reaches therapeutic concentrations there. The concentration of the drug in the blood plasma is extremely low. Ketoprofen is metabolized in the liver to form conjugates, which are mainly excreted in the urine. Ketoprofen is characterized by slow excretion in urine.
Indications for use
- Acute and chronic inflammatory diseases of the musculoskeletal system (articular syndrome with exacerbation of gout, rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, osteoarthritis, osteochondrosis with radicular syndrome, radiculitis, inflammatory damage to ligaments and tendons, bursitis, sciatica, lumbago);
- muscle pain of rheumatic and non-rheumatic origin;
- post-traumatic inflammation of soft tissues and the musculoskeletal system (damage and rupture of ligaments, bruises).
The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, and does not affect the progression of the disease.
Contraindications
- Individual hypersensitivity to ketoprofen or other components of the drug, acetylsalicylic acid or other NSAIDs (history of bronchospasm, urticaria or rhinitis caused by taking acetylsalicylic acid), tiaprofenic acid and fenofibrate;
- complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including a history);
- a history of increased skin sensitivity to solar radiation (photosensitivity);
- history of skin allergies to sunscreens or perfumes;
- exposure to the sun on the treated areas, including solariums, during the course of using the drug and 2 weeks after;
- weeping dermatoses, eczema, infected abrasions, wounds (at the site of application of the gel);
- children under 12 years of age (efficacy and safety have not been studied);
- pregnancy (III trimester) and breastfeeding period.
With caution:
Hepatic porphyria (exacerbation), erosive and ulcerative lesions of the gastrointestinal tract, severe dysfunction of the liver and kidneys, chronic heart failure, bronchial asthma, old age, pregnancy (I and II trimester).
Directions for use and doses
For external use.
A strip of gel 5-10 cm long is applied in a thin layer to the affected area or skin over the source of inflammation 2 times a day and rubbed in lightly.
The amount of gel applied depends on the size of the area being treated.
It is possible to use ketoprofen in combination with physiotherapy (phonophoresis and iontophoresis).
The dosage in children over 12 years of age corresponds to that in adults and depends on the area of application and the doctor’s recommendations.
Storage conditions
In a dark place at a temperature not exceeding 25° C. Keep out of the reach of children.
Best before date
3 years. Do not use after the expiration date.
special instructions
Do not apply to damaged (including open wounds) and inflamed skin!
Avoid contact with eyes (risk of conjunctival irritation).
It is recommended to wash your hands thoroughly after using the drug.
Do not use as hermetic dressings. Do not use in combination with sealed clothing.
Long-term use of topical agents may result in sensitization or local irritation.
To avoid any manifestations of hypersensitivity or photosensitivity, exposure to direct sunlight (including visiting a solarium) should be avoided during the treatment period and for two weeks after using the drug, and it is recommended to cover the treated areas with clothing. Patients with severe renal, cardiac or hepatic impairment should be careful when using ketoprofen.
You should stop using the drug if any skin reaction occurs, including reactions when simultaneously applying sunscreen or other cosmetics containing the organic sunscreen filter octocrylene to the skin.
When using the drug in large quantities, it is possible, in very rare cases, to develop systemic side effects (hypersensitivity, bronchial asthma, gastrointestinal disorders, aggravation of renal failure).
The risk of systemic side effects increases depending on the amount of gel applied, the area of the skin being treated, the condition of the skin, and the duration of treatment.
Avoid exposure of treated areas to sunlight or UV rays, including tanning beds, during treatment and for two weeks after treatment.
Description
Non-steroidal anti-inflammatory drug (NSAID).
Use in children
Contraindicated in children under 12 years of age (efficacy and safety have not been studied).
Pharmacodynamics
NSAIDs. It has analgesic, anti-inflammatory and anti-edema effects. Inhibits the activity of COX, which leads to inhibition of prostaglandin synthesis. In addition, ketoprofen inhibits lipoxygenase, bradykinin synthesis, stabilizes lysosomal membranes and prevents the release of enzymes involved in the inflammatory process.
Ketoprofen does not have a negative effect on the condition of articular cartilage.
Side effects
Possible side effects are listed in descending frequency of occurrence: very common (> 10%), common (> 1%, < 10%), uncommon (> 0.1%, < 1%), rare (> 0.01%, < 0.1%), very rare (<0.01%).
From the skin: infrequently - erythema, itching, eczema; rarely - photosensitivity, bullous dermatitis, urticaria; very rarely - contact dermatitis, angioedema.
From the gastrointestinal tract: very rarely - peptic ulcer, bleeding, diarrhea.
From the immune system: very rarely - anaphylactic reactions, hypersensitivity reactions.
From the urinary system: very rarely - aggravation of renal failure.
Use during pregnancy and breastfeeding
The use of the drug during breastfeeding is not recommended.
Interaction
When ketoprofen is used externally in the form of a gel, it is possible to enhance the effect of drugs that cause photosensitivity. Other interactions have not been established, however, patients taking coumarin anticoagulants are recommended to regularly monitor the international normalized ratio (INR).
