Producer: RUP of Belmedpreparata Republic of Belarus
Code of automatic telephone exchange: N07XX
Release form: Liquid dosage forms. Solution for injections.
General characteristics. Structure:
Active ingredient: 50 g of a meksidol.
Drug which renders antioxidant, antigipoksantny, membranoprotektorny, nootropic, anxiolytic, anticonvulsant action.
Pharmacodynamics. Increases resistance of an organism to a stress, influence of the major disturbing factors and to kislorodozavisimy morbid conditions (to shock, a hypoxia, ischemia, disturbance of cerebral circulation, intoxication alcohol and antipsychotic drugs). We possess moderate hypolipidemic action. Stabilizes membrane structures of blood cells, increases stability of thrombocytes and leukocytes at hemolysis, levels the changes of physical and chemical properties of cellular membranes of nervous tissue caused by a hypoxia (reduces viscosity lipidic бислоя, increases the flowability of a membrane and the lipid protein raises a ratio) that favorably affects its metabolic and biosynthetic activity.
Inhibits peroxide oxidation of lipids, increases activity of a superoxide scavenger, increases the intracellular maintenance of tsAMF and tsGMF, modulates activity of membrane-bound enzymes (Sa-nezavisimoy of phosphodiesterase, adenylatecyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GAMK, atsetilkholinovy), increasing their ability to contact receptors and improving transport of neurotransmitters and synoptic transfer.
Increases the maintenance of a dopamine in a brain. Strengthens compensatory activation of aerobic glycolysis, promotes recovery of mitochondrial oxidation-reduction processes in the conditions of a hypoxia, increases synthesis of ATP and a kreatininfosfat. Reduces a fermental toxaemia and endogenous intoxication at acute pancreatitis.
Improves memory and working capacity. Has anxiolytic effect, eliminates alarm, fear, tension, concern, improves the emotional status. Possesses neurotyre-tread action, stimulates recovery and adaptive processes in a brain at a craniocereberal injury.
Promotes acceleration of evolution intracerebral, including posttraumatic, hemorrhages. At the persons who transferred an acute disorder of cerebral circulation as a part of complex therapy exerts beneficial effect on processes of a mass transfer of oxygen in a brain in the conditions of a hypoxia, reducing the maximum breathing rate and increasing the stationary level of partial pressure of oxygen in nervous tissue. Reduces effects of a reperfusion syndrome at coronary insufficiency.
Pharmacokinetics. At intravenous administration in doses of 400-500 mg Smakh in a blood plasma makes 3,5-4,0 mkg/ml in 0,45-0,5 h and is defined in a blood plasma during 4 h. It is quickly distributed from a blood channel in bodies and fabrics. The average time of keeping of drug in an organism makes 0,7-1,3 h. Contacts blood proteins for 42%. It is metabolized in a liver with education phosphate-3-oksipirida and glyukuronkonyyugat.
The first metabolite – phosphate-3-oksipirid – in a blood channel under the influence of an alkaline phosphatase breaks up to oxypyridine and phosphoric acid. The second metabolite is pharmacological active and it is found in urine in the 1st and 2nd days after administration of drug. The third metabolite is also found in urine. The fourth and fifth metabolites represent glyukuronkonjyugata. On average for 12 h with urine 0,3% of drug in an invariable look and 50% – in the form of glyukuronkonjyugat are excreted.
Indications to use:
As a part of complex therapy at the acute disorder of cerebral circulation, disturbances of cerebral circulation caused by a craniocereberal injury; distsirkulyatorny encephalopathy, easy cognitive frustration against the background of atherosclerotic defeat of vessels of a brain, intoxications, dysmnesias and intellectual insufficiency at elderly people, alarming frustration at neurotic and nevrozny states, an abstinence syndrome at alcoholism in the presence of neurosis-like and vegeto-vascular disturbances, acute poisoning with neuroleptics, treatment of trophic ulcers of venous genesis, an ulitis, a periodontal disease, periodontosis, acute it is purulent - necrotic processes of an abdominal cavity (acute pancreatitis, peritonitis).
