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Young Professor
01-31-2008, 02:39 PM
Does anyone know EXACTLY the time release function for Oxys if used as directed? I've been told that half the dose is released immediately, and then the other half is released 6 hours later. So, if you're on 20s, 10mg gets released within 20-30 minutes of taking, and then the other 10mg 6 hours later. Supposed to last 12 hours, but we all know it doesn't. I've also been told that the entire amount is released proportionally over the 12 hour period. I asked my pharmacist, but he didn't know. I saw a semi-related thread on here somewhere, but answers were all over the fucking place, and most were way off base. Thanks!

Ludakris
01-31-2008, 03:19 PM
Well, I certainly can't give you an exact science on that...but I firmly believe that OC's don't have the dual layer properties of a lot of time release meds, thus, releasing an initial dose instantly and then a second layer with time release properties. An OC will release (supposedly) continuously over a period of about 6 hours, logic would make me think that a little more might be released in the beginning vs. the end of the time, so like, a 40mg would release like 9mg in the first hour, then releasing a steady flow of about 7mg/hr, but probably tapers off in the end to like, 5mg/hr.

Most people on OC's are also RX'd a Break Though Med for times when more pain control is needed, which also makes me think that OC's don't have a dual layer.

SpecialGuy69
01-31-2008, 03:25 PM
Luda is right on. The time release is not stepped. If you ever get a complete supply bottle (joy), read the package insert. Its also available online. It explains in great detail the rate at which oxycodone is released, but not the mechanism by which it is released.

Young Professor
01-31-2008, 10:12 PM
I've looked practically everywhere on-line and cannot find the actual time release breakdown. Everything I read talks about the time release in a general sense. Like I said in my OP, even the pharmacist didn't know. He's going to save the me package insert on the next supply bottle that comes in....He tears it off the outside (sticks on by glue) and throws it away because it always gets in the way as he's filling scripts.

EleusisII
01-31-2008, 10:16 PM
OT: You know, there's something about your nick that makes me want to give you a wedgie...


Any particulat reason you're asking? There are different relase mechanism for the different OC producers. From what I read on a manufacturers site, pretty sure it was a danish one, but not 100%, 40% gets released right away, and the rest gets released over a 12 hour period.

So that would be 16mg that gets released right away in a 40mg pill.

Makes sense that they would do it this way, instead of real constant release.

Young Professor
02-01-2008, 08:12 PM
Yes, there is a reason I'm asking. As a chronic pain sufferer, I have a script for Oxy as well as something else for breakthrough pain. Well, not to whine, but things have gotten worse, and I suspect it's because my baseline (Oxy) isn't working as well. Therefore, I need to use more of the breakthrough stuff than I'd like. Trying to figure out what the exact dosing mechanism is so I can further identify the problem. For example, if it's half than the half 6 hours later (which I've been told but not convinced), then this would explain why I'm having problems at hour 4 thorough 6 and hours 9-12. I may need to switch to the patch, which is more constant (every hour). Any help would be appreciated. Thxs.

reddragon3668
02-01-2008, 08:40 PM
A lot of it depends on how long you've been taking it and what your tolerance is. Six years ago, 120mg of Oxycontin would do me just fine. Today, I doubt it would do much unless I took a huge amount. The patch is by far about the best thing you can get for pain relief. I was on it for about three months and it was great for pain relief. I found it, however, to be a hassle in many ways.

So, I come off of it and went on Opana. Opana runs a close second to the patch and I would guess that for most people, it would run circles around oxycontin, when both are being taken for pain relief and taken as directed. Oxy definitely wins, hands down, in the recreation department, imo. Opana is the ONLY thing I've ever taken that comes anywhere near lasting as long as its supposed too. Even that patch, rated to last 72 hours, only lasted me for 48.

I am scripted 40mg of Opana every 8hrs, but I don't need it that often. I just asked for the extra so I could stockpile some, and with my insurance co-pay, it doesn't cost me anymore for 90 pills versus 60. If you have insurance, I would definitely give it a try if y ou can. Its allot easier to swallow a pill several tiems a day than to try and keep that damn patch on for two or three days.

Good luck!

