Tranquillizers (anxiolytics, ataractics): all of them!(Part2)

Anxiolytic action tranquillizers appears to reduce the emotional lability, withdrawal of mental stress, anxiety, fear, and their corresponding autonomic and endocrine changes. Man takes life more calmly, critically, able to make correct and deliberate actions, without too much emotion in stressful situations. These properties are manifested only when tranquillizers neurotic disorders. When psychosis (schizophrenia, manic-depressive psychosis, epilepsy, Organic lesions of the brain) tranquillizers are not effective. They fundamentally do not change picture of the disease, although they may reduce its flow. This is an important feature tranquillizers.

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Sedative effect is to remove the excessive excitation and motor activity in improving the process of sleep and increased sleep duration without significant changes in its structure, to enhance the action on the central nervous system of general anesthetics, ethanol. Sedative effect of weakly expressed in "daily" tranquillizers (Mezapam, Rudotel, Anxitol, Mebicar, Adaptol, Trioxazin, Sedoxazin). This type of activity should be taken into account in the appointment of persons working with moving machinery drivers, operators, as tranquillizers decrease the concentration of attention and precision performance.

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Activating effect observed while taking small doses of drugs with low sedative effect. There has been a recovery initiative, communication, courage to make responsible decisions. This effect is a consequence of the higher functions unbraking central nervous system.

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Soporific effect is typical for all benzodiazepines. Manifested in the acceleration of falling asleep, increasing the total duration of sleep, decrease in deep sleep. In neurotic disorders of sleep is also due to the normalization of anxiolytic action. Typically, soporific effect proportionally sedative effect. If sleeping problems preferred drugs with a long (Phenazepam, Nitrazepam, Radedorm, Dormicum, Eunoctin) or short (Temazepam, Signopam, Oxazepam, Aplakil, Seresta) type of action.

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Muscle relaxation effect evident decrease tone and force cuts in skeletal muscle. In the reinforcement function based on the segmental inhibitory control of excitability of motoneurons. The chemical nature of this phenomenon is also GABA-ergic, because benzodiazepines potentiation work intercalated GABA-ergic neurons, regulating motor reflex reaction. Through this mechanism, benzodiazepines are heterospecific antagonists poisoning convulsive poisons, which block the receptors GABA, such bicucullin and picrotocsin.

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Anticonvulsant action inherent in all benzodiazepines and fairly universally in respect of different genesis convulsions (epilepsy, poisoning convulsive poisons, neuroinfection etc). The most effective means of anticonvulsant Phenazepam, Valium, Serensin, Eridan, Nitrazepam, Neozepam, Lorazepam, Ativan, Duralozam. The mechanism of action is linked to the ability of drugs to suppress paroxysmal discharge in hippocamp via the GABA-receptors.

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Amnestic action tranquillizers seen with long-term use, is to reduce operational and short-term memory. The phenomenon of reversible, takes place after the abolition of tranquilizers, although not immediately.

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Indications for the use of tranquillizers extremely broad. However, it should be remembered that the appointment of uncontrolled drugs can lead to drug dependence.

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1) The border of the state in the form of neurotic reactions, neuroses, psychopathic. Funds under specified conditions of choice, since such expressions as fear, anxiety, tension is included in the "core" structure of these diseases.

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2) Psihosomatics disease (angina, myocardial infarction transferred, cardialgia, aggravation of hypertension, peptic ulcer, bronchial asthma, etc.), the genesis of which is important psychogenic factor.

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3) Epileptic status, epilepsy, muscular gipertonus as a result of the central nervous system injury, stroke. Used as a means of urgent (emergency) treatment.

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4) In surgery, consisting of premedication in connection with a high patient's emotional reaction to the forthcoming operation. In pediatrics, comprising ataralgesia to conduct transactions with preserved consciousness (similar to neuroleptanalgesia).

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5) For the prevention of stress in healthy people in extreme situations, including during the conduct of hostilities, after the disasters etc. It is important to remember that tranquillizers diminish attention and accuracy of performance, so they can not be applied to drivers, pilots, vysotnikam et al. The most preferred "daily" tranquilizers.

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Most of tranquilizers to soak slowly from the gastrointestinal tract and slowly metabolize in the body. The main way to metabolism - glucuronidation. Tranquilizers well enter all organs and tissues, it is easy to penetrate through biological barriers.

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For the duration of action drugs are divided into three groups:

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-Short duration (half-life period is less than 10 hours):

Oxazepam, Seresta, Grandaxin, Tofizopam, Temazepam, Signopam.

Drugs of choice for the treatment of sleep disorders;
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-Long-acting (half-life period 15 - 20 hours):

Valium, Diazepam, Relanium, Chlordiazepoxide, Elenium, Benzodiapin, Phenazepam, Radedorm,
Sereneh, Epinelbon, Nitrodiazepam.

The drugs of choice for the anxiolytic, sedative and anticonvulsant therapy;
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-Overlong action (half-life period of up to 100 hours): Flurazepam, Dalmadorm, Catazalam. Practical applications are not yet clearly defined.

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Tranquilizers are powerful psychotropic agents with a relatively large breadth of therapeutic action. Toxicities observed with the 5-10 fold increase in therapeutic doses. Typically, using an average therapeutic dose, slowly increasing up to their anxiolytic effect. High doses (up to multiples of 5-10 and above) used in a psychiatric clinic. Duration of treatment tranquilizers should not exceed 6-12 weeks, usually 4 - 6 weeks, as well as developing tolerance to the drug, requiring a dose increase to achieve the same therapeutic effect as well as possible medication. Type of Drug Dependence - more physical than mental. We recommend the appointment of tranquilizers for 7-10 days with short breaks.

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Widely known specific antagonist benzodiazepines is Flumazenil (Anexate), which has its antagonism against receptors benzodiazepines on transmembrane receptor complex GABAa/Cl-
channel. Flumazenil is used to remove residual effects of benzodiazepines, as well as their overdosage or acute poisoning.

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In appointing the tranquilizers may razvivatsya various side effects. There are several groups of side-effects:

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Mental. There are declining efficiency, mood, drowsiness, muscle weakness, slower psychomotor
action. These effects are due to sedative, soporific, and muscle relaxation properties of tranquilizers.

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Physical. There are unstable blood pressure, tachycardia, muscle weakness, antispasmodic effect on internal hollow organs.

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Dependence. There at the beginning of adaptation, the need to increase the dose, then the development of the typical rebound syndrome, accompanied by sleep disturbance, anxiety, irritability, weakness, headaches, muscle jumps, tremor, palpitation, increased sweating, dizziness, a violation of concentration, nausea, loss of appetite. Developed objective signs of depression, Depersonalization, derealizatsii, increasing sensitivity to the incentives sensory (olfactory, tactile, visual), perceptual disorder, or kinaesthetic illusions.

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Safety of the use of benzodiazepines ataraxics linked to the relatively large therapeutic breadth, ie the ratio between therapeutic and lethal doses substances, the lack of adverse effects on mbolshinstvo functional systems, as well as minimal unwanted interactions with other drugs. Evidence of the possibility of fatal complications in the treatment of derivatives benzodiazepine in therapeutic doses so far, no. Benzodiazepines do not have a clinically significant effect on liver function, endocrine and urinary system. However, it is necessary to bear in mind that benzodiazepines may interact with certain medications and general therapeutics, in some cases, such interaction should rassmatrivatsya as negative.