Help reducing pain of insulfating Ethylphenidate(EPH) or Isopropylphenidate (IPPD/IPD

[Mr TIMO]

Hello there,

I receive incredible pain when i insulfate IPD.
Without as yet testing it's PH in water, i believe it is highly alkaline from other revies (confirmation needed)
I tried mixing it with some phenibut which is quite acidic (2-3 in water) however no improvement. ALso no improvement from using crushed vitamin C, or L-Theanine (midly acidic)
Maybe i was wrong and it is actually acidic, i'll make a PH taste with Red cabbage right now.
If it is acidic, would mixing it with baking soda fix the issue?

My other idea is to neutralise it in a nasal spray. Water with some sodium chloride and a bit of vinegar (presuming the compounds are alkaline).

But with a nasal spray (and maybe even just with powders), i run the risk of possibly creating new bad chemicals, right?

Please help save my nasal cavity, and stop me from accidently making worse nastier chemicals.
Thanks!

Mr T

 

[Rybee]

IIRC Ethylphenidate is alkaline with pH ~9.

 

[Mr TIMO]

Hmmm well i just did a very unusual test.

I made a home made ph testing solution boiling some red cabbage leaves in water.

It is a purple solution. Slightly blue purple actually when i dropped it onto my clear pastic testing surface (which was placed over a white sheet of paper)

I tested with vinegar, it turned a moderate red.
I tested by dropping some phenibut hcl, it went a very strong red. (acid)
I tested dropping in some baking soda, it went a strong blue/green (alkaline)

Then I tested with the isopropylphenidate. It had a VERY subtle change to red, sugggesting it is slighty acidic nature.
Proof that i was making it MORE acidic and causing more pain yesterday!

But still it is only very mildly acidic. This suggests that baking soda in very minute will assist, so i'll do some more testing now.

I suggest the problem is more than just the PH level.

What are other properties of chemicals that cause pain?

 

[sekio]

All the *phenidates will be slighly acidic in solution as the water soluble HCl salts.

The solution is to not snort them or to make a buffered solution with some bicarbonate in it, I suppose.

 

[Mr TIMO]

This still does not work,i made a solution with water IPPD and bicarbonate. It tested very alkaline. Still lots of pain.
But maybe still a better option for the nose as you are supplying a buffering layer of moisture to handle some of the reaction that must take place?
I alsor run the risk of causing a chemical reaction. bases and acids react to create other compounds right?
And over time the original chemicals can break down further right? I know there isa certain PH level ideal to store most things, for example coke should be stored in a PH level of around 4 or something on the acidic side. otherwise it breaks down to one of it's metabolites faster i believe.

anyway so I have deduced that the causticity is NOT the issue. I looked up chemical burns on the old wiki, presuming the pain is clasified as a chemical burn, and it reads:
"acids, bases, oxidizers, solvents, reducing agents and alkylants."
so i feel i really only ruled out acids and bases as the issue. it could be a solvent, reducing agent, oxidiser or alkylant right?

any ideas on what of those it may be? and ways to change it?

I stupidly tried to add benzocaine to the mixture. THen when the stray wasn't working, i researched and found it is only mildly soluable in water - and it needs to be slightly ascidic water. SO perhaps just water, IPPD and benzocaine may be better... short of find ing a better option of course based on the solvent, reducing agent, oxidiser or alkylant idea...

come on chemists, help us out!

 

[Mr TIMO]

close to a solution...

Ok so im looking into research in the cosmetic industry. I believe we need to research how to relieve pain from neutral irritants. (if it's essentially neutral but still burns it's considered an irritant)

from: https://books.google.ro/books?id=3d...page&q=chemistry of neutral irritants&f=false

"with the exception of local anesthetics that are regulated as drugs in most countries and may have undesirable side effects and safely concerns, no compounds have been described that are able to broadly inhibit sensory irritation from cosmetics and pharmaceuticals. Because a safe compound capable of blocking sensory irriation and inflamation would provide considerable benefit, I sought to identify compounds that could block sensory irriant reactions. Simple water soluble strontium salts have proved to be potent and selective inhibitors of chemically induced sensory irritation and neurogenetic inflamation in humans and do no produce numbness or loss of other tactile sensations."

Intriguing.

Water Soluble strontium salts.
"Strontium chloride (SrCl2) is a salt of strontium and chloride. It is a typical salt, forming neutral aqueous solutions. Like all compounds of Sr, this salt emits a bright red colour in a flame; in fact it is used as a source of redness in fireworks. Its chemical properties are intermediate between those for barium chloride, which is more toxic, and calcium chloride."

