Meloksikam Aveksima

General characteristics. Structure:

Active ingredient: 7,5 mg or 15 mg of a meloksikam.

Excipients: lactoses monohydrate, potato starch, silicon dioxide colloid (aerosil), povidone low-molecular, sodium citrate, K25 povidone, calcium stearate, talc.

Pharmacological properties:

Pharmacodynamics. Non-steroidal anti-inflammatory drug, possesses antiinflammatory, febrifugal, analgeziruyushchy action. Belongs to the class of oksikam; derivative enoliyevy acid.

The action mechanism - inhibition of synthesis of prostaglandins as a result of selective suppression of enzymatic activity of TsOG-2. At appointment in high doses, prolonged use and specific features of an organism of TsOG-2 selectivity decreases. Suppresses synthesis of prostaglandins in the field of an inflammation more than in a mucous membrane of a stomach or kidneys that is connected with rather selective inhibition of TsOG-2. Causes erosive and ulcer gastrointestinal diseases in comparison with non-selective inhibitors of cyclooxygenase less often.

Pharmacokinetics. Absorption from a GIT after intake - 89%. Meal does not influence absorption. Concentration in plasma of a dozozavisim. Time of achievement of Cmax - 5-6 h. Equilibrium concentration is created in 3-5 days. Communication with proteins of plasma - 99%. Passes through gistogematichesky barriers, gets into synovial fluid. Concentration in synovial fluid - 50% of concentration in plasma. Metabolism in a liver - to inactive metabolites.

It is removed through intestines and kidneys (approximately in an equal proportion), in not changed look - 5% of a daily dose (through intestines). T1/2 is 20 h. Plasma clearance - on average 8 ml/min. (decreases at advanced age).

Indications to use:

— pseudorheumatism;

— osteoarthrosis;

— an ankylosing spondylitis (Bekhterev's disease) both the other inflammatory and degenerative diseases of joints which are followed by a pain syndrome.

It is intended for symptomatic therapy, reduction of pain and an inflammation at the time of use, does not influence progressing of a disease.

Route of administration and doses:

Inside, during food, in a daily dose of 7.5-15 mg. The maximum daily dose - 15 mg, at the patients with a heavy renal failure who are on a hemodialysis - 7.5 mg. At insignificant or moderate depression of function of kidneys (KK more than 30 ml/min.), and also at cirrhosis in a stable clinical condition of dose adjustment it is not required. The initial dose at patients with the increased risk of side effects makes 7.5 mg/days.

Features of use:

Use of drug is contraindicated to patients from a chronic renal failure, not exposed to dialysis (KK less than 30 ml/min.), the progressing diseases of kidneys.

With care: chronic renal failure (KK of 30-60 ml/min.).

The maximum daily dose at the patients with a heavy renal failure who are on a hemodialysis - 7.5 mg.

Use for children. Drug use is forbidden to children aged up to 12 years.

Use for elderly patients. To take with caution at advanced age.

At emergence of round ulcers or gastrointestinal bleeding, development of side effects from skin and mucous membranes drug should be cancelled.

At patients with the reduced volume of the circulating blood and reduced glomerular filtering (dehydration, chronic heart failure, cirrhosis, a nephrotic syndrome, clinically expressed diseases of kidneys, reception of diuretics, dehydration after big surgeries) emergence of clinically expressed chronic renal failure which is completely reversible after drug withdrawal (at such patients in an initiation of treatment it is necessary to monitorirovat a daily urine and function of kidneys) is possible. At permanent and essential increase in activity of "hepatic" transaminases and change of other indicators of function of a liver drug it is necessary to cancel and conduct a research of functions of a liver.

At patients with the increased risk of side effects treatment begin 7.5 mg with a dose. In an end-stage of a chronic renal failure at the patients who are on dialysis, the dose should not exceed 7.5 mg/days. During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions (at emergence of dizzinesses and drowsiness). For decrease in risk of development of the undesirable phenomena from a GIT it is necessary to use a minimal effective dose the greatest possible short course.

