Aspikam

General characteristics. Structure:

Active agent: meloksikama 7, 5 mg or 15 mg;

Other components: lactoses monohydrate, povidone, кросповидон, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Meloksikam belongs to nonsteroid antiinflammatory drugs of group of oksikam, the selection TsOG-2 inhibitor that in the structure includes enolevy acid; has expressed antiinflammatory, boleuspokaivayushchy and febrifugal actions. The mechanism of effect of medicine consists in ability to oppress biosynthesis of prostaglandins which is mediators an inflammation, thanks to the selection inhibition of TsOG-2. Clinical trials revealed considerably smaller toxicity of a meloksikam compared with other non-steroidal anti-inflammatory drugs (for example: Naproxenum, piroxicam and diclofenac), which, equally suppressing TsOG-1 and TsOG-2, can injure digestive tract and kidneys. The coefficient of selectivity of IC50 TsOG-1/TsOG-2 for a meloksikam makes 2, thanks to it medicine shows desired therapeutic effect and compared with the TsOG non-selective inhibitors makes side reactions from digestive tract and kidneys less often. Meloksikam does not influence aggregation of thrombocytes and a bleeding time.

Pharmacokinetics. Absorption. Meloksikam is well soaked up from digestive tract irrespective of reception of food. Biological availability of medicine makes 89%, the maximum concentration in blood is reached in 4 - 5 hour and makes depending on the accepted dose 0, 4 - 1 mg/ml after reception 7, 5 mg and 0, 8 - 2, 0 mg/ml after reception of 15 mg of medicine. Equilibrium concentration is reached on 3 – the 5th put treatments. Long-term medicine reception (more than one year) does not make increase in its concentration in a blood plasma in comparison with indicators for the beginning of use.

Distribution. About 99, 5% of medicine contact proteins of plasma. The volume of distribution averages 11 l. Meloksikam gets into synovial fluid where its concentration approximately on a half lower, than in a blood plasma.

Metabolism. Biotransformation results in a liver by oxidation of methyl groups with formation of four inactive metabolites.

Elimination (removal). About 43% of a dose are eliminirut with urine, by the rest – with bile. Less than 5% of a dose are removed in an invariable view with bile. The elimination half-life of medicine makes almost 20th hour.
Hepatic unsufficiency and kidneys do not find considerable influence on pharmacokinetics of a meloksikam. The plasma clearance makes 8 ml/minutes, decreases at elderly people.

Indications to use:

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

Route of administration and doses:

Aspikam appoint the adult, accept inside (orally) during food, washing down with a small amount of liquid of 1 times a day.
At an osteoarthritis – it is possible to increase 7, 5 mg a day, if necessary a dose to 15 mg a day.
At a pseudorheumatism and an ankylosing spondylitis apply in a dose 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.
Patients with high risk have development of side effects and that by which carry out dialysis, treatments need to be begun with a dose 7, 5 mg of 1 times a day.
The maximum daily dose of a meloksikam for adults makes 15 mg (2 tablets on 7, 5 mg or 1 tablet on 15 mg).
Duration of a course of treatment is defined individually.

Features of use:

It is necessary to control strictly administration of drug at patients with bronchial asthma in the anamnesis.

With care appoint to the weakened patients, elderly people, patients with heart failure, and also to those which are accepted by anticoagulants and antiagregant.
As well as other non-steroidal anti-inflammatory drugs, drug Aspikam, can cause sporadic intersticial nephrite, a glomerulonephritis, a necrosis of renal nipples or a nephrotic syndrome. To it complications inclined patients with a chronic renal failure, after extensive surgeries (which caused a hypovolemia), and also patients with cirrhosis.
In case of symptoms of gastrointestinal bleeding, skin changes, and also an ulitis or to conjunctivitis it is necessary to stop immediately reception of medicine and to see a doctor.
At patients with the insignificant or moderately expressed renal failures (clearance of creatinine> of 25 ml/minutes) the drug dose can be not reduced.

Influence on ability to manage vehicles and moving mechanisms which need big attention of concentration.
There are no data concerning influence of medicine on ability of driving by transport. In case of emergence dizziness or emergence of drowsiness it is necessary to refuse those types of activity which demand psychomotor activity.

Side effects:

Abdominal pains, locks, meteorism, diarrhea are possible; anemia, itch, dizziness, headache, peripheral hypostases.

Can seldom be observed: tranzitorny increase in indicators of functional hepatic trials (increase in activity of transferases or concentration of bilirubin in blood serum), an esophagitis, a round ulcer or gastrointestinal bleedings; leukopenia and thrombocytopenia; stomatitis, urticaria, sonitus, drowsiness; increase in arterial pressure, 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 a blood plasma). At a concomitant use of drugs with a potential negative impact on marrow (especially a methotrexate) development of a pancytopenia is possible.

Very seldom – perforation, hepatitis, a photosensitization, Stephens-Johnson's syndrome, a toxic epidermal necrolysis, an attack of so-called "aspirinovy" asthma, an acute renal failure, conjunctivitis, a vision disorder, a Quincke's disease, anaphylactoid/anaphylactic reactions.

Interaction with other medicines:

Aspikam can reduce efficiency of antihypertensives (beta adrenoblockers, APF inhibitors).
At women who use an intrauterine spiral simultaneous use of drug Aspikam can reduce its contraceptive action.
It is not necessary to accept at the same time to meloksika and other non-steroidal anti-inflammatory drugs (especially acetylsalicylic acid and an ibuprofen) as it can increase risk of ulcerogenic action and gastrointestinal bleeding.
Meloksikam can strengthen effect of a tiklopidin and heparin that increases risk of gastrointestinal bleedings.
The combined use with lithium salts is not recommended, considering decrease lithium removal by kidneys under the influence of non-steroidal anti-inflammatory drugs that can entail cumulation of lithium and manifestation of its toxic action.
It is not necessary to accept to meloksika along with a methotrexate, considering an opportunity strengthening of toxic action of a methotrexate on system of a hemogenesis.
It is not recommended to apply at the same time Aspikam together with cyclosporine as the risk of manifestations of nephrotoxic action of the last grows.
It is possible pharmacokinetic interaction of a meloksikam and other medicines on metabolism stages due to their influence on CYP 2C9 and/or CYP 3A4. At simultaneous use pharmacokinetic Aspikam of interactions with antacids, digoxin and furosemide is not revealed. Holestiramin accelerates removal of a meloksikam.
It is impossible to exclude interactions of medicine with peroral sugar-lowering means.

Contraindications:

Hypersensitivity to medicine, and also to other non-steroidal anti-inflammatory drugs, a round ulcer of a stomach or duodenum, gastrointestinal bleedings, a heavy liver and renal failure.

Medicine is not used during pregnancy and during the period feeding by a breast, and also at children and teenagers age up to 15 years.

Overdose:

The overdose of a meloksikam is shown generally in a look strengthening of side effects. In this case wash out a stomach and carry out a symptomatic treatment. Holestiramin accelerates removal of a meloksikam in digestive tract. There is no specific antidote.

Storage conditions:

To store in unavailable to children, the dry place, at a temperature of 15 - 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister; on 1,2 or 3 blisters in a cardboard box.