Artrosilene instructions for use analogues. Artrosilene in injections for the treatment of neuralgic conditions and pathologies of the musculoskeletal system

Composition and release form of the drug

◊ Aerosol for external use 15% in the form of a homogeneous foam of white or almost white color; after the gas is released, the contents of the cylinder are a transparent liquid from white to light yellow.

Excipients: polysorbate 80 - 4 g, propylene glycol - 4 g, - 3 g, lavender-nerolium flavor - 0.2 g, benzyl alcohol - 0.3 g, purified water - up to 100 ml, propane-butane mixture - 1.25 g.

25 g - aluminum aerosol cans with a capacity of 25 ml (1) with a spray nozzle and a protective cap - cardboard packs.

pharmachologic effect

NSAID, propionic acid derivative. It has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is associated with inhibition of the activity of COX, the main enzyme in the metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever.

The pronounced analgesic effect of ketoprofen is due to two mechanisms: peripheral (indirectly, through suppression of prostaglandin synthesis) and central (due to inhibition of prostaglandin synthesis in the central and peripheral nervous system, as well as the effect on the biological activity of other neurotropic substances that play a key role in the release of pain mediators in the spinal cord). brain). In addition, ketoprofen has antibradykinin activity, stabilizes lysosomal membranes, and causes significant inhibition of neutrophil activity in patients with rheumatoid arthritis. Suppresses platelet aggregation.

Pharmacokinetics

When taken orally and rectally, ketoprofen is well absorbed from the gastrointestinal tract. Cmax when taken orally is achieved after 1-5 hours (depending on the dosage form), with rectal administration - after 45-60 minutes, intramuscular administration - after 20-30 minutes, intravenous administration - after 5 minutes.

Plasma protein binding is 99%. Due to its pronounced lipophilicity, it quickly penetrates the BBB. C ss in blood plasma and cerebrospinal fluid persists from 2 to 18 hours. Ketoprofen penetrates well into the synovial fluid, where its concentration 4 hours after administration exceeds that in plasma.

Metabolized by binding to glucuronic acid and, to a lesser extent, by hydroxylation.

It is excreted mainly by the kidneys and to a much lesser extent through the intestines. T1/2 of ketoprofen from plasma after oral administration is 1.5-2 hours, after rectal administration - about 2 hours, after intramuscular administration - 1.27 hours, after intravenous administration - 2 hours.

Indications

Articular syndrome (osteoarthritis, ankylosing spondylitis, gout); symptomatic treatment of inflammatory and degenerative diseases of the musculoskeletal system (periarthritis, arthrosynovitis, tendonitis, tenosynovitis, bursitis, lumbago), pain in the spine, neuralgia, myalgia. Uncomplicated injuries, in particular sports injuries, sprains, sprains or ruptures of ligaments and tendons, bruises, post-traumatic pain.

As part of combination therapy for inflammatory diseases of the veins, lymphatic vessels, lymph nodes (phlebitis, periphlebitis, lymphangitis, superficial lymphadenitis).

Contraindications

For oral administration: erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, “aspirin triad”, severe dysfunction of the liver and/or kidneys; III trimester of pregnancy; age up to 15 years (for retard tablets); hypersensitivity to ketoprofen and salicylates.

For rectal use: history of proctitis and rectal bleeding.

For external use: weeping dermatoses, eczema, infected abrasions, wounds.

Dosage

Set individually depending on the clinical situation.

Used orally, intramuscularly, intravenously (as an infusion), rectally or externally in appropriate dosage forms.

Side effects

From the digestive system: pain in the epigastric region, nausea, vomiting, constipation or diarrhea, anorexia, gastralgia, liver dysfunction; rarely - erosive and ulcerative lesions of the gastrointestinal tract, bleeding and perforation of the gastrointestinal tract.

From the side of the central nervous system:, dizziness, tinnitus, drowsiness.

From the urinary system: renal dysfunction.

Allergic reactions: skin rash; rarely - bronchospasm.

Local reactions: when used in the form of suppositories, irritation of the rectal mucosa and painful bowel movements are possible; when used in gel form - itching, skin rash at the site of application.

Drug interactions

When ketoprofen is used simultaneously with other NSAIDs, the risk of developing erosive and ulcerative lesions of the gastrointestinal tract and bleeding increases; with antihypertensive drugs (including beta-blockers, ACE inhibitors, diuretics) - their effect may be reduced; with thrombolytics - increased risk of bleeding.

When used simultaneously with, it is possible to reduce the binding of ketoprofen to plasma proteins and increase its plasma clearance; with heparin, ticlopidine - increased risk of bleeding; with lithium preparations, it is possible to increase the concentration of lithium in the blood plasma to toxic levels due to a decrease in its renal excretion.

