Tuesday, October 23, 2012

Buprenorphine Dose Response Plots

These two graphs show the differences between a full agonist, partial agonist and an antagonist.  Note that the partial agonist graph begins to level off at higher dosages.  This is the "ceiling effect" where increasing the dose has no additional effect.

Two other things people should know.  Bupe grabs onto the mu opioid receptor (MOR) and doesn't let go easily.  It's harder to overdose (OD) on bupe than other opioids, but if someone is ODing on bupe it will require more narcan to revive them than a heroin OD.  Whereas a single vial of narcan would work for heroin a bupe OD may require several vials.  There is a flip side to this, the partial agonist action of bupe means that it can be used to reverse an OD caused by a full agonist.  I do not recommend this and would follow the advice posted on Heroin Helper regarding ODs.  HOWEVER if you cannot revive the person and either the EMTs or local hospital is too far off, giving a dose of suboxone  may bring them back.   There was a case printed in the Journal Addition.

A case of heroin overdose reversed by sublingually administered buprenorphine/naloxone (Suboxone). 
Addiction. 2008 Jul;103(7):1226-8.

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