Does rectal admin of morphine increase bioavailibility???

Discussion in 'Morphine' started by Wyborowa, Aug 26, 2006.

  1. Wyborowa

    Wyborowa Silver Member

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    How does rectal administration of morphine increase bioavailibility when taking it orally is only 30% bioavailible? Rectal would be similar to insufflation, right? Wouldn't the morphine turn into gell in the enema bottle? I am using the 30mg MS contin xtd release....would I have to take the coatin off then crush it? or just crush the whole pill, mix with more water than necessary and bum boot it?
    THANKS!
     
  2. Psych0naut

    Psych0naut Platinum Member

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    Insufflation is also more commonly called snorting, rectal is shoving it up your bum.
    If You wants to do it rectally, than the pill should first be crushed to get properly and faster absorbed.
    If will dissolve in water in the enema bottle, it won't turn into gell as it's very water soluble.
     
  3. Wyborowa

    Wyborowa Silver Member

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    swim knows that insufflation means snorting :) So it IS faster! YESSSS!

    DZIENKUJE!
     
  4. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    not only is it faster, but it should up the bioavailability. I find that morphine insufflated is alot more effective than morphine orally. he imagines that rectally would be even more effective.
     
  5. Fantasian

    Fantasian Gold Member

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    Morphine rectally has massively increased bioavailablity, be weary of starting at a too higher dose for You as this could lead to serious problems.
    Here are the benefits and disadvantages (From SWIF's personal experience) of Rectal Admin with all opioids including morphine.

    Increase Bioavailablity to to about 60-80%

    Onset is very rapid (SWIF believes faster than insufflation) 2 minutes or less

    Constipation seems to be somewhat worse (SWIF's experience)

    Experience is somewhat shorter than Oral however more intense.

    --

    As for destroying the extended time release mechanism, crush the pills and put them in water. Ensure they are small enough to go through the Syringe head (without needle) and push the syringe head up ones anus (again without needle) and squirt. The sensation is quite unpleasent and You may want to shit himself. This sensation will pass in around 30 seconds - 1 minute. At which point You should feel comfortable again. SWIF always found lying on the right side made the feeling less uncomfotable while administering rectally.

    Best of LUCK to You :D
     
  6. DrMuffy

    DrMuffy Silver Member

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    Yes taking morphine rectally is much better! I took 30mg rectally and it was amazing. Well I am bi so swim cant really speak for str8 guys but it doesnt feel all that bad and its fairly easy. All you need to do is crush up the pills, get a syringe (without needle of course), get bout 5mL of hot water, put crushed pill in it and stir until most of it is dissolved. Then suck up the water into the syringe and lubricate it ALOT, then lay on you side and slowly stick it in swiy's ass untill the plunger part is almost in there, then slower realease the liquid and nce done pull it out slowely, and your finish. A word for the wise tho, make sure u have a book or TV or something to entertain you wile you lay there, because for it to get absobed you will need to lie there for at least 20 minutes. Well Good luck
     
    Last edited by a moderator: Sep 15, 2006
    1. 5/5,
      Good post!
      Sep 15, 2006
  7. Sklander

    Sklander Silver Member

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    Re: Is rectal admin of morphine increase bioavailibility???

    SWIDrMuffy - I don't think that you have to lie on your side for twenty minutes or else absorption will not take place. I am very experienced with the procedure that You just described and SWIM usually is up and walking around in less than five minutes.

    Lubrication is the key to easy rectal administration of substances. Bottom line. ;)
     
  8. Nicaine

    Nicaine Titanium Member

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    Re: Is rectal admin of morphine increase bioavailibility???

    Agreed... lying still on your side appears to aid absorption somewhat (particularly in the first couple minutes) but is not absolutely necessary. There are many other factors affecting absorption such as intestinal pH, location/condition of stool and water-solubility of the main ingredient once the pill is dissolved. The subject is actually rather complicated.

    http://www.ncbi.nlm.nih.gov/entrez/...=Retrieve&dopt=abstractplus&list_uids=1717195

    http://www.ncbi.nlm.nih.gov/entrez/...=Retrieve&dopt=abstractplus&list_uids=6126289

    http://www.ncbi.nlm.nih.gov/entrez/...=Retrieve&dopt=abstractplus&list_uids=1678254
     
  9. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    Re: Is rectal admin of morphine increase bioavailibility???

    I have tried both laying on his side and back, and for the first 5-10 minutes, the side laying method does seem a bit more efficacious. Lubrication is also key as SWIsklander said, it makes the process completely painless for SWIM.

    As SWINicaine mentioned too, many factors influence the absorption for the rectal route. I find that the presence of feces is a big one...so make sure to go to the bathroom before plugging. Some substances apparently make people want to go to the bathroom after rectal administration, but opiates seem to be an exception due to their smooth muscle constriction and water retention action, this might make it a bit easier for the product to go where its supposed to rather than making one have to take a dump.

    As an aside, a year ago SWIM never thought he would be making this kind of post, but the ease and efficacy of this route has really made SWIM a fan.
     
  10. Nicaine

    Nicaine Titanium Member

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    Re: Is rectal admin of morphine increase bioavailibility???

