Opioids Optimal ROA for naloxone with oxycodone

[mindtools]

Hey guys,
I hope of getting some Targin soon - these are prolonged release (retard) tablets consisting of naloxone and oxycodone (in HCl form).
Unfortunately if I even get it, I'll get very little.

So I was wondering if there is a more efficient way of consumption than simply swallowing it.
I know that because of naloxone it wouldn't be wise to inject it (also, I don't want to inject any drugs that aren't in ampules meant to be IV'ed/IM'ed).
What do you think about plugging/snorting or at least parachuting it?

pzdr

 

[tricomb]

orally

 

[Tommyboy]

^ Agreed.

Considering that oxycodone has a very high oral BA and naloxone isn't really active as an antagonist at those doses when taken orally, I suggest just eating it. Since oxycodone has a lower intranasal BA compared to oral, and since naloxone can antagonize when administered intranasally, it's yet another reason why you should take it orally.

The only other ROA that might be worth trying is sublingual since oral and sublingual administration of naloxone only effect the GI tract by helping relieve opiate/opioid induced constipation.

Parachuting it wouldn't really help with faster onset unless you are doing it with extended release pills with a coating or time release mechanism. Instant release pills already work pretty quickly, but if you really feel like parachuting it then I see no problem with doing so. There was a medication that had naloxone coated in wax which was supposed to prevent crushing it since they claimed that it would activate the naloxone, but the medication was taken off the market relatively quickly, so it probably didn't work. I forgot the name of the medication, but it was morphine with naloxone, and the combination was used primarily as a deterrent against abuse. I don't think that's the case with Targin so it shouldn't be an issue. I would still just take it orally though, or crush it up before swallowing and drinking a glass of water to help it hit you faster.

 

[tricomb]

^Is it MS Mono? The 24 hour morphine/naloxone combo IIRC.

 

[RedRum OG]

Whoa whoa whoa.... Since when is anything except bupe combined with naloxone? I feel really stupid but if you take a full agonist with naloxone wouldn't that be like instant precip withdrawals? Or possibly blocking effects?

 

[tricomb]

There are quite a few medications containing naloxone, which does not induce PWD taken as directed since the naloxone is basically inert via the oral ROA.

 

[sekio]

Naloxone is exceedingly poorly absorbed via the oral route, hence why people don't give oral Narcan & a lot of these "abuse deterrents" don't actually work to deter abuse via oral roa.

 

[Tommyboy]

^Is it MS Mono? The 24 hour morphine/naloxone combo IIRC.

It was called Embeda. The name just came back to me. It was a capsule filled with tiny beads that all looked the same, but some of them were naloxone coated in wax, and the others were the morphine. The idea was that patients couldn't tell the beads apart, and were told that if they crushed the wax beads containing the naloxone that it would cause precipitated withdrawal. I don't think that there was enough naloxone in it to cause precipitated withdrawals when taken orally, unless maybe you took a very high dose, and crushed all the beads when doing so. It was probably just a scare tactic, but a cruel one at that whether it would cause PWDs when crushed or not.

 

[sekio]

I always thought the only benefit of adding naloxone to opioid preps was to (temporarily) deter IV usage anyway. Not that you'd wanna inject morphine in wax.

 

[tricomb]

Oh yeah, Embeda, I remember that one now.

 

[mindtools]

Thx for replies guys

That sucks, as I'll be happy if I'll get 20mg and I'm quite tolerant to opiates (although oxycodon is new for me).

 

[mindtools]

Ok, if I'm lucky, I'll get a bit more than I thought.
Recently I got to know my tolerance: throughout yesterday (first dose at 11am and last at 11pm) I've snorted 3,6mg of buprenorphine and felt good. I wasn't nodding out (just a bit after the last dose) and despite spending most of the day with my parents, they didn't notice anything.

Conversion of 4mg of oral bupe (I was snorting it) is said to be equivalent of 50-100mg of oxycodone (also oral). here

So I'm thinking about parachuting about 75mg. Do you think I should do more?

pzdr

 

[chase_in_56ace]

Embedda... I remember that

 

[Torsades]

According to this this article from the TGA or Therapeutic Goods Administration (Australia's FDA), trials have shown that if the combination of Oxycodone and Naloxone are administered either in instant or controlled release formulations, the analgesic effect will be the same. One might interpret these findingsto mean that the tablets could cause dangerous overdose if crushed and swallowed. If anyone has heard otherwise, please speak up though.
The studies of note in this article (after a quick perusal) are mainly OXN1008 and 1018 to a lesser extent (search for the number).

Study 1008 was a single dose comparison of the 40/20 tablet(Targin - Oxycodone and Naloxone)with oral solutions of oxycodone and naloxone given together[20mg Oxycodone IR (Instant Release) - OxyIR plus 10mg naloxone IR solution). This demonstrated bioequivalence with regard to AUC [Area Under the (plasma concentration time) Curve] for both oxycodone and naloxone-3-glucuronide. The Cmax(maximum plasma concentration) for the Targin tablets were only 29-37% of those for the oral solution, as expected for a prolonged release tablet (p5, AusPAR, 2010).

AusPAR (Australian Public Assessment Report) for Oxycodone Hydrochloride/Naloxone Hydrochloride 'Targin' (Mundipharma, Pty Ltd)
Australian Government: Department of Health and Ageing. Therapeutic Goods Administration. May, 2010.
https://www.tga.gov.au/pdf/auspar/auspar-targin.pdf