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Rectal pure Morphine HCl

And according to this, Intrarectal SR morphine has a delayed onset, and lower peak plasma levels, albeit reduced first pass metabolism (longer duration? Seems likely, compared with the absorption profiles of other opioids taken rectally, and morphine's solubility) compared to PO


https://www.ncbi.nlm.nih.gov/m/pubmed/1464164/

This one concludes that it is "still difficult to determine whether oral morphine can be replaced by rectal" in CHRONIC morphine treatment- the rest doesn't have much in the way of the juicy figures , although AUC of (presumably single dose) rectal morphine was slightly higher than by mouth, although steady state concentrations of morphine were apparently about the same (no "significant differences")

Https://www.ncbi.nlm.nih.gov/m/pubmed/10217341/?i=2&from=/1464164/related

Point is, it can take longer(apperantly) and the data is almost confoundly conflicting - with acute administration, though, rectal, done properly would seem to be less variable in terms of BA%/potency, with reduced first pass metabolism- it is, still, an experiment, until you become accustomed and find your own method/procedure, and if it works for you, then you have found a viable way to enchance your morphine - First time users should read over some of the data and realize morphine isn't a rapid acting drug by any non parenteral route
 
Ok, another pair

This is the more important one(ime)

https://www.ncbi.nlm.nih.gov/m/pubmed/4054201/

It claims that rectal absorption of morphine was "drastically " effected/improved by PH(adjusting)
It says a PH of 7 to 8 would be efficient

It demonstrates the importance of PH with opiates / opioids in general, and that rectal absorption of morphine is effected, and can presumably be improved, by adjusting it



https://www.ncbi.nlm.nih.gov/m/pubmed/1570227/

The above says rectal mscontin(or something similar) had a Tmax of 5hrs, vs 2.5 for PO, and ~ 70 minutes for rectal suppositories

Could this be added to morphine megathread? Hmm
 
I could definitely see how raising the pH slightly would be worthwhile, Also, I think you would have to screw up pretty badly to accidentally freebase the morphine in this scenario, not saying it wouldn't happen, but if you are using a moderately weak base and have some understanding of what level of change is going to be induced by certain amounts, you shouldn't accidentally add 10x the amount necessary.
 
Lorne??? said:
Ok, another pair

This is the more important one(ime)

https://www.ncbi.nlm.nih.gov/m/pubmed/4054201/

It claims that rectal absorption of morphine was "drastically " effected/improved by PH(adjusting)
It says a PH of 7 to 8 would be efficient

It demonstrates the importance of PH with opiates / opioids in general, and that rectal absorption of morphine is effected, and can presumably be improved, by adjusting it



https://www.ncbi.nlm.nih.gov/m/pubmed/1570227/

The above says rectal mscontin(or something similar) had a Tmax of 5hrs, vs 2.5 for PO, and ~ 70 minutes for rectal suppositories

Could this be added to morphine megathread? Hmm
Click to expand...

Yup. Good points and nice refs Lorne. Not only does research support the issue regarding Morphine and Ph, I can say from personal experience that it does indeed make a very significant difference. I typically will follow the instructions for making a Baking Soda antacid in water. This means 1/2 a teaspoon in a 4oz-6oz glass of water, then I use said water as the vehicle for the whole process. If your Morphine is already in solution, you can use some basic math to figure out the best way to adjust the Ph to the best level.
 
Yes I think it might eliminate a lot of the variability associated with rectal morphine, which seems pretty much the only alternative to a needle if you don't want to take it by mouth(sublingual isn't very good, although you could adjust ph in theory, intrarectal would be better)

It, and different dosage forms (suppositories vs solution, and yes, they have actually administered mscontin or equivalent intrarectally)

Your method seems well thought out, of course people will have to likely experiment a coupke times to find there method, however, with morphine being fairly common, and the PH issue(not to mention the variability) we really one or two "go - to " methods, and to let people know about PH possibly, so they can maximize their morphine via this ROA and have a better shot at a quick onset and decent BA% (ime)
 
^Yes, I think at any rate, everyone who is able should contribute their experiences to the discussion. I understand that it's highly subjective and anecdotal, but I think we just don't have enough information about rectal Morphine administration. Even the medical community is at an apparent loss, as the Bioavailability is stated as being anywhere between 40% - 70% or higher. There are many variables at play, but it would seem that Ph of the solution and probably the membranous walls of the rectum/colon are probably the most significant.

Please guys, contribute your experiences! I don't use Morphine but once in a blue moon.
 
Yes, in that case it would be good to know what ph the morphine goes from being a salt to being a free base. I believe that the maximum pH at which a concentration of sodium bicarbonate can reach is 9. I will try this method next month and publish the results.

