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