Primary therapeutic uses of barbiturates are as anesthetic and anticonvulsant medications. īarbiturates are classified as sedatives due to their central nervous system depressant and sleep-inducing effects. Increasing reports of bizarre and complex behavioral effects from z-drugs have prompted regulatory agencies to issue warnings and restrictions on prescribing, dispensing, and using z-drugs. However, adverse effects such as hallucinations and psychosis have been reported, particularly with zolpidem. They possess a shorter duration of action and half-life, do not disturb overall sleep architecture, and cause less residual effects during daytime hours, making them more clinically attractive than benzodiazepines. These sedatives are often called “z-drugs.” They are agonists that bind to the same binding site as benzodiazepines at the GABA-A receptor, but they only act on the BZ1 subtype receptor and, thus, are similar to typical benzodiazepines (i.e., diazepam, alprazolam, and others), even though they are more selective receptor subtype agonists. Food and Drug Administration (FDA) for treatment of insomnia: zaleplon (Sonata), zolpidem (Ambien), and eszopiclone (Lunesta). In addition to benzodiazepines, there are three non-benzodiazepine drugs approved by the U.S. Many different benzodiazepines are prescribed, with different durations of action, rates of onset, and intensities of euphoria. These properties have made it popular among sexual predators to add to the drink of a potential victim. It has achieved notoriety as a date-rape drug because it is colorless, odorless, and miscible with alcohol (which enhances the sedative and amnestic effects). Flunitrazepam (Rohypnol) is a short-acting benzodiazepine that is available by prescription in South America and Europe but not in the United States its potency is about 10 times that of diazepam. In addition to reducing anxiety and inducing sleep, benzodiazepines can cause euphoria and, therefore, are subject to abuse as recreational drugs. Some benzodiazepines (oxazepam, lorazepam, and temazepam ) are directly conjugated via glucuronyl transferase and then excreted, while others (alprazolam and diazepam ) are first metabolized by the cytochrome P-450 isozyme 3A4 and/or 3A5. The most commonly prescribed sedatives are benzodiazepines, which are similar to alcohol in that they facilitate the inhibitory effects of gamma-aminobutyric acid (GABA) at the GABA-A receptor complex, primarily by binding non-selectively to the benzodiazepine subtype 1 (BZ1) and BZ2 receptors. These are commonly prescribed for insomnia and other sleep problems and are also used for anxiety, either generalized or for panic attacks. Sedative drugs include benzodiazepines, barbiturates, and other sleeping pills (see Table 1). At that time, she was started on clonazepam (Klonopin), but she states she prefers alprazolam. She reports that her alprazolam vanished about a week ago she was not sure if it was stolen or if she had a blackout from taking it. She is widowed and lives alone, and she has poor coping skills and limited social support. She denies abusing illicit drugs or alcohol (she has one mixed drink per week) and denies suicidal ideation. However, she feels she needs it and wants something to help her anxiety symptoms and her insomnia. She wants to stop alprazolam because it has been causing memory problems (blackouts) and her physicians have expressed concern about her overuse without much improvement in her depression. She admits to taking more alprazolam than prescribed and denies buying any medications illegally without a prescription (“off the street”). She has gradually been increasing the amount of alprazolam she takes, up to 7-10 mg per day. For the past 3 months, she has had depressed mood with crying spells, decreased appetite, and weight loss. She describes episodes of shaking and dyspnea with anxiety lasting for about an hour several times per day for which she would take alprazolam 2-3 mg. She has been prescribed alprazolam (Xanax) for 5 years for anxiety and sleep problems. She has a long history of depression with periodic anxiety attacks. A 50-year-old woman presents for evaluation for anxiety and sleep problems.
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