Barbiturates, specific agents

Barbiturates. The very earliest treatments for generalized anxiety were sedating barbiturates. These agents had little in the way of specific antianxiety action they merely reduced anxiety in direct proportion to their ability to sedate. Because of serious dependency and withdrawal problems (see Chapter 13) and lack of a favorable... 

Benzodiazepines are a family of compounds that share the same basic chemical structure and pharmacological effects. Although the more famous members of this family are associated with treating anxiety (e.g., diazepam [Valium] see later in this chapter), several benzodiazepines are indicated specifically to promote sleep (Table 6-1). These agents exert hypnotic effects similar to those of nonbenzodiazepines—such as the barbiturates—but benzodiazepines are generally regarded as safer because there is less of a chance for lethal overdose.22 Benzodiazepines, however, are not without their drawbacks, and they can cause resid-... 

Thiopental Sodium, USP. Thiopental. sodium, sodium S-ethyl-S-(l-methylbutyl)-2-lhiobarbilurale (Pentothal Sodium). is the mo.st widely u.sed ultra-short-acting anc.sthctic barbiturate. Additionally, the compound is the prototype for the ultra-short-acting barbiturates. Most discussions of how structure influences duration of action in this group of agents relate specifically to it. The compound s onset of action is about equal to the time required for it to travel to the brain from the site of administration. Consciousness is regained within 30 minutes. 

To synthesize the target barbiturate 36 we identified l-bromo-8,8,8-trifluorooctane 43 (see Scheme 4.6) as the key building-block. This molecule is known, and was previously obtained only by fluorination of 8-bromooctanoic acid with SF4 [37]. Unfortunately, the use of such an aggressive fluorinating agent requires specific experimental apparatus and presents considerable safety hazards, which are difficult to address in an ordinary synthetic laboratory. We therefore developed several alternative routes to 43 based on user-friendly protocols as well as the use of a cheap and commercially available source of fluorine, such as trifluoroacetic esters. One of these novel approaches is shown in Scheme 4.6. 

Not all barbiturates are used as tranquilizing agents alone. Sodium pentothal, popular once in dentistry, has also been used as a truth serum in specific amounts. 

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