Route of administration and doses:
Drug is appointed intravenously or intramusculary. Intravenous administration is carried out struyno slowly, within 5-7 minutes; kapelno – with a speed of 40-60 minutes. At infusional introduction drug is dissolved in 0,9% chloride sodium solution. The mode of dosing is selected individually, depending on severity of a disease. The recommended dose – 5-10 mg/kg/days, but no more than 800 mg a day. Begin treatment with use of drug in a dose of 50-100 mg 1-3 times a day, gradually raising a dose to obtaining therapeutic effect.
At treatment of an acute disorder of cerebral circulation drug is used as a part of complex therapy intravenously kapelno in a dose 200-300 mg of 1 times a day in the first 5-7 days, and then – intramusculary on 200 mg 2 times a day. The dose of drug can be increased to 500 mg at more severe disease. Duration of treatment makes 10-14 days.
At distsirkulyatorny encephalopathy in a decompensation phase it is intravenously struyno necessary to appoint drug or kapelno in a dose of 100-200 mg 2-3 times a day within 14 days, and then – intramusculary on 200 mg a day within 2 weeks.
For prevention of distsirkulyatorny encephalopathy the drug is administered intramusculary in a dose of 100 mg by 2 times a day within 10-14 days.
At easy cognitive disturbances of atherosclerotic genesis at patients of advanced age and at neurotic frustration with an alarm syndrome drug is appointed intramusculary in a dose of 100-300 mg a day within 14-30 days.
At an abstinence alcoholic syndrome the drug is administered in a dose 100-200 mg intramusculary by 2-3 times a day or in a dose of 200-300 mg intravenously struyno, on 16 ml of isotonic solution of sodium chloride, 1-2 times a day within 5-7 days.
At acute intoxication antipsychotic means the drug is administered intravenously in a dose of 100-300 mg a day within 7-14 days.
At acute pyoinflammatory processes of an abdominal cavity (acute necrotic pancreatitis, peritonitis) the dose of drug depends on a form and disease severity, prevalence of process, options of a clinical current. Cancellation should be carried out gradually, only after steady positive clinical laboratory effect.
At acute edematous (intersticial) pancreatitis drug is appointed on 100 mg by 3 times a day intravenously kapelno and intramusculary.
At necrotic pancreatitis of easy severity drug is appointed on 100-200 mg by 3 times a day intravenously kapelno and intramusculary; at necrotic pancreatitis of moderate severity – on 200 mg 3 times a day intravenously kapelno. At heavy necrotic pancreatitis in the first days drug appoint 800 mg in pulse dose, having divided into two introductions, further 300 mg 2 times a day with gradual decrease in a daily dose. At extremely heavy course of necrotic pancreatitis the initial dose makes 800 mg a day before permanent stopping of manifestations of pankreatogenny shock, at stabilization of a state drug is appointed on 300-400 mg by 2 times a day intravenously kapelno with gradual decrease in a daily dose. Cancellation is carried out gradually, after steady improvement of clinical laboratory indicators.
Features of use:
Patients with the arterial pressure more than 180/100 mm Hg, the krizovy course of arterial hypertension and the expressed aforektivny instability need preliminary correction of arterial hypertension and sedative therapy, and also control of arterial pressure during performing therapy.
Others: drowsiness, feeling of "the spreading heat" in all body, allergic reactions.
Interaction with other medicines:
Strengthens action of anticonvulsants (carbamazepine), benzodiazepine anxiolytics and protivoparkinsonichesky means (levodopa).
Reduces toxic effect of alcohol.
Acute disorders of function of a liver and/or kidneys, hypersensitivity to drug, children's age up to 18 years, pregnancy, a lactation.
Symptoms: sleep disorders (sleeplessness, in certain cases – drowsiness); at intravenous administration – insignificant and short-term (to 1,5-2 h) increase in arterial pressure.
Treatment, as a rule, is not required as symptoms disappear independently within a day. If necessary symptomatic therapy is shown.
According to the recipe
Solution for injections of 5% in ampoules on 2 ml No. 10 (5x2 in blister strip packagings).