Strong tranquilizers and other psychotropic drugs: classification features, main differences. Tranquilizers Pharmacological action of tranquilizers
Anxiolytic drugs.
Anxiolytic effect - due to the influence on emotional excitability and affective tension of a neurotic nature:
a) decreased emotional excitability
b) elimination of fear, anxiety, worry
c) calming down, onset of sleep in adequate conditions
d) increasing the threshold of emotional excitability in healthy people
main psychotropic effects of anxiolytics.
Anxiolytics suppress:
emotional reactivity to aversive stimuli
Phobic reactions (fear, worry, anxiety)
· painful experiences (frustration)
Anxiolytics reduce:
hypochondriacal reactions
· intemperance
· irritability
As a result of the action of anxiolytics:
Ø behavior is streamlined
Ø CNS depletion is reduced
Ø social adaptation improves
Ø autonomic disorders are reduced
the most commonly used anxiolytics.
a) benzodiazepines:
anxiolytics with pronounced activity
alprazolam (Xanax), lorazepam, phenazepam - medium duration of action (t 1/2 5 - 24 hours);
chlordiazepoxide (Elenium), diazepam (Relanium) - long-acting (t 1/2 > 24 hours);
daytime anxiolytics:
b) non-benzodiazepine (atypical anxiolytics): buspirone hydrochloride, mexidol
Features of the action of “daytime” tranquilizers.
They have tranquilizing activity, but have a number of properties:
1) do not cause drowsiness during the day and do not worsen the quality of life
2) do not have muscle relaxant and anticonvulsant effects
"daytime" tranquilizers.
tofizepam, oxazepam - medium duration of action
medazepam, dipotassium clorazepate - long-acting
Buspirone:
Atypical anxiolytic.
Peculiarities:
ü non-benzodiazepine anxiolytic, azaspirodecanedione in structure
ü does not act through GABAergic systems
ü does not have hypnotic, anticonvulsant or muscle relaxant properties
ü has low dependence potential
ü the effect reaches its maximum within a week
Medazepam is a long-acting daytime tranquilizer.
Alprazolam is a benzodiazepine anxiolytic with pronounced activity and medium duration of action.
Oxazepam – Medium-acting daily tranquilizer.
It has a pronounced anxiolytic effect and minimal sedative-hypnotic effect.
Chlordiazepoxide is a benzodiazepine anxiolytic with pronounced long-acting activity.
Distinctive properties of buspirone compared to benzodiazepines.
Does not have hypnotic, anticonvulsant or muscle relaxant properties.
main side effects of benzodiazepine anxiolytics.
ü weakness, drowsiness, slow motor reactions
memory impairment, headache
ü nausea, in some cases jaundice, increased activity of liver transaminases
ü menstrual irregularities, decreased sexual potency
ü skin rashes
ü addiction, development of mental and physical drug dependence with long-term use
areas of medical use of anxiolytics.
Ø as sedative-hypnotics in psychiatry
Ø during anesthesia to potentiate the action of other anesthetics
Ø as antiepileptic drugs
Ø for muscle relaxation
Alprazolam, diazepam, chlordiazepoxide, oxazepam, medazepam, buspirone.
ALPRAZOLAM. 8-Chloro-1-methyl-6-phenyl-4H--triazolo benzodiazepine.
Synonyms: Alprax, Xanax, Neurol, Alprax, Cassadan, Frontal, Neurol, Prinax, Restil, Solanax, Tafil, Trankimazin, Tricca, Xanax, Xanor, Zotran.
Its chemical structure is similar to triazolam (see), differs by the absence of a Cl atom at phenyl in position 6. Alprazolam has a less pronounced hypnotic effect. It is used primarily for short-term relief of feelings of restlessness, fear, anxiety, and treatment of concomitant depression.
The drug is quickly absorbed. Peak plasma concentrations are observed 1 to 2 hours after oral administration. The half-life is 12 - 15 hours. Frequent repeated use may, however, lead to accumulation, especially in cases of impaired renal and hepatic function in the elderly.
For possible complications, precautions and contraindications, see Chlozepid, Sibazon.
Chlozepidum. 7-Chloro-2-methylamino-5-phenyl-3H-1, 4-benzodiazepine-4-oxide.
Synonyms: Napoton, Chlordiazepoxide, Elenium, Ansiacal, Benzodiapin, Chlordiazepoxidum, Chlordiazepoxide, Decadil, Droxol, Elenium, Equinbral, Labiton, Librium, Lixin, Napoton, Novosed, Radepur, Sonimen, Timosin, Viansin, etc.
Chlordiazepoxide (Librium, Chlozepid) was the first representative of the tranquilizers in the group of benzodiazepines. Currently, this group includes a number of more effective drugs, but chlordiazepoxide has not completely lost its importance.
Chlozepid has a calming effect on the central nervous system, causes muscle relaxation, has anticonvulsant activity, potentiates the effect of hypnotics and analgesics, and has a moderate hypnotic effect (usually manifested with continuous use only in the first 3 to 5 days).
A characteristic feature of chlozepid is the ability to suppress feelings of fear, anxiety, and tension in neurotic conditions. It has no antipsychotic effect. In large doses, it can reduce psychomotor agitation.
Pharmacokinetically, chlozepid (like other tranquilizers of this series) is characterized by relatively rapid absorption after oral administration. Peak plasma concentrations are observed after 2 to 4 hours; half-life 8 - 10 hours. Excreted mainly by the kidneys. Penetrates through the placental barrier.
