Flupirtine — Another Potassium Channel Opener

Very interesting. Have you tried it yet? Is there any more information on the backside of the package? What is the brand of the medicine? Apparently Flupirtine is often used in combination with Paracetamol because of its pain-killing properties, so it could be legit. Maybe you could contact your GP about it? Looking forward to hearing from you.

 

I don't think my GP will do anything as it is off the market in Europe. That is a photo of the medicine that a friend of mine from Pakistan sent to me. It can be found there and in India. As far as I know, no prescription is required over there. But I didn't see this kind of Flupirtine mentioned here, this one in combination with Paracetamol. So I was wondering if it would have the same effects.

I will try to find a prescription for it. But I don't know if a prescription from Europe would be accepted at the border. My friend can send it to me without problems as it is free of prescription over there, but what if they stopped it at the border on the way to me? I will probably need to call the border center in my country? I just thought of that.

 

As far as I know, the mechanism of action of the drug, the modulation of Kv7 channels, is not affected by it being taken together with Paracetamol. So for tinnitus it should not make a difference. But it is still a good idea to ask your GP for medical advice since Flupirtine is a pretty dangerous drug.

As far as I know, doctors in Europe cannot prescribe medicine that is off the market. There is a good possibility the medicine will be seized by customs. I would not call the border center but do my own research instead. How expensive is a strip? If it's not too high it might be worth risking it.

 

So I can't take it then? It's around $1 dollar for one packet. I would need a doctor from India to prescribe it for me? This medicine can be bought without prescription over there. I'm thinking if it can put me in legal trouble here in Romania? But it is not a "drug"... I really don't know what to say anymore.

 

Your friend can send it from Pakistan but there is a possibility it will be seized by customs. There is a risk you will lose your package and the money you spend on it, but as far as I know, you won't get into legal trouble. Prescriptions are useless in this case, don't bother.

You live in Romania, I'd suggest to investigate if you can get these capsules without prescription in neighboring non-EU countries (maybe Serbia?) and maybe drive there yourself. You can also have your friend send them to acquaintances in these countries if that is a possibility. Customs in these countries might be more lax.

 

Thank you for your advice! Are you saying the problem would be more with the country where the medicine is coming from?

Because no matter what country it comes from, I think it can be stopped at my border, not necessarily dependent on where it is coming from.

And if I drive there, they will control my packages as well at the border.

 

@Ela Stefan and @StoneInFocus, I found an online pharmacy where Flupirtine is available in generic form. When you go to purchase it, they take you through the KYC (Know Your Client) policy. But it requires you to provide proof-of-identification, like a driver’s license picture. They do that, they say, to prevent identity theft. It’s supposedly a policy that was put into law to protect businesses or organizations. Have you heard of that before? I was just curious and trying to figure out if it’s safe. Don’t want to get scammed. Thanks.

 

Never heard about that really. But there can be things like that I guess. My problem is the border control here!

 

Literally never heard of having to provide proof of identification for online shopping for the purpose of preventing identity theft. How does that even make sense? Did you find any online reviews from this company?

No, I didn't really specify which customs would intercept the package, but I meant the Romanian ones. The problem is getting the package across the Romanian border.

In that case, I'd just request your friend to send some of the stuff from Pakistan. Worst case scenario, you waste a couple of bucks. I would also suggest to ask your friend if he can find a couple packs of Flupirtine without paracetamol to spare your liver. But it's best to call a doctor about possible health risks of this medicine.

 

Ya, I don’t know what to make of it. They say that they want to prevent drug dealers from being involved. The “Know Your Client” policy enables them to verify someone’s identity and prevent stuff like that, supposedly. But I don’t know if it’s legit and I don’t want to get scammed. I know it’s used for cryptocurrency banking, but not sure if pharmacies do, too. So not sure whether it’s safe. I tried to research the company and verify all this, but wasn’t having much luck — is there a way to know for sure? It’s messed-up that people like us and @Ela Stefan have to resort to such extremes to find solutions to our problems. Not sure if it’s a risk that’s wise to take, but we’re left in the dark because our situations are so rare. Like animals put out to pasture, we feel written-off; overall, medical community doesn’t have our backs with these conditions.

