ФЕНОРЕЛАКСАН®

General characteristics. Structure:

Active ingredient: бромдигидрохлорфенилбензодиазепин – 1,0 mg; 

Excipient: povidone (polyvinylpirrolidone low-molecular medical) – 9,0 mg; glycerin (глицерол) – 100,0 mg; sodium disulphite (sodium metabisulphite) - 2,0 mg; the twin-80 (polysorbate 80) – 50,0 mg, sodium hydroxide 1M solution – to pH 6,0-7,5; water for injections – to 1 ml.

Description. The transparent, colourless or slightly painted liquid.

Pharmacological properties:

Pharmacodynamics. Anxiolytic means (tranquilizer) of a benzodiazepine row. Renders anxiolytic, sedative and somnolent, anticonvulsant and central myorelaxation action. Strengthens an inhibiting effect of piperidic acid (GAMK) on transfer of nervous impulses. Stimulates the benzodiazepine receptors located in the allosteric center of postsynaptic GAMK-receptors of the ascending activating reticular formation of a brainstem and internuncial neurons of side horns of a spinal cord; reduces excitability of subcrustal structures of a brain (limbic system, a thalamus, a hypothalamus), brakes polisinaptichesky spinal reflexes.

Anxiolytic action is caused by influence on an amygdaloid complex of limbic system and is shown in reduction of emotional pressure, weakening of alarm, a white crane, concern. Sedation is caused by influence on a reticular formation of a trunk of a brain and nonspecific kernels of a thalamus and are shown by reduction of symptomatology of a neurotic origin (alarm, fear).

Practically does not influence productive symptomatology of psychotic genesis (acute crazy, hallucinatory, affective frustration), reduction of affective tension, crazy frustration is seldom observed. Somnolent action is accompanied by oppression of cells of a reticular formation of a brainstem. Reduces influence of the emotional, vegetative and motor irritants breaking the backfilling mechanism. Anticonvulsant action is implemented by strengthening of presynaptic braking, suppresses a rasprostraniye of a convulsive impulse, but does not remove the excited condition of the center. The central myorelaxation action is caused caused by braking of the polisinaptichesky spinal afferent braking ways (to a lesser extent and monosinaptichesky). Possibly and direct inhibition of motor nerves and function of muscles.

Pharmacokinetics. It is widely distributed in an organism. It is metabolized in a liver. Biological half-life from 6 to 10-18 hours, drug excretion, is generally carried out through kidneys in the form of metabolites.

Indications to use:

Neurotic, neurosis-like, psychopathic and psychopatholike, etc. states (irritability, a trevogozhnost, nervous tension, emotional lability), reactive psychoses and senesto-ipokhondricheskiyerasstroystvo (including resistant to action of other anxiolytic means (tranquilizers), vegetative dysfunctions and frustration of a dream, prevention of conditions of fear and emotional pressure.

As anticonvulsant means - temporal and myoclonic epilepsy. In neurologic practice – hyperkinesias, tics, muscle tension, vegetative lability.

Route of administration and doses:

Drug is appointed intramusculary or intravenously (struyno or kapelno). For bystry stopping of fear, alarm, psychomotor excitement, and also at vegetative paroxysms and psychotic states, an initial dose of 0,5-1 mg (0,5 - 1 ml of 0,1% of solution), an average daily dose – 3-5 mg, in hard cases - to 7-9 mg. At the epileptic status and serial epileptic seizures the drug is administered intramusculary or intravenously since a dose of 0,5 mg. For treatment of alcoholic abstinence of Fenorelaksan® appoint intramusculary or intravenously in a dose of 2,5 - 5 mg a day. In neurologic practice at diseases with the raised muscle tone drug appoint intramusculary on 0,5 mg one or twice a day. For preoperative preparation - intravenously slowly enter 0,003-0,004 (3 - 4 ml of 0,1% of solution) Fenorelaksana®.

The average daily dose of drug makes 1,5 - 5 mg. Maximum daily dose of 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 Fenorelaksana®, 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 Fenorelaksana® 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 Fenorelaksana® 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" can be noted (depressions, irritability, sleeplessness, the increased sweating, etc.), especially at long reception (more than 8-12 weeks). During pregnancy apply only according to "vital" indications.

Has toxic effect on a fruit, and increase 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 TsNS 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 oppressing TsNS to effect of benzodiazepines. 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 of Fenorelaksanom® is not recommended. Фенорелаксан® it is contraindicated in operating time to the drivers of transport and other persons performing the work demanding bystry reactions and exact movements.

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; 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 bodies of a hemopoiesis: leukopenia, neutropenia, agranulocytosis (fever, hyperthermia, pharyngalgia, extraordinary 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 of "hepatic" transaminases 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 the I trimester), oppression of the central nervous system (CNS), disturbance of breath and suppression of a sucking reflex at newborns whose mothers used drug.

Others: accustoming, medicinal dependence; lowering of arterial pressure (ABP); seldom - a 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 hyperacusia, paresthesias, a photophobia; tachycardia, spasms, it is rare - psychotic reactions). Local reactions: phlebitis or venous thrombosis (redness, a swelling or pain in an injection site).

Interaction with other medicines:

Фенорелаксан® it is compatible to other drugs causing TsNS function oppression (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. Increases concentration of Imipraminum in blood serum. Antihypertensives can increase expressiveness of decrease in the ABP. Against the background of co-administration of clozapine strengthening of respiratory depression is possible.

Contraindications:

Hypersensitivity (including to other benzodiazepines), a coma, shock, a myasthenia, closed-angle glaucoma (a bad attack or predisposition), acute alcoholic poisonings (with weakening of the vital functions), narcotic analgetics and somnolent medicines, a heavy chronic obstructive pulmonary disease (strengthening of respiratory insufficiency is possible), acute respiratory insufficiency, a heavy depression (suicide bents can be shown); pregnancy (especially the I trimester), the lactation period, age up to 18 years (safety and efficiency are not defined).

Overdose:

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 Fenorelaksana® nitrate is recommended strychnine (an injection on 1 ml of 0,1% of solution 2-3 times a day). As the specific antagonist it can be used flumazenit (анексат) – intravenously (for 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).

Storage conditions:

In the place protected from light at a temperature from 15 °C to 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 1 ml in ampoules from neutral glass. On 5 ampoules in a blister strip packaging from a film polyvinyl chloride. Two planimetric packagings together with the application instruction and the scarificator ampoule in a pack from a cardboard. On 10 ampoules place in a box from a cardboard. Put the application instruction and the scarificator in each box ampoule. When using ampoules with a point or a ring of a break the scarificator is not put.