Artrosilene rectal suppositories. When is the drug prescribed? Non-steroidal anti-inflammatory drugs

When applied externally Artrosilene gel provides a local therapeutic effect in the affected joints, tendons, ligaments, muscles. With articular syndrome, it reduces pain in the joints at rest and during movement, morning stiffness and swelling of the joints.

Ketoprofen does not have a catabolic effect on articular cartilage.

Pharmacokinetics
When applied externally, 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. The bioavailability of the drug is about 5%.

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.

Exposure to sunlight, even on cloudy days, as well as visits to the solarium are contraindicated during treatment and within 2 weeks after the last use of the drug.

Carefully the drug should be prescribed for exacerbation of hepatic porphyria, erosive and ulcerative lesions of the gastrointestinal tract, severe violations of the liver and kidneys, chronic heart failure, bronchial asthma, in the I and II trimesters of pregnancy, as well as children aged 6 to 12 years and elderly patients.

The use of the drug during lactation is not recommended.

Avoid contact with eyes and mucous membranes.

In order to avoid manifestations of hypersensitivity and photosensitivity, it is recommended to avoid exposure of the treated skin to sunlight during treatment and for 2 weeks after the end of therapy.

After using the drug, wash your hands thoroughly.

An occlusive dressing should not be used.

You should immediately stop using the drug in case of any skin reaction while using sunscreens or other cosmetics containing octocrylene.

Influence on the ability to drive vehicles and control mechanisms

There is no evidence of a negative effect of the drug on the ability to drive vehicles and engage in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

In case of accidental ingestion of large amounts of the drug (more than 20 g), systemic adverse reactions characteristic of NSAIDs may occur.

Treatment: gastric lavage, activated charcoal.

Although interaction with other drugs for topical and systemic use is unlikely, in the case of prolonged treatment or treatment with the drug in high doses, the possibility of competition for binding to plasma proteins between absorbed ketoprofen and other drugs must be taken into account.

Patients taking coumarin anticoagulants are advised to regularly monitor INR.

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.

The composition of the capsule shell: body - titanium dioxide (E171), gelatin qsp; cap - quinoline yellow (E104), indigotine (E132), titanium dioxide (E171), gelatin qsp. 10 pieces. - blisters (1) - packs of cardboard.

Reduces morning stiffness and swelling of the joints, increases range of motion.

Ketoprofen lysine salt, unlike ketoprofen, is an instant 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 quite completely absorbed from the gastrointestinal tract, 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 Cmax and an increase in Tmax, without changing AUC.

Distribution
Up to 99% of ketoprofen binds to plasma proteins, mainly to albumin. V d -0.1-0.2 l / kg. Easily penetrates through histohematic barriers and is distributed in tissues and organs. Ketoprofen penetrates well into the 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 primarily metabolized in the liver, where it undergoes glucuronidation to form esters with glucuronic acid.

breeding
T 1/2 is 6.5 hours. Metabolites are excreted mainly in the urine. Less than 1% is excreted with feces.

Postoperative pain;
- post-traumatic pain;
- inflammatory pains.

Symptomatic treatment of rheumatic and inflammatory diseases, including:

Rheumatoid arthritis;
- spondyloarthritis;
- osteoarthritis;
- gouty arthritis;
- inflammation of the periarticular tissues.

- "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;
- III trimester of pregnancy;
- lactation period;
- Hypersensitivity to the components of the drug or other HPBC.

Carefully the drug should be prescribed for anemia, bronchial asthma, alcoholism, 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 I and II trimesters of pregnancy, as well as in elderly patients.

If necessary, the use of the drug during lactation, breastfeeding should be discontinued.

Women planning a pregnancy should refrain from taking the drug Artrosilene, because. against the background of its reception, the probability of egg implantation may decrease.

If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study.

Taking Artrozilene may mask signs of an infectious disease.

In case of impaired liver and kidney function, dose reduction and careful monitoring are necessary.

The use of Artrozilene in bronchial asthma can provoke an asthma attack.

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.

