Active substanceBromodihydrochlorophenylbenzodiazepineBromodihydrochlorophenylbenzodiazepine
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  • Dosage form: & nbspsolution for intravenous and intramuscular administration
    Composition:
    In 1 ml of solution contains:
    active substance:
    bromodihydrochlorophenylbenzodiazepine (phenazepam) -1.0 mg
    Excipients:
    povidone (polyvinylpyrrolidone low molecular weight medical) - 9.0 mg, glycerol (glycerin) - 100.0 mg, sodium disulfite (sodium pyrosulfite) 2.0 mg, polysorbate 80 (tween 80) 50.0 mg, sodium solution hydroxide (sodium hydroxide) 1M - to pH 6.0-7.5, water for injection-up to 1ml.
    Description:transparent colorless or slightly colored liquid
    Pharmacotherapeutic group:Anxiolytic agent (tranquilizer).
    ATX: & nbsp

    N.05.B.X   Other anxiolytics

    Pharmacodynamics:

    Phenazepam is a benzodiazepine derivative.

    Has a pronounced anxiolytic, hypnotic, sedative, as well as anticonvulsant and central muscle relaxant action.

    Increases the inhibitory effect of gamma-aminobutyric acid on the transmission of nerve impulses. Stimulates benzodiazepine receptors located in allosteric center of postsynaptic GABA receptors ascending activating the reticular formation of the brain stem and intercalary 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.

    Anxiolytic action is due to the influence on the amygdala complex of the limbic system and is manifested in a decrease in emotional tension, easing anxiety, fear, anxiety. Its severity depends not so much on the concentration of the drug in the blood, as on the rate of its absorption and dormancy in the systemic blood flow.

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

    The productive symptomatology of psychotic genesis (acute delusional, hallucinatory, affective disorders) practically does not affect, rarely a decrease in affective tension, delusional disorders.

    Sleeping effect is associated with depression of the cells of the reticular formation of the brain stem. Reduces the impact of emotional, vegetative and motor stimuli, which break the mechanism of falling asleep.

    Anticonvulsant action is realized by strengthening presynaptic inhibition, suppressing the spread of convulsive impulse, but the excited state of the focus is not removed.

    Central miorelaksiruyuschee effect due to inhibition of polysynaltic spinal afferent inhibitory pathways (to a lesser extent, monosynaptic). Perhaps a direct inhibition of the motor nerves and muscle functions.

    Pharmacokinetics:

    Metabolized in the liver with the formation of active metabolites (products of aliphatic and aromaticoxidation). The maximum concentration of the drug after intravenous injection occurs after 3 minutes. Reduction in the concentration of phenazepam ® with its intravenous administration occurs biphasic: alpha-phase of rapid reduction in concentration and beta-phase slow decrease in concentration. Phenazepam® is excreted mainly with urine in the form of metabolites.

    Fenazepam® steady-state levels of concentration are established in the blood plasma of patients 10 days after the start of treatment and vary from 6.4 to 292 ng / ml. The optimal therapeutic effect is achieved if the constant concentration of Phenazepam ® in the blood does not exceed 30-70 ng / ml, the side effects are most pronounced when the concentrations exceed 100 ng / ml.

    Indications:

    Neurotic, neurotic, psychopathic and psychopathic conditions, accompanied by anxiety, fear, increased irritability, tension and emotional lability, hypochondriacal-synastopathic syndrome (including resistant to the action of other tranquilizers), autonomic dysfunctions, sleep disorders, for the prevention of states of fear and emotional stress , reactive psychosis; as part of complex therapy for withdrawal and toxicomanic syndrome.

    As an anticonvulsant drug is used to treat patients with temporal and myoclonic epilepsy.

    In neurological practice the drug is used to treat hyperkinesis and tics, with rigidity of muscles, vegetative lability.

    In anesthesiology, the drug is used for premedication (as a component of anesthesia induction).

    Contraindications:

    Hypersensitivity to the components of the drug and other benzodiazepines, coma, shock, myasthenia gravis, zakratougolnaya glaucoma (acute attack or predisposition), acute alcohol poisoning (with weakening vital functions), narcotic analgesics and hypnotic drugs, severe chronic obstructive disease lungs (possibly increased respiratory failure), acute respiratory failure; pregnancy, lactation, age under 18 years (safety and efficacy not determined).

    Carefully:

    hepatic and / or renal insufficiency, cerebral and spinal ataxia, hyperkinesis, organic brain diseases, drug addiction in the anamnesis, propensity to abuse of psychoactive drugs,psychosis (possible paradoxical reactions) hypoproteinemia, nocturnal apnea (established or suspected), advanced age, depression (see section "Special instructions").

    Pregnancy and lactation:

    Contraindicated in pregnancy. For the duration of treatment, breastfeeding should be discontinued.

    Dosing and Administration:

    Phenazepam® is administered intramuscularly or intravenously (either by jet or by drip).

    For rapid relief of fear, alarms. psychomotor agitation. as well as in autonomic paroxysms and psychotic states: intramuscularly or intravenously, the initial dose for adults is 0.5-1 mg (0.5-1 ml 0.1% solution), the average daily dose is 3-5 mg (3-5 ml 0.1% solution), in severe cases up to 7-9 mg ( 7-9 ml of 0.1% solution). The duration of the drug is determined by the doctor.

    When serial epileptic seizures the drug is administered intramuscularly or intravenously, starting with a dose of 0.5 mg (0.5 ml 0.1% solution), the average daily dose of 1-3 mg (1 - 3 ml 0.1% solution).