Side effects:

From the alimentary system: more than 1% - dyspepsia, including nausea, vomiting, abdominal pains, a lock, a meteorism, diarrhea; 0.1-1% - passing increase in activity of "hepatic" transaminases, a hyperbilirubinemia, an eructation, an esophagitis, a gastroduodenal ulcer, bleeding from digestive tract (including hidden), stomatitis; less than 0.1% - perforation of a GIT, colitis, hepatitis, gastritis.

From bodies of a hemopoiesis: more than 1% - anemia; 0.1-1% - change of cellular composition of blood, including a leukopenia, thrombocytopenia.

From integuments: more than 1% - an itch, skin rash; 0.1-1% - a small tortoiseshell; less than 0.1% - a photosensitization, violent rashes, a multiformny erythema, including Stephens-Johnson's syndrome, a toxic epidermal necrolysis.

From respiratory system: less than 0.1% - a bronchospasm.

From a nervous system: more than 1% - dizziness, a headache; 0.1-1% - вертиго, a sonitus, drowsiness; less than 0.1% - confusion of consciousness, a disorientation, emotional lability.

From cardiovascular system: more than 1% - peripheral hypostases; 0.1-1% - increase in the ABP, a heart consciousness, "inflows" of blood to face skin.

From an urinary system: 0.1-1% - a giperkreatininemiya and/or increase in concentration of urea in blood serum; less than 0.1% - an acute renal failure; connection with reception of a meloksikam is not established - intersticial nephrite, an albuminuria, a hamaturia.

From sense bodys: less than 0.1% - conjunctivitis, a vision disorder, including a sight illegibility.

Allergic reactions: less than 0.1% - a Quincke's disease, anaphylactoid/anaphylactic reactions.

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; increases concentration of ions of lithium in plasma at simultaneous use with lithium drugs; reduces efficiency of vitaminnomineralny complexes, hypotensive medicines; indirect anticoagulants, тиклопидин, heparin, trombolitik increase risk of bleedings; the methotrexate strengthens miyelodepressivny action; diuretics increase risk of development of renal failures; cyclosporine strengthens nephrotoxic action; Colestyraminum accelerates removal.

Miyelotoksichny medicines strengthen manifestations of a gematotoksichnost of drug

Contraindications:

— hypersensitivity (including to non-steroidal anti-inflammatory drugs of other groups), a full or incomplete combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including in the anamnesis);

— a peptic ulcer of a stomach and duodenum (in an aggravation phase);

— a chronic renal failure at the patients who are not exposed to dialysis (KK less than 30 ml/min.);

— active gastrointestinal bleeding;

— the progressing diseases of kidneys,

— heavy liver failure or active disease of a liver;

— a state after performing aortocoronary shunting;

— the confirmed hyperpotassemia;

— inflammatory diseases of intestines;

— children's age (up to 12 years);

— pregnancy;

— lactation period;

— deficit of lactase;

— lactose intolerance;

— glyukozo-galaktozny malabsorption.

With care. Advanced age, coronary heart disease, chronic serdecheny insufficiency, cerebrovascular diseases, dislipidemiya/a lipidemia, a diabetes mellitus, diseases of peripheral arteries, smoking, a chronic renal failure (clearance of creatinine of 30-60 ml/min.), GIT cankers in the anamnesis, existence of an infection of N. of pylori, prolonged use of non-steroidal anti-inflammatory drugs, alcoholism, heavy somatopathies, a concomitant use of peroral glyukokortikosteriod (including Prednisolonum), anticoagulants (including warfarin), antiagregant (including klopidogret), selective serotonin reuptake inhibitors (including a tsitaloprama, fluoxetine, a paroksetin, sertraline).

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 plasma. There is no specific antidote.

Storage conditions:

To store drug in dry, protected from light and the place, unavailable to children, at a temperature not above 25 °C. Period of validity 3 years. Not to use after expiry date, specified on packaging.

Issue conditions:

According to the recipe

Packaging:

10 pieces - planimetric strip packagings (1) - packs cardboard.
10 pieces - planimetric strip packagings (2) - packs cardboard.
10 pieces - planimetric strip packagings (3) - packs cardboard.
10 pieces - planimetric strip packagings (4) - packs cardboard.
10 pieces - planimetric strip packagings (5) - packs cardboard.
20 pieces - banks polymeric (1) - packs cardboard.