Bupe half-life versus active agent

[littlebaggies]

Hi!

I have been trying to determine if there is any difference between the half-life of suboxone (or any drug) and the length of time the substance is actually active in your system. I know from research the average half-life of suboxone is 37.5 hours however I know from personal experience it doesn't feel like it is active that long. I am a former heroin-oxy-dilaudid user, 24 mg+ daily hydro, 1/2 - 1 g heroin or 240 mg+ oxy daily. In a week I've gone from that level to 1/2 mg twice daily of bupe-I've been doing that for 3 days now. In the past week I've taken a total of 14 mg and I've noticed the effects of the sub starts to wear off within a few hours even though most of that dose is still supposed to be present. Although the bupe is still in my system does that necessarily equate to it being active? Any thoughts would be welcome. Oh, I did review the suboxone mega-thread and I only found the basics of bupe metabolism, no discussion on whether there is a difference in half-life availability and action rate of the substance.

J

 

[sekio]

Half life is roughly correlated to drug potency, remember that tolerance can develop over the course of a single "session" though, and a half life won't tell you how long you will have theraputic blood levels in you. Drugs like e.g. diazepam have a startlingly long half life but rather short effects because they get distributed to fatty tissues after a while that don't have quite the same receptor density as the relatively wet brain. This results in insufficient concentration of the drug to activate receptors.

Generally, however, t1/2 and the presence of active metabolites are what determines a drug's duration.
Bupe lasts relatively long; it's half life is something like 20-40 hours.
Morphine is much shorter-acting, it has a T1/2 maybe 3-5hours
Fentanyl is really short acting, it has a half life of 2-10 minutes.

Cocaine has a t1/2 of maybe an hour. It lasts maybe 20 minutes tops.
Methylphenidate has a t1/2 of 2-4 hours. It lasts maybe 2 hours peak.

Half life is not a 1:1 determiner of drug activity duration, it's a good metric though.

 

[Tchort]

There is a lot of confusion regarding half-lives of drugs/medications. The numbers vary from study to study or resource to resource, generally resulting in a 'range. One important thing to remember is that every person is different, and will have a unique physiology, unique environmental and dietary factors, unique genetics, etc.

Also, the half-life numbers are in reference to a single dose administered one time. By taking a substance regularly, it can change the average half-life of each dose taken (Methadone in a new pain patient vs Methadone in a daily MMT long-term patient for example).

Also, half-life does not mean that the drug is active for this time, only that it is, on the average by studies done on blood serum levels, half-eliminated from the body at that time mark. Meaning, a group of 40 non-opioid dependant volunteers take one 10mg dose of Methadone, their blood serum levels of Methadone are checked at regular intervals and documented, and at the end when every last volunteer is showing up clean and how long it took, an average is taken and recorded. But long-acting drugs like Methadone and Buprenorphine will have long half-lives and long complete elimination times, but their period of active analgesia for example is only 6-8 hours. So for a pain patient taking Methadose or Temgesic, a new dose would be needed every 6-8 hours for pain relief, even though the drug is still lingering for a long time in the body.

Administration by the sublingual route.

Adults and children over 12:

200-400 micrograms to be dissolved under the tongue every 6-8 hours or as required. The recommended starting dose for moderate to severe pain of the type typically presenting in general practice is 200 to 400 microgram tablets, 8 hourly. The tablet should not be chewed or swallowed whole as this will reduce efficacy.

http://www.drugs.com/uk/temgesic-400-microgram-sublingual-tablets-spc-1241.html

Despite the fact that Buprenorphine's half-life is listed as 24-48 hours (the site I was just on listed 37, others vary).

 

[ONandOFF777]

I take Suboxone for pain, and I have found that when taken for pain and not just for maintenance 4 smaller doses throughout the day is far superior to 1 large dose once a day.

I typically take about 2mg in the AM, maybe 1mg mid day, 2mg in the afternoon and then sometimes 1mg or less at night pre-bed time. I find this gives me the best pain management.

I have taken Suboxon in a maintenance method, meaning 1 large dose a day in the morning and I found that it is almost like a completely different drug. When dosing in this manor I really never felt anything from my sub outside of the first few days and some very mild only slightly noticeable opiate like effects for a few hours post dose. Other than the mild almost placebo post dose effects there were no ups and downs, no times of the day that I felt my dose was wearing off, it was almost like I was not really taking anything.

Now the way I take my Suboxone now I can feel the doses wearing off, and I wake up in the morning feeling like I need to dose (not just because of pain but because the first stages of withdrawal are showing), and as I dose through out the day I feel a pronounced difference almost as if I was taking a full agonist.

Hope this helps.

 

[lorne667]

^ Yes, many people say "less is more" with suboxone, because in low doses you CAN get full agonist effects from Bupe

But half life in general is complicated, and as Sekio said, half life is not a 1-1 conversion, but does correlate strongly enough to provide a good reference.One thing that further complicates things, is that many drugs have active metabolites, and in these cases, it is the half life of the active metabolite that will primarily control effects, for example, off-hand I think Tramadol has a half-life of like 6-8 hours, which is slightly above average, BUT it's active metabolite has a much longer half life of like 10-12 hours. Now, remember that Tramadol itself has such negligible opioid effects that it is, for all intents and purposes useless as an analgesic, yet it's metabolite had a much higher affinity, so that it is a "true agonist", albeit a mild one.

So in that case, the half-life of Tramadol itself is almost irrelevant, instead it is the half life of the metabolite(which I couldn't remember how to spell to save my life!!!) That effects it's RC value.

Yet another example is Klonopin, that has a stupid long half-life that averages like 18 hours, but I can tell you from the fact that clonazepam is literally the only benzo I like, that the peak effects of a SINGLE DOSE last a few hours, and then you have true relaxation for several hours after that, but, again with a single dose, any appreciable effects are long gone by the time the 18 hour mark arrives. Of course, if your like me, you load up on a ridiculous amount of WGFJ and tagament, in which case, yeah, a large dose can honestly give near full effects, even past the 18 hour mark, but with P450 enyzmes completely clogged, the half-life would be increased anyway, so it evens out.

Ultimately, only experience can tell you how well your body metabolizes something. The best thing to do beforehand is research, and average out reported duration of effects with the half life, to at least get a solid range that you should land in.

Also, taking large doses of P450 inhibitors(not 1 z glass of Grapefruit juice, or a single tagament, that will most likely do nothing beyond placebo) will substantially reduce the body's ability to clear the drug, resulting in an increase in effects, and an even larger increase in half-life. Seriously, just a few nights ago, I drank over half a 2lt bottle of WGFJ along with 6 or 7 tagament, and it was ridiculous, I mean my dose was literally twice as strong as it should have been, and I was high for over 24 hours, my roommate even said I was talking out of my head the night before, and I was just like, "WTF, I took less than I normally would" but it goes to show the power of inhibitors(oh, and I took several Loperamide, as well)

But PLEASE don't exceed 600-800mg of tagament at once if you have never taken it before, I have been having stomach problems the past few nights, and am so constipated it hurts, so seriously, don't be a moron!

 

[littlebaggies]

That's why I love this website, you people really know your stuff. Thanks for the input!