ericsgagnon

Where's My Hypocretin/orexin Nasal Spray?

63 posts in this topic

Wow...all of that is pretty fascinating. I'm actually quite close to a pharmacist who is in his fourth year of his doctor of pharmacy program and some of the things they do at his college involve compounding pharmaceuticals...I wonder if they might be able to do this...

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I have EDS and have been lurking this site for a while. I've been scouring the web for a cure or a way to reduce symptoms and it seems that Orexin A is the key to not masking the symptoms but resolving them.  But the problem is lack of demand / profit, right?  Well, it seems that with all the interest in nootropics, there is a market, and I may have uncovered a cheap source.

There is a website that sells 120 doses of Orexin A Nasal spray for 99.99 Euros. I'd give the name if it is appropriate, but I'm excited that for under $120 that there may be some relief for us either now or in the near future.

Description says: Each actuation delivers 50 mcg Orexin A into the nasal passages. Shake the bottle before use and apply two sprays into each nostril, preferably in the morning or when needed.

I'm curious what the group thinks.  Does this sound like a product that would work, and if so, might this type of offering be available in the US soon?

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They're pretty liberal here with the moderating aspects of the forum. Go ahead and provide the link to what you found and/or you could take one for the team and try it out. As with all meds, it may or may not work but there's only one way to find out.

May the force be with you!

 

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Normally I wouldn't post a link to a product, especially if I hadn't used it, but this really got my interest:

http://www.anthropologyreviews.com/product/orexin-a-nasal-spray/

I did my research on the site and nothing bad came up other than dispensing nootropics is a bit of a gray area.  I think this is the first time I've seen the prices for the nasal spray to be something reasonable that, if it worked, could be a solution for us.

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Like others I am seriously considering testing spray on my own. There is no hope for cure and at least 10 years for better medication.

so yes, we are kinda on our own on this decision/experiment but in most ways have been on my own in managing this 24/7 condition for the last 30 years.

Fear would be that it works but is so unaffordable. A good summary of research and treatment options was Stanford Centre for Narcolepsy med.stanford.ede/narcolepsy

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They only new treatment coming down the pike that I am aware of is a wakefulness-promoting medication by the makers of Xyrem. This was the most recent information I could find: http://www.sleepreviewmag.com/2016/06/jazz-pharmaceuticals-presents-new-data-human-abuse-liability-study-jzp-110/

On a more random note, has anyone tried Bulletproof coffee? It's supposed to work better than "regular" caffeine. Maybe it should go on my things-to-try list. 

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I'm not clear as to how bulletproof coffee could help promote wakefulness anymore than regular coffee, unless its in contrast to coffee with a ton of sweetener in it, which can cause a sugar crash. I prefer to pound loose leaf oolong and green teas all day. The caffeine isnt much more than a soda, but there's also a generous amount of Theanine, which helps stimulate without creating anxiety (or so the internet says). It seems to have helped, along with a bunch of the supplements I ordered for energy boosting.

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I've had the chance to personally try the orexin-a from "Ceretropic". I've had the best month of the last 7 years since using it, if only I can find some way to make it permanent. There's a few studies that show that intranasally and even IM does in fact cross the BBB. And because most of us have problems with prepro-orexin containing neurons and not the orexin receptors (OX1 & OX2) themselves, orexin-a does in fact activate them and give a feeling of "normalness". I've been using 200-300mcg myself. My next target is seeing if I can upregulate orexin producing neurons with nicotine patches (https://www.ncbi.nlm.nih.gov/pubmed/11014216) and seeing if there's a way to activate neurotensin, especially because I always feel ridiculously hot (http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0062391).

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2 hours ago, Pereise1 said:

I've had the chance to personally try the orexin-a from "Ceretropic". I've had the best month of the last 7 years since using it, if only I can find some way to make it permanent. There's a few studies that show that intranasally and even IM does in fact cross the BBB. And because most of us have problems with prepro-orexin containing neurons and not the orexin receptors (OX1 & OX2) themselves, orexin-a does in fact activate them and give a feeling of "normalness". I've been using 200-300mcg myself. My next target is seeing if I can upregulate orexin producing neurons with nicotine patches (https://www.ncbi.nlm.nih.gov/pubmed/11014216) and seeing if there's a way to activate neurotensin, especially because I always feel ridiculously hot (http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0062391).

Pereise1:

You seem to be the main source of user experience info for Ceretropic's Orexin-A nasal spray atm, so thank you for that!

