As anxiolytics/hypnotics

FLUORINECOMPOUNDS,ORGANIC - FLUORINATED AROMATIC COMPOUNDS] (Volll) -as anxiolytic [HYPNOTICS, SEDATIVES, ANTICONVULSANTS, AND ANXIOLYTICS] (Vol 13)... 

Benzodiazepines. The benzodiazepines (BZs) are well established as anxiolytics, hypnotics, and muscle relaxants as represented bydiazepam,clonazepam,midazo-1am, and triazolam (Fig. 10.9). The BZ nucleus also occurs in natural products. Asperlicin is a... 

The CCK system shares one property with the opioid system, ie, the existence of selective nonpeptide antagonists. These include aspedicine, a natural benzodiazepine (136), and Devazepide (L-364,718 MK-329) (137). Selective, potent peptide antagonists for CCK, eg, Cl-988 and PD 134308, have been developed that maybe useful as anxiolytics and as dmgs which increase the analgesic effect of morphine but at the same time prevent morphine tolerance (138) (see Hypnotics, sedatives, anticonvulsants, and anxiolytics). 

Benzodiazepiaes have largely replaced barbiturates and barbiturate-like agents for use as anxiolytics and sedative—hypnotics. Because benzodiazepiaes rarely produce levels of CNS depression that require therapeutic iatervention, the need for analeptics has decreased considerably. 

Benzodiazepines have found wide therapeutic applications as anxiolytics, sedatives, hypnotics, anticonvulsants, and central muscle relaxants. 

TDM has improved the performance of anticancer, antidementia, antidepressant, antiepileptic, anticonvulsant, antifungal, antimicrobial, antipsychotic, antiretroviral, anxiolytic, hypnotic, cardiac, addiction treatment, immunosuppressant, and mood stabilizer drags for more than 30 years.2-9 Many analytical procedures evolved as analytical techniques and instrumentation have advanced. This chapter briefly reviews the different types of analytical methods the applications of high-throughput techniques in TDM are discussed in detail. 

Herbai sedatives and anxioiytics are a diverse group of plant drugs that commonly act as depressants of the central nervous system (CNS) (table 6.1). Pharmaceutical CNS depressants are used as anxiolytics, anti-epiieptics, sedatives, sleep-inducers (sedatives or hypnotics), general anesthetics, and recreationai drugs (e.g., ethanol) (table 6.2). CNS... 

Several Hi histamine antagonists (e.g., diphenhydramine, promethazine, and hydroxyzine) have been used as sedative-hypnotics, since they produce some degree of sedation. While this sedation is usually considered a side effect of their antihistaminic activity, in some cases the sedation is sufficient to allow the drugs to be used in the treatment of anxiety and sleep disturbances. For these drugs, the anxiolytic properties are thought to be a direct consequence of their ability to produce sedation. 

In this chapter, we discuss the pharmacology of medications that are classified as anxiolytic, sedative, or hypnotic—primarily the benzodiazepines, buspirone, zolpidem, eszopiclone, and zale-plon. Subsequently, we present diagnosis-specific treatment guidelines (outlined in Table 3-1). The commonly used anxiolytics and hypnotics, together with their usual doses, are shown in Table 3-2. Many antidepressant medications are also effective in the treatment of anxiety disorders. The pharmacology of antidepressants is discussed in Chapter 2 their clinical use in anxiety disorders is addressed in the diagnosis-specific sections later in this chapter. 

In principle, all drugs with damping action on the central nervous system could be used as anxiolytics or hypnotics, but the pharmacological and/or pharmacokinetic properties of most compounds are not appropriate for their therapeutic use ... 

