Anxiolytic drugs sedation caused

Most anxiolytic and sedative-hypnotic drugs produce dose-dependent depression of central nervous system function. The ideal anxiolytic drug should calm the patient without causing too much daytime sedation and drowsiness and without producing physical or psycho-... 

By producing sedation, many drugs will also decrease the level of anxiety in a patient. Of course, these anxiolytic properties often cause a decrease in the level of alertness in the individual. However, certain agents are available that can reduce anxiety without an overt sedative effect. Those medications that selectively produce antianxiety effects are discussed later in this chapter. 

Many drugs are known depressants of the CNS, for example opioids, anxiolytics and hypnotics, older antihistamines, antipsychotic drugs and antidepressants, Other drugs may cause fatigue or lethargy by other mechanisms, as is seen with calcium channel blockers, Even minor degrees of sedation can be dangerous, for example ... 

Buspirone (BuSpar) is the first example of a class of anxiolytic agents that can relieve some symptoms of anxiety in doses that do not cause sedation. Buspirone is structurally unrelated to existing psychotropic drugs. 

This section describes the partial agonists and the nonbenzodiazepine drugs that act at the benzodiazepine receptor. What these drugs have in common is that their development has been driven by the search for effective anxiolytics that do not have the adverse effects of sedation, amnesia, ataxia, interaction with alcohol, or the problems of tolerance, dependency, and withdrawal seen with classic benzodiazepines. These problems have been addressed by the development of partial agonists, subtype-selective ligands, and other drugs, the cyclopyrrolones, which do not seem to cause these problems. 

Anxiolytics with fast onset of action but not causing sedation or leading to drug dependency. 

Tea Tree (Melaleuca alternifolia) Uses Rx of superficial wounds (bacterial, viral, fungal, insect bites, minor burns, cold sores, acne Action Broad-spectrum antibiotic activity against E. coli, S. aureus, C. albicans Available forms Topical creams, lotions, oint, oil apply topically PRN Notes/SE Ataxia, contact dermatitis, D, drowsiness, GI mucosal irritation Interactions Effects OF drugs that affect histamine release EMS effects of Benadryl Valerian (Valeriana officinalis) Uses Anxiolytic, antispasmodic, dys-menorrheal, restlessness, sedative Action Inhibits uptake stimulates release of GABA, which T GABA concentration extracellularly causes sedation Available forms Ext 400-900 mg PO 30 min < hs, tea 2-3 g (1 tsp of crude herb) qid, PRN, tine 3-5 mL (1/2-1 tsp) (1 5 ratio) PO qid, PRN Efficacy Probably effective sedative (reduces sleep latency) Notes/SE GI upset, HA, insomnia, N/V, palpitations, restlessness, vision changes Interactions T Effects OF barbiturates, benzodiazepines, opiates, EtOH, catnip, hops, kavakava, passion flower, skullcap effects OF MAOIs, phenytoin, warfarin EMS T Effects of benzodiazepines and opiates abruptly D/C may cause withdrawal symptoms... 

Insomnia is a common complaint in the elderly. As people age they require less sleep, and a variety of physical ailments to which the elderly are subject can cause a change in the sleep pattern (e.g. cerebral atherosclerosis, heart disease, decreased pulmonary function), as can depression. Providing sedative hypnotics are warranted, the judicious use of short half-life benzodiazepines such as temazepam, triazolam, oxazepam and alprazolam for a period not exceeding 1-2 months may be appropriate. Because of their side effects, there would appear to be little merit in using chloral hydrate or related drugs in the treatment of insomnia in the elderly. It should be noted that even benzodiazepines which have a relatively short half-life are likely to cause excessive day-time sedation. The side effects and dependence potential of the anxiolytics and sedative hypnotics have been covered elsewhere in this volume (Chapter 9). 

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-... 

Several clinical studies have shown buspirone (14a) to have anxiolytic efficacy equivalent to that of DZ with significantly less sedation. ° Rats trained to discriminate oxazepam or pentobarbital from vehicle did not generalize to buspirone. At doses above those which are anxiolytically relevant in man, the drug caused a dose-related elevation of plasma prolactin in male subjects, and like the BZ s also increased growth hormone levels. Buspirone elicits a dose-dependent rise in rat striatal dopamine (DA) metabolite levels and may do so by selective antagonism of presynaptic DA autoreceptors with minimal postsynaptic effects. Its catalepsy-reversal effects may occur... 

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