Dose dumping to increase bio?

[LeChuck]

I was reading the wikipedia article (http://en.wikipedia.org/wiki/Oxymorphone) on oxymorphone and it said if it's taken orally with alcohol the bioavailability is increased from 10% to 70%, due to a phenomenon called dose dumping (http://en.wikipedia.org/wiki/Dose_dumping)

Has anybody noticed this? I've yet to try it and am a little reluctant to experiment in case the dumping works really well as I tend to get sick on the combination of alcohol plus opiates, when I've had more than a drink or two anyway. So, questions: does it work? How much alcohol should I use? Does it work for IR and ER or just IR? I only have the ERs and it seems the only thing to do with them is snort them, and the bioavailability has to be quite a bit under 70% so if the alcohol combination really works that would be pretty fucking great.

[Synack]

yes, it works - continue reading the source article, it tells you how much ethanol was administered. If it's not on wiki, check out the full prescribing info for opana ER... I know for a fact, it's there.

You should probably post your findings in case someone else has the question :)

If you still can't find it, I'll look it up for ya later.

[Restharrow]

I read the complete study that is linked to the Opana.com site. They used a LOT of alcohol for their study to acheive the 70% absorbtion.

IME a beer with Opana seems to increase the potency a lot. I do NOT like to nod, so I usually avoid alcohol with opiates.

Be careful.

Will

[Paregoric Kid]

alcohol raises the bioavailability of most opiates/opioids, through enzyme inhibition and increased absorbing properties. that combined with the fact that alcohol also causes dose dumping with many pills that are controlled and extended release means it has a dual effect at increasing the effects of ER and XR opiates/opioids.

[Chipper]

Alcohol is a great "carrier", as well; my mate has HIV and his viral load is very high. He has been advised by his primary doctor to take his meds with alcohol (he chooses apple cider) to increase their effectiveness.

[HistoryofMadness]

all that article on dose dumping is really talking about is a combination of potentiating with other drugs, breaking the extended release to make them instant, using alcohol or other acidic substances to open the cells in the mouth to make buccal or sublingual drugs absorb better, or just jacking up your plasma levels with some super-high fatty foods to increase oral bioavailability...

there are many ways to jack up the intensity of your "dose" and its to me "dose dumping" is just a slang way of saying your'e abusing your meds, or you're getting fucked up on the poly-substance plan...

i used to call my DOC "Polly" because I'd just cross a few drugs together to get the best effect.. i mean i loved dilaudid but i'd almost always kick it in with a little alcohol and some other drugs to get the "perfect high"

chasing the fucking rabbit.... that's "dose dumping"

[Paregoric Kid]

dose dumping is basically turning an ER or XR pill into an IR, or mostly IR. thats different than potentiating through enzyme inhibiting, etc.

[digby]

The difficulties that come from adding alcohol to the opiate mix are the wildly differing increases experienced by different users of the drug. I read one study on dilaudid where the subjects were all given an antagonist prior to IV injection to eliminate effects of toxic overdose, and when alcohol and hydromorphone were administered together, the addition of one ounce of 70 proof alchohol increased the effects of the dilaudid anywhere from 2X to 16X among the test subjects. I believe the average was around 6 fold increase in effects.

If a person combined the two chemicals and expected a four-fold increase but experienced an 8 or 10 fold increase, I can see how OD's happen when combining alcohol to the mix. I know it isn't something I'm willing to personally experiment with.

[antifox]

I read it was around 100ml-125ml to cause that 10%-70% jump. I could be wrong but that's only 2.5-3 beers.

This is what I remembered reading, I could be wrong, but I am almost positive it's not THAT much alcohol.

Remember when you dose dump, the range varies just like with any other BA. So if it jumps to 70% that could be +/- 30%. Be careful.

[digby]

Below is the link to the data from a pharmacological test used by the FDA on Palladone when combined with alcohol.

http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProvi ders/ucm129288.htm

[Synack]

The full prescribing information for Opana ER is here: http://www.endo.com/PDF/OPANA_ER_PI.pdf

You interested in the data listed at the end of page 5.


Ethanol Effect

In Vivo OPANA ER Formulation-Alcohol Interaction

Although in vitro studies have demonstrated that OPANA ER does not release oxymorphone more rapidly in 500 mL of 0.1N HCl solutions containing ethanol (4%, 20%, and 40%), there is an in vivo interaction with alcohol. An in vivo study examined the effect of alcohol (40%, 20%, 4% and 0%) on the bioavailability of a single dose of 40 mg of OPANA ER in healthy, fasted volunteers. The results showed that the oxymorphone mean AUC was 13% higher (not statistically significant) after co-administration of 240 mL of 40% alcohol. The AUC was essentially unaffected in subjects following the co-administration of OPANA ER and ethanol (240 mL of 20% or 4% ethanol).

There was a highly variable effect on Cmax with concomitant administration of alcohol and OPANA ER. The change in Cmax ranged from a decrease of 50% to an increase of 270% across all conditions studied. Following concomitant administration of 240 mL of 40% ethanol the Cmax increased on average by 70% and up to 270% in individual subjects. Following the concomitant administration of 240 mL of 20% ethanol, the Cmax increased on average by 31% and up to 260% in individual subjects. Following the concomitant administration of 240 mL of 4 % ethanol, the Cmax increased 7% on average and by as much as 110% for individual subjects. After oral dosing with a single dose of 40 mg in fasted subjects, the mean peak oxymorphone plasma level is 2.4 ng/mL and the median Tmax is 2 hours. Following co-administration of OPANA ER and alcohol (240 mL of 40% ethanol) in fasted subjects, the mean peak oxymorphone level is 3.9 ng/mL and the median Tmax is 1.5 hours (range 0.75 – 6 hours).

Co-administration of oxymorphone and ethanol must be avoided.

[Indy]

8 ounces of whiskey...that would just ruin the buzz unless you've got a damn high alcohol tolerance.

[digby]

It makes sense with the information that you all have posted that oxymorphone effects would be increased (as it is with almost all opiates) but less so than extended release hydromorphone (palladone) - otherwise, what basis would they have had to make palladone dangerous and illegal due to increased risks from mixing with alcohol but finding Opana to be safe and therefore legal?