МексиВ 6®

General characteristics. Structure:

Active agents: ethylmethylhydroxypyridine succinate of 125 mg, pyridoxine hydrochloride of 10 mg;

excipients: hydrophosphate calcium dihydrate, коповидон (коллидон
VA–64 or Plasdon Es-630), silicon dioxide colloid (aerosil), croscarmellose sodium (primelloza), magnesium a lactate, magnesium stearate, the castor oil hydrogenated cellulose microcrystallic;

structure of a film cover: Seleknut AQ–02003 [a gipromelloza (gidroksipropilmetil-cellulose), a macrogoal (polyethyleneglycol 6000), titanium dioxide].

Description

Round, biconvex tablets, film coated white or almost white color. On cross section of almost white color.

Pharmacological properties:

МексиВ 6® — the combined drug.

Pharmacodynamics. Etilmetilgidroksipiridina succinate inhibitor of free radical processes — the membranoprotektor possessing also anti-hypoxemic, stressprotektorny, nootropic, antiepileptic and anxiolytic action. The antioxidant drug regulating metabolic processes in a myocardium and a vascular wall.

The mechanism of action is caused antioxidant and membranoprotektorny by properties. Suppresses peroxide oxidation of lipids, increases activity of a superoksidoksidaza, the lipid protein raises a ratio, improves structure and function of a membrane of cells. Modulates activity of membrane-bound enzymes, receptor complexes that promotes preservation of the structurally functional organization of biomembranes, transport of neurotransmitters and improvement of synoptic transfer. Increases concentration in a dopamine brain.

Strengthens compensatory activation of aerobic glycolysis and reduces extent of oppression of oxidizing processes in a tricarbonic acid cycle in the conditions of a hypoxia with increase in adenozitrifosforny acid (ATP) and creatine phosphate, activates the power synthesizing function of mitochondrions.

Increases resistance of an organism to influence of various disturbing factors at morbid conditions (shock, a hypoxia and ischemia, disturbances of cerebral circulation, intoxication ethanol and antipsychotic medicines).

Improves metabolism and blood supply of a brain, microcirculation and rheological properties of blood, reduces aggregation of thrombocytes. Stabilizes membranes of blood cells (erythrocytes and thrombocytes), reducing probability of development of hemolysis. Possesses hypolipidemic action, reduces the content of the general cholesterol and lipoproteins of the low density (LPNP).

Improves a functional condition of an ischemic myocardium, reducing displays of systolic and diastolic dysfunction of the left ventricle (LV), and also electric instability of a myocardium.

In the conditions of critical decrease in a coronary blood-groove promotes preservation of the structurally functional organization of membranes of cardiomyocytes, stimulates activity of membrane enzymes — phosphodiesterases, adenylatecyclases, acetylcholinesterases. Supports the activation of aerobic glycolysis developing at acute ischemia and promotes in the conditions of a hypoxia to recovery of mitochondrial oxidation-reduction processes, increases synthesis of adenozitrifosforny acid (ATP), creatine phosphate and other makroerg. Increases collateral blood supply of an ischemic myocardium and activates the power synthesizing processes in an ischemia zone that promotes preservation of integrity of cardiomyocytes and maintenance of their functional activity.

At patients with a stable angina of exertion increases tolerance to an exercise stress and anti-anginal activity of nitrates, improves rheological properties of blood, reduces the frequency of development of acute coronary insufficiency.

Pyridoxine, coming to an organism, is phosphorylated, turns into piridoksal-5-phosphate and is a part of the enzymes which are carrying out decarboxylation, transamination and racemization of amino acids, and also enzymatic transformation of sulfur-containing and hydroxylated amino acids. Participates in a metabolism; it is necessary for normal functioning of the central and peripheral nervous system. The pyridoxine participates in exchange of tryptophane, methionine, cysteine, glutaminic and other amino acids. Plays an important role in exchange of a histamine. Contributes to normalization of lipidic exchange.

Pharmacokinetics. Etilmetilgidroksipiridina succinate is quickly soaked up at intake (the semi-absorption period — 0,08–1 h). Time of achievement of the maximum concentration (Tcmax) at intake — 0,46–0,5 h. The maximum concentration (Cmax) at intake — 50–100 ng/ml. It is quickly distributed in bodies and fabrics. The average time of deduction of ethylmethylhydroxypyridine of succinate in an organism at intake — 4,9–5,2 h.

