Flupirtine — Another Potassium Channel Opener

[StoneInFocus]

I have a GABA issue due to Fluoroquinolone intoxication + Mirtazapine messing up with my Serotonin causing my tinnitus and hyperacusis along with TTTS. It has improved so much from the beginning but the progression stopped and it's been like this for months. My ex-girlfriend, who is in Thailand, was able to get Flupirtine for me from India, she will bring it when she visits me next month or so, but I'm scared to take it in my current state, since Flupirtine can also mess with GABA receptors and I unfortunately got some visual snow due to being on Mirtazapine. I'll keep it just in case I can't take the noise anymore. I'm actually looking forward to BHV-7000 more since it doesn't have much GABA affinity...

I have the same pills.

On the package it says "Lupin Ltd." I don't know if the pills are legitimately from that company. Maybe I will contact the actual company at lupin.com to ask whether they still manufacture Flupirtine.

Wish I could give you some advice about your situation.

Mirtazapine sounds like a drug from hell.

 

[StoneInFocus]

It took some time but I'm officially a fan of Flupirtine now. I think I have a much clearer picture now of what flupirtine does to me. 2 pills have an immediate antidepressant effect for me. You just stop caring as much about what tinnitus & hyperacusis means for your life.

2 Flupirtine pills in the morning and in the evening seems to improve my hyperacusis overall.

Recently I've been mixing 25 mg Cinnarizine, 100 mg Flupirtine and about 1 gram of Vitamin C on an empty stomach in the morning and in the evening. The combo definitely seems to take the edge of my voice-induced hyperacusis pain. This morning I was feeling so down, took this combo and feel so much more optimistic and determined to find a solution.

I will probably add Magnesium to this combo soon.

I'm not entirely sure how doable this combo is in the long term. The main two issues are the limited availability of Flupirtine in Western countries and the possible dangers of Cinnarizine-induced Parkinsonism.

In any case this discovery might provide valuable information in the search for pharmacological treatments for hyperacusis.

I personally want to get a doctor involved with whom I can discuss possible drug combinations. If anyone knows a doctor who does online consultations and is willing to try a more experimental approach in regards to medication, please let me know.

Hoping we can get this polypharmacy ball rolling.

 

[BB23]

It took some time but I'm officially a fan of Flupirtine now. I think I have a much clearer picture now of what flupirtine does to me. 2 pills have an immediate antidepressant effect for me. You just stop caring as much about what tinnitus & hyperacusis means for your life.

2 Flupirtine pills in the morning and in the evening seems to improve my hyperacusis overall.

Recently I've been mixing 25 mg Cinnarizine, 100 mg Flupirtine and about 1 gram of Vitamin C on an empty stomach in the morning and in the evening. The combo definitely seems to take the edge of my voice-induced hyperacusis pain. This morning I was feeling so down, took this combo and feel so much more optimistic and determined to find a solution.

I will probably add Magnesium to this combo soon.

I'm not entirely sure how doable this combo is in the long term. The main two issues are the limited availability of Flupirtine in Western countries and the possible dangers of Cinnarizine-induced Parkinsonism.

In any case this discovery might provide valuable information in the search for pharmacological treatments for hyperacusis.

I personally want to get a doctor involved with whom I can discuss possible drug combinations. If anyone knows a doctor who does online consultations and is willing to try a more experimental approach in regards to medication, please let me know.

Hoping we can get this polypharmacy ball rolling.

Did it bring down your tinnitus as well? Or did it stay the same overall?

 

[StoneInFocus]

Did it bring down your tinnitus as well? Or did it stay the same overall?

I have not noticed much effect on tinnitus volume.

 

[StoneInFocus]

Co-administration of Cinnarizine with Flupirtine counteracts the disinhibitory, dare I say manic effects of the latter on my psyche.

 

[BB23]

Co-administration of Cinnarizine with Flupirtine counteracts the disinhibitory, dare I say manic effects of the latter on my psyche.

Any more updates my man? Still no reduction in volume? Does it help with the pain only or does it also take away hyperacusis as well?

Any permanent positive effects?

Do you think the medication is habit forming, can it lead to withdrawals? Do you think the manic effects are because of its GABA activity or something else?

I have my pills on hand ready as well, but scared to take them...

 

[StoneInFocus]

Any more updates my man? Still no reduction in volume? Does it help with the pain only or does it also take away hyperacusis as well?

