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  • BDD Moderators: Keif’ Richards | negrogesic

Oramorph potentiation

shadowhigh

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Joined
Jun 18, 2022
Messages
14
Hi all. I'm currently on oramorph due to various chronic health conditions causing chronic pain.

I've been researching the best way to increase bio-availability via potentiators and I found a few conflicting studies about propranolol. One study suggested that it potentiate opiates, the other concluded that it didn't.

1) Wondered if anyone has an knowledge/experience re propranolol as an opiate potentiator?

The top potentiators that I'm aware of are DPLA, DMSO, promethazine, magnesium, dextromorphene, grapefruit juice.

2) I found a very interesting article about proton pump inhibitors such as lansoprazole and its interactions with opiates. Can anyone suggest the best thread to post/share? https://www.elsevier.com/about/pres...y-opioids-can-cause-gastrointestinal-problems

3) Does anyone know whether amitriptyline should be taken before, with or after opiates for it to act as a potentiator?
 
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Certain potentiators such as grapegruit juice and lansoprazole/omeprazole aren't going to potentiate morphine. They work by inhibiting liver enzyme cyp3a4, suppressing the body's ability to break down and eliminate the drug. This will work for other opioids like oxycodone or codeine, but not morphine because morphine isn't metabolized this way.

Magnesium has muscle relaxation and sleep promoting properties on it's own, but chronic opioid use causes deficiency which may be why it's suggested. But it's a great supplement on it's own and I suggest it.

Propranolol will promote it's relaxation and drowsiness but I don't see how it would help with pain.

Never heard of amitriptyline for this purpose, but you should take it before dosing. Hypothetically antidepressants may blunt opioid euphoria.

I've never heard of a lot of these as opioid potentiators, and in reality they probably aren't worth a whole lot of effort in obtaining. A lot of opioid potentiators are overstated because people often obsess over this topic... and placebo is powerful.

The two I would recommend for sure and I know they work are DXM (dextromethorphan) and promethazine. In terms of raw pain relief, if that's your goal, adding acetaminophen or NSAIDS goes a long way. Black seed oil may be worth taking as well.
 
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thank you so much for your reply!

Yes, my goal is absolutely pain management. It's not about getting high -although, sometimes it's hard to seperate one from the other, seeing as the feeling of euphoria negates the negative effects of pain.

I have crohn's and Ehlers-Danlos, as well as other chronic disorders. I was on buprenorphine patches which, although I had background pain with them, were brilliant.

In terms of longer term pain management I am starting a physio course soon. Eventually I'll be going on a 3 week residential pain management course but it's catch 22 at the moment: I cannot attend an intensive, 9-5 pain management course until my health is in better shape. It isn't just pain that's the issue -it's all the other issues. I've had two bowel surgeries (no pain) which have taken their toll. I used to work in a fast paced IT project management role and, having worked since age 16, had grafted my way up to senior management. Unfortunately, the only way I managed was copious amounts of opiates. At one point I was taking up to fifty 30mg tabs of dhydrocodine each day. That had to end, for obvious reasons, but once I got down to the 'recommended' dose, my career ended. I tried for over a year to work but just couldn't manage it.

The problem I have is that I cannot take NSAIDs because I have crohn's. They are a huge no-no because they can trigger flare ups.

Currently am on oramorph - dose is 15mg every 6 hours but it just is not enough. I don't want to be wasted all day, I just want to get on with my life.

The other problem is chronic diarreah from surgery. Because my terminal ileum was removed I have bile salt diarreah. That was the main reason why I took opiates to begin with. I cannot take cholestyramine (which is the go-to product for Binding bile acids to prevent them from causing diarreah) because I'm on many other medications and cholestyramine can inhibit absorbance.

I'm at the point now where all I can really do to get quality of life is to self-medicate via less legal routes. I have a huge garden and am considering growing poppies. I've heard mushrooms or psychedelics can help but it's not something I want to play around with.

Doctors just shrug and tell me I have to live with it. So, unless I can find something that will potentiate my prescribed medication I'm going to have to take matters into my own hands.

If anyone is able to offer suggestions then I'd be so grateful. I just want to live my life and be a productive member of society again. At the moment, I'm just a waste of air!

PS. I'm actually already prescribed promethazine and am aware of its potentiator capability -I do use it for this very purpose, along with loperamide. One thing that I'm unsure about is the best time to take it. Do I take it before the morphine, after or at the same time?

pps. DXM: I think might do an online 'pharmacy hop' to aquire a supply. Never used it before. Again - when would be the best time to take it?
 
