Typical clinico-pharmacological article
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, the time to reach C max is 1-2 h.
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 anxiolytics (tranquilizers);
- autonomic dysfunction and sleep disorders;
- prevention of states of fear and emotional stress;
- as an anticonvulsant: temporal and myoclonic epilepsy;
- in neurological practice: hyperkinesis, tics, rigidity of muscles, vegetative lability.
DOSING MODE
In / m or in / in (jet or drip): for rapid relief of fear, anxiety, psychomotor agitation, as well as in autonomic paroxysms and psychotic conditions, the initial dose is 0.5-1 mg (0.5-1 ml 0.1% solution), daily average dose - 3-5 mg, in severe cases - up to 7-9 mg.
Inside: for sleep disorders - 0.25-0.5 mg 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 abstinence - inside, 2-5 mg / day or / m, 0.5 mg 1-2 times a day, with autonomic 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, in diseases with muscle hypertension, 2-3 mg once or twice a day are prescribed.
The maximum daily dose is 10 mg. To avoid the development of drug dependence in course treatment, the duration of bromodihydrochlorophenyl benzodiazepine, like other benzodiazepines, is 2 weeks (in some cases, the duration of treatment can be increased to 2 months). With the withdrawal of the drug, the dose is reduced gradually.
SIDE EFFECT
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, muscle weakness, 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).
On the part of the hematopoiesis system: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, excessive fatigue or weakness), anemia, thrombocytopenia.
On the part of the digestive system: dryness of the oral mucosa or drooling, heartburn, nausea, vomiting, decreased appetite, constipation or diarrhea; violations of the liver, increased activity of "liver" 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, skin itching.
Influence on the fetus: teratogenicity (especially I trimester), CNS depression, respiratory failure and suppression of the sucking reflex in newborns whose mothers used the drug.
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, perceptual disorders, h. Hyperacusia, paresthesia, photophobia, tachycardia, convulsions, rarely - acute psychosis).
CONTRAINDICATIONS
- hypersensitivity (including to other benzodiazepines);
- coma, shock;
- Myasthenia gravis;
- Closed-angle glaucoma (acute attack or predisposition);
- Acute alcohol poisoning (with impaired vital functions), narcotic analgesics and hypnotic drugs;
- severe COPD (possibly increased respiratory failure);
acute respiratory failure;
- severe depression (suicidal tendencies may appear);
- Pregnancy (especially the first trimester);
- lactation period;
- age under 18 years (safety and efficacy not determined).
With caution: hepatic and / or renal failure, 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), elderly age.
PREGNANCY AND LACTATION
Contraindicated in pregnancy (I trimester) and during lactation.
During pregnancy, use only for life indications. Has a toxic effect on the fetus and increases the risk of developing congenital malformations when used in the first trimester of pregnancy. Taking therapeutic doses at a later time of pregnancy can cause depression of the newborn's central nervous system. Continuous use during pregnancy can lead to physical dependence with the development of the "cancellation" syndrome in a newborn.
The use directly 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
With caution: kidney failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution: liver failure.
APPLICATION FOR CHILDREN
Contraindicated: children under 18 years. Children, especially at a young age, are very sensitive to the CNS depressing action of benzodiazepines.
APPLICATION IN ELDERLY PATIENTS
With caution: the elderly.
SPECIAL INSTRUCTIONS
In the process 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.
With renal / hepatic insufficiency and long-term treatment, control over the pattern of peripheral blood and the activity of hepatic enzymes is necessary.
Patients who did not take psychoactive drugs earlier respond to the drug at lower doses, compared with patients taking antidepressants, anxiolytics or patients with 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 syndrome of "withdrawal" (depression, irritability, insomnia, increased sweating), especially with prolonged admission (more than 8-12 weeks).
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.
Children, especially at a young age, are very sensitive to the CNS depressing action of benzodiazepines.
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 dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
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: gastric lavage, reception of activated charcoal. Symptomatic therapy (maintenance of respiration and blood pressure), administration of flumazenil (in hospital settings). Hemodialysis is ineffective.
DRUG INTERACTION
Reduces the effectiveness of levodopa in patients with Parkinsonism.
May increase the toxicity of zidovudine.
There is a mutual enhancement of the effect with simultaneous administration of antipsychotic (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 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.
