ARTROZILEN

Active material: Ketoprofen
When ATH: M02AA10
CCF: NSAIDs for outdoor use
ICD-10 codes (testimony): M05, M07, M10, M15, M42, M45, M46, M65, M70, M71, M79, M79.1, R52.0, R52.2, T14.3
When CSF: 05.01.01.06
Manufacturer: DOMPE FARMACEUTICI S. p. A. (Italy)

Pharmaceutical form, composition and packaging

Capsules hard gelatin, oblong, with a white shell and dark-green Cap; contents of capsules – round pellets of light-yellow color.

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

The composition of the shell capsules: Titanium dioxide (E171), gelatin.
The composition of the operculum capsules: quinoline yellow (E104), indigotin (E132), Titanium dioxide (E171), gelatin.

10 PC. – blisters (1) – packs cardboard.

Solution for in / and the / m clear, colorless or slightly yellow.

Excipients: Sodium hydroxide, lemon acid, water d / and.

2 ml – vials of dark glass (6) – Plastic trays (1) – packs cardboard.

Rectal Suppositories Homogeneous, from white to light yellow in color, torpedo-shaped.

Excipients: semisynthetic glycerides.

5 PC. – strips (2) – packs cardboard.

◊ The aerosol for external use 15% as a white homogeneous; After the release of the gas – transparent liquid bledno-jeltogo color.

Excipients: polysorbate 80, polypropylene glycol, polyvinylpyrrolidone (povidone), flavoring Lavender nerolen, benzyl alcohol, Purified water, a mixture of propane and butane.

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

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

Excipients: carboxypolymethylene, triethanolamine, polysorbate, ethanol 95%, metilparagidroksiʙenzoat, flavoring Lavender nerolen, water.

30 g – aluminum tuba (1) – packs cardboard.
50 g – aluminum tuba (1) – packs cardboard.

Pharmacological action

NSAIDs. Anti-inflammatory, analgesic and antipyretic effect. By inhibiting the Cox-1 and Cox-2, inhibits the synthesis of prostaglandins. Has antibradikininovoj activity, lizosomaiona stabilize membranes and delaying the release of these enzymes, contributing to the destruction of tissues in chronic inflammation. Reduces the secretion of cytokines, inhibits the activity of neutrophils.

Reduces morning stiffness and swelling of joints, increases the volume of movements.

Ketoprofen lysine salt, Unlike ketoprofen, is the instant connection with neutral pH, due to the almost non-irritating the INTESTINE.

After intake of maximum therapeutic effect was observed from 4 to 24 no.

When an external application Artrozilen reduces inflammation and pain in the area of the affected joints, tendons, ligaments, muscle. When the articular syndrome causes a weakening of joint pain at rest and during movement, reduce morning stiffness and swelling of joints.

Ketoprofen lizinovaja salt has no katabolicheskogo influence on articular cartilage.

Pharmacokinetics

Absorption

Ketoprofen capsules after ingestion quickly and adequately absorbed from the digestive tract, bioavailability is greater than 80%. C_max is 3-9 ug / ml achieved after 4-10 no, its value is directly dependent on the dose. Simultaneous eating helps reduce the values of C_max and an increase in T_max, without changing AUC.

After rectal ketoprofen is also rapidly absorbed. The time to reach C_max After rectal 45-60 m. The value of plasma concentration is linearly dependent on the dose.

The time to reach C_max when administered parenterally 45-60 m. The effective concentration is 24 no. Therapeutic concentrations in the synovial fluid is stored 18-20 no.

In nakojna software absorbed slowly; dose 50-150 mg after 5-8 h creates a level of concentration in plasma 0.08-0.15 ug / ml. Bioavailability – about 5%.

Distribution

To 99% ketoprofen is associated with plasma proteins, mostly to albumin. V_d – 0.1-0.2 l / kg. Easily permeates through gistogematicalkie barriers and distributed in the tissues and organs. Ketoprofen well penetrates into synovial fluid and connective tissue. Although ketoprofen concentration in synovial fluid slightly below, than in plasma, It is more stable (saved to 30 no).

Metabolism

Ketoprofen is mainly metabolised in the liver, where he undergoes glucuronidation with the formation of esters with glukuronova acid.