Please try to update your experience with details of ongoing effectiveness over time, dosage, and time of administration of the Orexin-A nasal spray. Does it get you through most, or all, of the day feeling normal (oh, joy!)? Do you notice an effect on sleep quality? Please tell us what other meds you take, if you are comfortable with doing so. Do you have N with C or just N?

https://www.ceretropic.com/orexin-a

Re: nicotine

https://academic.oup.com/endo/article-lookup/doi/10.1210/endo.141.10.7707

I self-medicated with nicotine for 25-30 years. It didn't cure anything, but did help me complete my working years to the point I didn't even realize I had a sleep disorder. I did wonder why I needed naps whenever I ingested the drug after mid-day though! I had to quit the drug a couple of years ago, because, as with all (semi-)good things, it finally ceased to get the job done, naps or not. Lozenges may be an option. Be aware of its addictive property!

Orexin A loss - N with C vs. N only:

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2717206/

 

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1 hour ago, HBr said:

Pereise1:

You seem to be the main source of user experience info for Ceretropic's Orexin-A nasal spray atm, so thank you for that!

Please try to update your experience with details of ongoing effectiveness over time, dosage, and time of administration of the Orexin-A nasal spray. Does it get you through most, or all, of the day feeling normal (oh, joy!)? Do you notice an effect on sleep quality? Please tell us what other meds you take, if you are comfortable with doing so. Do you have N with C or just N?

https://www.ceretropic.com/orexin-a

Re: nicotine

https://academic.oup.com/endo/article-lookup/doi/10.1210/endo.141.10.7707

I self-medicated with nicotine for 25-30 years. It didn't cure anything, but did help me complete my working years to the point I didn't even realize I had a sleep disorder. I did wonder why I needed naps whenever I ingested the drug after mid-day though! I had to quit the drug a couple of years ago, because, as with all (semi-)good things, it finally ceased to get the job done, naps or not. Lozenges may be an option. Be aware of its addictive property!

Orexin A loss - N with C vs. N only:

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2717206/

 

No problem, I saw it come out a couple months ago and after waiting and waiting for user reports, I finally decided to bite the bullet and buy it for myself. I've also bought some from nootropic source which was cheaper but didn't come in an insulated sleeve, which is concerning. Still works either way, just doesn't feel as potent although I may have overdiluted it.

I can get through most of the day with it, especially after continued use. However, I take several other things that may confound the half life, possibly making it longer or shorter.

As for nicotine, I don't see myself getting addicted to it as, despite the boost in wakefulness, I rather hate the anxious feeling of it. I've barely started that experiment so I'll weigh perceivable long term benefits with it. And thanks for the studies, I've read both of those before and they sent me down a deep research rabbit hole.

I'll probably make another post with everything I've taken as I'd have to elaborate on the reasoning for some.

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I'm glad to have found these forums, I have ordered the same Orexin-A from Ceretropic plus this thing which I hope can work with it for delivery.

https://www.mountainside-medical.com/products/mad-nasal-intranasal-mucosal-atomization-device-without-syringe

I'm new at this and currently avoiding any medication although I've been prescribed Alertec as my N. Alertec makes me feel strange in a bad way, like tired with no way to rest. I also never experienced cataplexy (boring life maybe), although I got sleep paralyzed once when going to bed.  With a baby on the way I need a plan B, with plan A being getting hourly slaps from my wife to stay awake haha  

Pereise, do you have any practical pointers for a complete noob?

How do you measure 200mcg? (that's only 25 doses per vial?)  How much water do you dilute it with before spraying through the nose? How many mL are u spraying?  What's the shelf life when diluted? Unopened, opened?

Thanks in advance

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10 hours ago, pwnage said:

I'm glad to have found these forums, I have ordered the same Orexin-A from Ceretropic plus this thing which I hope can work with it for delivery.

https://www.mountainside-medical.com/products/mad-nasal-intranasal-mucosal-atomization-device-without-syringe

I'm new at this and currently avoiding any medication although I've been prescribed Alertec as my N. Alertec makes me feel strange in a bad way, like tired with no way to rest. I also never experienced cataplexy (boring life maybe), although I got sleep paralyzed once when going to bed.  With a baby on the way I need a plan B, with plan A being getting hourly slaps from my wife to stay awake haha  

Pereise, do you have any practical pointers for a complete noob?

How do you measure 200mcg? (that's only 25 doses per vial?)  How much water do you dilute it with before spraying through the nose? How many mL are u spraying?  What's the shelf life when diluted? Unopened, opened?

Thanks in advance

Perhaps, I can help. I'm in day 2 of trialling Ceretropic's orexin-a. I wasn't going to post until I had a better concept of its efficacy, but you need help, so... . 

