Composition, form of production and packaging
Solution for intravenous and / m introduction 1 ml
phenazepam (7-bromo-1,3-dihydro-5- (2-chlorophenyl) -2H-1,4-benzodiazepin-2-one) 1 mg
1 ml - ampoules (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
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 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. 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 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 violate the sending mechanism.
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, monosynaltic). Perhaps a direct inhibition of the motor nerves and muscle functions.
Metabolised in the liver with the formation of active metabolites (products of aliphatic and aromatic oxidation). The maximum concentration of the drug after IV introduction occurs after 3 minutes. Decrease in the concentration of phenazepam with its intravenous administration occurs biphasic:? -phase of rapid decrease in concentration and? -phase slow decrease in concentration. Phenazepam is excreted mainly with urine in the form of metabolites.
The steady-state levels of phenazepam 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.
- 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 dysfunction;
- sleep disorders;
- for the prevention of states of fear and emotional stress;
- Reactive psychosis;
- as part of complex therapy for abstinent 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).
Phenazepam is prescribed in / m or in / in (jet or drip).
For rapid relief of fear, anxiety, psychomotor agitation, as well as in autonomic paroxysms and psychotic states: in / m or / in, the initial dose for adults is 0.5-1 mg (0.5-1 ml 0.1% solution), the average daily dose - 3-5 mg (3-5 ml 0.1% solution), in severe cases up to 7-9 mg (7-9 ml 0.1% solution). The duration of the drug is determined by the doctor.
For serial epileptic seizures, the drug is given in / m or IV, starting at a dose of 0.5 mg (0.5 ml 0.1% solution), the average daily dose 1-3 mg (1-3 ml 0.1% solution).
For the treatment of alcohol withdrawal syndrome, phenazepam is given in / m or / in a dose of 0.5 mg once a day (0.5-1 ml 0.1% solution).
In neurological practice for diseases with increased muscle tone, the drug is given in / m 0.5 mg 1-2 times a day (0.5-1 ml 0.1% solution).
Premedication: iv in 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.
From the nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, fatigue, dizziness, decreased ability to concentrate, ataxia, disorientation, gait instability, 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 outbursts, psychomotor agitation, fear, suicidal thoughts, 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 "liver" transaminases and alkaline phosphatases, jaundice.
On the part of the genitourinary system: urinary incontinence, urinary retention, impaired renal function, decreased or increased libido, dysmenorrhea.
Allergic reactions: skin rash, skin 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, 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 Hyperacusia, paresthesia, photophobia, tachycardia, convulsions, rarely - acute psychosis).
- hypersensitivity to the components that make up the drug and to other benzodiazepines;
- Myasthenia gravis;
- Closed-angle glaucoma (acute attack or predisposition);
- Acute alcohol poisoning (with impaired vital functions), narcotic analgesics and hypnotic drugs;
- severe chronic obstructive pulmonary disease (possibly increased respiratory failure);
acute respiratory failure;
- lactation period;
- age under 18 years (safety and efficacy not determined).
With caution: hepatic and / or renal insufficiency, cerebral and spinal ataxia, hyperkinesia, organic brain diseases, drug dependence in history, addiction to psychoactive drugs, psychosis (possible paradoxical reactions) hypoproteinemia, nocturnal apnea (established or suspected), old age, depression (see section "Special instructions").
PREGNANCY AND LACTATION
Contraindicated in pregnancy.
For the duration of treatment, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER
When renal insufficiency is necessary to monitor the picture of peripheral blood.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
When liver failure is necessary to monitor the picture of peripheral blood and liver enzymes.
APPLICATION FOR CHILDREN
Contraindicated for children under the age of 18, because safety and efficacy not determined.
APPLICATION IN ELDERLY PATIENTS
It is necessary to use the drug with caution in elderly patients.
Special care is required when administering 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.
In 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 antidepressants, anxiolytics or 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.
Impact on the ability to drive vehicles and manage mechanisms
Phenazepam is contraindicated during work by drivers of transport and other persons performing work requiring quick reactions and precise movements.
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 - 5% glucose solution or 0.9% sodium chloride solution).
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 blood pressure lowering.
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.
TERMS OF RELEASE FROM PHARMACY
TERMS AND CONDITIONS OF STORAGE
In the dark place at a temperature of 15 to 25 В° C. Keep out of the reach of children. Shelf life - 2 years.