SpecialGuy69
02-01-2008, 09:02 PM
I've looked practically everywhere online and cannot find the actual time release breakdown. Everything I read talks about the time release in a general sense. Like I said in my OP, even the pharmacist didn't know. He's going to save the me package insert on the next supply bottle that comes in....He tears it off the outside (sticks on by glue) and throws it away because it always gets in the way as he's filling scripts.luda and i both explained that its released at a constant (slightly declining) rate. If you take your oxy q8h instead of q12h you should be all right (if your dose is adequate). And if you really want to know, google "oxycontin packaging insert" or black box warning and you can find the whole packaging insert. Its also linked to from several opiophile threads.

I have a feeling the problem isn't the time release mechanism at all, but that your tolerance has gone up. That means you need a higher dose. Simple. Its easier to ask for a change of med or more frequent dosing than it is to ask for a higher dose, but it sounds like a higher dose would help. good luck.

Young Professor
02-02-2008, 07:28 AM
Thanks to all for the replies. I really do appreciate it. I'm gonna ask the Doc next time I see him about the time release, but I've visited other forums where people swear its half and half each 6 hours. I suspect it's time released evenly over the 12 hr period. I will report back after talking to the Doc. I don't mind talking to him, but I like to get info ahead of time and plan my discussion so that I don't look like an idiot. After all, he is my life line.

Red- Thanks for the tip on Opana...I'm gonna research it. Yes, I suspect my tolerance is the issue. I too did much better on the patch, but had to discontinue it two years ago because it just got too itchy in the hotter half of the year. I also had to change every 48. A lot of that has to due with your activity level and metabolism. The more active you are and the hotter your body gets, the more you absorb. Just as any fyi, the pharmacist told me that the patch was originally developed for cancer patients at the end of life, so it was developed with low activity involved...pretty much someone who was laying in a bed. Thus, this would explain why it doesn't last the full 72 for more active people. Also, I didn't like the whole patch thing in general like you describe. Was tolerable Nov - March though. I may explore and on/off thing based on time of year. Lose doses of fentanyl do work!

I also agree about your stockpiling strategy. Important for many reasons.

Thanks again to al!

Young Professor
02-02-2008, 07:46 AM
Red- If you don't mind me asking, when you switched from the patch to Opana, did you request it or did the Doc suggest it? Also, what strength patch were you on before you went to the 40 Opana? Again, thanks for your help...Life ain't so grand these days.

roxi*stardust
02-02-2008, 08:10 AM
My understanding of the time release mechanism is that 1/3 of the dose is released immediately then the other 2/3 over a 8-12 hours period. This is directly from the package insert from Purdue:




OxyContin Tablets exhibit a biphasic
absorption pattern with two apparent absorption half-lives of 0.6 and 6.9 hours, which
describes the initial release of oxycodone from the tablet followed by a prolonged release.

SpecialGuy69
02-02-2008, 05:32 PM
not exactly, roxi (this is just my understanding, as explained by my PM doc)- what you quoted is referring to a one time dosing. OC is intended to be taken at regular intervals, and so there is no initial burst. It is designed to keep very constant serum levels of oxycodone, and if there was an initial burst, 2-3 times a day, you would have much higher serum levels of oxycodone.

But I really think this is totally irrelevant- the OP's problem is not with the time release mechanism of oxycontin, but much more likely that he's growing a tolerance to his current dose and needs a little more to get him through.

OP- it can be very intimidating, but I think you need to ask your doc for a dose increase.

EleusisII
02-02-2008, 06:06 PM
It seems that there is consensus on this: Nobody knows exactly how the timerelease works, but in this case, it doesn't matter a fucking little bit. To the young professor, it's not the timerelease, it's just your tolerance.

I guess tolerance can be hard to measure, if you don't take OCs to get high. It could be a number of different things that make you feel worse.

If you just tell your doc straight out how it is: You've started to feel worse, I'm sure he'll increase your dose. Some people have found, that changing meds works wonder on tolerance if you're having pain. That might help. Besides Opana and Fentanyl, methadone is also really good for constant pain. It's also cheaper than most other meds.


Godd luck... And here's a good luck-wedgie for ya:

SNAAAAAAAAAAAAAAAAAAAAAAAAPPPP CRACK!!!