"Dental care[edit]
SrCl2 is useful in reducing tooth sensitivity by forming a barrier over microscopic tubules in the dentin containing nerve endings that have become exposed by gum recession. Known in the U.S. as Elecol and Sensodyne, these products are called "strontium chloride toothpastes", although most now use potassium nitrate instead which works as a nerve calming agent rather than a barrier.[3]"

Potasium nitrate as a nerve calming barrier sounds possibly better as it seems strontium chloride may actually limit the affect of the intended chemical to enter the blood vessels?

http://en.wikipedia.org/wiki/Potassium_nitrate

This requires more research. It may reduce pain, but will it destroy your ability to smell?

Hmm it is also used as a tree removal as it apparently burns according to some sold on ebay. It is also names as Nitric Acid!
Although it is also used as a preservative in foods, so food grade would first need to be considered.

However possibly not neccesary, if IPPD is only an irritant rathat than caustic, a water/saline nasal delivery may protect the nose - the the pain, well you just need to live with it.

Thoughts?

 

[Bagseed]

this is probably non-constructive, but maybe you should consider that highly irritant or caustic compounds are not very well suited for intranasal consumption?

 

[Mr TIMO]

Well surely not when no other precaustins are taken, and with highly caustic, for sure! that will eat away at your flesh. And trying to alter the PH can alter the chemistry of the drug.
Irritants that are neutral generally (according to my research) do not cause much damage (pain is not always damage), unless it dries out the membrane in which case that is easily cared for.

I'll look more into Potassium nitrate and Strontium chloride tomorrow. with some actual references not speculation. and possibly some more testing at some stage if research suggests they will firstly work, and secondly not cause permanent damage to nerve endings (which is where smell comes from)
I have very good sense of smell so i take this seriously, no one seems too woried about sense of smell, just a bloody nose or devaited septum

 

[sekio]

Ok so im looking into research in the cosmetic industry. I believe we need to research how to relieve pain from neutral irritants.

Adding more salts to it won't help... you're just going to make it burn MORE!

The research on what irritates tissue has already been known for a long, long time. There's 2 major reasons that a compound will irritate exposed mucus membranes.
1. Aciditry (pH). If the pH of a solution isn't right around 7.4 then it will be an irritant
2. Tonicity. If the solution is not roughly the same osmolarity as your blood, it will either pull water from your cells or force water into them. So you need to adjust the concentration to the point where there's the same number of ions in it as "normal saline".

This is evidenced by the fact that if you try to do something like snort salt, or put brine up your nose, IT STILL BURNS EVEN THOUGH IT'S NEUTRAL pH! The only way to get around this is diluting ethylphenidate large amounts, adjusting the pH to 7.4 with a small amount of bicarbonate & narrow range pH papers, etc.

Please, please don't add potassium nitrate or strontium chloride to your ethylphenidate! Those are chemicals that are made to reduce dental sensitivity. They are absolutely not for putting up your nose or on mucous membranes!

Or - better idea - DON'T SNORT COMPOUNDS THAT DESTROY YOUR NASAL TISSUE! Even cocaine will totally trash your nose, and that objectively "feels" like it doesn't burn.... only because it's an anesthetic. Cocaine is actually really acidic, moreso than ethylphenidate.

 

[sekio]

For further reading, here's a good PDF reference. on formulation of nasal sprays.

This still does not work,i made a solution with water IPPD and bicarbonate. It tested very alkaline. Still lots of pain.
But maybe still a better option for the nose as you are supplying a buffering layer of moisture to handle some of the reaction that must take place?

I don't mean "buffering" as in a buffering layer of moisture. I mean that the bicarbonate will absorb the acidity rather than your nasal tissue. The nose is actually slighly acidic, optimum pH for nasal sprays is around 5.5 - 7. Lots of drugs have a slightly acidic pH in a nasal spray, yet they don't irritate tissue. In fact, sometimes drug manufacturers will add very small amounts of sulfuric acid or sodium hydroxide to adjust the pH.

Adding benzocaine or other numbing agents to mask the pain is actually a really dumb idea because you will leave the damage to go unchecked. The whole reason ethylphenidate and friends are nasal irritants is beacause they shouldn't be put up your nose.

Osmolarity is probably the most important part of this. I know that, for instance, people who use neti pots or saline irrigation for their nose, and eye or ear drops both need to have a specific level of ions in them. Otherwise, if you do something like pour distilled water up your nose, it can hurt.

I have built up a spreadsheet to figure out osmolarity too. For a nasal spray the optimum concentration for ethylphenidate is 42 mg/mL. Any less than that and you will need to add some salt as well to ensure there's the same "osmotic pressure" in the spray as there is in your nose and tissues.

