Current Neuropharmacology - Volume 1, Issue 3, 2003

This, third, issue of Current Neuropharmacology marks a new departure from the format of previous issues. As part of this issue there is a special section of review papers centred around the theme of Gabapentin, a drug originally developed as an anti-epileptic but which has found uses in other spheres of clinical practice. The papers in this special section range from basic research to clinical findings with this drug, and thes Read More

The role of serendipity in scientific research and in drug development is significant; if under appreciated. It is reported that we all make our own luck. The rational design of a drug that might mimic the actions of a major inhibitory neurotransmitter γ-aminobutyric acid) formed part of an antiepilepsy drug discovery program. The finding that this drug didn't mimic the transmitter but had antiepileptic properties anyway mus Read More

Gabapentin is an antiepileptic drug, which decreases neuronal excitability and may act by increasing the availability of gamma-aminobutyric acid or by inhibiting Ca2+ channels. It has safe pharmacokinetic and side effect profiles. Not surprisingly, it has been tested as a treatment in a number of psychiatric conditions. The most robust evidence exists for it as an efficacious treatment in both social phobia and panic disorder. Howev Read More

Gabapentin is an important advancement for the treatment of neuropathic pain. This novel anticonvulsant has demonstrated efficacy and safety in multiple clinical trials. Its pharmacological properties especially lack of adverse effects on any major organ systems including cardiovascular and respiratory systems allows flexible titration in a wide range of patients. Certainly, there are many side effects but majority are managea Read More

Gabapentin (GBP), one of the newer antiepileptic drugs (AEDs), is a structural analogue of gamma-aminobutyric acid (GABA), initially approved for add-on treatment of partial seizures in patients 12 years and older and now widely used also in younger patients. Recent studies demonstrated its efficacy not only as adjunctive therapy but also as monotherapy for patients with partial seizures. GBP has an extremely low propensity t Read More

In this review we describe the genes encoding α2δ subunits, their topology and predicted structure. We then review the electrophysiological effects of α2δ subunits. It is clear from most studies that α2δ subunits increase channel density at the plasma membrane, but there is less agreement between studies and between channel subtypes concerning the effects of α2δ subunits on voltage-dependence of activation and inactiv Read More

In this review we outline the actions of gabapentin and pregabalin on the excitability of sensory dorsal root ganglion (DRG) neurones in culture and compare these effects with those seen in other neuronal and cultured cell preparations. We also consider the potential mechanisms of action of gabapentin and pregabalin that may contribute to their anti-nociceptive effects. Gabapentin and pregabalin have similar actions and at s Read More

Gabapentin ( Neurontin) is currently utilised in the treatment of a range of neurological and psychiatric conditions, including partial epilepsy, neuropathic pain and bipolar disorders. Gabapentin (GBP) mechanisms of action, although extensively investigated, are only partially known. This review examines GBP-mediated effects on voltage- and ligand-gated neuronal ionic currents. GBP binds in vivo to the alpha-2-delta sub- Read More

Microglia are bone marrow-derived, monocyte-lineaged cells in the central nervous system (CNS). They are considered to serve as sensor cells, receiving a variety of alterations in the circumstances and responding with morphological and functional transformations. These responses of microglia in the injured or the pathologically damaged brain have been generally described as “microglial activation”. The main function Read More

Several converging lines of evidence from molecular, animal, and clinical studies have demonstrated that the gamma-aminobutyric type A (GABAA) receptor complex plays a central role in the modulation of anxiety. While currently available therapeutic agents that act on this receptor (e.g., benzodiazepines) are effective anxiolytics, they are limited by side effects, tolerance, and abuse potential. Promising strategies to addre Read More