Opioids Methadone - 10 days in an I'm nodding, what is this?

[littlebaggies]

A little background: Started doing pills, etc., and long story short, I ended up with a severe H habit. Got to a gram/daily of really good Afgan-Chunky Gold, tried to quit several times using suboxone (which I can't stand) to now using methadone. I had about a month of solid suboxone at 3-4mg/day prior to methadone induction and now 10 days in, I've been sitting at 40mg/day (for the last 6). At the clinic they started me on 20mg/day (which was totally insufficient), moving up 5mg/day to 40mg where I told them I didn’t want to go higher. They wanted me to go to 80mg.

I typically dose at 7 am and by 1 – 4 pm I’m usually feeling minor detox symptoms which slightly increase till about 9pm when they dissipate completely. All the way through till my next dose at 7 am of 40mg I’m fairly even. Today however something strange happened: I dosed at 7am per usual but by 10:30 am I was nodding pretty solid! It was a nice, fuzzy feeling and I actually took a dream-filled nap, which I never do. Is this normal? I know 40mg is nothing to sneeze at but everyone at the clinic is telling me it’s the minimum. Any thoughts would be welcome!

baggies

 

[helium-4]

I'm not sure what you are asking? When I first started using methadone I was able to nod as well, but not any more. The time it takes for you to loose alot of the more recreational effects is dependent on your body, so there isn't a specific time frame, but it will probably go away in the near future, though as you increase your dose you may still retain the more recreational effects till your sustained.

Also they prefer MMT patients to dose around 80mg after working up to it because once you around taking around 60-80mgs the methadone begins to beable to "block" the recreational effects of other opioids, as well as studies show higher doses of methadone leads to less relaspes. Both those reasons are why doctors try and push your dosage up. You will also notice if you do relaspe that your tolerance to opioids will have increased because 80mgs+ is a large amount an opioid.

 

[littlebaggies]

Well, you answered my question, sorry it wasn't clear. I'm trying to quit all opiates, not trade one for another. I started the 'done thing thinking 35-40mg wasn't that high a dose but what I experienced today educated me on that. I was more concerned with the fact it took 6 days to hit me like that. Didn't know if that was common or not.

 

[helium-4]

When I first started on methadone I found I can fallasleep quickly about 2-3 hours after oral administration, and I still find myself able to fallasleep about that time after ingesting methadone and clonazepam. Some people find that methadone is pretty sedating, and when you start peaking orally (~3 hours or so, with usualy 10-12 hours of pupil constriction, basically showing the main "high" or effects last 10-14 hours), it can be easy to accidently fallasleep. Now after a while opioids can cause you to alter you sleep patterns which can lead to sleep disturbances even if you can accidently fall asleep. I'd like to just be on methadone for my RLS/PLMS and not need clonazepam, but I have to take the benzos to maintain sleep as the methadone messes up my sleep patterns (usually resulting in me sleeping 5 hours rather than a solid 8-9 hours).


Essentially the higher dose, the more side-effects possible, and the longer you maintain, the less opioid recreational effects it will have. But since you haven't been on it for very long and are increasing your dose, you'll still possibly catch a buzz along with have some potential increase in side-effects.

 

[Swimmingdancer]

Methadone is very potent and 40mg is a high dose, it's just not high numerically if you're comparing it to those people who are on massive amounts of methadone. The real reasons some clinics try to get people to people take more is that they are trying to achieve a stronger blockade of other opioids, are trying to completely elminiate cravings. There are also some people who take higher doses of methadone because they had a HUGE habit or are expecting to get some kind of buzz/noticeable mental effects from the methadone (I've noticed that a lot of people new to methadone were expecting it to make them feel like heroin or their opioid of choice did, and when it doesn't they think they are just not on a high enough dose and keep asking the doctor to raise their dose). If your goal is to get off methadone as quickly as you can I think you are doing the right thing in trying to keep your dose lower.

The fact that it took 6 days for you to notice the effects is normal. The reason is that methadone takes that long to reach peak levels in your system. Here is a graph:

It will also take about the same amount of time for the levels in your system to fully decrease after a dose decrease.

The effects you are noticing from the methadone will not last for long though. After about 3 weeks or so your body will adjust and you will no longer feel anything from the methadone except for relief from withdrawal symptoms.

That is very strange the pattern that you mentioned in your withdrawal symptoms after you take your methadone, it doesn't make sense. Perhaps it could be psychological/conditioning?

