Artrosilene
Artrozilen: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Artrosilene
ATX code: M02AA10
Active ingredient: ketoprofen (ketoprofen)
Producer: Dompe Farmaceutici (Italy), ISTITUTO de ANGELI (Italy), Zellaerosol GmbH (Germany), Valpharma SA (San Marino), Alfa Wassermann (Italy), Abiogen Pharma SpA (Italy)
Description and photo update: 2019-09-09
Prices in pharmacies: from 112 rubles.
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Artrosilene is a drug with analgesic, antipyretic and anti-inflammatory effects.
Release form and composition
Dosage forms of Artrosilene release:
- capsules: gelatinous, oblong, white body and dark green lid, capsules contain round granules from light yellow to white (10 pcs. in blisters, 1 blister in a cardboard box);
- solution for intravenous / intramuscular administration: transparent, slightly yellowish or colorless (in dark glass ampoules, 2 ml, 6 ampoules in a pallet, 1 pallet in a cardboard box);
- rectal suppositories: from light yellow to white, homogeneous, torpedo-shaped (5 pcs. in strips, 2 strips in a cardboard box);
- gel for external use: transparent, light yellow, has a characteristic odor (30 or 50 g in aluminum tubes, 1 tube in a cardboard box);
- aerosol for external use: a homogeneous almost white or white foam that forms when released from a container; the contents of the cylinder after the gas exit is a clear liquid from light yellow to white (25 g each in aluminum aerosol cans with a capacity of 25 ml, 1 cylinder in a cardboard box complete with a protective cap and a spray nozzle).
Each pack also contains instructions for the use of Artrosilene.
Composition of 1 capsule:
- active substance: ketoprofen lysine salt - 320 mg;
- auxiliary components: povidone -27.857 mg; diethyl phthalate - 2.286 mg; polymers of methacrylic and acrylic acids - 34.143 mg; carboxypolymethylene - 32.857 mg; talc - 27 mg; magnesium stearate - 15.857 mg;
- capsule shell: titanium dioxide (E171), gelatin; cap (optional) - indigotine (E132), quinoline yellow (E104).
Composition of 1 ml solution for injection:
- active substance: ketoprofen lysine salt - 80 mg;
- auxiliary components: citric acid, sodium hydroxide, water for injection.
Composition of 1 suppository:
- active substance: ketoprofen lysine salt - 160 mg;
- auxiliary component: semi-synthetic glycerides.
Composition of 100 mg gel:
- active substance: ketoprofen lysine (lysine salt of ketoprofen) - 5 mg (ketoprofen - 3.125 mg);
- auxiliary components: carbomer - 1 mg; trolamine - 1.9 mg; polysorbate-80 - 0.8 mg; 95% ethanol - 5 mg; methyl parahydroxybenzoate - 0.1 mg; lavender-neroli flavor - 0.2 mg; purified water - 0.086 ml.
Composition of 100 mg aerosol:
- active substance: ketoprofen lysine (ketoprofen lysine salt) - 15 mg (ketoprofen - 9.375 mg);
- auxiliary components: propylene glycol - 4 mg; polysorbate-80 - 4 mg; lavender-neroli flavor - 0.2 mg; povidone - 3 mg; propane-butane mixture - 1.25 mg; benzyl alcohol - 0.3 mg; purified water - up to 0.1 ml.
Pharmacological properties
Pharmacodynamics
Ketoprofen has anti-inflammatory, antipyretic and analgesic effects. Inhibits the synthesis of prostaglandins, inhibiting COX (cyclooxygenase) I and II types. Shows anti-bradykinin activity, stabilizes lysosomal membranes and delays the release of enzymes from them, which, in chronic inflammation, contribute to tissue destruction. Inhibits the activity of neutrophils, reduces the release of cytokines.
Thanks to the use of ketoprofen, morning stiffness and swelling of the joints decreases, and the range of motion increases. Unlike ketoprofen, ketoprofen lysine salt is a rapidly dissolving molecule with neutral pH and almost no irritant effect on the gastrointestinal tract.
When using an aerosol or gel Artrozilen provides a local therapeutic effect in relation to the affected ligaments, muscles, joints, tendons. Ketoprofen has no catabolic effect on articular cartilage.
