Rivastigmine: Difference between revisions

Rivastigmine is an [[Acetylcholinesterase]] (AChE) inhibitor. It binds to the active site of <scene name='Rivastigmine/Acetylcholinesterase/1'>AChE</scene>, utilizing many of the same residues which bind and break down acetylcholine. By inhibiting AChE, the important neurotransmitter, [[acetylcholine]], is degraded at a slower rate, helping reverse the marked decrease in neuronal function evident in [[Alzheimer's Disease]] patients. Rivastigmine is rapidly metabolized into its principal components (carbomyl and NAP moieties) which are powerful Acetylcholine inhibitors. These components primarily <scene name='Rivastigmine/Bound/1'>primarily interact with residues</scene> GLy 117, Gly 118, Gly 119 Ala 201, Trp 233, Phe 290, Trp 84, Phe 330, His 440, & Phe 288 in tightly binding to the AChE binding site via pi stacking and hydrogen bond interactions. Rivastigmine outcompetes acetylcholine for the active site of AChE, inhibiting the esterase<ref>PMID:11888271</ref>