medicalmeds.eu Medicines Non-steroidal anti-inflammatory drug (NPVP). Артрозан®

Артрозан®

Producer: JSC Pharmstandart Russia

Code of automatic telephone exchange: M01AC06

Release form: Firm dosage forms. Tablets.

Indications to use:

General characteristics. Structure:

Active agent - to meloksika of 7,5 mg or 15 mg.
Excipients: potato starch, lactoses monohydrate, povidone, trisodium citrate, magnesium stearate, silicon dioxide colloid.

Pharmacological properties:

Pharmacodynamics. Meloksikam - the non-steroidal anti-inflammatory drug possessing anesthetic, febrifugal and analgetic action.

Antiinflammatory action is connected with braking of enzymatic activity of cyclooxygenase-2 (TsOG-2) participating in biosynthesis of prostaglandins in the field of an inflammation. To a lesser extent to meloksika affects cyclooxygenase-1 (TsOG-1) participating in synthesis of the prostaglandin which is protecting a mucous membrane of digestive tract and taking part in regulation of a blood-groove in kidneys.

Pharmacokinetics. Absolute bioavailability of a meloksikam – 89% is well soaked up from digestive tract. The concomitant use of food does not change absorption. When using drug inside in doses of 7,5 and 15 mg of its concentration are proportional to doses. Equilibrium concentration are reached within 3 - 5 days. At prolonged use of drug (more than 1 year), concentration are similar to those which are noted after the first achievement of a steady condition of pharmacokinetics. Linkng with proteins of plasma makes more than 99%. Range of distinctions between the maximum and basal concentration of drug after its reception is rather small once a day and makes when using a dose 7,5 mg 0,4-1,0 mkg/ml, and when using a dose of 15 mg – 0,8–2,0 mkg/ml (are brought according to _{Cmin and Cmax value}). Meloksikam gets through gistogematichesky barriers, concentration and in synovial fluid reaches 50% of the maximum concentration of drug in plasma.

Almost it is completely metabolized in a liver with formation of four inactive derivatives in the pharmacological relation. The main metabolite 5 '-karboksimeloksikam (60% of dose size), is formed by oxidation of an intermediate metabolite, 5 '-gidroksimeloksikama which is also excreted, but to a lesser extent (9% of dose size). The researches in vitro showed that in this metabolic transformation an important role is played by CYP 2C9, additional value has CYP 3A4 isoenzyme. Peroxidase, activity which it probably individually varies takes part in formation of two other metabolites (making, respectively, 16% and 4% of size of a dose of drug).

It is removed equally with a stake and urine, it is preferential in the form of metabolites. With a stake in not changed look less than 5% of a daily dose are removed, in urine in an invariable look drug is found only in trace quantities. The elimination half-life _(T1/2) of a meloksikam makes 15-20 hours. The plasma clearance averages 8 ml/min. At elderly people the clearance of drug decreases. Distribution volume low, also averages 11 l.

Indications to use:

Symptomatic treatment of an osteoarthrosis, pseudorheumatism, ankylosing spondylarthritis (Bekhterev's disease) and other inflammatory and degenerative diseases which are followed by a pain syndrome.

Route of administration and doses:

Drug is accepted inside during food once a day.

The recommended dosing mode:

Pseudorheumatism: 15 mg a day. After achievement of therapeutic effect the dose can be lowered to 7,5 mg a day.
Osteoarthrosis: 7,5 mg a day. At inefficiency the dose can be increased to 15 mg a day.
Ankylosing spondylarthritis: 15 mg a day.

The maximum daily dose should not exceed 15 mg.

Patients with the increased risk have development of side effects, and also at the patients with the expressed renal failure who are on a hemodialysis, the dose should not exceed 7,5 mg a day.

Pregnancy and lactation
Drug is not recommended to be used during pregnancy and a lactation.