When used simultaneously with diuretics, the risk of developing renal failure increases due to a decrease in renal blood flow caused by inhibition of prostaglandin synthesis and against the background of hypovolemia.

When used simultaneously with probenecid, the clearance of ketoprofen and its binding to plasma proteins may be reduced; with possible increased side effects of methotrexate.

With the simultaneous use of warfarin, severe, sometimes fatal bleeding may develop.

special instructions

Use with extreme caution in patients with liver and kidney diseases, a history of gastrointestinal diseases, dyspeptic symptoms, and immediately after major surgical interventions. During treatment, systematic monitoring of liver and kidney function is necessary.

Pregnancy and lactation

Contraindicated for use in the third trimester of pregnancy. In the first and second trimesters of pregnancy, the use of ketoprofen is possible in cases where the potential benefit to the mother outweighs the potential risk to the fetus.

If it is necessary to use ketoprofen during lactation, it is recommended to stop breastfeeding.

• Part capsules active ingredient included: ketoprofen , presented in the form of lysine salt. Additional components: diethyl phthalate, carbopol, povidone, magnesium stearate, polymers of acrylic and methacrylic acid, talc, titanium dioxide, gelatin, indigotine and quinoline yellow.
• Injection solution also contains the active ingredient: ketoprofen – lysine salt. Auxiliary components: citric acid, sodium hydroxide, sterile water.
• Suppositories Artrosilene include the active substance: ketoprofen , in the form of lysine salt. Auxiliary components: semi-synthetic glycerides.
• The drug is in the form gel consists of the active substance: ketoprofen – lysine salt. Additional components: polysorbate, carbopol, TEM, ethanol, nerolen or lavender flavor, methylparaben and prepared water.
• Aerosol contains the active substance: ketoprofen – lysine salt. Auxiliary components: nerolen or lavender, polysorbate 80, PPG, benzyl alcohol, PVP, prepared water.

Release form

Artrosilene is produced in several pharmacological forms, namely in the form:

• gel for external use 30-50g;
• capsules for oral administration, 10 pieces per package;
• injection solution in ampoules of 2 ml, 6 pieces per package;
• rectal suppositories, 10 pieces per package;
• external aerosol 25 ml.

pharmachologic effect

All forms of Artrosilene are characterized by analgesic, antipyretic and anti-inflammatory effects.

Pharmacodynamics and pharmacokinetics

The manifestation of anti-inflammatory, analgesic and antipyretic effect is ensured by the ability of ketoprofen to inhibit COX-1 and -2 and inhibit PG synthesis. In addition, the drug is characterized by anti-bradykinin activity, stabilization of lysosomal membranes and inhibition of their release from the composition , which contribute to tissue destruction in cases of chronic inflammation. The release of cytokines decreases and the activity of neutrophils slows down.

The use of Artrosilene can reduce morning stiffness, swelling of joints, and increase range of motion.

The lysine salt included in the drug ketoprofen is a rapidly soluble molecule with a neutral pH. Therefore, Artrosilene has virtually no irritating effect on the gastrointestinal tract.

Outdoor use spray or gel renders local anti-inflammatory, anti-exudative And analgesic Effect. In this case, a high local therapeutic effect on the affected joints, tendons, ligaments, and muscles is manifested. Treatment with the drug for joint syndrome helps to relieve pain in the joints, both at rest and during movement, and reduces morning stiffness and swelling of the joints. It has been established that Artrosilene does not have a destructive effect on articular cartilage.

When taking capsules, the active substance is fully absorbed from the gastrointestinal tract, with a bioavailability above 80%. The maximum concentration is achieved 4-10 hours after administration, depending on the dosage. In this case, the therapeutic effect lasts 4-24 hours. Eating food can reduce the concentration of the substance in the body. There is a complete connection within the body ketoprofen with plasma proteins. The substance is able to penetrate histohematic barriers, tissues and synovial fluid, where its distribution occurs. Ketoprofen occurs in the liver, undergoing glucuronidation to produce esters and glucuronic acid. Removal carried out in urine and a small part in feces.

The effect of the injection solution appears after 20-30 minutes and lasts for 18-20 hours. The active substance is fully absorbed by binding to plasma proteins. The drug penetrates through histohematic barriers into tissues and physiological fluids, evenly distributed in the body. Metabolism occurs with the participation of liver enzymes, which are predominantly excreted by the kidneys, within 24 hours.

