Opioids Targin (oxycodone/naloxone) best way to consume?

[Chala]

Thank you so much for the detailed information. I?ll try it the water method and I will post back to let you know how I go.

This morning I tried crashing 2 pills as much as I could but still didn?t get the euphoria I get with OxyContin alone, if anything I felt like I was having withdrawals within 20mins and it gave me a lot of stomach cramps. I think naloxone definitely still works even when you take it orally

 

[kaosisallwesee]

This may come under synthesis, if so I'm sorry. But from what I've read the naloxone is fairly soluble in methanol, whereas oxycodone is only very slightly soluble.

 

[G_Chem]

Thanks Jeckyl I must have looked at a faulty source for the solubility of oxycodone HCl..

Chala do NOT use that method, if you did hang on to all liquids. The Merck index is a lot more reliable than whatever site I must have pulled up yesterday.

Back to square one. To be honest their solubility look to close, their stability is too close and their MP/BP too close.. Gonna be hard to separate.

-GC

 

[G_Chem]

After looking, the solubility in methanol does vary a decent amount. I saw one source that said Naloxone HCl is 50mg/ml and oxycodone is only "slightly soluble in methanol."

Slightly soluble is defined as .1g-1g per 100ml. Let's assume right down the middle at .5g or 500mg/100ml which would be 5mg/ml.

Oxycodone HCl should be only a tenth of the solubility of naloxone in methanol.

Start with 1ml methanol per 5pills then tweak it from there withmore methanol until you feel it detrimental to the positive effects.

Methanol can be found in almost pure form in some products meant to defreeze your gasoline in the winter.

And this is purely drug purification, no synthesis involved.

-GC

 

[Chala]

I tried the water method and it didn?t work. Got palpitations and got very sweaty so I think I may just leave it as I think naloxone seems to to almost impossible to separate from the Oxycodone and the last thing I want is to have withdrawals. I have been taken OxyContin for over 7 yrs for my severe osteoarthritis on my back and my spasms and my doctor won?t increase the dose of 20mg daily. He thinks panadeine forte and the oxy should be enough to manage it but it isn?t. I really feel this is because I?m a female ?
After having 2 c sections and pelvic disfunction my back it terrible regardless of physio and swimming. I can?t take anti inflammatory meds so it gets really hard sometimes.
Thank you to all that have taken the time to tried to help me out ?

 

[Jekyl Anhydride]

Naloxone goes through extensive first pass hepatic metabolism so as long as you plan on eating the Targin, extracting shouldn't be necessary. I would def mention the frequent flyer miles to the bathroom to your Doctor though.

If you just switched from a stronger dose of OXY to the weaker Targin, it might not be the Naloxone causing the problems but mild WD's from the dose change. Also using Panadeine forte (Codeine) for pain seems like cruel & unusual punishment.

 

[Chala]

Thanks Jekyl Anhydride I will definitively mention it to my doctor ?

 

[kleinerkiffer]

While naloxone undergoes high first pass metabolism it can still block opioid receptors in your gut

This controlled study demonstrates that orally administered naloxone improves symptoms of opioid associated constipation and reduces laxative use.

https://journals.lww.com/pain/pages...=2000&issue=01010&article=00013&type=abstract
I couldn't find the enzyme responsible for the metabolism, but the major metabolite seems to be naloxone-3-glucuronide (https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8535cc84-ad4a-4d67-8480-fb5a2e3406f8) so I guess it's metabolized via UGT and afaik there are some highly polymorphic isozymes, this means that some people might not metabolize naloxone as good as others, leading to systemic effects.
With codeine some is metabolized into morphine via CYP2D6, but some people have no functioning CYP2D6 enzymes so codeine isn't as effective.

This all means that it's possible that the naloxone in the targin might inhibit some of the analgesia and switching codeine for something else, dihydrocodeine for example, might be a good idea

 

[Keif' Richards]

This seems to be a lot like a "how to I get higher" thread. We're not here to help people get as fucked up as possible. These control mechanisms that are being compounded with the drugs are intended to make them unabusable. What do my fellow mods think?

 

[Chala]

It wasn?t to get higher actually it was because I was switched to targin and it didn?t work no way near as good as the OxyContin alone. It also seemed that it didn?t let the codeine work at all and it gave me diarrhoea and really bad cramps as well as withdrawal effects. My Doctor gave me 2 boxes of the targin 20/10 and they are useless so I was looking for ways of not wasting them. I am seen him on Monday and will ask to switch back as they don?t work for the pain and they have been horrible to take.

 

[RandomClean3]

I have found out that the rectal absorbtion of nalozone is 15% but I think that's too much. Only things I can think off is adding a base since their solubilities may change, find something that will precipitate only one of them but they're neearly identical, I don't think it can be done. I started wondering if electrophilic addition may attack the double bond of naloxone and somehow crash it out of solution and this is a crazy person talking, I'll just eat them fucking things..

 

[WellTram]

I use 20/10 pinky ones. The best ROA is ORAL. At 40mg i am fine for 5-10hours. If i dose more, i Will be Happy, comfy, painfree and slightly sedated on top of motivational high. By using more i mean 200/100, in 2 daily doses And after subtle comeup i am Věry satistied.

