Xanax was approved by the FDA in 1981 for the treatment of Generalized Anxiety Disorder (GAD), Panic Disorder with or without agoraphobia, and anxiety associated with depression (but not indicated for the treatment of depression alone).
Schedule IV controlled psychotropic
Alprazolam is a triazolobenzodiazepine – a benzodiazepine with a triazolo-ring attached to its structure. Alprazolam binds to the GABA subtype of the GABA receptor (Gamma-amino-butyric acid, a neurotransmitter found in the nervous system), increasing the inhibitory effects of GABA within the central nervous system (CNS). This binding site for benzodiazepines is different from the binding sites for barbiturates and GABA on the GABA receptor.
Unlike other benzodiazepines, alprazolam may also have some antidepressant activity, though clinical evidence of this is lacking.
Xanax’s mechanism of action is not completely understood, but the drug is readily absorbed from the gastrointestinal tract.
Indications and Dosage:
Xanax is indicated for the management of anxiety disorder or short-term relief of symptoms of anxiety. Anxiety or tension associated with the stress of day to day life normally does not warrant or require treatment with alprazolam.
Generalized Anxiety Disorder (GAD) is characterized by unrealistic or excessive anxiety and worry about two or more circumstances in one’s life, for a period of six months or more, during which the individual is bothered more than not by these concerns. At least 6 of the following symptoms are normally present in these patients: trembling, twitching, shakiness, muscle tension, soreness, restlessness, aches and pains, fatigue, shortness of breath, palpitations or accelerated heart rate, sweating, nausea, diarrhea, cold clammy skin, dry mouth, dizziness or lightheadedness, abdominal distress, flushes or chills, frequent urination, difficulty swallowing, feeling on edge, exaggerated startle response, difficulty concentrating, sleep disturbances, irritability. The symptoms must not be secondary to another psychiatric disorder or caused by some organic agent.
Demonstrations of the efficacy of Xanax by systematic clinical study are limited to 4 months for anxiety disorder and 4 to 10 weeks for panic disorder; however, patients with panic disorder have been treated for up to 8 months without any diminishment in benefit. The physician should periodically reassess the efficacy of the drug for the individual.
Xanax Side Effects and Interactions:
Common side effects associated with Xanax include somnolence (drowsiness), impaired motor functions such as clumsiness and dizziness, fatigue and headaches.
Rarer side effects may include blurred vision, sleep apnea, hypoventilation, disturbance in depth perception, slurred speech, confusion, disorientation, changes in personality, vivid dreams and/or nightmares, amnesia, bradycardia, tachycardia, jaundice, changes in plasma cortisol and ACTH levels, decreased or increased salivation, blood dyscrasias, incontinence, elevated liver enzymes, constipation, nausea.
There are rare and often paradoxical side effects including anxiety, nervousness, agitation, rage, insomnia and muscle spasms and rigidity. These types of adverse side effects are often a result of too high a dose (sometimes deliberate) and/or use in combination with alcohol. They often cease with proper dosage adjustment.
Long-term use of alprazolam may lead to physical and/or psychological dependence. Patients often develop a tolerance to the drug’s sedative effects, but tolerance to the anxiolytic effects is rare when used at proper dosage levels.
Many psychiatrists have now come to the general consensus that alprazolam poses a particularly high risk for abuse, misuse and dependence.
Information for Parents and Kids:
A physician should be consulted before administering Xanax to children, since the safety and efficacy have not been established in persons below the age of 18.
Alprazolam is an FDA category D drug, meaning that it is known be harmful to an unborn baby. Do not take this medication without first speaking to a physician if you are pregnant or could become pregnant during treatment.
It is unknown whether Xanax passes into breast milk. If you are breast feeding a baby, consult a physician before taking alprazolam.
Warnings and Precautions:
Adverse clinical events, some life-threatening, are a direct consequence of physical dependence to alprazolam. These include a number of withdrawal symptoms; most importantly being seizure. Even after relatively short-term use at the recommended dosage for transient anxiety and anxiety disorder, there is some risk of dependence. Reported data suggests that the risk of dependence and its severity appear to be greater in those patients taking more than 4mg/day for long periods of time (longer than 12 weeks).
Due to the fact that proper management of panic disorder with Xanax requires the use of average daily doses above 4mg, the risk of dependence among these patients may be greater than that among those treated for less severe anxiety.
Though alprazolam is not manufactured illegally, often it is diverted to the black market. The induced state of relaxation, disinhibition, euphoria and anxiolysis benzodiazepines provide is the primary cause of its illicit use.
Though alprazolam is sometimes insufflated nasally (snorted), this method is no more potent that oral consumption because the drug is not absorbed by the nose’s mucous membranes. As well, if snorted, the user often “passes out” into a deep sleep, later awakening in disorientation with no memory of what occurred prior to sleep.
Injecting alprazolam is extremely dangerous. When crushed in water, it does not dissolve, thus there is a potential to cause severe arterial damage if intravenously taken. While it is somewhat soluble in alcohol, the combination of the two, particularly when injected, can easily cause a serious (and potentially life-threatening) overdose.
Xanax is sometimes taken with other recreational drugs to relieve the panic or distress of dysphoric reactions to psychedelics such as LSD as well as to promote sleep in the “come-down” period. In some cases, it is taken in conjunction with marijuana or heroin to potentiate the relaxing effects of these drugs. It is often combined with Methadone to produce a unique, heroin-like “high” and sometimes used by heroin addicts to suppress withdrawal symptoms.
Withdrawal symptoms associated with Xanax often resemble symptoms of withdrawal from other depressants, such as alcohol, and include shaky hands, rapid heartbeat, insomnia or other sleep disturbances, rapid heartbeat, anxiety and agitation.
Over-dosage & Contraindications:
Alprazolam overdose includes such manifestations as confusion, impaired coordination, diminished reflexes, somnolence (drowsiness) and coma. Death has been reported in cases of overdoses of Xanax alone, as is the case with other benzodiazepines. As well, fatalities have been observed in individuals who overdosed with a combination of a single benzodiazepine, including Xanax, in conjunction with alcohol. Alcohol levels seen in some of these patients were lower than those usually associated with alcohol-induced death, such as severe alcohol poisoning.
Reports of overdose with Xanax tablets are limited. As with all drug overdoses, pulse rate, respiratory function and blood pressure should be closely monitored. The patient should be provided general support along with immediate gastric lavage. Intravenous fluids should be administered and the airway should remain clear. Dialysis is of limited value in these cases. The chance of multiple agents being ingested, especially in the case of intentional overdose, should be kept in mind.
Flumazenil (Mazicon) is indicated for the reversal of benzodiazepines’ sedative effects and may be employed in benzodiazepine overdosage. Prior to administering flumazenil, necessary measures should be taken to ensure proper airway, ventilation and intravenous access. The drug is intended as an adjunct measure to benzodiazepine overdose, not a substitute for proper overdose care. It should be noted there is a risk of seizure with the use of flumazenil, especially in persons with long-term history of benzodiazepine use and in cases of overdose with a cyclic antidepressant.
Alprazolam should not be used by persons with a known sensitivity to the drug or any other benzodiazepines. Alprazolam may be administered to individuals with open angle glaucoma who are receiving appropriate therapy, but is contraindicated in patients with acute narrow angle glaucoma.
Generic Name: alprazolam
Chemical Formula: C17H13ClN4
Routes of Administration: oral
Elimination Half Life: 6-12 hours
Legal Status: by prescription only