Young Professor
02-02-2008, 09:30 PM
I think the dosing mechanism could be an issue. For example, I've seen where people swear it's 1/2 initially then 1/2 six hours later...If so, that means you aren't getting anything in hours 4-6. Then, at hour 6, the other half is released, which takes about 30 minutes.

However, if there is some constant measure, then yes, tolerance is the issue. I plan on talking to the Doc. I would love to know the conversion of Oxy to Opana or the fentanyl patch to Opana.

I may inquire about methadone as well.

Again, a big THANKS to all! I really do appreciate your time in posting.

YP

roxi*stardust
02-02-2008, 10:51 PM
not exactly, roxi (this is just my understanding, as explained by my PM doc)- what you quoted is referring to a one time dosing. OC is intended to be taken at regular intervals, and so there is no initial burst. It is designed to keep very constant serum levels of oxycodone, and if there was an initial burst, 2-3 times a day, you would have much higher serum levels of oxycodone.

But I really think this is totally irrelevant- the OP's problem is not with the time release mechanism of oxycontin, but much more likely that he's growing a tolerance to his current dose and needs a little more to get him through.

OP- it can be very intimidating, but I think you need to ask your doc for a dose increase.
Well you might be right be my doctor explained it to me this way, along with one of the pharmacists I worked with. He pointed me to the package insert that says it has a bi-pasic release:


PHARMACOKINETICS AND METABOLISM

The activity of OxyContin Tablets is primarily due to the parent drug oxycodone.
OxyContin Tablets are designed to provide controlled delivery of oxycodone over 12 hours.


Oxycodone release from OxyContin Tablets is pH independent. Oxycodone is well absorbed
from OxyContin Tablets with an oral bioavailability of 60% to 87%. The relative oral
bioavailability of OxyContin to immediate-release oral dosage forms is 100%. Upon
repeated dosing in normal volunteers in pharmacokinetic studies, steady-state levels were
achieved within 24-36 hours. Dose proportionality and/or bioavailability has been
established for the 10 mg, 20 mg, 40 mg, 80 mg, and 160 mg tablet strengths for both peak
plasma levels (Cmax) and extent of absorption (AUC). Oxycodone is extensively metabolized

and eliminated primarily in the urine as both conjugated and unconjugated metabolites. The
apparent elimination half-life of oxycodone following the administration of OxyContin® was
4.5 hours compared to 3.2 hours for immediate-release oxycodone.


About 60% to 87% of an oral dose of oxycodone reaches the central compartment in
comparison to a parenteral dose. This high oral bioavailability is due to low pre-systemic
and/or first-pass metabolism. In normal volunteers, the t½ of absorption is 0.4 hours for
immediate-release oral oxycodone. In contrast, OxyContin Tablets exhibit a biphasic
absorption pattern with two apparent absorption half-lives of 0.6 and 6.9 hours, which
describes the initial release of oxycodone from the tablet followed by a prolonged release.


Dose proportionality has been established for the 10 mg, 20 mg, 40 mg, and 80 mg tablet
strengths for both peak plasma concentrations (Cmax) and extent of absorption (AUC)
(see Table 1 below). Another study established that the 160 mg tablet is bioequivalent to
2 x 80 mg tablets as well as to 4 x 40 mg for both peak plasma concentrations (Cmax) and
extent of absorption (AUC) (see Table 2 below). Given the short half-life of elimination of
oxycodone from OxyContin®, steady-state plasma concentrations of oxycodone are achieved
within 24-36 hours of initiation of dosing with OxyContin Tablets. In a study comparing
10 mg of OxyContin every 12 hours to 5 mg of immediate-release oxycodone every 6 hours,
the two treatments were found to be equivalent for AUC and Cmax, and similar for Cmin

(trough) concentrations. There was less fluctuation in plasma concentrations for the
OxyContin Tablets than for the immediate-release formulation.

Here is a graph showing plasma concentrations after a single dose of each strength, and a steady dose of the 10mg tablet. The graph shows there is definately and intial release of a "loading" dose from the pill because plasma levels go from zero to peak within the first 1-2 hours then taper down slowly. No doubt in my mind that you get about 1/3 of the dose intially then the other 2/3 slowly.


2564
Click me

SpecialGuy69
02-02-2008, 11:21 PM
No doubt in my mind that you get about 1/3 of the dose intially then the other 2/3 slowly.Ok- now we are talking about something I do understand- statistics/geek shit. The reason it looks like that is because they dont have any oxycodone in their system before taking the pill. I agree it releases a little faster at the beginning though.

