does pregabalin feel same as valium?

[hanshan]

Hi Dan

A typical example would be:

Elinor Ben-Menachem - Pregabalin Pharmacology and Its Relevance to Clinical Practice - Epilepsia -Volume 45, Issue Supplement s6, pages 13–18, August 2004 - Article first published online: 17 AUG 2004

“Pregabalin has no effect on GABAergic mechanisms
Evidence suggests that pregabalin, although structurally related to GABA, is not functionally related, and as such does not act via the GABAergic system. Pregabalin itself is inactive at GABAA, GABAB, and benzodiazepine receptors, and is not converted metabolically into GABA or a GABA agonist (5–7). In addition, clinically effective concentrations of pregabalin have no effect on GABA uptake or degradation. Furthermore, experiments conducted in the rat forebrain and in the rat optic nerve demonstrate that pregabalin does not elevate GABA levels acutely in these tissues (15).

A non-GABAergic mechanism of action for pregabalin could have important clinical implications. First, it is possible that a drug that influences brain excitability by a different mechanism may be effective in patients who are resistant to existing AEDs with a more traditional mechanism involving GABAergic transmission. Second, lack of interaction with GABAergic systems, particularly its failure to elevate GABA levels in the optic nerve, may explain why pregabalin exhibits no retinal or optic nerve toxicity (16)”.

I have seen the following information on secondary sites such as Drugs Forum, but I can't find any journal articles that back it up, so I have to regard it as suspect:

“Pregabalin increases the activity of the glutamic acid decarboxylase enzyme; which converts glutamate into GABA, so GABA concentrations increase. Continued application of pregabalin use increases the concentration of GABA transporter proteins, which increases the rate of GABA transport.”

[hanshan]

I managed to find some information concerning pregabalin's possible role assisting in the formation of GABA (see above post).

Pharmacology and mechanism of action of pregabalin: The calcium channel 2—(alpha2—delta) subunit as a target for antiepileptic drug discovery
Charles P. Taylor, Timothy Angelotti, Eric Fauman

Epilepsy Research (2007) 73, 137—150

"The initial chemical synthetic work that led to the discovery of pregabalin was based on the concept of altering inhibitory synaptic activity in brain by interacting with GABA synthetic enzymes in brain such as glutamic acid decarboxylase, the primary GABA synthetic enzyme. Although pregabalin and gabapentin both were reported to augment the activity of glutamic acid decarboxylase in vitro (Silverman et al., 1991), this occurred only at millimolar concentrations not achievable in vivo. A later rat brain microdialysis study showed that the maximum pregabalin drug concentration in rat brain after anticonvulsant doses was 10—50 _M, far below concentrations reported to activate enzyme activity (Feng et al., 2001)."

It would appear that it was an early in vitro finding that has not been replicated in vivo. It is also inconsistent with current research.

[ANG3LIC]

god im lost sorry.. fab replies but dnt understand i was told preg feels same as valium but without bein addictive??? is this true??? xxx

[hanshan]

Hi Ang3lic,

Sorry about all the science, but Dan was wanting information about how it works.

I'd say pregabalin doesn't feel exactly the same as Valium, but has similar effects. Two differences are that it's not as fast acting and that it mainly works on lower levels of anxiety. If you suffer full-on panic attacks, then a fast-acting benzodiazepine will work better, but if you suffer low to medium levels of anxiety every day, then pregabalin is worth a try. It can be combined with an antidepressant like mirtazapine or duloxetine. It doesn't work for everyone, and usually has side effects for the first few weeks.

It's not addictive, so doctors can put you on a long-term maintenance dose, like an antidepressant, which is an advantage it has over benzodiazepines.

Hanshan