Donepezil: Difference between revisions
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* Date of FDA Approval (Patent Expiration): 1996 (2008)<br /> | * Date of FDA Approval (Patent Expiration): 1996 (2008)<br /> | ||
* 2006 Sales: $800 Million | * 2006 Sales: $800 Million | ||
* Why You Should Care: One of the most effective treatments for | * Why You Should Care: One of the most effective treatments for the symptoms of [[Alzheimer's Disease]], although no definitive proof exists as to whether to alters the progression of the disease. | ||
* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information | * The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information | ||
===Mechanism of Action=== | ===Mechanism of Action=== | ||
Donepezil is a potent [[Acetylcholinesterase]] inhibitor to the active site of <scene name='Donepezil/Ache/1'>AChE</scene>. | Donepezil is a potent [[Acetylcholinesterase]] (AChE) inhibitor to the active site of <scene name='Donepezil/Ache/1'>AChE</scene> 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 . Donepezil binds along the active-site gorge, extending from the anionic subsite near <scene name='Donepezil/Trp_84/1'>Trp 84</scene> to the peripheral anionic site near <scene name='Donepezil/Trp_279/1'>Trp 279</scene>. Interestingly, it does not directly interact with the catalytic triad of acetylcholinesterase nor the oxyanion hole. Further, donepezil does not form any direct hydrogen bonds with AChE nor electrostatic interactions, but rather only interacts via aromatic stacking and solvent mediated interactions. It <scene name='Donepezil/Bound/1'>primarily interacts</scene> with Glu 199, His 440, Phe 330, Trp 84, Tyr 334, Tyr 121, Phe 331, Phe 288, Ser 286, Phe 290, Arg 289, Trp 279, & Leu 282 to tightly bind to AChE. | ||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||