N-Oxidation Flashcards
1
Q
What is this reaction?
A
An N+ — O- (nitrogen oxide) group is formed from a tertiary amine.
2
Q
What enzymes are involved?
A
Microsomal amine oxidase (NO CYP involved!)
3
Q
What is the problem with this metabolism of a drug?
A
The product is charged, so cannot use as a drug - won’t be able to cross the Blood Brain Barrier
4
Q
What could happen at body pH?
A
Tertiary amines have a 50% chance of undergoing N-Oxidation, so half of the drug formed will be charged, and won’t be able to reach target receptors in the brain.
5
Q
Give examples of drugs that undergo this metabolsim
A
Nicotine, Imparamine
