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Old 11-03-2008, 07:28
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Bupe, half-life, buildup, tapering

This is SWIM's very first result at an attempt to answer a question that has been troubling her for quite a bit of time. Now consider that this is merely a first round batch of data, and SWIM needs to check her algorithm over and over again to make sure it is producing accurate results.

buprenorphine has a half-life of 37 hours on average, but typically people are dosed every 24 hours. That would seem like a very high level of build up would occur in people who are maintained on this drug for long periods of time. SWIM awhile ago began writing a computer program to simulate the relative amount of buprenorphine in a person's system given different doses, dosing schedules, periods of time, etc... Well the spring semester began and SWIM no longer had time to continue work on it. Not that it's overly complex, SWIM just has no free time. But SWIM is on spring break now so figured she'd take a minute and look at one of her many unfinished programs. Well, SWIM didn't finish it, but added enough functionality to do some first run simulations of data. If what the program is showing SWIM is accurate, then SWIM just learned a major leason in pharmacology. The information SWIM is getting could probably be proved or disproved with some simple math. However SWIM's math done manually is showing the same results.

Anyways, SWIM assumed that with a 37 hour half-life and 24 hour dosing, that buildup of bupe in a person's system would eventually become way high. SWIM's first round test shows that blood levels of bupe after 10 days of 24 hour dosing are only only a microgram or two from reaching their peak which would occur on the 11th day. After the 11th day, with 24 hour dosing of the same dose each day would no longer yield higher levels of bupe in the system... Or the increases are so small that they are negligible. Assuming there is no error in SWIM's algorithm, to determine if in fact a peak blood level of bupe would be reached in basically 10 days, as after 11 days the slope of the equation becomes 0 or very close to it. SWIM needs to use more decimal places in his calculations for further exploration.

So basically a person should have equal amounts of bupe in their system regardless of whether they've taken the same dose each day for 10-11 days or 360 days... Even after 3 years, the blood levels remain the same.

SWIM knows that there are 100 different variables that could possibly make everything she is basing her work on totally wrong. If my assumptions based on the data I got are totally wrong, please let me know so that I don't waste anymore time trying to fine tune things. My mathematics are sound, as is my logic, however my understanding of the metabolism bupe is not.

A fact pulled from the suboxone/subutex manufacturers insert says that 30% bupe is excreted via urine and 69% is excreted via intestines 11 days after the a dose. The other 1% can be accounted for by 2 unidentified buprenorphine metabolites. So this means that according to Reckitt Benckiser Pharm, a single dose of bupe will be completely elminated from teh body in 11 days.

If no one understands what I'm rambling on about then just let this thread die and I will bring it back to life once I have done further testing come to some more concrete conclusions and am able to present some more user friendly data... and more confidently I might add. I have purposely omitted my raw data from the various simulations that I've run in case they are incorrect.

Last edited by Laudaphun; 03-05-2008 at 20:06. Reason: slightly altered title of thread
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Old 11-03-2008, 07:30
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Re: Bupe, half-life, buildup, explanation?

Quote:
A fact pulled from the suboxone/subutex manufacturers insert says that 30% bupe is excreted via urine and 69% is excreted via intestines 11 days after the a dose. The other 1% can be accounted for by 2 unidentified buprenorphine metabolites. So this means that according to Reckitt Benckiser Pharm, a single dose of bupe will be completely elminated from teh body in 11 days.
just wanted to point this paragraph out in my rather lengthy post above, as it is straight from the package insert and the only information contained in the above post that is not merely speculative on my part at this point
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Old 03-05-2008, 20:01
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Re: Bupe, half-life, buildup, explanation?

