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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 8 of 8. This is the beginning of the thread.
Posted by Quintal on October 9, 2007, at 16:38:23
Hey, I just saw this new anticonvulsant on the market! I've been wondering for a while if I should be on a mood stabilizer or something like that, both for my moods and impulse control. Lamictal was okay, but I got rashes on every occasion, and the last time I felt so sick I had to come off it. I've never heard of it before, and information is scant. Does anyone know more about it?
http://en.wikipedia.org/wiki/Rufinamide
Posted by Netch on October 9, 2007, at 18:08:37
In reply to Inovelon, posted by Quintal on October 9, 2007, at 16:38:23
Interesting... found this:
"Synosia Therapeutics today announced that it has signed an exclusive, worldwide licensing agreement (outside of Japan) with Novartis Pharma AG to develop and commercialise rufinamide for the treatment of anxiety disorders and bipolar mood disorders."
"Rufinamide was discovered and developed by Novartis, which granted certain licensing rights to Eisai of Japan in 2004. On January 16, 2007, Inovelon® (rufinamide) received marketing authorisation in the European Union as adjunctive therapy in Lennox-Gastaut Syndrome (LGS),a severe form of epilepsy that develops in early childhood. Eisai has also submitted an NDA for rufinamide to the US Food and Drug Administration (FDA) in November 2005 for adjunctive therapy in adults and adolescents (12 years of age and over). It received orphan drug status for LGS in October 2004. "
Posted by Phillipa on October 9, 2007, at 18:14:15
In reply to Re: Inovelon, posted by Netch on October 9, 2007, at 18:08:37
So the US is getting it? Will read whole article in a bit. Phillipa
Posted by Netch on October 9, 2007, at 19:11:04
In reply to Inovelon, posted by Quintal on October 9, 2007, at 16:38:23
"Rufinamide [1-(2,6-difluorophenyl)methyl-1H-1,2,3-triazole-4-carboxamide; E 2080, CGP 33101, RUF 331] is triazole (3 nitrogens in a 5-membered ring) compound that bears some structural similarity with lamotrigine, a triazine (3 nitrogens in a 6-membered ring). Rufinamide is effective in the mouse MES test (ED50, 15.5 mg/kg, i.p.) and at higher doses is the PTZ test (54 mg/kg) (Schmutz et al., 1993; White et al., 2005). It is ineffective against absence-like seizures in WAG/Rij rats. The drug has a very low propensity for toxicity in the rotorod test (TD50, >500 mg/kg, i.p.). Overall, rufinamide has a distinctive profile in animal testing—activity in both MES and PTZ models and a very high protective index—that differentiates it from marketed AEDs. The efficacy of rufinamide in the MES test is compatible with sodium-channel blocking activity. In fact, the drug has been reported to prolong the inactivation of sodium channels and to limit the frequency of action potential firing in cultured and acutely isolated neurons (Karolchyk and Schmidt, 2002; McLean et al., 2005). In other studies, there were no effects on sodium channels at the concentrations tested (Vickery et al., 2004). In view of its unique profile, it seems unlikely that effects on sodium channels entirely explain the anticonvulsant activity of rufinamide. To date, no alternative mechanisms have emerged: there is no evidence for interactions with GABA or glutamate systems."
http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=1562526
"protective index of rufinamide, as shown in rodent models of epilepsy, is much higher than that of most common AEDs. Features which make it a desirable AED are: (i) a broad spectrum of anti-epileptic actions including both partial and symptomatic generalised epilepsy; (ii) a statistically significant reduction in seizure frequency in clinical trials; (iii) efficacy and safety shown in a broad range of age groups including children and the elderly; (iv) rapid oral absorption enabling quick titration to effective dose and (v) a benign adverse event profile. Most of the events did not lead to discontinuation in clinical trials. These features offer considerable advantages over the existing anti-epileptic drugs."http://www.ingentaconnect.com/content/apl/eid/2000/00000009/00000004/art00014
Posted by Quintal on October 9, 2007, at 23:59:12
In reply to Re: Inovelon, posted by Netch on October 9, 2007, at 19:11:04
Interesting and mysterious. Thank you very much Netch.
Q
Posted by James_glasgow on October 12, 2007, at 11:55:04
In reply to Re: Inovelon » Netch, posted by Quintal on October 9, 2007, at 23:59:12
Hi Qunital
I would personally hold off on this for mood stablisation at the moment. As you can see from the wiki it was discovered in 2004, which as I am sure you will be well aware from the lab to the market usually takes 10+years, that was my main concern when I read about it. It appeared in the new product section of the pharmaceutical journal (www.pharmj.com) about 2 weeks ago which prompted me to take a closer look at it.
I know everyone is different but personally I find lithium to be practically miraculous, it works in about 5 days bringing me right down to the ground and thats with a blood level of 0.5 mmol/l.
James
Posted by Netch on October 12, 2007, at 12:00:00
In reply to Re: Inovelon, posted by James_glasgow on October 12, 2007, at 11:55:04
> Hi Qunital
>
> I would personally hold off on this for mood stablisation at the moment. As you can see from the wiki it was discovered in 2004, which as I am sure you will be well aware from the lab to the market usually takes 10+years, that was my main concern when I read about it. It appeared in the new product section of the pharmaceutical journal (www.pharmj.com) about 2 weeks ago which prompted me to take a closer look at it.
>
> I know everyone is different but personally I find lithium to be practically miraculous, it works in about 5 days bringing me right down to the ground and thats with a blood level of 0.5 mmol/l.
>
> James
James, how much elemental lithium do you take per day?/Netch
Posted by James_glasgow on October 13, 2007, at 3:26:24
In reply to Re: Inovelon » James_glasgow, posted by Netch on October 12, 2007, at 12:00:00
I take 13.5 mmol of Li+ once a day in the form of a sustained realise tablet marketed in the UK as Priadel, the dose of Pridael is 500mg of lithium carbonate at night. I am a relatively small person (weight about 58kg) which is why I seem to get a higher blood level at that dose than most. At 600mg I get a level of 0.7mmol/l.
James
This is the end of the thread.
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