Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Anxiolytic agent (tranquilizer) of benzodiazepine series. Has anxiolytic, sedative-hypnotic, anticonvulsant and central muscle relaxant effect.
Increases the inhibitory effect of GABA on the transmission of nerve impulses. Stimulates benzodiazepine receptors located in the allosteric center of postsynaptic GABA receptors of the ascending activating reticular formation of the brainstem 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.
The sedative effect is due to the effect 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 the polysynaptic spinal afferent inhibitory pathways (to a lesser extent, monosynaptic). Perhaps a direct inhibition of the motor nerves and muscle functions.
PHARMACOKINETICS
After oral administration it is well absorbed from the digestive tract, T max - 1-2 hours Metabolised in the liver. T 1/2 - 6-10-18 h. It is excreted mainly by kidneys in the form of metabolites.
INDICATIONS
Neurotic, neurotic, psychopathic and psychopathic and other conditions (irritability, anxiety, nervous tension, emotional lability), reactive psychoses and senesto-hypochondriacal disorders (including those resistant to the action of other anxiolytic drugs (tranquilizers), obsessive, insomnia, abstinence syndrome (alcoholism, substance abuse), epileptic status, epileptic seizures (of various etiologies), temporal and myoclonic epilepsy.
In extreme conditions - as a means to ease the overcoming of feelings of fear and emotional tension.
As an antipsychotic - schizophrenia with increased sensitivity to antipsychotic drugs (including the febrile form).
In neurological practice - rigidity of muscles, athetosis, hyperkinesia, tick, vegetative lability (paroxysms of sympathoadrenal and mixed character).
In anesthesiology - premedication (as a component of introductory anesthesia).
DOSING MODE
In / m or in / in (jet or drip): for rapid relief of fear, anxiety, psychomotor agitation, as well as in vegetative paroxysms and psychotic conditions, the initial dose is 0.5-1 mg, the average daily dose is 3-5 mg, in severe cases - up to 7-9 mg.
Inside: for violations of sleep - 250-500 mcg for 20-30 minutes before sleep. For treatment of neurotic, psychopathic, neurosis-like and psychopathic-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, the dose can be increased to 4-6 mg / day. With severe agitation, fear, anxiety, treatment starts with a dose of 3 mg / day, rapidly increasing the dose to obtain a therapeutic effect. In the treatment of epilepsy - 2-10 mg / day.
For the treatment of alcohol withdrawal - inside, 2-5 mg / day or in / m, 500 mcg 1-2 times / day, with vegetative paroxysms - in / m, 0.5-1 mg. 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 in the afternoon and up to 2.5 mg at night. In neurological practice, for diseases with muscular hypertension, 2-3 mg 1-2 times / day are prescribed. The maximum daily dose is 10 mg.
To avoid the development of drug dependence in course treatment, the duration of the use of phenazepam is 2 weeks (in some cases, the duration of treatment can be increased to 2 months). With the abolition of phenazepam, the dose is reduced gradually.
SIDE EFFECT
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, unsteadiness of gait, slowing of mental and motor reactions, confusion; rarely headache, euphoria, depression, tremor, memory loss, movement coordination disorders (especially at high doses), mood depression, dystonic extrapyramidal reactions (uncontrolled movements, including the eye), asthenia, myasthenia gravis, dysarthria, epileptic seizures (in patients with epilepsy); extremely rarely - paradoxical reactions (aggressive outbreaks, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, agitation, irritability, anxiety, insomnia).
From the hemopoiesis: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, excessive fatigue or weakness), anemia, thrombocytopenia.
On the part of the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, decreased appetite, constipation or diarrhea; violations of liver function, increased activity of hepatic transaminases and alkaline phosphatase, jaundice.
On the part of the genitourinary system: urinary incontinence, urinary retention, impaired renal function, decreased or increased libido, dysmenorrhea.
Allergic reactions: skin rash, itching.
Local reactions: phlebitis or venous thrombosis (redness, swelling or pain at the injection site).
