Artrosilene, 1 piece, 25 ml, 15%, aerosol for external use
Capsules
Suction.
When administered orally, ketoprofen is quite completely absorbed from the gastrointestinal tract, and its bioavailability exceeds 80%. Cmax in plasma when taking Artrosilene capsules is observed 4–10 hours after oral administration, its value directly depends on the dose taken and is 3–9 μg/ml. T1/2 is 6.5 hours. The maximum therapeutic effect is observed over a period of 4 to 24 hours. Food helps to reduce Cmax values and increase Tmax without changing AUC.
Distribution.
Up to 99% of absorbed ketoprofen is bound to plasma proteins, mainly albumin. Vd - 0.1–0.2 l/kg. Easily penetrates histohematic barriers and is distributed in tissues and organs. Ketoprofen penetrates well into synovial fluid and connective tissue. Although the concentration of ketoprofen in synovial fluid is slightly lower than in plasma, it is more stable (lasts up to 30 hours).
Metabolism.
Ketoprofen is primarily metabolized in the liver, where it undergoes glucuronidation to form esters with glucuronic acid.
Excretion.
Metabolites are excreted in the urine. Less than 1% is excreted in feces. The drug does not accumulate.
Solution for intravenous and intramuscular administration
Tmax for parenteral administration is 20–30 minutes. The effective concentration lasts 24 hours. Therapeutic concentration in synovial fluid lasts 18–20 hours.
Distribution.
Up to 99% of absorbed ketoprofen is bound to plasma proteins, mainly albumin. Vd - 0.1–0.2 l/kg. Easily penetrates histohematic barriers and is distributed in tissues and organs. Ketoprofen penetrates well into synovial fluid and connective tissue. Although the concentration of ketoprofen in synovial fluid is slightly lower than in plasma, it is more stable (lasts up to 30 hours).
Metabolized by microsomal liver enzymes. Excreted by the kidneys, 60–80% in the form of glucuronide in 24 hours.
Suppositories
Suction.
Ketoprofen lysine salt is rapidly absorbed: Tmax after rectal administration is 45–60 minutes. The plasma concentration depends linearly on the dose taken.
Distribution.
Up to 99% of absorbed ketoprofen is bound to plasma proteins, mainly albumin. Vd - 0.1–0.2 l/kg. Easily penetrates histohematic barriers and is distributed in tissues and organs. Ketoprofen penetrates well into synovial fluid and connective tissue. Although the concentration of ketoprofen in synovial fluid is slightly lower than in plasma, it is more stable (lasts up to 30 hours).
Metabolism.
Ketoprofen is primarily metabolized in the liver, where it undergoes glucuronidation to form esters with glucuronic acid.
Excretion.
Metabolites are excreted mainly in the urine (up to 76% after 24 hours). The drug does not accumulate.
Gel, aerosol
When applied cutaneously, it is absorbed slowly; a dose of 50–150 mg over 5–8 hours produces a plasma concentration level of 0.08–0.15 mcg/ml. Practically does not accumulate in the body. Bioavailability is about 5%.
Artrosilene, 15%, aerosol for external use, 25 ml, 1 pc.
Capsules
Suction.
When administered orally, ketoprofen is quite completely absorbed from the gastrointestinal tract, and its bioavailability exceeds 80%. Cmax in plasma when taking Artrosilene capsules is observed 4–10 hours after oral administration, its value directly depends on the dose taken and is 3–9 μg/ml. T1/2 is 6.5 hours. The maximum therapeutic effect is observed over a period of 4 to 24 hours. Food helps to reduce Cmax values and increase Tmax without changing AUC.
Distribution.
Up to 99% of absorbed ketoprofen is bound to plasma proteins, mainly albumin. Vd - 0.1–0.2 l/kg. Easily penetrates histohematic barriers and is distributed in tissues and organs. Ketoprofen penetrates well into synovial fluid and connective tissue. Although the concentration of ketoprofen in synovial fluid is slightly lower than in plasma, it is more stable (lasts up to 30 hours).
Metabolism.
Ketoprofen is primarily metabolized in the liver, where it undergoes glucuronidation to form esters with glucuronic acid.
Excretion.
Metabolites are excreted in the urine. Less than 1% is excreted in feces. The drug does not accumulate.
Solution for intravenous and intramuscular administration
Tmax for parenteral administration is 20–30 minutes. The effective concentration lasts 24 hours. Therapeutic concentration in synovial fluid lasts 18–20 hours.
Distribution.
Up to 99% of absorbed ketoprofen is bound to plasma proteins, mainly albumin. Vd - 0.1–0.2 l/kg. Easily penetrates histohematic barriers and is distributed in tissues and organs. Ketoprofen penetrates well into synovial fluid and connective tissue. Although the concentration of ketoprofen in synovial fluid is slightly lower than in plasma, it is more stable (lasts up to 30 hours).
Metabolized by microsomal liver enzymes. Excreted by the kidneys, 60–80% in the form of glucuronide in 24 hours.
Suppositories
Suction.
Ketoprofen lysine salt is rapidly absorbed: Tmax after rectal administration is 45–60 minutes. The plasma concentration depends linearly on the dose taken.
Distribution.
Up to 99% of absorbed ketoprofen is bound to plasma proteins, mainly albumin. Vd - 0.1–0.2 l/kg. Easily penetrates histohematic barriers and is distributed in tissues and organs. Ketoprofen penetrates well into synovial fluid and connective tissue. Although the concentration of ketoprofen in synovial fluid is slightly lower than in plasma, it is more stable (lasts up to 30 hours).
