Antianxiety agents

Antianxiety agents Antiaiis toxicaiia An ti air hy thnu c Antiairhythnnc agents Antiaithritics Antiasthmatic agents... 

Ethanol (1) is the most widely used antianxiety agent. In the 1950s, the pioneering work of Berger on the muscle relaxant mephenesin [59-47-17, (71), led to the identification of meprobamate (24) as an effective agent for the treatment of anxiety. 

Sales for hypnotic—sedative agents ia the United States for 1993 were estimated to be 139,000,000. Anticonvulsant sales for 1993 were estimated at 525,000,000. U.S. sales of antianxiety agents including both the BZs and buspirone-hke agents for 1993 were estimated at 1,046,000,000. 

Benzodiazepines as antianxiety agents, 1, 170 as anticonvulsants, 1, 166 organometallic complexes, 7, 604 as sedatives, 1, 166 IH- 1,2-Benzodiazepines conversion to 3H-1,2-benzodiazepines, 7, 604 synthesis, 7, 597, 598, 604 3H-1,2-Benzodiazepines acid-catalyzed reactions, 7, 601 nucleophilic reactions, 7, 604 oxidation, 7, 603 synthesis, 7, 596 thermal reactions, 7, 600 5H-1,2-Benzodiazepines photochemical reactions, 7, 599 synthesis, 7, 603... 

Chlorine and iodine can be introduced into aromatic rings by electrophilic substitution reactions, but fluorine is too reactive and only poor yields of monofluoro-aromatic products are obtained by direct fluorinafion. Aromatic rings react with CI2 in the presence of FeCl3 catalyst to yield chlorobenzenes, just as they react with Bi 2 and FeBr3. This kind of reaction is used in the synthesis of numerous pharmaceutical agents, including the antianxiety agent diazepam, marketed as Valium. 

To speed the process of drug discovery, combinatorial chemistry> has been developed to prepare what are called combinatorial libraries, in which anywhere from a few dozen to several hundred thousand substances are prepared simultaneously. Among the early successes of combinatorial chemistry is the development of a benzodiazepine library, a class of aromatic compounds much used as antianxiety agents. 

Pharmacodynamic tolerance to the psychomotor effects of benzodiazepines has been demonstrated after single or multiple doses (File 1985 Greenblatt and Shader 1978 Rosenberg and Chiu 1985). Pharmacodynamic tolerance to the anxiolytic effect (over a 6-month period) has not been demonstrated (Rickels et al. 1983), and clinical experience supports the view that many patients with anxiety disorders require long-term therapy with benzodiazepines or alternative antianxiety agents. An important clinical consequence of tolerance to sedative effects is observed in benzodiazepine overdoses, when patients may initially be... 

Priapism has been treated with analgesics, antianxiety agents, and vasoconstrictors to force blood out of the corpus cavernosum (e.g., phenylephrine, epinephrine), and vasodilators to relax smooth muscle (e.g., terbutaline, hydralazine). 

Drug choices for anxiety disorders are shown in Table 68-7, and non-BZ antianxiety agents for GAD are shown in Table 68-8. 

TABLE 68-8 Nonbenzodiazepine Antianxiety Agents for Generalized Anxiety Disorder ... 

Chlordiazepoxide is the pioneer member of the 1,4-benzodiazepines to be employed clinically as an antianxiety agent in humans. A number of methods based on extraction processes are available for the assay of this drug, namely spectrofluorometry, polarography and electron-capture GC-technique but RIA measures it directly in the blood without involving extraction and possesses very low sensitivity. 

May have additive effects with alcohol and other CNS depressants (eg, hypnotics, sedatives, tranquilizers, antianxiety agents) use with caution. 

Anxiety- The efficacy of hydroxyzine as an antianxiety agent for long-term use (longer than 4 months) has not been assessed periodically reevaluate its usefulness. 

Schedule IV (c-/V) - Less abuse potential than schedule III drugs and limited dependence liability (eg, some sedatives, antianxiety agents, nonnarcotic analgesics). 

CENTRAL NERVOUS SYSTEM AGENTS Antianxiety Agents... 

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