 

[-Guido-]

A little background: Started doing pills, etc., and long story short, I ended up with a severe H habit. Got to a gram/daily of really good Afgan-Chunky Gold, tried to quit several times using suboxone (which I can't stand) to now using methadone. I had about a month of solid suboxone at 3-4mg/day prior to methadone induction and now 10 days in, I've been sitting at 40mg/day (for the last 6). At the clinic they started me on 20mg/day (which was totally insufficient), moving up 5mg/day to 40mg where I told them I didn’t want to go higher. They wanted me to go to 80mg.

I typically dose at 7 am and by 1 – 4 pm I’m usually feeling minor detox symptoms which slightly increase till about 9pm when they dissipate completely. All the way through till my next dose at 7 am of 40mg I’m fairly even. Today however something strange happened: I dosed at 7am per usual but by 10:30 am I was nodding pretty solid! It was a nice, fuzzy feeling and I actually took a dream-filled nap, which I never do. Is this normal? I know 40mg is nothing to sneeze at but everyone at the clinic is telling me it’s the minimum. Any thoughts would be welcome!

baggies

You have stabilized. The Methadone has built up in your system. In a few months you will just feel normal.

 

[Znegative]

I agree that it's probably due to the fact that you are stabilized at a holding dose. However, I also think that relatively lower maintenance dosages (50mg and under), in the long run produce more of a pronounced buzz than higher dosages like upwards of eighty mg do. IMO, buprenorphine and methadone are very similar in this way. I've been at 30mg for over a month, and I still get a nice glow for five or so hours every day. However, I feel like the intensity of which I feel that 30mg depends on a variety of factors, such as, how much food I ate, how much sleep I got etc, etc..

 

[helium-4]

I know I'm pretty alone in snorting methadone (crush the pills, dissolve in water, filter, then snort), but it helps keep some consistency in the bioavaliability. The bioavaliability of oral administration can vary as low as 50% from the mean of ~85%, while snorting keeps it around 85% and increases the peroid of constricted pupils (longer duration of analgesic and if there are recreational effects). The come up also increases to ~7mins if snorted fasted enough.

I do agree with znegative keeping the doses low help keep a little buzz compared to constant higher doses, though somedays I will double my dose to 60, but not everyday after each other.

 

[-Guido-]

I know I'm pretty alone in snorting methadone (crush the pills, dissolve in water, filter, then snort), but it helps keep some consistency in the bioavaliability.

That is absolute bullshit. Methadone has a 90% oral availability. If anything snorting will lead to an inconsistency because some of that methadone is bound to get caught in mucous or be swallowed when leaking down nasal cavity into the back of the throat.

If Methadone had a superior bioavalibitly by being snorted junkies would of learned this a long time ago and it would be common practice.

 

[Swimmingdancer]

That is absolute bullshit. Methadone has a 90% oral availability. If anything snorting will lead to an inconsistency because some of that methadone is bound to get caught in mucous or be swallowed when leaking down nasal cavity into the back of the throat.

If Methadone had a superior bioavalibitly by being snorted junkies would of learned this a long time ago and it would be common practice.

I always thought that too, and I certainly do not want to encourage anyone to take their methadone by non-oral ROAs, but I recently read the product monograph for my methadone which says the following:

When administered orally, methadone is approximately one-half as potent as when given
parenterally. Oral administration results in a delay of the onset, a lowering of the peak, and an
increase in the duration of analgesic effect.

http://www.paladinlabs.com/our_products/metadol.pdf

I'm really not sure what to believe though, because I've always heard that the oral bioavailability of methadone was around 75%-95%. So it would be impossible for the parenteral bioavailability to be twice that. I wonder what exactly they mean by "one-half as potent"?

It sounds like Cloudy has read this study:

Nasal uptake of methadone was rapid, with maximum plasma concentrations occurring within 7 minutes. The maximum effects of intravenous, nasal, and oral methadone, on the basis of dark-adapted pupil diameter, were reached in about 15 minutes, 30 minutes, and 2 hours, respectively. The respective durations were 24, 10, and 8 hours. Both nasal and oral bioavailabilities were 0.85. Subjects reported that nasal methadone caused a burning sensation.

http://www.ncbi.nlm.nih.gov/pubmed/12426517

So from that one it says the bioavailability is the same as when taken orally (85% ), the onset was much faster with nasal, and that the duration was longer with nasal administration than with oral.