Deduction

T_1/2 is 6.5 no. Metabolites are excreted mainly with urine (to 76% during 24 no). Faeces thrown less than 1%. The drug is almost not koumouliruet in the body.

Testimony

For oral and rectal

Mild pain weak and moderate intensity, including:

-post-operative pain;

-post-traumatic pains;

— inflammatory pain.

Symptomatic treatment of rheumatic and inflammatory diseases, including:

- Rheumatoid arthritis;

— spondylarthritis;

- Osteoarthritis;

-gouty arthritis;

-inflammatory lesion of the periarticular tissues.

For parenteral administration

Short term treatment of acute pain syndrome:

-at the diseases of the musculoskeletal system of different Genesis;

— in the postoperative period;

after injuries and inflammatory processes.

For outdoor use

- Acute and chronic inflammatory diseases of the musculoskeletal system (incl. rheumatoid arthritis, psoriaticheskiy arthritis, ankylosing spondylitis, osteoarthritis of peripheral joints and spine, soft tissue rheumatic);

- Muscle pain rheumatic and rheumatic origin;

- Traumatic soft tissue injuries.

Dosage regimen

Inside Artrozilen appoint 1 caps. / day, during or after a meal. The duration of treatment may be 3-4 Months.

Rectal appoint 1 suppozitoriû 2-3 times / day. The maximum daily dose – 480 mg. Elderly patients nor should appoint more 2 suppositories per day.

At violation of the kidney and the liver It is necessary to reduce the dose of.

Parenteral (w / o or w / w) the drug is prescribed in a dose 160 mg (1 amp.)/d. The maximum daily dose is 320 mg (by 1 amp. 2 times / day).

Elderly patients age You should assign not more than 1 amp./day.

Parenteral drug should be short (to 3 days), then move on to the reception of the drug inside or on the use of suppositories.

In/in the introduction of the drug is permitted only in a hospital. To increase the duration of the drug recommended slow in/in infusion. The on/in infusion duration of not less than 30 m.

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% levulose, aqueous solution, 5% dextrose, solution Ringera acetate, solution ringer lactate Hartman, Colloidal solution of dextran in 0.9% sodium chloride or 5% dextrose.

Breeding Artrozilena in solutions of small volume (50 ml) the drug is injected into/in bolusno.

At an external application a single dose of the gel is 3-5 g (the volume of a large cherry), aerosol – 1-2 g (scope Walnut). The drug should be applied 2-3 times / day, gently vtiraya until saturation. The duration of treatment should not exceed 10 days (without consulting a doctor).

Side effect

From the digestive system: stomach ache, diarrhea, stomatitis, esophagitis, gastritis, duodenitis, erosive and ulcerative lesions of the gastrointestinal tract, gematomezis, ground, increased levels of bilirubin, increase in liver enzymes, hepatitis, hepatic failure, enlarged liver.

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

Allergic reactions: hives, angioedema, erythema multiforme exudative (incl. Stevens-Johnson syndrome), anaphylactoid reactions (swelling of the mucous membranes of the oral cavity, swelling of the throat, periorbital edema).

Dermatological reactions: eritematosnaya exantema, itch, maculo-papular rash.

From the urinary system: urodynia, cystitis, swelling, hematuria.

From the hematopoietic system: leukopenia, leukocytosis, limfangit, decrease of prothrombin time, thrombocytopenia, trombotsitopenicheskaya purpura, increasing the size of the spleen, vasculitis.

The respiratory system: bronchospasm, dyspnoea, sensation of spasm of the larynx, laringospazm, laryngeal edema, rhinitis.

Cardio-vascular system: hypertension, gipotenziya, tachycardia, chest pain, syncope, peripheral edema, paleness.

Other: conjunctivitis, menstrual disorders, increased sweating.

Local reactions when rectal use: burning, itch, heaviness in the anorectal area, aggravation of hemorrhoids.

Local reaction when an external application: skin manifestations of allergic reactions, photosensitivity. With long-term use of large skin surfaces may develop systemic side effects.

Ketoprofen lizinovaja salt is much less side effects compared to ketoprofenom.

Contraindications

- “aspirinovaâ triad”;

- III trimester of pregnancy;

- Lactation;

- Hypersensitivity to ketoprofen or other ingredients, aspirin or other NSAIDs.

