Producer: JSC VEROPHARM Russia
Code of automatic telephone exchange: M01AC06
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active agent: to meloksika of 7,5 mg and 15 mg. Excipients: sodium citrate dihydrate, lactose anhydrous (sugar milk), cellulose microcrystallic, povidone (коллидон, polyvinylpirrolidone 250000, silicon dioxide colloid (aerosil), кросповидон (полипласдон EL-10 X), magnesium stearate.
Description: tablets of light yellow color of a ploskotsilindrichesky form.
Pharmacodynamics. Meloksikam — the non-steroidal anti-inflammatory drug possessing anesthetic, antiinflammatory and febrifugal action. The action mechanism — the selection braking of enzymatic activity of cyclooxygenase-2 (TsOG-2) participating in biosynthesis of prostaglandins in the field of an inflammation. At appointment in high doses, prolonged use and specific features of an organism of TsOG2 selectivity can decrease. Suppresses synthesis of prostaglandins in the field of an inflammation more than in a mucous membrane of digestive tract and kidneys.
Pharmacokinetics. It is well soaked up from digestive tract, absolute bioavailability of a meloksikam — 89%, does not depend on meal. When using drug inside in doses of 7,5 and 15 mg, its concentration in dozozavisima plasma. 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 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, (Cmin and Cmax values are given, respectively). Meloksikam gets through gistogematichesky barriers, concentration in synovial fluid reaches 50% of the maximum concentration of drug in plasma. Almost it is completely metabolized in a liver with participation of CYP 2C9, CYP ZA4, peroxidase with formation of four inactive derivatives in the pharmacological relation. 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 the size of a daily dose are removed, in urine in not changed 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. The liver or renal failure of moderate severity has no significant effect on pharmacokinetics of a meloksikam.
Indications to use:
Route of administration and doses:
Drug is accepted 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 spondylarthritis: 15 mg a day. The maximum daily dose should not exceed 15 mg.
At patients with the increased risk of development of side effects the initial dose should not exceed 7,5 mg a day.
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 and 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, 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 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.
Bodies of the alimentary system: nausea, vomiting, abdominal pain, diarrhea, 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, hyperbilirubinemia, eructation.
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, drowsiness, emotional lability.
Urinogenital system: hypostases, intersticial nephrite, a renal medullary necrosis, an uric infection, a proteinuria, a hamaturia, a renal failure, a giperkreatininemiya and/or increase in urea in blood serum.
Organs of sight: konjyuktivit, a sight illegibility.
Integuments: an itch, skin rash, a small tortoiseshell, a mnogoformny exudative erythema (in t. h Stephens-Johnson's syndrome), a toxic epidermal necrolysis (Lyell's disease), the increased photosensitivity.
System of a hemopoiesis: anemia, leukopenia, thrombocytopenia.
Allergic reactions: anaphylactoid reactions (in t. h acute anaphylaxis), hypostasis of lips and language, allergic vasculitis.
Interaction with other medicines:
- At simultaneous use with other non-steroidal anti-inflammatory drugs (including salicylates) the risk of emergence erozivno of -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 increase in level of lithium in plasma is possible (control of concentration of lithium in blood is recommended);
- At simultaneous use with a methotrexate gematotoksichesky action of the last amplifies (periodic control of the general blood test is shown);
- At simultaneous use with diuretics and with cyclosporine there is potentiality of development of an acute renal failure in patients with dehydration;
- 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).
Holestiramin, connects to meloksika, his removal through a GIT as a result amplifies.
- hypersensitivity to any component of drug;
- aspirinovy bronchial asthma;
- aggravation of a peptic ulcer of a stomach and duodenum
- gastrointestinal, cerebrovascular bleeding or other bleeding;
- a heavy renal failure (if the hemodialysis is not carried out);
- heavy liver failure;
- heavy heart failure;
- children aged up to 15 years;
- lactation period.
Drug should be used with care at patients of advanced age a digestive tract erosive canker in the anamnesis.
Symptoms: strengthening of side effects. 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.
List B. In the dry, protected from light place unavailable to children, at a temperature not above 25 °C. Period of validity 2 years. Not to use after a period of validity.
According to the recipe
Tablets on 7,5 mg and 15 mg. On 10 tablets in a blister strip packaging. On 20 tablets in bank of light-protective glass. On 20 tablets in bank or a bottle from polymeric materials. Each can or a bottle or 1 blister strip packaging for tablets 15 mg or 2 blister strip packagings for tablets of 7,5 mg or 15 mg together with the application instruction in a pack from a cardboard.