In Chapter 1 of this book, psychopharmaceuticals were introduced as effective medicines that primarily have a symptomatic action but are problematic in several respects. Antipsvchotics can cause serious side effects and antidepressants often exert their therapeutic effects only after a delay of weeks and in many cases have unpleasant side effects. With anxiolytics, hypnotics and, in particular, psychostimulants, there are problems with habituation and the potential of dependency. It is therefore not surprising that psychopharmaceuticals do not enjoy a very high reputation among many doctors and the general public (see Box 8.1) and have been given names such as chemical strait-jackets for the older neuroleptics (Szasz, 1957) or chemical blinkers for the mind for tranquillizers. Elomaa (1993) even posed the question of whether the long-tom use of conventional antipsychotics should be considered a crime against humanity. 

BZDs differ considerably in potency, which refers to the milligram dose needed to produce a given clinical effect. These differences are in part due to differences in receptor site affinity. If given in the appropriate dose, any BZD may exert anxiolytic, hypnotic, or anticonvulsant effects. For example, anxiolytic BZDs, such as clorazepate and diazepam, are often used as hypnotics when anxiety is a prominent symptom associated with insomnia. 

Actions at benzodiazepine receptors are thought to underlie virtually all the pharmacological actions of the benzodiazepines, those that are desirable as well as those that are undesirable. This includes the desirable therapeutic actions of benzodiazepines as anxiolytics and sedative-hypnotics, as well as anticonvulsants and muscle relaxants. It also includes their undesirable side effects as amnestic agents and as agents that cause adaptations at the benzodiazepine receptor with chronic administration, which are thought to underlie the production of dependence and withdrawal from these agents (see Chapter 13). 

Most of the minor tranquilizers in the BZD exhibit similar clinical effects they differ primarily in their duration of action and in the dosage required to achieve the same effect. The BZDs are classified as short- (triazolam [Halcion]), intermediate- (alprazolam [Xanax] and lorazepam [Ativan]), and long-acting (chlordiazepoxide [Librium] and diazepam [Valium]). Of the various BZDs available in the United States in 2002, those primarily prescribed as anxiolytics and hypnotics include the intermediate- and long-acting variety. 

In SUMMARY, the naturally occurring ligands for the benzodiazepine and /or GABA-A receptor sites that act as sedative-hypnotics or anxiolytics all directly or indirectly augment GABA-A receptors and thereby depress neuronal activity. In this respect they act in a similar way to the various classes of drugs used to treat anxiety and insomnia. Such compounds do not induce natural sleep. They all increase slow-wave sleep but reduce REM sleep. 

Drugs and chemicals are known to cause activated interaction. The depressant action of opioid drugs is enhanced by drugs acting on the central nervous system (CNS) such as alcohol, anesthetics, anxiolytics, hypnotics, tricyclic antidepressants, and antipsychotics. Concomitant administration of opioid analgesics and monoamine oxidase inhibitors (MAOIs) should be avoided, or extra care should be taken if such a therapy is inevitable. Fatal reactions are reported when treated along with selegiline. Interactions also are reported with cyclizine, cimetidine, mexiletine, cisapride, metoclopramide, or domperidone. 

Corned answer = B. The anxiolytic properties of benzodiazepines, such as lorazepam, make them the drugs of choice in treating the anxiety and agitation of cocaine withdrawal. Lorazepam also has hypnotic properties. Phenobaibital has hypnotic properties but if s anxiolytic properties are inferior to those of the benzodiazepines. Cocaine itself could countered the agitation of withdrawal but its use would not be proper therapy. Hydroxyzine, an antihistaminic, is effective as an hypnotic and is sometimes used to deal with anxiety especially if emesis is a problem. Fluoxetine is an antidepressant with no immediate effects on anxiety. 

Lorazepam is a benzodiazepine with CNS, depressant, anxiolytic, and sedative properties, used as a hypnotic, sedative, and anxiolytic drug. 

Pharmacodynamic interactions. Many TCAs cause sedation and therefore co-prescription with other sedative agents such as opioid analgesics, antihistamines, anxiolytics, hypnotics and alcohol may lead to excessive drowsiness and daytime somnolence. The majority of TCAs can have undesirable cardiovascular effects, in particular prolongation of the QT interval. A similar risk of QT prolongation arises with many other cardiovascular drugs including amiodarone, disopyramide, procainamide, propa-... 

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