Anxiolytic drugs insomnia

Benzodiazepines are amongst the most frequently prescribed drugs they have well-established uses in the treatment of anxiety disorders (anxiolytics) and insomnia, preanaesthetic sedation, suppression of seizures, and muscle relaxation. 

A 65-year-old man who had had primary insomnia for 20 years, was given olanzapine 2.5 mg/day at nighttime because of lack of response to various anxiolytics he developed fecal incontinence during the 20 days of olanzapine treatment in combination with two anxiolytic drugs. The frequency of incontinence varied from 1 to 3 times a day, and withdrawal of olanzapine resulted in complete recovery. 

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... 

The term minor tranquilizer (which has been replaced by the more precise terms sedative-hypnotic or anxiolytic ) refers to drugs used to treat conditions such as insomnia and anxiety. Because they reduce anxiety and produce pleasantly sedating or tranquilizing effects, these drugs are more subject to abuse than the neuroleptics. 

Historically the first sedative hypnotics to be introduced were the bromides in the mid 19th century, shortly followed by chloral hydrate, paraldehyde and urethane. It was not until the early years of this century that the first barbiturate, sodium barbitone, was developed and this was shortly followed by over 50 analogues, all with essentially similar pharmacological properties. The major breakthrough in the development of selective, relatively non-toxic sedative hypnotics followed the introduction of chlordiazepoxide in 1961. Most of the benzodiazepines in current use have been selected for their high anxiolytic potency relative to their central depressant effects. Because of their considerable safety, the benzodiazepines have now largely replaced the barbiturates and the alcohols, such as chloral hydrate and trichloroethanol, as the drugs of choice in the treatment of insomnia. 

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). 

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. 

If the patient is heavily tobacco-dependent and severe anxiety, irritability, headache, insomnia and weight gain (about 3 kg) and tension are concomitants of attempts to stop smoking, an anxiolytic sedative (or P-adrenoceptor blocker) may be useful for a short time, but it is important to avoid substituting one drug-dependence for another. 

The benzodiazepines are primarily administered for their sedative-hypnotic effects. Benzodiazepines are commonly used as anxiolytics, muscle relaxants, anticonvulsants, and to treat alcohol withdrawal, insomnia, and agitation. They are administered pre-operatively for their anterograde amnesia effects and are combined frequently with other medications for conscious sedation before procedures. They are also utilized as drugs of abuse. 

HYPNOTICS are agents that induce sleep. They are used mainly to treat short-term insomnia, for instance in shiftwork, to cope with Jet-lag or in sleep disturbances due to emotional problems or in serious illness. The best-known and most-used hypnotics in current use are the benzodiazepines - and this class of drug is also used, at a lower dose, as ANXIOLYTICS. Examples from the class that are of relatively long-lasting action and may cause drowsiness the next day include diazepam, flunitrazepam, flurazepam and nitrazepam. Examples with a shorter duration include loprazolam, lormetazepam and temazepam. All can cause drug dependence on continued usage. Examples of hypnotics that are now much less used include chloral hydrate, chlormethiazole and triclofos. The barbiturates (e.g. amylobarbitone) are now very little used, as they are prone to cause serious dependence and are dangerous in overdose. 

One of the problems associated with benzodiazepine anxiolytics is rebound anxiety and/or insomnia, which may occur between dose intervals or after withdrawal of the drug [83, 84], In three experiments performed with squirrel monkeys, (92) (up to 20 mg/kg p.o.) did not cause any apparent physical or behavioural signs of withdrawal after abrupt discontinuation of treatment or even after attempted precipitation of withdrawal by administration of flumazenil. 

Indeed, they are known for their anxiolytic, cardiovascular, analgesic, antihypertensive, and neuroleptic among other activities. These heteroclyclic skeleton forms the core structure of several drug molecules like zolpidem used in the treatment of insomnia, alpidem, an anxiolytic agent, olprinone for the treatment of acute heart failure, minodronic acid useful for the treatment of osteoporosis, and zolimidine used for the treatment of peptic ulcer. Besides, imidazo[l,2-a] pyridines and pyrimidines are also attractive due to their physicochemical properties such as fluorescent activity [128]. 

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