Overdose
The extremely low systemic absorption of the active components of the drug when used externally makes overdose almost impossible.
If large quantities of the drug (more than 20 g) are accidentally ingested, systemic adverse reactions characteristic of NSAIDs may occur. It is necessary to lavage the stomach and take activated charcoal. Treatment is symptomatic.
Impact on the ability to drive vehicles and operate machinery
The drug does not affect the ability to drive a car or use other mechanical means.
Ketoprofen gel 25mg/g 30g
Name
Ketoprofen gel dnar.approx. 25 mg in tubes 30 g in pack No. 1
Description
Colorless transparent or almost transparent gel, homogeneous in consistency with an aromatic odor. Air bubbles are allowed.
Main active ingredient
Ketoprofen
Release form
gel
Dosage
2.5% 30 g
Pharmacological properties
Pharmacodynamics
With the appropriate composition of excipients, ketoprofen reaches the area of inflammation through the skin, thus providing the possibility of local treatment of lesions of joints, tendons, ligaments and muscles accompanied by pain.
Pharmacokinetics
After oral administration of a single dose of ketoprofen, its maximum concentration in the blood is achieved within 2 hours. The half-life of ketoprofen from plasma ranges from 1 to 3 hours. Plasma protein binding is 60-90%. Excretion occurs mainly in the urine, in the form associated with glucuronic acid; approximately 90% of the administered dose is eliminated within 24 hours. Absorption of a drug administered through the skin, on the contrary, occurs very slowly. Even with the introduction of 50 to 150 mg of ketoprofen through the skin, the concentration of the active substance in the blood plasma after 5-8 hours is 0.08-0.15 μg/ml.
Indications for use
Local treatment for pain in muscles, bones or joints of rheumatic or traumatic origin: for example, bruises, sprains, muscle strains, stiff neck, lumbago.
Directions for use and doses
Ketoprofen gel should be applied topically. It is applied to the affected area 1-3 times a day. The recommended duration of treatment is no more than 7 days. For better absorption, the application of the gel should be accompanied by light rubbing. With one application, a strip of gel 5-10 cm long (2 g) is applied.
Use during pregnancy and lactation
In the first and second trimester, no teratogenic or embryotoxic effects were observed in a study in mice and rats. In a study in rabbits, a small embryotoxic effect was noted, probably related to maternal toxicity. Since there have been no studies on the safety of ketoprofen in pregnant women, its use should be avoided in the first and second trimester of pregnancy. In the third trimester of pregnancy, all inhibitors of prostaglandin synthesis, including ketoprofen, cause toxic damage to the cardiopulmonary system and kidneys in the fetus. Late in pregnancy, both mother and baby may experience longer bleeding times. In this regard, ketoprofen is contraindicated in the third trimester of pregnancy. Use during lactation There are no data on the passage of ketoprofen into mother's milk. Ketoprofen is not recommended for use in nursing mothers.
Precautionary measures
The gel should be used with caution in patients with cardiac, hepatic or renal impairment. Isolated cases of systemic side effects associated with kidney damage have been reported. Local use of large quantities of the drug may lead to systemic effects such as hypersensitivity or asthma. If a rash appears, treatment with the drug must be stopped. During treatment with the drug, as well as in the next 2 weeks, it is necessary to avoid direct sunlight, including solariums. The recommended duration of treatment should not be exceeded, since the risk of developing contact dermatitis and photosensitivity reactions increases over time. After each use of the medicine, you should wash your hands thoroughly. If any skin reactions develop, including those associated with concomitant use of products containing octocrylene, treatment with the gel should be discontinued immediately. To avoid the development of skin photosensitivity, it is recommended to protect the areas to which the drug is applied with clothing - during treatment and for two weeks after its cessation. The use of the gel should not be combined with wearing an occlusive dressing. The gel should not come into contact with mucous membranes or eyes. The gel should not be used on areas of the skin where there are signs of damage, such as eczema, acne, infection or open wounds. Patients with asthma in combination with chronic rhinitis, chronic sinusitis, and/or nasal polyposis are at increased risk of allergic reactions to aspirin and/or NSAIDs compared to the general population. Use in the elderly When prescribing the drug to elderly patients, no dose adjustment is required. Use in children The safety and effectiveness of using ketoprofen gel in children has not been established.
Interaction with other drugs
There have been no reports of interactions between Ketoprofen gel and other drugs. Interactions with other drugs are unlikely because, due to local application, the concentration of the drug in the blood is low. However, regular monitoring of patients taking coumarin drugs is recommended.
Contraindications
Ketoprofen is contraindicated in the following cases:
- hypersensitivity to ketoprofen and/or to any of the excipients of the drug;
- any history of photosensitivity reactions;
- known hypersensitivity reactions, such as asthma symptoms, allergic rhinitis or urticaria, that have occurred with the use of ketoprofen, fenofibrate, tiaprofenic acid, acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (NSAIDs);
- a history of skin allergies when using ketoprofen, tiaprofenic acid, fenofibrate, UV blockers or perfume products;
- exposure to sunlight (even scattered light) or UV irradiation in a solarium during gel treatment and for 2 weeks after its cessation;
- ketoprofen is contraindicated in patients with hypersensitivity to any of the excipients of the drug;
- the gel should not be used on areas of the skin damaged or altered by a pathological process, for example, eczema, acne, various dermatoses, open wounds or infectious lesions, as well as on the area around the eyes;
- third trimester of pregnancy (see section "Precautions").
