Мелбек®

General characteristics. Structure:

Active ingredients: 15 mg of a meloksikam.

Excipients: меглумин, гликофурол, half-oxameasures 188, glycine, sodium chloride, 1 M solution of sodium of hydroxide or 1 M acid chlorohydrogen, water for injections.

Pharmacological properties:

Pharmacodynamics. Мелбек® is non-steroidal anti-inflammatory drug (NPVS), the selection TsOG-2 inhibitor. Belongs to the class of oksikam, is derivative enoliyevy acid. Has antiinflammatory, analgeziruyushchy and febrifugal effect. The mechanism of action is connected with decrease in synthesis of prostaglandins as a result of oppression of activity of cyclooxygenase. Meloksikam more influences TsOG-2 participating in synthesis of prostaglandins in the center of an inflammation and slightly influences TsOG-1.

Pharmacokinetics. At intramuscular introduction to meloksika it is soaked up completely, peak concentration is observed in 60 min. Concentration in a blood plasma at introduction of a meloksikam in the range of doses of 5-30 mg/days of a dozozavisim. Equilibrium concentration is reached for the 3-5th days from an initiation of treatment.

The average volume of distribution of a meloksikam makes about 10 l. 99.4 the % of a meloksikam contacts plasma blood proteins (preferential with albumine). Concentration in synovial fluid makes 50% of concentration in a blood plasma. Meloksikam is almost completely metabolized to inactive metabolites in a liver.

Average value of an elimination half-life (t1/2) makes from 15 to 20 h. The plasma clearance of drug averages 8 ml/min. 

Meloksikam is brought by kidneys and through intestines approximately in equal ratios. A liver and renal failure of easy and average degree significantly do not influence pharmacokinetic parameters of a meloksikam.

Indications to use:

For an initial and short-term symptomatic treatment at inflammatory and degenerative diseases of the joints which are followed by a pain syndrome including:

- pseudorheumatism,

- osteoarthritis.

Route of administration and doses:

Drug is appointed the adult. Appoint 0.75 - 1.5 ml (7.5-15 mg of a meloksikam) of 1 times in days in oil (deeply). The mode of dosing is set individually taking into account intensity of inflammatory process and expressiveness of a pain syndrome.

Use of an injection form of drug is possible only for the first 2-3 days of treatment then pass to reception of peroral dosage forms of a meloksikam. The recommended daily dose – 15 mg/days. The maximum daily dose - 15 mg/days.

Features of use:

МЕЛБЕК®, solution for injections should not be mixed in one syringe with other drugs. At use of an injection form of drug and diuretic means the risk of development of an acute renal failure in patients with dehydration therefore it is necessary that patients accepted enough liquid increases.

With care it is appointed to patients with gastrointestinal diseases and to the patients receiving anticoagulants. When developing gastrointestinal bleedings drug should be cancelled.

Patients with a renal failure have to be under special control. It is connected with the fact that excretion of metabolites is carried out by kidneys.

At patients with a reduced renal blood-groove and reduced general blood circulation use of Melbek® can lead to clinically expressed renal failure which is reversible at drug withdrawal. In most cases, patients with symptoms of dehydration, congestive heart failure, cirrhosis, a nephrotic syndrome, diseases of kidneys and the patients receiving diuretics and APF inhibitors, patients with a hypovolemia after big surgeries are subject to risk of development of this complication. At this category of patients in an initiation of treatment it is necessary to watch a daily urine and function of kidneys carefully. In rare instances drug can cause intersticial nephrite, a glomerulonephritis, a renal medullary necrosis and development of a nephrotic syndrome.

Before an initiation of treatment of Melbek® patients with symptoms of hepatic dysfunction have to be informed on possible complications.

At use of Melbek® increase in activity of transaminases and other indicators of function of a liver can be observed, these changes are insignificant and have reversible character. If permanent and essential increase in these indicators is observed, then drug should be cancelled.

It is necessary to appoint with care drug to patients of advanced age. At use of Melbek® there can be anaphylactoid reactions at which rendering the emergency help is necessary.

At use of Melbek® anemia owing to a delay of liquid, the concealed or plentiful gastrointestinal hemorrhages or, so-called, effect of an erythrogenesis which is insufficiently described can sometimes develop. At emergence of symptoms of anemia, especially at the patients accepting Melbek® for a long time it is necessary to control the level of hemoglobin and a hematocrit. The drugs inhibiting biosynthesis of prostaglandins can exert impact on function of thrombocytes and vascular reaction, causing bleeding.

Мелбек® suppresses aggregation of thrombocytes, thereby, increasing a bleeding time. Also can break function of thrombocytes, in particular, to suppress coagulation. In this regard such patients, and also the patients accepting anticoagulants along with Melbek® have to be under special control.

Liquid delay also swelled were noted at a number of the patients receiving Melbek®. Therefore use of Melbek® for patients with heart failure, hypertensia or hypostases, has to be carried out with extra care.