For instance a 10mg/mL ethylphenidate HCl solution will also need 6.7 mg/mL sodium chloride in it as well, or it will be irritating.
20 mg/mL ethylphenidate HCl needs 4.6 mg/mL salt.
30 mg/mL ethylphenidate HCl needs 2.6 mg/mL salt.

 

[serotonin2A]

^Agreed.

Unfortunately some drugs are not compatible with mucous membranes. The pain you are experiencing is due to tissue irritation and it is a signal that you should not be ingesting ethylphenidate by the intranasal route. Adding other salts or a local anesthetic isn't going to stop the irritation from occurring, and will just cause other problems.

 

[Mr TIMO]

Osmolarity is probably the most important part of this. I know that, for instance, people who use neti pots or saline irrigation for their nose, and eye or ear drops both need to have a specific level of ions in them. Otherwise, if you do something like pour distilled water up your nose, it can hurt.

I have built up a spreadsheet to figure out osmolarity too. For a nasal spray the optimum concentration for ethylphenidate is 42 mg/mL. Any less than that and you will need to add some salt as well to ensure there's the same "osmotic pressure" in the spray as there is in your nose and tissues.

For instance a 10mg/mL ethylphenidate HCl solution will also need 6.7 mg/mL sodium chloride in it as well, or it will be irritating.
20 mg/mL ethylphenidate HCl needs 4.6 mg/mL salt.
30 mg/mL ethylphenidate HCl needs 2.6 mg/mL salt.

Ahhh fantastic. Thanks for this. How did you calcualte these? I wonder how i would to this for IPPD.
With IPPD, the PH according to my testing should be fine for the nose. You only need to add a tiny amount of bicarb soda to make it more alhaline (btw i saw nasal sprays that were generally PH 7-9 which is contradictory to what you've seen)

So i agree this suggests (unless there is a third factor), that osmolarity is the issue. I actually had this discussion with a pharmacist in the shop the other day but totally forgot.

So this means if the osmolarity of the solution is causing pain, the pain can be illiminated, which should also limit damage, right?
The unusual thing though with those stats is that they suggest the the stronger then concentration, the less the pain.
Souunds counter intuitive to me, because if you you don't have a solution at all and just insulfate the powder, that's about as high as possible concentration right? care to elaborate on that?

Actually wait i think i've realised the problem. I've been making my solution too concentrated with the IPPD. so if i dilute it further it should work better i imagine.

And so if you can let me know how this might be worked out with isopropylphenidate, that would be great

Finally we're getting some science in here!

 

[Mr TIMO]

http://en.wikipedia.org/wiki/Tonicity

"Tonicity is a measure of the effective osmotic pressure gradient (as defined by the water potential of the two solutions) of two solutions separated by a semipermeable membrane. In other words, tonicity is the relative concentration of solutions that determine the direction and extent of diffusion.

There are three classifications of tonicity that one solution can have relative to another. The three are hypertonic, hypotonic, and isotonic
There are three classifications of tonicity that one solution can have relative to another. The three are hypertonic, hypotonic, and isotonic

Hypertonic refers to a greater concentration. In biology, a hypertonic solution is one with a higher concentration of solutes outside the cell than inside the cell. When a cell is immersed into a hypertonic solution, the tendency is for water to flow out of the cell in order to balance the concentration of the solutes.

Hypotonic refers to a lesser concentration. In biology, a hypotonic solution has a lower concentration of solutes outside the cell than inside the cell. In an attempt to balance the concentrations of solutes inside and outside the cell, water will rush into the cell, and can cause it to burst

An isotonic solution is one in which its effective osmole concentration is the same as the solute concentration of a cell. In this case the cell neither swells nor shrinks because there is no concentration gradient for water across the cell membrane. Water molecules diffuse through the plasma membrane in both directions, and as the rate of water diffusion is the same in each direction that cell will neither gain nor lose water"

So i guess you need it to be isotonic is what you were saying, interesting.

Although this is confusing: "tonicity is influenced only by solutes that cannot cross the membrane,"
doesn't IPPD HAVE to cross the membrane to enter the bloodstream, in which case this whole tonicity is irrelevant?

 

[endotropic]

Don't some chemicals produce a burning sensation irrespective of tonicity and pH? Ethanol comes to mind, and in that case the burning probably comes from a specific interaction between the chemical and heat sensing receptors.

If ethylphenidate behaves the same way nothing you can do (safely) will help much.

