Anxiolytic, hypnotic, sedative, anticonvulsant, muscle relaxant. Enhances 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 brain stem and intercalated neurons of the lateral horns of the spinal cord; reduces the excitability of the subcortical structures of the brain (limbic system, thalamus, hypothalamus), inhibits polysynaptic spinal reflexes. The anxiolytic effect is due to the effect on the amygdala complex of the limbic system and is manifested in a decrease in emotional stress, easing anxiety, fear, anxiety. The sedative effect is due to the effect on the reticular formation of the brain stem and non-specific 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. Hypnotic effect is associated with inhibition of the cells of the reticular formation of the brain stem. Reduces the effects of emotional, vegetative and motor stimuli that violate the mechanism of falling asleep. The anticonvulsant effect is realized by enhancing presynaptic inhibition, suppresses the spread of the convulsive impulse, but the excited state of the focus is not removed. The central muscle relaxant effect is due to inhibition of the polysynaptic spinal afferent inhibitory pathways (to a lesser extent, monosynaptic). Direct inhibition of motor nerves and muscle function is also possible.
Neurotic, neurosis-like, psychopathic and psychopathic states, accompanied by anxiety, fear, increased irritability, tension and emotional lability; sleep disorders, obsessive states, panic disorder, phobias, reactive psychosis; autonomic lability, hypochondriac-synestopathic syndrome; convulsive seizures of various etiologies, temporal and myoclonic epilepsy, status epilepticus, muscle stiffness, tic, athetosis, hyperkinesis; premedication (as a component of induction anesthesia); as part of complex therapy for withdrawal and substance abuse syndrome, schizophrenia (febrile form, hypersensitivity to antipsychotic drugs); prevention of states of fear and emotional stress.
Inside, in / m or in / in (stream or drip). The dosage regimen is set strictly individually depending on the indications, course of the disease, tolerance, etc. For quick relief of fear, anxiety, psychomotor agitation, as well as in case of vegetative paroxysms and psychotic conditions: i / m or iv, the initial dose for adults is 0 , 5-1 mg (0.5-1 ml of a 0.1% solution), the average daily intake is 3-5 mg, in severe cases, up to 7-9 mg. Premedication: iv slowly 3-4 mg (3-4 ml of a 0.1% solution). When taken orally, a single dose for adults is usually 0.5-1 mg (for sleep disorders - 0.25-0.5 mg), the average daily intake is 1.5-5 mg in 2-3 doses (usually 0.5 -1 mg in the morning and in the afternoon and up to 2.5 mg at night), the maximum daily intake is 10 mg. Neurotic, neurosis-like, psychopathic and psychopathic conditions: inside, the initial dose of 0.5-1 mg 2-3 times a day, after 2-3 days (if necessary) - up to 4-6 mg / day; with severe agitation, the initial dose is 3 mg / day, then the dose is rapidly increased until a therapeutic effect is obtained. Neurological practice (diseases with increased muscle tone): inside 2-3 mg 1-2 times a day or IM 0.5 mg 1-2 times a day. Status epilepticus, serial epileptic seizures: IM or IV, starting with a dose of 0.5 mg. In the treatment of epilepsy - 2-10 mg / day. Alcohol withdrawal: by mouth, 2.5-5 mg / day. The course of treatment with oral administration is 2 weeks (if necessary - up to 2 months), with parenteral administration - up to 3-4 weeks. Use with caution in old age and in children (the daily dose is reduced by 2-3 times).
From the nervous system and sensory organs: dizziness, headache, drowsiness, muscle weakness, impaired memory, concentration of attention, coordination of movements, paradoxical agitation, ataxia, mydriasis. From the digestive tract: dry mouth, nausea, diarrhea. Allergic reactions: skin rash, itching. Other: dysuria, dysmenorrhea, decreased libido, addiction, drug dependence.
Severe myasthenia gravis, severe liver damage (cirrhosis, Botkin's disease) and kidney; poisoning with other tranquilizers, antipsychotics, sleeping pills, drugs, alcohol; pregnancy, breastfeeding.
Enhances (mutually) the action of antipsychotics, tranquilizers, sleeping pills, narcotic, analgesic, anticonvulsants, alcohol.
T = + (15-25) C
As a corrector that removes or reduces some side effects, the use of mesocarb is possible. Use with caution in organic cerebral insufficiency. Cancellation should be carried out gradually, by reducing the dose, to reduce the risk of withdrawal syndrome. It should not be used while drivers of vehicles and people whose profession is associated with increased concentration of attention. At the time of treatment, you should refuse to take alcohol.
Symptoms: marked inhibition of consciousness, cardiac and respiratory activity. Treatment: monitoring the vital functions of the body, maintaining respiratory and cardiovascular activity, symptomatic therapy. Specific antagonist flumazenil (iv 0.2 mg - if necessary up to 1 mg - on 5% glucose solution or 0.9% sodium chloride solution),.
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