Chlozepid is used for neurotic conditions accompanied by anxiety, agitation, tension, increased irritability, and insomnia. Can be used for organ neuroses (functional neuroses of the cardiovascular system, gastrointestinal tract), migraines, menopausal disorders, etc.
In anesthesiological practice it can be used for preoperative preparation of patients and in the postoperative period.
Due to the ability to reduce muscle tone, it is also used for spastic conditions associated with lesions of the brain and spinal cord (including movement disorders in children), as well as for myositis, arthritis, bursitis and other diseases accompanied by muscle tension.
Also prescribed for eczema and other skin diseases accompanied by itching and irritability.
In psychiatric practice, chlozepid is sometimes used in borderline conditions with symptoms of obsession, anxiety, fear, affective tension, in minor depressive and hypochondriacal states, including those associated with diencephalic pathology, as well as in the complex treatment of patients with epilepsy and for the treatment of withdrawal syndrome in alcoholism and drug addiction.
Chlozepid is usually well tolerated. Sometimes drowsiness, slight dizziness, unsteadiness of gait, skin itching, nausea, constipation, menstrual irregularities, decreased libido are possible. In some cases, agitation may occur at the beginning of treatment.
The drug is contraindicated in acute diseases of the liver and kidneys, and myasthenia gravis. Monoamine oxidase inhibitors (see) and phenothiazine derivatives should not be prescribed simultaneously. Chlozepid (as well as other drugs in this group) should not be prescribed during pregnancy. The drug should not be taken during or on the eve of work by transport drivers and other persons whose work requires quick mental and physical reactions. During treatment with chlozepid and other drugs in this group, you must strictly abstain from drinking alcohol.
NOZEPAM (Nozepamum). 7-Chloro-2, 3-dihydro-3-hydroxy-5-phenyl-1H-1, 4-6enzodiazepin-2-one.
Synonyms: Tazepam, Adumbran, Oxazepam, Oxazepamum, Praxiten, Psicopax, Rondar, Serax, Serenal, Tazepam, etc.
Its structure and pharmacological properties are similar to chlordiazepoxide and diazepam, but have a less dramatic effect than diazepam. Nozepam is somewhat less toxic, its muscle relaxant effect is less pronounced, and its anticonvulsant properties are weak. In some cases, it is better tolerated than diazepam and chlordiazepoxide.
Used for neuroses, psychopathy, neurosis-like and psychopath-like conditions, as well as for sleep disorders and convulsive conditions.
Use of the drug in large doses may be accompanied by drowsiness, muscle weakness, lethargy, and staggering when walking. In addition, allergic reactions and dyspeptic symptoms are possible. In such cases, reduce the dose or discontinue the drug.
Contraindications and precautions are the same as for treatment with chlordiazepoxide.
ME3APAM (Mezapamum). 7-Chloro-2, 3-dihydro-1 methyl-5-phenyl-1H-1, 4-benzodiazepine.
Synonyms: Nobrium, Rudotel, Ansilan, Anxitol, Benson, Emopan, Enobrin, Imazepam, Medaurin, Medazepam, Medazepol, Megasedan, Merlit, Nivelton, Nobrium, Pazital, Rudotel, Stratium, etc.
Greenish-yellow fine-crystalline powder. Practically insoluble in water, easily soluble in alcohol.
Like other benzodiazepine tranquilizers, it has a sedative, anxiolytic, muscle relaxant, and anticonvulsant effect, but the muscle relaxant and general depressant effect is relatively less pronounced. The calming effect of mezapam is combined with some activating effect. In this regard, it is considered as a less disruptive tranquilizer during the day.
The drug potentiates the effect of sleeping pills, narcotics, and analgesics.
Mezapam is prescribed to patients with neuroses, psychopathy and other neuropsychic disorders with neurosis-like and psycho-like disorders, accompanied by increased excitability, irritability, tension, anxiety, fear, emotional lability, as well as with withdrawal syndrome.
The absence of pronounced muscle relaxant and hypnosedative properties allows mezapam to be prescribed to debilitated patients, the elderly and children.
Mezapam is taken orally (regardless of food intake).
When treating children, it is recommended to use a special dosage form of mezapam - granules (for preparing a suspension). The required amount of the drug is measured with a dosage spoon. Doses are selected individually according to the age of the child and the severity of the disease.
When treating alcoholism, mezapam is prescribed in average daily doses for 1-2 weeks.
Despite its lesser depressant effect on the central nervous system, mezapam should be used with caution by persons whose work requires rapid mental and physical reactions.
During treatment, drowsiness, dizziness, constipation, impaired accommodation, and tachycardia may occur.
Contraindications are the same as for chlozepid.
Anxiolytics (tranquilizers) - a group of drugs that eliminate anxiety, restlessness, reduce mental tension, cause muscle relaxation, and stabilize impaired autonomic functions.
In 1967, WHO introduced the term “anxiolytics” to define drugs most often called tranquilizers (from lat. tranquilloare - make you calm, serene). The main drugs in this group are benzodiazepine derivatives. Tranquilizers of a different chemical structure - hydroxyzine, mebicar, afobazole – are used less frequently.
Classification of tranquilizers (anxiolytics)
- 1. “Large” (strong) tranquilizers.
- 1.1. Benzodiazepine derivatives: bromodihydrochlorphenshbenzodiazepine("Phenazepam"), diazepam("Seduxen"), lorazepam("Lorafen"), oxazepam("Nozepam").
- 1.2. Diphenylmethane derivatives: hydroxyzine("Atarax").
