- Part capsules the active ingredient is included: ketoprofen presented in the form of a lysine salt. Additional ingredients: diethyl phthalate, carbopol, povidone, magnesium stearate, acrylic and methacrylic acid polymers, talc, titanium dioxide, gelatin, indigotin and quinoline yellow.
- Injection solution also contains active ingredient: ketoprofen - lysine salt. Auxiliary components: citric acid, sodium hydroxide, sterile water.
- Suppositories Artrozilen include an active substance in their composition: ketoprofen , in the form of a lysine salt. Auxiliary components: semi-synthetic glycerides.
- Preparation in the form gel consists of an active substance: ketoprofen - lysine salt. Additional components: polysorbate, carbopol, TEA, ethanol, nerolen or lavender flavoring, methylparaben and prepared water.
- Spray can contains active substance: ketoprofen - lysine salt. Auxiliary components: nerolen or lavender, polysorbate 80, PPG, benzyl alcohol, PVP, treated water.
Release form
Artrozilen is produced in several pharmacological forms, namely in the form:
- gel for external use 30-50g;
- capsules for oral administration, 10 pieces per pack;
- injection solution in ampoules of 2 ml, 6 pieces per package;
- rectal suppositories, 10 per pack;
- external aerosol 25 ml.
pharmachologic effect
All forms of Artrozilene are characterized by analgesic, antipyretic and anti-inflammatory effects.
Pharmacodynamics and pharmacokinetics
The manifestation of anti-inflammatory, analgesic and antipyretic effect is provided by the ability of ketoprofen to inhibit COX-1 and -2, inhibit the synthesis of PG. In addition, the drug is characterized by anti-bradykinin activity, stabilization of lysosomal membranes and inhibition of their release from the composition that contribute to tissue destruction in cases of chronic inflammation. The release of cytokines decreases, the activity of neutrophils slows down.
The use of Artrozilen allows you to reduce morning stiffness, joint swelling, and increase the range of motion.
Lysine salt, which is part of the ketoprofen preparation, is a rapidly dissolving molecule with a neutral pH. Therefore, Artrozilene practically does not irritate the gastrointestinal tract.
Outdoor use spray or gel provided by local anti-inflammatory, anti-exudative and analgesic the effect. In this case, a high local therapeutic effect is manifested on the affected joints, tendons, ligaments, muscles. Treatment with a drug for articular syndrome allows you to relieve joint pain, both in a calm state and during movement, morning stiffness and swelling of the joints decreases. It was found that Artrozilene does not have a destructive effect on the articular cartilage.
When taking capsules, the active substance is fully absorbed from the gastrointestinal tract, with a bioavailability higher than 80%. The maximum concentration is reached after 4-10 hours from the moment of 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 full-fledged connection inside the body ketoprofen with plasma proteins. The substance is able to penetrate histohematogenous barriers, into tissues and synovial fluid, where it is distributed. ketoprofen occurs in the liver, undergoing glucuronidation with the production of esters and glucuronic acid. Withdrawal carried out as part of urine and an insignificant part with feces.
The action of the injection solution manifests itself 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 the histohematogenous barriers into tissues and physiological fluids, being evenly distributed in the body. Metabolism occurs with the participation of liver enzymes, which are mainly excreted by the kidneys, within 24 hours.
When using the drug in the form of rectal suppositories, its effect is manifested 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. The penetration of the substance through the histohematogenous barriers, being distributed in tissues and important organs, was noted. Metabolism occurs in the liver, with the production of esters and glucuronic acid. Excretion of metabolites occurs in the urine.
The use of external gel and aerosol products is marked by slow absorption. In this case, the effect of the substance manifests itself for a short time and lasts 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 the 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.
The indications for the appointment of gel and aerosol are:
- diseases of the musculoskeletal system, for example - rheumatoid and psoriatic arthritis, osteoarthritis peripheral joints or spine, ankylosing spondylitis, rheumatic damage soft tissues;
- traumatic soft tissue injuries
muscle rheumatic and non-rheumatic pains.
Contraindications for use
- high sensitivity to the drug;
- aspirin;
- , ;
- exacerbation of gastric ulcer and 12-duodenal ulcer, peptic ulcer;
- diverticulitis;
- acute ulcerative , Crohn's disease;
- chronic ;
- childhood;
- and other disorders associated with blood clotting, and so on.
- weeping 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 disorders in the activity of the digestive tract, liver, nervous system, sensory organs and hematopoiesis, 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, the occurrence of photosensitization is possible.
In any case, a specialist consultation is required.
Instructions for the use of Artrozilen (Way and dosage)
The drug is available in several pharmacological forms intended for oral, rectal, parenteral and external administration.
Tablets for oral administration are prescribed daily for 1 piece at the same time or after meals. The therapeutic course can last 3-4 months.
A solution for i / m or i / v is prescribed for use in 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 Artrozilen instructions for use recommend to apply in small amounts daily 2-3 times. In this case, a single dosage of an aerosol is 1-2 g. The duration of therapy is set by the attending physician, but it should not be longer than 10 days.
Overdose
Cases of overdose with Artrozilen drugs have not been described.
Interaction
Simultaneous use with inducers of microsomal oxidation in the liver - phenytoin, barbiturates, flumecinol, phenylbutazone, tricyclic antidepressants increases the production of hydroxylated active metabolites.
It has been found that Artrozilene reduces the effectiveness of some uricosuric agents , enhances efficiency and anticoagulants, fibrinolytics, antiplatelet agents, side effects mineralocorticoids,, as well as hypotensive and diuretics.
Sharing with NSAIDs, GCS, corticotropin, ethanol can cause the development of ulcers and bleeding of the gastrointestinal tract, 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, with simultaneous administration, dose recalculation is required. Combination with valproate leads to aggregation disorders , from , lithium, increases their concentration in the 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, then the drug is canceled before the study for 48 hours.
The use of ketoprofen often masks the symptoms of an infectious disease.
Dysfunctions of the kidneys and liver require lower dosage and careful monitoring of the patient's condition.
Patients suffering from an attack of bronchial asthma may occur.
Aerosol and Gel Artrosilene must be applied to the skin without damage. It is important that the drug does not get into the eyes and mucous membranes. You can avoid hypersensitivity or photosensitivity by protecting your skin from sunlight during the entire treatment period.
Terms of sale
The drug in the form of capsules and solution for injection is available with a prescription. Artrosilene ointment and spray are non-prescription drugs.
The drug Artrozilene, a non-steroidal anti-inflammatory drug, the main active ingredient of which is ketoprofen lysine salt. This component does not cause a negative effect on the gastrointestinal tract, the body accepts it more easily, while ketoprofen irritates the stomach walls.
The medicine has several forms: topical gel, capsules, liquid for injection into muscles or veins, rectal suppositories, spray.
Composition, release form
- Artrosilene capsules consist of the main ingredient - ketoprofen in the form of a soluble form of acetylsalicylic acid (lysine salt) and excipients.
- Solution for injection: lysine salt and additional components.
- Suppositories: the main substance is ketoprofen in the form of a soluble form of acetylsalicylic acid and auxiliary substances: semi-synthetic glycerols.
- Artrosilene gel has the following composition: the main component is lysine salt and additional substances.
- Aerosol: active ingredient - ketoprofen and auxiliary ingredients.
As you can see, the composition of all types of the drug, regardless of the form of release, is the same.
Artrosilene is produced in the following forms:
- Gel for external use in a package of 30-50 grams. External data: transparent, medium density with a lavender scent.
