Alprazolam available under the trade name Xanax among others, is a short-acting anxiolytic of the benzodiazepine class. It is commonly used for the treatment of panic disorder, and anxiety disorders, such as generalized anxiety disorder (GAD) or social anxiety disorder (SAD).It was the 12th most prescribed medicine in 2010. Alprazolam, like other benzodiazepines, binds to specific sites on the GABAA receptor. It possesses anxiolytic, sedative, hypnotic, skeletal muscle relaxant, anticonvulsant, and amnestic properties.Alprazolam is available for oral administration in compressed tablet (CT) and extended-release capsule (XR) formulations.
Alprazolam has a fast onset of action and symptomatic relief. Ninety percent of peak effects are achieved within the first hour of using either the CT formulation or the XR formulation in preparation for panic disorder, and full peak effects are achieved in 1.5 and 1.6 hours respectively.Peak benefits achieved for generalized anxiety disorder (GAD) may take up to a week. Tolerance to the anxiolytic/antipanic effects is controversial with some authoritative sources reporting the development of tolerance, and others reporting no development of tolerance; tolerance will, however, develop to the sedative-hypnotic effects within a couple of days. Withdrawal symptoms or rebound symptoms may occur after ceasing treatment abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction.
Alprazolam was first released by Upjohn (now a part of Pfizer). It is covered under U.S. Patent 3,987,052, which was filed on 29 October 1969, granted on 19 October 1976, and expired in September 1993. Alprazolam was released in 1981.The first approved indication was panic disorder and within two years of its original marketing Upjohn's Xanax became a blockbuster drug in the US. Presently, alprazolam is the most prescribedand the most misused benzodiazepine on the U.S. retail market. The potential for misuse among those taking it for medical reasons is controversial with some expert reviews stating that the risk is low and similar to that of other benzodiazepine drugsand others stating that there is a substantial risk of misuse and dependence in both patients and non-medical users of alprazolam and that the pharmacological properties of alprazolam, high affinity binding, high potency, having a short elimination half-life as well as a rapid onset of action may increase the misuse potential of alprazolam. Compared to the large number of prescriptions, relatively few individuals increase their dose on their own initiative or engage in drug-seeking behavior.Alprazolam is classified as a schedule IV controlled substance by the U.S. Drug Enforcement Administration (DEA).
Alprazolam is mostly used to treat anxiety disorders, panic disorders, and nausea due to chemotherapy. The FDA label advises that the physician should periodically reassess the usefulness of the drug.Alprazolam may also be indicated for the treatment of generalized anxiety disorder, as well as for the treatment of anxiety conditions with co-morbid depression.Alprazolam is also often prescribed with instances of hypersomnia and co-morbid sleep deficits.
Alprazolam is effective in the relief of moderate to severe anxiety and panic attacks.However, it is not a first line treatment since the development of selective serotonin reuptake inhibitors, and alprazolam is no longer recommended in Australia for the treatment of panic disorder due to concerns regarding tolerance, dependence and abuse.Evidence supporting the effectiveness of alprazolam in treating panic disorder has been limited to 4 to 10 weeks. However, people with panic disorder have been treated on an open basis for up to 8 months without apparent loss of benefit.
In the United States, alprazolam is FDA-approved for the treatment of panic disorder with or without agoraphobia. Alprazolam is recommended by the World Federation of Societies of Biological Psychiatry (WFSBP) for treatment-resistant cases of panic disorder where there is no history of tolerance or dependence.
Anxiety associated with depression is responsive to alprazolam. Demonstrations of the effectiveness by systematic clinical study are limited to 4 months duration for anxiety disorder. However, the research into antidepressant properties of alprazolam is of poor quality and only assessed the short-term effects of alprazolam against depression. In one study, some long term, high-dosage users of alprazolam developed reversible depression.In the US, alprazolam is FDA-approved for the management of anxiety disorders (a condition corresponding most closely to the APA Diagnostic and Statistical Manual DSM-IV-TR diagnosis of generalized anxiety disorder) or the short-term relief of symptoms of anxiety. In the UK, alprazolam is recommended for the short-term treatment (2–4 weeks) of severe acute anxiety.
Nausea due to chemotherapy
Alprazolam may be used in combination with other medications for chemotherapy-induced nausea and vomiting.
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