Novel intranasal benzo administration

[kapten]

It seems to me that given the correct medium, most benzos can be dissolved or emulsified quite easily. It would then be a simple task to use a nasal spray to deliver the drug much quicker than by ingestion, and safer than injection.

SWIM is going to attempt crushing up, dissolving and filtering xanax using some of these methods and post the results here. If you already have knowledge/experience in this area, please share.

The simplest approaches use solvents and/or co-solvents.

• In "Intranasal bioavailability of diazepam in sheep correlated to rabbit and man", Karsten Lindhardt et.al.

7mg of diazepam is dissolved in polyethylene glycol 300 at 47 mg/ml. Adsorption by the nose is shown to be a fast delivery route. Note: This would be quite painful, and I'd think that diluting with water would help.

• In "Electroencephalographic effects and serum concentrations after intranasal and intravenous administration of
  diazepam to healthy volunteers", Karsten Lindhardt et. al.

This study uses an I.N. solution of 4 mg diazepam in Polyethylene glycol 300 and shows that the bioavailability is similar to that of I.V.

• In "Absorption of diazepam and lorazepam following intranasal administration", S.W.J. Lau et. al.

This study uses Cremophor EL (Blagden, U.K.) as it is less irritating to the nasal passages. 10 mg diazepam is dissolved in 220ul Cremophor EL and 4 mg lorazepam is dissolved in 100ul Cremophor EL. This paper recommends that absorption is rather slow and peak concentration is low relative to that found after i.v. administration.


Here are some more advanced papers FYI:

• "Development of an ethyl laurate-based microemulsion for
  rapid-onset intranasal delivery of diazepam", Lianli Li et. al.

• "Intranasal Drug Delivery:An Alternative to Intravenous Administration in Selected Emergency Cases", Timothy R. Wolfe et.al.

• "Intranasal nanoemulsion based brain targeting drug delivery system of risperidone", Mukesh Kumara et.al

This study dissolves diazepam at 41 mg/ml in a microemulsion consisting of 15% ethyl laurate, 15% H2O, and 70% (w/w) surfactant/cosurfactant (Tween 80,propylene glycol,ethanol at 1:1:1 weight ratio). Nasal absorption of diazepam from this microemulsion was found to be fairly rapid!

• "Improvement of Drug Properties by Cyclodextrins", Kaneto Uekama and Fumitoshi Hirayama

• "Pharmacokinetics and brain uptake of diazepam after intravenous and intranasal administration in rats and rabbits", Paramjeet Kaur et.al.

This study The creates the I.N solution with diazepam and 1% sodium glycocholate into microemulsion system composed
of 15% ethyl laurate, 25% Labrasol®, 37.5% Transcutol®P, 12.5% ethanol, and 10%water. The study also shows that the difference in absorption time and concentration is negligible.

 

[theWorldWithin]

Unless you have panic attacks from hell I see no point. Many benzos are not more euphoric just because they come on quicker. In fact many that can be IVed feel exactly the same as oral only stronger because of a high BA, but essentially the same exact buzz and level of euphoria.

 

[kapten]

SWIM wishes !! She is so tolerant to benzos that diazepam doesn't give a buzz at any level. Xanax does, but at a very high dose.

 

[MurphyClox]

SWIM wishes

Just a kind request: Stop this annoying "SWIM"ming. It's pointless. Thx! - Murphy

 

[Doctor Abalaba]

You seem to have spent a lot of time thinking about this...

 

[shepj]

interesting post.

And theWorldWithin I didn't know that.. cool info tho.

 

[Dude Man]

seriously that SWIM BULLSHIT is so fucking stupid it makes reading the post annoying. Even on that drug-forum site it takes away significantly from any value that the site would have with all the SWIM and SWIY blah blah fucking blah. It does no good in protecting anyone in any way shape or form and is retarded.
Sorry had to rant cause that crap is spilling over to this site way to much lately.

the idea for making a benzo nasal spray is interesting though. If it works out let please let us know

 

[Mariposa]

A note that is less rude than others: the usage of "SWIM" is discouraged on Bluelight. It offers no legal protection or even plausible deniability.

I am intrigued by this as I have panic disorder, and I do not abuse my benzodiazepines. I am scripted Xanax and Klonopin. I wonder if this technique would be effective in a situation in which I have a panic attack. Usually I swallow or sublingually administer myself 1 mg Xanax. A faster mechanism of action would be most welcomed by many of us with panic disorder/PTSD/GAD/anxiety disorder NOS.