- Capsules - 10 pieces in a blister. They have a rounded granulate in a gelatin capsule.
- Darkened glass ampoules of 2 ml in a cardboard box in the amount of 10 pieces. Appearance: transparent, colorless or with a yellowish tint. The content of the basic substance is 160 mg.
- Rectal suppositories in the amount of 10 pieces in a cardboard box. Outwardly homogeneous, torpedo-like, white or light yellow. The content of the main active ingredient is 160 mg.
- Aerosol 25 ml. Appearance: white homogeneous foam. 1 gram contains 150 mg of the main component.
Each package of Artrosilene contains instructions for use.
Pharmacological effect
Artrozilene is used in the complex therapy of ailments of the spine and mobile joints. This remedy has an analgesic effect and also helps to remove fever and inflammation. Taking a course of medication helps to eliminate morning stiffness, reduce swelling of the affected area and restore the motor ability of the joint.
This drug affects only the musculoskeletal system, reducing inflammation, soreness and fever. It relieves the symptoms of ailments, but does not affect the factors of occurrence of diseases. Therefore, it is prescribed against the background of drugs that affect the causes of the development of ailments in complex therapy. Due to the almost instantaneous effect on pain, it is used quite actively after surgery, as well as for any injuries of the musculoskeletal system.
The effect against inflammation, pain and fever is achieved by inhibition of cyclooxygenase-1 and -2, as well as by suppressing the synthesis of prostaglandins. The drug has the ability not to lower blood pressure, normalizes lysosomal plates and inhibits the release from their composition of substances that contribute to destructive processes in tissues during the chronic course of the inflammatory process. Reduces the release of specific proteins of cytokines and reduces the intense action of neutrophils. 
Gel and spray
When using a gel or spray, it locally affects inflammation, increased vascular permeability and exudate release into the tissue, as well as eliminating pain. At the same time, it has a high local effect on the movable joint, tendons, ligaments and the muscular system. In the process of joint therapy, it relieves pain both at rest and during physical activity. Stiffness in the morning and swelling in the movable joint are reduced. It does not have an aggressive effect on cartilage tissue.
Slow adsorption is noted when using gel and aerosol. They have a short duration of action and retain the healing effect for up to 5-8 hours. Biological activity is about 5%.
Capsules
When capsules are taken orally, the main ingredient is completely absorbed through the gastrointestinal tract with a bioavailability of more than 80%. The highest content in the circulatory system is reached after 4-10 hours from the moment of consumption, depending on the dose. The healing effect lasts from 4 hours to a day. Eating can cause a decrease in the content of a substance in the plasma of the circulatory system. A full-fledged relationship of ketoprofen with the protein components of the circulatory system is observed.
It can penetrate internal barriers into tissues and fluid filling the joint cavity. Metabolic processes occur in the liver, and metabolic products are excreted from the body with urine or, to a small extent, with feces.
Injections
If Artrozilena injections are prescribed, the effect on the body occurs after 20-30 minutes, and the therapeutic effect lasts for 18-20 hours. The main component is completely absorbed, entering into contact with the protein substances of the circulatory system. Injections have a penetrating ability through internal barriers into tissues and body fluids. Metabolic processes occur in the liver, and the removal of metabolic products is carried out through the kidneys during the day.
Candles
When using candles, the effect on the body begins after 45-60 minutes. The highest plasma concentration directly depends on the dose of the drug. The main component is completely absorbed, entering into contact with the protein substances of the circulatory system. Possesses penetrating ability through protective barriers into tissues and organs. Metabolic processes take place in the liver, and metabolic products are excreted in the urine.
Indications for use
For capsules and suppositories:
- moderate or mild soreness with inflammation, after surgery and trauma;
- inflammatory process in the joints of a rheumatoid or gouty nature;
- deforming arthrosis;
- ankylosing spondylitis;
- inflammation of the tissues located near the joint.
Short-term treatment injections:
- diseases of the musculoskeletal system of various etiologies;
- soreness associated with an inflammatory process after surgery or injury.
Gel and aerosol:
- diseases of the musculoskeletal system: inflammation in the joints of a rheumatoid or gouty nature, deforming arthrosis of the spinal column and peripheral mobile joints, ankylosing spondylitis, soft tissue disorders in rheumatoid processes;
- soft tissue injuries;
- soreness in the muscular system of a different nature - rheumatic and not rheumatic.
Use with great care in the following cases:
- bronchial asthmatic status;
- chronic heart failure;
- low hemoglobin content;
- painful craving for alcohol;
- liver failure;
- erosive and ulcerative lesions of the gastrointestinal tract;
- inflammation of the oral mucosa;
- conditions accompanying an increase in bilirubin in the circulatory system;
- old age;
- smoking;
- a group of endocrine diseases.
Contraindications
- hypersensitivity to the components of the drug;
- bronchial asthma on drugs based on aspiric acid;
- period of gestation and breastfeeding;
- ulcers of the stomach and duodenum in the stage of relapse, as well as local damage to the lining of the digestive tract under the influence of gastric juice;
- inflammation of the lining of the colon in the acute stage with ulcerative lesions and granulomatous enteritis;
- renal failure in the chronic stage;
- diseases associated with poor blood clotting.
Aerosol and ointment, in addition to the above contraindications, are not recommended for use in the background:
- ailments of the skin of a weeping nature;
- chronic recurrent inflammatory processes of the skin;
- skin damage.
Suppositories are not prescribed for hernial protrusions of the intestinal wall.
Undesirable consequences
When taking Artrozilen, changes in the performance of the gastrointestinal tract, liver, nervous system, genitourinary organs and respiration, changes in touch and smell, hemopoiesis, as well as mood swings, black shapeless emptyings with a characteristic unpleasant odor, dizziness, hallucinations, pain during urination can be observed , puffiness, the presence of bloody contents in the urine, heart palpitations and others.
There may also be manifestations of the skin in the form of an allergic reaction and changes in the skin.
When using a gel and an aerosol, phenomena of increased sensitivity of the body to the action of ultraviolet and visible radiation can be observed.
Important! If any side effect occurs, it is necessary to consult with a specialist for further decisions on the use of this drug or the transition to analogues.
Methods of administration and dosage of the drug
This medicine is produced in the form of suppositories, gel, capsules, injection and aerosol.
Capsules are prescribed orally 1 time per day, 1 capsule at the end of a meal or immediately after it ends. Duration of admission is from 3 to 4 months.
Injections are intended for intramuscular or intravenous infusion of 1 ampoule during the day. This type of drug is prescribed for a short period of treatment (no more than 3 days) in a clinical hospital. To continue therapy, they switch to the use of capsules or use rectal suppositories. Intravenous infusion is carried out only in a clinical hospital. The duration of the drip is approximately 30 minutes. The solution for intravenous infusion is produced on the basis of 50 or 500 ml of aqueous solutions: isotonic, 10% levulose, 5% dextrose, Ringer's acetate or Hartmann.
Suppositories are administered by insertion into the rectum. 1 suppository is prescribed 2-3 times a day. The highest dosage during the day should not be more than 480 mg. For the elderly age category of people, a dosage of no more than 2 suppositories is recommended per day.
The aerosol and gel are applied to the skin in small portions 2-3 times throughout the day by rubbing into the skin and wait until the product is completely absorbed. A single dosage of the drug does not exceed 1-2 grams. The duration of therapy is determined by a specialist, but should not exceed more than a 10-day course.