- 1.3. Tranquilizers of different chemical groups: tetramethyltetraazabicyclooctanedione("Mebicar"), Afobazole, Proroxan("Prorokon").
- 2. “Small” (daytime) tranquilizers.
- 2.1. Benzodiazepine derivatives: medazepam("Rudotel"), tofisopam("Grandaxin"),
- 2.2. Other groups: buspirone("Spitomin"), aminophenolic acid("Phenibut"),
The main property of tranquilizers - a decrease in mental activity without affecting consciousness, physical, intellectual status - is associated with the suppression of the limbic system of the brain due to increased action of the inhibitory transmitter GABA.
In Fig. Figure 4.14 shows a diagram of the structure and function of the benzodiazepine receptor coupled with the GAM K receptor and the chloride channel.
Rice. 4.14.
BR – benzodiazepine receptor; the benzodiazepine molecule is depicted as a triangle; GABA-R – GABA receptor; CL- – chloride passing through the chlorine rope
Activation of the GABA receptor by benzodiazepines leads to the opening of the chloride channel and hyperpolarization of the postsynaptic membrane. In the absence of GABA, benzodiazepines do not affect the chloride conductance of the neuronal membrane. However, not all effects of benzodiazepines are mediated by the GABA-benzodiazepine receptor complex. In high concentrations, benzodiazepines cause sleep and amnesia, in the implementation of which other mechanisms may also be involved - inhibition of adenosine absorption and calcium permeability.
Intrareceptor interactions are manifested in the activating (1) effect of GABA and benzodiazepine agonists on the chloride channel, increasing the frequency of its opening. At the same time, benzodiazepine agonists enhance (2) their own effect of GABA on the chloride channel and increase the affinity of the GABA-A receptor for agonists (4), and the latter, in turn, increase the binding of benzodiazepines (5). Barbiturates bind to a specific receptor (BR), in low doses they increase (6) the time the channel is in the open state (after its activation by GABA), and in high doses they directly open it (7). They also increase (8) the affinity of the GLMA receptor for agonists and promote the binding of the latter to the benzodiazepine receptor. The binding sites of GABA and benzodiazepines on the GLBA receptor are shown in Fig. 4.15.
Rice. 4.15.
gray circles – barbiturate binding sites, black circle – benzodiazepine binding site
Specific benzodiazepine receptors have been found in the cells of the central nervous system. Benzodiazepine receptors are the binding site for benzodiazepines in the GABA-A receptor complex. Benzodiazepines, allosterically interacting with the GABA-A receptor site, increase the affinity of gamma-aminobutyric acid for these receptors, while increasing the flow of chlorine ions into neurons due to increased opening of ion channels. The inhibitory postsynaptic potential increases, which reduces the excitability of neurons. The GABA-A receptor complex is represented by five protein subunits - two α, two β and one γ. A schematic diagram of the α1β2γ2 – GABA-A receptor complex is shown in Fig. 4.16.
Each subunit has subtypes (α1_6, β1_3, γ1_3, etc.). GABA-A receptors, forming different combinations of subunit subtypes, have different properties, distribution in the brain, pharmacological and clinical effects.
Figure 4.16.
α1β2γ2 – protein subunits. In the center is the chloride ion channel. GABA sue– GABA binding site at the α1β2 border; BZD site benzodiazepine binding site at the α1γ2 interface
The mechanism of action of tranquilizers is associated with a decrease under their influence in the excitability of the subcortical areas of the brain (limbic system, thalamus, hypothalamus), responsible for emotional reactions, and inhibition of interaction between these structures and the cerebral cortex. The emergence of emotions is usually associated with the limbic system, the basis of which is the Peipets circle. Limbic system – a complex of nervous structures of the telencephalon, diencephalon and midbrain (cingulate and parahippocampal gyri, hippocampus, hypothalamus, thalamus, amygdala and other formations) involved in the regulation of sleep, wakefulness, concentration, depth of emotions, and in the formation of behavioral motivation. The limbic system is under the control of the frontal cortex; it affects the functioning of all cortical areas of the cerebrum. Amygdala - a collection of gray matter lying deep in the temporal lobe in front of the hippocampus in close proximity to the uncus. This structure is part of the limbic system of the brain and controls the body's motor and autonomic reactions associated with emotions. According to modern concepts, emotional arousal arises in the hippocampus, then passes to the hypothalamus and through the anterior nuclei of the thalamus to the cingulate gyrus.
Tranquilizers reduce the excitability of subcortical areas of the brain and have an inhibitory effect on polysynaptic spinal reflexes, thereby causing muscle relaxation. Tranquilizers have an inhibitory effect on the course of excitation along the Peipets circle, shown in Fig. 4.17.
Figure 4.17.
Unlike antipsychotics, tranquilizers do not have a pronounced antipsychotic effect on delusional and hallucinatory disorders. They have four pharmacodynamic properties to varying degrees: anxiolytic, hypnotic, muscle relaxant and anticonvulsant.
Anxiolytic (antiphobic ) and general calming effect – the most important feature of tranquilizers. Tranquilizers eliminate feelings of fear, anxiety, tension, and restlessness. Therefore, they are used to treat various psychogenic disorders: neurasthenia, obsessive-compulsive neuroses, hysteria, psychopathy. Due to the fact that fear and anxiety can manifest themselves during anticipation of a surgical operation or serious stress, tranquilizers are used not only in psychiatry.
Hypnotic effect is expressed in facilitating the onset of sleep, enhancing the effect of sleeping pills; The effect of narcotic and painkillers is also enhanced.
