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Benzodiazepines All about benzodiazepines (downers)

 
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  #1  
Old 23-10-2010, 21:18
Jimmyyyy Jimmyyyy is offline
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rectal use of alprazolam??

sim utfse and he couldnt find anything on the subject. what is the bioavailibility for rectal alprazolam/is it worth it? swim doesnt mind shoving things in him bum, its kinda relaxing(swim is by far not gay though)
  #2  
Old 23-10-2010, 21:37
psychedelaholic psychedelaholic is offline
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Re: rectal use of alprazolam??

After a quick forum search:
Rectal Administration (Benzodiazepines rectally?) is another method of taking benzodiazepines. When benzodiazepines are taken rectally, only about 33% of the benzodiazepines undergo first-pass metabolism. Therefore, rectal administration has an increased effect over oral administration for the same amount of benzodiazepine
  #3  
Old 23-10-2010, 21:51
Jimmyyyy Jimmyyyy is offline
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Re: rectal use of alprazolam??

thanks fellow swimmer. swim was also wondering this: what is the proper way to administer drugs rectally? cris the pills in watner thenput in syringe and shoot it up the butt? or does one have to cook it like a shot of H or something? please explain this to swim so he doesnt wanste his supply.!

many thanks, swim.
  #4  
Old 23-10-2010, 22:08
FCTLIS FCTLIS is offline
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Re: rectal use of alprazolam??

As a suggestion-

First off, safety! Wash your hands and make sure you are working with sanitary instruments.

Use SWIY's preferred method of crushing the pill. No need to cook it, just use comfortable temperature water and a syringe minus the needle. Some lube also wouldn't hurt

Feel free to ask SWIM anything. SWIM has experimental with rectal administration with many classes of drugs, happy to answer questions.

Happy Plugging!
  #5  
Old 23-10-2010, 22:10
psychedelaholic psychedelaholic is offline
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Re: rectal use of alprazolam??

Well with most drugs SWIY would mix with water then pipette or syringe up there however like almost all benzos alprozalam is barely soluble in water. Although if the pills were crushed, added to water then sucked up in a syringe as a suspension and plugged that should work. It is soluble in ethanol and propylene glycol (I think). Not sure about how good an idea putting neat ethanol up your bum is. Diluting it with water would be fine though. Don't see why PEG couldn't be plugged. But I reckon suspending the crushed pills in water and plugging it will work perfectly well.

Xanax's oral bioavailability is actually 100% anyway but plugging will increase the duration as it will be metabolised slower. This same effect could be achieved orally with enzyme inhibition. Benzos are metabolised by the cytochrome P450 family. These enzymes can be prevented from doing this by drinking grapefruit or pomegrenate juice or taking tagamet an hour before hand. This has been discussed extensively on the forum.
  #6  
Old 23-10-2010, 22:12
Space Numpty Space Numpty is offline
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Re: rectal use of alprazolam??

Quote:
Originally Posted by Jimmyyyy View Post
thanks fellow swimmer. swim was also wondering this: what is the proper way to administer drugs rectally? cris the pills in watner thenput in syringe and shoot it up the butt? or does one have to cook it like a shot of H or something? please explain this to swim so he doesnt wanste his supply.!

many thanks, swim.
It depends on the drug, but in the case of alprazolam:

  • Dissolve crushed pill in a small amount of warm water, say 10ml
  • Suck fluid up into syringe
  • Insert into anus
  • Depress syringe plunger until all fluid has left the syringe
  • Remove syringe from anus (important)
All this is well covered in the relevant forum section.
  #7  
Old 23-10-2010, 23:43
FCTLIS FCTLIS is offline
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Re: rectal use of alprazolam??

Some tip's from SWIM's rectum-

Make sure SWIY is "clean" and "empty" before trying this. It's best to try it in a tub until SWIY has more experience. Try to keep the liquid in as long as possible. SWIM recommends at least 20 minutes. The deeper the syringe is inserted, generally, the easier it is to keep in.
  #8  
Old 24-10-2010, 17:10
kailey_elise Gold member kailey_elise is offline
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Re: rectal use of alprazolam??

Quote:
Originally Posted by psychedelaholic View Post
Xanax's oral bioavailability is actually 100% anyway
That's not true; oral bioavailability of alprazolam is 80-90%.

I don't think the oral administration of any drug/medication/chemical results in 100% bioavailability, but I'm more than willing to be proven wrong on that.

