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

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

Ketoprofen does not have a catabolic effect on articular cartilage.

Pharmacokinetics
When used 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 mcg/ml. Bioavailability of the drug is about 5%.

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

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

With caution the drug should be prescribed for exacerbation of hepatic porphyria, erosive and ulcerative lesions of the gastrointestinal tract, severe dysfunction of the liver and kidneys, chronic heart failure, bronchial asthma, in the first and second trimesters of pregnancy, as well as for 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.

To avoid hypersensitivity and photosensitivity, it is recommended to avoid exposure of treated areas of skin to sunlight during treatment and for 2 weeks after completion of therapy.

After using the drug, you must wash your hands thoroughly.

An occlusive dressing should not be used.

You should immediately stop using the drug if any skin reaction occurs while using sunscreens or other cosmetics containing octocrylene.

Impact on the ability to drive vehicles and operate machinery

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

If large quantities of the drug (more than 20 g) are accidentally ingested, systemic adverse reactions characteristic of NSAIDs may occur.

Treatment: gastric lavage, taking activated carbon.

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

Patients taking coumarin anticoagulants are advised to regularly monitor their 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.

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

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

Ketoprofen lysine salt, unlike ketoprofen, is a rapidly soluble 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 within 4 to 24 hours.

Pharmacokinetics
Suction
After oral administration, ketoprofen is quite completely absorbed from the gastrointestinal tract, bioavailability exceeds 80%. Cmax is 3-9 mcg/ml and is achieved 4-10 hours after oral administration; its value directly depends on the dose taken. Simultaneous food intake helps to reduce Cmax and increase Tmax, without changing AUC.

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

Removal
T1/2 is 6.5 hours. Metabolites are excreted mainly in the urine. Less than 1% is excreted in feces.

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

Symptomatic treatment of rheumatic and inflammatory diseases, including:

Rheumatoid arthritis;
- spondyloarthritis;
- osteoarthritis;
- gouty arthritis;
- inflammatory damage to 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 of age;
- III trimester of pregnancy;
- lactation period;
- hypersensitivity to the components of the drug or other NSAIDs.

With caution 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.

If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Women planning a pregnancy should refrain from taking the drug Artrosilene, because taking it may reduce the likelihood of egg implantation.

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.

If liver and kidney function are impaired, dose reduction and careful monitoring are necessary.

The use of Artrosilene for bronchial asthma can provoke an attack of suffocation.

Treatment: in case of overdose, if necessary, symptomatic therapy and monitoring of respiratory and cardiovascular activity should be carried out. There is no specific antidote. Hemodialysis is ineffective.

During simultaneous use with the drug Artrosilene, the effectiveness of uricosuric drugs decreases, the effect of anticoagulants, antiplatelet agents, fibrinolytics, ethanol, and the side effects of mineralocorticoids, glucocorticoids, and estrogens are enhanced; the effectiveness of antihypertensive drugs and diuretics decreases.

The simultaneous use of the drug Artrosilene with other NSAIDs, corticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, increasing the risk of developing renal dysfunction.

The simultaneous administration of Artrosilene with oral anticoagulants, heparin, thrombolytics, antiplatelet agents, cefoperazone, cefamandole and cefotetan increases the risk of bleeding.

The drug Artrosilene, when used simultaneously, enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs (dose recalculation is necessary).

The combined use of Artrosilene with sodium valproate causes a violation of platelet aggregation.

Ketoprofen, when used simultaneously, increases the plasma concentration of verapamil and nifedipine, lithium, and methotrexate.

Antacids and cholestyramine reduce the absorption of ketoprofen.

Drug: ARTHROZILEN
Active substance: 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
Registration date: 10/28/05
Owner reg. cred.: DOMPE FARMACEUTICI S.p.A. (Italy)

DOSAGE FORM, COMPOSITION AND PACKAGING

Capsules hard gelatin, 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.

Composition of the capsule body: titanium dioxide (E171), gelatin.
Cap compositioncapsules: quinoline yellow (E104), indigotine (E132), titanium dioxide (E171), gelatin.

10 pcs. - blisters (1) - cardboard packs.

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

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

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

Rectal suppositories uniform, from white to light yellow, torpedo-shaped.

Excipients: semi-synthetic glycerides.

5 pcs. - strips (2) - cardboard packs.

Aerosol for external use 15% in the form of white homogeneous foam; after the gas comes out, it is a transparent liquid of pale yellow color.

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

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

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

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

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

ARTHROZILENE INSTRUCTIONS FOR SPECIALISTS.
The description of the drug ARTHROZILENE was approved by the manufacturer for the 2008 printed publication.

PHARMACOLOGICAL ACTION

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 joints, increases range of motion.

Ketoprofen lysine salt, unlike ketoprofen, is a rapidly soluble 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 within 4 to 24 hours.

When used externally, Artrosilene reduces the manifestations of inflammation and pain in the affected joints, tendons, ligaments, and muscles. In case of articular syndrome, it causes a decrease in joint pain 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 taking capsules orally, ketoprofen is quickly and fairly completely absorbed from the gastrointestinal tract, bioavailability exceeds 80%. Cmax is 3-9 mcg/ml and is achieved after 4-10 hours, its value directly depends on the dose taken. Simultaneous food intake helps to reduce the Cmax value and increase the Tmax value, 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 depends linearly on the dose taken.

