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Alprazolam 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 a and a ? 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 a1 are associated with sedation whereas those with higher affinity for GABAA receptors containing a2 and/or a3 subunits have greater anxiolytic activity.

The binding site for benzodiazepines is distinct from the binding site for barbiturates and GABA on the GABA receptor.

There is some evidence for antidepressant treatment of clinical depression in out patient settings, evidence for inpatients is lacking; other benzodiazepines are not known to have antidepressant activity.

Use:
Benzodiazepine anxiolytic. Anxiety disorders: Adults, initially, 0.25 mg 2 or 3 times daily. Increase dosage by 0.25 mg increments, if required. Maximum: 3 mg/day in divided doses.

Elderly or debilitated patients: Initially, 0.125 mg 2 or 3 times daily; increased gradually, if required, depending on tolerance and response.

Impaired hepatic or renal function: 0.125-0.25 mg 2 or 3times daily. Increase gradually if needed and tolerated.

Panic disorders: Initially, 0.5 - 1 mg at bedtime or 0.5 mg 3 times/day. Increase by increments no greater than 1 mg every 3-4 days until patient is free of attacks.

Some patients may require up to 10 mg/day. Discontinue Alprazolam slowly by decreasing the daily dosage by no more than 0.5 mg every 3 days. A decrease of 0.5 mg every 2-3 weeks is more appropriate when a dose of 6 mg daily or more has been administered even for only a few months. Once a dose of 2 mg daily is achieved, decrease the dose by 0.25 mg per 2 to 3 weeks.

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Do not stop taking abruptly.
Do not give this drug to anyone who is psychotic.
Narcotics may increase the sedative effects of this drug.
Do not take other sedatives, benzodiazepines,or sleeping pills with this drug. The combinations could be fatal.
Do not drink alcohol when taking benzodiazepines. Alcohol can lower blood pressure and decrease your breathing rate to the point of unconsciousness.
The habit-forming potential is high; it is possible to become dependent in the first few days.
Do not stop taking this drug abruptly; this could cause psychological and physical withdrawal symptoms.
Do not take Alprazolam if you have narrow-angle glaucoma. Alprazolam may worsen this condition.
Before taking this medication, tell your doctor if you have:

kidney disease.
liver disease.
a history of alcohol or drug abuse.
asthma or bronchitis.
emphysema.
any respiratory disease.
depression or suicidal thoughts.
mania.
bipolar disorder.
any psychiatric condition.

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