Бромдигидрохлорфенилбензодиазепин

neurotic, neurosis-like, psychopathic, psychopath-like and other conditions accompanied by anxiety, fear, increased irritability, tension, emotional lability,

reactive psychoses and hypochondriac-senestopathic syndrome (including those resistant to the action of other tranquilizers),

autonomic dysfunction and sleep disorders,

prevention of states of fear and emotional tension,

temporal lobe and myoclonic epilepsy (as an anticonvulsant),

treatment of hyperkinesis and tics, muscle rigidity, vegetative lability.

neurotic, neurosis-like, psychopathic and psychopath-like and other conditions (irritability, anxiety, nervous tension, emotional lability),

reactive psychosis and senestopathic-hypochondriac disorders (including those resistant to the action of other anxiolytic drugs (tranquilizers),

autonomic dysfunction and sleep disorder,

prevention of states of fear and emotional tension,

as an anticonvulsant — temporal lobe and myoclonic epilepsy,

in neurological practice-hyperkinesis, tics, muscle rigidity, vegetative lability.

Inside.

Sleep disorders. 0.5 mg for 20-30 minutes before bedtime.

Treatment of neurotic, psychopathic, neurosis-like, and psychopathic conditions. The initial dose is 0.5-1 mg 2-3 times a day. After 2-4 days, taking into account the effectiveness and tolerability, the dose can be increased to 4-6 mg/day.

Pronounced agitation, fear, anxiety. Treatment begins with a dose of 3 mg/day, rapidly increasing the dose until a therapeutic effect is obtained.

Treatment of epilepsy. 2-10 mg/day.

Treatment of alcohol withdrawal. 2-5 mg/day.

The average daily dose is 1.5-5 mg, it is divided into 2-3 doses, usually 0.5-1 mg in the morning and afternoon and up to 2.5 mg at night. In neurological practice for diseases with muscle hypertonicity appoint 2-3 mg 1-2 times per day.

The maximum daily dose is 10 mg.

To avoid the development of drug dependence in the course of treatment, the duration of use of the drug Phenazepam^® it is 2 weeks (in some cases, the duration of treatment can be increased to 2 months). When the drug is discontinued, the dose is reduced gradually.

Tablets: inside.

In case of sleep disorders-0.25-0.5 mg 20-30 minutes before bedtime.

For the treatment of neurotic, psychopathic, neurosis-like and psychopath-like conditions, the initial dose is 0.5-1 mg 2-3 times a day. After 2-4 days, taking into account the effectiveness and tolerability of the drug, the dose can be increased to 4-6 mg/day.

With severe agitation, fear, anxiety, treatment begins with a dose of 3 mg/day, quickly increasing the dose until a therapeutic effect is obtained.

In the treatment of epilepsy-2-10 mg/day.

For the treatment of alcohol withdrawal — 2.5-5 mg/day.

The average daily dose is 1.5-5 mg, it is divided into 2-3 doses, usually 0.5-1 mg in the morning and afternoon and up to 2.5 mg at night. In neurological practice, for diseases with muscular hypertension-2-3 mg 1 or 2 times a day.

The maximum daily dose is 10 mg.

To avoid the development of drug dependence in the course of treatment, the duration of use of Bromodihydrochlorophenylbenzodiazepine^® as with other benzodiazepines, it is 2 weeks (in some cases, the duration of treatment can be increased to 2 months).

When the drug is discontinued, the dose is reduced gradually.

Solution for intravenous and intravenous administration: intravenous or intravenous (jet or drip).

For rapid relief of fear, anxiety, psychomotor agitation, as well as for vegetative paroxysms and psychotic states, the initial dose is 0.5-1 mg (0.5-1 ml of 0.1% solution), the average daily dose is 3-5 mg, in severe cases-up to 7-9 mg.

With epileptic status and serial epileptic seizures, the drug is administered intravenously or intravenously, starting with a dose of 0.5 mg.

For the treatment of alcohol withdrawal — in/m or in / in at a dose of 2.5-5 mg per day.

In neurological practice, in diseases with increased muscle tone-in/m 0.5 mg 1 or 2 times a day. For preoperative preparation, 0.003–0.004 g (3-4 ml of 0.1% solution) is slowly administered in/in.

