Metamaks-Darnitsa

General characteristics. Structure:

Active ingredient: 1 ml of solution contains 3-(2,2,2-trimetilgidraziniya) of propionate of a dihydrate 100 mg;

excipient: water for injections.

Pharmacological properties:

Pharmacodynamics. 3-(2,2,2-Trimetilgidraziniya) of propionate of a dihydrate – a structural analog

to γ-butyrobetaine which improves metabolism and power supply of cells. Cardiotyre-tread, anti-anginal, anti-hypoxemic and angioprotektorny means.
 
Drug suppresses activity of a γ-butyrobetainehydroxylase, reduces the maintenance of a free carnitine, reduces karnitinzavisimy oxidation of fatty acids. In the conditions of ischemia recovers balance of processes of delivery of oxygen and its consumption in cells, prevents disturbance of transport of ATP, along with it activates glycolysis that occurs without additional consumption of oxygen. As a result of decrease in concentration of a carnitine the γ-butyrobetaine in which vazodilatatorny properties are inherent is strenuously synthesized.
 
The action mechanism the trimetilgidraziniya of propionate defines a wide range of its pharmacological effects. It increases working capacity, reduces symptoms of a mental and physical overstrain, activates immunity of fabrics and humoral immunity. At heart failure increases reduction of a myocardium, tolerance to exercise stresses, reduces the frequency of attacks of stenocardia.
 
At acute and chronic ischemic disorders of cerebral circulation the trimetilgidraziniya propionate improves blood circulation in the ischemia center, promotes redistribution of a brain blood-groove in favor of the ischemic site.
 
Trimetilgidraziniya also tonic action on TsNS is peculiar to propionate, it eliminates functional disturbances somatic and the autonomic nervous system, including at an abstinence syndrome at patients with an alcoholism. Drug also exerts positive impact on dystrophic the changed vessels of a retina and on cellular immunity.
 
Pharmacokinetics. Bioavailability of drug makes 100%. The maximum concentration in a blood plasma is reached at once after introduction. The elimination half-life makes 3-6 hours. It is metabolized in an organism with formation of two main metabolites which are removed by kidneys.

Indications to use:

As a part of complex therapy:

–       coronary heart disease (stenocardia, myocardial infarction, chronic heart failure, dishormonal cardiomyopathy);

–       acute and chronic disorders of cerebral circulation (stroke and cerebrovascular insufficiency);

–       a physical overstrain (including at athletes);

–       an abstinence syndrome at an alcoholism (in a combination with specific therapy of alcoholism);

–       hemophthalmia, retinal apoplexies of various etiology;

–       fibrinferment of the central vein of a retina and its branches;

–       retinopathies of various etiology (diabetic, hypertensive).

Route of administration and doses:

Due to a possibility of development of the stimulating effect it is recommended to appoint drug in the first half of day.
 
1. Cardiovascular diseases. The daily dose at intravenous administration makes
5-10 ml of 10% of solution (0,5-1 g according to). A course of treatment – 4-6 weeks.
 
2. Disturbances of cerebral circulation.
Acute phase – on 0,5 g once a day intravenously within 10 days, further pass to intake. The general course of treatment – 4-6 weeks.
 
Chronic disturbances – apply a peroral dosage form.
Repeated courses (usually 2-3 times a year) are possible after consultation with the doctor.
 
3. Vascular pathology and dystrophic diseases of a retina. Parabulbarno and subkonjyunktivalno on 0,5 ml of 10% of solution of Metamaks for 10 days. At inflammatory diseases of an eye treatment is combined with parenteral or local administration of corticosteroids, at vascular and dystrophic diseases – with drugs which improve microcirculation.
 
4. Alcoholism. Intravenously and intramusculary on 0,5 g 2 times a day. The general course of treatment – 7-10 days.

Features of use:

Metamax. is not drug of the first row at an acute coronary syndrome.
 
Patients with chronic diseases of a liver and kidneys at drug use need to control their function for a long time.
 
It is necessary to be careful at simultaneous use of Metamaks with nitroglycerine, nifedipine, β-adrenoblockers and peripheral vazodilatator because of development of moderate tachycardia and arterial hypotension.
 
At treatment of patients with chronic heart failure Metamax. it is possible to combine with cardiac glycosides.
 
Ability to influence speed of response at control of motor transport or work with other mechanisms.

At use of drug it is necessary to avoid control of vehicles and work with other mechanisms which requires special attention and speed of response, considering a possibility of development of side reactions (a lowering of arterial pressure, tachycardia).
Use during pregnancy or feeding by a breast.

Safety of use of drug during pregnancy is not proved. In order to avoid possible adverse influence on a fruit during pregnancy Metamax. do not fix. It is not found out whether drug in mother's milk is emitted. If treatment by Metamaks is necessary for mother, feeding by a breast should be stopped.
 
Children.
There are no sufficient data concerning Metamaks's use for treatment of children.

Side effects:

From cardiovascular system: seldom – tachycardia, arrhythmia, changes of arterial pressure.
From system of a hemopoiesis: eosinophilia.
From the central nervous system: seldom – a headache, dizziness, psychomotor disturbances, paresthesias, a tremor, excitement.
From digestive tract: seldom – diarrhea, nausea, vomiting, an abdominal pain, the dispetichesky phenomena, metal smack in a mouth, dryness in a mouth or hypersalivation.
Allergic reactions: seldom – reddening and an itch of skin, a small tortoiseshell, rashes, is rare – an acute anaphylaxis.

From system of breath: short wind, dry cough.

The general disturbances and reactions in an injection site: a hyperemia, pain in an injection site.
Others: fever, stethalgia, weakness, hyperthermia, perspiration.

Interaction with other medicines:

Drug can be combined with anti-anginal means, anticoagulants and antiagregant, antiarrhytmic means, cardiac glycosides, diuretic means and other drugs.
 
Metamax. can exponentiate effect of nitroglycerine, nifedipine, alpha adrenoblockers, antigipertenzivny means and peripheral vazodilatator and to cause development of moderate tachycardia, arterial hypotension (it is necessary to be careful at use of this combination).
At combined use Metamax. strengthens action of anti-anginal means, some hypotensive drugs, cardiac glycosides.

Contraindications:

Hypersensitivity to drug components.
Increase in intracranial  pressure (at disturbance of venous outflow, intracranial tumors), organic lesions of the central nervous system.
Period of pregnancy or feeding by a breast.
Children's age.

Overdose:

Symptoms: Cases of overdose of Metamaks are unknown. Drug малотоксичен also does not cause side effects which can threaten health of the patient. At use of high doses of Metamaks emergence of the symptoms similar to side effect is possible. Sharp changes of arterial pressure are possible.
 
Treatment: Gastric lavage, salt laxative, cleansing enema. In cases when the deviation of arterial pressure from norm is considerable, use the corresponding drugs. Further treatment – symptomatic.

Storage conditions:

Period of validity - 2 years. To store in the place, unavailable to children, in original packaging at a temperature not above 25 °C. Not to freeze.

Issue conditions:

According to the recipe

Packaging:

On 5 ml in an ampoule; on 5 ampoules in a blister strip packaging; on the 2nd blister strip packagings in a pack.