2010/09/21

Artrosilen

Composition, structure and packing

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

1 capsule. ketoprofen lysine salt 320 mg.

Excipients: diethyl phthalate, karboksipolimetilen, magnesium stearate, povidone, acrylic and methacrylic acid polymers, talc. The composition of the shell capsules: titanium dioxide (E171), quinoline yellow (E104), indigo, titanium dioxide, gelatin.

Solution for in / and / m the introduction of transparent, colorless or slightly yellow.

1 ml of 1 amp. ketoprofen lysine salt 80 mg 160 mg.

Excipients: sodium hydroxide, citric acid, water d / and.

Rectal suppositories homogeneous, white to light yellow, torpedoobraznoy form.

A TIS. ketoprofen lysine salt 160 mg.

Excipients: semisynthetic glycerides.

Aerosol for external use only 15% in the form of a homogeneous foam after the release of gas - a transparent liquid of pale yellow color. 1 g of foam ketoprofen lysine salt 150 mg. Excipients: polysorbate, polypropylene, povidone, liquid nerolenovaya, benzyl alcohol, purified water, propellant - propane-butane.

Gel for external use only 5% transparent, thick with the smell of lavender. 1 g of ketoprofen lysine salt 50 mg Excipients: karboksipolimetilen, triethanolamine, polyoxyethylene sorbitan monooleate (vegetable oil), ethanol, metilparagidroksibenzoat, nerolenovaya liquid, distilled water.

Clinico-pharmacological group: NSAID.

Pharmacological action

NSAID. Has anti-inflammatory, analgesic and antipyretic effect. By inhibiting COX-1 and COX-2 inhibits the synthesis of prostaglandins. Has antibradikininovoy activity, stabilizes lysosomal membranes and prevents the release of these enzymes that contribute to tissue damage in chronic inflammation.

Reduces the allocation of cytokines, inhibits the activity of neutrophils. Reduces morning stiffness and swelling of the joints, increases range of motion. Ketoprofen lysine salt, in contrast to ketoprofen, an instant connection with a neutral pH, due to which almost does not irritate the digestive tract. Once inside the maximum therapeutic effect was observed for 4 to 24 hours when applied externally Artrozilen reduces the expression of inflammation and pain in damaged joints, tendons, ligaments and muscles.

When articular syndrome causes a weakening of joint pain at rest and in motion, decrease morning stiffness and swelling of the joints. Ketoprofen lysine salt does not have a catabolic effect on articular cartilage.

Pharmacokinetics

Absorption

After oral ketoprofen capsules quickly and adequately absorbed from the gastrointestinal tract, bioavailability exceeds 80%. Cmax of 3.9 mcg / ml and reached after 4-10 h, its value is directly dependent on the applied dose. Simultaneous food intake reduces the value of Cmax and an increase in Tmax, without changing the AUC. After rectal ketoprofen is also rapidly absorbed.

Time to reach Cmax following rectal 45-60 min. The concentration in plasma is linearly dependent on the applied dose. Time to reach Cmax for parenteral administration 45-60 min. The effective concentration remains 24 hours therapeutic concentrations in synovial fluid remain 18-20 h. epicutaneous application absorbed slowly; dose of 50-150 mg every 5-8 h creates a level of concentration in plasma of 0.08-0.15 mg / ml. Bioavailability of the drug - about 5%.

Distribution

Up to 99% ketoprofen bound to plasma proteins, primarily albumin. Vd - 0.1-0.2 L / kg. Easily penetrates through histohematogenous barriers and is distributed in the tissues and organs. Ketoprofen well into the synovial fluid and connective tissue. Although the concentration of ketoprofen in the synovial fluid is slightly lower than in plasma, it is more stable (save up to 30 h).

Metabolism

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

Withdrawal

T1 / 2 was 6.5 h. The metabolites are derived mainly from urine (up to 76% within 24 h). Since feces derived less than 1%. Drug is not cumulative in the body.