Metabolism.
Ketoprofen is primarily metabolized in the liver, where it undergoes glucuronidation to form esters with glucuronic acid.
Excretion.
Metabolites are excreted mainly in the urine (up to 76% after 24 hours). The drug does not accumulate.
Gel, aerosol
When applied cutaneously, it is absorbed slowly; a dose of 50–150 mg over 5–8 hours produces a plasma concentration level of 0.08–0.15 mcg/ml. Practically does not accumulate in the body. Bioavailability is about 5%.
Artrosilene Foam for external use 15%, 25 g, cylinders, cardboard packs
Registration Certificate Holder
DOMPE FARMACEUTICI (Italy)
Dosage form
Medicine - Artrosilen
Description
Foam for external use
from white to light yellow in color, with a specific odor, formed when released from a container with a spray nozzle; after the foam settles, a yellow to brownish-yellow liquid is formed.
100 ml
ketoprofen lysine (ketoprofen lysine salt) 15 g, which corresponds to the content of ketoprofen 9.375 g
Excipients
: polysorbate 80 - 4 g, propylene glycol - 4 g, povidone K-25 - 3 g, lavender-neroli flavor - 0.2 g, benzyl alcohol - 0.3 g, purified water - up to 100 ml, propane-butane mixture - 5 g.
25 g - aluminum cylinders with a capacity of 25 ml (1) with a spray nozzle and a protective cap - cardboard packs.
Indications
Symptomatic treatment of painful and inflammatory processes of various origins, including: rheumatoid arthritis and periarthritis; ankylosing spondylitis (ankylosing spondylitis); psoriatic arthritis; reactive arthritis (Reiter's syndrome); osteoarthritis of various localizations; tendinitis, bursitis; myalgia; neuralgia; radiculitis; injuries of the musculoskeletal system (including sports), bruises of muscles and ligaments, sprains, ruptures of ligaments and muscle tendons.
Contraindications for use
Hypersensitivity to ketoprofen; hypersensitivity to salicylates, tiaprofenic acid or other NSAIDs, fenofibrate, UV blockers, fragrances; violation of the integrity of the skin (eczema, weeping dermatitis, open or infected wound); indications in the anamnesis of attacks of bronchial asthma caused by taking NSAIDs and salicylates; history of photosensitivity reactions; exposure to sunlight, incl. indirect sunlight and UV irradiation in a solarium throughout the entire treatment period and for another 2 weeks after stopping treatment; III trimester of pregnancy; children under 15 years of age.
Carefully
Impaired liver and/or kidney function, erosive and ulcerative lesions of the gastrointestinal tract, blood diseases, bronchial asthma, chronic heart failure.
pharmachologic effect
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.
Drug interactions
Since the concentration of ketoprofen in the blood plasma is extremely low, symptoms of interaction with other drugs (similar symptoms with systemic use) are possible only with frequent and prolonged use.
The simultaneous use of other topical products containing ketoprofen or other NSAIDs is not recommended.
Simultaneous administration of acetylsalicylic acid reduces the degree of binding of ketoprofen to plasma proteins.
Ketoprofen reduces the excretion of methotrexate and increases its toxicity.
Patients taking coumarin-containing anticoagulant drugs are advised to undergo treatment under medical supervision.
Dosage regimen
Apply externally 2-3 times/day.
The duration of treatment without consulting a doctor should not exceed 14 days.
Side effect
Allergic reactions: very rarely - angioedema, anaphylaxis.
From the skin and subcutaneous fat: infrequently - erythema, itching, burning, eczema, mild transient dermatitis; rarely - urticaria, rash, photosensitivity, bullous dermatitis, purpura, erythema multiforme, lichenoid dermatitis, skin necrosis, Stevens-Johnson syndrome; very rarely - a single case of severe contact dermatitis (due to poor hygiene and insolation), a single case of severe generalized photodermatitis, toxic epidermal necrolysis.
From the respiratory system: very rarely - asthmatic attacks (as a variant of an allergic reaction).
From the urinary system: very rarely - deterioration of renal function in patients with chronic renal failure.
special instructions
It is necessary to avoid contact of this product with the eyes, the skin around the eyes, and mucous membranes.
Ketoprofen can be used externally in combination with oral administration. The total daily dose, regardless of the dosage form, should not exceed 200 mg.
To reduce the risk of developing photosensitivity, it is recommended to protect skin areas treated with ketoprofen with clothing from exposure to ultraviolet radiation throughout the entire treatment period and for another 2 weeks after stopping use of the gel.
Do not use as occlusive dressings.
Use during pregnancy and breastfeeding
Restrictions during pregnancy - Contraindicated. Restrictions when breastfeeding - Contraindicated.
Use is contraindicated in the third trimester of pregnancy. Use in the first and second trimesters is possible in cases where the expected benefit of therapy for the mother outweighs the potential risk for the fetus.
Use during lactation (breastfeeding) is not recommended.
Use for renal impairment
Restrictions in case of impaired renal function - With caution. Use with caution in case of impaired renal function.
Use for liver dysfunction
Restrictions in case of liver dysfunction - With caution. Use with caution in case of liver dysfunction.
Use in elderly patients
Restrictions for elderly patients - Use with caution. Use with caution in elderly patients.
Use in children
Restrictions for children - Contraindicated. Contraindicated: children under 15 years of age.
Terms of sale
The drug is approved for use as a means of OTC.