To see what I mean, look at the red line on the graph- this is the only line where they are tracking someone who is already established on 10mg oxycontin. Once established at a steady-state dose, plasma levels are very consistent, only varying by 5-10% plus or minus from the average concentration. That proves that the time release isn't YP's problem.

YP- several people (roxi, myself, luda, and el) have already clearly explained what the problem is to you, and you still insist on the hypothesis you proposed. Why ask the question if you dont want to listen to the answer?

roxi*stardust
02-03-2008, 06:45 AM
Ok- now we are talking about something I do understand- statistics/geek shit. The reason it looks like that is because they dont have any oxycodone in their system before taking the pill. I agree it releases a little faster at the beginning though.

To see what I mean, look at the red line on the graph- this is the only line where they are tracking someone who is already established on 10mg oxycontin. Once established at a steady-state dose, plasma levels are very consistent, only varying by 5-10% plus or minus from the average concentration. That proves that the time release isn't YP's problem.

YP- several people (roxi, myself, luda, and el) have already clearly explained what the problem is to you, and you still insist on the hypothesis you proposed. Why ask the question if you dont want to listen to the answer?
A person taking an immediate release dose of oxy taken every 4 hours around the clock would also have a steady plasma concentration. The package insert says "an intial release of oxycodone from the tablet followed by a prolonged release.



OxyContin Tablets exhibit a biphasic
absorption pattern with two apparent absorption half-lives of 0.6 and 6.9 hours, which
describes the initial release of oxycodone from the tablet followed by a prolonged release

You can see that 1-2 hours after the intial dose blood levels rech their peak. If the tablet was only releasing small amounts over that 12 hours period, you would not reach peak blood levels so quickly. It appears that there is a "loading dose" released from the tablet.

Young Professor
02-03-2008, 02:36 PM
Roxi- Thanks so much for the time in posting. The graph makes perfect sense and helps explain things. I will report back after talking to the Doc if he provides any worthwhile information.

If a person were to switch to the patch, methadone, or Opana, do the new drugs attach to the same receptors or different ones? I'm wondering if one would go through minor wd from ceasing Oxy even though you replaced it with one of the others?

Again, I appreciate the help and I hope to reduce some of the suffering. That's why I ask the questions, Agent Orange. Sorry if my posts bother you.

Young Professor
02-03-2008, 03:11 PM
As a quick side note, I read somewhere on this forum that if even if one crushes and therefore defeats the time release functionality, there is still some small amount of time release in the crushed pieces and therefore not 100% is immediately released. Not sure if this is true or not, but it so, that would further lead me to believe that a certain amount of Oxy (after the 1st release) is released over time on a fairly steady schedule, over the 12 hour period. This is all dependent upon your individual metabolism and why some report that it doesn't work for 12 hours. Personally, I get about 8-9 hours, tops.

SpecialGuy69
02-03-2008, 04:11 PM
A person taking an immediate release dose of oxy taken every 4 hours around the clock would also have a steady plasma concentration. The package insert says "an intial release of oxycodone from the tablet followed by a prolonged release.


You can see that 1-2 hours after the intial dose blood levels rech their peak. If the tablet was only releasing small amounts over that 12 hours period, you would not reach peak blood levels so quickly. It appears that there is a "loading dose" released from the tablet.hmm... I'll have to look into it.


YP- your posts dont bother me and I never said that. All I said was why ask the question if you already have the answer established in your head?

Young Professor
02-03-2008, 06:42 PM
From Roxi's post, this was very interesting:

"In a study comparing 10 mg of OxyContin every 12 hours to 5 mg of immediate-release oxycodone every 6 hours,
the two treatments were found to be equivalent for AUC and Cmax, and similar for Cmin (trough) concentrations." Although it did add that there was less fluctuation with the steady dose.

I also found the graph interesting in that with the single dosing, the blood concentration levels stayed pretty high and semi constant for quite a while after administration. For me, it seems that after a single dosing of any Oxycodone (Oxyfast for example), there is quite a punch initially, but wears off quickly. The graph seems to contradict that, but I guess everyone is different.

Great information.