Dr. Proteau AChE Inhibitors Flashcards
T/F most AChE inhibitors are non-selective towards AChE and BuChE
True
what structural feature allows AChE inhibitors to enter CNS?
having a tertiary amine
what structural feature determines if the AChE inhibitor is a covalent modifier?
carbamate group
which enantiomer of Rivastigmine is the only one used?
S-enantiomer
Galantamine is more or less potent compared to Donepezil? why?
less potent
less aromatic groups
what is Sarin?
nerve gas
why does Sarin have slower regeneration compared to Echothiophate?
The O-C(CH3)2 group of Sarin is bulkier than the OE+ group of Echothiophate
what is malathion therapeutically used for?
lice
what are the two factors needed for an AChE reactivator?
- high selectivity/binding affinity for AChE (aromatic ring and a (+)-charge)
- need a hydroxylamine-like nucleophile that can be close to the modified serine of AChE
T/F reactivators have the ability to reactivate “aged” enzymes
false, unable to
would you expect dorzolamide and brinzolamide to potentially cause hypersensitivity in patients with sulfa allergies?
no because they’re structures do not contain sulfanilamides
which two structures are identical in dorzolamide and brinzolamide?
aryl sulfonamide and thiophene
what are the limitations of prostaglandin F2a?
poor penetration into the eye
rapid metabolism via oxidation at C15, B-oxidation, and w(omega)-oxidation
what structural feature of latanoprost helped it have better penetration into the eye?
isopropyl ester
what type of drug is latanoprost?
ester prodrug