The average daily dose is 1.5-5 mg. The maximum daily dose is 10 mg.

After achieving a stable therapeutic effect, it is advisable to switch to taking an oral dosage form of the drug.

To avoid the development of drug dependence in the course of treatment, the duration of use of Bromodihydrochlorophenylbenzodiazepine^® as with other benzodiazepines, it is 2 weeks. But in some cases, the duration of treatment can be increased to 3-4 weeks.

When the drug is discontinued, the dose is reduced gradually.

hypersensitivity (including to other benzodiazepines),

coma,

shock,

myasthenia gravis,

angle-closure glaucoma (acute attack or predisposition),

acute poisoning with alcohol (with the weakening of vital functions), narcotic analgesics and sleeping pills,

severe chronic obstructive pulmonary disease (possibly increased respiratory failure),

acute respiratory failure,

severe depression (suicidal tendencies may occur),

pregnancy (especially the first trimester),

lactation period,

children and adolescents under 18 years of age (safety and efficacy not determined).

With caution: hepatic and / or renal insufficiency, cerebral and spinal ataxia, a history of drug dependence, a tendency to abuse psychoactive drugs, hyperkinesis, organic brain diseases, psychosis (paradoxical reactions are possible), hypoproteinemia, nocturnal apnea (established or suspected), old age.

hypersensitivity (including to other benzodiazepines),

coma,

shock,

myasthenia gravis,

angle-closure glaucoma (acute attack or predisposition),

acute poisoning with alcohol (with the weakening of vital functions), narcotic analgesics and sleeping pills,

severe COPD (possibly increasing respiratory failure),

acute respiratory failure,

severe depression (suicidal tendencies may occur),

pregnancy (especially the first trimester),

lactation period,

under 18 years of age (safety and efficacy not determined).

With caution:

hepatic and / or renal insufficiency,

cerebral and spinal ataxia,

a history of drug addiction,

propensity to abuse psychoactive drugs,

hyperkinesis,

organic diseases of the brain,

psychosis (possible paradoxical reactions),

hypoproteinemia,

sleep apnea (or suspected to be installed),

old age.

From the central nervous system and peripheral nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, fatigue, dizziness, decreased ability to concentrate, ataxia, disorientation, gait instability, slow mental and motor reactions, confusion, rarely-headache, euphoria, depression, tremor, memory loss, impaired coordination of movements (especially at high doses), mood depression, dystonic extrapyramidal reactions (uncontrolled movements, in t.tsch. eye), asthenia, muscle weakness, dysarthria, epileptic seizures (in patients with epilepsy), extremely rare-paradoxical reactions (aggressive outbursts, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, agitation, irritability, anxiety, insomnia)

From the side of the hematopoietic organs: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, excessive fatigue or weakness), anemia, thrombocytopenia.

From the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, decreased appetite, constipation or diarrhea, impaired liver function, increased activity of hepatic transaminases and alkaline phosphatase, jaundice.

From the genitourinary system: urinary incontinence, urinary retention, impaired kidney function, decreased or increased libido, dysmenorrhea.

Allergic reactions: skin rash, itching.

Other: addiction, drug dependence, decreased blood pressure, rarely-visual impairment (diplopia), weight loss, tachycardia.

With a sharp reduction in the dose or discontinuation of administration-withdrawal syndrome (irritability, nervousness, sleep disorders, dysphoria, spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perception disorders, including hyperacusis, paresthesia, photophobia, tachycardia, convulsions, rarely — acute psychosis).

Pills

Sometimes there are violations of memory, concentration, coordination of movements (especially at high doses), drowsiness, muscle weakness, ataxia, sometimes paradoxical arousal, dizziness, headache, dry mouth, nausea, diarrhea, menstrual disorders, decreased libido, dysuria, skin rash, itching.

With long-term use (especially in high doses) - addiction, drug addiction.