Features of influence of medicine on ability to manage the vehicle or potentially dangerous mechanisms. Certain clinical tests for the purpose of identification of effect of drug for attention and speed of reactions were not carried out. However at development of such by-effects as dizziness and blackout, is recommended to refrain from the driving of the car and other types of activity demanding the increased concentration of attention.

Treatment by drug is not recommended to the patients with a renal failure who is on a hemodialysis.

Side effects:

- stomatitis, eructation, nausea, vomiting, abdominal pains, meteorism,  esophagitis, gastritis, digestive tract erosive cankers, concealed or explicit hemorrhages, colitis, diarrhea, lock;

- passing changes of activity of transaminases, level of bilirubin and other indicators of function of a liver;

- anemia, leukopenia, agranulocytosis, thrombocytopenia;

- photosensitization;

- cough, upper respiratory tract infections, acute disorder of bronchial passability (bad attacks of bronchial asthma);

- a headache, dizziness, a ring in ears, blackout, sleeplessness, drowsiness, orientation disturbance, change of mood;

- hypostases, increase in the ABP, heartbeat, "inflows";

- change of indicators of function of kidneys (increase in creatinine and/or urea of blood serum), acute renal failure, interstinal nephrite, glomerulonephritis, renal medullary necrosis, nephrotic syndrome;

- reactions of immediate hypersensitivity (including anaphylactic and anaphylactoid reactions), itch, skin rash, Quincke's disease, small tortoiseshell, violent reactions (mnogoformny erythema, Stephens-Johnson's syndrome, toxic epidermal necrolysis);

- conjunctivitis, vision disorders (in sight t.ch.ostrota) and hearing;

- arthralgia, dorsodynia;

- puffiness, morbidity in an injection site.

Interaction with other medicines:

At co-administration of Melbek® with salicylates and other non-steroidal anti-inflammatory drugs the risk of development of ulcer damages and bleedings from digestive tract increases. At combined use of Melbek® and anticoagulants, the tiklopidina, heparin, trombolitik raises risk of development of gastrointestinal bleedings.

Мелбек® can lead to increase in concentration of lithium in blood at use with lithium-containing drugs.

At joint appointment with a methotrexate and other potentially miyelotoksichny drugs the risk of development of a pancytopenia increases.

Simultaneous use of Melbek® and diuretics can lead to development of an acute renal failure in patients with symptoms of dehydration of an organism. It is necessary to compensate dehydration and to watch function of kidneys.

Мелбек® weakens effect of β-adrenoblockers, APF inhibitors, vazodilatator and diuretics.

Holestiramin considerably increases clearance of a meloksikam. Simultaneous use with cyclosporine can lead to nephrotoxicity strengthening as Melbek® reduces synthesis of prostaglandins synthesized in kidneys.

NPVS can cause a delay of sodium, potassium, liquid and to weaken action of saluretics. As a result at predisposed patients purpose of NPVS can lead to progressing of heart failure and arterial hypertension

At combined use of warfarin or its analogs with Melbek®, it is necessary to exercise careful control of a picture of blood, in view of the increased risk of development of bleeding.

There are messages that NPVS reduce efficiency of intrauterine contraceptives.

Combined use of 200 mg of Cimetidinum does not influence pharmacokinetics of a single dose of a meloksikam.

Digoxin does not exert considerable impact on pharmacokinetics of a meloksikam. It is impossible to exclude a possibility of medicinal interaction of a meloksikam with hypoglycemic means.

Contraindications:

- hypersensitivity to a meloksikam;

- bronchial asthma, polyposes mucous a nose, the Quincke's disease or urtikarny rashes caused by reception of acetylsalicylic acid or other NPVS;

- a peptic ulcer of a stomach and duodenum in an aggravation phase;

- heavy liver and renal failure;

- pregnancy and period of a lactation;

- children's and teenage age up to 18 years.

Overdose:

Symptoms: slackness, block, drowsiness, nausea, vomiting, pain in epigastric area, gastrointestinal bleeding, anaphylactoid reactions; symptoms of a serious poisoning: increase in arterial pressure, acute renal failure, abnormal liver function, respiratory depression, coma, convulsions, vascular collapse and cardiac standstill.

Treatment: there is no specific antidote, the symptomatic and supporting treatment. The artificial diuresis, urine alkalization, a hemodialysis or hemoperfusion are ineffective (at a meloksikam high extent of linkng with proteins of a blood plasma).

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. To store the place, unavailable to children! Period of storage 2 years. Not to apply after a period of storage.

Issue conditions:

According to the recipe

Packaging:

Solution for intramuscular injections, 1,5 ml. On 3 ampoules in a blister strip packaging from a PVC film together with the application instruction in the state and Russian languages place in a pack from a cardboard with the hologram of manufacturing firm.