E. The medicinal chemistry of opioid analgesics 3 Flashcards
1
Q
Why does morphine-6-glucuronide possess a higher analgesic activity onse it crosses the BBB?
A
Has a higher affinity of meu receptors
2
Q
Why should patients with poor renal function or renal failure be monitored when taking medicine that are metabolised into morphine-6-glucuronide ?
A
Morphine-6-glucuronide is readily excreted, therefore can accumulate in patients what have poor renal function or renal failure. Especially in elderly patients. This can increase the risk of inadvertent overdose.
3
Q
What are the normal strategies of developing morphine analogues?
A
Vary substituents
Extend molecular structure
Simplify
Conformational/rotational restrictions