Against the background of simultaneous use with the drug Artrozilene, the effectiveness of uricosuric drugs decreases, the effect of anticoagulants, antiplatelet agents, fibrinolytics, ethanol increases, side effects of mineralocorticoids, glucocorticoids, estrogens; the effectiveness of antihypertensive drugs and diuretics decreases.

Simultaneous use of the drug Artrozilene with other NSAIDs, corticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, to an increased risk of developing impaired renal function.

The simultaneous appointment of Artrozilene with oral anticoagulants, heparin, thrombolytics, antiplatelet agents, cefoperazone, cefamandol and cefotetan increases the risk of bleeding.

The drug Artrozilen, with simultaneous use, enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs (dose recalculation is necessary).

The combined use of Artrozilene 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.

Preparation: ARTROSILEN
Active ingredient: ketoprofen
ATX code: M02AA10
KFG: NSAIDs for external use
ICD-10 codes (indications): M05, M07, M10, M15, M42, M45, M46, M65, M70, M71, M79, M79.1, R52.0, R52.2, T14.3
KFU code: 05.01.01.06
Reg. number: P No. 010596/02
Date of registration: 28.10.05
The owner of the reg. acc.: DOMPE FARMACEUTICI S.p.A. (Italy)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Capsules hard gelatinous, oblong, with a white body and a dark green cap; the contents of the capsules are round granules of light yellow color.

Excipients: diethyl phthalate, carboxypolymethylene, magnesium stearate, povidone, acrylic acid polymer, methacrylic acid polymer, talc.

The composition of the capsule body: titanium dioxide (E171), gelatin.
Cap Compositioncapsules: quinoline yellow (E104), indigotine (E132), titanium dioxide (E171), gelatin.

10 pieces. - blisters (1) - packs of cardboard.

Solution for intravenous and intramuscular administration transparent, colorless or slightly yellowish.

Excipients: sodium hydroxide, citric acid, water for injections.

2 ml - dark glass ampoules (6) - plastic pallets (1) - cardboard packs.

Suppositories rectal homogeneous, from white to light yellow, torpedo-shaped.

Excipients: semi-synthetic glycerides.

5 pieces. - strips (2) - packs of cardboard.

Aerosol for external use 15% in the form of a white homogeneous foam; after the release of gas - a transparent liquid of pale yellow color.

Excipients: polysorbate 80, polypropylene glycol, polyvinylpyrrolidone (povidone), nerolene lavender flavor, benzyl alcohol, purified water, a mixture of propane and butane.

Cylinders with a capacity of 25 ml (1) with a spray nozzle - packs of cardboard.

Gel for external use 5% transparent, thick, with the smell of lavender.

Excipients: carboxypolymethylene, triethanolamine, polysorbate, ethanol 95%, methyl parahydroxybenzoate, lavender flavor nerolene, water.

30 g - aluminum tubes (1) - packs of cardboard.
50 g - aluminum tubes (1) - packs of cardboard.

ARTROSILEN INSTRUCTION FOR A SPECIALIST.
The description of the drug ARTROSILEN is approved by the manufacturer for the printed edition in 2008.

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 during chronic inflammation. Reduces the release of cytokines, inhibits the activity of neutrophils.

Reduces morning stiffness and swelling of the joints, increases range of motion.

Ketoprofen lysine salt, unlike ketoprofen, is an instant 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.

When applied externally, Artrosilene reduces the manifestations of inflammation and pain in the affected joints, tendons, ligaments, muscles. With articular syndrome, it causes a weakening of pain in the joints at rest and during movement, a decrease in morning stiffness and swelling of the joints.

Ketoprofen lysine salt does not have a catabolic effect on articular cartilage.

PHARMACOKINETICS

Suction

After oral administration of capsules, ketoprofen is rapidly and fairly completely absorbed from the gastrointestinal tract, bioavailability exceeds 80%. C max is 3-9 μg / ml and is achieved after 4-10 hours, 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 AUC.

After rectal administration, ketoprofen is also rapidly absorbed. The time to reach Cmax after rectal application is 45-60 minutes. The plasma concentration is linearly dependent on the dose taken.

