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By A. Malir. Barry University.

It is used much less than benzodiazepines in treating insomnia for a number of reasons generic top avana 80 mg on line. However, it does not have any advantage over benzodiazepines, and therefore it is rarely used. Reacting this with ammonia transforms it into 4-aminomethylen-2,2-diethylacetoacetic ester (4. Treatment of the resulting product with sodium ethoxide results in intermolecular cyclization into 3,3-diethyl-1,2,3,4- tetrahydropyridin-2,4-dione (4. Hydrogenation of the double bonds using a palladium catalyst gives 3,3-diethylpiperidin-2,4-dione (4. Reduction of the introduced hydroxymethyl group into a methyl group using hydrogen gives the desired methyprylon (4. However, barbiturates are beginning to give way, thanks to the introduction of benzodi- azepines into medical practice. It can be accompanied by headaches, increased perspiration, nausea, tachycardia, dry mouth, etc. A state of anxiety can originate from neurological reasons, and can also be of a somatopsychic nature, which is associated with pathological development in diseases of the cardiovascular system, neoplasms, hypertonia, and diseases of the gastrointestinal tract. Drugs used for relieving anxiety, stress, worry, and fear that do not detract attention from or affect psychomotor activity of the patient are called anxiolytics or tranquilizers. Most of them have sedative and hypnotic action, and in high doses their effects are in many ways similar to barbiturate action. However, the primary advantage of this group over barbiturates lies in their significantly increased value in terms of the ratio of sedative/hypnotic effects. In other words, the ratio between doses that reduce stress and doses that cause sleep is significantly higher in anxiolytics than in barbiturates. The primary use of tranquilizers is alleviation of emotional symptoms associated with psychoneurotic or psychosomatic disturbances, such as excitement, anxiety, worry, muscle tension, and elevated motor activity. Used independently, they are not acceptable for rapid relief of severe psychotic conditions, and are used in such cases in combination with antipsychotic drugs. They are benzodiazepines: diazepam, chlordiazepoxide, chlorazepate, galazepam, lorazepam, midazolam, alprazolam, oxazepam, prazepam, and other anxiolytics, or nonbenzodiazepine structures which are represented by meprobamate, buspirone, chlormezanone, and hydroxyzine. Benzodiazepines turned out to be extremely effective drugs for treating neurotic conditions. The first representative of this large group of compounds, chlordiazepoxide, was synthesized in the 1930s and introduced into medical practice at the end of the 1950s. More than 10 other benzodiazepine derivatives were subsequently introduced into medical practice. They all displayed very similar pharmacological activity and therapeutic efficacy, and differed only in quantitative indicators. Anxiolytics (Tranquilizers) and it differs from sedative and hypnotic drugs of other classes. They depress the respiratory system to a lesser degree than hypnotics and sedative drugs, and they also cause addiction to a lesser degree. A few representatives of drugs of the benzodiazepine series have a slightly different spectrum of use. Flurazepam, triazolam, and temazepam are used as soporific agents, whereas carbamazepine is used as an anticonvulsant. Benzodiazepines with expressed anxiolytic action and either the absence of or poorly expressed sedative–hypnotic effects are called “daytime tranquilizers” (medazepam). From the chemical point of view, benzodiazepines are formally divided into two main groups: simple 1,4-benzodiazepines (chlordiazepoxide, diazepam, lorazepam), and hetero- cyclic 1,4-benzodiazepines (alprazolam, medzolam, and others). A condition necessary for the expression of anxiolytic activity of benzodiazepines is the presence of an electronega- tive group on C7 of the benzodiazepine system. The presence of a phenyl group on C5 of the system also increases the pharmacological activity of these compounds. The primary use of benzodiazepines turns out to be symptomatic relief of feelings of anxiety, tension, and irritability associated with neurosis, neurosis-like conditions, depression, and psychosomatic disorders. Benzodiazepines are used in premedication before operational interventions in order to achieve ataraxia in the patient, as an adjuvant supplementary drug in treating epilepsy, tetanus, and other pathological conditions accompanied by skeletal muscle hypertonicity. As was previously mentioned, a few benzodiazepines are used as soporifics (flurazepam, triazolam, and temazepam) and even as anticonvulsant drugs (carbamazepine). Diazepam: From a chemical point of view, diazepam, 7-chloro-1,3-dihydro-1-methyl- 5-phenyl-2H-1,4-benzodiazepin-2-one (5. Various ways for the synthesis of diazepam from 2-amino-5-chlorobenzophenone have been proposed. The first two ways consist of the direct cyclocondensation of 2-amino-5-chlorobenzophenone or 2-methylamino- 5-chlorobenzophenone with the ethyl ester of glycine hydrochloride.

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