- Synthetic phenylpropylamine opioid
- Has weak mu-receptor activity and inhibits reuptake of noradrenaline
- Noradrenaline effects thought to help with neuropathic pain
- 18 times LESS binding affinity for mu opioid receptor than morphine
- Dose equivalent is 2.5:1
- Half-life is around 5 hours
- NB: Advere effects include hypotension and increased seizure risk
- Due to first pass metabolism oral bioavailability is around 32%
- Low protein binding
- Metabolism through phase 2 glucoronidation (55%) and sulfation (15%) to inactive metabolites
- 99% excreted in urine
- NOT recommended for renal impairment <30 mL/min - but no dosage adjustments for 30-90 mL/min
Comments