Muscle relaxant effect tranquilizers are associated with an effect on the central nervous system, and not with a peripheral curare-like effect, which is why they are sometimes called central muscle relaxants. This effect is often a positive factor when using tranquilizers to relieve tension, feelings of fear, and excitement, but it limits the use of drugs that have a pronounced muscle relaxant property in patients whose work requires a quick, concentrated reaction (transport drivers, etc.).
Anticonvulsant action allows the use of certain tranquilizers (diazepam) to relieve seizures.
When choosing a tranquilizer, it is necessary to take into account the differences in the spectrum of their action. Some drugs have all the properties characteristic of tranquilizers (for example, diazepam), others have a more pronounced anxiolytic effect. Some drugs (eg. mezapam("Rudotsl")) have a relatively weak muscle relaxant property, so they are more convenient for use during the daytime and are often called daytime tranquilizers. However, in relatively large doses, all tranquilizers can exhibit all the pharmacological properties characteristic of this group of drugs.
Midazolam(“Dormikum”) is a short-acting drug, half-life is 1–12 hours. With prolonged use, it can cause withdrawal symptoms the next day in the form of increased anxiety. After its discontinuation, insomnia may return.
Flunitrazepam, clonazepam, lorazepam("Lorafen"), n itrazepam– benzodiazepines of medium duration of action, have a half-life of 12–40 hours. They cause drowsiness in the first half of the day if used as a sleeping pill.
Diazepam("Seduxen"), chlordiazepoxide("Elenium"), bromodihydrochlorophenylbenzodiazepine(“Phenazepam”) are long-acting benzodiazepines with a half-life of 40–250 hours. When taken, there is a risk of accumulation in old age and in people with severe liver dysfunction, but they cause a less pronounced rebound effect and withdrawal syndrome. The “rebound” effect occurs when you stop or reduce drug intake due to the fact that the drug is eliminated from the body very quickly. It is manifested by a deterioration in the patient’s condition due to the intensification of the disease, the elimination of which the drug was aimed at eliminating.
Different tranquilizers are effective for various neurotic and neurosis-like conditions. Neuroses – these are personality breakdowns, painfully experienced and accompanied by somato-vegetative and emotional-affective disorders. They do not have a causal connection with organic changes in the brain, as they relate to functional disorders. Features of neuroses:
- tendency to protracted course;
- not accompanied by hallucinations and delusions;
- are not accompanied by a decrease in the patient’s critical attitude towards his disease.
The cause of neuroses: a combination of a psychogenic factor with certain circumstances, namely: a low or insufficient level of protection to a certain type of stress.
Anxiolytics, or tranquilizers, improve a person’s adaptation to environmental conditions by eliminating emotional instability, reducing feelings of tension, anxiety, fear, and restlessness.
Diazepam(“Seduxen”, “relium”, “valium”) relieves all types of anxiety in neuroses, panic attacks, insomnia, obsessions with the presence of rituals, in Gilles de la Tourette syndrome (manifests in childhood and is characterized by multiple motor tics), normalizes nighttime dream. It is often prescribed parenterally for the treatment of persistent obsessions and can be used to relieve status epilepticus.
Chlordiazepoxide(“Librium”, “Elenium”) is historically the first of the benzodiazepine tranquilizers. It has a pronounced anti-anxiety, anxiolytic and muscle relaxant effect. It is used in the treatment of obsessive states of various types, neuroses, to relieve emotional stress, panic attacks.
Lorazepam(“Lorafen”) has a powerful antiphobic and hypnotic effect, is effectively used for all types of neuroses for the treatment of hypochondriacal, senestopathic disorders, and helps stabilize the autonomic nervous system.
Hydroxyzine(“Atarax”) is a non-addictive drug used to treat asthenia and mild phobic manifestations. The drug is a powerful vegetative corrector, indicated for the treatment of various somatic disorders, relieves the sensation of hot flashes, shortness of breath of neurogenic origin, nausea, dizziness, and sweating.
Tranquilizers have found wide use not only in psychiatric and neurological practice, but also in other areas of practical medicine.
The main areas of use of tranquilizers:
- treatment of conditions accompanied by anxiety;
- premedication – preparation for surgery;
- as sleeping pills;
- relieving seizures (using intravenous diazepam);
- treatment of alcohol withdrawal.
Side effects are associated with disruption of the central nervous system: depression, drowsiness, impaired coordination of movements (ataxia), convulsions, speech impairment (dysarthria). Psychotic effects are possible (paradoxical excitement, insomnia), other undesirable effects are noted from the gastrointestinal tract - nausea, diarrhea, vomiting.
It is possible to become addicted to benzodiazepines and develop drug dependence.
For persons performing work that requires a quick mental reaction and precise coordination of movements (vehicle drivers, pilots), most drugs are prescribed only under the condition of removal from work. Benzodiazepine derivatives that do not have a hypnotic effect and have little effect on muscle tone (“daytime tranquilizers”) – medazepam("Rudotel"), tofisopam(“Grandoksin”) – less likely to cause drowsiness during the daytime. Tranquilizers do not relieve depression and are not used to treat depressive conditions.
Despite the relatively low toxicity of the main tranquilizers (benzodiazepines, propanediol derivatives), they can only be used if there are appropriate indications and under medical supervision. Unreasonable and uncontrolled use of them can cause side effects, mental dependence and other undesirable effects. It should also be borne in mind that alcohol potentiates the effect of tranquilizers, so you should not drink alcoholic beverages while using them.