Overdose
Overdose cases with this drug have not been established.
Interaction with other medicinal products
Against the background of taking drugs, microsormal oxidation of substances that activate the synthesis of cytochrome and the transfer of the corresponding mRNA (phenytoin, barbiturates, rifampicin, antidepressants and others) in the liver site contribute to the increased production of glycols of active substances.
Artrosilene helps to reduce the effect of certain drugs that increase the secretion of uric acid. It increases the effectiveness of drugs that prevent the formation of blood clots and cause the destruction of the formed fibrin filaments, reduces the undesirable effects of mineralocorticosteroid drugs, steroid female sex hormones, as well as drugs aimed at lowering blood pressure, and diuretics.
Against the background of taking glucocorticosteroids, non-steroidal anti-inflammatory drugs and ethanol, Artrosilene can cause the formation of ulcers and bleeding in the gastrointestinal tract, increase the likelihood of the formation of abnormalities in the functioning of the kidneys.
- Increases the likelihood of bleeding while taking by mouth with drugs that reduce the activity of blood coagulation, with increased thrombus formation, as well as with Heparin, Cefoperazone, Cefotetan, Tsefamandol.
- Strengthens the action of insulin and drugs, the effect of which is aimed at lowering glucose levels in the circulatory system. With simultaneous use, it is necessary to recalculate the dosage of hypoglycemic drugs.
- Against the background of use with Valproate, it leads to a change in platelet aggregation. And when taken simultaneously with veropomil, lithium, nifedipine, methotrexate, it increases the platelet count in the circulatory system.
- Joint reception with Antacid and Kolestiramine can help to reduce the absorption of Artrosilene.
Special conditions
During therapy with suppositories, injections and capsules of this drug, it is necessary to monitor the parameters of the peripheral circulatory system and the performance of the liver and kidneys.
- Before the analysis for 17-ketosteroids, it is necessary to cancel Artrolysin 2 days before the examination.
- While taking this medication, it is possible to hide the symptoms of infectious diseases.
- In diseases of the liver and kidneys, the dosage of the drug must be reduced, and constant monitoring of the patient's condition is also necessary.
- With the existing bronchial activity, asthma exacerbation is possible.
- When planning to carry a fetus, this drug should be discontinued due to the reduced likelihood of egg engraftment.
The gel and aerosol must be applied to the skin, which is not damaged. It is necessary to ensure that the drug does not get on the mucous membranes of the mouth and eyes. To avoid the negative effects of these forms of the drug, it is necessary to protect the skin from direct sunlight during their use.
Important! With the use of this drug with alcohol-containing products, the likelihood of bleeding in the gastrointestinal tract increases significantly.
- Terms of sale. It is dispensed in a retail pharmacy network on a prescription form for capsules, suppositories and injections, without it - for ointments and aerosols.
- Storage data. It is necessary to store the drug in a dark place, protected from sunlight and children, at a temperature not exceeding 25 degrees Celsius.
- Shelf life. 36 months from the date of manufacture.
- Similar funds. Ketoprofen, Ketonal, Oruvel, Fastum, Flamax, Ostofen, Ultrafastin and other drugs of a similar effect.
Composition and form of release
in a blister 10 pcs .; in a pack of cardboard 1 blister.
in dark glass ampoules, 2 ml; 6 pcs in a pallet, 1 pallet in a cardboard box.
in a strip 5 pcs.; in a pack of cardboard 2 strips.
in aluminum tubes of 30 and 50 g; in a pack of cardboard 1 tube.
in cylinders with a capacity of 25 ml with a spray nozzle; in a pack of cardboard 1 cylinder.
Description of the dosage form
Capsules: oblong hard gelatin capsules; body - white, lid - dark green. The contents of the capsule are round granules from white to light yellow.
Solution for intravenous and intramuscular administration: transparent colorless or slightly yellowish solution.
Rectal suppositories: uniform, from white to light yellow, torpedo-shaped.
Gel: transparent, thick, with a lavender scent.
Spray can: white homogeneous foam; after the gas escapes, it is a clear, pale yellow liquid.
pharmachologic effect
pharmachologic effect - antipyretic, analgesic, anti-inflammatory.Pharmacodynamics
It has anti-inflammatory, analgesic and antipyretic effects. By inhibiting COX-1 and -2, it inhibits GHG synthesis. It has anti-bradykinin activity, stabilizes lysosomal membranes and delays the release of enzymes from them that contribute to tissue destruction in chronic inflammation. Reduces the release of cytokines, inhibits the activity of neutrophils.
Reduces morning stiffness and swelling of joints, increases range of motion.
Ketoprofen lysine salt, unlike ketoprofen, is a rapidly dissolving molecule with a neutral pH and almost does not irritate the gastrointestinal tract.
When applied topically, it has a local anti-inflammatory, anti-exudative and analgesic effect. In the form of a spray or gel, it provides a local healing effect on the affected joints, tendons, ligaments, muscles. With articular syndrome, it causes a decrease in joint pain at rest and during movement, a decrease in morning stiffness and swelling of the joints. The lysine salt of ketoprofen has no catabolic effect on the articular cartilage.
Pharmacokinetics
Capsules
Suction. Assigned internally, ketoprofen is sufficiently fully absorbed from the gastrointestinal tract, and its bioavailability exceeds 80%. C max in plasma when taking Artrosilene capsules is noted 4-10 hours after oral administration, its value directly depends on the dose taken and is 3-9 μg / ml. T 1/2 is 6.5 hours. The maximum therapeutic effect is observed for 4 to 24 hours. Food contributes to a decrease in C max values \u200b\u200band an increase in T max without changing the AUC.
Distribution.
Metabolism.
Excretion. Metabolites are excreted in the urine. Less than 1% is excreted with feces. The drug does not cumulate.
T max for parenteral administration - 20-30 minutes. The effective concentration is maintained for 24 hours. The therapeutic concentration in the synovial fluid is maintained for 18-20 hours.
Distribution. Up to 99% of absorbed ketoprofen binds to plasma proteins, mainly albumin. V d - 0.1-0.2 l / kg. Easily penetrates the histohematogenous barriers and is distributed in tissues and organs. Ketoprofen penetrates well into synovial fluid and connective tissues. 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 liver microsomal enzymes. It is excreted by the kidneys, 60-80% - in the form of glucuronide in 24 hours.
Suppositories
Suction. Ketoprofen lysine salt is rapidly absorbed: T max after rectal administration - 45-60 minutes. The value of plasma concentration is linearly dependent on the dose taken.
Distribution. Up to 99% of absorbed ketoprofen binds to plasma proteins, mainly albumin. V d - 0.1-0.2 l / kg. Easily penetrates the histohematogenous barriers and is distributed in tissues and organs. Ketoprofen penetrates well into synovial fluid and connective tissues. 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 mainly metabolized in the liver, where it undergoes glucuronidation to form glucuronic acid esters.
Excretion. Metabolites are excreted mainly in the urine (up to 76% after 24 hours). The drug does not cumulate.
Gel, aerosol
When applied to the skin, it is absorbed slowly; a dose of 50-150 mg after 5-8 hours creates a plasma concentration level of 0.08-0.15 μg / ml. Virtually no cumulates in the body. Bioavailability is about 5%.
Indications of the drug Artrosilene
Capsules, suppositories
relief of pain of mild and moderate intensity (including pain of an inflammatory nature, postoperative and post-traumatic).
