Following oral administration, alprazolam is quickly absorbed and metabolised by the body. Peak concentrations in plasma (proportionate to the dose) occur approximately 1 to 2 hours after ingestion. The metabolites 4-hydroxyalprazolam and a-hydroxyalprazolam are chiefly responsible for alprazolam’s metabolisation.

The precise mechanism of action in alprazolam is not currently known; merely that it enhances the body’s GABA, the CNS’s primary inhibitory neurotransmitter. Alprazolam is believed to act by strengthening (rather than adding to) the body’s existing GABA, which quietens the neurons in the brain, thereby calming the brain and subsequently the mind.

Alprazolam and its metabolites are largely excreted in urine.