When using the drug in the form of rectal suppositories, its effect manifests itself within 45-60 minutes. The maximum concentration of the substance is directly dependent on the dosage taken. In the body, ketoprofen is fully absorbed by binding to plasma proteins. Penetration of the substance through histohematic barriers was noted, distributing in tissues and important organs. Metabolism occurs in the liver, with the production of esters and glucuronic acid. Metabolites are excreted in urine.

The use of external gel and aerosol products is characterized by slow absorption. In this case, the effect of the substance manifests itself within a short time and persists for 5-8 hours. Bioavailability is approximately 5%.

Indications for use

The main indications for the use of capsules and suppositories are:

• inflammatory, postoperative or post-traumatic mild to moderate pain;
• rheumatoid and gouty ;
• spondyloarthritis;
• inflammatory damage to periarticular tissues.

Injections are prescribed for short-term treatment of acute pain syndromes accompanying:

• diseases of the musculoskeletal system of various origins;
• postoperative and post-traumatic pain associated with inflammation.

Indications for prescribing the gel and aerosol are:

• diseases of the musculoskeletal system, for example, rheumatoid and psoriatic arthritis, osteoarthritis peripheral joints or spine, ankylosing spondylitis, rheumaticdamage soft tissues;
• traumatic lesions of soft tissues
  muscular rheumatic and non-rheumatic pain.

Contraindications for use

• high sensitivity to the drug;
• aspirin;
• , ;
• exacerbation of gastric and duodenal ulcers, peptic ulcers;
• diverticulitis;
• acute form of ulcerative , Crohn's disease;
• chronic ;
• childhood;
• and other disorders associated with blood clotting and so on.

• getting wet dermatosisOh;
• violation of the integrity of the skin.

Caution is required when treating patients suffering from:

• chronic heart failure;
• anemia;
• liver failure;
• and so on.

Side effects

The use of Artrosilene can lead to the development of disturbances in the functioning of the gastrointestinal tract, liver, nervous system, sensory and hematopoietic organs, genitourinary, cardiovascular and respiratory systems.

In addition, the development of various skin disorders and allergic reactions is possible.

When using external preparations - gel and aerosol, photosensitivity cannot be ruled out.

In any case, consultation with a specialist is necessary.

Instructions for use of Artrosilene (Method and dosage)

The drug is available in several pharmacological forms intended for oral, rectal, parenteral and external administration.

Tablets for oral administration are prescribed 1 piece daily at the same time or after meals. The therapeutic course can last 3-4 months.

The solution for IM or IV is prescribed for use as an ampoule per day. As a rule, this form of the drug is used for short-term treatment of no more than 3 days in a hospital setting. When it is necessary to continue treatment, the use of capsules or suppositories is allowed.

Rectal suppositories are used daily, 1 piece 2-3 times. The maximum daily dosage should not exceed 480 mg. Elderly patients are prescribed a daily dose of up to 2 suppositories.

External forms of aerosol and gel Artrosilene instructions for use recommend applying in small quantities daily 2-3 times. In this case, a single aerosol dosage is 1-2g. The duration of therapy is determined by the attending physician, but it should not be longer than 10 days.

Overdose

Cases of overdose with Artrosilene drugs have not been described.

Interaction

Simultaneous use with inducers of microsomal oxidation in the liver area - phenytoin, barbiturates, flumecinol, phenylbutazone, tricyclic antidepressants increases the production of hydroxylated active metabolites.

It has been established that Artrosilene reduces the effectiveness of certain uricosuric drugs , enhances efficiency A anticoagulants, fibrinolytics, antiplatelet agents, side effects mineralocorticoids,, and hypotensive And diuretics.

Sharing with NSAIDs, GCS, corticotropin, ethanol can cause the development of ulcers and bleeding of the gastrointestinal tract, and increase the likelihood of abnormalities in kidney function.

When used simultaneously with oral anticoagulants, thrombolytics, heparin,, cefamandole antiplatelet agents And cefotetan the risk of bleeding increases.

In addition, this drug enhances the hypoglycemic effect insulin and hypoglycemic agents, therefore, when administered simultaneously, a dose recalculation is required. Combination with valproate leads to aggregation disorders , With , lithium, increases their concentration in plasma. Combined reception with santacid And cholestyramine may reduce the absorption of Artrosilene.

special instructions

When treating with capsules, injection solution and suppositories, monitoring of peripheral blood parameters, as well as the state of liver and kidney functions is required.

When it is necessary to determine 17-ketosteroids, the medication is discontinued 48 hours before the study.

The use of ketoprofen often masks the symptoms of an infectious disease.

Impaired renal and liver function require dosage reduction and careful monitoring of the patient's condition.