Capsules, suppositories
rheumatic diseases:
rheumatoid arthritis;
spondyloarthritis;
osteoarthritis;
gouty arthritis;
inflammatory damage to the periarticular tissues.
Solution for i / v and i / m administration
short-term treatment of acute pain syndrome in diseases of the musculoskeletal system of various origins, postoperative pain, post-traumatic pain associated with inflammation.
Gel, aerosol:
diseases of the musculoskeletal system (including rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, osteoarthritis of the peripheral joints and spine, rheumatic lesions of soft tissues);
muscle pains of rheumatic and non-rheumatic origin;
traumatic soft tissue injuries.
Contraindications
All forms:
hypersensitivity, incl. to other NSAIDs;
aspirin asthma;
lactation period;
peptic ulcer of the stomach and duodenum in the acute phase, peptic ulcer;
ulcerative colitis in the acute phase, Crohn's disease;
diverticulitis;
hemophilia and other blood clotting disorders;
chronic renal failure.
children under 18 years of age.
Capsules, suppositories, gel, aerosol
pregnancy (III trimester).
Solution for i / v and i / m administration
pregnancy.
For external use additionally:
weeping dermatoses;
violation of the integrity of the skin;
children under 6 years of age.
Carefully:
All forms
bronchial asthma;
chronic heart failure;
elderly age.
Capsules, suppositories, gel, aerosol
pregnancy (I, II trimester).
Capsules, solution for i / v and i / m administration, suppositories
alcoholism;
smoking;
alcoholic cirrhosis of the liver;
hyperbilirubinemia;
liver failure;
diabetes;
dehydration;
arterial hypertension;
blood diseases (including leukopenia);
deficiency of glucose-6-phosphate dehydrogenase;
stomatitis.
Gel, aerosol
hepatic porphyria;
erosive and ulcerative lesions of the gastrointestinal tract;
severe violations of liver and kidney function;
children under 12 years of age.
Application during pregnancy and lactation
Capsules, solution for i / v and i / m administration, suppositories
Like other NSAIDs, Artrozilene should not be used in the third trimester of pregnancy. The use of the drug in the I and II trimesters should be carefully monitored by the attending physician. Breastfeeding while using the drug should be discontinued.
Gel, aerosol
Cannot be used in the third trimester of pregnancy.
There is no experience of using Artrosilene during lactation. Use in the I and II trimesters is possible only after consulting a doctor.
Side effects
Capsules, solution for i / v and i / m administration, suppositories
From the digestive tract: abdominal pain, diarrhea, stomatitis, esophagitis, gastritis, duodenitis, erosive and ulcerative lesions of the gastrointestinal tract, hematomesis, melena.
From the liver: increased bilirubin levels, increased activity of liver enzymes, hepatitis, liver failure, enlarged liver
From the nervous system: dizziness, hyperkinesia, tremors, vertigo, mood swings, anxiety, hallucinations, irritability, general malaise.
From the senses: conjunctivitis, visual impairment.
From the side of the skin: urticaria, angioedema, erythematous exanthema, itching, maculopapular exanthema, increased sweating, erythema multiforme exudative (including Stevens-Johnson syndrome).
From the genitourinary system: painful urination, cystitis, edema, hematuria, menstrual irregularities.
From the side of the hematopoietic organs: leukocytopenia, leukocytosis, lymphangitis, decreased PT, thrombocytopenia, thrombocytopenic purpura, enlarged spleen, vasculitis.
From the respiratory system: bronchospasm, dyspnea, laryngeal spasm sensation, laryngospasm, laryngeal edema, rhinitis.
On the part of the cardiovascular system: hypertension, hypotension, tachycardia, chest pain, syncope, peripheral edema, pallor.
Allergic reactions: anaphylactoid reactions, edema of the oral mucosa, pharyngeal edema, periorbital edema.
Suppositories additionally
Local reactions: burning, itching, heaviness in the anorectal region, exacerbation of hemorrhoids.
Gel, aerosol
Allergic reactions, photosensitivity.
If any undesirable phenomenon develops, you should consult a doctor.
Interaction
Inducers of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, flumecinol, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites.
Reduces the effectiveness of uricosuric drugs, enhances the effect of anticoagulants, antiplatelet agents, fibrinolytics, ethanol, side effects of mineralocorticoids, corticosteroids, estrogens; antihypertensive and diuretics.
Co-administration with other NSAIDs, corticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, to an increase in the risk of developing renal dysfunction.
Concomitant administration with oral anticoagulants, heparin, thrombolytics, antiplatelet agents, cefoperazone, cefamandol and cefotetan increases the risk of bleeding.
Increases the hypoglycemic effect of insulin and oral hypoglycemic drugs (dose recalculation is required).
Co-administration with sodium valproate causes impaired platelet aggregation.
Increases plasma concentration of verapamil and nifedipine, lithium, methotrexate.
Antacids and cholestyramine reduce absorption.
Method of administration and dosage
Inside, parenteral, rectally, externally.
Inside the drug is prescribed for 1 caps. a day during or after meals. The duration of treatment can be 3-4 months.
V / m or i / v 1 amp. per day. The maximum daily dose is 1 amp. 2 times a day. Intravenous administration of the drug is allowed only in a hospital. The drug is used for short-term treatment - up to 3 days. If further use of the drug is necessary, it is recommended to switch to taking oral dosage forms or suppositories. In elderly patients, use no more than 1 amp. per day.
Ampoules should be opened along a special fracture line. After opening the ampoule, use the solution immediately.
Aqueous solutions of ketoprofen lysine salt can be used in physiotherapeutic treatment (iontophoresis, mesotherapy); with iontophoresis, the solution is applied to the negative pole.
When used intravenously, a slow intravenous infusion is recommended to increase the duration of the drug's action. 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 solution of levulose, 5% aqueous solution of dextrose, Ringer's acetate solution, Ringer's lactate (Hartmann) solution, colloidal dextran solution at 0 , 9% sodium chloride solution or 5% dextrose solution. When Artrosilene is diluted in solutions of a small volume (50 ml), the drug is injected into / in bolus. In solutions of large volume (500 ml), the duration of the infusion is at least 30 minutes.
Rectally 1 supp. 2-3 times a day. The maximum daily dose is 480 mg. In elderly patients, no more than 2 suppositories should be used. per day.
Outwardly. A single dose of gel is 3-5 g (volume of a large cherry), aerosol - 1-2 g (volume of a walnut). Depending on the size of the damaged area, the drug should be applied 2-3 times a day or according to the doctor's prescription, rubbing gently until completely absorbed. In iontophoresis, the drug is applied to the negative pole. The duration of treatment without consulting a doctor should not exceed 10 days.
Overdose
Currently, no cases of an overdose of the drug Artrozilen have been reported.
Treatment: in case of overdose, monitoring of respiratory and cardiac activity is necessary. There is no specific antidote. If necessary, symptomatic therapy should be carried out. Hemodialysis is ineffective.
special instructions
Capsules, solution for i / v and i / m administration, suppositories
During treatment, it is necessary to control the picture of peripheral blood and the functional state of the liver and kidneys.
If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study.
Taking ketoprofen can mask the signs of an infectious disease.
In case of impaired renal and liver function, dose reduction and careful monitoring are necessary.
The use of ketoprofen by patients suffering from bronchial asthma can lead to an attack of bronchial asthma.
Women planning pregnancy should refrain from using the drug, because the chance of egg implantation may decrease.