Statement

For oral and rectal pain docking weak to 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 periarticular tissues.

For parenteral

Short-term treatment of acute pain:
in diseases of the musculoskeletal system of various origins;
in the postoperative period;
after injury and 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, soft tissue rheumatism);
muscle pain and rheumatoid Non-rheumatic origin;
traumatic injuries of soft tissues.

Dosage regimen

Inside Artrozilen appoint 1 kaps. / day, during or after a meal. Duration of treatment may be 3-4 months. Rectal appoint 1 suppository 2-3 times / day. The maximum daily dose - 480 mg. Elderly patients should not appoint more than 2 suppositories per day.

If any function of the kidneys and liver need to reduce the dose. Parenteral (IM or IV) drug is administered in a dose of 160 mg (1 amp.) A day. The maximum daily dose is 320 mg (1 amp. 2 times / day). Elderly patients should be appointed not more than 1 amp. / day. Parenteral drug should be administered short duration (up to 3 days), then move on to taking the drug by mouth or by the use of suppositories. In / to the introduction of the drug is allowed only in the hospital.

To increase the duration of the drug recommended to carry out a slow i / v infusion. Duration / v infusion of 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, 10% aqueous solution of levulose 5% aqueous solution of dextrose, Ringer's acetate, Ringer Lactate Hartmann, colloidal solution of dextran in 0.9% sodium chloride or 5% dextrose.

When breeding Artrozilena in solutions of small volume (50 ml) the drug is introduced into / in the bolus. For exterior use single dose of gel is 5.3 g (large amount of cherries), Aerosol - 1-2 grams (size of a walnut). The product should be applied 2-3 times a day, rubbing gently until completely absorbed. Duration of treatment should not exceed 10 days (without consulting a doctor).

Side effect
On the part of the digestive system: abdominal pain, diarrhea, stomatitis, esophagitis, gastritis, duodenitis, erosive and ulcerative lesions gastrointestinal gematomezis, melena, increased bilirubin, increased liver enzymes, hepatitis, liver failure, enlarged liver.
From the central nervous system and peripheral nervous system: dizziness, hyperkinesia, tremor, vertigo, mood swings, anxiety, hallucinations, irritability, malaise, visual disturbances. Allergic reactions: urticaria, angioedema, erythema multiforme exudative (including Stevens-Johnson syndrome), anaphylactoid reaction (swelling of the oral mucosa, pharyngeal edema, periorbital edema). Dermatological reactions: erythematous rash, itching, Makulo-papular rash.
From the urinary system: painful urination, cystitis, edema, hematuria.
On the part of the hemopoietic system: leykotsitopeniya, leukocytosis, lymphangitis, a decrease prothrombin time, thrombocytopenia, thrombocytopenic purpura, an increase in the size of the spleen, vasculitis.
On the part of the respiratory system: bronchospasm, dyspnoea, sensation of spasm of the larynx, laryngism, larynx edema, rhinitis.
Since the cardiovascular system: hypertension, hypotension, tachycardia, chest pain, syncopal states, peripheral edema, pallor.

Other: conjunctivitis, menstrual disorders, increased sweating. Local reactions in rectal: burning, itching, heaviness in the anorectal region, exacerbation of hemorrhoids.

Local reactions when used externally: Skin manifestations of allergic reactions, photosensitivity. With prolonged use over large surface of the skin may develop systemic side effects. Ketoprofen lysine salt is much less common cause side effects compared with ketoprofenom.

Contraindications
"Aspirin triad";
III trimester of pregnancy;
lactation;
Hypersensitivity to ketoprofenu or other components of the drug, acetylsalicylic acid or other NSAIDs.

For regular use:
stomach ulcer and duodenal ulcer exacerbation;
Ulcerative colitis exacerbation;
Crohn's disease;
diverticulitis;
peptic ulcer;
blood coagulation disorders (including hemophilia);
chronic renal failure;
childhood and adolescence to 18 years.