Any permanent positive effects?

Do you think the medication is habit forming, can it lead to withdrawals? Do you think the manic effects are because of its GABA activity or something else?

I have my pills on hand ready as well, but scared to take them...

A while ago I took 400 mg elemental Magnesium + Vitamin C 1 g + 200 mg Flupirtine + 50 mg Cinnarizine. Loved how that combo made me feel. I think it helped with the pain and discomfort too. I don't know what your definition of 'hyperacusis' is.

I only take Flupirtine sporadically, until I can find a reliable source that is not too expensive. I don't think occasional usage is sufficient to achieve permanent positive effects.

I think the manic effects are due to its NMDA receptor antagonism and its positive allosteric modulation of the GABAa receptor.

Considering your addiction questions, I'd friendly suggest to do your own research.

The NO/ONOO cycle theory is a game changer for me. Looking for ways to incorporate it in a more concrete treatment strategy. Read the thread and the papers if you have not already.

 

[AverageJoe12]

It took some time but I'm officially a fan of Flupirtine now. I think I have a much clearer picture now of what flupirtine does to me. 2 pills have an immediate antidepressant effect for me. You just stop caring as much about what tinnitus & hyperacusis means for your life.

2 Flupirtine pills in the morning and in the evening seems to improve my hyperacusis overall.

Recently I've been mixing 25 mg Cinnarizine, 100 mg Flupirtine and about 1 gram of Vitamin C on an empty stomach in the morning and in the evening. The combo definitely seems to take the edge of my voice-induced hyperacusis pain. This morning I was feeling so down, took this combo and feel so much more optimistic and determined to find a solution.

I will probably add Magnesium to this combo soon.

I'm not entirely sure how doable this combo is in the long term. The main two issues are the limited availability of Flupirtine in Western countries and the possible dangers of Cinnarizine-induced Parkinsonism.

In any case this discovery might provide valuable information in the search for pharmacological treatments for hyperacusis.

I personally want to get a doctor involved with whom I can discuss possible drug combinations. If anyone knows a doctor who does online consultations and is willing to try a more experimental approach in regards to medication, please let me know.

Hoping we can get this polypharmacy ball rolling.

Where are you based? Naturopathic doctors in many western US states can prescribe medications and have worked with me on off label treatments for my anxiety. There are also very interesting integrative psychiatrists that are big on polypharmacy, I'm just yet to consult with them specifically for my tinnitus/hyperacusis. But I have the angle now, specifically when talking to my psychiatrist in the new year. 0.5 mg of Clonazepam last night and 22.5 mg Mirtazapine eliminated my hyperacusis overnight. Temporarily I'm sure, but whatever mechanism of action those two drugs have, I need more of it to have any hope of re-gaining a sense of normalcy.

 

[gameover]

0.5 mg of Clonazepam last night and 22.5 mg Mirtazapine eliminated my hyperacusis overnight. Temporarily I'm sure, but whatever mechanism of action those two drugs have, I need more of it to have any hope of re-gaining a sense of normalcy.

Loudness hyperacusis?

 

[AverageJoe12]

Loudness hyperacusis?

Both pain and loudness. Less pain since I've withdrawn from most prior activities. Now mostly just bothersome, intense discomfort from everyday sounds in the house.

 

[BB23]

I believe the TTTS bothers me more than the tinnitus and is the source of my hyperacusis.

I remembered that Flupirtine has muscle relaxant properties that Retigabine didn't have, at least to my knowledge.

While searching for the reason, this paper popped up:

Muscle relaxant action
The muscle relaxation is due to inhibition of both mono- and polysynaptic reflexes. The spinal polysynaptic flexor reflex, mediated by NMDA receptors, was depressed by flupirtine, whereas the monosynaptic Hoffmann reflex (H-reflex), mediated by non-NMDA receptors, was not influenced.

Also:

It has been found that flupirtine also antagonizes both glutamate and NMDA induced increase in intracellular levels of Ca++, as observed in in vitro cultures of cortical and hippocampal neurons.

Sounds similar to Magnesium, when it comes to muscle relaxant properties.

I wonder if Flupirtine could bring relief to TTTS.

I don't think XEN1101 will have this action, as it is only "supposed" to work on Kv7 channels.

Duck TTTS!

 

[StoneInFocus]

I believe the TTTS bothers me more than the tinnitus and is the source of my hyperacusis.