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

When applied cutaneously, it is absorbed slowly; a dose of 50-150 mg after 5-8 hours creates a plasma concentration level of 0.08-0.15 mcg/ml. Bioavailability of the drug is about 5%.

Distribution

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

Metabolism

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

Removal

T1/2 is 6.5 hours. Metabolites are excreted mainly in the urine (up to 76% within 24 hours). Less than 1% is excreted in feces. The drug practically does not accumulate in the body.

INDICATIONS

For oral and rectal use

Relief of pain of mild and moderate intensity, including:

Postoperative pain;

Post-traumatic pain;

Inflammatory pain.

Symptomatic treatment of rheumatic and inflammatory diseases, including:

Rheumatoid arthritis;

Spondyloarthritis;

Osteoarthritis;

Gouty arthritis;

Inflammatory damage to periarticular tissues.

For parenteral use

Short-term treatment of acute pain syndrome:

For diseases of the musculoskeletal system of various origins;

In the postoperative period;

After injuries and during inflammatory processes.

For external use

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

Muscle pain of rheumatic and non-rheumatic origin;

Traumatic injuries of soft tissues.

DOSING REGIME

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

Rectally Prescribe 1 suppository 2-3 times a day. The maximum daily dose is 480 mg. Elderly patients You should not prescribe more than 2 suppositories per day.

At impaired renal and liver function dose reduction is necessary.

Parenterally(i.m. or i.v.) 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.

The drug should be administered parenterally for a short time (up to 3 days), then switch to taking the drug orally or using suppositories.

IV administration of the drug is allowed only in a hospital. To increase the duration 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 levulose solution, 5% aqueous dextrose solution, Ringer acetate solution, Ringer lactate Hartmann solution, colloidal dextran solution in 0.9% sodium solution chloride or 5% dextrose solution.

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

At external use 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 a day, gently rubbing until completely absorbed. The duration of treatment should not exceed 10 days (without consulting a doctor).

SIDE EFFECTS

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 activity of liver enzymes, hepatitis, liver failure, increased liver size.

From the central nervous system and peripheral nervous system: dizziness, hyperkinesia, tremor, vertigo, mood swings, anxiety, hallucinations, irritability, general malaise, blurred vision.

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, maculopapular 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 laryngeal spasm, laryngospasm, laryngeal edema, rhinitis.

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

Other: conjunctivitis, menstrual irregularities, increased sweating.

Local reactions after rectal use: burning, itching, heaviness in the anorectal area, exacerbation of hemorrhoids.

Local reactions for external use: skin manifestations of allergic reactions, photosensitivity. With prolonged use on large areas 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 teenagers up to 18 years of age.

For external use

Weeping dermatoses;

Violation of the integrity of the skin;

Children's age up to 6 years.

WITH caution the drug should be prescribed in the first and second trimesters of pregnancy, as well as in elderly patients. At systemic use caution should be exercised in case of 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; at external use- with exacerbation of hepatic porphyria, erosive and ulcerative lesions of the gastrointestinal tract, severe dysfunction 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 Artrosilene in the third trimester of pregnancy is contraindicated. In the first and second trimesters of pregnancy, the drug Artrosilene should be used with caution and under the supervision of a physician. If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Women planning a pregnancy should refrain from taking the drug Artrosilene, because taking it may reduce the likelihood of egg implantation.

SPECIAL INSTRUCTIONS

During treatment with Artrosilene, it is necessary to periodically monitor the peripheral blood picture 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.

The use of Artrosilene for bronchial asthma can provoke an attack of suffocation.

When used externally, the drug should be applied only to intact skin. Avoid contact with eyes and mucous membranes. To avoid 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 gel for external use, can be used in physiotherapeutic treatment (iontophoresis, mesotherapy): with iontophoresis, the drug is applied to the negative pole.

Impact on the ability to drive vehicles and operate machinery

During the period of use of the drug, you should refrain from potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

OVERDOSE

Currently, no cases of overdose with Artrosilene have been reported.

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

During simultaneous use with the drug Artrosilene, the effectiveness of uricosuric drugs decreases, the effect of anticoagulants, antiplatelet agents, fibrinolytics, ethanol, and the side effects of mineralocorticoids, glucocorticoids, and estrogens are enhanced; the effectiveness of antihypertensive drugs and diuretics decreases.

The simultaneous use of the drug Artrosilene with other NSAIDs, corticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, increasing the risk of developing renal dysfunction.

The simultaneous administration of Artrosilene with oral anticoagulants, heparin, thrombolytics, antiplatelet agents, cefoperazone, cefamandole and cefotetan increases the risk of bleeding.

The drug Artrosilene, when used simultaneously, enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs (dose recalculation is necessary).

The combined administration of Artrosilene with sodium valproate causes a violation of platelet aggregation.

Ketoprofen, when used simultaneously, increases the plasma concentration of verapamil and nifedipine, lithium, and methotrexate.

Antacids and cholestyramine, when taken orally with Artrosilene, reduce the absorption of ketoprofen.

CONDITIONS OF VACATION FROM PHARMACIES

Dosage forms for systemic use are available with a prescription.

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

CONDITIONS AND DURATION OF STORAGE

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