Tranquilizers) psychotropic drugs that selectively suppress feelings of emotional stress, restlessness, anxiety, fear; are used mainly for neurotic conditions. According to the chemical structure among A. s. There are benzodiazepine derivatives (bromazepam, diazepam, lorazepam, medazepam, nozepam, phenazepam, etc.) and A. s. from other classes of chemical compounds (buspirone, grandaxin, mebicar, trioxazine, etc.). Anxiolytic drugs have anxiolytic (elimination of feelings of emotional stress, restlessness, anxiety, fear) properties. In addition, most A. s. They also cause sedative and hypnotic effects, have an anticonvulsant effect, reduce skeletal muscle contraction and enhance the effect of substances that depress the central nervous system: anesthetics, hypnotics, opioid analgesics, ethyl alcohol, etc. A. s. is most widely used in medical practice. from the group of benzodiazepine derivatives. These substances increase the effectiveness of inhibitory processes in the central nervous system, the mediator of which is γ-aminobutyric acid (). This occurs as a result of activation of benzodiazepine receptors, which are part of the so-called GABA-benzodiazepine receptor complex. Interaction of A. with. with benzodiazepine receptors leads to an increase in the effectiveness of endogenous GABA, which contributes to an increase in the frequency of “opening” of chloride channels in neuronal membranes and the occurrence of hyperpolarization of these membranes. The anxiolytic, sedative, hypnotic, anticonvulsant and muscle relaxant effects of A. s., apparently, are associated with benzodiazepine receptors of different types, the density of which in certain structures of the central nervous system. not the same. Serotonergic, adrenergic, dopaminergic and cholinergic neurons are indirectly involved in the implementation of the anxiolytic and other effects of benzodiazepines. In addition, benzodiazepine A. s. weaken the effects of excitatory amino acids (glut min ova, aspartic) in relation to neurons of different levels of the central nervous system. The anxiolytic effect of buspirone and its analogs is apparently due to a decrease in the activity of serotonin-containing neurons, in particular the raphe nuclei of the brain stem, which is the result of activation by these substances of serotonin receptors of subtype 1A in the inhibitory somatodendritic synapses of these neurons. These substances, unlike benzodiazepines, do not interact with the GABA-benzodiazepine receptor complex, have almost no anticonvulsant or hypnotic effects, do not promote muscle relaxation and do not cause drug dependence. Diazepam and phenazepam have the greatest anxiolytic activity, sedative and hypnotic activity - phenazepam and nitrazepam, anticonvulsant activity - clonazepam and phenazepam. When taken orally A. s. well absorbed from the gastrointestinal tract. Biotransformation of A. s. occurs in the liver. For some A. s. (for example, diazepam, clonazepam, phenazepam) is characterized by the formation of active metabolites with pronounced pharmacological activity. Other A. s. (medazepam, lorazepam, nozepam) do not form active metabolites during biotransformation in the liver. A. s. are derived. mainly by the kidneys. Apply A. s. in order to eliminate feelings of emotional stress, anxiety, anxiety, fear and other disorders due to neuroses, incl. for organ neuroses (cardiovascular system, gastrointestinal tract), for the treatment of insomnia, hypertension, gastric and duodenal ulcers, for psychological rehabilitation of patients suffering from coronary heart disease, arrhythmias, broncho-obstructive syndrome. In addition, A. s. prescribed to reduce increased skeletal muscle tone in spastic conditions associated with lesions of the brain and spinal cord, as well as to relieve alcohol withdrawal. Ability A. s. enhance the effect of anesthesia, opioid analgesics are used in anesthesiological practice. Long-term use of A. s. accompanied by a weakening of cognitive and motor processes, a shortening of the rapid phase of sleep. Possible weakening and the emergence of drug dependence. Contraindications: benign prostate gland, acute liver and kidney diseases, respiratory disorders of central origin, myasthenia gravis; I trimester of pregnancy, period of breastfeeding. In outpatient practice, A. s. should not be prescribed. drivers of vehicles and other persons whose work requires quick psychomotor reactions. The forms of release and use of the main drugs are outlined below. Alprazolam(alzolam, zoldak, cassadan, xanax, lamoz, neurol, etc.) - tablets of 0.25; 0.5; 1; 2 and 3 mg. Prescribed orally for adults in an average therapeutic dose of 0.25-0.5 mg 3 times a day. Highest daily allowance 3 mg. Benzoclidine(oxylidine) - tablets of 20 and 50 mg; 2% and 5% solutions in ampoules of 1 ml. Prescribed orally 20-50 mg 3-4 times a day. It is administered subcutaneously and intramuscularly 2 times a day. initially at a dose of 20 mg, then the single dose is increased to 50-100 mg and more; daily dose up to 200-300 mg. Bromazepam(bromazep, lexilinum, lexotan, caltepat, norgok, etc.) - tablets 1.5; 3 and 6 mg. Prescribed for adults orally at 1.5-3 mg 2-3 times a day. Gidazepam- tablets of 20 and 50 mg. Prescribed orally 20-50 G 3 times a day. The highest daily dose for relieving alcohol withdrawal symptoms is 500 mg. Diazepam(apaurin, Valium, Relanium, Seduxen, Sibazon, etc.) - 2 tablets; 2.5; 5 and 10 mg; 2 and 5 each mg; (15 ml-2 mg active substance); injection solution 0.5%. Prescribed orally for adults, starting with a dose of 2.5-5 mg 1-2 times a day, then the dose is gradually increased: the average single dose is 5-10 mg. Highest daily dose 60 mg. Children are prescribed 1 appointment at the age of 1-3 years. mg, 3-7 years 2 mg, 7 years and older - 3-5 mg. The daily dose is respectively 2; 6 and 8-10 