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  • robinapark

Buprenorphine

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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