 

I'm afraid to get into legal trouble because of it. That's my worry. Could that be possible since Flupirtine is not allowed in the market here?

 

It's not like Flupirtine is heroin or cocaine. If the border control confiscates it, they will most likely just throw it away. You don't go to jail for that. Maybe you can get a small fine, but likely not. You can plead ignorance when it's your first time ordering something like that online.

 

It is important to note that Flupirtine is not legal in the U.S. I doubt the kind of pharmacy that asks for identification is the kind of pharmacy to smuggle Flupirtine across a border. It's most likely a scam.

At the moment I am eyeballing some Flupirtine sellers from an online Indian marketplace. I have contacted about six of them now, they mostly ask shipping fees between 30 and 40 bucks, so it would be a shame if my package would be intercepted (although it is not too big of deal of course). If I can strike a good deal with one of these people I'll let you guys know.

 

UPDATE:

After contacting a lot of scammers I've found a seller who seems somewhat reliable, but after doing some research I am pretty pessimistic about the possibility of the package getting though my country's (EU) customs.

The new small-value regulations from July last year probably won't help either. If we as Westerners want to try this, we have to start thinking about different methods to acquire this medication.

I am seriously considering traveling to India or some other country for a couple weeks just to try it out locally.

I could not find any information on the status of Flupirtine in Switzerland.

Maybe someone on here knows?

Thanks.

EDIT #1:

I found out Flupirtine is not legal in Switzerland, so that is not an option.

Another possibility is smuggling the medication from a non-EU country into the Schengen zone.

Maybe if you could drive up to the border of some Eastern European country and cross the border on foot, you could get the medication relatively risk free.

What a tinnitus & hyperacusis sufferer has to do just for a possible treatment...

EDIT #2:

Again did some research on acquiring flupirtine.

The only countries that seem to stock flupirtine are India and Pakistan (thanks to @Ela Stefan's suggestion).

I don't think smuggling the stuff into the airplane back to the EU is a foolproof idea, so if we want to acquire the stuff from these countries we need to use it locally for a couple of weeks or more.

Now, I don't know about you guys but I am not overly excited to spend an extended amount of time in these countries. Maybe it is possible to spend a month in a resort somewhere? Very cumbersome indeed, but, if it would cure my hyperacusis and provide significant relief for my tinnitus, it would totally be worth it. If we would want to do something like this we would have to do it in the next couple of months before COVID-19 makes a return again in the autumn.

I've checked Russia and Turkey, maybe drive into the Kalingrad Oblast region, but it is illegal in these countries. My initial idea was to drive to Bosnia and Herzegovina, because crossing their border is relatively easy and you do not need a visa, but I found out Flupirtine is not registered there. The medication policies of Serbia, Montenegro, Kosovo and Albania probably conform to EU legislation, pharmacies very likely won't sell it. That means acquiring Flupirtine from a local pharmacy in Europe is likely not possible.

Then we are back to the option of shipping it from India.

It's a bit of a risk, we can get scammed, the package can be intercepted, no guarantee we get anything at all etc.

I am still on the fence about ordering it.

Another possibility (in my country at least) is that a doctor who knows you requests a special permission from the government to import this unauthorized medication.
It's a bit of long shot, but I will discuss this option with my GP.

Last possible option I can think of is somehow ordering the stuff on the dark web. I have absolutely no experience on that though.

If anyone knows another solution, let me know.

 

According to this article, "between April 2013 and December 2017, cases of serious liver injury (total numbers not specified), including 23 cases of acute liver failure after flupirtine use, have been reported in the European database of suspected adverse drug reaction reports (EudraVigilance). The incidence of liver injury in clinical practice is not obvious from the recommendation report. The incidence of flupirtine-related hepatobiliary adverse events in the German Federal Institute for Drugs and Medical Devices database was estimated in 2011 to be about 8 in 100,000 patients (>0.01%)."

So I really wouldn't compare taking the drug with playing Russian roulette, as the risk of dying from Russian roulette is more than a thousand times greater than the percentage of people experiencing flupirtine-related hepatobiliary adverse events.

