Benzodiazepines
The benzodiazepines were introduced into clinical practice in the 1960sfor the treatment of anxiety and sleep disorders. Members of this class of drug were classified initially as minor tranquilizers although this term has fallen into disfavor. These agents have proven to be safe and effective alternatives to older SEDATIVE-HYPNOTIC agents such as BARBITURATES, CHLORAL HYDRATE, glutethimide, and carbamates. Benzodiazepines are widely prescribed drugs, with 8.3 percent of the U.S. population reporting medical use of these agents in 1990.
Basic Pharmacology
All benzodiazepines produce similar pharmacologic effects, although the potency for each effect may vary with individual agents. They decrease or abolish ANXIETY, produce sedation, induce and maintain sleep, control certain types of seizures, and relax skeletal muscles. The basic chemical structure is shown in Figure 1.
Dissimilarity in the effects of different benzodiazepines tend to be more quantitative than qualitative in nature. Many of these differences are attributable to how benzodiazepines are absorbed, distributed, and metabolized in the body. A few benzodiazepines—clorazepate for example—are pro-drugs; that is, they become active only after undergoing chemical transformation in the body. The extent to which a benzodiazepine is soluble in fatlike substances—that is, the degree to which it is lipophilic—determines the rate at which it crosses the tissue barriers that protect the brain.
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