Pharmacokinetics
Capsules, rectal suppositories, injection solution
Suction:
- capsules: after oral administration, ketoprofen is almost completely absorbed from the gastrointestinal tract, its bioavailability is more than 80%. With max (maximum concentration of the substance) in plasma is achieved in 4-10 hours, its value is dose-dependent and is 3-9 μg / ml. T 1/2 (half-life) - 6.5 hours. The maximum therapeutic effect is observed within 4-24 hours. Food decreases C max and lengthens the time to reach it, while the AUC (area under the concentration-time curve) does not change;
- rectal suppositories: ketoprofen is rapidly absorbed after rectal administration. Time to reach C max is 45 to 60 minutes. The value of the plasma concentration is linearly dependent on the dose taken.
- injection solution: for parenteral administration, the time to reach C max is 20-30 minutes. Effective concentration is maintained for 24 hours. In the synovial fluid, the therapeutic concentration lasts from 18 to 20 hours;
Up to 99% of absorbed ketoprofen binds to plasma proteins, mainly albumin. V d (volume of distribution) ranges from 0.1 to 0.2 l / kg. It easily penetrates through histohematogenous barriers, is distributed in organs and tissues. The substance penetrates well into connective tissues and synovial fluid. Although the concentration of ketoprofen in the synovial fluid is slightly lower than the plasma concentration, it is more stable (lasts up to 30 hours).
Metabolism of ketoprofen occurs mainly in the liver, where the substance undergoes glucuronidation, followed by the formation of esters with glucuronic acid.
Excretion of metabolites is carried out in the urine. Up to 1% is excreted with feces. Does not cumulate.
Gel, aerosol for external use
When applied externally, ketoprofen is absorbed slowly.
A dose of 50-150 mg of the gel after 5-8 hours creates a plasma level of 0.08-0.15 μg / ml. Bioavailability of the gel is approximately 5%.
The level of ketoprofen in the blood after aerosol application is less than 0.1 μg / ml, the amount of the substance (free or conjugated) excreted in the next 48 hours by the kidneys is equivalent to 0.62% of the dose of the drug. The level of ketoprofen in synovial fluid is equivalent to 0.2–2 μg / ml (depending on the applied dose).
Indications for use
Capsules, rectal suppositories
- mild / moderate pain, including inflammatory pain, postoperative / post-traumatic pain (relief);
- rheumatic / inflammatory diseases, including spondyloarthritis, osteoarthritis, rheumatoid / gouty arthritis, inflammatory lesions of the periarticular tissues (symptomatic treatment).
Injection solution
Acute pain syndrome in the presence of the following diseases / conditions (short-term treatment):
- diseases of the musculoskeletal system of various etiologies;
- postoperative / post-traumatic period;
- inflammatory processes.
Gel, aerosol for external use
- muscle pains of non-rheumatic / rheumatic genesis;
- inflammatory diseases of the musculoskeletal system in acute and chronic course, including ankylosing spondylitis, rheumatoid / psoriatic arthritis, osteoarthritis of the spine and peripheral joints, rheumatic lesions of soft tissues;
- damage to soft tissues of traumatic origin.
Contraindications
Absolute contraindications for Artrosilene in all dosage forms:
- "Aspirin triad";
- pregnancy (III trimester) and lactation;
- hypersensitivity to the components of Artrosilene, as well as to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs.
Additional absolute contraindications for systemic use:
- blood clotting disorders, including hemophilia;
- peptic ulcer of the stomach and duodenum with exacerbation;
- ulcerative colitis with exacerbation;
- diverticulitis;
- Crohn's disease;
- peptic ulcer;
- chronic renal failure;
- age up to 18 years.
Additional absolute contraindications for external use:
- violation of the integrity of the skin;
- eczema;
- weeping dermatoses;
- age up to 6 years.
Relative (the appointment of Artrosilene in all dosage forms requires caution in the presence of the following diseases / conditions):
- I and II trimesters of pregnancy;
- elderly age.
Relative contraindications for systemic use of Artrosilene:
- smoking;
- anemia;
- alcoholism;
- sepsis;
- bronchial asthma;
- diabetes;
- arterial hypertension;
- swelling;
- hyperbilirubinemia;
- alcoholic cirrhosis of the liver;
- liver failure;
- dehydration;
- chronic heart failure;
- deficiency of glucose-6-phosphate dehydrogenase;
- stomatitis;
- blood diseases, including leukopenia.
Relative contraindications for external use of Artrosilene:
- erosive and ulcerative lesions of the gastrointestinal tract;
- bronchial asthma;
- chronic heart failure;
- hepatic porphyria with exacerbation;
- severe functional disorders of the kidneys / liver;
- age from 6 to 12 years.
Artrozilen, instructions for use: method and dosage
Capsules
Artrozilen capsules are taken orally, preferably at the same time / after a meal.
The daily dose is 1 capsule (in 1 dose).