Patients suffering may experience an attack of bronchial asthma.

Aerosol and gel Artrosilene should be applied to the skin without damage. It is important that the drug does not get into the eyes and mucous membranes. Hypersensitivity or photosensitivity can be avoided by protecting the skin from sunlight during the entire treatment period.

Terms of sale

The drug in the form of capsules and injection solution is available with a prescription. Artrosilene ointment and spray are over-the-counter drugs.

Artrosilene is a spray with pronounced analgesic and anti-inflammatory effects, intended for external application to the area of ​​affected joints, muscles, ligaments and tendons. The main component of the drug is ketoprofen, a substance from the group of propionic acid derivatives, classified as non-steroidal anti-inflammatory drugs (NSAIDs). The action of Artrosilene is based on inhibition of the activity of COX-1 and COX-2 - enzymes that play a decisive role in the development of inflammatory processes, pain and hyperthermia in the body.

Appearance, components and effect of the aerosol

The developer of the Artrosilene spray is the Italian company Dompe Farmaceutici. It is produced by two pharmaceutical companies - Aerosol Service Italiana from Italy and Zellaerosol from Germany. The medicine is a homogeneous white foam with a delicate lavender aroma, placed in 25 ml aluminum aerosol cans. Each bottle is equipped with a spray nozzle and is packaged in a separate branded box.

The active ingredient of Artrosilene is ketoprofen lysine salt. The content of this component in 100 ml of the product is 15 g. In addition to it, the composition of the medicine includes:

• phenylcarbinol;
• propylene glycol;
• povidone;
• Twin 80;
• propane-butane mixture;
• neroli-lavender flavoring, water.

It is used for diseases of the musculoskeletal system and helps reduce pain, swelling and inflammation in the connective tissue.

In addition, the drug has a moderate antipyretic effect, eliminates morning stiffness of joints and improves their mobility. Ketoprofen has an antibrakinin effect. It suppresses the activity of neutrophil granulocytes, reduces the production of cytotoxins and has no effect on energy metabolism in articular cartilage.

Artrosilene in the form of a spray is intended to relieve pain from injuries and diseases of the musculoskeletal system, accompanied by inflammation of the connective tissue. It is used as part of complex treatment and does not stop the progression of dystrophic changes in the joints and spinal column. The drug has the following indications for use:

• arthritis of various origins;
• osteoarthritis;
• rheumatism;
• gout;
• osteochondrosis;
• Bekhterev's disease;
• periarthritis;
• tenosynovitis;
• tendinitis;
• arthro- and tenosynovitis;
• lumbago;
• neuralgia;
• myalgia;
• traumatic injuries (dislocations, sprains, bruises, rupture of tendons and ligaments).

How to use correctly

Artrosilene (aerosol) should be used externally. To relieve pain, the contents of the bottle must be sprayed onto the surface of the problem area, then rubbed into the skin with light massaging movements. The frequency of use of the product is determined by the doctor. The duration of use of Artrosilene depends on the patient’s condition and can range from 3-5 days to 1 month.

Iontophoresis enhances the healing properties of ketoprofen. When using it, the drug should be placed on the negative pole.

Artrosilene must be applied to previously cleansed skin. Spraying is carried out by pressing the spray nozzle with your fingers. Before each use, the medicine container should be inverted and shaken vigorously. This will ensure uniform distribution of ketoprofen lysine salt in the preparation. After completing the procedure, you must wash your hands thoroughly with soap.

Artrosilene is applied only to intact areas of the skin. You need to make sure that it does not get on the mucous membranes. The areas of the body treated with the medicine should be provided with free access to air. They should not be bandaged or covered with airtight bandages.

During the period of use of the aerosol and for 14 days after completion of treatment, patients are advised to refrain from visiting beaches and solariums. Interaction of treated skin areas with ultraviolet radiation can lead to the development of a photosensitivity reaction.

Restrictions on use

The medical annotation attached to the Artrosilene spray lists contraindications for its use. The medicine must not be used for:

• individual intolerance to its components;
• hypersensitivity to NSAIDs, fenofibrate and products containing sunscreen;
• violation of the integrity of the skin (abrasions, wounds, ulcers) in the area intended for treatment with the drug;
• eczema;
• weeping dermatitis;
• increased sensitivity of the body to ultraviolet radiation;
• "aspirin" asthma.

Instructions for use prohibit aerosol treatment for women in the last trimester of pregnancy. The drug can be used in the first and second trimesters only when absolutely necessary and under the supervision of a specialist.