Solution for intravenous and intravenous administration

From the nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, fatigue, dizziness, impaired concentration, ataxia, disorientation, slow mental and motor reactions, confusion, rarely-headache, euphoria, depression, tremor, memory loss, impaired coordination of movements (especially at high doses), decreased mood, dystonic extrapyramidal reactions (uncontrolled movements, in t.tsch. eye), asthenia, myasthenia gravis, dysarthria, extremely rare-paradoxical reactions (aggressive outbursts, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, anxiety, sleep disorders)

From the side of the hematopoietic organs: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, extreme fatigue or weakness), anemia, thrombocytopenia.

From the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, decreased appetite, constipation or diarrhea, impaired liver function, increased activity of hepatic transaminases and alkaline phosphatase, jaundice.

From the genitourinary system: urinary incontinence, urinary retention, impaired kidney function, decreased or increased libido, dysmenorrhea.

Allergic reactions: skin rash, itching.

Effect on the fetus: teratogenicity (especially in the first trimester), central nervous system depression, respiratory disorders, and suppression of the sucking reflex in newborns whose mothers took the drug.

Other: addiction, drug dependence, decreased blood pressure, rarely-visual impairment (diplopia), weight loss, tachycardia. With a sharp reduction in the dose or discontinuation of administration-withdrawal syndrome (sleep disturbance, dysphoric reactions, spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perception disorder, including hyperacusis, paresthesia, photophobia, tachycardia, convulsions, rarely — psychotic reactions).

Local reactions: phlebitis or venous thrombosis (redness, swelling or pain at the injection site).

Symptoms: severe depression of consciousness, cardiac and respiratory activity, severe drowsiness, prolonged confusion, decreased reflexes, prolonged dysarthria, nystagmus, tremor, bradycardia, shortness of breath or difficulty breathing, decreased blood pressure, coma.

Treatment: gastric lavage, administration of activated charcoal, control of vital body functions, maintenance of respiratory and cardiovascular activity, symptomatic therapy. Hemodialysis is ineffective.

A specific antagonist is flumazenil (in a hospital setting) in / in 0.2 mg, if necessary-up to 1 mg in 5% glucose solution or 0.9% sodium chloride solution.

Pills

Symptoms: severe drowsiness, prolonged confusion, decreased reflexes, prolonged dysarthria, nystagmus, tremor, bradycardia, shortness of breath or difficulty breathing, decreased blood pressure, coma.

Treatment: gastric lavage, taking activated charcoal. Symptomatic therapy (maintenance of respiration and blood pressure), administration of flumazenil (in a hospital setting). Hemodialysis is ineffective.

Solution for intravenous and intravenous administration

Symptoms: with a moderate overdose-an increase in the therapeutic effect and side effects, with a significant overdose-pronounced depression of consciousness, cardiac and respiratory activity.

Treatment: control of vital functions of the body, maintenance of respiratory and cardiovascular activity, symptomatic therapy. As antagonists of the muscle relaxant action of Bromodihydrochlorophenylbenzodiazepine^® strychnine nitrate is recommended (injections of 1 ml of 0.1% solution 2-3 times a day). Flumazenil (anexate) can be used as a specific antagonist.) - in/in (on a 5% solution of glucose (dextrose) or 0.9% solution of sodium chloride) at an initial dose of 0.2 mg (if necessary, up to a dose of 1 mg).

An anxiolytic agent (tranquilizer) of the benzodiazepine series. It has an anxiolytic, sedative-hypnotic, anticonvulsant and central muscle relaxant effect.

Increases the inhibitory effect of GABA on the transmission of nerve impulses. It stimulates benzodiazepine receptors located in the allosteric center of postsynaptic GABA receptors of the ascending activating reticular formation of the brain stem, reduces the excitability of subcortical structures of the brain (limbic system, thalamus, hypothalamus), inhibits polysynaptic spinal reflexes.

The anxiolytic effect is due to the influence on the amygdala complex of the limbic system and manifests itself in reducing emotional tension, easing anxiety, fear, and anxiety.

The sedative effect is due to the effect on the reticular formation of the brain stem and the nonspecific nuclei of the thalamus and is manifested by a decrease in the symptoms of neurotic origin (anxiety, fear).

The productive symptoms of psychotic genesis (acute delusional, hallucinatory, affective disorders) are practically not affected, rarely there is a decrease in affective tension, delusional disorders.