First, I found Ceretropic's site and business operation to be completely reliable and upfront about the product. Shipping was next day after a weekend order placement and I received the well-packaged product within a week by mail, including crossing a border with no issues.

You should also order bariostatic water and a nasal spray bottle from Ceretropic's site as well. You will need to get a package (mine was 10 for ~$5) of insulin needles from your local druggist. When you have all this together - water, powder (orexin-a) in a little injection type bottle, needles (one use type - careful they're sharp and the needle bends easily, so, if you're like me and never handled one before, you'll need a bit of 'nursing' practice), and a nasal spray bottle, you are ready to reconstitute the orexin-a powder. 

Remove the metal tabs from the bariostatic water bottle, and the orexin-a bottle. Poke the needle through the rubber top of the water bottle and slowly and carefully (flip the water bottle up like you see the nurse do, and keep everything aligned, otherwise the needle will bend) draw up the water until the syringe is full - mine only held 1ml* and the reconstitution process requires 10 ml, iirc, so you'll get lots practice by the time you're done. Now, remove the full syringe and poke it into the rubber top of the orexin-a bottle and slowly inject the water into the container. After a few tries, you'll get the hang of it. Keep going until the powder bottle is pretty well full. The powder will easily mix with the water after a shake or two. 

* I didn't know enough to ask at the time, but possibly larger sizes are available. 10ml would be ideal, but anything larger than 1ml would be helpful. 

Next, remove the lid from the nasal spray bottle and slowly suck up a syringe full of reconstituted orexin-a and squirt it into the spray bottle. Repeat a few times. You don't need to fill the spray bottle all at once - I just put enough in to get started. I store everything in its roughly 4" x 4" x 6"  shipping box in the fridge. I do not know the shelf life, but Pereise1 has ordered his second vial and still is happy with the product, I understand.

I'm a light-weight, ~120 pounder, so I figure one squirt up each nostril taken before my pm EDS gets real bad, is about right for me for testing purposes. You can adjust that dosage according to your weight. I'd suggest getting off the Alertec before testing, but please do consult your doctor first.

To the best of my knowledge, no negative side effects of this molecule's use have been reported, and I have seen none myself after two days of dosing. I will not make a statement yet about its efficacy for me until more time has passed, but for now, it's suffice to say my outlook is positive. Ceretropic makes it clear that this product is not FDA approved and should be considered experimental. They do their own lab testing, and I personally am inclined to accept the quality of their products, but that is only my personal opinion. The owner does personally test his product on himself, I believe. You can find more info on Reddit under 'orexin-a' and Ceretropic's owner is 'MrYouAreSoDumb' on Reddit.

Full Disclosure: I am not a doctor - consult yours first!

I have absolutely no connection with Ceretropic. At this point, I do not have a formal narcolepsy diagnosis. I do know full well what daily disabling EDS is, and nightly severely fragmented sleep, as well.

Orexin-a is a naturally occurring brain peptide that most of us are short on, or missing almost altogether. Your report, should you decide to try it, would be highly valued.

https://www.ncbi.nlm.nih.gov/pubmed/24406723

http://www.jneurosci.org/content/27/52/14239

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Has anyone tried this over a period of months who can speak to its efficacy in reducing sleep needs and reducing grogginess during the day? There doesn't seem to be a lot of data on its long-term effects.

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Sorry for the late response, I've been traveling these days. But basically, Hbr summarized it better than I would have as far as reconstituting the orexin.

As far as the long term effects, it's very unfortunate that there hasn't been any human or even rat studies on its long term effects. I've been taking it for 2 months with a 10 day break and as of right now, a 5 day break.

The first time I tried it, I only dosed for 3 days before going on a preplanned vacation. The effects lingered for a few days but by the 10th day, I was up to 30mg dextroamphetamine and 150mg armodafinil, down from 40mg dex and 150mg 'finil but more than the 20/150mg I was taking before during the first 3 days. 

In the time since then, I've been able to get by with 20-30mg dextroamphetamine and 75mg of armodafinil or, lately, none. Since starting my current vacation sans orexin, I've been able to stick to 20-30mg dex and no armodafinil although I have felt a little less alert. I have on the other hand upped my caffeine intake from 100mg to 150-200mg in the last 5 days. The coffee here in Latinoamerica is amazing though and I've drinken copious amounts of caffeine (300mg+) since I was 14 so I don't feel the added caffeine is making a big difference. I feel like the positive effects have lingered longer this time after dosing more continuously in the last 6 weeks. I'll try to update as I don't get back until 4/3 so I'll be able to measure any decline in function as time goes on.

