Because Buprenorphine is metabolized relatively quickly by the liver, oral use is not recommended but instead sublingually or under the tongue. Buprenorphine primarily affects the mu-opioid receptor acting as a partial agonist; therefore the receptor activation increases as the dose does until the plateau is reached. This is beneficial because, in the case of full opioid agonists, the receptor activation increases as the dose increases which can lead to death. Buprenorphine has a high affinity and slow dissociation from mu-opioid receptors which allow it to block other receptors temporarily(4). This is the process that causes patients who have recently used opioids to go through withdrawal.
Dosing
Managing opioid addiction with buprenorphine can be put into three phases: induction, stabilization, and maintenance. The induction phase is the switch from illicit opioid use to buprenorphine, lasting around a week. Making sure the patient understands and is aware of the risks of sudden withdrawal if buprenorphine is begun too quickly(4).
Once the patient begins to present opioid withdrawal symptoms, the physician will administer the initial dose under observation for side effects. If the patient continues to experience opioid withdrawal, illicit opioid use should be suspected and