Etilmetilgidroksipiridina succinate is metabolized in a liver by a glyukuronirovaniye. 5 metabolites are identified: 3 oxypyridines phosphate — are formed in a liver and with the participation of an alkaline phosphatase breaks up to phosphoric acid and 3 oxypyridine; the 2nd metabolite — pharmacological active, is formed in large numbers and it is found in urine for 1–2 days after introduction; the 3rd — is brought in large numbers with urine; the 4th and 5th — glyukuronkonjyugata. An elimination half-life at intake — 4,7–5 h. It is quickly removed with urine generally in the form of metabolites (50% for 12 h) and in insignificant quantity — in not changed look (0,3% for 12 h). It is most intensively removed during the first 4 h after succinate ethylmethylhydroxypyridine reception. Removal indicators with urine of not changed ethylmethylhydroxypyridine of succinate and metabolites have considerable individual variability.

The pyridoxine is soaked up quickly throughout a small bowel, the bigger quantity is absorbed in a jejunum. It is metabolized in a liver with formation pharmacological of active metabolites (пиридоксаль phosphate and пиридоксаминофосфат). Piridoksal phosphate contacts proteins of plasma for 90%. Well gets into all fabrics; collects preferential in a liver, it is less — in muscles and the central nervous system (CNS). Gets through a placenta, cosecretes with breast milk. An elimination half-life (T1/2) — 15–20 days. It is removed by kidneys (at intravenous administration — with bile of 2%), and also during a hemodialysis.

Indications to use:

As a part of a combination therapy:
distsirkulyatorny encephalopathy;
syndrome of vegetative dystonia;
alarming states at neurotic and neurosis-like states;
abstinent syndrome at alcoholism with dominance of neurosis-like and vegetovascular frustration;
coronary heart disease (prevention of attacks);
states after acute intoxication antipsychotic means;
asthenic states, and also for prevention of development of somatic diseases under influence of extreme factors and loadings;
influence extreme (stressornykh) factors.

Route of administration and doses:

Inside, on 1 tablet 3 times a day; an initial dose on 1–2 tablet 1–2 times a day with gradual increase to obtaining therapeutic effect. Maximum daily dose 6 таб / days. Treatment duration — 2–8 weeks. If necessary carrying out repeated courses is possible.

Features of use:

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.

Side effects:

Nausea, dryness in a mouth, diarrhea, drowsiness, allergic reactions, hypersecretion of Acidum hydrochloricum (HCl), numbness, emergence of feeling of a prelum in extremities — a symptom of "stockings" and "gloves", decrease in a lactation (sometimes it is used as medical effect).

Interaction with other medicines:

Strengthens effect of benzodiazepine anxiolytics, antiepileptic (carbamazepine),
protivoparkinsonichesky medicines (levodopa), nitrates

Reduces toxic effects of ethanol.

Strengthens effect of diuretics; it is well combined with cardiac glycosides (the pyridoxine promotes increase in synthesis of sokratitelny proteins in a myocardium), with glutaminic acid and potassium and magnesium asparaginate (resistance to a hypoxia increases). The pyridoxine pharmaceutical is incompatible with thiamin and cyanocobalamine. The isoniazid, Penicillaminum, Cycloserinum and estrogensoderzhashchy oral contraceptives weaken effect of a pyridoxine.

Contraindications:

Hypersensitivity; acute liver and/or renal failure;
pregnancy, lactation, children's age.
With care: Peptic ulcer of a stomach and 12-perstny gut.

Overdose:

Symptoms: sleep disorders (sleeplessness, in certain cases — drowsiness).

Treatment, as a rule, is not required — symptoms disappear independently within a day. In hard cases at sleeplessness — nitrazepam of 10 mg, oxazepam of 10 mg or diazepam of 5 mg.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity: 2 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated.

On 10 or 15 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.

On 1, 2, 3, 6, 10 blister strip packagings on 10 tablets or on 1, 2, 4, 6 blister strip packagings on 15 tablets together with the application instruction place in a pack from a cardboard.