Benzodiazepines antianxiety drugs

Tranquilizers (also called antianxiety drugs) are used to treat a variety of psychiatric disorders which go along with anxiety (anxiety disorders). Serotonin-reuptake inhibitors and the benzodiazepines are the most commonly employed drugs for the treatment of common clinical anxiety disorders. 

Benzodiazepine withdrawal may occur when use of the antianxiety drugs is abruptly discontinued after 3 to 4 months of therapy. Occasionally, withdrawal symptoms may occur after as little as 4 to 6 weeks of therapy. Symptoms of benzodiazepine withdrawal include increased anxiety, concentration difficultiesi, tremor, and sensory disturbances, such as paresthesias photophobia, hypersomnia, and metallic taste. To help prevent withdrawal symptoms, the nurse must make sure the dosage of the benzodiazepine is gradually decreased over a period of time, usually 4 to 6 weeks... 

In summary, buspirone is an effective generalized anxiety treatment that differs from conventional antianxiety drugs in speed of symptom reduction and types of symptoms affected. Although buspirone might seem to be the drug of choice for treatment of chronic anxiety, it has not displaced the use of benzodiazepines in the treatment of anxiety, perhaps because of its side-effect profile [dizziness, sedation, nausea], slow onset of action, and the opinion of some clinicians that its anxiolytic efficacy is less robust than that of benzodiazepines. Buspirone is accepted as an anxiolytic treatment much more widely in the United States than in most other countries [Kunovac and Stahl 1995]. 

Benzodiazepines are also known as minor tranquilizers. Not as potent or dangerous as barbiturates, the benzodiazepines do find use as antianxiety drugs because of their safety and efficacy. In higher doses they will also induce sleep. All benzodiazepines cause a dose-... 

The quinazolones methaqualone (129 R = Me) and mecloqualone (129 R = Cl) are anticonvulsants, but little structural variation can be made without loss of activity. The benzodiazepines which were first introduced as antianxiety drugs have proved useful as anticonvulsants, particularly diazepam (135) and nitrazepam (136). 

More importantly, buspirone has a much better side-effect profile than traditional antianxiety drugs. Buspirone seems to produce less sedation and psychomotor impairment than benzodiazepine agents.2... 

Antidepressant drugs, however, might have direct anxiolytic effects. That is, certain antidepressants such as paroxetine (Paxil) or venlafaxine (Effexor) can help reduce anxiety independent of their effects on depression.1,47 These antidepressants have therefore been advocated as an alternative treatment for anxiety, especially for people who cannot tolerate the side effects of traditional anxiolytics, or who might be especially susceptible to the addictive properties of drugs like the benzodiazepines.1,9,46 Moreover, antidepressants such as paroxetine or venlafaxine are now considered effective as the primary treatment for several forms of anxiety, including generalized anxiety disorder, social phobia, and panic disorder.4,29,53 Antidepressants, either used alone or in combination with antianxiety drugs, have become an important component in the treatment of anxiety. 

Benzodiazepine drugs can cause a range of side effects, including dizziness, confusion, and impaired motor control. Long-term benzodiazepine use can lead to physical dependence. Despite these problems, benzodiazepines have remained the standard antianxiety drugs for approximately 50 years. 

Central nervous system depressants include the barbiturates, such as phenobarbital, and the antianxiety drugs, including diazepam (VaUum), chlordiazepoxide Odbrium), oxazepam (Serax), flurazepam hydrochloride (Dalmane), and lorazepam (Ativan). The benzodiazepines, including diazepam, occasionally cause mydriasis, presumably because of their anticholinergic side effects. 

Synonyms Minor tranquilizers Antianxiety drugs Sedative-hypnotics Benzodiazepines (BZDs)... 

Roche converted 2-amino-5-chlorobenzophenone (147) into the first benzodiazepine antianxiety agent, chlorodiazepoxide (148) (Scheme 30). The ring enlargement was unexpected, and was soon incorporated into similar products. The same intermediate, 147, is the starting point for diazepam (149), and provides one of two routes to oxazepam (150) discovered at Wyeth (Scheme 31)82. The full range of benzodiazepines exceeds fifteen different drugs used as tranquillizers, and in some case as hypnotics. 

BuSpar (buspirone) An antianxiety drug that is not often associated with abuse because of the absence of withdrawal phenomena, cognitive impairment, and sedation. It has a short half-life and therefore must be taken several times daily. It is also said not to have the same addicting or euphoric quality that is often noted in the benzodiazepines. BuSpar is not a benzodiazepine and is referred to as a nonbenzodiazepine. BuSpar is generally prescribed for a limited time to help control the symptoms of anxiety and allows the client to be calmer while learning new ways of coping with anxiety-producing events. 

Anxiety and insomnia are relatively common and sometimes can be managed by psychotherapy techniques rather than with drugs. Antianxiety drugs are mainly the benzodiazepines, which work by enhancing the effects of GABA in the brain. This relieves the effects of anxiety. In higher doses, the hypnotic effect of benzodiazepines can be useful in short-term treatment of insomnia. 

The benzodiazepines are used primarily as sedative-antianxiety drugs (see Chapters 16 and 17) but also have broad antiseizure properties. Clonazepam (KLONOPIN) and clorazepate (TRANXENE-SD, others) have been approved in the U.S. for the long-term treatment of certain types of seizures. Diazepam (VAUUM, diastat others) and lorazepam (ativan) have well-defined roles in the management of status epilepticus. 

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