Pirenzepine
 

Hi all,

Can any longer term members remember posts from a member who was self-trialing Pirenzepine for a short period of time?

I distinctly remember her(?) describing the ongoing sensations, but then she ended the trial.

Or am I mis-remembering?

Thank you!

Paul

Are you going to give it a try?seems to be a harmless drug other than stomach discomfort

The results of this technical rodent model study look encouraging.

Selective antagonism of muscarinic receptors is neuroprotective in peripheral neuropathy

"Are you going to give it a try?seems to be a harmless drug other than stomach discomfort"

I thought a bit about it, but I've heard that oral administration has proved an ineffective route. The focus of the trials is on topical administration because of this and because of safety issues. Of course, it's early very, very early days.

I also worry about potential side-effects (I actually have colitis, but have also heard of possible concerns regarding dementia, though haven't read anything to this fact).

I believe that research will be coming out in a few months regarding early trials of the topical lotion. It's a long-shot. But at least it is something.

Cheers
Paul

Topical cream was made to mainly combat the side effects from pills.The studies that i have read says that oral is effective as topical

Hi Liqidz--are you sure about that? If you have any links to abstracts of articles I would be very interested.

Cheers
Paul

When do they expect the early trial results to be published? Does anyone know how to be included in the clinical trials?

Results of pilot trial to be published in the next few months.

Phase 2 human trials are currently taking place on human subjects:


Pipeline - WinSanTor

Current focus is on diabetic PN, with an intent to move to chemo- and HIV-related.

Here are the complete studies that they have ever done i think compiled into this pdf.
Just click on ''download PDF'' and you'll be able to see it.
If you do a key word search on oral within the pdf,you'll be able to see that it is effective

US2�19��4654�A1 - Treatments for diabetic symmetrical polyneuropathy
- Google Patents




Also i spoke to someone on reddit which stated that they were working on a topical drug for neuropathy which is going really well,didn't state which company or cream ,but pretty obvious :P

We are two scientists and we are walking into a bar AMA! : IAmA

Two very encouraging quotes from "We are two scientists and we are walking into a bar AMA! : IAmA" link above

"I'm currently working on a topical drug specifically targeting small fiber neuropathy. We are in phase II clinical trials and it's going really, really well. It's a topical drug that should really help with basically no side effects"

"We think our cure works regardless of the etiology behind the neuropathy, but there are some exceptions to this rule"

That's an interesting find!

Thanks a bunch, Liquidz. My pdf app is only a reader so I can't search specifically for "oral," but I intend to skim these readings as soon as I get a chance.

Is Pirenzepine available in the united states ? None of the pharmacies seem to know about it. If one could get Pirenzepine from another source does any one know where directions could be found to compound it into a cream ? I found a pharmacy that offered to compound oxybutynin (another drug in the Pirenzepine family) into a trans dermal cream but does anyone think a pharmacies compounded oxybutynin cream would actually work. I'm currently taking the oral version of oxybutynin and it seems to be having a positive effect on my Peripheral neuropathy but oral has a lot more side effects. But I would like to try the trans dermal cream version of Pirenzepine as it would be going directly to the nerve endings in my hands .
Thanks for any and all help on this subject.

You should be looking for Oxytrol. It is a transdermal patch used for bladder spasms. I am trying it right now with interesting results. I have less numbness / improved sensation in numb area of feet, more skin wrinkling in water with my hands ( improvement in autonomic neuropathy), more tingling in neuropathic areas (maybe Tinel's sign for regenerating axons).

It is a bit of a mixed bag though because I still experience stinging pains and the electrical pains. However, I just read a paper that said that these pains occur with regenerating axons because of changes in the number of sodium channels. The issue appears that continuous neuropathic pain is an ongoing regeneration process that never succeeds in fully reinnervating the tissue. Ironically enough the people who just develop numbness without pain have a less healthy peripheral nervous system because no regeneration is going on. They just lose nerves and go totally numb. The people who have pain going on have regeneration happening but the regeneration is overwhelmed by the neuropathic disease process. Some researchers are trying out drugs to turn off the regeneration process to bring relief to people with pain where there is no hope for successful regeneration. Personally, I would be reluctant to use it.

