.Pharmacolibrary.Drugs.N_NervousSystem.N07B_DrugsUsedInAddictiveDisorders.N07BC01_Buprenorphine.Buprenorphine

Information

Buprenorphine is a semi-synthetic opioid used primarily in the treatment of opioid dependence and chronic pain. It is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor. It is approved for use in opioid substitution therapy and is available in multiple formulations including sublingual tablets, subcutaneous injection, and transdermal patches.

Pharmacokinetics

Pharmacokinetic parameters reported for healthy adult subjects, mixed sex, after single sublingual administration.

References

1. Gu, M, et al., & Zhu, X (2023). Population pharmacokinetics of buprenorphine and naloxone sublingual combination in Chinese healthy volunteers and patients with opioid use disorder: Model-based dose optimization. Frontiers in pharmacology 14 1089862–None. DOI:10.3389/fphar.2023.1089862 PUBMED:https://pubmed.ncbi.nlm.nih.gov/36744255

2. Ng, CM, et al., & Kraft, WK (2015). Population Pharmacokinetic Model of Sublingual Buprenorphine in Neonatal Abstinence Syndrome. Pharmacotherapy 35(7) 670–680. DOI:10.1002/phar.1610 PUBMED:https://pubmed.ncbi.nlm.nih.gov/26172282

3. Jones, AK, et al., & Laffont, CM (2021). Population Pharmacokinetics of a Monthly Buprenorphine Depot Injection for the Treatment of Opioid Use Disorder: A Combined Analysis of Phase II and Phase III Trials. Clinical pharmacokinetics 60(4) 527–540. DOI:10.1007/s40262-020-00957-0 PUBMED:https://pubmed.ncbi.nlm.nih.gov/33135125

Revisions

• 06/2025 Tomas Kulhanek, generated model from data extracted from PUBMED, DrugBank and LLM(GPT4.1)