Ревмоксикам®

General characteristics. Structure:

Deystvuyushcheeveshchestvo: meloxicam;

1 tablet contains a meloksikam of 7,5 mg or 15 mg;

vspomogatelnyeveshchestvo: lactose, monohydrate; cellulose microcrystallic; sodium citrate; povidone; кросповидон; silicon dioxide colloid anhydrous (aerosil), magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Drug belongs to nonsteroid antiinflammatory medicines of a class of oksikam, is the selection TsOG-2 inhibitor. Has antiinflammatory, analgeziruyushchy and febrifugal effect. The mechanism of action is connected with inhibition of synthesis of prostaglandins (the known mediators of an inflammation) owing to oppression of enzymatic activity of TsOG-2 in the inflammation center; slightly influences TsOG-1 that reduces risk of development of side effect.

Pharmacokinetics. Meloksikam after intake is well absorbed from a digestive tract. Bioavailability makes 89%. Stable concentration is reached on 3 - the 5th days. The use of food does not influence absorption of a meloksikam. In plasma of 99% of a meloksikam is in the look connected with proteins. Concentration of a meloksikam in synovial fluid makes 50% of concentration in a blood plasma. Meloksikam is almost completely metabolized to inactive metabolites in a liver. The elimination half-life of a meloksikam makes 20 h. The plasma clearance averages 8 ml/min. Meloksikam is brought by kidneys and through intestines approximately in equal proportions. A liver and renal failure easy and moderate severity significantly do not influence pharmacokinetic parameters of a meloksikam.

Pharmaceutical characteristics

 

Main physical and chemical properties: tablets of yellow color, with a flat surface, a facet and risky. On a surface of a tablet the mramornost is allowed.

Indications to use:

Symptomatic treatment:

- a pain syndrome at osteoarthrites, arthroses, degenerative joint diseases;

- pseudorheumatisms;

- ankylosing spondylites.

Route of administration and doses:

Adult.

Osteoarthrites: the daily dose makes 7,5 mg, in need of it increase up to        15 mg/days.

Pseudorheumatisms: drug is appointed on 15 mg/days, at achievement of positive therapeutic effect the dose can be lowered to 7,5 mg/days.

Ankylosing spondylites: drug is appointed on 15 mg/days, at achievement of positive therapeutic effect the dose can be lowered to 7,5 mg/days.

At patients with the increased risk of side reactions the initial medical dose makes 7,5 mg/days.

At the patients with a heavy renal failure who are on a hemodialysis, the dose should not exceed 7,5 mg/days.

It is necessary to apply the smallest effective daily dose and the smallest duration of treatment as with increase in a dose and duration of treatment the risk of development of side reactions increases.

The maximum recommended daily dose for children over 12 years makes 0,25 mg/kg of body weight.

The maximum recommended daily dose of Revmoksikam of 15 mg.

The combined use: the general daily dose of Revmoksikam at its use in the form of tablets and suppositories should not exceed 15 mg.

Considering that the dose for children is younger than 12 years it is not established, it is necessary to be limited to drug use only for children 12 years and adults are more senior.

The pill should be taken during food, not to chew, wash down with water or other liquid.

Duration of a course of treatment is established individually depending on the course of a disease and efficiency of the carried-out therapy.

Features of use:

It is necessary to watch attentively a condition of patients at drug use (as well as other NPVS) at patients:

- with gastrointestinal diseases and in case of simultaneous use of anticoagulants. It is forbidden to appoint Revmoksikam, to patients with a round ulcer or gastrointestinal bleeding. At any time in the course of treatment at existence or without the previous symptoms, serious gastrointestinal diseases in the anamnesis, potentially fatal gastrointestinal bleedings, an ulcer or perforation can develop the Most serious effects observed at people of advanced age;

- with cardiovascular diseases or with risk factors of development of such diseases. Non-steroidal anti-inflammatory drugs can increase risk of emergence of the serious cardiovascular trombotichesky phenomena, a myocardial infarction and stroke which can be fatal. At increase in duration of treatment this risk can increase.

NPVS can strengthen a delay of sodium, potassium and water and to affect natriuretic effects of diuretics. As a result, at predisposed patients heart failure or arterial hypertension can arise or amplify. Carrying out clinical monitoring is recommended to such patients.

- with a reduced renal blood-groove as use of NPVS (NPVS inhibit synthesis of renal prostaglandin that plays an important role in maintenance of a renal blood-groove) can serve as the reason of the renal failure passing at the termination of antiinflammatory therapy by nonsteroid means.