The hypnotic effect is associated with the suppression of the cells of the reticular formation of the brain stem. Reduces the effect of emotional, vegetative and motor stimuli that disrupt the mechanism of falling asleep.

The anticonvulsant effect is realized by strengthening the presynaptic inhibition, suppresses the spread of the convulsive impulse, but does not eliminate the excited state of the focus.

The central muscle relaxant effect is caused by the inhibition of the polysynaptic spinal afferent inhibitory pathways (to a lesser extent — and monosynaptic). Direct inhibition of motor nerves and muscle function is also possible.

Increases the inhibitory effect of GABA on the transmission of nerve impulses. It stimulates benzodiazepine receptors located in the allosteric center of postsynaptic GABA receptors of the ascending activating reticular formation of the brainstem and the insertion neurons of the lateral horns of the spinal cord, reduces the excitability of subcortical structures of the brain (limbic system, thalamus, hypothalamus), inhibits polysynaptic spinal reflexes.

The anxiolytic effect is due to the influence on the amygdala complex of the limbic system and manifests itself in reducing emotional tension, easing anxiety, fear, and anxiety.

The sedative effect is due to the effect on the reticular formation of the brain stem and the nonspecific nuclei of the thalamus and is manifested by a decrease in the symptoms of neurotic origin (anxiety, fear).

The productive symptoms of psychotic genesis (acute delusional, hallucinatory, affective disorders) are practically not affected, rarely there is a decrease in affective tension, delusional disorders.

The hypnotic effect is associated with the suppression of the cells of the reticular formation of the brain stem. Reduces the impact of emotional, vegetative and motor stimuli that disrupt the mechanism of falling asleep.

The anticonvulsant effect is realized by strengthening the presynaptic inhibition, suppresses the spread of the convulsive impulse, but does not relieve the excited state of the focus.

The central muscle relaxant effect is caused by the inhibition of the polysynaptic spinal afferent inhibitory pathways (to a lesser extent, monosynaptic ones). Direct inhibition of motor nerves and muscle function is also possible.

After oral administration, it is well absorbed from the gastrointestinal tract, T_max in the blood plasma-1-2 hours. It is metabolized in the liver. T_1/2 — 6-10-18 hours. It is mainly excreted by the kidneys in the form of metabolites.

Pills

After oral administration, it is well absorbed from the gastrointestinal tract, TC_max - 1-2 hours. It is metabolized in the liver. T_1/2 — 6-10-18 hours. It is mainly excreted by the kidneys in the form of metabolites.

Solution for intravenous and intravenous administration

It is widely distributed in the body. It is metabolized in the liver. T_1/2 from the body from 6 to 10-18 hours, the drug is mainly excreted through the kidneys in the form of metabolites.

With simultaneous use of the drug Phenazepam^® reduces the effectiveness of levodopa in patients with parkinsonism.

The drug Phenazepam^® may increase the toxicity of zidovudine.

There is a mutual strengthening of the effect with the simultaneous use of antipsychotic, antiepileptic or hypnotic drugs, as well as central muscle relaxants, narcotic analgesics, and ethanol.

Microsomal oxidation inhibitors increase the risk of toxic effects. Inducers of microsomal liver enzymes reduce the effectiveness.

Increases the concentration of imipramine in the blood serum.

When used simultaneously with antihypertensive agents, it is possible to increase the antihypertensive effect.

Against the background of simultaneous administration of clozapine, increased respiratory depression is possible.

Bromodihydrochlorophenylbenzodiazepine^® It is compatible with other drugs that cause depression of the central nervous system (hypnotics, anticonvulsants, neuroleptics, etc.), but when used in combination, it is necessary to take into account the mutual strengthening of their action.

Reduces the effectiveness of levodopa in patients with parkinsonism.

May increase the toxicity of zidovudine.

Microsomal oxidation inhibitors increase the risk of toxic effects.

Inducers of microsomal liver enzymes reduce the effectiveness.

Increases the concentration of imipramine in the blood serum.

Antihypertensive agents can increase the severity of a decrease in blood pressure.

Against the background of simultaneous administration of clozapine, increased respiratory depression is possible.

Optional for tablets: there is a mutual strengthening of the effect with the simultaneous administration of central muscle relaxants, narcotic analgesics, and ethanol.