3. Old stuff
          3.1. Old pharm stuff (pre 2009)
              3.1.3. Pharmacology
                  3.1.3.5. Opioids
                      3.1.3.5.5. Opioid antagonists
 3.1.3.5.5.4. Methylnaltrexone 

Methylnaltrexone

[SH4:p121]

Structure

  • Quaternary opioid receptor antagonist
  • Highly ionised quaternary methyl group limits transfer across BBB
    --> Methylnaltrexone is only active at peripheral opioid receptors

Effects

  • Attenuates morphine-induced changes in gastric emptying
  • Decreases incidence of N&V
    * Direct antagonism of morphine at the chemoreceptor trigger zone (located outside BBB)
    * Improved gastric emptying