If it is any interest, an 8mg suboxone pill (buprenorphine 8mg naloxone 2mg) weighs almost exactly 0.400 grams. Almost every pill SWIM has weighed ranged from a minimum of .395g to .400g A fresh pill that hasn't been rattled around in a pill bottle for a few months should wieght .400g This is sort of good to know if you have a balance that will weigh down to the mg as you can assume that every 1/10 or .100 gram of pill material contains 2mg bupe. So if you've got a bunch of powder from pills that were rather roughly handled you can calculate the exact dose of bupe you are getting. Example: you have some crushed up, fragmented, chunks, or whatever of suboxone. Weigh it out and divide whatever you get by .050 and this will give you a pretty exact value for the amount of suboxone (buprenorphine you have). You can purchase one of these scales for 20 dollars USD, and is by far the best method SWIM has found for titrating buprenorphine doses when in the U.S. we are only provided with either 2mg or 8mg non-scored tablets. Weighing of fragments/powdered suboxone with balance accurate to the nearest mg allows for reliable dose reduction in very small increments. i.e. 5.0mg to 4.9mg... assuming one was so inclined to do so.

For example, a pill with all it's fillers weighs .400mg and contains 8mg active ingredient. Just weigh out a piece of the pill, or a pile of powered pill and suppose you get 0.328 grams or 328mg. Just multiply the amount of your material with a conversion factor which in this case would be 8mg/.400mg and it will give you a fairly accurate estimation at the amount of active ingredient contained in the weighed out portion. So, in this case your weighed out portion of 0.328 gram (328mg) would contain approximately 6.560 active ingredient.

---------------This portion was intended as a response in another thread, but decided to just put it here and provide link-------------------

If SWIY has been on suboxone for awhile, do NOT try to titrate your dosage downward any faster than 2mg per month... If you are on a lower dosage, think more in terms of % decrease than a fixxed amount. For example... many people get down to 1 or 2mg and find it incredibly hard to get off of that... Probably because 2mg is (in the U.S. anyways) the lowest dosage unit available. Once you are under 6-8mg per day... 2mg dosage reductions will hurt...

Since it has such a long half life, you might get comfortable on 6mg then cut down to 4mg and feel like your losing your mind, while not physically ill from withdrawl symptoms. This can be very confusing at times. You don't feel sick, but since the long half-life and the potency of the drug, you will
spend a month going through psychological withdrawl symptoms. Do not let anyone tell you that these are in your head, because most of us know that
with opiates, you are not indirectly manipulating neurotransmitters, but rather tricking your body by using artificial ones, so your brain chemistry
WILL become unbalance when you decrease the dosage of artificial opiates that it has become accustomed to.

SWIM made a post somewhere else about this... as she had been trying to get off of suboxone for almost 2 years, unable to get below the 3-8mg range. Dr.s will tell you to get a pill cutter to get around the fact that we only have dosage units available in 2mg and 8mg... Well in other countries, they have 0.2mg and 0.4mg dosage units available, so that should tell you something about the potency of the narcotic. But we don't have access to anything like that in the U.S. Even breaking a 2mg pill into quarters gives you (rough approximations of) 0.5mg portions... It will take your body up to a month to get used to even a meager % reduction in dosage, so please do not rush things or you will find yourself feeling like your are losing your mind... SWIM knows this from personal experience. It's almost a gaurenteed thing for SWIM that she will become SUPER emotional and wind up crying at the end of every movie (happy or sad).

To avoid this there is a little trick that most people don't implement. Get yourself a digital scale that measures out to .001 grams. These are very easy to find and very cheap. I cannot give you sources for these or prices, but they are easy to find and very affordable. You will find that each 8mg suboxone pill weighs exactly .400 to .390 (depending on how fresh it is from the pharmacy and how much it has been rattled around in the bottle. So, just do the math. If you are on 6mg and want to cut down to 5.8mg, you know that 8mg = 400mg weighed out material. So just multiply the dose you want by 400mg (weight of the pill) and divide by 8mg (amount of buprenorphine in pill) and it will give you the amount of material you need to weigh out to obtain that dosage

Last edited by Laudaphun; 03-05-2008 at 20:11.
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