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Information about Alprazolam*
Alprazolam is a short acting benzodiazepine used for its
anxiolytic effects to treat anxiety disorders. It is sold under several brand
names such as Xanax, Xanor, Alplax, Tranquinal, Trankimazin, and Tafil.
Alprazolam has a calming effect, with potential side effects of drowsiness,
clumsiness, fatigue, and headache. The drug can also have more severe side
effects, such as blurred vision, slurred speech, and changes in normal behavior.
The drug is habituating, and users develop a tolerance. Physical and
psychological dependence after several months of alprazolam treatment is common.
As a result, long-term alprazolam treatment cannot be abruptly terminated, but
must instead be slowly reduced in dosage over a course of weeks (as is the case
with many drugs operating on neurotransmitters). Abrupt cessation may cause
rebound anxiety, insomnia, and seizures, among other symptoms.
For more long-term relief of anxiety, selective serotonin reuptake inhibitor
medicines such as paroxetine, sertraline, or fluoxetine are often prescribed.
In the United States, the sale of alprazolam is regulated by the Food and Drug
Administration, and requires a doctor's prescription. Internationally,
alprazolam is a Schedule IV drug under the Convention on Psychotropic
Substances[1].
Mechanism of action
Alprazolam is a triazolobenzodiazepine, that is, a benzodiazepine with a
triazolo-ring attached to its structure. Alprazolam binds to the GABA receptor
GABAA, causing a conformational change and thus increasing inhibitory effects of
GABA. Unlike other benzodiazepines, alprazolam also has some antidepressant
activity.
Pharmacokinetics
Alprazolam 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 albumin. Alprazolam is hydroxylated in the liver to a-hydroxyalprazolam,
which is also active. This and other metabolites are later excreted in urine as
glucuronides. Some of alprazolam is also excreted in unchanged form.
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