Details:
- Semi-synthetic
- Partial mu-receptor agonist
- Kappa-opioid ANTAgonist and agonist at opioid-receptor-like receptors (ORL-1)
- These opioid-receptor-like receptors are thought to help contribute to antihyperalgesic effects and use in neuropathic pain
- 'Phenanthrene opioid'
- High affinity for mu-opioid receptor - gives a ceiling for respiratory depression
- Dissociates slowly from the mu-opioid receptor --> slow onset, long half-life, and less risk of withdrawals
- Extensive first-pass metabolism so bioavailability around 10%
- Highly lipophilic and highly bound to plasma proteins
- Metabolised by glucoronidation to an inactive metabolite and by CYP3A4 to an active norbuprenorphine
- Most norbuprenorphine is excreted in faeces (70%)
- Pharmacokinetics of buprenorphine are NOT affected in kidney dysfunction
- Norbuprenorphine can accumulate, it has a lower potency compared to parent drug
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