Impact on the ability to drive vehicles and control mechanisms - during the period of use of the drug, one should refrain from potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.
Gel, aerosol
The drug should only be applied to intact skin. Avoid contact with eyes and mucous membranes. In order to avoid manifestations of hypersensitivity and photosensitivity, it is recommended to avoid exposure of the skin to sunlight during the course of treatment.
Terms of dispensing from pharmacies
Capsules, solution for i / v and i / m administration. On prescription.
Storage conditions of the drug Artrozilen
In a dark place, at a temperature not exceeding 25 ° C.Keep out of the reach of children.
Shelf life of the drug Artrozilen
solution for intravenous and intramuscular administration of 160 mg / 2 ml - 2 years.
rectal suppositories 160 mg - 5 years.
gel for external use 5% - 3 years.
capsules 320 mg - 3 years.
aerosol for external use 15% - 2 years.
Do not use after the expiration date printed on the package.
Synonyms for nosological groups
| ICD-10 heading | Synonyms of diseases according to ICD-10 |
|---|---|
| L40.5 Psoriasis arthropathic (M07.0-M07.3 *, M09.0 *) | Psoriatic arthritis |
| Arthropathic form of psoriasis | |
| M06.9 Rheumatoid arthritis, unspecified | Rheumatoid arthritis |
| Pain in rheumatoid arthritis | |
| Inflammation in rheumatoid arthritis | |
| Degenerative forms of rheumatoid arthritis | |
| Children's rheumatoid arthritis | |
| Exacerbation of rheumatoid arthritis | |
| Acute rheumatism | |
| Acute rheumatic arthritis | |
| Acute articular rheumatism | |
| Rheumatic arthritis | |
| Rheumatic polyarthritis | |
| Rheumatic arthritis | |
| Rheumatic polyarthritis | |
| Rheumatoid arthritis | |
| Rheumatoid arthritis | |
| Active rheumatoid arthritis | |
| Rheumatoid periarthritis | |
| Rheumatoid arthritis | |
| M07.3 Other psoriatic arthropathies (L40.5 +) | Psoriatic arthritis |
| Generalized form of psoriatic arthritis | |
| Psoriatic arthritis | |
| M10 Gout | Exacerbation of gout |
| Acute joint attack with gout | |
| Acute gouty attack | |
| Gouty attack | |
| Recurrent gout attacks | |
| Chronic gout | |
| M19.9 Osteoarthritis, unspecified | Arthrosis |
| Deforming arthrosis | |
| Arthrosis of large joints | |
| Pain syndrome in osteoarthritis | |
| Pain syndrome in osteoarthritis | |
| Deforming arthrosis | |
| Deforming osteoarthritis | |
| Deforming osteoarthritis of the joints | |
| Changes in the hand with osteoarthritis | |
| Osteoarthritis | |
| Osteoarthritis in the acute stage | |
| Osteoarthritis of large joints | |
| Post-traumatic osteoarthritis | |
| Rheumatic osteoarthritis | |
| Spondylarthrosis | |
| Chronic osteoarthritis | |
| M35.3 Polymyalgia rheumatica | Pain syndrome in rheumatic diseases |
| Muscle pain with rheumatism | |
| Extra-articular rheumatism | |
| Extra-articular rheumatic syndrome | |
| Extra-articular rheumatic diseases | |
| Extra-articular rheumatic soft tissue lesions | |
| Extra-articular forms of rheumatism | |
| Polymyalgia rheumatic | |
| Rhizomelic pseudoarthritis | |
| Soft tissue rheumatism | |
| Rheumatic soft tissue diseases | |
| Rheumatic diseases of periarticular soft tissues | |
| Rheumatic collagen diseases | |
| Rheumatic soft tissue lesions | |
| Rheumatic soft tissue injury | |
| M42 Osteochondrosis of the spine | Pain in osteochondrosis of the spine |
| Radicular syndrome with osteochondrosis | |
| Intervertebral osteochondrosis | |
| Osteochondrosis | |
| Osteocondritis of the spine | |
| Osteochondrosis with radicular syndrome | |
| Cervical osteochondrosis | |
| M45 Ankylosing spondylitis | Ankylosing spondylitis |
| Ankylosing spondylarthrosis | |
| Bechterew disease | |
| Pain syndrome in acute inflammatory diseases of the musculoskeletal system | |
| Pain syndrome in chronic inflammatory diseases of the musculoskeletal system | |
| Diseases of the spinal column | |
| Bechterew's disease | |
| Ankylosing spondylitis-Marie-Strumpell disease | |
| Marie-Strumpel disease | |
| Rheumatic spondylitis | |
| Ankylosing spondylitis | |
| M65 Synovitis and tendosynovitis | |
| Nonspecific tendosynovitis | |
| Acute tendovaginitis | |
| Tenosynovitis | |
| Tenosynovitis (tenovaginitis) | |
| Tendosynovitis | |
| Tenosynovitis (tenosynovitis) | |
| Tenosynovitis | |
| M71 Other bursopathies | Bursitis |
| Bursopathy | |
| Inflammatory soft tissue disease | |
| Diseases of soft tissues | |
| Edema syndrome in muscular-articular diseases | |
| Subacute bursitis | |
| M77.9 Enthesopathy, unspecified | Capsulitis |
| Periarthritis | |
| Periarthropathy | |
| Tendinitis | |
| Tendopathy | |
| M79.0 Rheumatism, unspecified | Degenerative rheumatic disease |
| Degenerative and rheumatic tendon diseases | |
| Degenerative rheumatic diseases | |
| Localized forms of soft tissue rheumatism | |
| Rheumatism | |
| Rheumatism with a pronounced allergic component | |
| Articular and extra-articular rheumatism | |
| Rheumatic attack | |
| Rheumatic complaints | |
| Rheumatic diseases | |
| Rheumatic diseases of the intervertebral disc | |
| Rheumatic disease | |
| Rheumatic spine disease | |
| Rheumatoid diseases | |
| Relapses of rheumatism | |
| Articular and extra-articular rheumatism | |
| Articular and muscular rheumatism | |
| Articular rheumatism | |
| Articular syndrome in rheumatism | |
| Chronic rheumatic pain | |
| Chronic articular rheumatism | |
| M79.1 Myalgia | Pain syndrome in musculoskeletal diseases |
| Pain syndrome in chronic inflammatory diseases of the musculoskeletal system | |
| Pain in the muscles | |
| Muscle soreness | |
| Muscle soreness during heavy physical exertion | |
| Painful conditions of the musculoskeletal system | |
| Pain in the musculoskeletal system | |
| Muscle pain | |
| Resting pain | |
| Muscle aches | |
| Muscle pain | |
| Musculoskeletal pain | |
| Myalgia | |
| Myofascial pain syndromes | |
| Muscle pain | |
| Muscle pain at rest | |
| Muscle pain | |
| Muscle pains of non-rheumatic origin | |
| Muscle pains of rheumatic origin | |
| Acute muscle pain | |
| Rheumatic pain | |
| Rheumatic pain | |
| Myofascial syndrome | |
| Fibromyalgia | |
| M79.9 Disease of soft tissue, unspecified | Localized forms of soft tissue inflammation |
| R52.0 Acute pain | Acute pain syndrome |
| Acute pain syndrome in osteoarthritis | |
| Severe neurogenic pain | |
| Severe pain | |
| Pain syndrome during childbirth | |
| R52.2 Other persistent pain | Pain syndrome of non-rheumatic origin |
| Pain syndrome with vertebral lesions | |
| Pain syndrome with neuralgia | |
| Pain syndrome with burns | |
| Pain syndrome is mild or moderate | |
| Neuropathic pain | |
| Neuropathic pain | |
| Perioperative pain | |
| Moderate to severe pain | |
| Moderate or mild pain syndrome | |
| Moderate to severe pain syndrome | |
| Ear pain with otitis media | |
| T14.3 Dislocation, sprain and injury of the capsular-ligamentous apparatus of the joint of an unspecified region of the body | Painful muscle sprains |