Fyi
 

Pirenzepine is an anticholinergic drug which are linked to an increased risk of dementia.

You are correct that anticholernergic drugs have been associated with an increased risk of dementia. I believe though that people need to weigh the risk of dementia against the very rule and pervasive problems that someone with small fiber neuropathy potentially faces. Obviously, there is pain and sensory issues which can be harsh but there is also the very real danger of autonomic neuropathy.

Many people with small fiber neuropathy experience some level of autonomic neuropathy. These range from cardiovascular complaints ( palpitations / arrhythmias, POTS, more generalized higher beat, exercise intolerance, etc.) to gastrointestinal issues ( constipation, diarrhea, gastroparesis, GERD, etc.), to other more miscellaneous issues ( sweating problems, other organ issues). Let me be clear: autonomic neuropathy can kill you. Cardiac Autonomic Neuropathy kills people all the time. Whenever you hear people dying from "complications of diabetes", one of the big ones is cardiac autonomic neuropathy triggering an episode of sudden cardiac death. As for Enteric Neuropathy ( GI neuropathy), constipation and diarrhea are a pain but gastroparesis can really negatively impact health.

If the M1R antagonists ( pirenzepine, oxybutynin, etc.) can trigger small fiber nerve regeneration, regrowing these nerves would have the potential of halting the progression of the neuropathy and reversing these symptoms. On balance, I would take halting the progression and/or reversing the sensory and autonomic neuropathic symptoms of this disease for an increased risk of dementia. In addition, if you get to a good place with your neuropathy, there is no indication that you would need to keep the dosage the same which might ameliorate somewhat the risk of developing dementia. Just my two cents.

Thank you so much for your sensible reply. I had also heard of the dementia risk and I'm more than willing to take the risk because it also might no cause dementia so again thanks for your sensible reply. A doctor had prescribed oxybutynin 5mg oral dosage but at a little over 4 weeks my feet began to swell, I quit for a few days and my swelled feet went down I then tried 1/2 of the 5mg pill but again after a few more weeks my feet again swelled badly. I think trans dermal is suppose to side step some of the swelling while applying the medicine directly to the effected nerves for better repair of the nerves but I would need a trans dermal gel for that. That's why I was asking about trans dermal delivery. Does anyone think trans dermal will sidestep the swelling feet problem? Also I've found an online supplier for pirenzepine but Its hard to trust foreign pharmaceutical suppliers. I'm not so much afraid of the medicine not being the correct medicine as much as I am afraid of them simply taking the money and just not sending anything therefore costing more time in getting relief and I read some where that the closer to the onset of the neuropathy the medicine is applied the better the chances the medicine will work, I don't know if this is true or not. perhaps others here may know more about this. I have used aldaychemist (an india based company) with great success for other needs but they don't carry pirenzepine. It would be of great help if anyone knows of a legit foreign supplier of pirenzepine. Its not on any US banned list or anything so it shouldn't be a problem. And I might mention that towards the end of the 6 to 7 weeks total I used the oxybutynin my fingers started getting a very slight electrical sensation to touch where before there was no sensation at all so I know this stuff does do something. Sorry for the long post but thanks again for an encouraging reply and also thanks for your and everyone else's time in reading this.

Sorry about the above post. I typed it very fast then when I went back to read the actual post I realized I didn't put it in paragraphs or anything. I realized this when I gave myself a headache trying to read my own post.
I found a supplier of Pirenzepine but its for Pirenzepine hydrochloride when most articles written about this subject states Pirenzepine dihydrochloride. Does anyone know if Pirenzepine hydrochloride will work as well as Pirenzepine dihydrochloride? This is the most important info I need to know at the moment.
If the order goes through I will post a link or at least the name of the pharmacy for others to consider as a supplier for themselves. If its allowed to give out that information on this forum
Thanks a ton for all the help so far.