I remembered that Flupirtine has muscle relaxant properties that Retigabine didn't have, at least to my knowledge.

While searching for the reason, this paper popped up:

Also:

Sounds similar to Magnesium, when it comes to muscle relaxant properties.

I wonder if Flupirtine could bring relief to TTTS.

I don't think XEN1101 will have this action, as it is only "supposed" to work on Kv7 channels.

Duck TTTS!

Also, Flupirtine has in all likelihood a greater affinity for Kv7.4 channels than XEN1101:

Flupirtine exhibits efficacy on all four subunits, Kv7.2, Kv7.3, Kv7.4 and Kv7.5, with an apparent preference for Kv7.3.

(Source)

In my opinion, it was a great mistake of Dirk de Ridder to use only 2 x 100 mg of Flupirtine in his trial for the treatment of tinnitus.

Does anyone else think that was just plain idiotic, and he should have used higher doses?

By the way, do you still have some Flupirtine pills lying around?

 

[BB23]

Also, Flupirtine has in all likelihood a greater affinity for Kv7.4 channels than XEN1101:

(Source)

In my opinion, it was a great mistake of Dirk de Ridder to use only 2 x 100 mg of Flupirtine in his trial for the treatment of tinnitus.

Does anyone else think that was just plain idiotic, and he should have used higher doses?

By the way, do you still have some Flupirtine pills lying around?

In one of my posts, I attached a paper noting that Retigabine also had a preference for Kv7.3. It's no surprise since it was derived from flupirtine originally.

I have a hundred Flupirtine pills. I'm fraid to touch them because of my kindled brain and ongoing insomnia issues. If my insomnia improves a bit, I intend to take a few pills.

As for the muscle relaxant properties of Kv7 openers, this paper states just the opening of the channels inhibits the intracellular Ca++ release, meaning that they still might bring relief to TTTS. I'll try to find that paper again.

What's even more idiotic is that nobody is testing XEN1101, Retigabine, or some other potassium channel opener on tinnitus patients. We are going to be the guinea pigs when they come out.

 

[BB23]

I haven't been sleeping for the past two days at all.

Today's my birthday. If I die today, I want to die knowing that there is hope on the horizon for us.

So, I decided to pop two capsules of Flupirtine (200 mg).

Absolutely nothing happened other than mild numbing of the roof of my mouth and tongue. There was no effect on my TTTS either.

The side effects were nausea, a slight dizziness for a few minutes, and numbing of the limbs for less than a minute after some time.

I believe the reduction in tinnitus reported by some individuals may have been due to a placebo effect, as Flupirtine has a slight relaxing effect.

Anyway, that's it. No amount of paper sharing will get us rid of it. Good luck with potassium channel openers.

 

[StoneInFocus]

I haven't been sleeping for the past two days at all.

Today's my birthday. If I die today, I want to die knowing that there is hope on the horizon for us.

So, I decided to pop two capsules of Flupirtine (200 mg).

Absolutely nothing happened other than mild numbing of the roof of my mouth and tongue. There was no effect on my TTTS either.

The side effects were nausea, a slight dizziness for a few minutes, and numbing of the limbs for less than a minute after some time.

I believe the reduction in tinnitus reported by some individuals may have been due to a placebo effect, as Flupirtine has a slight relaxing effect.

Anyway, that's it. No amount of paper sharing will get us rid of it. Good luck with potassium channel openers.

Two pills on just one day won't do shit. If you really want to test it out, you have to start low and build the dose up.

Why not try Gabapentin, by the way?

 

[2noist]

Why not try Gabapentin, by the way?

I find that so perplexing. @BB23 is apparently ready to throw in the towel and be placed six feet under, so why be scared of trying anything and everything?

I would rather have tried everything before I call it quits, I wouldn't mind the potential risks and side effects at that point.

 

[BB23]

Two pills on just one day won't do shit. If you really want to test it out, you have to start low and build the dose up.

Why not try Gabapentin, by the way?

I don't want to risk taking Flupirtine long-term yet, and no, I'm scared of Gabapentin, due to it reportedly being ototoxic and making visual symptoms worse for some people.

I was hopeful about Flupirtine since a couple of users reported positive results just with one dose, but oh well.

I'm considering Clonazepam since my sleep is totally gone. I'll see if it helps with my visual symptoms as well. I will consider other stuff after a benzodiazepine. I hope I don't get like @Travis Henry.