Producer: LLC MTs Ellara Rossiya
Code of automatic telephone exchange: N05BX
Release form: Liquid dosage forms. Solution for injections.
General characteristics. Structure:
Active agent: 1 ml of solution contains 1 mg of a bromdigidrokhlorfenilbenzodiazepin.
Excipients: polyvinylpirrolidone low-molecular medical (povidone), глицерол, sodium disulphite, polysorbate (twin-80), water for injections.
Pharmacodynamics. Possesses the expressed anxiolytic. somnolent, sedative, and also anticonvulsant and central myorelaxation action. Has the oppressing effect on the central nervous system which is implemented preferential in a thalamus, a hypothalamus and limbic system. Strengthens an inhibiting effect of the piperidic acid (GAMK) which is one of the main mediators pre-and postsynaptic braking of transfer of nervous impulses in the central nervous system. The mechanism of action of Elzepam is defined by stimulation of benzodiazepine receptors supramolecular GAMK-benzodiazepin-hlorionofor a prescription complex, the GAMK leading to activation of a receptor causing decrease in excitability of subcrustal structures of a brain, braking of polisinaptichesky spinal reflexes.
Pharmacokinetics. It is widely distributed in an organism. It is metabolized in a liver. Biological half-life from 6 to 10 - 18 hours, excretion of drug is generally carried out through kidneys in the form of metabolites.
Indications to use:
Drug is used at various neurotic, neurosis-like psychopathic, psychopatholike and other states which are followed by alarm, fear, an acrimony, tension, emotional lability. At reactive psychoses, hypochiondrially - a senestopathetic syndrome (including other tranquilizers, resistant to action), vegetative dysfunctions and frustration of a dream, for prevention of conditions of fear and emotional pressure.
As an anticonvulsant drug is used for treatment of patients with temporal and myoclonic epilepsy. In neurologic practice apply to treatment of hyperkinesias and tics, muscle tensions, vegetative lability.
Route of administration and doses:
Elzepam appoint intramusculary or intravenously (struyno or kapelno).
The single dose usually makes 0,0005 - 0,001 g (0,5 - 1 mg), and at sleep disorders of 0,0005-0,001 g (0,5 - 1 mg) before going to bed.
For stopping of fear, alarm, psychomotor excitement, and also at vegetative paroxysms and psychotic states Elzepam apply intramusculary or intravenously, an initial dose of 0,0005 - 0,001 g (0.5 - 1 ml of 0,1% of solution), an average daily dose of 0,003 - 0,005 g (3 - 5 ml of 0,1% of solution), in hard cases up to 0,007 - 0,009 g.
At the epileptic status and serial epileptic seizures the drug is administered intramusculary or intravenously since a dose of 0,0005 g (0,5 mg).
For treatment of alcoholic abstinence drug appoint intramusculary or intravenously in a dose 0,0025 - 0,005 (2,5 - 5 mg) in days.
In neurologic practice at diseases with the raised muscle tone drug appoint intramusculary on 0,0005 g (0,5 mg) one or twice a day.
For preoperative preparation - intravenously slowly enter 0,003 - 0,004 g (3-4 ml of 0.1% of solution).
The average daily dose of Elzepam makes 0,0015 - 0,005 g (1,5-5 mg). Maximum daily dose of 0,01 g (10 mg).
After achievement of steady therapeutic effect it is reasonable to pass to reception of peroral dosage forms of drug.
In order to avoid development of medicinal dependence, at course treatment duration of use of Elzepam, as well as other benzodiazepines makes 2 weeks. But in some cases duration of treatment can be increased up to 3-4 weeks. At drug withdrawal the dose is reduced gradually.
Features of use:
Respect for extra care at purpose of Elzepama® at heavy depressions since drug can be used for implementation of suicide intentions is required. It is necessary to use with care drug at the elderly and weakened patients. At a renal/liver failure and prolonged treatment control of a picture of peripheral blood and "hepatic" enzymes is necessary. Frequency and the nature of side effect depend on individual sensitivity, a dose and duration of treatment. At reduction of doses or the termination of reception of Elzepam side effects disappear.
Like other benzodiazepines, has ability to cause medicinal dependence at long reception in high doses (more than 4 mg/days).
At the sudden termination of reception the syndrome of "cancellation" (depressions, irritability, sleeplessness, the increased sweating, etc.) can be noted, especially at long reception (more than 8-12 weeks).
During pregnancy apply only according to "vital" indications. Has toxic effect on a fruit and increases risk of development of inborn defects at use in the I trimester of pregnancy. Reception of therapeutic doses in later durations of gestation can cause oppression of the central nervous system of the newborn. Constant use during pregnancy can result in physical dependence with development of a syndrome of "cancellation" in the newborn.
Children, especially at younger age, are very sensitive to the effect of benzodiazepines oppressing the central nervous system.
Use just before childbirth or at the time of delivery can cause in the newborn respiratory depression, decrease in a muscle tone, hypotonia, a hypothermia and the weak act of suction (a syndrome of "the sluggish child").