For external use
weeping dermatitis;
eczema
violation of the integrity of the skin;
Children under 6 years.

Precautions should be prescribed the drug in I and II trimesters of pregnancy, as well as elderly patients.

The systems use caution should be exercised with anemia, asthma, alcoholism, smoking, alcoholic cirrhosis, hyperbilirubinemia, hepatic failure, diabetes, dehydration, sepsis, chronic heart failure, edema, hypertension, blood diseases (including leukopenia ), deficiency of glucose-6-phosphate dehydrogenase, stomatitis, when used externally - with acute hepatic porphyria, erosive and ulcerative lesions of the gastrointestinal tract, severe violations of liver and kidney function, congestive heart failure, asthma, and children under the age of 12 years.

Bermennost and lactation

Use of the drug Artrozilen in III trimester of pregnancy is contraindicated. In I and II trimesters of pregnancy should use the drug Artrozilen with caution and under medical supervision.

If necessary, use during lactation breastfeeding should be discontinued. Women planning pregnancy, should refrain from taking the drug Artrozilen, because against the background of their intake may decrease the probability of implantation of the embryo.

Application for violations of liver function

If abnormal liver function should reduce the dose.

Application for violations of renal function

In case of violation of renal function should reduce the dose.

Cautions

During treatment with Artrozilen necessary to carry out periodic monitoring of the pattern of peripheral blood and functional state of the liver and kidneys.

If necessary, determine the 17-ketosteroids drug should be abolished for 48 h before the study. Receiving Artrozilena may mask signs of infection.

Application Artrozilena bronchial asthma can provoke an attack of breathlessness.

For exterior use medication should be applied only to intact skin. Avoid contact with eyes and mucous membranes. To avoid reflections of the heightened sensitivity and photosensitivity, it is recommended to avoid skin damage the sun during the course of treatment.

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

Effects on ability to drive vehicles and management mechanisms

During the period of the drug should avoid potentially hazardous activities that require high concentration and quickness of psychomotor reactions.

Overdose

Currently, cases of drug overdose Artrozilen not reported. In case of overdose should be symptomatic therapy, monitoring of respiratory and cardiovascular activity. Specific antidote exists. Hemodialysis is ineffective.

Drug Interactions

Inductors microsomal oxidation in the liver (including phenytoin, ethanol, barbiturates, flumetsinol, rifampicin, fenilbutazon, tricyclic antidepressants), while the use of the drug Artrozilen increase metabolism ketoprofen (increase production of hydroxylated active metabolites). Against the background of the simultaneous application of the drug reduced the effectiveness Artrozilen urikozuricheskih drugs, increases the effects of anticoagulants, antiplatelet agents, fibrinolytics, ethanol, side effects mineralokortikoidov, glucocorticoids, estrogen, decreases the effectiveness of antihypertensive drugs and diuretics.

The simultaneous use of the drug Artrozilen with other NSAIDs, SCS, ethanol, corticotropin may lead to ulceration and the development of gastrointestinal bleeding, increased risk of renal dysfunction.

The simultaneous appointment Artrozilena with oral anticoagulants, heparin, thrombolytics, antiagregantami, cefoperazone, and tsefamandolom tsefotetanom increases the risk of bleeding.

The drug Artrozilen while the application increases the hypoglycemic effect of insulin and oral hypoglycemic agents (requires recalculation of dose).

Joint appointment Artrozilena with sodium valproate causes a disturbance of platelet aggregation. Ketoprofen in odnovremennnom application increases plasma concentration of nifedipine and verapamil, lithium, methotrexate. Antacids and kolestiramin while ingestion of the drug reduces the absorption of ketoprofen Artrozilen.

Terms and Conditions of storage

The drug should be kept in the dark, away from children below 25 ° C. The container with the aerosol can overheat! Expiration capsules and suppositories rectal - 5 years, a solution for in / and / m the introduction, gel and aerosol for external use - 3 years.