 

[Mr TIMO]

Ethanol is a solvent, (though as is water), however i believe that ethanol is consdiered Hypertonic? unless you have it very diluted in twater perhaps.

if what sekio said is true, then yes there is something you can do, you simply dilute it in water to the correct dilution to match the osmolarity of the membranes. But if you put a high sugr content in water, why does this not cause such a burn?

still trying to understand the chemistry. there is not a lot of good informaton around on what seems like a straightforward thing. i think its a charge/electron thing here
surely chemical burns and irritants have been higly researched

 

[endotropic]

^OK ethanol might not be the best example but imagine putting a pH 7.4 isotonic solution of capsaicin up your nose. The point I was trying to make is that some chemicals just burn no matter how you dissolve them.

By all means try the adjustments discussed in this thread, I just wouldn't be surprised if some of the burning lingers no matter what you do.

 

[sekio]

doesn't IPPD HAVE to cross the membrane to enter the bloodstream, in which case this whole tonicity is irrelevant?

No, isopropylphenidate doesn't have to enter the cell (cross the cell membrane), it acts on surface-bound transport proteins. Maybe you have confused cell membranes with the blood-brain barrier.

if you put a high sugr content in water, why does this not cause such a burn?

I would expect it would. Even distilled water can cause nasal irritation!

Souunds counter intuitive to me, because if you you don't have a solution at all and just insulfate the powder, that's about as high as possible concentration right? care to elaborate on that?

Anything above 40 mg/ml ethylphenidate is hypertonic and will be an irritant - I didn't clarify that. By my math 42 mg/ml ethylphenidate and no salt added is an isotonic solution.

I am calculating osmolarity by first figuring out what the molarity of ethylphenidate solution is, and multiplying by 2 (ethylphenidate dissociates into 2 ions in solution). If the osmolarity comes out to less than 300 mOsm I subtract to find the excess osmolarity, divide by 2, and use that number as the number of moles of salt to add.

I think that, in the end, you will have to come to grips with the fact that putting chemicals up your nose is often not a good idea for the long term. Even if you find a way to mask the burning, ethylphenidate will still cause nasal damage over time because ethylphenidate is a strong local vasoconstrictor, and just like cocaine it will decrease blood flow to the tissue it touches. Eventually your nasal septum or sinuses will rot away if you keep snorting ethylphenidate. You can't get around this fact by combining other drugs or taking supplements or praying to God either. It's a consequence of the stimulant effects of ethylphenidate and all stimulants.

 

[Mr TIMO]

Anything above 40 mg/ml ethylphenidate is hypertonic and will be an irritant - I didn't clarify that. By my math 42 mg/ml ethylphenidate and no salt added is an isotonic solution.

I am calculating osmolarity by first figuring out what the molarity of ethylphenidate solution is, and multiplying by 2 (ethylphenidate dissociates into 2 ions in solution). If the osmolarity comes out to less than 300 mOsm I subtract to find the excess osmolarity, divide by 2, and use that number as the number of moles of salt to add.

I think that, in the end, you will have to come to grips with the fact that putting chemicals up your nose is often not a good idea for the long term. Even if you find a way to mask the burning, ethylphenidate will still cause nasal damage over time because ethylphenidate is a strong local vasoconstrictor, and just like cocaine it will decrease blood flow to the tissue it touches. Eventually your nasal septum or sinuses will rot away if you keep snorting ethylphenidate. You can't get around this fact by combining other drugs or taking supplements or praying to God either. It's a consequence of the stimulant effects of ethylphenidate and all stimulants.

excellent post, thankyou.

Are you able to work out if isopropylphenidate is the same, i.e. dissassociates 2 ions in solution?
I tried it at half that amount, so 200mg in 10ml and it was fine, no pain

Is there an alernative to reducing the molarity rather than adding more water?

 

[Mr TIMO]

Even if you find a way to mask the burning, ethylphenidate will still cause nasal damage over time because ethylphenidate is a strong local vasoconstrictor, and just like cocaine it will decrease blood flow to the tissue it touches. Eventually your nasal septum or sinuses will rot away if you keep snorting ethylphenidate. You can't get around this fact by combining other drugs or taking supplements or praying to God either. It's a consequence of the stimulant effects of ethylphenidate and all stimulants.

what about adding a vasodilator to the mix? a drop of alchol or something, amyl nitrate (that sounds dangerous). Maybe it could even improve absorption. i was reading somewhere else about something improving absorption, but I think is not really a need

 

[sekio]

Adding a vasodilator won't help. And the only way to reduce the concentration is dilute it.

Isopropylphenidate will have roughly the same math as ethylphenidate: the molecular weights are similar and they both behave the same in solution.