 

[Jabberwocky]

Naloxone definitely numbs effects of oxy. I took 60mg these with zero tolerance (i am not opioid naive though) and got dull effects, i would say The high was same as i took 20-30mg oxycodone without naloxone(i crushed The pills and took them All at once), i have tried this many times... When i took oxycodone (without naloxone) 60mg i got pleasant high and i was enjoying myself.

 

[sekio]

Normally speaking naloxone has a BA of 1-2% orally.
There was a case of a 65 year old cancer patient with liver damage who seemingly absorbed more naloxone than usual and resulted in an OD after switching from oxy+naloxone to just oxy[ref] bur that is not common in healthy people.

Alfa Aesar says, for naloxone HCl, "Soluble in water (73 mg/ml), ethanol (3.3 mg/ml), methanol (50 mg/ml) and dimethyl sulfoxide (73 mg/ml). Insoluble in ether".
Another reference " Soluble in water, dilute acids, strong alkali; slightly soluble in alcohol; practically insoluble in ether, chloroform.".
I cannot find data for the freebase sadly.

You may be able to seperate the two because naloxone has a 3-hydroxy and oxycodone has a 3-methoxy: the same factors allow morphine and codeine to be separated.
Presumably in strong base (for morphine, calcium hydroxide is usual) the naloxone will form a water soluble phenolate, and the oxycodone remains as a precipitated freebase, which can be extracted with dichloromethane or chloroform, and turned back into a salt by adding a measured amount of acid.

But for me, I'd just eat them as they are meant to be taken...

 

[carbonhalo]

Targin uses a crystalline matrix to regulate release. Chew them up fine for immediate release.
I graduated to naloxone free immediate release by telling pain clinic targin kept me awake, and I wanted more granularity between pain/fuzzy thinking.
Not sure what my cytochrome balance is as I have a connective tissue disorder which a rheumatologist once told me would affect my sensitivity to many pharmaceuticals.(but I couldn't drag out the mechanics of that statement from him)

 

[NurofenPlus]

Sorry to resurrect an old thread, but just came across it while googling. So I’ve been on Targin for a few months after bupe patches were useless. Only overnight at the moment with codeine all day (which is what they’ve been trying to deprescribe for about 8 years).

Anyway, I randomly had a couple of these in my mouth and didn’t swallow them, so inadvertently sucked off the blue shit. Half hour later the opioid blanket wrapped me up like I used to remember, like codeine did 15/20 years ago haha.

So that’s nice. I’m def opioid dependent as I’ve been taking them for decades (I presume, anyway - I’ve never gone through it thankfully, somehow managed to never completely run out so start tapering when I start running low), but the naloxone in oral form doesn’t cause any noticeable wd. It does seem to help with the GI part, no longer shitting a dry brick once a week.

 

[4DQSAR]

Just eat them. If you are prescribe a modified release formulation, be aware that slowly pain clinics are realizing that for a reasonable proportion of patients, those modified release fomulations do not act for as long as is stated.

This is almost certainly why the US saw an oxycodone epidemic. Because the makers of Oxycontin tolde their reps to advise doctors that if their medication did not last as long as stated... increase the dose.

In 99% of patients, simply switching to a lower dose taken more frequently (so the dose over 24 hours remains unaltered) solved that issue. But of course it's not the most PROFITABLE solution.

Never ever trust a drug rep. The conflict of interest makes them worse than useless.

 

[NurofenPlus]

Just eat them. If you are prescribe a modified release formulation, be aware that slowly pain clinics are realizing that for a reasonable proportion of patients, those modified release fomulations do not act for as long as is stated.

This is almost certainly why the US saw an oxycodone epidemic. Because the makers of Oxycontin advised their rept to advise doctors that if their medication did not last as long as stated... increase the dose.

In 99% of patients, simply switching to a lower dose taken more frequently (so the dose over 24 hours remains unaltered) solved that issue. But of course it's not the most PROFITABLE solution.

Never ever trust a drug rep. The conflict of interest makes them worse than useless.

Couldn’t agree more. The duration of action is what worries me, they don’t last 12h, 6 maybe 8 (they keep me through the night, but I’m starting to hurt come morning, when I go back to IR meds).

Aim is to switch entirely at some point. I’ve got not intention of abusing them, I don’t get enough to even consider that these days.

 

[4DQSAR]

Well, I got my Oxylan swapped from two large doses to three smaller doses and it worked.

Obviously I have no way of knowing how common this is. GPs seem to feel that they must abide by BNF protocols but all of the consultans I've seen were comfortable with the swap. So they write to the GP so IF something goes wrong, the consultant is responsible, not the GP.

 

[NurofenPlus]

Well, I got my Oxylan swapped from two large doses to three smaller doses and it worked.

Obviously I have no way of knowing how common this is. GPs seem to feel that they must abide by BNF protocols but all of the consultans I've seen were comfortable with the swap. So they write to the GP so IF something goes wrong, the consultant is responsible, not the GP.

That's good! Yeah, I've been very clear that I don't get 8-12 hours, more like 6-8 at best; similar with IR pills, 2-3 hours instead of 4-6 hours, not just painkillers, seems to be across the board.

Thankfully I have had the same GP for a long enough time, they're actually more flexible than the specialists have been, which is good given the narrative here in recent years. But my MME isn't huge compared to some, not going to pretend it's perfect but I can get by and it means I don't end up on the radar, either at my own reviews or when the powers that be are looking at who is prescribing what, so it's ok.