There is no information on the safety of using Artrosilene spray during breastfeeding. To prevent possible negative effects of the drug on the baby’s body, nursing mothers are advised not to use it during lactation. In pediatric practice, the medicine is approved for use after the child reaches 6 years of age.

The spray should be used with extreme caution in patients suffering from severe heart pathologies, renal or liver failure, porphyria, bronchial asthma, ulcerative lesions of the gastrointestinal tract, as well as elderly people and children 6–12 years old.

Undesirable effects and overdose

Side effects from Artrosilene aerosol are rare and manifest themselves mainly in the form of redness, itching, burning and rash on areas of the skin in contact with the product. People with hypersensitivity to ketoprofen and other components of the drug may experience allergic reactions (urticaria, dermatitis, contact eczema, etc.) during treatment.

Medical practice knows of isolated cases where the external use of Artrosilene provoked kidney dysfunction in a person.

An overdose of Artrosilene when applied to the skin is unlikely, since ketoprofen has a low absorption system and practically does not penetrate into the systemic bloodstream.

Accidental ingestion of the contents of the cylinder may lead to undesirable reactions from the gastrointestinal tract, heart and respiratory system. When they appear, the patient is recommended to undergo symptomatic therapy.

Implementation conditions and patient responses

Artrosilene is intended for over-the-counter sale from pharmacy outlets. Its cost in different pharmacies, according to data as of September 2017, varies from 353 to 435 rubles per pack. In addition to the aerosol under the trade name Artrosilene, today you can purchase capsules and a solution for intravenous and intramuscular administration.

Artrosilene spray must be stored in a dry place protected from sunlight at a temperature not exceeding 25°C. Its shelf life should not exceed 2 years from the date of manufacture indicated on the cylinder.

Artrosilene in injections, capsules or on a gel basis is a non-steroidal anti-inflammatory drug that is based on derivatives of propionic acid. The analgesic, anti-inflammatory and antipyretic effect is based on the fact that under the influence of the active substance the activity of COX is inhibited.

Composition and description

The injection drug “Artrosilene” is based on a pharmacological substance – ketoprofen. Against the background of peripheral and central effects on the body, the component also has anti-bradykinin activity. The state of lysosomal membranes is also stabilized, which is especially important for the effective treatment of patients with rheumatoid arthritis.

The injection solution contains only one active ingredient - lysine salt (ketoprofen). Citric acid, sodium hydroxide and water are used as auxiliary components.

Release forms

"Artrosilene" is a fairly popular drug. The widespread use of the drug has become the reason that for the treatment of various forms of pathologies of the nervous and musculoskeletal systems, manufacturers produce the drug in several dosage forms at once:

1. Gel for external use;
2. Capsules for oral administration;
3. Rectal suppositories;
4. External aerosol;
5. Injection form (solution in ampoules of 2 ml).

Pharmacokinetics

According to the instructions for use, the drug is well absorbed and binds to plasma proteins. The substance has pronounced lipophilicity and quickly penetrates the hematological barrier and brain “shield”. The active substance penetrates into the blood plasma and synovial fluid.

Metabolism occurs against the background of connection with glucuronic acid and in the process of hydroxylation. It is excreted mainly through the kidneys, and also to a small extent through the intestines.

Indications for use

The instructions for use of this pharmacological product contain all the necessary information about the list of diseases and pathological conditions that can be treated with Artrosilene. Main indications for use of the drug:

1. Pathologies that are accompanied by articular syndrome (osteoarthritis, spondylitis, gout of various origins);
2. Elimination of symptoms that accompany the active phase or period of exacerbation of pathologies of the musculoskeletal system (periarthritis, synovitis, tendinitis, bursitis, lumbago);
3. Painful sensations in vertebral structures of various origins;
4. Neuralgia;
5. Myalgia;
6. Uncomplicated injuries (dislocations, sprains, bruises, ligament tears);
7. Prolonged post-traumatic pain;
8. A combination of several diseases at once, complicated by inflammatory processes of the venous system of the lower extremities (phlebitis, periphlebitis, lymphangitis of various origins, superficial lymphadenitis);
9. Postoperative moderate pain;
10. Inflammatory lesions of periarticular tissues;
11. Rheumatic soft tissue damage;
12. Non-rheumatic muscle pain.

Contraindications

Like any other drug, Artrosilene cannot always be used freely. There are a number of absolute contraindications for this drug:

1. Extremely high sensitivity to the components of the drug;
2. Aspirin asthma;
3. Active lactation period;
4. Pregnancy;
5. Exacerbation of ulcerative pathology of the stomach or duodenum;
6. Diveticulitis;
7. Crohn's disease;
8. Colitis;
9. Chronic renal failure;
10. Early childhood;
11. Hemophilia.

