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Alprazolam was invented by Upjohn (now a part of Pfizer) and is marketed under various trade names. Its patent (#3,987,052 [1]) was filed on October 29, 1969, granted on October 19, 1976 and expired in September 1993.
HistoryAlprazolam was first marketed as an atypical benzodiazepine, but only classified for use treating anxiety neurosis. Researchers later speculated, however, that alprazolam could be studied for serotonergic effects. On October 20, 1976, Dr. Guy Chouinard was the first to conduct a clinical trial of alprazolam in panic disorder. Patients diagnosed with panic disorder were included among participants in the study. 50 patients were given either the alprazolam or a placebo during an 8-week double-blind controlled study. Results proved that both somatic and psychic anxiety was decreased significantly in those who took the alprazolam, compared to the placebo. 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.
The binding site for benzodiazepines is distinct from the binding site for barbiturates and GABA on the GABA receptor. Clinical evidence of antidepressant activity is lacking, other benzodiazepines are not antidepressant. 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. IndicationsImage:Alprazolam2mgresize.jpg alprazolam 2mg tablet bottle The main medical uses for alprazolam include:
AvailabilityAlprazolam is generally sold in generic form in Italy and the United States. It is also sold under many other brand names, depending on the country:
PackagingThe inscriptions on tablets vary depending on manufacturer and on the country where it is marketed. Appearance is generally as follows in the United States [3]. Usually, Xanax® comes in the following dosages:
The Xanax XR® formulation is usually marketed as:
Xanor SR® (slow release) similar to "XR" above:
Side effectsCommon side effects of alprazolam can include:
Less common side effects can include:
Rare side effects can include:
Rare paradoxical side effects can include:
Paradoxical side effects are usually a result of too high a dose (sometimes deliberate) and/or combination with alcohol. Adjusting the dosage usually causes them to cease. Concentrations of alprazolam in cigarette smokers may be reduced up to 50% when compared to non-smokers.[4]. Long-term treatment with alprazolam may lead to physical and/or psychological dependence. Users often develop a tolerance to the drug's sedative effects, though tolerance to its anxiolytic efficacy rarely develops when used at therapeutic dosage levels. There is now a general consensus among psychiatrists that alprazolam (a so-called 'high-potency' benzodiazepine) poses a particularly high risk for misuse, abuse and dependence. Withdrawal after long-term treatment should be done slowly over a period of weeks (or even months) to avoid serious withdrawal symptoms such as agitation, panic attacks, rebound anxiety, muscle cramps and seizures. Some patients may benefit from a substitution with diazepam or clonazepam as these drugs remain in the bloodstream longer and have a somewhat lower risk of dependency. Patients taking a dosing regimen larger than 4mg per day have an increased potential for emotional and physical dependence.[citation needed] Patients who have this dependence may find it difficult to discontinue use and should seek a healthcare professional immediately so they may put you on a proper regimen to discontinue use. In addition to dependence, this medication may cause withdrawal symptoms, and in some cases has been known to cause seizures. The use of this medication may also cause a reaction called rebound anxiety. When a patient discontinues use, they may experience the symptoms they had before taking medication. Symptoms may also be accompanied other reactions including changes in mood, anxiety or sleep. Rebound anxiety is usually a result of abrupt discontinuation of this medication; patients who taper off are less likely to experience these symptoms. ContraindicationsUse of alprazolam should be avoided in individuals with the following conditions:
Women who are pregnant should avoid alprazolam. Children of mothers who are taking alprazolam are considered at risk for withdrawal symptoms during the postnatal period. Some children born under these conditions have been reported to have neonatal flaccidity and respiratory problems. Likewise, nursing mothers should avoid alprazolam due to the fact that benzodiazepines are known to be passed into breast milk. This can cause infants to become lethargic and lose weight. [5] [6] Elderly individuals should be cautious in the use of alprazolam due to the possibility of increased sensitivity to side effects, especially loss of coordination and drowsiness. [7] Eating grapefruits or drinking grapefruit juice while using alprazolam increases blood concentrations by inhibiting the intestinal metabolism.[1] Patients at a High Risk for Abuse and DependenceAt a particularly high risk for misuse, abuse, and dependence are:
Patients from the aforementioned group should be monitored very closely during therapy for signs of abuse and development of dependence. Discontinue therapy if any of these signs are noted. Long-term therapy in these patients is not recommended. Recreational useImage:Xanax2mg.jpg alprazolam 2mg tablets Alprazolam, like all benzodiazepines, has the potential for abuse. Although it is not manufactured illegally, it is often diverted to the black market. The state of relaxation, anxiolysis, disinhibition and euphoria induced by benzodiazepines is the main reason for their illicit use. Injecting alprazolam is considered especially dangerous by medical professionals. When crushed in water, it will not dissolve, potentially causing severe damage to arteries if not filtered properly. While it is somewhat soluble in alcohol, the combination of the two, particularly when injected, have the potential to cause a serious, and potentially fatal overdose. Alprazolam may also be insufflated and, although it is not water soluble, clinical testing dispels the rumor about less activity via insufflation[2] Alprazolam is sometimes used with other recreational drugs to relieve the panic or distress of dysphoric reactions to psychedelics such as LSD and also to promote sleep in the "come-down" period following use of recreational drugs with stimulant or insomniac properties (such as LSD, cocaine, amphetamines, DXM, and MDMA along with the related amphetamines), although other benzodiazepines arere. It is also often used in conjunction with marijuana or heroin to potentiate the relaxing effect. It is also often used by heroin addicts to suppress withdrawal symptoms, as its effects in conjunction with methadone produce a high which closely resembles that of heroin. Legal statusIn the United States, alprazolam is a prescription drug and is assigned to Schedule IV of the Controlled Substances Act by the Drug Enforcement Administration. Internationally, alprazolam is included under the United Nations Convention on Psychotropic Substances.[3] References
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