It's implied in a few studies I've read that endogenous orexin-a increases ghrelin expression which is theoretically good as ghrelin increases prepro-orexin mRna expression. It's a natural homeostasis that is balanced in normal people's brains by leptin, the satiety hormone. Pwn have a problem with energy homeostasis as this is heavily regulated by orexin itself. Exogenous orexin should theoretically function as endogenous orexin does in a narcoleptic's brain, so I don't believe long term use would unbalance our hormones in any significant way.

That said, I've definitely noticed an uptick in appetite these last 2 months, which is great for me as I went from being a foodie to lightweight hating the idea of food in general. I've also lost an additional 10 pounds in the last 2 months and started getting a little lean muscle which could either be to the change in calorie utilization or simply an increased desire to be psychically active. 

So that's as far as much as I can say from 2 months of use. I can't say I feel like I did before I got sick, but I also have a possible mold/histamine problem compounding things and I have felt the best I've felt in years, up to 70% sometimes. I look forward to hearing how it goes for y'all!

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Thank you guys for all the advice. I can't wait for my stuff to arrive, will definitely update once I tried it.

From what I can research, several people have tried it, but none have reported back after several months. Maybe they're all dead, or just too busy being happy hehe

I remember reading the account of one person without N that tried in 2013, he stopped after some time because it lost effectiveness. That was on reddit I think ...

Still a bit confused about dosage. Let's say I want to start with a minimal dose of just 50ug (1ug to 10ug per kg of body weight).

Apparently this restricted access article says that the concentration for humans is 774.35 ug/ml 

 http://www.sciencedirect.com/science/article/pii/S0166432813007948

So I'll have to mix the whole 5mg with 6.46mL to get that concentration?

Then I'll have to nasal spray 0.0646 mL exactly to get 50ug? If that works, I'll have 100 dose each costing a bit more than 1$.  Adios coffee budget!  I remember reading that someone else had a good effect after 15 min on just 30ug, I doubt he's lighter than me.

Hbr, you're practically the same weight as me btw.  ;)

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This is something that I would try. It MAY not work for me because I have no orexin producing neurons left and my orexin receptors may have shriveled up and died from loneliness. On the other hand, maybe they can be resurrected as in "build it and they will come". Dunno... just another variable to be considered.

 

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5 hours ago, Ferret said:

This is something that I would try. It MAY not work for me because I have no orexin producing neurons left and my orexin receptors may have shriveled up and died from loneliness. On the other hand, maybe they can be resurrected as in "build it and they will come". Dunno... just another variable to be considered.

 

I believe in the 'plastic' brain, meaning if you can remove any ongoing source of damage and start being kind and helpful to your brain, then over time, it can start to repair itself. This not my hare-brained idea - it's a more recent, but documented fact.

Hypothalamic neurogenesis persists in the aging brain and is controlled by energy-sensing IGF-I pathway.

So juice it up a bit with orexin-a, if you dare, and see what happens. Even though you are T1N you may just find out that your orexin receptors are happy again and were only resting peacefully. :)

Does anyone know what type of narcos were enrolled in human studies (2007)? I would like to find a link to the original studies by Revant(sp?). I may have it buried in my files somewhere. 

Intranasal orexin-A administration affects sleep and vigilance. • Orexin-A reduces wake-REM sleep transitions in the day. • Orexin-A reduces REM sleep duration. • Orexin-A improves attention in narcolepsy with cataplexy. • Our results support orexin-A to be a REM sleep stabilizing factor. 

Cautionary thoughts to consider:

http://forums.narcolepsynetwork.org/index.php?/topic/13890-at-my-wits-end-don’t-know-what-to-do-no-diagnosis-uk/&page=4

...starting at

Posted Sunday at 01:46 PM

 

                          ...towards the end of the page. And onto Page 5 as well.

 

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9 hours ago, pwnage said:

Thank you guys for all the advice. I can't wait for my stuff to arrive, will definitely update once I tried it.

From what I can research, several people have tried it, but none have reported back after several months. Maybe they're all dead, or just too busy being happy hehe

I remember reading the account of one person without N that tried in 2013, he stopped after some time because it lost effectiveness. That was on reddit I think ...

Still a bit confused about dosage. Let's say I want to start with a minimal dose of just 50ug (1ug to 10ug per kg of body weight).

Apparently this restricted access article says that the concentration for humans is 774.35 ug/ml 

 http://www.sciencedirect.com/science/article/pii/S0166432813007948

So I'll have to mix the whole 5mg with 6.46mL to get that concentration?

