Амелотекс®

General characteristics. Structure:

Active agent to meloksika - 7,5 mg or 15 mg.
Excipients: lactoses monohydrate, cellulose microcrystallic, sodium citrate, povidone, кросповидон, silicon dioxide colloid, magnesium stearate.
 
Tablets of 7,5 mg: round, biconvex tablets, color, pale yellow or pale yellow with a weak greenish shade, existence of a mramornost and easy roughness is allowed.

Tablets of 15 mg: round, biconvex tablets, with risky on one party, color, pale yellow or pale yellow with a weak greenish shade, existence of a mramornost and easy roughness is allowed.

Pharmacological properties:

Pharmacodynamics. Meloksikam – the non-steroidal anti-inflammatory drug possessing anesthetic, antiinflammatory and febrifugal action.

Antiinflammatory action is connected with braking of enzymatic activity of cyclooxygenase-2 (TsOG-2) participating in biosynthesis of prostaglandins in the field of an inflammation.

To a lesser extent to meloksika affects cyclooxygenase-1 (TsOG-1) participating in synthesis of the prostaglandin which is protecting a mucous membrane of digestive tract and taking part in regulation of a blood-groove in kidneys.

Pharmacokinetics. Absolute bioavailability of a meloksikam – 89% is well soaked up from digestive tract. The concomitant use of food does not change absorption. When using drug inside in doses of 7,5 and 15 mg of its concentration are proportional to doses. Equilibrium concentration are reached within 3-5 days. At prolonged use of drug (more than 1 year), concentration are similar to those which are noted after the first achievement of equilibrium concentration. Linkng with proteins of plasma makes more than 99%. Range of distinctions between the maximum and basal concentration of drug after its reception is rather small once a day and makes when using a dose 7,5 mg 0,4 - 1,0 mkg/ml, and when using a dose of 15 mg - 0,8-2,0 mkg/ml, (Cmin and Cmax values are given, respectively). Meloksikam gets through gistogematichesky barriers, concentration in synovial fluid reaches 50% of the maximum concentration of drug in plasma.

Almost it is completely metabolized in a liver with formation of four inactive derivatives in the pharmacological relation. The main metabolite, to 5-karboksimeloksika (60% of dose size), is formed by oxidation of an intermediate metabolite, a 5-gidroksimetilmeloksikam who is also excreted, but to a lesser extent (9% of dose size). The researches in vitro showed that in this metabolic transformation an important role is played by CYP 2C9 isoenzyme, additional value has CYP 3A4 isoenzyme. Peroxidase which activity probably individually varies takes part in formation of two other metabolites (making, respectively, 16% and 4% of drug dose size). 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);

It is intended for symptomatic therapy, reduction of pain and an inflammation at the time of use, does not influence progressing of a disease.

Route of administration and doses:

Drug is accepted inside during food once a day.

Pseudorheumatism: 15 mg a day. Depending on medical effect the dose can be lowered to 7,5 mg a day.
Osteoarthrosis: 7,5 mg a day. At inefficiency the dose can be increased to 15 mg a day.
Ankylosing spondylarthritis: 15 mg a day.

The maximum daily dose should not exceed 15 mg.

Patients with the increased risk have development of side effects, and also at the patients with the expressed renal failure who are on a hemodialysis, the dose should not exceed 7,5 mg a day.

Features of use:

It is necessary to be careful at use of drug for patients who have in the anamnesis a peptic ulcer of a stomach and duodenum, and also at the patients who are on anticoagulating therapy. At such patients the risk of developing of ulcer and erosive diseases of digestive tract is increased.

It is necessary to be careful and control indicators of function of kidneys at use of drug for patients of advanced age, patients with chronic heart failure with the circulatory unefficiency phenomena, at patients with cirrhosis, and also at patients with a hypovolemia as a result of surgical interventions.

At patients with a renal failure if clearance of creatinine more than 30 ml/min., are not required to correction of the mode of dosing.

At the patients who are on a hemodialysis, the dosage of drug should not exceed 7,5 mg/days.

At permanent and essential increase in transaminases and changes of other indicators of function of a liver drug should be cancelled and carried out control tests.

The patients accepting at the same time diuretics and to meloksika have to accept enough liquid.

If in the course of treatment there were allergic reactions (an itch, skin rash, a small tortoiseshell, a photosensitization) it is necessary to stop administration of drug.

Meloksikam, also as well as other non-steroidal anti-inflammatory drugs, can mask symptoms of infectious diseases.

