What is the mechanism of action of buprenorphine in the treatment of opioid abuse?

Updated: Jun 21, 2018
  • Author: David W Dixon, DO; Chief Editor: Glen L Xiong, MD  more...
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Buprenorphine is a partial agonist at the mu receptor (it can only partially activate the receptor). Therefore the intensity of mood alteration induced by buprenorphine plateaus, and users do not generally feel the rush or intense high they feel when using other opioids. This has been termed a ceiling effect. Fortunately, buprenorphine’s partial agonism is sufficient to prevent cravings and withdrawal symptoms. Therefore, like methadone, buprenorphine can be used to replace other more destructive opioids via maintenance therapy.

Buprenorphine also binds extremely tightly to the mu receptor. This tight binding prevents other opioids from accessing the mu receptor, in turn preventing a user from getting high on other opioids. Moreover, buprenorphine’s binding is so strong that it displaces other opioids from mu receptors. Therefore, if buprenorphine is taken while a patient has significant serum levels of another opioid, the patient will rapidly experience withdrawal symptoms as the other opioid is displaced from receptors. The Substance Abuse and Mental Health Services Administration (SAMHSA) recommends the induction phase of buprenorphine be preceded by 12 to 24 hours of opioid abstinence in order to avoid the acute withdrawal symptoms caused by the displacement of opioid agonists from mu receptors. [11]

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