Just curious if you found a supplier happy and if you have tried the pirenzepine.. definitely interested

No I haven't tried the pirenzepine yet. I found through a google search websites offering pirenzepine but in hydrochloride form not in dihydrochloride form that seems to be the form most of the studies are based on. I was thinking of taking the chance of ordering and not getting anything therefore losing my money and or if getting anything and its not fake as most are these days I would pass the website name on so others may benefit. But first I have to make sure I wont be breaking any laws before I do. I don't think this medicine would be on the schedule controlled list as its for peptic ulcers but again I must make sure. But again I have to figure out the whole hydrochloride vs dihydrochloride thing.
But to add again I am very sure the pirenzepine will work because I was experiencing such good results with oxubutin my doctor prescribed until my feet started swelling and I had to stop taking it. Please see post no 18 to see the question I have about the hydrochloride vs dihydrochloride thing.

I doubt this will matter. The active species is pirenzepine; whether it comes as the hydrochloride or the dihydrochloride should not make a difference.

Trandermal delivery of oxybutynin ends up in your blood stream. The oxybutnin patch is to treat bladder spasms. The only way to treat the spasms is to get the medication into your blood stream. Consequently, the oxybutynin medication can get to areas of your body where there is no direct application of a gel or a patch.

Two other examples of transdermal delivery systems are smoking patches (to deliver nicotine) and the contraceptive patch ( to deliver contraceptive medication).

I know it's only been a short time since this comment but do you still think the oxytrol transdermal patch is working for you?

I do think that it is helping me but it is pretty subjective at this point. I feel like I am regaining sensation in my toes. I have had a definite change in the types of symptoms that I experience. I get more itching and tingling than I have had in the past and these can be signs of nerve regeneration (Tinel's sign). I also seem to get more skin wrinkling in water which is a good sign. The only way to figure out if this is happening is to look back retrospectively and see where you have been and where you are. Hit me up a few months from now and ask me again. I suspect that I will have a better answer then.

Here is some of the research that I looked at for oxybutynin. I chose it because of this research and the fact that it is available over the counter (OTC).

Muscarinic Receptor Antagonist Improves Nerve Fiber Function in Subjects with Type 2 Diabetes and Peripheral Neuropathy | Diabetes

A 6�-YEAR-OLD WOMAN WITH SMALL FIBER PERIPHERAL NEUROPATHY RECOVERY ON OXYBUTYNIN - ProQuest

Selective antagonism of muscarinic receptors is neuroprotective in peripheral neuropathy. - PubMed - NCBI

Does anyone know if Pirenzepine is on a schedule controlled list in the US? I'm asking because I've noticed an irregularity in the normal path my packages takes just before arriving (its almost to my front door) when using the tracking number I was given. I've never seen a package take this path before. I've googled every possible way I could such as "Is Pirenzepine a schedule controlled substance" with no results saying it is. Anyone know? Thanks in advance for any and all info.

Is it sent to you (I presume, in the US?) by a non-US pharmacy? It's not a DEA scheduled drug, but it's also not listed as approved by the FDA. (So it's not available from US pharmacies.) Almost all drugs approved for use in the US are listed in the "Orange Book" (Orange Book: Approved Drug Products with Therapeutic Equivalence Evaluations).

A listing of scheduled drugs can be found at Drug Scheduling. (Interesting that the list includes Lyrica/pregabilin, but not gabapentin, even though--I'm told--they act on the same exact receptor.) Pirenzepine is not on that list.

Sorry this site won't let me post actual links yet but you can get the ideal of which site it is from this. ** and received Pirenzepine but still made my feet swell. So I guess I'm screwed with getting the use from this. unless the gel might work a little different.

I guess there are many of us interested in this. Just diagnosed with SFPN (small fiber peripheral neuropathy). Some toe, balls of feet numbness, slight burning and the shock thing.

I've ordered the 25mg pirenzepine tablets from an overseas pharmacy and will be trialing this shortly myself.

