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Optimizing Absorption of Buprenorphine

Posted Apr 22 2010 1:42pm 1 Comment

A ‘quick one’…  I have written before about getting the most buprenorphine from a God-awfully expensive tablet of Suboxone, and will repeat myself for newcomers.  Note that my description is based on an understanding of pharmacology, organic chemistry, and physiology– NOT on the recommendations of Reckitt-Benckiser or the FDA.  My suggestions also come from knowledge of other, similar medications that are absorbed through mucous membranes– for example fentanyl, which is dispensed with a trans-mucosal delivery system for cancer pain.

A bit of background…  the reason you can’t just swallow a tablet of buprenorphine and expect it to work is because of something called ‘first pass metabolism.’  The liver is very good at breaking down buprenorphine in MOST people.  Buprenorphine and other medications, if swallowed, pass through the lining of the small intestine into the ‘portal vein’, which delivers them very efficiently to the liver, where they are effectively metabolized.  Some medications including fluoxetine (Prozac) will interfere with liver metabolism; I have not seen studies showing the levels of buprenorphine in such cases, but I would presume that levels of buprenorphine would be higher in general in people taking fluoxetine, especially comparing levels in people who swallow buprenorphine tablets whole.  As an aside, naloxone, the other ingredient in Suboxone, is also rapidly destroyed by ‘first pass metabolism.’  Because of first pass metabolism, little naloxone or buprenorphine accumulates in the bloodstream after oral ingestion.

Buprenorphine diffusion

Schematic of Oral Mucosa

Suboxone is therefore designed to be taken ‘trans-mucosally’, i.e. via absorption through the lining of the oral cavity into the bloodstream (the lining of the oral cavity is called ‘mucosa.’  The passage of molecules through the oral mucosa is affected by a number of things– the size of the molecule, the lipid solubility of the molecule, the concentration of the molecule, etc.  Buprenorphine is a lipid-soluble molecule that passes through the mucosa relatively easily, whereas naloxone is more water-soluble, and crosses the mucosa very poorly.  THAT is the basis for why the naloxone in Suboxone is not active;  only buprenorphine enters the bloodstream in significant amounts through the oral mucosa, and BOTH buprenorphine and naloxone are destroyed after being swallowed.

The goal with buprenorphine is to keep a level of the medication in the bloodstream that is above the ‘ceiling’ level– the level where the maximum opiate effect is obtained, above which no more effect can be gained with higher levels.  If the blood level stays above that ceiling level during the entire interval between doses, there will be no drop-off in opiate effect, i.e. no withdrawal, and no cravings for opiates (except for psychological cravings that can be quite intense initially, but that can be reduced through proper use of the medication.)  A constant level above the ‘ceiling’ is also necessary to prevent feeling ups and downs while on the medication.  If the level remains above the ceiling point, the person feels ‘normal’ all of the time, and gets no ‘high’ from taking the medication. 

Suboxone is, of course, too expensive;  the generic form of Subutex was initially priced at about $2.50 per 8 mg tablet, but the price is now approaching the price of brand-name Suboxone.  Some people require higher doses of medication than others, depending on body size, liver function, other medications, and other factors.  Most of my patients take around 12 mg of buprenorphine per day;  some take 8, some take 16, and some take doses as low as 2 mg per day.  In my experience the need for doses above 16 mg is rare, and if a person is getting ‘withdrawal’ at 16 mg I consider ineffective dosing as a potential problem.  In some cases the ‘withdrawal’ is actually psychologically-based, and would not respond to any dose of buprenorphine without an intervention to correct the patient’s perceptions.   But when the problem is ineffective dosing, I have seen very good results by making some changes in the way the person takes the buprenorphine, in order to optimize absorption.  Here was my suggestion to optimize absorption for a person who wrote to me the other day:

Absorption of buprenorphine is affected by a number of factors.  The three things that affect absorption that you can control are the concentration of buprenorphine in solution, the amount of surface area for buprenorphine to pass through, and the time allowed for absorption to occur.  So start with a dry mouth (swallow first), then crush an entire tab between your teeth to get it dissolved right away, in a very small amount of saliva.  That will increase the concentration of buprenorphine in solution, driving the diffusion of the molecule down the concentration gradient, into tissue.  Then ‘paint’ all of the surfaces in your mouth using your tongue as the paintbrush.  Try to spread the concentrated mixture over every surface;  there is nothing special about the tissue under the tongue.  The buprenorphine molecule will stick to the fresh surfaces, then pass through the mucosa, eventually diffusing into the bloodstream at a capillary.  After painting and re-painting the oral surfaces for 10-15 minutes, you can swallow the rest;  most of the absorption will have occurred by that time.   Be sure not to eat or drink for at least 10 minutes, though, so that buprenorphine molecules that are bound to the mucosa are not rinsed away, and rather can be absorbed.

I have seen good responses to this technique.  I have also been told that taking buprenorphine in this way shortens the time that it takes to dose.  For those who hate the taste, try putting an Altoid or half of a Life Saver in your mouth while dosing;  just avoid increasing the volume to a large extent, as that will reduce diffusion and absorption of buprenorphine.  You could also try sucking on an ice cube and then dosing, as the cold will reduce the function of your taste buds;  I would have a little concern, though, that absorption of buprenorphine will be slowed down by the cold as well, since blood flow through capillaries will be reduced after chilling the mucosa.

I expect there eventually to be a number of options for taking buprenorphine.  Hopefully we will eventually have some ‘American-style competition’ that gets the price per tablet out of the stratosphere!

Comments (1)
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i thought  that graphic drawing of the oral muscoa  initially was a drawing of an abstract garden!ha

 Helpful article especially swallowing first,swishing around.Someones i wish sub came in a swallow tablet,as its awkward at work if i take sub and someone rings or talks to me and im mumbling away!.Occasionally ive said i have a homeopathic tab- i.e schussler? salts-  dissolving in my mouth,but then i have to n.b to have a bottle of them on me,as the person  often wants to look at the homepathic out of interest. sigh.its complicated.Also nicotine replacement microtabs are another good excuse.

Sometimes ive said ive bn to the dentist if i have to talk (while out in a shop or businness) while its dissolving!

Interestingly ,an acquaintence  of mine takes her  sub doses at work up the rectum-like a suppository,so she dosent have to explain her mumbling.Shes an ex addict so cant tell  work people shes on sub.I mean its all mucosa right?!This method could perhaps  help  sub people who suffer nausea,asthma or other conditions.What do u think doc?Of course youd have to have a clean bum! zac.

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