A long course is possible - from 3 to 4 months.
Rectal suppositories
Artrozilene is used rectally.
Single dose - 1 suppository, frequency of application - 2-3 times a day.
The maximum daily dose is 3 suppositories, for elderly patients - no more than 2 suppositories per day.
For functional disorders of the liver / kidneys, a dose reduction is required.
Injection solution
Artrosilene injections are administered intramuscularly or intravenously.
The daily dose is 160 mg.
Maximum - 320 mg per day, for elderly patients - 160 mg per day.
In the form of injections, Artrozilen is used for a short time (up to 3 days), after which they switch to the use of capsules or suppositories.
The solution is administered intravenously only under stationary conditions. To increase the duration of the action of Artrozilen, it is recommended to carry out slow intravenous infusions - at least 30 minutes.
The solution for infusion is prepared on the basis of 50 or 500 ml of the following aqueous solutions: 0.9% sodium chloride solution, 10% aqueous levulose solution, 5% aqueous dextrose solution, Ringer's acetate solution, Ringer's lactate solution according to Hartmann, colloidal dextran solution in 5% dextrose solution or 0.9% sodium chloride solution.
When diluting Artrozilen in small volumes (50 ml) of the solution, it is administered intravenously by bolus.
Gel, aerosol for external use
Gel and spray Artrozilene is used externally.
Recommended single dose: gel - 3-5 g (approximately corresponds to the volume of a large cherry), aerosol - 1-2 g (approximately corresponds to the volume of a walnut).
The drug is applied 2-3 times a day, rubbing it gently until completely absorbed.
The duration of the course is up to 10 days (unless otherwise prescribed by a doctor).
Side effects
- central and peripheral nervous system: general malaise, hyperkinesia, dizziness, tremor, vertigo, anxiety, mood swings, irritability, hallucinations, visual impairment;
- digestive system: duodenitis, abdominal pain, gastritis, diarrhea, esophagitis, stomatitis, erosive and ulcerative lesions of the gastrointestinal tract, melena, hematemesis, increased bilirubin levels, liver failure, hepatitis, increased activity of liver enzymes, increased liver size;
- urinary system: painful urination, edema, cystitis, hematuria;
- cardiovascular system: syncope, hypertension, tachycardia, hypotension, chest pain, pallor, peripheral edema;
- hematopoietic system: thrombocytopenia, leukocytopenia, lymphangitis, thrombocytopenic purpura, leukocytosis, decreased prothrombin time, vasculitis, enlarged spleen;
- respiratory system: laryngeal edema, laryngeal spasm sensation, bronchospasm, dyspnea, laryngospasm, rhinitis;
- allergic and dermatological reactions: angioedema, urticaria, erythema multiforme (including Stevens-Johnson syndrome), maculopapular rash, anaphylactoid reactions (edema of the pharynx, oral mucosa, periorbital edema), pruritus, erythematous exanthema;
- others: menstrual irregularities, conjunctivitis, increased sweating;
- local reactions when applied externally: photosensitivity, skin manifestations of allergic reactions; with prolonged use on large areas of the skin - the development of systemic side effects;
- local reactions when using suppositories: exacerbation of hemorrhoids, itching, burning, heaviness in the anorectal region.
In comparison with ketoprofen, the lysine salt of ketoprofen causes side reactions much less frequently.
Overdose
Cases of an overdose of Artrozilene with systemic use have not been reported. When applied externally, an overdose is almost impossible, due to the extremely low systemic absorption of ketoprofen.
Therapy: monitoring of cardiac and respiratory activity. If necessary, symptomatic treatment is carried out. There is no specific antidote. Hemodialysis is ineffective.
special instructions
During the period of therapy, periodic monitoring of the peripheral blood picture and the functional state of the kidneys / liver is required.
If necessary, the determination of 17-ketosteroids Artrosilene is canceled 2 days before the study.
Therapy can mask the symptoms of an infectious disease.
In bronchial asthma, the use of Artrosilene can lead to the development of an attack of suffocation.
The drug can be applied externally only to intact skin areas. Avoid getting Artrosilene in the eyes and mucous membranes.
Aqueous solutions of the ketoprofen lysine salt, as well as an external gel, can be used in physiotherapeutic therapy (mesotherapy, iontophoresis): during iontophoresis, the drug is applied to the negative pole.
In order to prevent the manifestations of photo- and hypersensitivity, it is recommended to avoid exposure to the sun's rays during the treatment course.