The following study shows a graph where methadone was administered intravenously, orally, and rectally and compares the plasma concentrations. The IV was 5mg and the oral was 10mg, and they have almost the same plasma concentrations. So perhaps that is what the first source meant when they said oral methadone is 1/2 as potent as parenterally? (if by parenterally they were referring solely to IV)
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1884589/figure/fig01/

Interestingly they said the rectal bioavailability was slightly lower than oral (76% vs 86% ) but the absorption was more rapid.

 

[Swimmingdancer]

I also think that relatively lower maintenance dosages (50mg and under), in the long run produce more of a pronounced buzz than higher dosages like upwards of eighty mg do. IMO, buprenorphine and methadone are very similar in this way. I've been at 30mg for over a month, and I still get a nice glow for five or so hours every day.

That has not been my experience at all and I have been on methadone on and off for over 10 years at varying doses. Also I don't think that just over a month is long enough to be able to make any conclusion about the "buzz"/"glow" because most people do get noticeable effects for the first 3-10 weeks. I read one study that said that for about the first month methadone metabolizes differently than it does after that. And it takes around a month or more to adjust to any dose of methadone. I have never seen, heard, read or experienced anything that would suggest that methadone has more pronounced psychoactive effects at a lower dose, other than your post. Personally my experience and that of people I've talked to, and what I've been told by doctors, is that you develop a tolerance to the buzz/glow feeling after a couple months, no matter what dose you are taking. It has more to do with the duration of action than the dose.

Perhaps a higher dose would have a longer duration of action and so maybe someone at 80mg might develop a tolerance to the effects slightly sooner than someone at 30mg, but someone at 30mg is still going to develop that tolerance within a relatively short amount of time.

 

[helium-4]

That is absolute bullshit. Methadone has a 90% oral availability. If anything snorting will lead to an inconsistency because some of that methadone is bound to get caught in mucous or be swallowed when leaking down nasal cavity into the back of the throat.

If Methadone had a superior bioavalibitly by being snorted junkies would of learned this a long time ago and it would be common practice.

I never said it was the nasal bioavaliability is higher, I said it is more consistant if snorted properly (in a filtered solution with no more than .200 mL at a time in each nostril). One issue is the pain caused by nasal administration, yeah even with filtration it still stings a little. Alot less than snorting the pills. Also it doesn't give you much of a rush, even with the short duration. Studies back this up, however you can believe what you want. I've posted the study and summerization many times in varies threads (methadone mega thread for one) so I wont bother explaining it again, especially to someone who arrogantly responding to my post.

Objective: Nasal administration of many opioids demonstrates rapid uptake and fast onset of action. Nasal
administration may be an alternative to intravenous and oral administration of methadone and was therefore
studied in human volunteers.
Methods: The study was approved by the Institutional Review Board of the University of Washington, Seattle.
Eight healthy volunteers (6 men and 2 women) aged 19 to 33 years were enrolled after informed written
consent was obtained. Subjects received 10 mg methadone hydrochloride nasally, orally, or intravenously on
3 separate occasions in a crossover design. Nasal methadone (50 mg/mL in aqueous solution) was given as a
100-
L spray in each nostril (Pfeiffer BiDose sprayer). Blood samples for liquid chromatography-mass
spectrometry analyses of methadone and the metabolite 2-ethyl-1,5-dimethyl-3,3-diphenylpyrrolinium were
drawn for up to 96 hours. The methadone effect was measured by noninvasive infrared pupilometry coincident
with blood sampling.
Results: Nasal uptake of methadone was rapid, with maximum plasma concentrations occurring within 7
minutes. The maximum effects of intravenous, nasal, and oral methadone, on the basis of dark-adapted pupil
diameter, were reached in about 15 minutes, 30 minutes, and 2 hours, respectively. The respective durations
were 24, 10, and 8 hours. Both nasal and oral bioavailabilities were 0.85. Subjects reported that nasal
methadone caused a burning sensation.
Conclusions: Nasal administration of methadone results in rapid absorption and onset of effect and high
bioavailability, which was greater than that reported for other nasal opioids, with a similar duration of effect.
Nasal administration may be an alternative route of methadone administration; however, improved formulations
are desirable to reduce nasal irritation. (Clin Pharmacol Ther 2002;72:536-45.)