The greatest risk of such reaction takes place at patients of advanced age, with dehydration, with chronic heart failure, cirrhosis, a nephrotic syndrome, chronic diseases of kidneys which receive the accompanying therapy with diuretic drugs, APF-inhibitors or antagonists angiotensin II the turning receptors, or after extensive surgical interventions which led to a hypovolemia. Such patients need control of a diuresis and function of kidneys at the beginning of therapy. In isolated cases of NPVS can lead to intersticial nephrite, a glomerulonephritis, a renal medullary necrosis or to development of nephrotic syndromes.

At treatment of NPVS separate cases of increase in level of transaminases or other indicators of function of a liver which in the majority were insignificant and temporary are described. At a resistant and essential aberration treatment by Revmoksikam should be stopped and carried out control tests. At clinically stable patients with cirrhosis it is not necessary to reduce Revmoksikam's doses.

The weakened patients need more careful observation as side effects at them have more difficult character. As well as at treatment by other NPVS, it is necessary to appoint with care them the patient of advanced age at whom depression of function of kidneys, a liver and heart is more probable.

Meloksikam, as well as any other NPVS, can mask symptoms of the basic infectious disease.

Use of a meloksikam, as well as other medicines inhibiting synthesis of cyclooxygenases / prostaglandins can influence fertilization and therefore it is not recommended for use for women who try to become pregnant. It is necessary to refuse reception of a meloksikam to women at whom fertilization is complicated or which undergo inspection concerning infertility.

Seldom or never at use of non-steroidal anti-inflammatory drugs, serious skin reactions (some of them were fatal) including exfoliative dermatitis, Stephens-Johnson's syndrome and a toxic epidermal necrolysis were observed. The high risk of emergence of such reactions is observed in an initiation of treatment, at the same time in most cases such reactions appeared within the first month of treatment. At the first emergence of skin rashes, damages of mucous membranes or other signs of hypersensitivity it is necessary to stop Revmoksikam's use. Because of possible emergence of side effects with localization on skin and mucous membranes it is necessary to pay special attention to emergence of the corresponding symptoms. At emergence of side effects treatment by Revmoksikam should be stopped.

The structure of tablets of Revmoksikam (on 7,5 mg and 15 mg) includes lactose, and at introduction of the maximum recommended dose to an organism 92,34 mg of lactose at Revmoksikam's dose of 7,5 mg and 122,70 mg of lactose at Revmoksikam's dose of 15 mg get. Therefore this drug is not recommended to be accepted to patients with inborn intolerance of a galactose, with deficit of lactase or disturbance of absorption of glucose or a galactose.

Ability to influence speed of response at control of motor transport or work with other mechanisms

 

There are no data on influence of drug on ability to drive the car or to work with other mechanisms. It is recommended to the patients noting at themselves disorders of function of sight, drowsiness or other disturbances of the central nervous system to refuse such occupations.

Side effects:

Below the undesirable phenomena which communication using drug Revmoksikam was regarded as possible are described. It is supposed that the frequency of these phenomena makes 0,1%.

From system of breath: it is less than 0,1% - emergence of attacks of asthma in persons with hypersensitivity to acetylsalicylic acid or on other NPVS.

From the alimentary system:> 1% - dyspepsia, nausea, vomiting, a meteorism, diarrhea, a lock, intestinal colic; 0,1-1% - an esophagitis, stomatitis, the latent or macroscopically visible gastrointestinal bleedings, are rare – erosive cankers of a digestive tract, passing abnormal liver functions (increase in activity of hepatic transaminases or bilirubin); <0,1% - perforation of a GIT, colitis, gastritises, hepatitis.

From the central nervous system:> 1% - a headache; 0,1-1% - dizziness, a sonitus, drowsiness; <0,1% - lability of mood, irritability, a disorientation, confusion of consciousness.

From an organ of sight: <0,1% – sight dysfunctions (a sight illegibility), conjunctivitis.

From cardiovascular system:> 1% - hypostases; 0,1-1% - increase in arterial pressure, a heart consciousness, inflows.

From an urinary system: 0,1-1% - change of indicators of function of kidneys (increase in creatinine and/or urea of blood serum); <0,1% - an acute renal failure, frustration of an urination, including an acute ischuria.