    For the treatment of alcohol withdrawal syndrome Phenazepam ® is administered intramuscularly or intravenously at a dose of 0.5 mg - 1 time per day (0.5-1 ml 0.1% solution).

    In neurological practice for diseases with increased muscle tone, the drug is administered intramuscularly by 0.5 mg 1-2 times a day (0.5-1 ml 0.1%solution).

    Premedication: intravenously slowly 3-4 ml 0.1% solution.

    The maximum daily dose is 10 mg. The course of treatment for parenteral admission - up to 3 - 4 weeks. With the withdrawal of the drug, the dose is reduced gradually.

    After achieving a sustainable therapeutic effect, it is advisable to switch to oral dosage forms of the drug.

    Side effects:

    From the nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, fatigue, dizziness, decreased ability to concentrate, ataxia, disorientation, unsteadiness of gait, slowing of mental and motor reactions, confusion; rarely headache, euphoria, depression, tremor, memory loss, movement coordination disorders (especially at high doses), depression of mood, dystonic extrapyramidal reactions (uncontrolled movements, including eyes), asthenia, myasthenia gravis, dysarthria, epileptic seizures (in patients with epilepsy); extremely rarely - paradoxical reactions (aggressive outbursts, psychomotor agitation, fear, suicidal thoughts, muscle spasm, hallucinations, agitation, irritability, anxiety, insomnia).

    On the part of the organs of hematopoiesis: 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; violations of liver function, increased activity of "liver" trances and called alkaline phosphatases, jaundice.

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

    Allergic reactions: skin rash, itching of the skin.

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

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

    With a sharp decrease in dose or discontinuation of reception, there may be a withdrawal syndrome (irritability, nervousness, sleep disturbances, dysphoria, spasm of smooth muscles of the internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perceptual disorders, in tons .h.hyperaemia, paresthesia, photophobia; tachycardia, convulsions, rarely - acute psychosis).

    Overdose:

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

    Treatment: control of vital body functions, maintenance of respiratory and cardiovascular activity, symptomatic therapy. Specific antagonist flumazenil (iv 0.2 mg - if necessary up to 1 mg - on 5% solution of glucose or 0.9% solution of sodium chloride).

    Interaction:

    Strengthens the action of neuroleptics, tranquilizers, hypnotics, anesthesia, analgesics, anticonvulsants, alcohol.

    Reduces the effectiveness of levodopa in patients with Parkinsonism.

    May increase the toxicity of zidovudine.

    Inhibitors of microsomal oxidation increase the risk of toxic effects.

    Inducers of microsomal liver enzymes reduce efficacy.

    Increases the concentration of imipramine in the serum.

    Hypotensive drugs can increase the severity of lowering blood pressure.

    Against the background of simultaneous administration of clozapine, an increase in respiratory depression is possible. With simultaneous use with sidnokarbom the effectiveness of phenazepam decreases sharply, which is accompanied by a decrease in the concentration of phenazepam in the blood.

    Special instructions:

    It is necessary to observe special care in the appointment of Phenazepam ® in severe depression; the drug can be used to implement suicidal intentions. It is necessary to use the drug with caution in elderly and weakened patients.

    With renal / hepatic insufficiency and long-term treatment, control over the picture of peripheral blood and "hepatic" enzymes is necessary.

    Patients who did not take previously psychoactive drugs "respond" to the drug at lower doses compared with patients taking anti-depressants, anxiolytics or suffering from alcoholism.

    When patients develop such unusual reactions as increased aggressiveness, acute excitement, feelings of fear, thoughts of suicide, hallucinations, increased muscle cramps, difficult sleep, superficial sleep, treatment should be discontinued.

    The frequency and nature of side effects depend on the individual sensitivity, dose and duration of treatment. With decreasing doses or stopping the use of phenazepam, side effects disappear.

    The drug enhances the effect of alcohol, so the use of alcohol during treatment with phenazepam ® is not recommended.

    Phenazepam® is contraindicated during operation by transport drivers and other persons performing work requiring quick reactions and precise movements.

    Effect on the ability to drive transp. cf. and fur:Phenazepam® is contraindicated during operation by transport drivers and other persons performing work requiring quick reactions and precise movements.
    Form release / dosage:

    Solution for intravenous and intramuscular injection 1 mg / ml.

    Packaging:

    Solution for intravenous and intramuscular injection 1 mg / ml.

    1 ml in ampoules, glass, 10 ampoules with instructions for use and ampoule scapegrip are placed in a box of cardboard, or 5 or 10 ampoules are placed in a contiguous cell pack of a polyvinyl chloride film.

    For 1 or 2 contour packs with instructions for use and a scapegrator ampullum is placed in a pack of cardboard.

    For 50 or 100 ampoules with instructions for use and a scapegrator ampoule in a pack of cardboard with a cardboard grid.

    When packaging ampoules with a color break ring or break point, the ampoule scaper is allowed not to be put.

    When packing 50 or 100 ampoules per pack of cardboard with a cardboard grill, the scapper can be ampouled separately.

    Storage conditions:

    In the dark place at a temperatureround from 15 to 25 ° C.

    Keep out of the reach of children.

    Shelf life:2 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-001772/09
    Date of registration:10.03.2009
    The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Manufacturer: & nbsp
    Representation: & nbspVALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Information update date: & nbsp10.12.2015
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