| Pain and inflammation when stretching | |
| Reduction of dislocation | |
| Degenerative changes in the ligamentous apparatus | |
| Swelling due to sprains and bruises | |
| Edema after interventions for dislocations | |
| Ligament damage and rupture | |
| Damage to the musculo-ligamentous apparatus | |
| Ligament damage | |
| Joint damage | |
| Habitual stretching and tearing | |
| Ligament rupture | |
| Ligament tears | |
| Tendon ruptures | |
| Muscle tendon ruptures | |
| Joint injuries | |
| Stretching | |
| Crick | |
| Muscle strain | |
| Sprain | |
| Ligamentous apparatus stretching | |
| Stretching the tendons | |
| Stretching | |
| Muscle sprains | |
| Sprains | |
| Ligamentous apparatus sprains | |
| Tendon sprains | |
| Musculo-ligamentous apparatus injury | |
| Joint injuries | |
| Capsule-articular tissue injuries | |
| Musculoskeletal system injuries | |
| Ligament injuries | |
| Joint injuries | |
| T14.9Injury, unspecified | Pain syndrome after trauma |
| Pain syndrome in trauma | |
| Pain syndrome in trauma and after surgery | |
| Injury pain | |
| Traumatic pain | |
| Joint pain due to injury | |
| Postoperative and post-traumatic pain | |
| Pain in trauma | |
| Pain of traumatic origin | |
| Severe pain syndrome of traumatic origin | |
| Deep tissue damage | |
| Deep scratches on the torso | |
| Closed injury | |
| Minor household injuries | |
| Minor skin lesions | |
| Violations of the integrity of soft tissues | |
| Uncomplicated injuries | |
| Extensive traumatic injury | |
| Acute pain syndrome of traumatic origin | |
| Swelling with injuries | |
| Past sports injuries | |
| Post-traumatic pain | |
| Soft tissue injuries | |
| Joint injuries | |
| Sports injuries | |
| Injury | |
| Traumatic pain | |
| Traumatic pain | |
| Traumatic infiltration | |
| Sports injuries | |
| Z100 * CLASS XXII Surgical Practice | Abdominal surgery |
| Adenomectomy | |
| Amputation | |
| Angioplasty of the coronary arteries | |
| Angioplasty of the carotid arteries | |
| Antiseptic skin treatment for wounds | |
| Antiseptic hand treatment | |
| Appendectomy | |
| Atheroectomy | |
| Balloon coronary angioplasty | |
| Vaginal hysterectomy | |
| Coronal bypass | |
| Interventions on the vagina and cervix | |
| Bladder interventions | |
| Intervention in the oral cavity | |
| Reconstructive surgery | |
| Hand hygiene of medical personnel | |
| Gynecological surgery | |
| Gynecological interventions | |
| Gynecological operations | |
| Hypovolemic shock during operations | |
| Disinfection of purulent wounds | |
| Disinfection of wound edges | |
| Diagnostic interventions | |
| Diagnostic procedures | |
| Diathermocoagulation of the cervix | |
| Long-term surgical operations | |
| Replacing fistula catheters | |
| Orthopedic Surgical Infection | |
| Artificial heart valve | |
| Cystectomy | |
| Short-term outpatient surgery | |
| Short-term operations | |
| Short-term surgical procedures | |
| Cricothyrotomy | |
| Blood loss during surgery | |
| Bleeding during surgery and in the postoperative period | |
| Culdocentesis | |
| Laser coagulation | |
| Laser coagulation | |
| Retinal laser coagulation | |
| Laparoscopy | |
| Laparoscopy in gynecology | |
| CSF fistula | |
| Small gynecological operations | |
| Minor surgical interventions | |
| Mastectomy and subsequent plasty | |
| Mediastinotomy | |
| Microsurgery on the ear | |
| Mucogingival operations | |
| Suture | |
| Minor surgical interventions | |
| Neurosurgery | |
| Immobilization of the eyeball in ophthalmic surgery | |
| Orchiectomy | |
| Complications after tooth extraction | |
| Pancreatectomy | |
| Pericardiectomy | |
| Rehabilitation period after surgery | |
| The period of convalescence after surgery | |
| Percutaneous transluminal coronary angioplasty | |
| Pleural thoracocentesis | |
| Postoperative and post-traumatic pneumonia | |
| Preparing for surgical procedures | |
| Preparing for surgery | |
| Preparing the surgeon's hands before surgery | |
| Colon preparation for surgery | |
| Postoperative aspiration pneumonia in neurosurgical and thoracic operations | |
| Postoperative nausea | |
| Postoperative bleeding | |
| Postoperative granuloma | |
| Postoperative shock | |
| Early postoperative period | |
| Myocardial revascularization | |
| Root apex resection | |
| Stomach resection | |
| Bowel resection | |
| Uterus resection | |
| Liver resection | |
| Small bowel resection | |
| Resection of part of the stomach | |
| Reocclusion of the operated vessel | |
| Bonding of tissues during surgical procedures | |
| Removing stitches | |
| Condition after eye surgery | |
| Condition after surgery | |
| Condition after surgery in the nasal cavity | |
| Condition after gastric resection | |
| Condition after resection of the small intestine | |
| Condition after tonsillectomy | |
| Condition after removal of the duodenum | |
| Condition after phlebectomy | |
| Vascular surgery | |
| Splenectomy | |
| Sterilization of surgical instruments | |
| Sterilization of surgical instruments | |
| Sternotomy | |
| Dental operations | |
| Dental intervention on periodontal tissues | |
| Strumectomy | |
| Tonsillectomy | |
| Thoracic surgery | |
| Thoracic surgery | |
| Total gastrectomy | |
| Transdermal intravascular coronary angioplasty | |
| Transurethral resection | |
| Turbinectomy | |
| Removal of a tooth | |
| Removal of cataracts | |
| Removal of cysts | |
| Removal of tonsils | |
| Removal of fibroids | |
| Removal of movable milk teeth | |
| Removal of polyps | |
| Removing a broken tooth | |
| Removal of the body of the uterus | |
| Removing stitches | |
| Urethrotomy | |
| Fistula of the cerebrospinal fluid | |
| Frontal ethmoidogaymorotomy | |
| Surgical infection | |
| Surgical treatment of chronic limb ulcers | |
| Surgery | |
| Anal surgery | |
| Colon surgery | |
| Surgical practice | |
| Surgical procedure | |
| Surgical interventions | |
| Surgical interventions on the gastrointestinal tract | |
| Surgical interventions on the urinary tract | |
| Surgical interventions on the urinary system | |
| Surgical interventions on the genitourinary system | |
| Heart surgery | |
| Surgical manipulations | |
| Surgical operations | |
| Vein surgery | |
| Surgical intervention | |
| Surgical intervention on the vessels | |
| Surgical treatment of thrombosis | |
| Surgery | |
| Cholecystectomy | |
| Partial gastric resection | |
| Transperitoneal hysterectomy | |
| Percutaneous transluminal coronary angioplasty | |
| Percutaneous transluminal angioplasty | |
| Coronary artery bypass surgery | |
| Tooth extirpation | |
| Extirpation of milk teeth | |
| Pulp extirpation | |
| Extracorporeal circulation | |
| Tooth extraction | |
| Extraction of teeth | |
| Extraction of cataract | |
| Electrocoagulation | |
| Endourological interventions | |
| Episiotomy | |
| Ethmoidotomy |
3416 0
The drug Artrozilen, which contains the main active ingredient Ketoprofen, is widely used in inflammatory processes of the periarticular tissues, accompanied by increased pain.