Other: addiction, drug dependence; a decrease in blood pressure; rarely - visual impairment (diplopia), weight loss, tachycardia.
With a sharp decrease in dose or discontinuation of reception - 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, perception disorders, incl. hyperaemia, paresthesia, photophobia, tachycardia, convulsions, rarely - acute psychosis).
CONTRAINDICATIONS
Coma, shock, myasthenia gravis, occlusive glaucoma (acute attack or predisposition), acute alcohol poisoning (with impaired vital functions), narcotic analgesics and hypnotics, severe COPD (possibly increased respiratory failure), acute respiratory failure, severe depression (may manifest suicidal tendencies); I trimester of pregnancy, lactation, children and adolescents under 18 years (safety and efficacy not determined), hypersensitivity (including to other benzodiazepines).
PREGNANCY AND LACTATION
In pregnancy, use is only possible for life indications. Has a toxic effect on the fetus and increases the development of congenital malformations when applied in the first trimester of pregnancy. Admission to therapeutic doses in later periods of pregnancy can cause CNS depression in a newborn. Continuous use during pregnancy can lead to physical dependence with the development of withdrawal syndrome in a newborn. Children, especially at a young age, are very sensitive to the CNS depressing action of benzodiazepines.
The use immediately before childbirth or during labor can cause a respiratory depression in the newborn, a reduction in muscle tone, hypotension, hypothermia, and a weak act of sucking ("sluggish child" syndrome).
APPLICATION FOR FUNCTIONS OF THE LIVER
Use with caution in renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Use with caution in liver failure.
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 18 years of age (safety and efficacy not determined).
SPECIAL INSTRUCTIONS
Use with caution in patients with hepatic and / or renal insufficiency, cerebral and spinal ataxia, drug dependence in history, addiction to psychoactive drugs, hyperkinesia, organic brain diseases, psychosis (possible paradoxical reactions), hypoproteinemia, nocturnal apnea (established or suspected ), in elderly patients.
In renal and / or hepatic insufficiency and long-term treatment, it is necessary to monitor the picture of peripheral blood and the activity of hepatic enzymes.
Patients who had not previously taken psychoactive drugs had a therapeutic response to the use of phenazepam in lower doses, compared with patients taking antidepressants, anxiolytics or alcoholism.
Like other benzodiazepines, it has the ability to induce drug dependence in long-term admission in large doses (more than 4 mg / day). With a sudden discontinuation of reception may be a withdrawal syndrome (including depression, irritability, insomnia, increased sweating), especially with prolonged admission (more than 8-12 weeks). When patients develop such unusual reactions as increased aggressiveness, acute excitations, feelings of fear, thoughts of suicide, hallucinations, increased muscle cramps, difficulty falling asleep, superficial sleep, treatment should be discontinued.
In the course of treatment, patients are strictly prohibited from drinking ethanol.
The efficacy and safety of the drug in patients under the age of 18 years is not established.
In case of an overdose, severe drowsiness, prolonged confusion, decreased reflexes, prolonged dysarthria, nystagmus, tremor, bradycardia, shortness of breath or shortness of breath, a decrease in blood pressure, coma may occur. Recommended gastric lavage, the reception of activated charcoal; symptomatic therapy (maintenance of respiration and blood pressure), administration of flumazenil (in hospital settings); hemodialysis is ineffective.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
DRUG INTERACTION
With simultaneous use of phenazepam reduces the effectiveness of levodopa in patients with Parkinsonism.
Phenazepam may increase the toxicity of zidovudine.
There is a mutual enhancement of the effect with simultaneous use of antipsychotic, antiepileptic or hypnotic drugs, as well as central muscle relaxants, narcotic analgesics, ethanol.
Inhibitors of microsomal oxidation increase the risk of toxic effects. Inducers of microsomal liver enzymes reduce efficacy.
Increases the concentration of imipramine in the blood serum.
With simultaneous use with antihypertensive agents, it is possible to increase antihypertensive action. Against the background of simultaneous administration of clozapine, an increase in respiratory depression is possible.