Use of a meloksikam, as well as other drugs blocking synthesis of prostaglandins can influence fertility therefore it is not recommended to the women planning pregnancy.

Influence on ability to control of motor transport and mechanisms

Use of drug can cause emergence of undesirable effects in the form of a headache and dizzinesses, drowsiness. It is necessary to refuse control of vehicles and service of the cars and mechanisms demanding concentration of attention.

Side effects:

From digestive tract: more than 1% — dyspepsia, including nausea, vomiting, abdominal pains, a lock, a meteorism, diarrhea; 0,1-1% — passing increase in activity of "hepatic" transaminases, a hyperbilirubinemia, an eructation, an esophagitis, a gastroduodenal ulcer, bleeding from digestive tract (including hidden), stomatitis; less than 0,1% — perforation of digestive tract, colitis, hepatitis, gastritis.

From bodies of a hemopoiesis: more than 1% — anemia; 0,1-1% — change of a blood count, including a leukopenia, thrombocytopenia.

From integuments: more than 1% — an itch, skin rash; 0,1-1% — a small tortoiseshell; less 0,1%nbsp; — photosensitization, violent rashes, multiformny erythema, including Stephens-Johnson's syndrome, toxic epidermal necrolysis.

From respiratory system: less than 0,1% — a bronchospasm.

From a nervous system: more than 1% — dizziness, a headache; 0,1-1% — вертиго, a sonitus, drowsiness; less than 0,1% — confusion of consciousness, a disorientation, emotional lability.

From cardiovascular system: more than 1% — peripheral hypostases; 0,1-1% — increase in arterial pressure, heartbeat, "inflows" of blood to face skin.

From an urinary system: 0,1-1% — a giperkreatininemiya and/or increase in urea in blood serum; less than 0,1% — an acute renal failure; connection with reception of a meloksikam is not established - intersticial nephrite, an albuminuria, a hamaturia.

From sense bodys: less than 0,1% — conjunctivitis, a vision disorder, including a sight illegibility.
Allergic reactions: less than 0,1% — a Quincke's disease, anaphylactoid/anaphylactic reactions.

Interaction with other medicines:

At simultaneous use with other non-steroidal anti-inflammatory drugs (and also with acetylsalicylic acid) the risk of emergence of rozivno-cankers and bleedings from digestive tract increases.

At simultaneous use with hypotensive drugs, decrease in a ffektivnost of action of the last is possible.

At simultaneous use with drugs of lithium development of cumulation of lithium of increase in its toxic action is possible (control of concentration of lithium in rov is recommended).

At simultaneous use with a methotrexate side effect of the last on the hemopoietic system amplifies (danger of developing of anemia and a leukopenia, periodic control of the general blood test is rendered).

At simultaneous use with diuretics and with cyclosporine the risk of development of a renal failure increases.

At simultaneous use with intrauterine contraceptive means decrease in efficiency of action of the last is possible.

At simultaneous use with anticoagulants (heparin, тиклопидин, warfarin), and also with thrombolytic drugs (Streptokinasa, fibrinolysin) the risk of development of bleedings increases (periodic control of indicators of coagulability of blood is necessary).

At simultaneous use with Colestyraminum, as a result of binding of a meloksikam, its removal through digestive tract amplifies.

At simultaneous use with selective serotonin reuptake inhibitors the risk of development of gastrointestinal bleedings increases.

Contraindications:

hypersensitivity to active agent or auxiliary components;
it is contraindicated during the period after performing aortocoronary shunting;
dekompensirovanny 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 of a mucous membrane of a 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.

Due to the existence in composition of drug of lactose patients with rare hereditary diseases, such as a lactose intolerance, deficit of lactase or glyukozo-galaktozny malabsorption should not accept drug.

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: consciousness disturbance, nausea, vomiting, pains in epigastriums, gastrointestinal bleeding, an acute renal failure, a liver failure, an apnoea, an asystolia.

Treatment: there is no specific antidote; at overdose of drug it is necessary to carry out a gastric lavage, reception of absorbent carbon (within the next hour), symptomatic therapy. Colestyraminum accelerates removal of drug from an organism. The artificial diuresis, a hemodialysis - are ineffective because of high communication of drug with blood proteins.

Storage conditions:

Period of validity: 2 years. Not to use after a period of validity. 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:

Tablets of 7,5 mg and 15 mg.
On 10 tablets in a blister strip packaging. On 1 or 2 blister strip packagings together with the application instruction in a pack from a cardboard.