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Alprazolam (Xanax, Xanor) - Description

PHARMACOLOGICAL ACTION:
Alprazolam is an anxiolytic agent of the benzodiazepine group. Benzodiazepines, including alprazolam, are thought to bind to central nervous system benzodiazepine receptors, thereby increasing the affinity of the receptor for gamma-aminobutyric acid (GABA). GABA, an inhibitory neurotransmitter, modulates the activity of other neurotransmitter systems, including the noradrenergic system
Pharmacokinetics:
The pharmacokinetics of alprazolam are linear over the recommended dosage range, with plasma concentrations being proportional to dose given. Alprazolam is almost completely bioavailable following oral administration. The bioavailability and pharmacokinetic characteristics of Xanax Tablets or Xanax SR Tablets are comparable, except for a slower rate of absorption of alprazolam from Xanax SR Tablets. The slower absorption rate for Xanax SR Tablets results in peak plasma alprazolam concentrations that are approximately one-half that of an equivalent dose of Xanax Tablets; peak concentrations occur within one to two hours after a single dose of Xanax Tablets, and 5 to 11 hours after a single dose of Xanax SR Tablets.
Steady-state plasma concentrations are achieved within three to four days of continuous dosing with either dosage form. When equivalent daily doses are given, steady-state peak and trough plasma alprazolam concentrations for Xanax SR Tablets given once or twice a day are comparable to Xanax Tablets given three or four times a day.
Alprazolam and its metabolites are excreted primarily in the urine. The predominant metabolites are alpha-hydroxy-alprazolam, 4-hydroxy alprazolam, and a benzophenone derived from alprazolam. Although they possess some pharmacological activity, the plasma levels of these metabolites are extremely low during chronic dosing. In vitro, alprazolam is bound (80%) to human serum protein.
The plasma elimination half-life of alprazolam has been found to be about 11 to 15 hours in healthy adults. A comparable elimination half-life for Xanax SR Tablets indicates that the metabolism and elimination of alprazolam are the same for both dosage forms. Alprazolam clearance has been reported to be delayed in patients with impaired hepatic and renal function, alcoholism, in elderly or obese patients, and by the co-administration of certain medicines.

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