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tapentadol

tapentadol

introduction

  • synthetic opiate-like analgesic similar to tramadol invented in the late 1980's and approved by TGA in Australia in 2010 as an S8 controlled drug
  • as with tramadol it has a dual mode of action as an agonist of the μ-opioid receptor and as a norepinephrine reuptake inhibitor (NRI)
  • analgesic efficacy comparable to that of oxycodone despite an alleged lower incidence of side effects
  • 100mg immediate release tapentadol appears to have similar analgesia to 15mg oxycodone but with less N/V although more somnolence
  • 100-250mg SR tapentadol bd appears to equate to 20-50mg SR oxycodone bd for analgesia

P/K

  • only 1/3rd of dose makes it past 1st pass hepatic metabolism
  • onset of action after oral administration is around 30min
  • duration of action of immediate release oral form is 4-6hrs
  • cleared mainly via hepatic metabolism
  • those who are rapid or ultra rapid metabolizers for the CYP2C9, CYP2C19, and CYP2D6 enzymes may not respond adequately to tapentadol therapy

C/I

  • epilepsy or in those prone to seizures as lowers seizure threshold
  • raises intracranial pressure so avoid in head injuries, patients with brain tumours, etc
  • patients at risk of respiratory depression eg. COPD, OSA, other resp. depressant medications
  • patients with low BP as may cause further lowering of BP
  • biliary disease or pancreatitis as may cause spasms of the sphincter of Oddi
  • liver disease as risk of reduced clearance and toxicity
  • patients on monoamine oxidase inhibitors (MAOIs) as risk of adrenergic storm
  • patients taking anti-muscarinic anticholinergic agents as risk of urinary retention

usual adult doses

  • immediate release form:
    • 50-100mg 4-6hrly o
  • slow release form:
    • 100mg bd o
tapentadol.txt · Last modified: 2019/07/10 00:25 by gary1