Compound
1 g of gel contains: active ingredient: ketoprofen – 25 mg; excipients: carbomer 980, ethyl alcohol 96%, lavender oil, macrogol 400, diethanolamine, purified water.
Overdose
When applied topically, an overdose is unlikely. If the gel is accidentally swallowed, systemic side effects may develop, the severity of which depends on the amount of the drug swallowed. However, if overdose occurs, symptomatic and supportive treatment should be provided, consistent with treatment for overdose of anti-inflammatory drugs.
Side effect
Like all medicines, Ketoprofen can cause side effects, although not everyone gets them. Local skin reactions have been reported, which may subsequently extend beyond the site of application of the drug. Rare phenomena include cases of more severe reactions, such as bullous or phlyctenulous eczema, which can spread and become generalized. The frequency and severity of these effects are significantly reduced by limiting exposure to sunlight (even diffuse light) or UV irradiation in a tanning bed during gel treatment and for 2 weeks after its cessation. Other side effects of anti-inflammatory drugs (hypersensitivity, disorders of the gastrointestinal tract and kidneys) depend on the penetration of the active ingredient through the skin and, therefore, on the amount of gel applied, the area of the treated surface, the integrity of the skin, the duration of treatment and the use of occlusive dressings. The following side effects have been reported since marketing. They are listed by organs and organ systems and classified according to frequency of occurrence: very common (?1/10); often (? 1/100 to
Storage conditions
At a temperature not higher than 25 °C. Keep out of the reach of children.
Ketoprofen
Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID), a derivative of methylacetic acid. It is used mainly for the treatment of inflammatory and degenerative diseases of the musculoskeletal system, diseases of the joints and spine. It has analgesic, anti-inflammatory and antipyretic effects. It is used as a symptomatic remedy, i.e. in order to eliminate the negative manifestations of the disease, but not its causes. One of the main objectives of the drug is pain relief. Pain is the main reason for seeking medical help. First of all, this applies to elderly patients, whose general condition is affected by the presence of multiple concomitant pathologies. And given the trend towards an aging population, the relevance of effective pain management will only increase in the future. The elimination of mild and moderate pain has traditionally relied on the use of NSAIDs. If the pain does not subside, or, on the contrary, intensifies, they resort to the help of heavy analgesic “artillery” in the form of more serious drugs, including narcotics. NSAIDs are the first choice drugs for pain relief in rheumatic diseases. The “classic” side effect of this group of drugs - a negative effect on the mucous membrane of the gastrointestinal tract - can be neutralized by careful monitoring of the dose taken and duration of treatment, as well as the adequacy of concomitant therapeutic measures.
The mechanism of action of ketoprofen is due to the suppression of the activity of the enzyme cyclooxygenase, which is involved in the metabolism of the prostaglandin “substrate” - arachidonic acid. Prostaglandins are known to be mediators of pain and inflammation. The pronounced analgesic effect of the drug is due to a dual mechanism of action: through inhibition of prostaglandin synthesis in the periphery (peripheral component) and in the central nervous system (central component).
In addition, the drug affects the biological activity of various neurotropic substances involved in the secretion of pain mediators in the spinal cord. In addition to this, ketoprofen is endowed with antibradykinin activity, normalizes the state of lysosome membranes, and significantly suppresses the activity of neutrophils in patients suffering from rheumatoid arthritis. Inhibits the ability of platelets to aggregate. When taken orally, ketoprofen is well absorbed from the digestive tract. The maximum concentration of the active substance in the blood plasma is observed after 1-5 hours (for the tablet form), after 20-30 minutes (for the injection form with intramuscular administration), after 5 minutes (for the injection form with intravenous administration). Ketoprofen is available in three dosage forms: in addition to the already mentioned tablets and solution for injection, it is a gel for external use. The dosage regimen of the drug is established individually depending on the nature of the disease. For the tablet form, the initial daily dose is 300 mg 2-3 times a day. For the treatment of acute pain syndrome or exacerbation of chronic pain, preference is given to an injectable dosage form, which is administered as a single intramuscular injection in an amount of 100 mg. Ketoprofen in the form of an injection solution should not be used for more than 2-3 days. Then the patient is transferred to the tablet form of the drug. The maximum daily dose of injectable ketoprofen is 200 mg. Ketoprofen gel is applied to the surface of the skin in the area of the inflammatory focus 2 times a day. Pharmacotherapy with ketoprofen provides for a number of restrictions on taking other medications. Thus, the drug is incompatible with injectable tramadol. Ketoprofen increases the side effects of gluco- and mineralocorticosteroids, female sex hormones, and reduces the effectiveness of antihypertensive and diuretic drugs.