There is also a list of conditions for which it is permissible to use the drug, but with extreme caution. These include the following pathologies:

1. Bronchial asthma;
2. Chronic heart failure;
3. Anemia;
4. Alcohol addiction;
5. Liver problems;
6. Diabetes;
7. Elderly age;
8. Excessive smoking;
9. Hyperbilirubinemia;
10. Dehydration of the body;
11. Edema condition;
12. Acute infectious processes aggravated by fever;
13. Arterial hypertension;
14. Stomatitis of varying degrees of intensity.

About the nuances of combination

According to the instructions for use, the simultaneous use of the drug "Artrosilene" with such pharmacological products as rifampicin, phenylbutazone, barbiturates and a number of antidepressants leads to liver overload. If patients have a history of diseases associated with this organ, the therapeutic regimen should be adjusted.

"Artrosilene" reduces the medicinal potency of uricosuric drugs. At the same time, the drug enhances the effect of anticoagulants and other pharmacological products that can thin the blood.

It was also noted that the combination of Artrosilene with hormones, antihypertensive and diuretics leads to an increased risk of side effects. The combined use of drugs based on lysine salt and alcohol leads to an exacerbation of chronic ulcerative pathologies of the stomach, as well as the formation of multiple erosions on the surface of the mucous membrane of the gastrointestinal tract.

How to use the drug correctly

The instructions for use of the drug explain all the nuances regarding how to correctly determine the dosage and method of using the drug in any pharmacological form. Let's consider the basic rules for using the injectable form of the drug for medicinal purposes.

The injection method of administering the drug is practiced as a short-term treatment. Therapy is carried out on average for three days. There are solutions for intramuscular and intravenous injections.

The maximum dose per day is one ampoule twice a day. After opening the ampoule, the solution is immediately drawn into a syringe and injected.

Intravenous administration

Intravenous infusions are given slowly. It is customary to use sodium chlorine solutions (0.9%), water-based levulose solution (10%), and dextrose aqueous solution (5%). You can also use Ringer's solution and Hartmann's solution. Large volumes of 500 ml, as well as small dosages of 50 ml are used.

Using the solution in physiotherapy

Physiotherapists also actively practice the use of an aqueous solution of lysine salt. The drug is justified when exposed through iontophoresis and during mesotherapy.

Side effects

1. Severe abdominal cramps;
2. Diarrhea;
3. Stomatitis;
4. Primary gastritis, exacerbation of chronic processes;
5. The occurrence of erosions on the surface of the mucous membranes;
6. Melena;
7. Increased bilirubin levels;
8. Development of hepatitis;
9. Dizziness;
10. Hyperkinesia;
11. Tremor;
12. Vertigo;
13. Sudden mood swings;
14. Irritability;
15. General malaise;
16. Rhinitis.

Much less frequently, visual impairment or conjunctivitis may occur. Occasionally, patients experience various manifestations of an allergic nature: itching, urticaria, tissue swelling, laryngospasm and laryngeal edema.

Least often, patients may suffer from the following undesirable manifestations:

1. Cystitis or exacerbation of the chronic form of this disease;
2. Hematuria (traces in the blood);
3. Deterioration of the general blood picture;
4. Hepatomegaly (if the drug is stopped in a timely manner, the pathological changes are reversible);
5. Vasculitis;
6. Dyspnea;
7. Increased blood pressure at the time of intravenous administration of the drug;
8. Increased heart rate;
9. Feeling of increasing discomfort in the anorectal area;
10. Exacerbation of chronic forms of hemorrhoids;
11. Intense photosensitivity.

Considering such a large number of quite serious complications and side effects, it is unacceptable to start self-medication with the drug “Artrosilene”. The therapeutic regimen is formed only by the attending physician, after carrying out all appropriate diagnostic measures and taking into account the intake of other pharmacological products.

Artrosilene: instructions for use and reviews

Latin name: Artrosilene

ATX code: M02AA10

Active substance: ketoprofen

Manufacturer: Dompe Farmaceutici (Italy), ISTITUTO de ANGELI (Italy), Zellaerosol GmbH (Germany), Valpharma S.A. (San Marino), Alfa Wassermann (Italy), Abiogen Pharma S.p.A. (Italy)

Updating the description and photo: 09.09.2019

Artrosilene is a drug with analgesic, antipyretic and anti-inflammatory effects.