Features of use:

It is necessary to be careful at use of drug for patients who have in the anamnesis a peptic ulcer of a stomach or duodenum, and also at the patients who are on anti-coagulative therapy. At such patients the risk of developing of ulcer and erosive diseases of digestive tract is increased.
It is necessary to be careful and control indicators of function of kidneys at use of drug for patients of advanced age, patients with chronic heart failure with the circulatory unefficiency phenomena, at patients with cirrhosis, at patients with a hypovolemia as a result of surgical interventions.
At patients with a renal failure if the clearance of creatinine more than 25 ml/min. is not required to correction of the mode of dosing.
At the patients who are on dialysis, the dosage of drug should not exceed 7,5 mg/days.
The patients accepting at the same time diuretics and to meloksika have to accept enough liquid.
If in the course of treatment there were allergic reactions (an itch, skin rash, a small tortoiseshell, a photosensitization) it is necessary to see a doctor for the purpose of the solution of a question of the termination of administration of drug.

Control of vehicles, service of cars and mechanisms
Use of drug can cause emergence of undesirable side effects in the form of a headache and dizziness, drowsiness. It is necessary to refuse control of vehicles and service of the cars and mechanisms demanding concentration of attention.

Side effects:

Bodies of the alimentary system: nausea, vomiting, abdominal pain, diarrhea or lock, meteorism, GIT erosive cankers, perforation of a stomach or intestines, gastrointestinal bleeding (hidden or explicit), increase in activity of "hepatic" enzymes, hepatitis, colitis, stomatitis, dryness of a mouth, esophagitis.

Cardiovascular system: tachycardia, increase in arterial pressure, feeling of "inflows".

Respiratory system: aggravation of a course of bronchial asthma, cough.

Central nervous system: headache, dizziness, sonitus, disorientation, confusion of thoughts, sleep disorder.

Urinogenital system: hypostases, intersticial nephrite, renal medullary necrosis, uric infection, proteinuria, hamaturia, renal failure.

Organs of sight: conjunctivitis, sight illegibility.

Integuments: an itch, skin rash, a small tortoiseshell, a mnogoformny exudative erythema (including Stephen-Johnson's syndrome), a toxic epidermal necrolysis (Lyell's disease), the increased photosensitivity.

System of a hemopoiesis: anemia, leukopenia, thrombocytopenia.

Allergic reactions: anaphylactoid reactions (including acute anaphylaxis), hypostasis of lips and language, allergic vasculitis.

Others: fever.

Interaction with other medicines:

At simultaneous use with other non-steroidal anti-inflammatory drugs (and also with acetylsalicylic acid) the risk of emergence of erosive cankers and bleedings of a GIT increases;
At simultaneous use with hypotensive drugs, decrease in efficiency of action of the last is possible;
At simultaneous use with drugs of lithium development of cumulation of lithium and increase in its toxic action is possible (control of concentration of lithium in blood is recommended);
At simultaneous use with a methotrexate side effect of the last on the hemopoietic system amplifies (danger of developing of anemia and a leukopenia, periodic control of the general blood test is shown);
At simultaneous use with diuretics and with cyclosporine the risk of development of a renal failure increases;
At simultaneous use with intrauterine contraceptive means decrease in efficiency of action of the last is possible;
At simultaneous use with anticoagulants (heparin, тиклопидин, warfarin), and also with thrombolytic drugs (Streptokinasa, fibrinolysin) the risk of development of bleedings increases (periodic control of indicators of coagulability of blood is necessary).
At simultaneous use with Colestyraminum, as a result of binding of a meloksikam, its removal through a GIT amplifies.

Contraindications:

hypersensitivity to any component of drug;
aspirinovy bronchial asthma;
aggravation of a peptic ulcer of a stomach and duodenum;
chronic renal failure (if the hemodialysis is not carried out);
heavy liver failure;
children aged up to 15 years;
pregnancy;
lactation period.

Overdose:

Symptoms: consciousness disturbance, nausea, vomiting, pains in epigastriums, GIT bleeding., acute renal failure, liver failure, apnoea, asystolia.
Treatment: there is no specific antidote; at overdose of drug it is necessary to carry out a gastric lavage, reception of absorbent carbon (within the next hour), symptomatic therapy. Holestiramin accelerates removal of drug from an organism. The artificial diuresis, urine alkalinization, a hemodialysis – are ineffective because of high communication of drug with blood proteins.