The article also mentions that "N-acetylcysteine [which is freely available as a supplement] is an essential building block for the replenishment of depleted glutathione stores and when administered intravenously for 7 days replenishes glutathione stores and resolved severe flupirtine-induced liver injury. By regular hepatic monitoring during flupirtine treatment and when applicable, inclusion of N-acetylcysteine [NAC] in the treatment regime would reduce the appearance of this already rare adverse event and avoid cases of liver failure.

So the chance of seriously damaging our liver when taking appropriate measures is practically nothing. We most likely need to be taking this medication for only a couple of months, while your first article suggests flupirtine is actually "safe when given for a period of one year.".

 

Wish I could get a hold of Flupirtine here in the US somehow.

 

Honestly the liver damage potential just makes this a non starter especially with Xenon on the horizon.

Flupirtine opens Kv7.2 which doesn't seem to do much for tinnitus. Barely touched Kv7.1 which Trobalt did and is what Xenon is working on making safer, currently in Phase 2b I believe. The original formula will also be out in a different form for infants with seizures that don't primarily respond to GABA drugs.

 

When you stop taking Flupirtine, will tinnitus not come back? Or can you take it for a long time by taking breaks?

 

Sorry but that sounds like total bollocks.

"Flupirtine exhibits efficacy on all four subunits, Kv7.2, Kv7.3, Kv7.4 and Kv7.5, with an apparent preference for Kv7.3... Reduction in Kv7.2 and Kv7.3 channel activity leading to hyperactivity in the dorsal cochlear nucleus (an auditory brainstem nucleus) has been associated with the initiation of the auditory disorder tinnitus. Flupirtine inhibited the spontaneous activity in mouse auditory cortical networks which was suggested to involve Kv7 channel activation[93]. These findings are consistent with the pharmacological properties of flupirtine being relevant to the treatment of tinnitus."

Lawson K. Pharmacology and clinical applications of flupirtine: Current and future options. World J Pharmacology 2019; 8(1): 1-13 [DOI: 10.5497/wjp.v8.i1.1]​

Also, I don't know if you are talking about Xen-1101 but that drug does not show activity on the Kv7.1 channel.

https://www.xenon-pharma.com/wp-con...ilepsyFoundationPresentation_February2018.pdf

That's your opinion, everyone should decide for themselves if they want to take the risk. I've argued in my previous post that the danger for liver damage is almost nil. Plus, waiting a couple years for a potential tinnitus treatment seems like a huge leap of faith to me. Especially to someone with debilitating tinnitus & hyperacusis such as me.

Honestly I don't know the answer to that question. My suspicion is that taking the drug for a couple of months (I'm thinking 400 mg a day) will definitely lower the perceived volume of the tinnitus even after we stop taking the drug, at least for a while. But when our tinnitus spikes we might have to take it again for some time. What we are going to do is totally experimental, we are pioneering a DIY treatment course for tinnitus.

 

Update:

I've received the package with 100 Flupirtine capsules in my mailbox. Thank God. Tomorrow I am going to contact a doctor for advice and guidance on taking it. Specifically, I want to know how much N-Acetylcysteine I should take during the treatment, if it's safe to take 400 mg at once, and if he is willing to regularly check my blood for elated liver enzymes.

I've found a package leaflet of Flupirtine online (see attachment). I am a bit worried about how the more common side effects like sleep problems, loss of appetite, headaches etc. will affect my general well being and mood. I am going to try extra hard to get my general health to the best level possible.

 

Please keep us updated! God be with you!

 

I think I'll treat the background I have and my own research as trumping your wall of text on the subject.

One PDF you definitely didn't take the time to digest doesn't really mean much...

I've kinda obsessed about it as this is obviously hell to deal with. But I would rather not end up dead like some members here have from things getting worse or sudden death.

Good luck with Flupirtine. I hope it doesn't fuck you up.

It's XEN-496 FYI which will supercede Trobalt for pediatrics (XEN-1101 has an added methyl group to protect against reactivity).

No, Flupirtine is not the same thing.

I'd just wait for the less toxic, better binding version.