From system of a hemopoiesis:> 1% - anemia; 0,1-1% - a leukopenia, thrombocytopenia, changes of a leukocytic formula. Co-administration of potentially myelotoxic drug, especially a methotrexate, can lead to development of a pancytopenia.

Dermatological reactions:> 1% - an itch, skin rash; 0,1-1% - a small tortoiseshell; <0,1% - a photosensitization. Development of a syndrome of Stephens-Johnson, a toxic epidermal necrolysis, violent reactions, a multiformny erythema is in rare instances possible;

Allergic reactions: <0,1% - a Quincke's disease, anaphylactic and/or anaphylactoid reactions.

Interaction with other medicines:

Revmoksikam together with other NPVS can increase risk of developing of ulcers of a mucous membrane of a GIT and gastrointestinal bleedings owing to their synergism. Joint appointment of Revmoksikam and other NPVS is not recommended.

Together with anticoagulants, antiagregant, thrombolytic means, heparin and selective serotonin reuptake inhibitors Revmoksikam increases risk of development of bleedings because of braking of function of thrombocytes. If it is impossible to avoid their simultaneous use, it is necessary to control a condition of the patient.

Revmoksikam can reduce renal excretion of lithium that leads to increase in its concentration in a blood plasma to toxic level.

At simultaneous use with a methotrexate the negative impact on the hemopoietic system (risk of development of anemia and a leukopenia) therefore periodic control of indicators of blood is necessary increases.

There are data that drug can reduce efficiency of intrauterine contraceptives, but this statement demands a further research and confirmation.

At simultaneous use with Revmoksikam of a holestiramin removal of a meloksikam accelerates.

Revmoksikam can reduce efficiency of anti-hypertensive drugs (b-blockers, APF inhibitors) that is connected with the inhibiting impact on vazodilatatorny prostaglandins.

Together with diuretics there can be a risk of development of an acute renal failure therefore it is necessary to control function of kidneys and to support the adequate level of hydration.

NPVS and antagonists angiotensin of the II turning receptor, and also ACE inhibitors render synergy effect on reduction of glomerular filtering. At patients with the existing disturbance of renal function it can lead to an acute renal failure.

NPVS influencing renal prostaglandins increase nephrotoxicity of cyclosporine that demands the strengthened control of function of kidneys at simultaneous use of drugs.

Meloksikam almost completely collapses by hepatic metabolism which about two thirds pass with the participation of cytochrome (CYP) P450 and one third - by peroksidazny oxidation.

Perhaps pharmacokinetic interaction of Revmoksikam and other drugs at a metabolism stage due to their influence on the RMS 2C9 and/or RMS 3A4.

At a concomitant use of Revmoksikam with antacids, Cimetidinum, digoxin and furosemide of interaction at the pharmacokinetic level it is not revealed.

It is impossible to exclude interactions of drug with peroral anti-diabetic means.

Contraindications:

Hypersensitivity to a meloksikam and other non-steroidal anti-inflammatory drugs, including acetylsalicylic acid;
existence of the symptoms (connected using acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (NPVS)): bronchial asthma, nasal polyps, a Quincke's disease or small tortoiseshells in an anemneza as reactions of cross hypersensitivity are possible;
ulcers of a gastrointestinal path / perforation (active form or their recent emergence);
active form of inflammatory diseases of a large intestine (disease Krone or ulcer colitis);
heavy liver failure;
the renal failure which is not subject to a hemodialysis;
any frustration with bleedings, manifest gastrointestinal bleeding, recent cerebrovascular bleeding;
heavy uncontrollable heart failure;
children up to 12 years;
period of pregnancy and breastfeeding;
treatment for elimination of postoperative pain at aortocoronary shunting.
inborn disturbances at which inactive components of drug can be harmful (see the section "Features of Use").

Overdose:

At overdose strengthening of the described side effects is possible. It is necessary to wash out a stomach, to carry out symptomatic therapy. There are no specific antidotes and antagonists.

Use during pregnancy and feeding by a breast

 

In spite of the fact that the teratogenic effect during preclinical trials is not revealed, meloksika should not apply during pregnancy and during breastfeeding.

Children

 

Considering that the dose for children is not established, it is necessary to be limited to drug use only for children 12 years and adults are more senior. The maximum recommended daily dose for children over 12 years makes 0,25 mg/kg of body weight.

Storage conditions:

Period of validity. 2 years. Not to use drug after the termination of the period of validity specified on packaging. To store in the unavailable to children, protected from light place at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister, on 1 or 2 blisters in a pack.