Does rectal admin of morphine increase bioavailibility???

[Wyborowa]

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? Swim is using the 30mg MS contin xtd release....would swim 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!

[Psych0naut]

Insufflation is also more commonly called snorting, rectal is shoving it up your bum.
If SWIY 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.

[Wyborowa]

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

DZIENKUJE!

[Forthesevenlakes]

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

[Fantasian]

Morphine rectally has massively increased bioavailablity, be weary of starting at a too higher dose for SWIY 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 SWIY may want to shit himself. This sensation will pass in around 30 seconds - 1 minute. At which point SWIY should feel comfortable again. SWIF always found lying on the right side made the feeling less uncomfotable while administering rectally.

Best of LUCK to SWIY

[DrMuffy]

Yes taking morphine rectally is much better! SWIM took 30mg rectally and it was amazing. Well swim is 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

Reputation Comments on this post:

Good post!

[Sklander]

SWIDrMuffy - SWIM doesn't think that you have to lie on your side for twenty minutes or else absorption will not take place. SWIM is very experienced with the procedure that SWIY 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.

[Nicaine]

Originally Posted by Sklander

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

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/q...t_uids=1717195

http://www.ncbi.nlm.nih.gov/entrez/q...t_uids=6126289

http://www.ncbi.nlm.nih.gov/entrez/q...t_uids=1678254

[Forthesevenlakes]

Originally Posted by Sklander

SWIDrMuffy - SWIM doesn't think that you have to lie on your side for twenty minutes or else absorption will not take place. SWIM is very experienced with the procedure that SWIY 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.

SWIM has 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. SWIM finds 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.

[Nicaine]

SWIM 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, SWIM is 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/.../full/40/3/185

[Sklander]

Originally Posted by Nicaine

SWIM 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, SWIM is 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/.../full/40/3/185

Great tips, SWINicaine.

SWIM is about to get a few Morphine pills for his pet. SWIM is going to use rectal administration tonight and is going to try putting a touch of backing soda in his 8cc's of water with about 50MG of Morphine mixed in. SWIM tries to make sure that his rectum is fairly clean before he even thinks of rectal administration. Clean your colon and have a great time.

SWIM should be getting the pills very soon and will report throughout the night his findings with using the baking soda.

SWINicaine - Is SWIY talking about a pinch of baking soda mixed with the H20 and opiate and mixing it all together and using that for rectal admin.?

[Forthesevenlakes]

SWIM thinks 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. SWIM is 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.

[Nicaine]

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).

[Forthesevenlakes]

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 SWIY just discovered, some do not. Hm, wonder which opiates may not work well rectally (if any!)

[DrMuffy]

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...

[Nicaine]

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

http://aappolicy.aappublications.org...rics;100/1/143

The rate of rectal transmucosal absorption is affected by the following factors:

Formulation (time to liquefaction of suppositories)
Volume of liquid
Concentration of drug
Length of rectal catheter (site of drug delivery)
Presence of stool in the rectal vault
pH of the rectal contents
Rectal retention of drug(s) administered
Differences in venous drainage within the rectosigmoid region

Anatomical differences in hemorrhoidal venous drainage of the rectum may substantially influence the systemic drug level achieved. Drugs administered high in the rectum (drained by the superior rectal veins) are usually carried directly to the liver and, thus, are subject to metabolism. Drugs administered low in the rectum are delivered systemically by the inferior and middle rectal veins before passing through the liver.155-157 Problems may occur with drugs that normally have a high hepatic extraction ratio. The clinical implications of rectal venous drainage for absorption and metabolism of most drugs are not well-defined.

Diluent volume is also an important determinant of rectal drug uptake, as demonstrated with methohexital administered rectally for preprocedure sedation. Equivalent deep sedation was achieved with 25 mg/kg of a 10% solution (0.25 mL/kg) and with 15 mg/kg of a 2% solution (0.75 mL/kg). Peak blood levels of the drug, however, were significantly higher for a longer time in the children treated with the 2% solution.158 This finding could have important clinical implications for the depth and duration of sedation.

Rectal pH may also influence drug uptake by altering the amount of drug that is ionized. The greater lipid solubility of nonionized drugs enhances their movement across biological membranes.74 The pH of the rectal vault in children ranges from 7.2 to 12.2.159 This pH range favors absorption of the barbiturates that will remain in a nonionized state because their pKa is near the physiologic range (~7.6).

