Элзепам®

General characteristics. Structure:

One tablet of 0,5 mg contains: active ingredient – бромдигидрохлорфенилбензодиазепин 0,5 mg.

One tablet of 1 mg contains: active ingredient – бромдигидрохлорфенилбензодиазепин 1 mg.

Excipients: polyvinylpirrolidone low-molecular medical (povidone), глицерол, sodium disulphite, polysorbate (twin-80), water for injections.

Pharmacological properties:

Pharmacodynamics. Anxiolytic action is caused by influence on an amygdaloid nucleus of limbic system and is shown in reduction of emotional pressure, weakening of alarm, fear, concern. Sedation is caused by influence on a reticular formation of a trunk of a brain and nonspecific kernels of a thalamus and is shown by reduction of symptomatology of a neurotic origin (alarm, fear). Somnolent action is accompanied by oppression of cells of a reticular formation of a trunk of a brain. Reduces influence of the emotional, vegetative and motor irritants breaking the backfilling mechanism. Anticonvulsant action is implemented by strengthening of presynaptic braking, drug suppresses distribution of a convulsive impulse, but does not remove the excited condition of the center. The central myorelaxation action is caused by braking of the polisinaptichesky spinal afferent braking ways (to a lesser extent monosinaptichesky). Perhaps direct inhibition of motor nerves and contractility of muscles.

Pharmacokinetics. At intake drug is well soaked up from digestive tract, time of achievement of the maximum concentration of a bromdigidrokhlorfenilbenzodiazepin in blood from 1 to 2 h. It is metabolized in a liver, the elimination half-life makes from 6 to 18 h. It is removed generally by kidneys in the form of metabolites.

Indications to use:

- The neurotic, neurosis-like frustration which are followed by alarm, fear, an acrimony, emotional lability and tension, vegetative frustration, a hypochiondrial and senestopathetic syndrome (including resistant to action of other tranquilizers).

- Frustration of a dream.

- As a part of complex therapy of an alcoholic abstinence syndrome.

- As supportive application for treatment of patients with temporal and myoclonic epilepsy.

- Treatment of the raised muscle tone, hyperkinesias and rigidity at damage of the central nervous system.

Route of administration and doses:

Inside.

The single dose usually makes 0,5-1 mg, at sleep disorders – 0,5 mg in 20-30 min. prior to a dream.

At neurotic, neurosis-like frustration, a hypochiondrial and senestopathetic syndrome on 0,5-1 mg 2-3 times a day. In 2-4 days taking into account efficiency and portability of drug the dose can be increased to 4-6 mg/days, morning and day doses make 0,5-1 mg, for night of 2,5 mg.

At the expressed concern treatment begin 3 mg/days with a dose, quickly increasing a dose before obtaining therapeutic effect.

As a part of complex therapy of an alcoholic abstinence syndrome appoint in a dose 2,5-6 mg a day.

As supportive application for treatment of patients with temporal and myoclonic epilepsy the dose makes 2-10 mg/days.

At the raised muscle tone, hyperkinesias and rigidities at defeat of TsNS drug appoint on 2-3 mg one or twice a day.

Maximum daily dose of 10 mg.

In order to avoid development of medicinal dependence, at course treatment drug use duration, as well as other benzodiazepines makes two weeks. In some cases duration of treatment can be increased up to 2 months.

Features of use:

At a renal/liver failure and prolonged treatment control of a picture of peripheral blood and liver 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 administration of drug of Elzepam®  side effects, as a rule, disappear.

Like other benzodiazepines, has ability to cause medicinal dependence at reception more than 2 weeks.

Use just before childbirth or at the time of delivery can cause in the newborn respiratory depression, decrease in a muscle tone, a lowering of arterial pressure, a hypothermia and the weak act of suction (a syndrome of "the sluggish child"). The drug Elzepam®  strengthens effect of alcohol therefore the use of alcoholic drinks during treatment by drug contraindicated.

Influence on ability to manage vehicles, work with mechanisms.

At administration of drug of Elzepam®  it is forbidden to manage vehicles and to be engaged in other types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

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; 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, spasms (at patients with epilepsy); paradoxical reactions (aggression flashes, psychomotor excitement, fear, suicide bent, muscular spasm, hallucinations, alarm, sleep disorders).

From bodies of a krovetvoreniya:leykopeniye, neutropenia, agranulocytosis (fever, gipetermiya, pharyngalgia, unusual fatigue or weakness), anemia, thrombocytopenia.

From the alimentary system: dryness in a mouth or hypersalivation, heartburn, nausea, vomiting, a loss of appetite, a lock or diarrhea; abnormal liver functions, increase in activity "печеночныхтрансаминаз" and alkaline phosphatase, jaundice.

From urinogenital system: urine incontience, ischuria, renal failure, decrease or increase in a libido, dysmenorrhea.

Allergic reactions: skin rash, itch.

Influence on a fruit: teratogenecity (especially in 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; vision disorder (diplopia), decrease in body weight, tachycardia.

At a sharp dose decline or the termination of reception – a syndrome of "cancellation" (a sleep disorder, dysphoric reactions, a spasm of unstriated muscles of internals and skeletal muscles, depersonalization, sweating strengthening, a depression, nausea, vomiting, a tremor, disorders of perception including a giperkuziya, parestenziya, a photophobia; tachycardia, spasms, psychotic reactions).

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 side effects disappear.

Interaction with other medicines:

Элзепам®  it 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.

Inhibitors of microsomal enzymes of a liver increase risk of development of toxic effects and reduce efficiency.

Increases concentration of Imipraminum in blood serum.

Antihypertensives can increase expressiveness of a lowering of arterial pressure. Simultaneous use of Elzepama®  with clozapine can cause respiratory depression.

Contraindications:

— hypersensitivity to drug components Elzepam, and also to other derivatives of benzodiazepine;

— coma, shock, myasthenia, closed-angle glaucoma (bad attack or predisposition);

— acute alcoholic poisonings (with weakening of the vital functions), narcotic analgetics and hypnagogues;

— a heavy chronic obstructive pulmonary disease (strengthening of respiratory insufficiency is possible);

— acute respiratory insufficiency;

— a heavy depression (can be shown suicide a naklonnosta);

— age up to 18 years (safety and efficiency are not established);

— deficit of lactase;

— lactose intolerance, glyukozo-galaktozny malabsorption.

With care: a liver and/or renal failure, a cerebral and spinal ataxy, medicinal dependence in the anamnesis, tendency to abuse of psychoactive medicines, hyperkinesias, organic diseases of a brain, psychosis (paradoxical reactions are possible), a hypoproteinemia, night an apnoea (established or assumed), advanced age.

Overdose:

At moderate overdose — strengthening of therapeutic action and dozozavisimy side effects; at considerable overdose — the expressed oppression of consciousness, cordial and respiratory activity.

Treatment: gastric lavage, reception of absorbent carbon, control of the vital functions of an organism, maintenance of respiratory and cardiovascular activity, symptomatic therapy. The hemodialysis is ineffective. As the specific antagonist it can be used flumazenit — intravenously (for 5% solution of a dextrose or 0,9% chloride sodium solution) in an initial dose of 0,2 mg (if necessary — to a dose of 1 mg).

Storage conditions:

In dry, protected from light and the place, unavailable to children, at a temperature up to 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets on 0,5 mg and 1 mg.

On 10 tablets in the blister packaging.

On 1, 2 or 5 blister packagings in a cardboard box with the application instruction.