Galantamine: Difference between revisions
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<applet load="" size="480" color="" frame="true" spin="on" Scene ="Galantamine/Galantamine/ | <applet load="" size="480" color="" frame="true" spin="on" Scene ="Galantamine/Galantamine/2" align="right" caption="Galantamine, also known as Razadyne"/> | ||
===Better Known as: Razadyne=== | ===Better Known as: Razadyne=== | ||
* Marketed By: <br /> | * Marketed By: Ortho Mcneil Janssen Pharmaceuticals (Subsidiary of Johnson & Johnson)<br /> | ||
* Major Indication: [[Alzheimer's Disease]]<br /> | * Major Indication: [[Alzheimer's Disease]]<br /> | ||
* Drug Class: [[Acetylcholinesterase]] Inhibitor | * Drug Class: [[Acetylcholinesterase]] Inhibitor | ||
* Date of FDA Approval (Patent Expiration): <br /> | * Date of FDA Approval (Patent Expiration): 2001 (2008) <br /> | ||
* 2006 Sales: $225 Million<ref>Irena Melnikova, Therapies for Alzheimer's disease, Nature Reviews Drug Discovery 6, 341-342 (May 2007)</ref> | * 2006 Sales: $225 Million<ref>Irena Melnikova, Therapies for Alzheimer's disease, Nature Reviews Drug Discovery 6, 341-342 (May 2007)</ref> | ||
* Importance: | * Importance: Part of a newer generation of treatments for [[Alzheimer's Disease]], although no definitive proof exists as to whether it alters the progression of the disease. | ||
* | * See [[Pharmaceutical Drugs]] for more information about other drugs and disorders | ||
===Mechanism of Action=== | ===Mechanism of Action=== | ||
Galantamine is a potent [[Acetylcholinesterase]] (AChE) inhibitor to the active site of <scene name='Galantamine/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. Galantamine binds to the same active site gorge as acetylcholine <scene name='Galantamine/Binding/1'>interacting with the residues</scene> Glu 199, Phe 330, Trp 84, His 440, Phe 288, PHe 290, Tyr 121, Phe 331, Gly 119, Ser 200, Gly 118, and Gly 117 to tightly bind to AChE.<ref name="Guillou">PMID:15563167</ref> These interactions, which are primarily hydrophobic and pi stacking interactions, allow Galantamine outcompete Acetylcholine for the AChE active site. | |||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
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{{:Acetylcholinesterase Inhibitor Pharmacokinetics}} | |||
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===References=== | ===References=== | ||