 

[ErgicMergic]

In addition to keeping your wd symptoms stabilized, your cravings reduced, and your opioid tolerance saturated making H almost useless, don't high doses also ensure that you will get heavily dependent on methadone, keeping you coming back each month for your medicine?

Methadone clinics are privately run, for-profit businesses, at the end of the day. It is much easier to kick 30-40mg than it is 80-120mg.

 

[Swimmingdancer]

Methadone clinics are privately run, for-profit businesses, at the end of the day. It is much easier to kick 30-40mg than it is 80-120mg.

Unfortunately I suspect that this is a very likely factor. Many methadone clinics really want you to be on methadone - and therefore keeping them in business - for the rest of your life. Many also think that taking a high dose of methadone forever is the only way to keep you off heroin or other illicit opioids (which is seen by many as the most important goal). I remember when methadone was severely rotting my teeth and I was told "Yes it's probably caused by the methadone but isn't having no teeth better than being a heroin addict?"

 

[tricomb]

It's addictive stuff, definitely a plus for the profiting business, they go through the paperwork to make it all legal, just like the alcohol and tobacco industries.

At least methadone serves a purpose without an insane risk vs reward ratio.

 

[ErgicMergic]

At least methadone serves a purpose without an insane risk vs reward ratio.

Very true, but it's sad to see how easily they'll put someone with a minor 0.5g dope or 100mg oxycodone daily habit on an ever-increasing dose of Methadone, though.

That should be criminal, they should have a minimum daily reported usage before they're allowed to slap on the Methadone handcuffs, they shouldn't grabbing the first person they see on 100mg of daily hydro/oxycodone and put them on Methadone.

Also, I don't understand why the clinics allowed to let people chase the high. Patients who have been on a steady 70mg for 6 months straight don't need any more to stabilize, but they're allowed to chase the nod if they want, and the clinics love that since they are just getting more and more dependent. There should be a 3-6 month titration period, and then a lock-out on dose increases, unless they are CPP patients and need to increase dosages for analgesia, not for recreation.

That's just my opinion, and in the end of the day, they are following the rules by the book, so they are legally immune. It might be time that "book" revised its guidelines a bit, though.

 

[Swimmingdancer]

Also, I don't understand why the clinics allowed to let people chase the high. Patients who have been on a steady 70mg for 6 months straight don't need any more to stabilize, but they're allowed to chase the nod if they want, and the clinics love that since they are just getting more and more dependent. There should be a 3-6 month titration period, and then a lock-out on dose increases, unless they are CPP patients and need to increase dosages for analgesia, not for recreation.

Unfortunately I think that having a lock-out on dose increases could do more harm than good. What about when someone has been using heroin (or whatever opioid) on top of their methadone and has raised their tolerance? If they couldn't get their methadone dose increased it wouldn't be enough to keep them out of WDs and it would be very easy for them to rationalize continuing to use heroin. Or what about someone who has legit pain and can't get any legal pain meds because they are on methadone, maybe a dose increase for them would provide some analgesia and they wouldn't turn to illicit drugs.

Personally I think that a big step would be requiring methadone doctors/clinics to be completely truthful with prospective patients about methadone's effects, side-effects, physical dependence, etc. Back when I first got on methadone all they told me was that it was a legal substitute for heroin which would completely alleviate all my cravings, that you don't develop a tolerance, that I could go on it for as long as I wanted and would be able to quit painlessly without any withdrawal symptoms at all at any time as long as I tapered my dose over the period of about a month, and that there were no side effects. Of course now I know that's all complete bullshit

 

[tricomb]

By no means do I support methadone for an oxycodone habit, IMO it is only for: pain patients, and those who abuse fentanyl, heroin/morphine, or oxymorphone, AND have all made multiple failed attempts at buprenorphine therapy.

 

[littlebaggies]

By no means do I support methadone for an oxycodone habit, IMO it is only for: pain patients, and those who abuse fentanyl, heroin/morphine, or oxymorphone, AND have all made multiple failed attempts at buprenorphine therapy.

Why? Oxy is comparable to heroin mg/mg and also in the qualitative/subjective affects. Certainly Oxy is just as addictive. I know, everyone says H is worse because of that "punch" you get when you push but I was/am addicted to much more than that initial punch, which I only got from the first spoon of the day. When I didn't have a good connect for H, I sometimes did have access to a lot of Oxy 80s. I couldn't push them (Opana) but I think I was just as addicted to the Oxy as the H.

Baggies