Arthrosilene is produced in various forms:
- capsules for oral administration;
- injections for intramuscular and intravenous injections;
- gel for external use;
- aerosol applied externally;
- suppository for rectal use.
pharmachologic effect
Being a non-steroidal anti-inflammatory drug, Artrozilen stops chronic inflammatory processes, inhibiting the activity of enzymes that destroy tissues, inhibits the synthesis of prostaglandins, inhibits COX-1 and COX-2.
Having a slight negative effect on the gastrointestinal tract, the drug gives a good therapeutic result, acts as an analgesic, has an antipyretic effect.
Thanks to the effect of the drug, patients gain the ability to develop the necessary volumes of movement, stiffness disappears after a period of rest, tissue edema decreases. When administered orally, the maximum effect is observed after 4 hours.
The action of external drugs is analgesic, decongestant, they are used as anti-inflammatory for lesions of joints and soft tissues: muscles, tendons, ligaments.
Pharmacokinetics of the drug
Assimilation of the oral form, the drug in capsules gives the maximum effect after 4 hours, the persistence of the result depends on the dose of the drug taken, the bioavailability exceeds 80%, when administered parenterally, the maximum concentration in the synovial fluid appears after one hour, and the therapeutic effect lasts longer than when using others forms, up to 24 hours.
When used rectally, the degree of absorption of the drug and the manifestation of the therapeutic effect are also high, and when used externally, the drug is absorbed slowly, the bioavailability is 5%.
By binding to plasma proteins, the active substance ketoprofen is well distributed in organs and tissues, in the synovial fluid, in the connective tissue. The drug metabolism occurs in the liver. Metabolic products are excreted by the kidneys during the day.
Indications for use
Depending on the form, Artrozilene is used in such cases: 
- Used internally capsules and suppositories used as analgesics in postoperative conditions, with pain due to overload or, with moderate pain, indicating the presence of inflammation in the periarticular tissues. Drugs are prescribed for various types of inflammation.
- Solutions for injection are used to relieve acute pain syndrome and postoperative pain, with inflammation of the periarticular tissues of various origins.
- Gels and aerosols more often used for soft tissue lesions and injuries; with osteoarthritis of the spine, with muscle pain of a non-rheumatic nature.
Contraindications for admission
Contraindications for taking any form of the drug are:
- individual intolerance to the active substance, hypersensitivity to it or to other non-steroidal anti-inflammatory drugs;
- aspirin asthma;
- peptic ulcer and ulcerative colitis, Crohn's disease;
- diverticulitis;
- hemophilia and other blood clotting disorders;
- chronic renal failure;
- lactation period.
Children's age is a contraindication for the use of the drug in all forms, except for gel and aerosols.
During pregnancy, the drug is prescribed with caution only as an external agent in the third period of pregnancy.
Mechanism of action
The active substance of the drug ketoprofen in a content of 99% penetrates the blood plasma, binding with albumin and distributed in tissues, inhibiting the synthesis of prostaglandins and inhibiting COX-1 and COX-2, inhibiting the activity of pathogenic enzymes.
How to use the medicine?
Depending on the form of release, the instructions for use for Artrosilene are also different.
The drug is produced:
Learn more about dosages
The use of Artrozilen orally with or after meals for 3 or 4 months, one capsule per day.
Intravenous or intramuscularly in a slow mode of administration, intravenously 500 ml for 30 minutes, one ampoule no more than twice a day for 3 days.
Injections are carried out in a hospital. The prepared solutions should be used immediately.
1 suppository is used rectally 2-3 times a day, the maximum dose per day is no more than 480 mg.
Outwardly, the drug is used in an amount corresponding to the area of \u200b\u200bthe painful surface, but not more than 5 g in one application when using a gel and not more than 2 g when using an aerosol, this is the size of a pea and the volume of a teaspoon, respectively, for a course of no more than 10 days.
In case of overdose
If there is a suspicion of exceeding the permissible dose of the drug, monitoring of respiratory and cardiac activity should be carried out, in case of violations, symptomatic therapy should be carried out.
Side effects
The side effects that occur when taking the drug can be characterized by the following changes:
- the digestive system suffers from ulcerative disorders, the patient feels abdominal pain, diarrhea;
- the hematopoietic system reacts with an increase in the level of bilirubin and an increase in the activity of liver enzymes, the liver is larger than normal;
- the nervous system reacts with general malaise, involuntary tremors, anxiety;
- lacrimation, vision problems may occur;
- various types of skin allergies;
- cystitis, hematuria. failure of the menstrual cycle;
- bronchospasm, laryngeal spasm, rhinitis;
- tachycardia, edema, hyper- and hypotension.
- allergic reactions: anaphylactoid reactions, edema of the oral mucosa, pharyngeal edema, periorbital edema.
Allergic reactions to suppositories can appear several hours after the administration of the drug: itching, burning, feeling of heaviness, hemorrhoids and its aggravation.
If, against the background of taking the drug, the patient's condition worsened or the above symptoms appear, it is necessary to urgently consult a doctor.
special instructions
When applied externally, skin dermatoses and eczema can also occur. With bronchial asthma, the drug is prescribed with caution, as well as in old age.
Capsules and solutions are not used for anemia, diabetes mellitus, sepsis, edema, high blood pressure, stomatitis, children under 12 years of age.
Capsules, dissolving for administration and suppositories are contraindicated in alcoholism.
In case of severe violations of the liver and kidneys, the drug is not prescribed.
Drugs taken internally during lactation are contraindicated. Also contraindicated in the third period of pregnancy.
Gels and aerosols are used in the first and second stages of pregnancy if necessary under the supervision of a physician.
Internal drugs are not prescribed to persons under 18 years of age. Gels and aerosols are used after the patient reaches 12 years of age.
Interaction with other drugs
Barbiturates and tricyclic antidepressants increase the activity of ketoprofen.
The effect of anticoagulants increases, the effect of diuretics decreases, and the side effects of glucocorticoids increase.
Simultaneous administration with other anticoagulants increases the risk of bleeding.
Enhances the action of insulin, the dose must be calculated differently. Affects platelet production.
We will study a qualified opinion
Testimonial from a doctor who uses Artrosilene in his practice.
When prescribing a drug, we carefully study the patient's medical history. we monitor whether he has diseases of the hematopoietic organs and others.
The drug works flawlessly and has already helped hundreds of sick people. The course of taking capsules lasts up to 4 months. Injections cannot be taken for a long time.
Orthopedic clinic doctor, V.P. Khanaev
P N010596 / 05Release form, composition and packaging
Capsules hard gelatinous, oblong, body - white, cap - dark green; the contents of the capsules are round, light yellow granules.Excipients:diethyl phthalate - 2.286 mg, carboxypolymethylene - 32.857 mg, magnesium stearate - 15.857 mg, povidone - 27.857 mg, polymers of acrylic and methacrylic acids - 34.143 mg, talc - 27 mg.
