Insomnia benzodiazepine receptor agonists

The focus of this section will be the prevention of sleep loss through the use of sleep-promoting medications. Choice of sleep medications will not be considered, as others have thoroughly discussed this issue (6). Short-acting benzodiazepine receptor agonists are generally the type of medication recommended for the treatment of transient insomnia and chronic primary insomnia, and as adjunctive therapy for secondary chronic insomnias. 

Another advantage of these agents over even fast-onset, short-duration benzodiazepines such as triazolam is that the binding of nonbenzodiazepines to the benzodiazepine receptor is different from benzodiazepine binding to this receptor, and may exhibit partial agonist properties (Fig. 8—28). Perhaps because of this, rebound insomnia (i.e., insomnia caused by withdrawal of the drug), dependence, withdrawal... 

From the published clinical studies, it would appear that the partial agonists bretazenil and abercamil are less likely to cause physiological dependence, have lower reinforcing effects and a lower incidence of subjective effects associated with abuse liability than the conventional 1,4-benzodiazepine sedative-hypnotics. It is presently unclear whether the full agonists for the GABA-A receptor, zolpidem and zopiclone, offer a real advance in the treatment of insomnia although their adverse effect profiles and abuse liability may be lower than that of the conventional benzodiazepines. 

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