mg. Clobazam(clarmyl, maginol, etc.) - tablets of 5 and 10 mg. Prescribed orally for adults 10-20 mg. Children under 3 years of age are not prescribed; reduced doses are recommended for children over 3 years of age and elderly patients. Lorazepam(calmese, merlit, trapex, etc.) - tablets of 0.5, 1, 2 and 2.5 mg. Prescribed orally 1 mg 2-3 times a day. Mebicar- tablets of 300 and 500 mg. Prescribed orally at 300-500 mg 2-3 times a day. regardless of food intake. Medazepam(mezapam, nobrnum, rudotel, etc.) - 10 tablets mg; granules for cooking (for children), container contains 40 mg drug. For adults, the average single dose is 10-20 mg, daily - 30-40 mg, highest daily dose 60 mg. Average doses for children 1-2 years old - one time 1 mg, daily allowance 2-3 mg; 3-6 years - one-time 1-2 mg, daily allowance 3-6 mg; 7-10 years - one-time 2-8 mg, daily - 6-24 mg. Oxazepam(nozepam, tazepam, serax, etc.) - tablets of 10, 15 and 30 mg. Prescribed orally regardless of food intake in an average single dose for adults 20-30 mg, daily dose 30-90 mg. Temazepam(signopam) - tablets 10 mg. Prescribed orally 10 mg 3 times a day. can be increased to 20 mg to the reception. Tofisopam(grandaxin) - tablets 50 mg. Prescribed orally at 50-100 mg 1-3 times a day. Trimetozin(trioxazine) - tablets 300 mg. Prescribed orally after meals, 300 G 2 times a day. Phenazepam- tablets of 0.5, 1 and 25 mg. Prescribed orally for adults at 0.25-0.5 mg 2-3 times a day. Maximum daily dose 10 mg. Chlordiazepoxide(librium, napothon, chlozepid, elenium, etc.) - tablets of 5, 1 and 25 mg. Prescribed orally for adults, starting from 5-10 mg per day Gradually increase to a daily dose of 30-50 mg in 3-4 doses. 1. Small medical encyclopedia. - M.: Medical encyclopedia. 1991-96 2. First aid. - M.: Great Russian Encyclopedia. 1994 3. Encyclopedic Dictionary of Medical Terms. - M.: Soviet Encyclopedia. - 1982-1984.
See what “Anxiolytic drugs” are in other dictionaries:
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- (Late Latin sedativus soothing, from Latin sedo I make you sit down, I calm down) a chemically heterogeneous group of medicinal substances of plant and synthetic origin that have a calming effect.… … Great Soviet Encyclopedia
I Tranquilizers (tranquilisantia, French tranquilliser from Latin tranquillare to calm down; synonym: anxiolytics, antiphobic sedatives, ataractics, ataractic drugs, minor tranquilizers) see Anxiolytic drugs. II... ... Medical encyclopedia Wikipedia
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The drug is non-toxic, is well absorbed into the bloodstream from the intestines and quickly enters the brain tissue, excreted in urine and feces, without accumulating in the body even with long-term use.
What is this pharmaceutical drug?
Relanium is a tranquilizer that has sedative, anticonvulsant and muscle relaxant properties. In addition, Relanium also has anxiolytic and hypnotic properties. By influencing the human body, this psychotropic drug helps to reduce general excitability, inhibit spinal reflexes, and also inhibit the performance of the central nervous system. Relanium is used for the treatment of both neurotic and neurosis-like disorders. In addition, this drug is also prescribed to stop epileptic seizures and excessive psychomotor agitation. You cannot do without the help of Relanium in conditions that are characterized by increased muscle tone.
As for the side effects that can be caused by using this tranquilizer, there are actually a lot of them. Here are some of them: nausea, vomiting, general weakness, drowsiness, dizziness, tachycardia, allergic reactions. If we talk about possible dosages, they are prescribed by a specialist in accordance with the age of the patient and the existing disease. There are also plenty of contraindications to the use of Relanium. This and coma, and apnea syndrome, and pregnancy, and severe forms of myasthenia and so on.
Despite the fact that tranquilizers, compared to antidepressants and antipsychotics, cause much fewer side effects in people, some of them are still observed, and quite often. The most common side effects that can make themselves felt during the use of tranquilizers are: muscle relaxation, mental and physical dependence, a state of hypersedation, “paradoxical” reactions, as well as “behavioral toxicity”.
As for muscle relaxation, it means both general weakness and weakness that a person can feel in a specific muscle group. “Behavioral toxicity” involves the development of impairments in both cognitive functions and psychomotor skills. All these disorders can be identified using neuropsychological testing. The phenomena of hypersedation mean such symptoms as: lack of attention, forgetfulness, daytime sleepiness, decreased level of wakefulness and some others. As for mental or physical dependence, it makes itself felt as a result of prolonged use of a particular tranquilizer and is accompanied by various symptoms that resemble signs of neurotic anxiety.
And finally, “paradoxical” reactions are a condition that is characterized not only by sleep disturbances, but also by increased aggressiveness and agitation. To reduce the risk of developing all these, as well as some other side effects, to a minimum, it is worth using the help of special dietary supplements (dietary supplements).
Such drugs are often called anxiolytics and ataractics. Tranquilizers mean a group of psychotropic pharmaceutical drugs that are used to reduce the manifestation of anxiety, emotional stress, fear, and restlessness. The very first drugs of this kind began to be used in medicine already in the fifties. They, like all other pharmaceuticals, have both their indications and their contraindications for use. In addition, tranquilizers also have special instructions for use. Let’s try to figure out what exactly these contraindications are right now.
