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alprazolam
Alprazolam is a short-acting drug in the benzodiazepine class used to treat anxiety disorders and as an adjunctive treatment for depression. It is also used as a medication to aid the beginning of treatment with SSRI type drugs, since these can cause anxiety in the initial stages of use. 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. Fifty 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 were 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. In order for GABAA receptors to be sensitive to the action of benzodiazepines they need to contain an α and a γ subunit, where the benzodiazepine binds. Once bound, the benzodiazepine locks the GABAA receptor into a conformation where the neurotransmitter GABA has much higher affinity for the GABAA receptor, increasing the frequency of opening of the associated Chloride ion channel and hyperpolarising the membrane. This potentiates the inhibitory effect of the available GABA leading to sedatory and anxiolytic effects. As mentioned, different benzodiazepines can have different affinities for GABAA receptors made up of different collection of subunits. For instance, benzodiazepines with high activity at the α1 are associated with sedation whereas those with higher affinity for GABAA receptors containing α2 and/or α3 subunits have greater anxiolytic activity. 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. Indications
 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:
Packaging
The 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:
Side effectsCommon side effects of alprazolam can include:
Rare side effects can include:
There is now a general consensus among psychiatrists that alprazolam and other benzodiazepines can cause withdrawal symptoms after long-term treatment and 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 therfore have less potential for abuse and dependence. 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. When a patient discontinues use, they may experience the symptoms they had before taking medication. Symptoms may also be accompanied by 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. Most patients do not experience negative side effects to stop taking alprazolam. Consult your doctor for more information on how benzodiazepines can successfully treat anxiety disorders. ContraindicationsUse of alprazolam should be avoided in individuals with the following conditions:
PregnancyWomen who are pregnant or are planning on becoming pregnant should avoid alprazolam [4]. TeratogenicityTeratogenic effects: Pregnancy Category D. Nonteratogenic EffectsNonteratogenic Effects: It should be considered that the child born of a mother who is receiving benzodiazepines may be at some risk for withdrawal symptoms from the drug during the postnatal period. Also, neonatal flaccidity and respiratory problems have been reported in children born of mothers who have been receiving benzodiazepines. Labor and DeliveryXANAX has no established use in labor or delivery. Nursing Mothers/NeonatalBenzodiazepines are known to be excreted in human milk. It should be assumed that alprazolam is as well. Chronic administration of diazepam to nursing mothers has been reported to cause their infants to become lethargic and to lose weight. As a general rule, nursing should not be undertaken by mothers who must use XANAX. 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] Geriatric useElderly 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] Food and drug interactionsEating grapefruits or drinking grapefruit juice while using alprazolam increases blood concentrations by inhibiting the intestinal metabolism. [1] In fact, any drug that inhibits CYP3A4, for which alprazolam is a substrate, will increase serum concentrations of alprazolam significantly if administered prior or concurrently. Cimetidine is a widely used antacid that inhibits numerous cytochrome P450 enzymes. 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 use
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; 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). 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] ReferencesExternal links
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