alprazolam
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alprazolam
AlprazolamSystematic (IUPAC) name8-chloro-1-methyl-6-phenyl-4H-triazolobenzodiazepineIdentifiersCAS number28981-97-7ATC codeN05BA12PubChem2118DrugBankAPRD00280ChemSpider2034Chemical dataFormulaC17H13ClN4 Mol. mass308.765Pharmacokinetic dataBioavailability80-90%MetabolismHepatic, via Cytochrome P450 3A4Half lifeImmediate release: 11.2 hours; Extended release: 10.7-15.8 hoursExcretionRenalTherapeutic considerationsPregnancy cat.D(US)Legal statusSchedule IV(US)RoutesOralAlprazolam, also known under the trade names Xanax, Reclam and Niravam, is a short-acting drug of the benzodiazepine class used to treat moderate to severe anxiety disorders, panic attacks, and as an adjunctive treatment for anxiety associated with major depression. It is also available in an extended release form, Xanax XR. Both forms are now available generically.// History" underestimate the extent to which certain disorders affect the general populace. When you treat them, it can make a tremendous amount of difference in their lives." (David Sheehan, first discovered alprazolam's efficacy in treating panic disorder.)Alprazolam was first synthesized by Upjohn (now a part of Pfizer). Its patent (#3,987,052) was filed on October 29, 1969, granted on October 19, 1976 and expired in September 1993. It was released in 1981. The first indication for which alprazolam was approved was panic disorder. Upjohn took this direction at the behest of a young psychiatrist David Sheehan. Sheehan's suggestion was to use the confusion DSM-III created in the classification of anxiety disorders (a distinction had just been made in DSM-III between generalized anxiety disorder (GAD) and panic disorder). Panic disorder was, at that point, perceived to be rare and treatable only with tricyclic antidepressants; benzodiazepines were thought to be ineffective. However, from his clinical experience, Sheehan knew panic disorder to be both widespread among the populace and well responding to benzodiazepines. He suggested to Upjohn that marketing alprazolam for panic disorder will both cover new diagnostic territory and stress the unique potency of this drug. Sheehan describes that the first group of patients treated by alprazolam was so impressed by its action that they knew outright—this drug was going to be a hit. A few of those patients actually pooled their money and purchased stock in Upjohn. Several months later, when alprazolam was approved by the FDA, they sold out and made a profit. PharmacologyAlprazolam is a triazolobenzodiazepine, that is, a benzodiazepine with a triazolo-ring attached to its structure. Benzodiazepines produce a variety of effects by modulating the GABAA subtype of the GABA receptor, the most prolific inhibitory receptor within the brain. The GABAA receptor is made up from 5 subunits out of a possible 19, and GABAA receptors made up of different combinations of subunits have different properties, different locations within the brain and importantly, different activities in regards to benzodiazepines.There is some evidence for antidepressant treatment of clinical depression in outpatient settings, evidence for inpatients is lacking; other benzodiazepines are not known to have antidepressant activity. PharmacokineticsAlprazolam is readily absorbed from the gastrointestinal tract. The peak plasma concentration is achieved in 1-2 hours. Most of the drug is bound to plasma protein, mainly serum albumin. Alprazolam is hydroxylated in the liver to α-hydroxyalprazolam, which is also pharmacologically active. This and other metabolites are later excreted in urine as glucuronides. Some of the drug is also excreted in unchanged form. IndicationsThe main medical uses for alprazolam include:Alprazolam is FDA-approved for the short term treatment (up to 8 weeks) of panic disorder, with or without agoraphobia. Alprazolam is very effective in preventing moderate to severe anxiety, essential tremor, panic attacks and other types of convulsive behaviors. Physicians who elect to prescribe alprazolam for longer than 8 weeks should be aware that continued efficacy has not been systematically demonstrated beyond 8 weeks use as tolerance to alprazolam's effects may occur after 8 weeks and necessitate discontinuation or physician-directed dose escalation. However, long-term maintenance therapy on alprazolam is not unheard-of in the medical community, and, if a genuine therapeutic need exists, benefits must be weighed against risks.Alprazolam is recommended for the short-term treatment (2-4 weeks) of severe acute anxiety. Alprazolam should only very rarely be used for longer periods of time -- the body becomes rapidly tolerant to the drug's effects, which may translate to decreased efficacy. Decreased efficacy can lead to dose escalation, and the use of high doses puts the patient at higher risk for withdrawal if the drug is discontinued suddenly.However, in 1992 Romach and colleagues reported that dose escalation was not a characteristic of long-term alprazolam users, and the majority of patients indicated that alprazolam continued to be effective. A 2003 study did not support the hypothesis that long-term use of benzodiazepines frequently results in notable dose escalation.In a 1-year follow-up study of patients with panic disorder continuing treatment with clonazepam, 90% maintained