Piggybacking on @Snafu in the Void who explained it well:

Not all drugs are the same in that they can be "potentiated" through the means I believe that you're implying.

First, to define "potentiation" as we will use it here. This word "potentiation" is going to refer solely to the process of effecting a higher bioavailability of a certain drug or otherwise increase that drug's innate potency. In most cases discussed through our service, this implies playing with enzymes. In simple terms, enzymes have a large role in mediating the end-potency of a drug. We have relatively simple means of changing the efficiency of different enzymes.

There are innumerable means of changing the efficiency of these enzymes. Different medications, for instance, SSRI antidepressants are widely prescribed and are well-known for their propensity for effecting the action of these enzymes. It doesn't stop there. Grapefruit and related fruits like Bergamot for instance are known to reduce the efficacy of enzymes of the P450 family (responsible for a SIGNIFICANT proportion of all metabolism of commonly used drugs). The ingredients that lead to this change are flavonoids found within the fruit, but I'm digressing. The point here is that these enzymes are indeed influenceable.

I encourage you to check out google for future sources of this enzymatic change, as they are too numerous to list here. For a more extreme case to help you understand how broad this change can be, check out this reading regarding Methadone patients being treated with the first-generation SSRI Fluvoxamine (Luvox). There are multiple cases of Methadone-maintained patients initiation treatment with Fluvoxamine, only to present at the ED a week or two later one blood levels of the Fluvoxamine reach steady state with symptoms of full-blown Opioid overdose, some requiring ventilation for survival. Here is the link:


Note specifically that they refer to increased serum levels of Methadone. That is true potentiation as we've defined it here. The use of adjunct substances like antihistamines (common), Benzodiazepines, Alcohol or whatever are not the same kind of potentiation. You are just getting more fucked up, which is a different thing entirely. If you enjoy it and you're being safe, great, but you're not truly changing the ultimate potency of the drug in your body. As we all know, the more substances at play, the harder it is for the body and mind to adjust and synergy comes into play, yes, but this is still not potentiation as defined here. It's a completely different thing.

In addition to enzymatic influences, there are drugs like, for simplicity we will again use Methadone are impacted by the alkalinity of the digestive system and urine. Thus, taking antacids can increase the bioavailability of a substance, but this will pale in comparison to what a true modulator like Fluvoxamine can do. For reference, there are reports of Methadone levels increasing by a full 50% with Fluvoxamine. With antacids, you will be unlikely to break 15% on your best days. Furthermore, proton pump inhibitors like Cimetidine both impact enzymes while also decreasing the acidity of the stomach. I am not educated enough to tell you if the two are directly related or not and I've been unable to find that answer myself.

Morphine

To take advantage of the enzymatic processes, enzymes must have a prime role in the metabolism of that drug. Methadone is used as an example, as it is a drug widely known for variances due to genetic/artificial enzyme activity. Morphine is not in this same group. Morphine is a drug that is valued for this lack of complication and a general expectation of similar effects upon most humans.

I've read conflicting information regarding Morphine and antacids, but from what I've read, the only answer I can give is "possibly", but it's not going to be the game-changer that you're looking for, even if you do get that extra 15% we discussed.

The best and most effective way of potentiating Morphine, so to speak, is to change the route of administration to one with a more favorable bioavailability. For this purpose, the rectal route of administration has shown to be twice as potent as oral usage in some literature. My personal experience confirms this fact, at least to myself.

Normally, people go to the needle or vaporization for a quick powerful 100% bioavailability from the drug, but vaporization is not practical with the Morphine medium (or most others available) you're using and injecton carries with it a host of problems that greatly outweigh any benefit one might get from that ROA.

The rectal route is a good way of taking advantage of these differences, with essentially no more danger to your health whatsoever over taking the drug orally. If you're taking Oral Solution, all you need to do is draw up your dosage with a rectal syringe and inject into the rectum. It's a simple process, but if you have questions, I'm here for ya.

Doubling potency is not a solution though. Opioid tolerance builds quickly. You will likely find yourself at this same impasse 1-2 weeks after the change, with a greater dependence and really nothing good or lasting to show for it.
 