Quote:
Originally Posted by psychedelaholic View Post
but plugging will increase the duration as it will be metabolised slower.
Really? Usually, plugging any substance results in a faster & harder onset time, a quicker peak and a shorter duration. I would find it interesting that alprazolam works differently.

Quote:
Originally Posted by psychedelaholic View Post
This same effect could be achieved orally with enzyme inhibition.
I agree completely on this, and Tagamet (cimetidine) is known to increase both effects & duration of alprazolam.

In addition, "oral syringes" (also known as medicine syringes or baby syringes) are easily available at any drugstore in the Baby Care aisle near the medicine - the "turkey baster" style ones tend to be easier to use while plugging. They're inexpensive, and no one will think anything of someone making a purchase of such an item. They make the plugging of tablets a breeze (with the addition of some lube, that is - even hand lotion, or vegetable oil from the kitchen will work in a pinch).

Also as stated, if one can empty the bowels prior to plugging, that can help - one wouldn't want a poo log soaking up all the goodies! One could use the oral syringe with just water and load it up there a few times with water to act as an enema prior to plugging, just to be safe.

If anyone is going to be using an enema to "clean the pipes" for any reason and buys a "pre-mixed" enema, it's highly recommended to empty the contents of the enema bottle when you get home, and refill with just warm water (maybe with a dash of salt in it, but it's not like this is enough water to really throw your electrolyte balance off). The pre-mixed enemas often contain some chemicals in them that cause the user to cramp painfully. So, especially if you're not constipated, and just wanna use an enema "just in case", empty the juice that comes with the enema!

I, personally, would recommend buying a reusable "enema bulb syringe" instead of those Fleet (and generic version thereof) enemas. And I bed those enema bulb syringes would also come in handy for plugging though many might find the oral syringe easier to handle, esp at first.

~Kailey
  #9  
Old 25-10-2010, 19:47
psychedelaholic psychedelaholic is offline
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Re: rectal use of alprazolam??

Quote:
Originally Posted by kailey_elise View Post
Really? Usually, plugging any substance results in a faster & harder onset time, a quicker peak and a shorter duration. I would find it interesting that alprazolam works differently.
When I said it would increase duration by plugging I was going by this statement:
Quote:
When benzodiazepines are taken rectally, only about 33% of the benzodiazepines undergo first-pass metabolism. Therefore, rectal administration has an increased effect over oral administration for the same amount of benzodiazepine
I thought it meant that it isn't metabolised as quickly as it is entering the blood stream before going through the stomach and into the liver. So when benzos are taken orally more undergoes first pass metabolism quicker. At least that's what I took it to mean I might be wrong. Will look for the thread I found the statement in. Plugging does definitely increase duration of certain drugs over taking them orally. Plugging ketamine makes it last 2-3hours whereas orally it lasts 1-1.5hours and snorted less than an hour.

Last edited by psychedelaholic; 25-10-2010 at 19:55.
  #10  
Old 25-10-2010, 19:55
kailey_elise Gold member kailey_elise is offline
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Re: rectal use of alprazolam??

No, it means it's metabolised MORE quickly; all of the benzo (I think - at least most of it) has to undergo first pass metabolism via oral administration, so via oral it gets into ones system slower because it has to go to the liver first.

Via rectal, it absorbs through the mucous membrane and somehow gets right into that big ass (Ha!) vein that's in there and goes right into your bloodstream.

At least, that's how it works for water-soluble chemicals. I'm not sure exactly if/how that works for (most) benzodiazepines, as they aren't water-soluble. Someone with more chemical knowledge can chime in on that one.

~Kailey
  #11  
Old 25-10-2010, 20:22
psychedelaholic psychedelaholic is offline
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Re: rectal use of alprazolam??

Quote:
Originally Posted by kailey_elise View Post
No, it means it's metabolised MORE quickly; all of the benzo (I think - at least most of it) has to undergo first pass metabolism via oral administration, so via oral it gets into ones system slower because it has to go to the liver first.
Once it undergoes first pass metabolism the effect of the drug is weakened. When plugged it enters the bloodstream straight away with only 33% undergoing first-pass metabolism. When taken orally it goes through the liver before going into the bloodstream where 50% of it undergoes first pass metabolism. So plugging would increase effects and I would of thought duration as well.

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acetone, alprazolam, anal administration, aprazolam, benzodiazepine, benzos, bioavailability, drugs, drugs forum, enema, grapefruit, lorazepam, plugging, rectal administration, rectal administration of benzodiazepines, sleeping pills, xanax

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