    I was just researching, and came upon two important points.

    (1) More fluid volume (within limits) means contact with more intestinal surface area and thus better bioavailability. Don't plug 2cc's, plug 8 or 10cc's (still not enough to get the feeling of having to 'go').

    (2) Increased pH generally means better rectal absorption. So dissolve a little baking soda in with whatever is being administered! This one was a real gem, I am going to experiment with it *immediately*. Increasing pH is also supposed to be helpful for sublingual absorption, and (for all I know) perhaps snorting as well.

    Another point of research: http://psy.psychiatryonline.org/cgi/content/full/40/3/185
     
    Last edited: Nov 21, 2006
  11. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    Re: Is rectal admin of morphine increase bioavailibility???

    I think that increased pH would really help for opiates as well, good find, swiNicaine! Opiates are generally quite basic (hence the term 'opium alkaloids') and increasing the pH of the stomach speeds absorption, it stands to reason this would help in the rectum too. Hadn't thought about this one before, but SWIM might try it this week and report on the results. I am going to attempt this with Tagamet and oxycodone! It seems like this would really help with morphine, which has a pretty low bioavailability through most routes.
     
  12. Nicaine

    Nicaine Titanium Member

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    Re: Is rectal admin of morphine increase bioavailibility???

    SWIM loves the way he keeps learning new stuff. Apparently he's been wasting a LOT of ambien administering it rectally. Earlier this evening he tried dissolving the same dosage in liquid, but instead of plugging it he dripped the fluid under his tongue and kept it there for a few minutes before swallowing. Easily double the high he's been getting from rectal zolpidem. He even tried snorting 5mg on a whim, with a faster and more potent effect than he gets rectally. Apparently it's just not one of those drugs that works too well via that route (unless it's a low pH thing too, I dunno).
     
  13. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    Re: Is rectal admin of morphine increase bioavailibility???

    It might be nice to make a thread on which drugs DO NOT work well when administered rectally. The usual heuristic for most pluggin' druggies is that everything works better with the rectal route but as You just discovered, some do not. Hm, wonder which opiates may not work well rectally (if any!)
     
  14. DrMuffy

    DrMuffy Silver Member

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    Re: Is rectal admin of morphine increase bioavailibility???

    Yes SWIsklander, you do not have to lie on our side for 20 mins, but SWIdr has found this adds a fair amount to the experience. SWIdr has also tried plugging it and had to get up to answe his tele, and felt that it decreased the effects sligthly and created a stronger urge to use the restroom. But thats just SWIdr's opinion, to every man his own...
     
  15. Nicaine

    Nicaine Titanium Member

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    Re: Is rectal admin of morphine increase bioavailibility???

    More on this (admittedly fascinating and somewhat unpredictable) route of drug administration:

    http://aappolicy.aappublications.org/cgi/content/full/pediatrics;100/1/143

     
  16. tehsyfdan

    tehsyfdan Newbie

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    Re: Is rectal admin of morphine increase bioavailibility???

    I tried morphine rectally last night and he found virtually no effects whatsoever. I was very sad indeed. But I am concerned that maybe he didn't insert the syringe far enough in. SWIM inserted it as far as he could and injected the solution. Then SWIM layed there for a good 20 minutes waiting for something to happen and nothing really happened. I used a 15mg extended release, so I am thinking perhaps he should try two of those.
     
  17. Psych0naut

    Psych0naut Platinum Member

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    Re: Is rectal admin of morphine increase bioavailibility???

    *delete*
     
    Last edited: Jan 4, 2007
  18. Nicaine

    Nicaine Titanium Member

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    Re: Is rectal admin of morphine increase bioavailibility???

    It's possible that little or no morphine was released from the pill constituents. XR tablets are typically made to release the active drug very slowly over certain pH ranges, and sometimes even crushing + adding water will not do the trick.
     
  19. Forthesevenlakes

    Forthesevenlakes Platinum Member

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    Re: Is rectal admin of morphine increase bioavailibility???

    Perhaps the dosage was too small or other factors influenced it as well. Make sure to go to the bathroom before rectal administration, it might seem like a minor factor but I say that it can make a LOT of difference. Also using a larger amount of water seems to help. I use about 10 mL (divided between 2 syringes) for a pill.

    What is you's normal oral dose with these, when he/she gets recreational effects? 15 mg is a lot for a person without opiate tolerance, and they would probably feel that amount orally, but perhaps You has a larger tolerance than that. And as Nicaine said maybe simply crushing the pill wasnt enough to disable the time release. Finally, some people simply dont find morphine to be a very noticable or salient high, and morphine is often said not to be euphoric by some. Perhaps You would get more euphoria from a different opiate.
     
  20. Nagognog2

    Nagognog2 Iridium Member

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    Re: Is rectal admin of morphine increase bioavailibility???

    From older literature I read, morphine was thought by medical authorities to require @60mg orally to equal 8mg I.V. This was oral - not rectal. Apparently, though, morphine is active rectally. There used to be suppositories on the market that were opium-based. These were called Pantopon - as I recall. I don't know if they are still made.