Regarding the margin of dose rectally, it is evident that there are few studies.
In order for rectal administration to be feasible, it is necessary to follow some steps carefully:
1. Empty the rectum with an enema.
2. Adequately dissolve the active ingredient in a minimum of sterile water.
3. Connect the syringe at least 3-4cm inside the rectum.

I'm sure that many people do not have good effects rectally because they do not clean their rectum well and use too much water for injection.


DocLad
 
^ Good

You know it occurs to me, with <5ml of water, you could perform a basic enema - well make a glass of water, add a teaspoon or two of baking soda, then use a (preferably) 5ml (or larger, although a 3ml should work) draw up the water, and perform the enema - This shall raise the PH, giving the morphine a better environment - Grabted studies say at PH 7-8 absorption is "drastically improved, however a PH enchancing enema would have two purposes, cleaning, and raising PH. Just a thought
 
The enema that I use for the emptying of the rectum is called Micralax, it is a very used laxative where I live and it works very well. When I do the bowel cleansing (twice a year) I use Bhoom Evacuating Solution, which should be drunk one every 15 minutes for 4 hours, this medication literally empties the intestines completely.
Regarding the enema for colon cleanse I've no problem.

For the psychoactive solutions I don't like to use more than 1ml of water, if I could add the sodium bicarbonate next to the Morphine it would be preferable.

Do you think there is any advantage in rectally administering bicarbonate before morphine?


DocLad
 
Just curious if anyone has had luck with plugging the ABG 30mg morphine pills. I?ve tried and gotten some effect but it seemed about equal to oral. These are the ones that gel, do you think raising the PH would work well for them?

I always feel like i?m wasting so much with them because pretty much the only choice i have is to take them orally.
 
Do you have many tablets? In that case I would try to separate the morphine from the gelling agents and the other components looking at the solubilities in different solvents. I've no experience with these tablets since I've pure hcl morphine, I can't help you much.

Another important point is tolerance. Do you use Morphine sporadically? Perhaps by reducing your consumption you could obtain greater effects of the pills.


DocLad
 
@ Falsified: What is your method?

You gotta grind those things down finely and you really need 1ml per tablet

And yes, raise the PH slightly; if done correctly it will speed absorption and could double the potency

Surely you could hit 50% with right technique?
 
I usually chop one into 4 pieces, let my tap get as hot as it can get, which is pretty damn hot, and load an oral syringe with the pills and about 8ml of scalding hot water. Then i shake it vigorously for 5-10 minutes but the pills don?t dissolve completely, there is still some jelly in the syringe.

The gelling agent seems to impede the absorption by delayed action, i can?t remember if the duration was longer then oral but i only remember the onset and peak being very slightly better than oral. It?s been a little while since i had these pills but i?ll probably get them again.
 
You need a good razorblade and something to
crush them with (or mortar and pestle) and crush them a bit, then grind it as finely as possible; takes several minutes.

And no hot water; warm is fine; when crushed as finely as possible add 3-5ml of water into a shot glass (with the powder inside) and shake a bit for maybe 40 seconds, load into syringe, and go

You could a bit more water afterwards I suppose, that’s for injection mostly

Morphine was my doc (well aside front occasional H) so
I'm experienced with mscontin/ generic equivalents

I may mod this comment...
 
Last edited by a moderator:
I?ll try crushing them to a fine powder next time but i have a feeling these pills are just stubborn and will still need the high temp water to get better and faster solubility. I shouldn?t need anymore water then 8ml, i?m sensitive to morphine so i should need more then 1-2 of these at a time.
 
Trust me Falsified, I used to bang the ABG’s. They are not the friendliest, however you can pretty much completely dissolve them; and it’s simple when you get the hang of it. I’ve done multiple tablets (at once) with a BD syringe
 
Falsified, I thought you might find this article interesting. I admittedly didn't read through the entire thing in the interest of time, but I think it's the same one I've read before, in which, sustained-release Morphine pills were actually used rectally, with the same or similar results to what one would expect with instant release pills. I found that pretty interesting, but I do imagine that you would do well to thoroughly grind those things down before making solution.

https://www.ncbi.nlm.nih.gov/pubmed/1464164

I really want to say that an enema would be helpful, but with rectal Morphine administration, it's never that simple it seems. I don't know exactly how an enema would effect the environment. Would it effect the Ph of the environment in a non-helpful way? I don't know. At any rate, I think we know that a more alkaline environment is better than a basic one. You will find though, that even the medical establishment seems to be still trying to understand the finer points of this route of administration when Morphine is concerned.
 
^ Yes, however, it depends on the brand; a different brand had a Tmax That averaged 5 hours! Vs 2.5 by mouth (for the same SR formulation) and ~ 70 minutes for a suppository, IIRC

Note that a University did a study with mscontin, in 2 different sessions they extracted ~90% of the morphine. They used cold and warm warm or hot water(?), didn’t make much of a difference, again AFAIK - If you get highly frustrated it’s something to try
 
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