Buprenorphine and its formulations: a comprehensive review

Abstract

Buprenorphine, a novel long-acting analgesic, was developed with the intention of two purposes: analgesia and opioid use disorder. Regarding its pharmacodynamics, it is a partial agonist at mu receptors, an inverse agonist at kappa receptors, and an antagonist at delta receptors. For the purpose of analgesia, three formulations of buprenorphine were developed: IV/IM injectable formulation (Buprenex®), transdermal patch formulation (Butrans®), and buccal film formulation (Belbuca®). Related to opioid dependence, the formulations developed were subcutaneous extended release (Sublocade®), subdermal implant (Probuphine®), and sublingual tablets (Subutex®). Lastly, in order to avoid misuse of buprenorphine for opioid dependence, two combination formulations paired with naloxone were developed: film formulation (Suboxone®) and tablet formulation (Zubsolv®). In this review, we present details of each formulation along with their similarities and differences between each other and clinical considerations.

ASAM Clinical Considerations: Buprenorphine Treatment of Opioid Use Disorder for Individuals Using High-potency Synthetic Opioids

“…Extended release buprenorphine has been available since 2017 for the treatment of moderate to severe OUD 32 . There are 2 formulations of XR buprenorphine: Sublocade and Brixadi.…”

Availability and prescribing of extended release buprenorphine injection for Medicaid beneficiaries, 2018-2022

“…In 2017, a monthly buprenorphine injection (INJ-BUP), called Sublocade, was approved by the Food and Drug Administration for the treatment of opioid use disorder (OUD). (1) A second INJ-BUP, with both monthly and weekly dosages, called Brixadi, was approved in May 2023 and became available in September 2023. (2) These extended release formulations of buprenorphine have the potential to positively impact OUD treatment outcomes.…”

The Effectiveness of Buprenorphine Transdermal Patch and Low Dose Sublingual Buprenorphine Induction to Transition to Long-Acting Subcutaneous Buprenorphine Injection in Opioid Use Disorder in Inpatient Setting

“… 1 All forms of buprenorphine possess a unique pharmacological profile, functioning as a high-affinity partial agonist at μ-opioid receptors. 2 With an extended serum half-life and prolonged duration of action compared to traditional full agonists, it presents an attractive option for OUD treatment, as it induces less tolerance and poses a lower risk of respiratory depression. 1 This combination of factors makes it an appealing option for OUD as it produces less tolerance, and carries a lower risk for respiratory depression.…”