Buprenorphine: Clinical use, abuse and compliance monitoring

Buprenorphine was introduced in the United States as an injectable analgesic in 1981 and treatment option for opioid dependence in 2002; a transdermal formulation was approved for pain management in 2010. Following the introduction of this variety of dosage forms, buprenorphine use and misuse have increased significantly. This article reviews the pharmacology of buprenorphine and Co-Ingredient naloxone; Use in addiction medicine and pain management; and clinical challenges, with special emphasis on Drug-Drug interactions (pharmacokinetic and pharmacodynamic), safety concerns, and buprenorphine misuse. Buprenorphine accessibility for nonmedical use is widespread in some settings, and burgeoning prescription and abuse rates have led to multiple reports of overdoses and fatalities associated with its use. Buprenorphine abuse potential, prevalence and patterns of misuse, and risk factors associated with fatal overdose are discussed. Given the epidemic of prescription drug misuse, practitioners have an increasing need for clinical monitoring for compliance and misuse of controlled substances, including buprenorphine. Most guidelines recommend urine drug testing, but monitoring of buprenorphine presents special challenges to laboratories and practitioners interpreting results. Compliance and abuse monitoring for buprenorphine may be performed by different test methodologies, with immunoassay and mass spectrometry methods in most frequent use; each technology offers unique advantages and disadvantages. Testing of other specimen types for buprenorphine including blood, oral fluid, hair, sweat, breath, and meconium is feasible. The disposition of buprenorphine and its metabolites in each specimen type varies and may impact specific testing methodology. Interpreting drug tests requires understanding of buprenorphine's unique properties and factors that influence detection. Considerations include metabolic and dispositional patterns in tissues, and differences in the use of specific formulations or routes of administration (e.g., injection, sublingual, or transdermal) for specific applications.