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4 The Benzodiazepines

1983; Elsevier BV; Linguagem: Inglês

10.1016/s0079-6468(08)70219-4

1875-7863

Thomas A. Hamor, Ian L. Martin,

Sleep and Wakefulness Research

This chapter focuses on the 1,4- and 1,5-benzodiazepines that lack cyclic structures on the b- or c-faces, as these have markedly different pharmacological profiles. The 1,4-benzodiazepines have become the most frequently prescribed of all psychotropic drugs, being used as anxiolytics, hypnotics, anticonvulsants, and muscle relaxants. Fifteen benzodiazepines are available for clinical use as anxiolytics, sedative-hypnotics, anticonvulsants, and muscle relaxants. A large number of simple 1,5-benzodiazepines involving various modifications of the clobazam-type framework have been reported. Only a relatively small number, however, have useful CNS activity. The benzodiazepines, with few exceptions, are very poorly soluble in water and as a result, systemic administration is frequently carried out with the aid of organic solvents or emulsifiers. The benzodiazepines produce their major therapeutic effects as anticonvulsants, anxiolytics, muscle relaxants and sedatives and at the doses used clinically to achieve such responses there is little evidence of any direct actions on peripheral systems. The most frequent use of the benzodiazepines is in the treatment of anxiety. This condition is a normal response to stressful situations and it is only when the condition becomes excessive or chronic, frequently termed "pathological anxiety", that some type of clinical intervention is required. Currently, the most cost-effective treatment is the prescription of benzodiazepines.