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  • robinapark

Tapentadol

- 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


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