Arthrosilen - instructions for use, dose, side effects, contraindications

Has anti-inflammatory, analgesic and antipyretic effect. Inhibiting cyclooxygenase I and II type, inhibits the synthesis of prostaglandins. It has anti-bradykinin activity, stabilizes lysosomal membranes, and delays the release of enzymes that promote tissue destruction in chronic inflammation. Reduces the secretion of cytokines, inhibits the activity of neutrophils.

Reduces the morning stiffness and swelling of the joints, increases the volume of movements. Ketoprofen lysine salt, in contrast to ketoprofen, is a rapidly dissolving molecule with a neutral pH and almost does not irritate the gastrointestinal tract.

Pharmacokinetics:

Suction. Ketoprofen lysine salt is rapidly absorbed: the time to reach the maximum concentration (T_mOh) after rectal administration 45-60 minutes. The concentration in the plasma depends linearly on the dose taken.

Distribution. Up to 99% of absorbed ketoprofen binds to plasma proteins, mainly with albumin. The volume of distribution is 0.1-0.2 l / kg. Easily passes through the histohematological barriers and is distributed in tissues and organs. Ketoprofen well penetrates into the synovial fluid and connective tissue. Although the concentration of ketoprofen in the synovial fluid is slightly lower than in the plasma, they are more stable (lasting up to 30 hours).

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

Excretion. Metabolites are excreted mainly with urine (up to 76% after 24 hours). The drug does not cumulate.

Indications:

Pain relief of mild to moderate intensity, including: postoperative pain, inflammatory post-traumatic pain.

Rheumatic diseases:

- rheumatoid arthritis;

- Spondyloarthritis;

- osteoarthrosis;

- gouty arthritis;

- Inflammation of the periarticular tissues.

Contraindications:

Hypersensitivity (including to other NSAIDs), "aspirin" asthma, peptic ulcer and duodenal ulcer (exacerbation), ulcerative colitis (exacerbation), Crohn's disease, diverticulitis, peptic ulcer, hemophilia and other disorders of blood coagulation, CRF, children's age (under 18 years), pregnancy (III trimester), lactation.

Carefully:

Anemia, bronchial asthma, alcoholism, tobacco smoking, alcoholic liver cirrhosis, hyperbilirubinemia, hepatic insufficiency, diabetes mellitus, dehydration, sepsis, CHF, edema, arterial hypertension, blood diseases (including leukopenia), glucose-6-phosphate dehydrogenase deficiency, stomatitis, advanced age, pregnancy (I, II trimester).

In case of deterioration of the patient should stop treatment with the drug.

Pregnancy and lactation:

Like other NSAIDs, Arthrosilen should not be used in the third trimester of pregnancy. The use of the drug in I and II trimester should be carefully monitored by the attending physician.

Breastfeeding with the use of the drug should be discontinued.

Dosing and Administration:

One suppository 2-3 times a day. The maximum daily dose of 480 mg. In elderly patients, no more than 2 suppositories per day should be used.

Side effects:

Gastrointestinal tract: abdominal pain, diarrhea, duodenitis, erosive-ulcerative lesions of the gastrointestinal tract, gastritis, hematomesis, esophagitis, stomatitis, melena.

Liver: increased bilirubin, increased "hepatic" enzymes, hepatitis, liver failure, increased liver size.

Nervous system: dizziness, hyperkinesia, tremor, vertigo, mood swings, anxiety, hallucinations, irritability, general malaise.

Sense organs: conjunctivitis, impaired vision.

Skin: urticaria, angioedema, erythematous exanthema, pruritus, maculopapular exanthema, increased sweating, multiform exudative erythema (including Stevens-Johnson syndrome).

Genitourinary system: painful urination, cystitis, swelling, hematuria, menstrual irregularity.

Organs of hematopoiesis: leukocytosis, leukocytosis, lymphangitis, decrease in prothrombin time, purpura, thrombocytopenia, thrombocytopenic purpura, enlarged spleen, vasculitis.

Respiratory system: bronchospasm, dyspnoea, sensation of spasm of the larynx, laryngospasm, laryngeal edema, rhinitis.

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

Allergic reactions: anaphylactoid reactions, edema of the oral mucosa, swelling of the pharynx, periorbital edema.

Local Reactions: burning, itching, heaviness in the anorectal area, exacerbation of hemorrhoids.

Overdose:

At present, cases of overdose with Arthrosylen have not been reported.

Interaction:

Inductors 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, antiaggregants, fibrinolytics, ethanol, side effects of mineral corticosteroids, glucocorticosteroids, estrogens. Reduces the effectiveness of antihypertensive and diuretics.

Joint reception with other NSAIDs, glucocorticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, an increased risk of kidney dysfunction.

Simultaneous administration with oral anticoagulants, heparin, thrombolytic agents, antiaggregants, cefoperazone, cefamandol and cefotetan increases the risk of bleeding.

Increases hypoglycemic action of insulin and oral hypoglycemic drugs (dose recalculation is necessary).

Co-administration with sodium valproate causes disruption of platelet aggregation. Increases the concentration in the plasma of verapamil and nifedipine, lithium preparations, methotrexate. Antacids and colestramine reduce absorption.

Special instructions:

During treatment, it is necessary to 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 test.

Reception of ketoprofen can mask signs of an infectious disease.

If the kidney and liver function is impaired, a dose reduction and careful monitoring is necessary. The use of ketoprofen by patients suffering from bronchial asthma can lead to an attack of bronchial asthma.

Women planning a pregnancy, should refrain from taking the drug, tk. can reduce the likelihood of implantation of the egg.

Effect on the ability to drive transp. cf. and fur:

During the period of application of the drug, one should refrain from potentially dangerous activities related to the need for concentration of attention and rapid psychomotor reactions.

Form release / dosage:

Suppositories rectal, 160 mg.

Packaging:

For 5 suppositories in a strip made of Al-foil.

2 strips in a cardboard box with instructions for use.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children!

Shelf life:

5 years.

Do not use the product after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N010596 / 04

Date of registration:30.06.2010

Expiration Date:Unlimited

The owner of the registration certificate:Dompe Pharmacetici SpA Dompe Pharmacetici SpA Italy

Manufacturer: & nbsp

DOMPE FARMACEUTICI, S.p.A. Italy

Representation: & nbspCBS CJSC LTDCBS CJSC LTDItaly

Information update date: & nbsp13.09.2017

Illustrated instructions

Instructions

Arthrosilen (Artrosilene)