Mesipol

General characteristics. Structure:

Active agent: to meloksika - 10 mg.

Excipients: Megluminum, гликофурол, half-oxameasures 188, sodium chloride, glycine, sodium hydroxide, water for injections.

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. Absorption: to meloksika it is completely absorbed after intramuscular introduction. Bioavailability of drug makes about 100%. After intramuscular introduction of 15 mg of a meloksikam the maximum concentration of drug (Cmax) in plasma making 1,62 mkg/ml is reached approximately in 1 hour.

Distribution: to meloksika contacts proteins of plasma (mainly with albumine) substantially - 99%. Passes through gistogematichesky barriers, gets into synovial fluid. Concentration in synovial fluid makes 50% of plasma concentration of drug. The volume of distribution (Vd) low also makes 11 l.

Metabolism: to meloksika it is almost completely metabolized in a liver with formation of four pharmacological inactive metabolites. The main metabolite, to 5-karboksimeloksika (60% of the entered dose), is formed by means of oxidation of an intermediate metabolite, a 5-gidroksimetilmeloksikam (9% of the entered dose). In vitro of a research showed that in this metabolic transformation an important role is played by an isoenzyme of CYP 2C9 and additional value has CYP 3A4 isoenzyme. Peroxidase which activity individually varies takes part in formation of two other metabolites which make 16% and 4% of the entered drug dose probably.

Elimination: the considerable enterohepatic circulation characteristic of a meloksikam does not influence drug elimination. Meloksikam is brought preferential in the form of metabolites, equally by kidneys and intestines. In not changed look less than 5% of a meloksikam are removed by intestines, and only trace amounts of not changed drug are defined in urine.

Average elimination half-life (Т½) the meloksikama makes 20 hours. The plasma clearance averages 8 ml/min.

Indications to use:

- symptomatic treatment of a pseudorheumatism;

- symptomatic treatment of an osteoarthrosis;

- symptomatic treatment of an ankylosing spondylitis (Bekhterev's disease);

 - a symptomatic treatment of other inflammatory and degenerative diseases of the joints which are followed by a pain syndrome.

Route of administration and doses:

Intramuscular administration of drug is shown only during the first 2-3 days. Further treatment is continued using peroral forms (tablet). The recommended dose makes 7,5 mg or 15 mg once a day, depending on intensity of pains and weight of inflammatory process.

The drug is administered by means of a deep intramuscular injection.

Considering possible incompatibility, contents of ampoules Mesipol it is not necessary to mix in one syringe with other medicines.

At patients with the increased risk of side reactions and with the expressed renal failure, being on a hemodialysis, the dose should not exceed 7,5 mg a day.

The drug cannot be administered intravenously.

The maximum daily dose of a meloksikam makes 15 mg.

The combined use. The total daily dose of the drug Mesipol used in the form of tablets, candles, suspension for intake and injections should not exceed 15 mg.

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 25 ml/min., are not required to correction of the mode of dosing.

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

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 NPVP, 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 wishing to become pregnant.

Side effects:

From the alimentary system: 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, GIT erosive cankers, the concealed or explicit hemorrhage from a GIT, stomatitis; less than 0,1% - perforation of bodies of a GIT, colitis, hepatitis, gastritis.

From system 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 than 0,1% - a photosensitization, violent rashes, a multiformny erythema, including Stephens-Johnson's syndrome, a toxic epidermal necrolysis.

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

From the central 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 the ABP, a heart consciousness, "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 organs of sight: 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.

Local reactions: burning and pain in the place of an injection are possible.

Interaction with other medicines:

At simultaneous use with other non-steroidal anti-inflammatory drugs (and also with acetylsalicylic acid) the risk of emergence of erosive cankers and bleedings of a GIT increases.

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

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

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

At simultaneous use with cyclosporine nephrotoxic action of a meloksikam amplifies.

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 holestiraminy, as a result of binding of a meloksikam, its removal through a GIT amplifies.

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

Myelotoxic medicines strengthen manifestations of a gematotoksichnost of a meloksikam.

Contraindications:

- hypersensitivity to active agent or auxiliary components;

- a full or incomplete combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid and other NPVP (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);

- it is contraindicated during the period after performing aortocoronary shunting;

- dekompensirovanny heart failure;

- cerebrovascular bleeding or other bleedings;

- the expressed liver failure or an 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 18 years.

With care: Advanced age, coronary heart disease, chronic heart failure, cerebrovascular diseases, дислипидемия / a lipidemia, a diabetes mellitus, diseases of peripheral arteries, smoking, clearance of creatinine less than 60 ml/min., GIT cankers in the anamnesis, existence of an infection of Helicobacter pylori, long use of NPVP, frequent alcohol intake, heavy somatopathies, a concomitant use of peroral GKS (including Prednisolonum), anticoagulants (including warfarin), antiagregant (including acetylsalicylic acid, клопидогреля), selective serotonin reuptake inhibitors (including a tsitaloprama, fluoxetine, a paroksetin, sertraline).

Overdose:

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

Treatment: The specific antidote is absent.

It is recommended: gastric lavage and symptomatic therapy. In clinical trials it is shown what холестирамин accelerates removal of a meloksikam. The hemodialysis is ineffective because of high communication with blood proteins.

Storage conditions:

To store in the place protected from light, at a temperature not above 25 °C. 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 of solution in glass ampoules of the 1st type, with a capacity of 2 ml with the coding ring of green color applied on an ampoule surface.
On 3 or 5 ampoules together with the instruction on a medical use in a cardboard pack.