 

What is your background then? You don't think the sources I quoted are reliable? If you really think the few sentences I posted are a "wall of text", I'm really skeptical you've done any research at all. You're free to disagree with what I said but at least back it up with some sources.

You're being so dramatic.

You still have not responded to my argument that Flupirtine induced liver damage is totally preventable by taking the right measures. Have you even read what I wrote?

Don't know if you are implying Danny Boy (rest in peace) died from taking Retigabine, but that is total speculation. So don't use that example in your argument.

Never said it was.

Great, do you have any sources whatsoever to prove that XEN-496 is any less toxic than Flupirtine?

If you want to wait years on an anticonvulsant drug that may or may not be granted market authorization, be my guest. In my opinion, you're totally out of your mind if you really think that is the best option for tinnitus sufferers right now. The earlier you start treating your tinnitus with this type of medication, the better your chances of recovery are. Time is not in our favor here. You'll never know what is going to happen.

 

Is Flupirtine a good option for tinnitus? Why is there not more people talking about it?

 

Yah I do have sources, but I have better things to do than argue with a buffoon attempting to cross examine me on a forum right now.

I'll use whatever speculation I wish, the truth is you cannot guarantee less toxicity by supplementing with something else when you don't even know the MECHANISM of toxicity. I rushed treatment based on "free information" where I knew just enough to hurt myself and was simply keeping you from doing the same.

Time is on your side when it comes to risk taking, and that argument goes against a ton of people who recovered over the 2 year span, doing basically nothing but protecting. Unless there's something underlying (which no Kv drug will fix) that's also blatant speculation that time is "not on your side" whatever that vague ass statement means.

Peace.

 

That's what I thought. You're just talking out of your bum then. You have zero valid counterarguments so that is why you resort to name-calling. Absolutely zero points of the other things you've said make sense, so I'm not going to bother to respond to them.

If you really cared about the safety of the people on here, you'd at least take the time to the research the subject and post some reliable sources of information about this medicine. You're a scaremonger who contributes nothing of value to this thread except for eliciting a response from me.

So anyway, yesterday I've taken 200 mg Flupirtine, and today 400 mg, both at once. I'm not going to write an elaborate experience report about it now, but I'm pretty enthusiastic so far. I've also ordered some N-acetyl-L-cysteine which I hope to receive soon. The doctor has not responded to my email yet. I will give a detailed update in the next days.

 

It's in most countries not available anymore. Interestingly I found some entry in a German medical forum where someone is asking for an alternative for Flupirtine as he was using it for years for treating his tinnitus.

Flupirtin gibt es nicht mehr?

On ClinicalTrials.gov there are just 3 studies for Flupirtine but none of them tinnitus related.

 

Because some of us still have jobs with workplace accommodations to work through tinnitus and hyperacusis, so no... I can't be bothered arguing with a fool going to possibly kill himself... I have money to make instead at 9am.

"That's what you thought", not a surprise it's wrong.

Hope your enthusiasm isn't placebo.

And again, NAC isn't going to magically save your liver if there's another toxicity mechanism other than glutathione deficiency (which could be limited by enzymes as the rate limiting step).

I'll say it again. You think you know what you're doing just enough to hurt yourself. Experience trumps a guy who's barely scientifically literate reading random "free" journals.

 

You"can't be bothered" arguing with me yet you continue to engage with me . Mr. money-making big shot. If you would truly be unbothered you'd shut your mouth and get back to work then. You are 32 years old pretending to be an expert online. Reading forum posts on Tinnitus Talk does not count as expertise. I've argued with people before on this website but at least they came with some solid arguments. You still have not disproven anything I said.

I have no interest in engaging with you further because you have absolutely zero value to contribute to the discussion. If you want to respond to me because you have a fragile ego and want to have the last word, be my guest. But I'm not going to take anything you write seriously (and I hope no one else does as well) just because you claim to have a "background", whatever that means. Again, if you'd care about anyone's safety you would actually post some information then. But you are only interested in arguing for the sake of it.

 

Interesting to note that some people have seen benefit to their tinnitus from taking NAC by itself... though I've tried it at very high doses with no effect. Curious if it will affect your tinnitus along with Flupirtine.

Looking forward to your updates @StoneInFocus, praying for success.