Release form and composition

Dosage forms of Artrosilene:

• capsules: gelatin, oblong, white body and dark green cap, capsules contain round granules from light yellow to white (10 pieces in blisters, 1 blister in a cardboard box);
• solution for intravenous/intramuscular administration: transparent, slightly yellowish or colorless (in dark glass ampoules of 2 ml, 6 ampoules per tray, 1 tray in a cardboard box);
• rectal suppositories: from light yellow to white, homogeneous, torpedo-shaped (5 pieces 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 is released is a transparent liquid from light yellow to white (25 g 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 using Artrosilene.

Composition of 1 capsule:

• active ingredient: lysine salt of ketoprofen – 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 ingredient: lysine salt of ketoprofen – 80 mg;
• auxiliary components: citric acid, sodium hydroxide, water for injection.

Composition of 1 suppository:

• active ingredient: lysine salt of ketoprofen – 160 mg;
• auxiliary component: semi-synthetic glycerides.

Composition of 100 mg gel:

• active ingredient: 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 ingredient: ketoprofen lysine (lysine salt of ketoprofen) – 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 by inhibiting COX (cyclooxygenase) types I and II. It exhibits antibradykinin activity, stabilizes lysosomal membranes and delays the process of 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 are reduced, and the range of movements increases. Unlike ketoprofen, ketoprofen lysine salt is a rapidly soluble molecule with a neutral pH and has almost no irritant effect on the gastrointestinal tract.

When using an aerosol or gel Artrosilene, a local therapeutic effect is provided on the affected ligaments, muscles, joints, and tendons. Ketoprofen does not have a catabolic effect on articular cartilage.

Pharmacokinetics

Capsules, rectal suppositories, injection solution

Suction:

• capsules: ketoprofen after oral administration is almost completely absorbed from the gastrointestinal tract, its bioavailability is more than 80%. Cmax (maximum concentration of the substance) in plasma is achieved in 4–10 hours, its value is dose-dependent and amounts to 3–9 μg/ml. T1/2 (half-life) – 6.5 hours. The maximum therapeutic effect is observed within 4–24 hours. Food reduces Cmax and lengthens the time to reach it, while the AUC (area under the concentration-time curve) does not change;
• rectal suppositories: ketoprofen is quickly absorbed after rectal use. The time to reach Cmax is from 45 to 60 minutes. The plasma concentration depends linearly on the dose taken.
• injection solution: with parenteral administration, the time to reach Cmax is 20–30 minutes. The effective concentration is maintained for 24 hours. In synovial fluid, the therapeutic concentration lasts from 18 to 20 hours;

Up to 99% of absorbed ketoprofen is bound to plasma proteins, mainly albumin. Vd (volume of distribution) ranges from 0.1 to 0.2 l/kg. It penetrates easily through histohematic barriers and is distributed in organs and tissues. The substance penetrates well into connective tissue 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 with subsequent formation of esters with glucuronic acid.

Metabolites are excreted in the urine. Up to 1% is excreted in feces. Does not accumulate.

When applied externally, ketoprofen is absorbed slowly.

A dose of 50–150 mg of gel over 5–8 hours produces a plasma level of 0.08–0.15 mcg/mL. The bioavailability of the gel is approximately 5%.

The level of ketoprofen in the blood after application of the aerosol is less than 0.1 mcg/ml, the amount of the substance (free or conjugated) excreted by the kidneys in the next 48 hours is equivalent to 0.62% of the drug dose. The level of ketoprofen in the synovial fluid is equivalent to 0.2–2 μg/ml (depending on the dose applied).

Indications for use

Capsules, rectal suppositories

• pain of mild/moderate intensity, including pain of an inflammatory nature, postoperative/post-traumatic pain (relief);
• rheumatic/inflammatory diseases, including spondyloarthritis, osteoarthritis, rheumatoid/gouty arthritis, inflammatory lesions of 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 pain of non-rheumatic/rheumatic origin;
• 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;
• soft tissue damage of traumatic origin.

Contraindications

Absolute contraindications for Artrosilene in all dosage forms:

• "aspirin triad";
• pregnancy (III trimester) and lactation period;
• 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:

• bleeding disorders, including hemophilia;
• peptic ulcer of the stomach and duodenum during exacerbation;
• ulcerative colitis during 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 (prescribing 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;
• 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 during exacerbation;
• severe functional disorders of the kidneys/liver;
• age from 6 to 12 years.

Artrosilene, instructions for use: method and dosage

Capsules

Artrosilene capsules are taken orally, preferably at the same time/after meals.

Daily dose – 1 capsule (in 1 dose).

It is possible to carry out a long course - from 3 to 4 months.

Rectal suppositories

Artrosilene is used rectally.

Single dose – 1 suppository, frequency of use – 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.

Daily dose – 160 mg.

Maximum – 320 mg per day, for elderly patients – 160 mg per day.