The most important special instruction for the use of these drugs is that this type of medication can only be used under the strict supervision of a specialist doctor. This is explained by the fact that for a huge number of people, these drugs cause both addiction and dependence. Another special indication for the use of these funds is the age limit. So, for example, it is not advisable to prescribe such medications to children under eighteen years of age. The use of these medications by children or adolescents is only possible if absolutely necessary.
Particular care should be taken when using psychotropic drugs and those people whose work involves technology or transport. The fact is that these drugs tend to reduce attention, which can lead to accidents and injuries at work. Under no circumstances should you drink alcohol while taking such medications. And one more special instruction for the use of tranquilizers - when using this type of medication, each patient must follow the principle of gradually increasing the dose.
There are actually a lot of contraindications to the use of such drugs. First of all, it is worth noting that this group of drugs is strictly contraindicated for use in patients with severe forms of myasthenia gravis. You should also avoid using tranquilizers if the patient has any serious kidney or liver diseases. These drugs are also contraindicated for pregnant women. The lactation period is another strong contraindication to the use of psychotropic drugs. Under no circumstances should this type of pharmaceutical product be used in case of acute alcohol intoxication.
If a person’s work requires increased attention from him and he cannot give up his activities during treatment with tranquilizers, then he should not be prescribed such drugs. Every specialist knows about this, which is why doctors ask all patients the same question - Who do you work for?
This contraindication is explained quite simply. The fact is that during treatment with tranquilizers, there is a significant decrease in the attention of patients, which becomes the cause of numerous injuries in the workplace or accidents on the roads.
However, there is a way out of this situation. If these people really cannot do without the help of such means, then they are prescribed the same tranquilizers, but with a stabilizing component of the effect. These drugs include the following drugs: mezapam, grandaxin, mebicar, and also trioxazine. All of them do not tend to cause drowsiness and general weakness.
Osteochondrosis of the spine is one of the most common diseases that tends to “attack” people of working age. This disease is accompanied by degenerative-dystrophic damage to the intervertebral discs, which causes the human spine to lose not only its elasticity, but also its elasticity. Osteochondrosis of the spine, as a rule, leads to the development of intervertebral hernias. We note right away that the course of treatment for this disease is complex. One of the drugs that are included in the treatment of this pathology are tranquilizers.
Tranquilizers are prescribed to patients with osteochondrosis most often to combat insomnia, fear, and tension. All these conditions are observed with osteochondrosis quite often, since they arise against the background of very strong pain experienced by the patient. These psychotropic drugs are also prescribed to enhance the effect of painkillers. Moreover, these drugs not only enhance, but also prolong their therapeutic effects. When prescribing psychotropic drugs for osteochondrosis, specialist doctors also take into account the fact that these drugs can cause addiction in the patient. That is why the course of treatment of osteochondrosis with tranquilizers is short-lived.
If a patient with osteochondrosis takes any psychotropic drug, he must be prepared for the fact that at any moment he may experience general weakness, apathy, or impaired attention. These are all side effects of these drugs.
Today, all medications of this kind are considered to be low-toxic. Despite this, quite often this group of drugs becomes the cause of poisoning. Moreover, not only adults, but also children are poisoned by them. Poisoning with tranquilizers is accompanied by a number of far from pleasant symptoms. According to specialist doctors, all these symptoms are very similar to the symptoms of poisoning barbiturates. The very first signs of poisoning with these drugs include areflexia, muscle relaxation and ataxia. These conditions arise due to the fact that tranquilizers tend to primarily have a relaxing effect directly on the muscle muscles.
In addition to these signs, low blood pressure can also make itself known, along with rapid heartbeat and sinus arrhythmia. It is worth drawing the attention of all readers to the fact that each drug in this group has a different effect on blood pressure. Cardiovascular collapse is another fairly common symptom of tranquilizer poisoning. As a rule, this symptom inevitably leads to respiratory depression, which in turn can cause death.
In case of severe poisoning, in addition to all the above symptoms, the patient may also experience cyanosis and obvious impairment of consciousness. Convulsions are also quite possible in this condition. In some cases, lung complications such as pneumonia are also observed. edema and atelectasis. In case of such poisoning, you need to act immediately: rinse your stomach and call an ambulance.
In any instructions for the use of a particular tranquilizer, you can read that this type of drug should under no circumstances be taken by either pregnant women or breastfeeding mothers. Indeed, the period of pregnancy is a serious contraindication to the use of such medications, and all because this group of psychotropic drugs tends to not only easily, but very easily and quickly penetrate the placenta. Clinical studies have proven that taking tranquilizers during pregnancy causes the amount of these drugs in the umbilical cord blood to significantly exceed their concentration in the blood of the mother herself.
It's no secret that the fetus in the womb, or rather its central nervous system, reacts very strongly to all external factors. That is why at the moment it is considered to be ultra-vulnerable. Tranquilizers, having penetrated the placenta, primarily affect the nervous system of the fetus. This can cause serious violations. The use of psychotropic drugs in the third trimester of pregnancy is especially dangerous, since it is during this period that the central nervous system begins to develop at an accelerated pace.
What are tranquilizers?
This concept refers to a group of psychotropic drugs that are used to suppress or reduce the performance of the body.
What are sleeping pills?