a positive response without developing significant tolerance. In a 2.5-year follow-up study of alprazolam therapy, little evidence of tolerance emerged. AvailabilityAlprazolam is available in english speaking countries under the following brand names. Alprax, Alprox, Alzam, Anxirid, Apo-Alpraz, Azor, Calmax, Gerax, Kalma, Niravam, Novo-Alprazol, Nu-Alpraz, Xanax, Xanor, Zopax. PackagingImprints vary depending on drug manufacturer. The imprints above refer to the name-brand design in the United States and other first world countries, however, every variety of alprazolam is generically available and thus individual pill design is left up to the manufacturer. Side effectsSide effects of alprazolam may occur in patients and are more likely the higher the dosage taken. If signs of an allergic reaction occur such as hives, difficulty breathing, swelling of face, lips, tongue or throat occur medical attention should be sought immediately. Medical attention should also be sought immediately if signs of jaundice appear such as yellowing of the skin or eyes. Other side effects which may occur are as follows:euphoriadrowsinessdecreased inhibitions, no fear of danger (increased risk taking behavior)depressed mood with thoughts of suicide or self harm or elevated mood and confidencehallucinations, agitation and hostilityfeeling dizziness, light headed or faintingurinating less than usual or not at allheadache, fatigue, joint pain and unusual weakness (flu like symptoms)speech problems,Short term (anterograde amnesia) and concentration problemschanges in appetite (including changes in weight)blurred vision, unsteadiness and clumsiness (impaired coordination and balance)constipation, diarrhea, nausea and vomitingdecreased or increased sex drivedry mouth or. more likely, increased salivationsweatingpounding in the chest or rapid heartbeatskin inflammationParadoxical side effectsParadoxical side effects occasionally occur. Severe paradoxical effects such as seizures only rarely occur.hyperactivitynervousnessrestlessnesssleeplessnessmuscle twitchingtremorseizure (convulsions) Physical dependence and withdrawalAlprazolam and other benzodiazepines cause withdrawal symptoms during dose reduction or cessation of therapy after long-term treatment. Discontinuation should be done gradually over a period of months (or even up to a year) to avoid serious withdrawal symptoms such as agitation, panic attacks, rebound anxiety, muscle cramps and seizures. Some patients on alprazolam (Xanax) may benefit from a substitution with a benzodiazepine equivalent dose of another benzodiazepine drug such as diazepam (Valium) or chlordiazepoxide (Librium) as these drugs remain in the bloodstream longer and therefore have less potential for abuse and dependence. There is a higher chance of withdrawal symptoms if the drug is administered in a higher dosage than recommended, or if a patient stops taking the medication altogether without slowly allowing the body to wean itself off the drug.If a consumer of the drug feels the need to end treatment with alprazolam, they should consult their doctor/physician before discontinuing medication. Some immediate symptoms of alprazolam withdrawal include:Common Withdrawal SymptomsA rapid heartbeat (Tachycardia)DepressionDry mouth/chapped lipsTemporary inability to stop talking/moving (OCD)Mental sensitivityStrong loss of appetiteExtreme InsomniaAnxietyDizzinessMinor tremorsPossible/Less Common Withdrawal SymptomsNausea, vomiting, or diarrheaPanic attacksMood swingsHeart palpitationsHallucinationsMemory lossSeizuresFeverPatients treated with alprazolam or other benzodiazepines for generalized anxiety disorder were found (when abruptly discontinuing their medication) to experience withdrawal symptoms such as a worsening of anxiety, as well as the development of physical withdrawal symptoms.Patients taking a dosing regimen larger than 4 mg per day have an increased potential for dependence. This medication may cause withdrawal symptoms, which in some cases have been known to cause seizures. The discontinuation of this medication may also cause a reaction called rebound anxiety. Other withdrawal effects reported from discontinuing alprazolam therapy include homicidal ideation, rage reactions, hyperalertness, increased nightmares, and intrusive thoughts.After 8 - 9 weeks of alprazolam taken at a fixed prescribed dose, the following symptoms have been found to occur during abrupt discontinuation: dysphoric mood, fatigue, low energy, confusion, and elevated systolic blood pressure, severe anxiety.When a patient discontinues use, they may experience the symptoms they had before taking medicati
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alprazolam
Alprazolam, also known under the trade names Xanax and Niravam, is a short-acting drug of the benzodiazepine class used to treat moderate to severe anxiety disorders, panic attacks ...
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Stress, anxiety, depression, even panic disorders – all are a part of today’s fast-paced, stressful world. Nearly everyone suffers from one, or even a combination, of these ...
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Alprazolam is used to treat anxiety disorders, panic disorders, and anxiety. Includes alprazolam side effects, interactions and indications.
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