In the form of injections, Artrosilene 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 in stationary conditions. To increase the duration of action of Artrosilene, slow intravenous infusions are recommended - 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 Artrosilene in small volumes (50 ml) of the solution, it is administered intravenously as a bolus.

Gel, aerosol for external use

Artrosilene gel and spray are used externally.

The drug is applied 2-3 times a day, rubbing it in carefully until completely absorbed.

The duration of the course is up to 10 days (unless otherwise prescribed by the doctor).

Side effects

• central and peripheral nervous system: general malaise, hyperkinesia, dizziness, tremor, vertigo, anxiety, mood swings, irritability, hallucinations, blurred vision;
• 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, swelling, 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, sensation of laryngeal spasm, bronchospasm, dyspnea, laryngospasm, rhinitis;
• allergic and dermatological reactions: angioedema, urticaria, exudative erythema multiforme (including Stevens-Johnson syndrome), maculopapular rash, anaphylactoid reactions (swelling of the pharynx, oral mucosa, periorbital edema), itching, erythematous exanthema;
• others: menstrual irregularities, conjunctivitis, increased sweating;
• local reactions when used 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 area.

Compared to ketoprofen, the lysine salt of ketoprofen causes side effects much less frequently.

Overdose

Cases of overdose of Artrosilene with systemic use have not been reported. When used externally, overdose is practically impossible, which is 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 therapy, periodic monitoring of the peripheral blood picture and the functional state of the kidneys/liver is required.

If it is necessary to determine 17-ketosteroids, Artrosilene is canceled 2 days before the study.

Therapy may mask the symptoms of an infectious disease.

In case of bronchial asthma, the use of Artrosilene can lead to the development of an attack of suffocation.

The drug can be applied externally only to undamaged areas of the skin. It is necessary to avoid getting Artrosilene into the eyes and mucous membranes.

Aqueous solutions of lysine salt of ketoprofen, as well as external gel, can be used in physiotherapeutic therapy (mesotherapy, iontophoresis): when carrying out iontophoresis, the drug is applied to the negative pole.

In order to prevent manifestations of photo- and hypersensitivity, it is recommended to avoid exposure of the skin to sunlight during the treatment course.

Impact on the ability to drive vehicles and complex mechanisms

While using Artrosilene, you should refrain from potentially dangerous types of work, the performance of which requires increased concentration and rapid psychomotor reactions.

Use 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.

Use in childhood

Age restrictions for the use of Artrosilene:

• gel, aerosol: contraindicated for children under 6 years of age; children 6–12 years old – prescribed with caution;
• capsules, injection solution, rectal suppositories: contraindicated for children under 18 years of age.

For impaired renal function

Artrosilene in the form of capsules, solution and suppositories is contraindicated for use in chronic renal failure.

Arthrosilene aerosol and gel should be used with caution in severe renal impairment.

For liver dysfunction

The use of Artrosilene requires caution:

• capsules, solution and suppositories: patients with alcoholic cirrhosis and liver failure;
• gel, aerosol: for severe liver dysfunction.

Use in old age

For elderly patients, Artrosilene is prescribed with caution.

Drug interactions

When Artrosilene is used in combination 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 effect;
• uricosuric, antihypertensive drugs, diuretics: decrease in their effectiveness;
• other non-steroidal anti-inflammatory drugs, glucocorticosteroids, ethanol, corticotropin: increased likelihood of ulcers and gastrointestinal bleeding, renal functional disorders;
• mineralocorticoids, glucocorticoids, estrogens: increased severity of their side effects;
• insulin and oral hypoglycemic drugs: increased hypoglycemic effect (dose adjustment may be required);
• oral anticoagulants, heparin, thrombolytics, antiplatelet agents, cefoperazone, cefamandole and cefotetan: increased likelihood of bleeding;
• verapamil, nifedipine, lithium, methotrexate: increase in their plasma concentration;
• sodium valproate: impaired platelet aggregation;
• cholestyramine, antacids: decreased absorption of ketoprofen.

Analogs

Analogs of Artrosilene are: Febrofid, Ketoprofen, Fastum, Oruvel, Spazgel, Ketospray, Flexen, VALUSAL, Artrum, Ketonal, Bystrumgel.

Terms and conditions of storage

Store in a place protected from light, out of reach of children at temperatures up to 25 °C. The aerosol container must not be overheated.

Best before date:

• capsules, rectal suppositories – 5 years;
• injection solution, gel, aerosol – 3 years.

Conditions for dispensing from pharmacies

Released:

• capsules, solution, suppositories: according to prescription;
• gel, aerosol: without prescription.

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