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Old 09-10-2007, 05:55 PM #1
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Alkymst Alkymst is offline
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Location: Pennsylvania
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Alkymst Alkymst is offline
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Join Date: Jan 2007
Location: Pennsylvania
Posts: 231
15 yr Member
Default A new and improved AED perhaps?

I just saw this info re: lacosamide (Schwarz Biosciences) on the American Pain Foundation site and pass it along to this forum. It is also known as harkoseride or ADD234037 and from looking at the structure it is a synthetic derivative of the naturally occuring amino acid serine BUT IT IS NOT A NATURAL COMPOUND ITSELF! If this is old news I'm sorry but I don't remeber seeing it before. In any case the 1st 2 links are descriptions of 2006 Phase III trails of lacosamide which look promising for treatment of pain associated w/diabetic PN.

http://www.medscape.com/viewarticle/546044

http://www.docguide.com/news/content...2573470065259A

The next link is to a Phase III study which predates the above work but also showed promising results.

http://www.bioportfolio.com/aug_05/2...sitive_in.html

This last link may be way too much info and an info overload but it appears to be a detailed and complete, recent (2007) summary of the PRECLINICAL pharmacology of lacosamide and a very detailed and complete description of the biochemistry of neuropathic pain - VERY COMPLEX as we all know. Lacosamide seems to have a novel mechanism of action for an anticonvulsant or antiepileptic drug (AED), at least as much as is understood.

I haven't digested this paper in its entirety but a VERY BRIEF paraphrase would be that a key aspect of lacosamide seems to be that it has a dual mode of action as an analgesic and as anticonvulsant. In particular, it enhances slow inactivation of voltage-gated sodium channels but it does not affect fast inactivation. The significance of the selectivity seems to be that slow inactivation of these sodium channels is a critical component in the pathophysiology of epilepsy and neuropathic pain both of which exhibit hyperexcitability of neurons with a lower activation threshold and/or an exaggerated neuronal response. The mechanism of hyperexcitability is still not well understood in the scientific community and certainly not by me.

http://www.bioportfolio.com/aug_05/2...sitive_in.html

There were AE''s (Adverse Events or side affects) associated w/ the treatment but overall the 400mg dose seemed to combine the best efficacy w/ the fewest side affects and the fewest number of patients opting out of the trials due to the SE's.

Maybe worthwhile to add to the burgeoning database.

Alkymst
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