Drug strengthens effect of alcohol therefore the use of alcoholic drinks during treatment by Elzepam is not recommended.
Elzepam is contraindicated in operating time to the drivers of transport and other persons performing the work demanding bystry reactions and exact movements.
From a nervous system: in an initiation of treatment (especially at elderly patients) - drowsiness, feeling of fatigue, dizziness, disturbance of concentration of attention, an ataxy, a disorientation, delay of mental and motor reactions, confusion of consciousness; seldom a headache, euphoria, a depression, a tremor, decrease in memory, a lack of coordination of movements (especially at high doses), decrease in mood, dystonic extrapyramidal reactions (the uncontrollable movements, including an eye), an adynamy, a myasthenia, a dysarthtia; extremely seldom - paradoxical reactions (aggressive flashes, psychomotor excitement, fear, suicide bent, a muscular spasm, hallucinations, alarm, a sleep disorder).
From the alimentary system: dryness in a mouth or hypersalivation, heartburn, nausea, vomiting, a loss of appetite, a lock or diarrhea; abnormal liver function, increase in activity of "hepatic" transaminases and alkaline phosphatase, jaundice.
Allergic reactions: skin rash, itch.
Influence on a fruit: teratogenecity (especially the I trimester), oppression of the central nervous system, disturbance of breath and suppression of a sucking reflex at newborns whose mothers used drug.
Others: accustoming, medicinal dependence; lowering of arterial pressure (LD); seldom - a vision disorder (diplopia), decrease in body weight, tachycardia. At a sharp dose decline or the termination of reception a syndrome of "cancellation" (the sleep disorder, dysphoric reactions, a spasm of unstriated muscles of internals and skeletal muscles, depersonalization, sweating strengthening, a depression, nausea, vomiting, a tremor, disorder of perception, including a hyperacusia, paresthesias, a photophobia, tachycardia, spasms, is rare - psychotic reactions).
Interaction with other medicines:
Elzepam is compatible to other drugs causing oppression of function of the central nervous system (somnolent, anticonvulsant, antipsychotic, etc.), however at complex use it is necessary to consider mutual strengthening of their action.
Reduces efficiency of a levodopa at patients with parkinsonism.
Can increase toxicity of a zidovudine.
Inhibitors of a microsomal oxidation increase risk of development of toxic effects.
Inductors of microsomal enzymes of a liver reduce efficiency.
Increase concentration of an imipramid in blood serum.
Antihypertensives can increase expressiveness of a lowering of arterial pressure.
Against the background of co-administration of clozapine strengthening of respiratory depression is possible.
Hypersensitivity (including to other benzodiazepines), a coma, shock, a myasthenia, closed-angle glaucoma (a bad attack or predisposition), a heavy chronic obstructive pulmonary disease (strengthening of respiratory insufficiency), acute respiratory insufficiency, pregnancy (especially the I trimester is possible), the breastfeeding period; age up to 18 years (safety and efficiency are not defined).
With care - a liver and/or renal failure, a cerebral and spinal ataxy, a hyperkinesia, tendency to abuse of psychotropic drugs, organic diseases of a brain (paradoxical reactions are possible), a hypoproteinemia, advanced age, a depression (see. "Special instructions").
At moderate overdose - strengthening of therapeutic action and side effects; at considerable overdose - the expressed oppression of consciousness, cordial and respiratory activity.
Treatment: control of the vital functions of an organism, maintenance of respiratory and cardiovascular activity, symptomatic therapy. As antagonists of miorelaksantny action of Elzepam nitrate (injections on 1 ml of 0,1% of solution 2-3 times a day) or Corazolum solution is recommended strychnine (an injection on 1 ml of 10% of solution 1-2 times a day). As the specific antagonist it can be used flumazenit (анексат) - intravenously (a pas of 5% solution of glucose (dextrose) or 0,9% sodium chloride solution) in an initial dose of 0,2 mg (if necessary to a dose of 1 mg).
List B. In dry, protected from light and the place, unavailable to children, at a temperature up to 20 °C.
According to the recipe
On 1 ml in ampoules of neutral glass. On 5 ampoules in a blister strip packaging from a PVC film without covering a foil, together with a knife for opening of ampoules or the scarificator and the application instruction in a box cardboard. 10 ampoules of drug (two blister strip packagings from a PVC film without covering a foil) together with a knife for opening of ampoules or the scarificator and the application instruction in a box cardboard. 50 ampoules of drug (10 blister strip packagings from a PVC film without covering a foil), the application instruction, the scarificator ampoule put in a pack from a cardboard bandbox. On a pack specify: "For hospitals" without indication of conditions of issue. On 5 or 10 ampoules together with a knife ampoule either the scarificator or a knife ampoule ceramic and the application instruction put in a pack from a cardboard bandbox with a corrugated insert from paper renal. When using ampoules with a point or a ring of a break the knife ampoule or the scarificator in a cardboard pack is not put. Ampoules on 1 ml of 0,1% of solution, in packagings on 5, 10 and 50 ampoules.