Pregabalin
Pregabalin is a potent ligand for the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system that exhibits potent anticonvulsant, analgesic, and anxiolytic activity. It decreases presynaptic calcium currents, thus decreasing the release of several excitatory neurotransmitters that play an important role in anxiety. Interestingly, although Pregabalin is a GABA analogue, it has no demonstrated effects on GABA receptors or GABA metabolism.
Pregabalin demonstrates highly predictable and linear pharmacokinetics, a profile that makes it easy to use in clinical practice. Absorption is extensive, rapid, and proportional to dose. Time to maximal plasma concentration is approximately 1 h and steady state is achieved within 24-48 hours. These characteristics reflect the observed onset of efficacy as early as day two in clinical trials
It has a high bioavailability, a mean elimination half life of 6.3 hours.
Administration with food has no clinically relevant effect on the amount of pregabalin absorbed, providing for a dosing regimen uncomplicated by meals.
Pregabalin does not bind to plasma proteins and is excreted virtually unchanged by the kidneys. It is not subject to hepatic metabolism and does not induce or inhibit liver enzymes such as the cytochrome P450 system. Therefore, pregabalin is unlikely to cause, or be subject to, pharmacokinetic drug-drug interactions.
There is some potential for abuse of pregabalin, however, the euphoric effects of pregabalin disappear with prolonged use.
Pregabalin demonstrates highly predictable and linear pharmacokinetics, a profile that makes it easy to use in clinical practice. Absorption is extensive, rapid, and proportional to dose. Time to maximal plasma concentration is approximately 1 h and steady state is achieved within 24-48 hours. These characteristics reflect the observed onset of efficacy as early as day two in clinical trials
It has a high bioavailability, a mean elimination half life of 6.3 hours.
Administration with food has no clinically relevant effect on the amount of pregabalin absorbed, providing for a dosing regimen uncomplicated by meals.
Pregabalin does not bind to plasma proteins and is excreted virtually unchanged by the kidneys. It is not subject to hepatic metabolism and does not induce or inhibit liver enzymes such as the cytochrome P450 system. Therefore, pregabalin is unlikely to cause, or be subject to, pharmacokinetic drug-drug interactions.
There is some potential for abuse of pregabalin, however, the euphoric effects of pregabalin disappear with prolonged use.
