Mesipol

General characteristics. Structure:

Active agent - to meloksika of 7,5 mg or 15 mg.

Excipients: corn starch, the modified corn starch, silicon dioxide colloid anhydrous, sodium citrate, lactose, microcrystallic cellulose, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Meloksikam - the non-steroidal anti-inflammatory drug possessing anesthetic, antiinflammatory, 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 its concentration are proportional to doses. Equilibrium concentration it is 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. Meloksikam gets through gistogematichesky barriers, concentration in synovial fluid reaches 50% of the maximum concentration in synovial fluid reaches 50% of the maximum concentration of drug in plasma.

It is removed equally with a stake and urine, it is preferential in the form of metabolites. With a stake in an invariable look less than 5% of the size of a daily dose are removed, in urine in an invariable look drug is found only in trace quantities. The elimination half-life of a meloksikam makes 15-20 hours. The plasma clearance averages 8 ml/min. At elderly people the clearance of drug decreases.

The liver or renal failure of moderate severity has no significant effect on pharmacokinetics of a meloksikam.

Indications to use:

- symptomatic treatment of a pseudorheumatism;

- symptomatic treatment of an osteoarthrosis;

- symptomatic treatment of an ankylosing spondylitis (Bekhterev's disease).

Route of administration and doses:

To accept drug inside during food once a day.

The recommended dosing mode:

- pseudorheumatism: 15 mg a day. depending on medical 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 spondylarthrosis: 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.

Features of use:

It is necessary to be careful at use of drug for patients in whose anamnesis a peptic ulcer of a stomach and duodenum, and also at the patients accepting anticoagulants. At such patients the risk of developing of ulcer and erosive gastrointestinal diseases 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, at patients with cirrhosis, and also 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.

If in the course of treatment there were allergic reactions, it is necessary to see a doctor for the purpose of the solution of a question of the termination of administration of drug.

Side effects:

Bodies of the alimentary system: nausea, vomiting, stomach ache, diarrhea, lock, meteocopes, pervoration of a stomach or intestines, gastrointestinal bleeding, 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 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: konjyuktivit, a sight illegibility.

Integuments: an itch, skin rash, a small tortoiseshell, a mnogoformny exudative erythema, a toxic epidermal necrolysis, the increased photosensitivity.

System of a hemopoiesis: anemia, leukopenia, thrombocytopenia.

Allergic reactions: anaphylactoid reactions, hypostasis of lips and language, allergic vasculitis.

Others: fever.

Interaction with other medicines:

At a concomitant use with other non-steroidal anti-inflammatory drugs the risk of development of cankers of a GIT and gastrointestinal bleeding 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.

At simultaneous use with a methotrexate side effect of the last on the hemopoietic system amplifies.

At simultaneous use with diuretics the risk of development of renal failures increases.

At simultaneous use with Colestyraminum, as a result of binding of a meloksikam, its removal through a GIT increases.

Contraindications:

- hypersensitivity to any component of drug;

- aspirinovy bronchial asthma;

- aggravation of a peptic ulcer of a stomach and 12-perstny gut;

- heavy renal failure;

- active gastrointestinal bleeding; 

- heavy liver failure;

- children's age (up to 15 years);

- pregnancy, lactation period.

With caution drug should be taken to patients of advanced age. In the presence of a digestive tract erosive canker in the anamnesis.

Overdose:

Symptoms: consciousness disturbance, nausea, vomiting, pains in epigastriums, bleeding from a GIT, an acute renal failure, an acute liver failure, an apnoea, an asystolia.

Treatment: gastric lavage, reception of absorbent carbon, symptomatic therapy. The artificial diuresis, urine alkalinization, a hemodialysis are ineffective because of high extent of linkng of a meloksikam with proteins of a blood plasma. There is no specific antidote.

Storage conditions:

To store in the place protected from light, at a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of 7,5 mg and 15 mg.

On 10 tablets in the blister from AI/PVC foil. 2 blisters (20 tablets) (for tablets of 7,5 mg) or 1 or 2 blisters (10 or 20 tablets) (for tablets of 15 mg) in a pack together with the application instruction.