Opioid effects gone after short sleep

[Orlando_Doom]

Hey everybody,

so I get prescription pain meds for several years now (Tilidine, it's Sch. I in the US but normally used in EU and halfway between codein/tramadol and morphine)
and, as anybody could guess, am dependent on them.

I do not use them to get high and take my prescribed dose - 3x 150 mg extended release at the moment (recently changed) and instant release for breakthrough. It's always taken orally (naloxone is mixed in and it's also more a prodrug for nortilidine, the actual strong agonist) and onset after swallowing is between 5 and 10 minutes, and instant release lasts about 3 - 4 hours.

Now my problem is if I take a dose and lay down to take a nap, and sleep maybe 30 minutes, which would be ~40 minutes into the dose, I wake up in withdrawal. All opioid effects are lost with basically any amount of sleep over ~15 minutes, and that makes me use more of my meds than I want because I dont want early refills and my doc trusts me, I like him, and I rather get high on other things anyway.

So does anyone know something about this effect, do you know it with other opioids? And maybe what to do about it (besides dosing again)?

Thanks a lot.

 

[DelRi0]

I believe the acute withdrawal symptoms you're experiencing are from the Naloxone, its actually an opioid antagonist which basically means it does just the exact opposite of what opiates do to your body when opiates attach to opioid receptors they 'agonize' them (that's what causes the 'opiate-like' effects), hence why they're called 'agonists' and when used in combination drugs like you're referring to, the Opiates (opioid agonists) are fighting with the Naloxone (opioid antagonists) inside your body. I would recommend talking to your doctor about it first and foremost, as it seems like you may need to lower your dosage or switch to something else. Hope this helped somewhat.

 

[Orlando_Doom]

I know the technical stuff in detail, the naloxone is only mixed in so you cant dose over a certain amount and so you don't inject it (which would avoid the first pass effect in the liver). Naloxone has a first pass effect through the liver where 99% of it is destroyed. If you take more than 400mg Tilidine (which would also contain 32mg Naloxone), enough comes through to the receptors in the brain.

I'm always far below the threshold. Also if I redose immidiately, the full effect is back again. If it was the naloxone, this shouldn't be because it has an acute effect time of about 1 hour.

 

[DelRi0]

I know the technical stuff in detail, the naloxone is only mixed in so you cant dose over a certain amount and so you don't inject it (which would avoid the first pass effect in the liver). Naloxone has a first pass effect through the liver where 99% of it is destroyed. If you take more than 400mg Tilidine (which would also contain 32mg Naloxone), enough comes through to the receptors in the brain.

I'm always far below the threshold. Also if I redose immidiately, the full effect is back again. If it was the naloxone, this shouldn't be because it has an acute effect time of about 1 hour.

Hmmm, well, I'm not sure then, my money would be on the naloxone causing your problems but maybe someone else could shed some light on this.

 

[NeighborhoodThreat]

I'm not sure about the naloxone, but I could be dead wrong...

 

[DelRi0]

I mean, look at Suboxone...enough naloxone and opioid agonists in your body at the same time can cause precipitated withdrawals really quickly and that's a fact. It just sounded to me like this is whats happening to you when you "fall asleep and wake up in withdrawal 30 minutes later". Just my 2 cents.

 

[Cane2theLeft]

^ this is a bit of a misnomer here.

With suboxone, the naloxone doesn't produce precipitated withdrawals - it's the action of buprenorphine as a mixed agonist-antagonist (often called a partial agonist). It will produce agonism up to the equivalent of 30mg of methadone however if you are physically dependent on more than than much it'll will throw you into precipitated withdrawal and largely block doses of other opioids for a period.

If someone is physically dependent on less than the equivalent of 30mg of methadone, they'll experience precipitated withdrawals when the buprenorphine displaces the full agonist but it will not last nearly as long.

Regarding the original question, I highly doubt that sleep itself causes any effect on opioid metabolism or anything like that and there is no reason that I can think of that sleep would induce precipitated withdrawal or make the medication do so.

With just about any drug, people here have reported that if they fall asleep for a short period of time, they will not feel the effects as strongly whether this be alcohol, opioids, amphetamines, benzodiazepines, etc.

This is especially common and well documented with alcohol and morning DUI's. Essentially someone will go out and drink a lot and say they hit .12 BAC at midnight and they certainly realize they are a little past where they can drive and they keep drinking a lot, get a couple hours of sleep and then go to drive in the morning. They got some sleep, had some coffee and do not feel anything comparable to how they felt at midnight but they get pulled over and still blow .12

I think this is less to do with changes in physical processing of the substances but more to do with subjective perception of the effects and how sleep impacts this. One of the most important factors in how subjectively high someone feels is the speed of onset as well as the quantity of change in their sobriety - you often hear heroin addicts talk about getting so much higher when they are sick because they are going from feeling so shitty to feeling good. You can also see people get far more intoxicated off (liquor) shots because the speed these kick in makes the effects feel stronger because of how quickly they went from sober to shitfaced. If that person had been drinking beer or wine and took 2-3x as long to get to the same BAC, they wouldn't feel nearly as inebriated.

I suspect that when you're falling asleep you're losing this transition from how you felt before the medication to how you felt after and without this indicator that you're used to experiencing proceeding the opioid effects, you feel like it's not working as well (or at all). It's basic classical conditioning and if you lose that bell you've paired with salivating, you aren't going to salivate.

 

[Orlando_Doom]

I'm shooting in the dark too, and sadly, my doc too. He has NO clue what it could be, he puts it on tolerance, and would put me on oxycontin which I actually dont want because what I have is enough for my pain.

EDIT: posted before I saw Cane2theLeft's post. Sounds logical. Thing is I don't get high from it at all, I`m taking my dose daily for several years now. At least I don't feel any high, but my usual dose leaves very low levels of pain like most opioids do in my experience, and if I combine that with your well-written information, I think the pain in general, and possibly uncomfortable feelings surpressed by the opioid are just much more perceivable after waking up.

It just really bugged me because I take my meds by script to the letter, have a nice and good doc, and still such problems

Thanks for your help and contributions guys, I think this is the best solution for my question.

 

[Cane2theLeft]

^ we posted at the same time so sometimes it's easy to miss the post before yours... I don't think you can miss that essay though! Fuck I didn't realize I typed that much

 

[paper planes]

if i go to sleep i notice diminshed effects but not withdrawl..on the other hand ive been on suboxone for over a yr but almost every morning i get up i feel slight withdrawl

 

[Cane2theLeft]

I don't see why the intent of your use would have any impact on the theory I presented - the examples I cited were using recreational users' experiences because they are more prevalent and pronounced but the same facts about perception of effects (including analgesia) being affected by speed of onset, the transition period proceeding the relief and classical conditioning, etc. still apply.

Why do you fall asleep for short periods after taking that? How about you use a little caffeine or don't lay down after taking it? (sorry if this comes off condescending - it just seems like this should be easily correctable if the right steps are taken and if not and your medicine makes you pass out that perhaps the dose is too high. If there's NO WAY around it, you could discuss supplementing with a medication for Opioid-Induced Sedation such as provigil).