Амелотекс®

General characteristics. Structure:

Active agent to meloksika – 15 mg
excipients: меглумин, glycofurfural, half-oxameasures 188, sodium chloride, глицерол, sodium hydroxide solution of 1 M, water for injections.

Description: transparent or with easy opalescence liquid of color, yellow with a greenish shade.

Pharmacological properties:

Pharmacodynamics. Non-steroidal anti-inflammatory drug, possesses antiinflammatory, febrifugal, analgetic action.

Selectively inhibits enzymatic activity of cyclooxygenase-2. Suppresses synthesis of prostaglandins in the field of an inflammation more than in a mucous membrane of a stomach or kidneys. Causes digestive tract erosive cankers less often.

Belongs to the class of oksikam; derivative enoliyevy acid.

Pharmacokinetics. Communication with proteins of plasma – 99%. Passes through gistogematichesky barriers, gets into synovial fluid. Concentration in synovial fluid reaches 50% of the maximum concentration in plasma.

It is removed equally through intestines and kidneys, it is preferential in the form of metabolites. Through intestines in not changed look less than 5% of the size of a daily dose are removed, in urine in not changed look drug is found only in trace quantities. The elimination half-life (T1/2) of a meloksikam makes 15-20 hours. The plasma clearance averages 8 ml/min. At elderly people the clearance of drug decreases. Distribution volume low also averages 11 l.

The liver or renal failure of moderate severity has no significant effect on pharmacokinetics of a meloksikam.

Indications to use:

- pseudorheumatism;
- osteoarthrosis;
- ankylosing spondylarthritis (Bekhterev's disease);
- the inflammatory and degenerative diseases of joints which are followed by a pain syndrome.

Route of administration and doses:

Intramusculary, it is deep – on 7,5 – 15 mg of 1 times a day. At insignificant or moderate depression of function of kidneys (clearance of creatinine more than 25 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.

The maximum daily dose - 15 mg, at the patients with a heavy renal failure who are on a hemodialysis - 7,5 mg.

Features of use:

At emergence of round ulcers or gastrointestinal bleeding, development of side effects from skin and mucous membranes drug should be cancelled. At patients with reduction of volume of the circulating blood and reduced glomerular filtering (dehydration, chronic heart failure, 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 transaminases and change of other indicators of function of a liver drug should be cancelled and carried out control tests. 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).

Side effects:

From the alimentary system: nausea, vomiting, eructation, abdominal pain, locks or diarrhea, meteorism, increase in activity of "hepatic" transaminases, hyperbilirubinemia, stomatitis, digestive tract erosive cankers, esophagitis, gastritis, colitis, perforation of bodies of digestive tract, gastrointestinal bleeding (hidden or explicit), hepatitis.

From a nervous system: dizziness, вертиго, headache, sonitus, confusion of consciousness, drowsiness, disorientation, emotional lability.

From respiratory system: bronchospasm.

From bodies of a hemopoiesis: anemia, leukopenia, thrombocytopenia.

From cardiovascular system: peripheral hypostases, increase in arterial pressure, "inflows" of blood to face skin and an upper part of a thorax, heartbeat.

From an urinary system: hypostases, a giperkreatininemiya, increase in concentration of urea in blood serum. In rare instances – an acute renal failure, intersticial nephrite, an albuminuria, a hamaturia.

From sense bodys: conjunctivitis, vision disorder including illegibility of sight.

From integuments: itch, skin rash, small tortoiseshell, photosensitization, violent rashes, multiformny erythema, toxic epidermal necrolysis.
Allergic reactions: Quincke's disease, anaphylactoid, anaphylactic reactions.
Local reactions: burning and pain in the place of an injection are possible.

Interaction with other medicines:

At simultaneous use with other nonsteroid protivospalitelny drugs the risk of development of cankers of digestive tract and gastrointestinal bleeding increases.

Increases concentration of lithium in plasma; reduces efficiency of intrauterine contraceptives, 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. Myelotoxic medicines strengthen manifestations of a gematotoksichnost of drug.

Contraindications:

hypersensitivity to active agent or auxiliary components;
it is contraindicated during the period after performing aortocoronary shunting;
noncompensated heart failure;
full or incomplete combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid and other nonsteroid protivospalitelny means (including in the anamnesis);
erosive and ulcer changes mucous stomach or 12-perstny gut, active gastrointestinal bleeding;
inflammatory diseases of intestines (nonspecific ulcer colitis, disease Krone);
cerebrovascular bleeding or other bleedings;
the expressed liver failure or active disease of a liver;
the expressed renal failure at the patients who are not exposed to dialysis (clearance of creatinine less than 30 ml/min.), the progressing diseases of kidneys including the confirmed hyperpotassemia;
pregnancy, breastfeeding period;
children's age up to 15 years.

With care

For decrease in risk of development of the undesirable phenomena it is necessary to use a minimal effective dose minimum possible short course at coronary heart disease, cerebrovascular diseases, congestive heart failure, дислипидемии / a lipidemia, a diabetes mellitus, diseases of peripheral arteries, smoking, clearance of creatinine less than 60 ml/min., anamnestic data on development of a canker of digestive tract, in the presence of Helicobacter pylori infection, at advanced age, at long use of non-steroidal anti-inflammatory drugs, frequent alcohol intake, heavy somatopathies, the accompanying therapy by the following drugs: anticoagulants (for example, warfarin), antiagregant (for example acetylsalicylic acid, klopidogret), peroral glucocorticosteroids (for example Prednisolonum), selective serotonin reuptake inhibitors (for example to tsitalopra, fluoxetine, пароксетин, sertraline).

Overdose:

Symptoms: strengthening of side effects. Treatment: symptomatic. There are no specific antidotes and antagonists.

Storage conditions:

Period of validity - 2 years. Not to use after a period of validity. List B. In the place protected from light at a temperature from 8 to 25 °C. Not to store in the refrigerator. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Solution for intramuscular introduction of 10 mg/ml.

On 1,5 ml in ampoules. On 3 or 5 ampoules in a blister strip packaging. 1 or 2 blister strip packagings together with the application instruction in a pack from a cardboard.