Capsule shell composition:body - titanium dioxide (E171), qsp gelatin; lid - quinoline yellow (E104), indigotine (E132), titanium dioxide (E171), gelatin qsp. 10 pieces. - blisters (1) - cardboard packs.
pharmachologic effect
NSAIDs. It has anti-inflammatory, analgesic and antipyretic effects. By inhibiting COX-1 and COX-2, it inhibits the synthesis of prostaglandins. It has anti-bradykinin activity, stabilizes lysosomal membranes and delays the release of enzymes from them that contribute to tissue destruction in chronic inflammation. Reduces the release of cytokines, inhibits the activity of neutrophils.Reduces morning stiffness and swelling of joints, increases range of motion.
Ketoprofen lysine salt, unlike ketoprofen, is a rapidly dissolving compound with a neutral pH, due to which it almost does not irritate the gastrointestinal tract.
After oral administration, the maximum therapeutic effect is observed for 4 to 24 hours.
Pharmacokinetics
Suction
After oral administration, ketoprofen is sufficiently completely absorbed from the gastrointestinal tract, the bioavailability exceeds 80%. C max is 3-9 μg / ml and is achieved 4-10 hours after ingestion, its value directly depends on the dose taken. Simultaneous food intake contributes to a decrease in C max and an increase in T max, without changing the AUC.
Distribution
Up to 99% of ketoprofen binds to plasma proteins, mainly albumin. V d -0.1-0.2 l / kg. Easily penetrates the histohematogenous 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).
The drug practically does not accumulate in the body.
Metabolism
Ketoprofen is mainly metabolized in the liver, where it undergoes glucuronidation to form esters with glucuronic acid.
Withdrawal
T 1/2 is 6.5 hours. Metabolites are excreted mainly in the urine. Less than 1% is excreted in the feces.
Indications:
Relief of pain of mild to moderate intensity, including:Postoperative pain;
- post-traumatic pain;
- inflammatory pains.
Symptomatic treatment of rheumatic and inflammatory diseases, incl .:
Rheumatoid arthritis;
- spondyloarthritis;
- osteoarthritis;
- gouty arthritis;
- inflammatory damage to the periarticular tissues.
Dosage regimen
The drug is taken orally 1 capsule / day, during or after meals. The duration of treatment can be 3-4 months.Side effect
From the digestive system:abdominal pain, diarrhea, duodenitis, erosive and ulcerative lesions of the gastrointestinal tract, gastritis, hematomezis, esophagitis, stomatitis, melena, increased bilirubin levels, increased activity of liver enzymes, hepatitis, liver failure, an increase in liver size.
From the side of the central nervous system and peripheral nervous system: dizziness, hyperkinesia, tremors, vertigo, mood swings, anxiety, hallucinations, irritability, general malaise.
On the part of the organ of vision: conjunctivitis, visual impairment.
From the hematopoietic system:leukocytopenia, leukocytosis, lymphangitis, decreased prothrombin time, thrombocytopenia, thrombocytopenic purpura, enlarged spleen, vasculitis.
From the respiratory system: bronchospasm, dyspnea, laryngeal spasm sensation, laryngospasm, laryngeal edema, rhinitis.
On the part of the cardiovascular system: hypertension, hypotension, tachycardia, chest pain, syncope.
From the urinary system: painful urination, cystitis, edema, hematuria.
On the part of the skin and subcutaneous tissues: erythematous exanthema, itching, maculo-papular rash, increased sweating.
Allergic reactions: urticaria, angioedema, exudative erythema multiforme (including Stevens-Johnson syndrome), anaphylactoid reactions (edema of the oral mucosa, pharyngeal edema, periorbital edema).
Others: peripheral edema, pallor, menstrual irregularities.
Contraindications:
For systemic use- "aspirin" asthma;
- peptic ulcer of the stomach and duodenum in the acute phase;
- ulcerative colitis in the acute phase;
- Crohn's disease;
- diverticulitis;
- peptic ulcer;
- blood clotting disorders (including hemophilia);
- chronic renal failure;
- children and adolescents up to 18 years old;
- III trimester of pregnancy;
- lactation period;
- hypersensitivity to drug components or other HPBCs.
Carefully the drug should be prescribed for anemia, bronchial asthma, alcoholism, tobacco smoking, alcoholic cirrhosis of the liver, hyperbilirubinemia, liver failure, diabetes mellitus, dehydration, sepsis, chronic heart failure, edema, arterial hypertension, blood diseases (including leukopenia), deficiency glucose-6-phosphate dehydrogenase, stomatitis, in the first and second trimesters of pregnancy, as well as in elderly patients.
Pregnancy and lactation
Like other HPBCs, Artrosilene should not be used in the third trimester of pregnancy. In the I and II trimesters of pregnancy, the drug Artrozilen should be used with caution and under medical supervision.If necessary, the use of the drug during lactation, breastfeeding should be discontinued.
Women planning a pregnancy should refrain from taking Artrozilen, because against the background of its administration, the likelihood of egg implantation may decrease.
special instructions
During treatment with Artrozilen, it is necessary to periodically monitor the picture of peripheral blood and the functional state of the liver and kidneys.If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study.
Taking Artrosilene can mask the signs of an infectious disease.
In case of impaired liver and kidney function, dose reduction and careful monitoring are necessary.
The use of Artrosilene in bronchial asthma can provoke an attack of suffocation.
Overdose
Currently, no cases of overdose with Artrozilen have been reported.Treatment:in case of overdose, if necessary, symptomatic therapy, monitoring of respiratory and cardiovascular activity should be carried out. There is no specific antidote. Hemodialysis is ineffective.
Drug interactions
Inducers of microsomal oxidation in the liver (including phenytoin, ethanol, barbiturates, flumecinol, rifampicin, phenylbutazone, tricyclic antidepressants), when used simultaneously with Artrozilen, increase the production of hydroxylated active metabolites.Against the background of simultaneous use with Artrozilen, the effectiveness of uricosuric drugs decreases, the effect of anticoagulants, antiplatelet agents, fibrinolytics, ethanol, side effects of mineralocorticoids, glucocorticoids, estrogens increases; the effectiveness of antihypertensive drugs and diuretics decreases.
The simultaneous use of the drug Artrozilen with other NSAIDs, GCS, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, to an increase in the risk of developing renal dysfunction.
The simultaneous appointment of Artrozilen with oral anticoagulants, heparin, thrombolytics, antiplatelet agents, cefoperazone, cefamandol and cefotetan increases the risk of bleeding.
The drug Artrozilen, when used simultaneously, enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs (dose recalculation is required).
The combined use of Artrosilene with sodium valproate causes a violation of platelet aggregation.
Ketoprofen, with simultaneous use, increases the plasma concentration of verapamil and nifedipine, lithium, methotrexate.
Antacids and cholestyramine reduce the absorption of ketoprofen.
Storage conditions and periods
The drug should be stored in a dry place out of the reach of children at a temperature not exceeding 25 ° C.The shelf life is 3 years.
Terms of dispensing from pharmacies:
The drug is available by prescription.
Manufacturer
registered
DOMPE FARMACEUTICI S.p.A. (Italy)
produced
Valpharma S.A. (Republic of San Marino) or ISTITUTO de ANGELI S.r.L. (Italy)