For systemic use

- Gastric ulcer and duodenal ulcer in the acute phase;

is ulcerative colitis in the acute phase;

- Crohn's disease;

-diverticulitis;

-peptic ulcer;

is human blood clotting (incl. hemophilia);

- Chronic renal failure;

- Childhood and adolescence up 18 years.

For outdoor use

-leg dermatoses;

- Eczema;

- Violation of the integrity of the skin;

- Children up to age 6 years.

FROM caution should designate product in the I and II trimestrah pregnancy, and elderly patients. At System application caution should be exercised when anemia, asthma, alcoholism, tobacco use, alcoholic liver cirrhosis, giperʙiliruʙinemii, hepatic insufficiency, diabetes, degidratacii, sepsis, chronic heart failure, edema, hypertension, blood diseases (incl. leukopenia), definition, glucose-6-fosfatdegidrogenazы, Stomat; at an external application – in acute hepatic porfirii, erosive and ulcerative lesions of the gastrointestinal tract, severe violations of liver and kidney function, chronic heart failure, asthma, as well as children under the age of 12 years.

Pregnancy and lactation

Application of Artrozilen in the third trimester of pregnancy is contraindicated. In the I and II trimestrah pregnancy drug Artrozilen with caution and under the supervision of a physician. If necessary, use during lactation should stop breastfeeding.

Women, planning pregnancy, It should refrain from taking the drug Artrozilen, tk. against the background of his admission may decrease the likelihood of implantation of the egg.

Cautions

During drug treatment Artrozilen should be periodically monitored picture peripheral blood and functional status of the liver and kidney.

If you want to determine the 17-ketosteroids drug should be discontinued for 48 h before the test.

Welcome Artrozilena can mask signs of infection.

Application of Artrozilena in bronchial asthma may trigger a bout of breathlessness.

When an external application drug should be applied only on intact skin. Avoid contact with eyes and mucous membranes. To avoid manifestations of hypersensitivity and photosensitivity, It is advisable to avoid exposure to the Sun's rays on the skin during the course of treatment.

Aqueous solutions of ketoprofen lizinovoj salt, as well as gel for external use can be used in physiotherapy treatment (ionoforeze, Mesotherapy): When ionoforeze the drug caused the negative pole.

Effects on ability to drive vehicles and management mechanisms

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

Overdose

Currently, the cases of drug overdose Artrozilen were reported.

In the case of an overdose should be symptomatic therapy, monitoring of respiratory and cardiovascular activity. There is no specific antidote. Hemodialysis maloeffyektivyen.

Drug Interactions

Inductors of microsomal oxidation in the liver (incl. phenytoin, ethanol, barbiturates, flumetsinol, rifampicin, phenylbutazone, tricyclic antidepressants) together with the use of a drug Artrozilen increase the metabolism of ketoprofen (increase the production of hydroxylated active metabolites).

Amid simultaneous application with the drug Artrozilen is reduced the effectiveness of urikozuricheskih drugs, intensifies anticoagulants, antiagregantov, fibrinolitikov, ethanol, side effects of mineralokortikoidov, glюkokortikoidov, estrogen; decreases the effectiveness of antihypertensive drugs and diuretics.

Simultaneous application of Artrozilen with other NSAIDS, GCS, ethanol, corticotropin may lead to the development of ulcers and gastrointestinal bleeding, to increase the risk of violations of the kidney.

The simultaneous appointment Artrozilena with oral anticoagulants, geparinom, thrombolytics, antiplatelet, cefoperazone, Tsefamandol tsefotetanom and increases the risk of bleeding.

Drug Artrozilen while applying enhances gipoglikemicescoe effect of insulin and oral hypoglycemic drugs (recalculation of the dose needed).

Joint appointment with Artrozilena sodium valproatom leading to the disruption of platelet aggregation.

Ketoprofen in odnovremennnom application increases concentration in plasma nifedipine and verapamil, lithium, methotrexate.

Antacids and kolestiramin while ingestion with the drug Artrozilen reduce the absorption of ketoprofen.

Conditions of supply of pharmacies

Dosage forms for system application sold by prescription.

Dosage forms for external use are allowed to use as OTC tools.

Conditions and terms

The drug should be stored in the dark, inaccessible to children at temperature to 25 ° C. Spray tank cannot overheat! Shelf life of capsules and suppositories-rectal 5 years, solution for the on/in and/m introduction, gel and spray for external use- 3 year.