Besides the potentiators already mentioned, there's some research that suggests that stimulants like methylphenidate and d-amphetamine can enhance the analgesic effects of opioids. This article summarizes a lot of the available evidence but there haven't been many human studies looking specifically at the analgesic effects of the combo. Of course, adding stimulants into the mix would bring the potential for more side effects and dependence as well as being expensive.

You mentioned being wary of psychedelics, but there is some evidence showing that microdosing has been effective in cases of chronic pain. If you used volumetric dosing for LSD or a good scale for mushrooms, you can be pretty accurate with your doses and not have to worry about tripping.

Also have you tried cannabis? If you are going to go down the illicit drugs route this would be probably the safest option (along with microdosing). Depending on where you live and how much money you have it may even be possible to get medicinal cannabis. I believe Oramorph is a UK brand, so I'm assuming you're from the UK? It is technically possible to get prescribed off-label cannabis through private doctors. If I recall correctly, there's also a medicinal cannabis clinic that's trying to price match street cannabis so that people don't have to get it illegally.

There's also legal cannabinoids like HHC and Palmitoylethanolamide (PEA) that may have some use in pain management.
 
I just want to say THANK YOU for your amazing responses. The time and care that you all have put into your posts in order to help a total stranger out restores my faith in humanity.

I will give these a proper read -but, just to say, I have actually done pretty substantial research on Google already. I came up with a lot of helpful info but I have been lacking in the basics of chemistry.

I want to understand the way these things work as much as I possibly can before messing around with this sort of thing. I even found a massive list of potentiators for a range of different painkillers which was from a study about that very thing.

I forgot to mention a couple of pretty crucial information, which is as follows:

I have Chron's, and a large section of small intestine - specifically, the terminal ileum and appendix - was surgically removed a number of years ago.

One of the functions of the terminal ileum is that it reabsorbs bile acids. Bile acids are produced in the gall bladder, and are released into the digestive system to break down fats. The bile acids are then reabsorbed back into the body via the terminal illeum.

As my terminal ileum was removed, the bile salts stay in my digestive tract. The knock on effect of this is chronic diarreah (there are ways of managing this via cholestyramine but I'm unable to take this because it interferes with other meds).

I also have a Hiatus Hernia which I beleive could also affect things but I do take PPIs.

I'll take care to read through and 'digest' (pun intended) your posts. I just wanted to reply to say thanks and add this info 😀

I beleive that there are issues going on that inhibit the efficacy of the painkillers - even if it is just how my body is. I am aware that some people just naturally have a higher tolerance due to the way the body processes opiates. I've got many reasons to beleive this.

Unfortunately there isn't any testing available to see if this is the case. I know that there's a desire in pharmaceutical circles to tailor the doseage per patient, but from what I understand we are a long way off that.
 
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Hey @shadowhigh sorry to dump more research on you (and sorry if this is stuff you already know) but I was researching some supplements and stumbled on some articles that I thought you might find useful. As Keif mentioned, potentiation will only get you so far, and building a tolerance will reduce the effectiveness of your medication.

There's been some research (largely with rats though) on different supplements that can reduce the buildup of tolerance to morphine.

Taurine: "Combination of taurine and morphine is an effective strategy to attenuate both morphine analgesic tolerance and dependence and this also seems to depend on activity of muscarinic receptors, however through differential cellular mechanisms."

This study found a combination of Tramadol/Paracetamol/Caffeine/Taurine to be more effective than just Tramadol/Paracetamol.

Taurine seems to be analgesic in its own right, but I did find this older study that mentions Taurine reducing the analgesia of morphine? However the first study I linked is more recent and found that the combination of Taurine and Morphine produced the same analgesia as Morphine alone.

This study talks about reduction in Morphine tolerance by using Nefiracetam.

Also, low oral doses of Delta 9 THC can seemingly potentiate the effects of morphine as well as reduce the tolerance buildup.

And in relation to your question about Amitryptilline, I found this study where they gave morphine tolerant rats Amitryptilline before the morphine.

As in our previous study, morphine challenge (15 μg, i.t.) on day 5, 3 h after discontinuation of morphine infusion, produced a significant antinociceptive effect in saline-infused rats, but not in morphine-tolerant rats (Fig. 1a). However, pretreatment with amitriptyline (15 μg, i.t.) 30 min before morphine challenge preserved its antinociceptive effect in morphine-tolerant rats. Amitriptyline (i.t.) alone had no antinociceptive effect in either saline-infused controls or morphine-tolerant rats

Hope this helps!
 
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