The time to reach C max with parenteral administration is 45-60 minutes. The effective concentration lasts 24 hours. Therapeutic concentration in the synovial fluid lasts 18-20 hours.

With cutaneous application, 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. The bioavailability of the drug is about 5%.

Distribution

Up to 99% of ketoprofen binds to plasma proteins, mainly to albumin. V d - 0.1-0.2 l / kg. Easily penetrates through histohematic barriers and is distributed in tissues and organs. Ketoprofen penetrates well into the synovial fluid and connective tissue. Although the concentration of ketoprofen in synovial fluid is slightly lower than in plasma, it is more stable (lasts up to 30 hours).

Metabolism

Ketoprofen is primarily metabolized in the liver, where it undergoes glucuronidation to form esters with glucuronic acid.

breeding

T 1/2 is 6.5 hours. Metabolites are excreted mainly in the urine (up to 76% within 24 hours). Less than 1% is excreted with feces. The drug practically does not accumulate in the body.

INDICATIONS

For oral and rectal use

Pain relief of mild to moderate intensity, including:

Postoperative pain;

Post-traumatic pain;

Inflammatory pains.

Symptomatic treatment of rheumatic and inflammatory diseases, including:

Rheumatoid arthritis;

Spondyloarthritis;

Osteoarthritis;

gouty arthritis;

Inflammatory damage to the periarticular tissues.

For parenteral use

Short-term treatment of acute pain syndrome:

In diseases of the musculoskeletal system of various origins;

In the postoperative period;

After injuries and in inflammatory processes.

For outdoor use

Acute and chronic inflammatory diseases of the musculoskeletal system (including rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, osteoarthritis of the peripheral joints and spine, rheumatic soft tissue lesions);

Muscular pain of rheumatic and non-rheumatic origin;

Traumatic injuries of soft tissues.

DOSING MODE

inside Artrosilene is prescribed 1 caps./day, during or after meals. The duration of treatment can be 3-4 months.

Rectally appoint 1 suppository 2-3 times / day. The maximum daily dose is 480 mg. Elderly patients do not prescribe more than 2 suppositories per day.

At dysfunction of the kidneys and liver dose reduction is necessary.

Parenterally(in / m or in / in) the drug is prescribed at a dose of 160 mg (1 amp.) / day. The maximum daily dose is 320 mg (1 amp. 2 times / day).

Elderly patientsage no more than 1 amp./day should be prescribed.

Parenterally, the drug should be administered for a short time (up to 3 days), then they switch to taking the drug orally or to the use of suppositories.

In / in the introduction of the drug is allowed only in the hospital. To increase the time of action of the drug, a slow intravenous infusion is recommended. The duration of the IV infusion is at least 30 minutes.

The solution for infusion is prepared on the basis of 50 ml 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 Hartman's solution, colloidal solution of dextran in 0.9% sodium solution chloride or 5% dextrose solution.

When diluting Artrozilene in solutions of a small volume (50 ml), the drug is administered intravenously as a bolus.

At outdoor application a single dose of gel is 3-5 g (the volume of a large cherry), an aerosol - 1-2 g (the volume of a walnut). The drug should be applied 2-3 times / day, gently rubbing until completely absorbed. The duration of treatment should not exceed 10 days (without consulting a doctor).

SIDE EFFECT

From the digestive system: abdominal pain, diarrhea, stomatitis, esophagitis, gastritis, duodenitis, erosive and ulcerative lesions of the gastrointestinal tract, hematomesis, melena, increased bilirubin levels, increased liver enzymes, hepatitis, liver failure, liver enlargement.

From the side of the central nervous system and peripheral nervous system: dizziness, hyperkinesia, tremor, vertigo, mood swings, anxiety, hallucinations, irritability, general malaise, visual impairment.

Allergic reactions: urticaria, angioedema, erythema multiforme exudative (including Stevens-Johnson syndrome), anaphylactoid reactions (edema of the oral mucosa, pharyngeal edema, periorbital edema).

Dermatological reactions: erythematous exanthema, itching, maculo-papular rash.