Influence on the ability to drive vehicles and complex mechanisms
During the use of Artrozilene, you should refrain from potentially dangerous types of work, the performance of which requires increased concentration of attention and quick psychomotor reactions.
Application during pregnancy and lactation
- III trimester of pregnancy, breastfeeding period: therapy is contraindicated;
- I and II trimesters of pregnancy: Artrosilene can only be used under medical supervision.
Pediatric use
Age restrictions for the use of Artrosilene:
- gel, aerosol: children under 6 years old - contraindicated; children 6–12 years old - are prescribed with caution;
- capsules, injection solution, rectal suppositories: contraindicated in children under 18 years of age.
With impaired renal function
Artrozilene in the form of capsules, solution and suppositories for chronic renal failure is contraindicated.
Aerosol and gel Artrozilen should be used with caution in severe renal impairment.
For violations of liver function
The use of Artrosilene requires caution:
- capsules, solution and suppositories: patients with alcoholic cirrhosis of the liver and liver failure;
- gel, aerosol: for severe hepatic impairment.
Use in the elderly
For elderly patients, Artrozilen is prescribed with caution.
Drug interactions
With the combined use of Artrozilen with certain drugs / substances, the following effects may develop:
- inducers of microsomal oxidation in the liver, including ethanol, tricyclic antidepressants, phenytoin, phenylbutazone, barbiturates, rifampicin, flumecinol: increased metabolism of ketoprofen (there is an increase in the production of hydroxylated active metabolites);
- anticoagulants, antiplatelet agents, fibrinolytics, ethanol: enhancing their action;
- uricosuric, antihypertensive drugs, diuretics: decrease in their effectiveness;
- other non-steroidal anti-inflammatory drugs, glucocorticosteroids, ethanol, corticotropin: an increase in the likelihood of ulceration and the occurrence of gastrointestinal bleeding, functional renal disorders;
- mineralocorticoids, glucocorticoids, estrogens: increased severity of their side effects;
- insulin and oral hypoglycemic drugs: increased hypoglycemic action (dose adjustment may be required);
- oral anticoagulants, heparin, thrombolytics, antiplatelet agents, cefoperazone, cefamandol and cefotetan: increased risk of bleeding;
- verapamil, nifedipine, lithium, methotrexate: increasing their plasma concentration;
- sodium valproate: impaired platelet aggregation;
- cholestyramine, antacids: reduced absorption of ketoprofen.
Analogs
The analogues of Artrosilene are: Febrofid, Ketoprofen, Fastum, Oruvel, Spazgel, Ketospray, Flexen, VALUSAL, Artrum, Ketonal, Bystrumgel.
Terms and conditions of storage
Store in a dark place, out of reach of children, at temperatures up to 25 ° C. Do not overheat the aerosol can.
Shelf life:
- capsules, rectal suppositories - 5 years;
- injection solution, gel, aerosol - 3 years.
Terms of dispensing from pharmacies
Released:
- capsules, solution, suppositories: prescription;
- gel, aerosol: no prescription.
Reviews about Artrosilene
Reviews about Artrosilene are different. It is often recommended by users as a fast-acting pain reliever. In some cases, when using the drug in the form of an injection solution, they indicate pain at the injection site. It is also sometimes noted that the therapeutic effect of the drug is insufficient or short-lived.
When applied externally, there are more positive responses about the preparation in the form of a gel. Spray Artrosilene leaves a sticky film after application and has uneconomical consumption. The cost of the drug is estimated to be high.
The price of Artrozilene in pharmacies
The approximate price for Artrozilen is: injection solution (6 ampoules of 2 ml each) –176–201 rubles, capsules (10 pcs.) - 282–322 rubles, gel (1 tube of 50 g each) - 289–331 rubles, aerosol (1 can of 25 ml) - 408–464 rubles.
Artrosilene: prices in online pharmacies
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Drug name Price Pharmacy |
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Artrozilene 80 mg / ml solution for intravenous and intramuscular administration 2 ml 6 pcs. 112 RUB Buy |
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Artrozilene solution for intravenous and intramuscular injection. 80mg / ml 2ml 6 pcs. 135 RUB Buy |
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Artrosilene 320 mg capsules 10 pcs. 177 r Buy |
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Arthrosilene 15% aerosol for external use 25 ml 1 pc. RUB 250 Buy |
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Artrosilene 5% gel for external use 50 g 1 pc. 251 RUB Buy |
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Artrosilene capsules 320mg 10 pcs. 304 RUB Buy |
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Artrosilene gel 5% 50g 333 r Buy |
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Artrosilene foam for external use 15% 25ml RUB 471 Buy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