Despite the limitations associated with drug absorption in the rectum, many drugs usually administered by the intravenous and orogastric routes have also been administered rectally. Sedatives commonly administered by this route include midazolam, diazepam, and ketamine.138,140,141 In children, the rectal route is convenient for the administration of benzodiazepines to treat status epilepticus because an intravenous line is not required.146,147 The rectal dose generally must be higher than the dose administered intravenously or orally. The extent of the increase depends on the factors that affect absorption (listed earlier). The most important considerations are the slow onset of effect (minutes) and the prolonged duration of effect (hours). The peak blood levels vary considerably from patient to patient. The potential for rapid and almost complete absorption has serious implications when drugs with cardiac or pulmonary depressant effects are administered. Practitioners must be prepared to monitor the patient after drug administration and to manage an emergency should it occur; equipment suited to the size of the patient is required.160 The patient also may expel an unmeasurable amount of the drug, which makes it difficult for the practitioner to decide how much more of the drug to administer.

[tehsyfdan]

SWIM tried morphine rectally last night and he found virtually no effects whatsoever. SWIM was very sad indeed. But SWIM is 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. SWIM used a 15mg extended release, so SWIM is thinking perhaps he should try two of those.

[Nicaine]

Originally Posted by tehsyfdan

SWIM tried morphine rectally last night and he found virtually no effects whatsoever. SWIM was very sad indeed. But SWIM is 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. SWIM used a 15mg extended release, so SWIM is thinking perhaps he should try two of those.

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.

[Forthesevenlakes]

Originally Posted by tehsyfdan

SWIM tried morphine rectally last night and he found virtually no effects whatsoever. SWIM was very sad indeed. But SWIM is 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. SWIM used a 15mg extended release, so SWIM is thinking perhaps he should try two of those.

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 SWIM says that it can make a LOT of difference. Also using a larger amount of water seems to help. SWIM uses about 10 mL (divided between 2 syringes) for a pill.

What is SWIY'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 SWIY 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 SWIY would get more euphoria from a different opiate.

[Psych0naut]

*delete*

[Nagognog2]

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.

[Forthesevenlakes]

Originally Posted by Nagognog2

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.

This is probably true. SWIM got the 15 mg orally active number from some opiate-naive lab rats who had used at this dosage and had some effects. Granted, their body weight was rather low which may have factored into it. SWIM knows other lab rats who required 60 mg their first time, but he did not want to mention too high of a number for fear that some might overshoot the mark. However, the number stated by the literature is very likely correct.

SWIM has read a couple threads on morphine suppositories which seem to have been made more recently, so those are still around, although probably quite rare. An opium based suppository, though, thats an interesting concept, but it makes sense. SWIM has read reports of plugging poppy tea (which had some of the water evaporated, and the solution cooled, thank god), and it seemed to work well for those involved. So the Pantopon idea seems like a quite feasible one, would likely be very useful for people with concomitant pain and nausea...since morphine is sometimes not tolerated very well when taken orally.

[Forthesevenlakes]

Mixing in a bit of baking soda with the water and opiate would be the best and most direct way to increase the pH of the rectum/colon for absorption. SWIM has heard of lab rats putting a bit of crushed antacid for the same purpose (the non-chewable kind of antacid, Tums in the bum would mean too much volume! Sing it with me!)

[Sklander]

SWIM is about to try a pinch of baking soda about the size of his dose of Morphine. SWIM will let you fellow SWIMMERS how it went in twenty minutes.

Haha... Wish SWIM luck!

*EDIT* SWIM just injected 50MG Morphine into his rectum along with a pinch of baking soda. Administration was completed about ten minutes ago and SWIM's eyelids are already heavy. Thats where SWIM feels opiates first, always... eye lids get heavier and your body is buzzing... SWIM guesses the baking soda thing helps...

[Sklander]

SWIM is feeling great. He ended up taking 100MG total tonight. He administered ~50MG in his ass and insulfated ~50MG about two hours after that.

Morphine is a great drug. SWIM likes the feeling because he feels like he has more control over what he is feeling. SWIM just doesn't like to get sloppy. A friend of SWIM's drove his car through his garage door last night after eating a handful of soma's. He said he remembered eating the pills before he left for his house, which was only about a ten minute drive, then waking up with the garge door smashed in and the car still running. SWIM couldn't stress enough how lucky he was to even make it home. Its better to smash up your own property than to swerve into another lane and kill another human being. He needs to be more careful and think about what he is doing.

His Mom and I have been talking a lot, and I think she is feeling much better after I talked to her and calmed her down a bit.