I've never plugged a drug, any drug. I do wonder after yanking a pen from my neurologist's office that was advertising Diastat - Diazepam Rectal Gel if benzos would be more effective rectally. I'm not intrigued enough to try it, though. Diazepam has an uncomfortably long half-life for me and is not as effective in vivo as my current regimen.

To kapten: can you legally (meaning without violating copyright law) post links to the studies? I can pull them through a university connection but cannot post links myself, and would appreciate a synopsis of what you've read in the interest of time. I note that the solution you describe contains ethanol which is probably necessary as a solvent, but what effect do you believe ethanol would have in addition to the benzodiazepine in an intranasal administration?

With reference to the Diastat preparation, it is marketed as an antiepileptic and alternative to the emergency room per their website (see above). The ease of administration seems to be a significant advantage, and can clearly result in lower patient care costs and less load on emergency room personnel. I wonder if an intranasal preparation of a benzodiazepine could benefit anxious patients as well as epileptics.

A most novel question, certainly. Welcome to Bluelight, kapten - and do keep in mind that the usage of "SWIM" is discouraged here. Your post is well-researched and I look forward to your follow-ups. This is well worth looking into! Thanks for sharing.

 

[alkap555]

What I like to do with all drugs that SWIM insufflates is to first make up a 70% solution od DMSO (dimethyl sulfoxide) in saline and put it in a sterile nosespray bottle. First irrigate the nasal passages with the DMSO solution (burns a little but is completely harmless) then snort that line. For those that don't about DMSO, it is an excellent solvent, so much so that it can facilitate the transportation of drug molecules through the skin, especially mucous membranes.
SWIM always uses this method with amphetamines-HCl and it increases the potency by roughly 30% I would guess.

 

[alkap555]

What I like to do with all drugs that SWIM insufflates is to first make up a 70% solution od DMSO (dimethyl sulfoxide) in saline and put it in a sterile nosespray bottle. First irrigate the nasal passages with the DMSO solution (burns a little but is completely harmless) then snort that line. For those that don't about DMSO, it is an excellent solvent, so much so that it can facilitate the transportation of drug molecules through the skin, especially mucous membranes.
SWIM always uses this method with amphetamines-HCl and it increases the potency by roughly 30% I would guess.

 

[d-Dexter-25]

Sounds good for stopping bad trips fast with no need for a needle which sticking yourself with a needle while tripping is no fun i'd think well not while on a bad trip atleast!!! Waiting the 15-30 minutes for a pill of alprolazam to kick in while your having a total bad hellish trip can seem like forever and this would mean insuffulate a spray from a little nasal spray bottle and your trip is either terminated or atleast brought down quite a bit plus you could judge how much you need too. Gonna extract some alprolazam from some tablets and make a solution for nasal use, Thanks!!!

 

[Jamshyd]

I've never plugged a drug, any drug. I do wonder after yanking a pen from my neurologist's office that was advertising Diastat - Diazepam Rectal Gel if benzos would be more effective rectally. I'm not intrigued enough to try it, though.

Benzos can be very easily and effectively plugged, and are much more efficient that way than oral (less is needed, significantly faster onset). Simply dissolve said benzo in milk, load a needle-less syringe, insert (lubed? if you need) tip, and fire away.

As byzantine as that sounds, it works very well and makes perfect sense. If you don't believe me, ask FnB .

 

[kapten]

MurphyClox

Just a kind request: Stop this annoying "SWIM"ming. It's pointless. Thx! - Murphy

Mariposa and Dude Man ...

Sorry, but the Hive burnt me the heard way and personalising posts is not a good idea. Just enqire about such "mythical persons" as Ozmium and Rhodium (if you don't know what I'm talking about then I rest my case.

Anonymyity is alwasys the safest option.

 

[kapten]

Unless you have panic attacks from hell I see no point. Many benzos are not more euphoric just because they come on quicker. In fact many that can be IVed feel exactly the same as oral only stronger because of a high BA, but essentially the same exact buzz and level of euphoria.

Obviously alprazolam (xanax) can be substituted.

 

[dread]

Sorry, but the Hive burnt me the heard way and personalising posts is not a good idea. Just enqire about such "mythical persons" as Ozmium and Rhodium (if you don't know what I'm talking about then I rest my case.

Swimming is not going to protect you whatsoever.

 

[MescalitoBandito]

Some friends told me about lying upside down and dropping a bit of alprazolam tincture into their noses (using alcohol I believe) and raved about it. Very few were able to stay awake long enough to really enjoy the experience. Though if you must snort benzos, it seems you need a solvent.

Also, there's nothing anonymous about substituting SWIM for I/me. Everyone knows who you're talking about. If you're really so worried you should not be posting anything online. In fact, go live a truly anonymous life alone in nature.