Posted by Larry Hoover on June 16, 2003, at 11:53:49
In reply to Trials for pregabalin, posted by Maxime on June 16, 2003, at 11:08:03
> I know that pregabalin is supposed to be related to Neurotin in some way so I can see where it would be used for anxiety and as a mood stabiliser.
>
> So has anyone tried it? Does anyone have any information on the drug?
>
> MaxGabapentin, when used as a mood stabilizer, is off-label, so I wouldn't be surprised to find this drug used that way as well.
Expert Opin Investig Drugs. 2003 Apr;12(4):663-72.
Pregabalin: a new anxiolytic.Lauria-Horner BA, Pohl RB.
Department of Psychiatry, Dalhousie University, Halifax, NS, Canada.
Pregabalin (S-[+]-3-isobutylgaba) was designed as a lipophilic GABA (gamma-aminobutyric acid) analogue substituted at the 3'-position in order to facilitate diffusion across the blood-brain barrier. It was originally developed as an anticonvulsant agent, however it has been shown to be effective in the treatment of several disorders including hyperalgesia and behavioural disorders. Although its exact mode of action remains unclear, pregabalin interacts with the same binding site and has a similar pharmacological profile as its predecessor, gabapentin (1-[aminomethyl] cyclohexane acetic acid). Its main site of action appears to be on the alpha(2)delta subunit of voltage-dependent calcium channels, widely distributed throughout the peripheral and central nervous system. Pregabalin appears to produce an inhibitory modulation of neuronal excitability. In healthy volunteers, it is rapidly absorbed with peak blood concentrations within 1 h and it has a bioavailability of approximately 90%. In preclinical trials of anticonvulsant activity, pregabalin is three to ten times more potent than gabapentin. It is well-tolerated and associated with dose-dependent adverse effects (ataxia, dizziness, headache and somnolence) that are mild-to-moderate and usually transient. There are no known pharmacokinetic drug-drug interactions reported to date. Preliminary animal and human studies showed beneficial effects in both ethological and conflict models of anxiety, as well as having some sleep-modulating properties. In Phase II and III trials, pregabalin shows promising anxiolytic action when compared to placebo in generalised anxiety disorder, social phobia and panic disorder.
poster:Larry Hoover
thread:234311
URL: http://www.dr-bob.org/babble/20030614/msgs/234327.html