Melbek solution for infection. 15 mg of amp. 1.5 ml No. 3

Pharmacological properties

Pharmacodynamics. to meloksika of group of oksikam, selection inhibitor tsog-2 which contains enolevy acid belongs to npvp. medicament renders the significant anti-inflammatory, analgeziruyushchy and febrifugal action. the mechanism of effect of medicine consists in ability to inhibit biosynthesis of prostaglandins — inflammation mediators thanks to selection inhibition tsog-2. during clinical trials the smaller toxicity of a meloksikam in comparison with other means is revealed considerably (for example Naproxenum, piroxicam and diclofenac) which, to the same extent oppressing tsog-1 and tsog-2, can injure a GIT and kidneys. the coefficient of selectivity of ic50 tsog-1/tsog-2 for a meloksikam — 2, thanks to it medicament shows necessary therapeutic effect and in comparison with non-selective inhibitors tsog becomes more rare the reason of side reactions from a GIT and kidneys. to meloksika does not influence aggregation of thrombocytes and a bleeding time.

Pharmacokinetics. Absorption. Meloksikam is well soaked up in a GIT irrespective of meal. Biological availability of medicine makes 89%, the C _max in blood plasma is reached in 5–6 h and makes depending on the accepted dose 0.4-1 mg/ml after reception of 7.5 mg and 0.8-2.0 mg/ml after reception of 15 mg of drug. Equivalent concentration is reached for the 3-5th day of treatment. Long administration of medicament (more than 1 year) does not cause increase in its concentration in blood plasma in comparison with indicators at the beginning of use.

Distribution. About 99.5% of medicament contact proteins of blood plasma. The volume of distribution averages 11 l. Meloksikam gets into synovial fluid where its concentration is approximately twice lower, than in blood plasma.

Metabolism. Biotransformation happens in a liver by oxidation of methyl groups to formation of 4 inactive metabolites.

Elimination. About 43% of a dose are excreted with urine, other quantity — with bile. 5% of a dose are removed in not changed view with bile. The t _½ medicine makes 20 h

Liver and renal failure have no considerable impact on pharmacokinetics of a meloksikam. The plasma clearance is 8 ml/min. and decreases at elderly people.

Indication

Treatment of the diseases which are followed by a pain syndrome: an osteoarthritis, arthrosis, degenerative diseases of joints, a pseudorheumatism ankylosing a spondylitis.

Use

At adults melbek is applied 1 time a day, washing down with a small amount of liquid.

In an osteoarthritis: 5 mg/days; if necessary the dose can be raised to 15 mg/days

In a pseudorheumatism and an ankylosing spondylitis: 15 mg of 1 times a day; depending on therapeutic effect the dose can be lowered to 7.5 mg of 1 times a day.

to Patients with high risk of development of side effects and to the patient who are on dialysis, treatment it is necessary to begin with a dose 7.5 mg of 1 times a day.

Maximum daily dose of a meloksikam for adults makes 15 mg.

individually.

Contraindication

Hypersensitivity to a meloksikam and also others npvp, a round ulcer of a stomach or duodenum, gastrointestinal bleedings, a heavy liver and renal failure; age up to 12 years; period of pregnancy and feeding by a breast.

Side effects

an abdominal pain, a constipation, a meteorism, diarrhea; anemia, itching, dizziness, headache, peripheral hypostases.

tranzitorny increase in indicators of functional hepatic trials (increase in activity of transferases or concentration of bilirubin in blood plasma), the esophagitis, a round ulcer or gastrointestinal bleedings can Seldom arise; leukopenia and thrombocytopenia; stomatitis, urticaria, sonitus, drowsiness; increase in the ABP, an erythema of the person with feeling of heat, tachycardia; change of functional indicators of kidneys (increase in level of creatinine and/or urea in blood plasma). At a concomitant use of medicament with potential negative influence on marrow cells (especially a methotrexate) development of a pancytopenia is possible.

It is very rare — perforation, hepatitis, a photosensitization, Stephens's syndrome — Johnson, a toxic epidermal necrolysis, asthma attack which arises owing to intake of acetylsalicylic acid, OPN, conjunctivitis, a disorder of vision, a Quincke's disease, anaphylactoid/anaphylactic reactions.

Special instructions

needs to control strictly administration of medicament at patients with oh in the anamnesis. with care it is necessary to apply medicine at conditions of dehydration, to the weakened patients, elderly people sick with heart failure and also those who takes the anticoagulating and antiagregantny drugs.

As well as other NPVP, to meloksika interstitial nephrite, a glomerulonephritis, necrosis of renal nipples or a nephrotic syndrome can irregularly cause. Such complications can arise at patients with HPN, after extensive surgeries (which caused a hypovolemia) and also at patients with cirrhosis.

in case of symptoms of gastrointestinal bleeding, skin changes and also an ulitis or conjunctivitis needs to stop medicament use immediately.

At patients with insignificant or moderate renal failures (clearance of creatinine of 25 ml/min.).

Influence on ability to run vehicles and to work with other mechanisms. There are no data on influence of medicament on ability to run vehicles or to work with difficult mechanisms. In case of developing of dizziness or drowsiness it is necessary to refuse those types of activity which demand psychomotor activity.

Interaction

Melbek can reduce efficiency of antihypertensives (blockers of β-adrenoceptors, inhibitors apf).

At women who use an intrauterine spiral the simultaneous use of the medicament Melbek can reduce its contraceptive action.

should not be accepted at the same time to meloksika and other NPVP (especially acetylsalicylic acid and an ibuprofen) as it can increase risk of ulcerogenic action and gastrointestinal bleeding.

Meloksikam can enhance effect of a tiklopidin and heparin which increases risk of gastrointestinal bleedings.

, considering lithium removal reduction by kidneys under the influence of NPVP that can cause cumulation of lithium and manifestation of its toxic action.

should not be accepted to meloksika along with a methotrexate, considering a possibility of strengthening of toxic action of the last on the system of a hemopoiesis. It is not recommended to apply Melbek together with cyclosporine as the risk of manifestation of nephrotoxic action of the last increases.

Perhaps pharmacokinetic interaction of a meloksikam with other medicaments at a metabolism stage due to their influence on P450 2C9 cytochrome and/or P450 3A4 cytochrome. At simultaneous use the pharmacokinetic interaction of medicament with antacids, digoxin and furosemide is not revealed. Colestyraminum accelerates removal of a meloksikam.

Cannot exclude interactions of medicine with glucose-lowering medicaments for oral administration.

Overdose of a meloksikam is shown by

generally in the form of strengthening of side effects. in this case wash out a stomach and carry out symptomatic treatment. Colestyraminum increases removal of a meloksikam from a GIT. there is no specific antidote.

Storage conditions

At a temperature not above 25 °C.