Then I'll have to nasal spray 0.0646 mL exactly to get 50ug? If that works, I'll have 100 dose each costing a bit more than 1$.  Adios coffee budget!  I remember reading that someone else had a good effect after 15 min on just 30ug, I doubt he's lighter than me.

Hbr, you're practically the same weight as me btw.  ;)

Please do update us with your results.  If possible, include your diagnosis, co-morbidities if any, and dosing regimen.

You're getting over my head with those numbers.

Quote

It's 5mg right? Nasal spray bottle holds 10ml and shoots .1-.13ml each spray. So if you put in 10 ml you'll get 50mcg per spray

If you use the recommended nasal spray bottle purchased from Ceretropic and mix the orexin-a vial full (or almost full) with bariostatic water, then each spray from the nasal spray bottle delivers ~50 mcg apparently. Max dose/dy is said to be 250 mcg iirc, but initially anyone, not just us lightweights, should use, IMO, only 1 spray per nostril per day for a total of 100 mcg until you can assess your reaction. Your results and final dosage levels will depend on your diagnosis and associated degree of loss of orexin producing neurons, as well as your weight.

IMO, it is best to dose earlier in the day rather than later. I got my best results when I dosed right when I felt a 'fogs rolling in, brains's gonna shut down' type of sleep attack begin - it was not effective for me for later day 'overwhelming desire to lie down and sleep/nap' type of attack and may have been, in fact, detrimental. Keep a cool head and rest and have a coffee to get through this period should you dose and not like the effect. I've only dosed for 5 days, so it may be that I need to only dose every second, or even third day, now I've topped up my orexin-a. It was extremely effective in the first situation I noted above. This is all very preliminary and likely will change as time goes on.

Please be careful, do your own research, and be aware of the dangers. This is not an FDA approved substance and is experimental only.

Quote

I remember reading the account of one person without N that tried in 2013, he stopped after some time because it lost effectiveness. That was on reddit I think ...

Ceretropic's version of orexin-a only came on the market in late 2016, I understand. Some other available products in the past may not have been effective.

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Okay, so now we learn this stuff can cure cancer too, but my question is more basic. Is there a blood test for orexin-a, and if not, why not?

http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0169908

Quote

Even if the half live of orexin-A is short 27 min [29], as the orexin-A concentration used was far larger than the physiological level measured in human blood (50 to 100 ng/ml)

A good summary of treatment options and new ideas including orexin-a:

https://www.dovepress.com/unmet-needs-of-patients-with-narcolepsy-perspectives-on-emerging-treat-peer-reviewed-fulltext-article-NSS

Apparently, we should be using phenylephrine with our orexin-a nasal spray.

Quote

One study combined 1% phenylephrine with an intranasal hypocretin preparation, reducing systemic absorption by 65%. Olfactory epithelial deposition was increased threefold and CNS hypocretin concentration was significantly higher.

Wikipedia:

Quote

Phenylephrine is used as a decongestant sold as an oral medicine or as a nasal spray.

 

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10 hours ago, HBr said:

Okay, so now we learn this stuff can cure cancer too, but my question is more basic. Is there a blood test for orexin-a, and if not, why not?

http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0169908

A good summary of treatment options and new ideas including orexin-a:

https://www.dovepress.com/unmet-needs-of-patients-with-narcolepsy-perspectives-on-emerging-treat-peer-reviewed-fulltext-article-NSS

Apparently, we should be using phenylephrine with our orexin-a nasal spray.

Wikipedia:

 

Nice, this is great information! I'm receiving another vial Monday so I'll try to see about mixing it with phenylephrine.

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2 hours ago, Pereise1 said:

phenylephrine

If this is available as a nasal spray, I was thinking it might be better just to use both at the same time, rather than trying to mix them - I'll be checking on availability.

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ceretropic.com only accepts e-check for payment.  They are asking for my checking and routing numbers.  Has anyone had any issues with fraud after ordering from this site?  

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1 hour ago, donnyd89 said:

ceretropic.com only accepts e-check for payment.  They are asking for my checking and routing numbers.  Has anyone had any issues with fraud after ordering from this site?  

I haven't had any problems with fraud in my bank account, and I'm on my 3rd vial from them. I've mainly had problems with fraud with credit card purchases from other websites but never with my checking account. It seems the reason they don't do card processing, per their reddit account, is mainly due to competitors reporting them so that visa dropped them to avoid any liability, and not because their website is insecure.

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