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PBS refuses to fund oxycodone / naloxone combo

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Flexistentialist

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From the Age recently:

Cabinet 'no' to heighten the pain
Mark Metherell
March 10, 2011

UP TO 100,000 Australians in severe pain face continued distress as a result of a government decision to defer an expert panel's recommendation to subsidise a new painkiller.

The drug, Targin, quells the pain of cancer and other diseases along with the agony of constipation triggered by current opioid painkillers.

It also contains a feature that is expected to cut rapidly growing criminal trafficking in the opioid OxyContin.

But Cabinet has deferred a decision to list Targin for Pharmaceutical Benefits Scheme subsidies, along with six other new medicines, on cost grounds as part of a budgetary crackdown because of what it says are ''fiscal difficulties''.

The director of Pain Australia, Michael Cousins, said the new medicine would help thousands of cancer patients and others on painkillers by ending the gruelling constipation that opioids cause.

This was because the drug was a combination in one tablet of the pain-relief opioid oxycodone and the drug naloxone, which countered the opioid impact on the bowel.

But the catch for illicit traffickers who acquired opioid prescriptions from doctors under false pretences was that once dissolved and taken in liquid form, the drug exposed users to the agonies of withdrawal.

''This is a medication which is clearly a standout. I am very disappointed in this decision,'' said Professor Cousins. He said it was particularly so given the modest cost of subsidising Targin - less than $10 million, according to estimates given to the expert panel, the Pharmaceutical Benefits Advisory Committee.

The growth in abuse of prescriptions for Oxycontin and similar drugs to manufacture ''hillbilly heroin'' has prompted Medicare Australia to launch an investigation into suspect doctors and ''doctor-shopper'' patients.

The committee also recommended the listing for subsidies of other drugs for conditions including enlarged prostate, lung disease, heavy sweating and schizophrenia, which the government has deferred. It has agreed to fund seven other drugs recommended by the committee.

Health Minister Nicola Roxon yesterday denied the government was ignoring the committee. She said the committee could not make decisions ''which prioritise between government expenditure in times when fiscal circumstances are difficult. That's what the Cabinet is there to do.''
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Here's a link to the TGA's decision (pdf)
 
So excuse my ignorance here, but I understood that naloxone was used to reverse an overdose, ie I assume it kind of counteracts the effect of opiates. How come the oxycodone's pain relief effect isn't also counteracted?
 
^ I can only assume there is some extended-release mechanism at play? They noted that users who dissolevd the pills first wouldn't be able to use them recreationally so that could hint towards the same?
 
^ That's it basically. It's an extended release tablet; when used properly, the amount of naloxone released is gradual and small enough to not cause WD. If crushed though, you get it all at once.

From physical stats taken from google, the difference between boiling point of oxycodone and naloxone is great enough (at least 25C) that a simple distillation would be able to separate them. Though the temperatures I am seeing mentioned are 501C for oxycodone and 532C for naloxone (at atmospheric pressure). I wonder if you would see degradation before reaching the boiling point...
 
Hrm interesting idea.

Wonder if the naloxone would help reduce tolerance at all? It doesn't work like that with suboxone, so guessing no.
 
Christ! said:
Hrm interesting idea.

Wonder if the naloxone would help reduce tolerance at all? It doesn't work like that with suboxone, so guessing no.
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Buprenorphine is a partial agonist though, so we can expect a different pharmacology from it then from the full agonist opioids.

For what it's worth though, a user in OD claimed he carried out a Low Dose Naltrexone experiment and didn't notice any reduction in tolerance.
 
belarki said:
^ I can only assume there is some extended-release mechanism at play? They noted that users who dissolevd the pills first wouldn't be able to use them recreationally so that could hint towards the same?
Click to expand...

Isn't it simply to do with first pass metabolism?

My view is this:
Naloxone, when taken orally (as intended) would act as an antagonist locally on the stomach and intestinal opioid receptors, restoring peristalsis and preventing constipation but would be sufficiently broken down in first pass metabolism therefore not crossing the BBB in significant quantities. However sniffing or banging the tablet would bypass the liver and induce withdrawls. It would make sense that the Naloxone is distributed in the same way through the time release mechanism as oxy is.
 
I thought naloxone was only able to cross the BBB when injected but I could be wrong. I don't know it for a fact to be true but your theory of it still being an opioid antagonist in the stomach and intestines makes sense since they are claiming it would stop constipation.

Assuming I am right about naloxone only being able to cross the BBB when injected then this would only really prevent the injecton of the oxy and it has a high oral bioavailability anyway.
 
drug_mentor said:
I thought naloxone was only able to cross the BBB when injected but I could be wrong.

Assuming I am right about naloxone only being able to cross the BBB when injected then this would only really prevent the injecton of the oxy and it has a high oral bioavailability anyway.
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Any drug has a certain ability to cross the BBB which is independent of the ROA (assuming it's not metabolised). What changes is the bio availability which effects whether the drug even makes it into the blood in the first place (a drug can't pass from the blood through the BBB if it doesn't make it into the blood in the first place, if that makes sense).

Naloxone, like say morphine, is highly metabolised by the liver to inactive metabolites (2% of Naloxone gets into the blood system unchanged when taken orally). ROA's such as IV, IM, Intranasal, maybe others; have a a higher bioavailability for Naloxone than the oral ROA as they skip the first pass metabolism process of the body. For that reason there is more naloxone in the blood and hence more to cross the BBB.
 
^ That's correct basically; I'm not sure what your first sentence was saying though, it sounded like you were stating that everything has an ability to cross the BBB which is not true obviously.
 
thats fucking ridiculous... you wanna get high take roxicodone and if you wanna get clean use suboxone.... if there trying to find something for people that have pain and havent taken painkillers yet ... this might somehow be a good idea so they dont geet the euphoric effect of opiates and just the pain killed... but if its meant for some other purpose cause they want to make money and also make peole think that there all worried about getting addicted to opiates and ruining theres lives but then they take targinact and thats there solution thats fucking crazy.... assuming they made it for the wrong reasons ... that drug sounds like a fucking boring combination and why ruin perfectly good oxycodone by mixing it with naloxone ????http://i.bluelight.ru/s/confused.gif??? :?
 
if there trying to find something for people that have pain and havent taken painkillers yet ... this might somehow be a good idea so they dont geet the euphoric effect of opiates and just the pain killed...
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That's not what they are aiming for, and not how it works. The aim is to prevent abuse via nalaxone which is not active when taken orally. Why shouldn't the drug companies work on combinations like this? They do not make their products so that you can get high; they make them to help people and of course to make money.
 
Mr Blonde said:
^ That's correct basically; I'm not sure what your first sentence was saying though, it sounded like you were stating that everything has an ability to cross the BBB which is not true obviously.
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No definitely not saying that. Just saying that each drug has a specific, quantifiable rate at which it crosses the BBB which is independent (not changed) by the ROA.

For example morphines rate at which is crosses the BBB is the same if taken intranasaly as it is if it is IV'd. (of course there would be more crossing the BBB if Iv'd).

THIS IS NEGATING METABOLISM! <- before someone whines why they can't take heroin orally and get a better rush than oral morphine.
 
dude...australia should step up to the game....i mean they got hydrocodone over there, fucking all different types of serious painkillers THAT are used to treat pain
 
^ Well I really don't care much for hydrocodone (I reckon oxy is much better) but I do agree with the general statement. Would be great to see Oxymorphone and Levorphanol hit the shelves.
 
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