I'll keep you posted.

Note that a person on reddit did this too and good results. 25mg a day, slight stomach discomfort.

Any thoughts on making your own topical med from your pirenzepine?

If you search reddit for pirenzepine you'll read another story of an SFN sufferer who reversed many of their symptoms.

Just posting an update. I've been on 100mg pirenzepine for about three weeks now. I'm not having any stomach issues and am tolerating it quite well.

Will report back again on neuropathy results.

Is there any update on pirenzepine? Where did you get it?

Hi guys,

New to this forum. Have suffered with SFN for several years now. Just got some pirenzipine from a japanese pharmacy, arrived yesterday.

Wanted to revive this thread. Was curious if there were any updates on those who are trying pirenzipine or Oxytrol?

Hi dcd2103

Welcome to NeuroTalk :).

I hope that other members will be able to share their experiences of pirenzepine with you.

You can also use the Search option (https://www.neurotalk.org/search.php) to find other threads here where it has been discussed.

Best wishes.

Hiya. Here is my experience using oxybutynin patches:

--I used the patches for 6 months and stopped taking my regular meds
--During the time I was on it, my PN symptoms seemed to improve; however, they did not completely disappear. Calf fasciculations remained as did periodic buzzing and itching on my thigh. That said, these symptoms were tolerable, and, for the most part, I was doing well with less noticeable symptoms and without meds.
--There are side-effects if you exceed the one patch dose that are not to be ignored, including cognitive
--Once I came off the patches, I went through a highly stressful period including international travel; in retrospect, this was a BAD time for me to stop the treatment
--My symptoms got worse again within a month of coming off the patches and probably somewhat worse than they had been prior to the experiment
--I am now back on notriptyline and doing much better

On balance, it is difficult to draw conclusions. I don't know how much the improvement I felt was due to placebo, springing from the hope it inspired. And, although the timing I stopped the treatment was really unfortunate, one would have thought the results might have been more enduring than they were if Oxybutynin is really efficacious in actually healing damaged nerves.

Obviously pirenzipine is the preferred option, particularly if applied topically.

Thank you street legal!

I'm currently trying to find a pharmacy to compound the pirenzipine. This is probably not giong ot happen however because of stupid rules. IF pirenzipine were FDA recognized it would be easy.

I've looked into the chemistry, and in the topical studies they used a free base. The pirenzipine you order is HCl, but thats just to make it water soluble and shouldnt affect it very much. I"m thinking I can crush it up, mix it in some DMSO (which makes you absord it), and absorb it that way. The chemist at one of the compounding companies who wanted to help me said this isnt necessarily a crazy idea, although you can never be sure about side effects.

Since oxybutin is FDA approved, maybe they will allow us to compound this?

My question to you is if this stuff helps rebuild the nerves, it shouldnt matter if its stopped? The results should last, in theory.

Indeed.

As stated, I stopped using the patches at the worst possible time--just before I embarked on international travel, long-haul flights, and stressful circumstances. I was highly conscious of the stress, both physical and mental, I was putting myself under. And there is no doubt at all that stress is highly embodied for me--even positive emotions set off my paresthesia.

That said, if oxybutynin were implicated in healing damaged nerves and not just suppressing symptoms, one would have thought that I would have withstood the stress.

In short, within a month of coming off the patches, my symptoms were probably worse than when I had embarked on the experiment, if I am to be brutally honest--that is, pain set in rather than just buzzing and itching.

On the other hand, a self-trial of a patch designed for other purposes is hardly an ideal setting, involving a host of variables.

Hi, I think this is a great idea, have you managed to make any progress with this ? Its something that I would love to replicate.

Hello,

Are there any results yet?

Hi Beatle,

When searching for side effects about Pirenzepine i didnt find anything that would indicate that Perenzepine would cause Dementia.This is very serious issue

I know a girl on one of the facebook neuropathy groups that is using this for atleast more then a year and she claims that it helped her to heal for 80% she only has numbness at the moment.

So please provide me with this information