Sleeping pills are a group of psychoactive pharmaceutical drugs that are used both to facilitate the onset of sleep and to ensure its duration. Sometimes you really can’t do without both tranquilizers and sleeping pills, but every person should remember that these drugs should be used rationally. Otherwise, it may lead to the development of serious health problems. It is also very important that both of these groups of drugs are taken strictly as prescribed by a specialist doctor and in the dosages indicated by him.
Why can't sleeping pills and tranquilizers be taken in unlimited quantities? coronary heart disease, bronchial asthma, and hypertension. The disease is really serious, which is why it requires a very long complex treatment.
Treatment of vegetative dystonia involves a number of measures. These include: maintaining a healthy lifestyle, physical exercise, proper nutrition, water treatments, massage, psychotherapy, physiotherapeutic treatment, as well as taking antipsychotics and tranquilizers. We note right away that such medications for vegetative dystonia are prescribed to children only if the herbal medicines they take do not have the proper therapeutic effect on their psyche. By influencing the child’s body, tranquilizers not only normalize the general emotional state, but also restore autonomic dysfunction.
It is very important in this case that the correct drug is selected for the child. So, for example, if a child has hypersthenic symptoms, then he simply cannot do without the help of tranquilizers that have a sedative effect. These drugs include: seduxen, sibazon, tazepam and some others. If we are talking about a hyposthenic neurotic state, then drugs with a moderate activating effect such as medazepam and grandaxin.
Tranquilizers are a group of pharmacological drugs whose main task is to eliminate anxiety and psycho-emotional stress. In addition to these effects, this group of drugs may have a hypnotic, anticonvulsant, as well as muscle relaxant and stabilizing effect. The main diseases for which tranquilizers are used are neurosis-like conditions. However, these are not all indications for use. Today there are a huge number of tranquilizers. Each drug has its own characteristics, allowing the doctor to approach the treatment process individually. This article will help you form an idea of what tranquilizers are, how they work, and what they are. You will be able to get acquainted with the most common representatives of this group of medicines, their range of applications, and features of use.
So, tranquilizers. The name comes from the Latin word “tranquillo”, which means to soothe. Synonyms of this term are words such as “anxiolytics” (from the Latin “anxius” - anxious and “lysis” - dissolution) and “ataractics” (from the Greek “ataraxia” - equanimity, calm). However, the most common term is still “tranquilizers”. Based on the name, it becomes clear that this group of medications is aimed at eliminating anxiety and fears, eliminating irritability and emotional tension. Tranquilizers calm the human nervous system.
Tranquilizers have been known to medicine since 1951, when the first drug of this class, Meprobamate, was created. Since then, this group of drugs has expanded significantly and continues to do so. The search for new tranquilizers is driven by the need to minimize the side effects of their use, eliminate the addictive effect of some of them, and achieve a rapid onset of anti-anxiety effect. This does not mean at all that of the existing drugs there is not a single worthy one. It’s just that the whole world strives for perfection, including medicine.
What types of tranquilizers are there?
The group of tranquilizers is heterogeneous in its chemical composition. Their classification is based on this principle. In general, all tranquilizers are divided into two large groups:
- benzodiazepine derivatives;
- drugs of other pharmacological groups with anti-anxiety effects.
The most common benzodiazepine derivatives are Diazepam (Sibazon, Relanium, Valium), Phenazepam, Gidazepam, Alprazolam, Tofisopam (Grandaxin). Among tranquilizers from other chemical groups, the most common are Hydroxyzine (Atarax), Mebicar (Adaptol), Afobazol, Tenoten, Phenibut (Noofen, Anvifen), Buspirone (Spitomin).
Expected effects of tranquilizers
Most tranquilizers have a wide range of effects:
- reduce anxiety and calm (that is, sedate);
- relax muscles (myorelaxation);
- relieve convulsive readiness during epileptic seizures;
- have a hypnotic effect;
- stabilize the functions of the autonomic nervous system.
This or that effect of a tranquilizer is largely determined by its mechanism of action, the characteristics of absorption and breakdown. That is, not every drug “can” do all of the above.
What are “daytime” tranquilizers?
Due to the characteristics of their effects, a group of so-called “daytime” drugs is distinguished among tranquilizers. "Day tranquilizer" means, first of all, that it does not have a sleeping effect. This tranquilizer does not reduce concentration, does not relax muscles, and maintains the speed of thinking. In general, it is generally accepted that it does not have a pronounced sedative effect. Daytime tranquilizers include Gidazepam, Buspirone, Tofisopam (Grandaxin), Mebicar (Adaptol), Medazepam (Rudotel).
How do tranquilizers work?
All tranquilizers work at the level of brain systems that form emotional reactions. This includes the limbic system, the reticular formation, the hypothalamus, and the thalamic nuclei. That is, this is a huge number of nerve cells scattered throughout different parts of the central nervous system, but interconnected. Tranquilizers lead to the suppression of excitation in these structures, and therefore the degree of a person’s emotionality decreases.
The direct mechanism of action is well studied for benzodiazepine derivatives. There are various benzodiazepine receptors in the brain that are closely related to gamma-aminobutyric acid (GABA) receptors. GABA is the main inhibitory substance in the nervous system. Benzodiazepine derivatives act on their receptors, which is transmitted to GABA receptors. As a result, the inhibition system is activated at all levels of the central nervous system. Depending on which benzodiazepine receptors are involved, the nervous system realizes one or another effect. Therefore, for example, there are tranquilizers with a pronounced hypnotic effect, which are used primarily for the treatment of sleep disorders (Nitrazepam). And other tranquilizers from the benzodiazepine group have a more pronounced anticonvulsant effect, and therefore are used as antiepileptic drugs (Clonazepam).