From the urinary system: painful urination, cystitis, edema, hematuria.

From the hematopoietic system: leukocytopenia, leukocytosis, lymphangitis, decreased prothrombin time, thrombocytopenia, thrombocytopenic purpura, enlarged spleen, vasculitis.

From the respiratory system: bronchospasm, dyspnea, sensation of spasm of the larynx, laryngospasm, laryngeal edema, rhinitis.

From the side of the cardiovascular system: hypertension, hypotension, tachycardia, chest pain, syncope, peripheral edema, pallor.

Others: conjunctivitis, menstrual irregularities, increased sweating.

Local reactions with rectal application: burning, itching, heaviness in the anorectal region, exacerbation of hemorrhoids.

Local reactions with external use: skin manifestations of allergic reactions, photosensitivity. With prolonged use on large surfaces of the skin, systemic side effects may develop.

Ketoprofen lysine salt is much less likely to cause side effects compared to ketoprofen.

CONTRAINDICATIONS

- "aspirin triad";

III trimester of pregnancy;

lactation period;

Hypersensitivity to ketoprofen or other components of the drug, acetylsalicylic acid or other NSAIDs.

For systemic use

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 of age.

For outdoor use

Weeping dermatoses;

Violation of the integrity of the skin;

Children's age up to 6 years.

FROM caution the drug should be prescribed in the I and II trimesters of pregnancy, as well as in elderly patients. At systemic use caution should be exercised in case of anemia, bronchial asthma, alcoholism, 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; at outdoor application- with exacerbation of hepatic porphyria, erosive and ulcerative lesions of the gastrointestinal tract, severe violations of the liver and kidneys, chronic heart failure, bronchial asthma, as well as in children under 12 years of age.

PREGNANCY AND LACTATION

The use of the drug Artrozilen in the III trimester of pregnancy is contraindicated. In the I and II trimesters of pregnancy, Artrozilene should be used with caution and under the supervision of a physician. If necessary, the use of the drug during lactation, breastfeeding should be discontinued.

Women planning a pregnancy should refrain from taking the drug Artrosilene, because. against the background of its reception, the probability of egg implantation may decrease.

SPECIAL INSTRUCTIONS

During treatment with Artrozilene, 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 Artrozilene may mask signs of an infectious disease.

The use of Artrozilene in bronchial asthma can provoke an asthma attack.

For external use, the drug should be applied only 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.

Aqueous solutions of ketoprofen lysine salt, as well as a gel for external use, can be used in physiotherapeutic treatment (iontophoresis, mesotherapy): in iontophoresis, the drug is applied to the negative pole.

Influence 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.

OVERDOSE

Currently, cases of overdose with Artrozilene have not been reported.

In case of overdose, 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 Artrosilene, increase the metabolism of ketoprofen (increase the production of hydroxylated active metabolites).

Against the background of simultaneous use with the drug Artrozilene, the effectiveness of uricosuric drugs decreases, the effect of anticoagulants, antiplatelet agents, fibrinolytics, ethanol increases, side effects of mineralocorticoids, glucocorticoids, estrogens; the effectiveness of antihypertensive drugs and diuretics decreases.

Simultaneous use of the drug Artrozilene with other NSAIDs, corticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, to an increased risk of developing impaired renal function.

The simultaneous appointment of Artrozilene with oral anticoagulants, heparin, thrombolytics, antiplatelet agents, cefoperazone, cefamandol and cefotetan increases the risk of bleeding.

The drug Artrozilen, with simultaneous use, enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs (dose recalculation is necessary).

The joint appointment of Artrozilene 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, when taken orally with Artrosilene, reduce the absorption of ketoprofen.

TERMS AND CONDITIONS OF DISCOUNT FROM PHARMACIES

Dosage forms for systemic use are dispensed by prescription.

Dosage forms for external use are approved for use as over-the-counter products.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored in a place protected from light, out of the reach of children, at temperatures up to 25°C. The aerosol can must not be overheated! The shelf life of rectal capsules and suppositories is 5 years, the solution for intravenous and intramuscular administration, gel and aerosol for external use is 3 years.