Acetylcholinesterase galantamine

Galantamine is a reversible inhibitor of acetylcholinesterase that also possesses nicotinic receptor agonist properties, and which is used in mild-to-moderate dementia in Alzheimer s disease. 

Galantamine hydrobromide (43 Reminyl ) Galantamine (42) Alkaloid NP Plant Alzheimer s disease Inhibits the activity of acetylcholinesterase (AChE) 393 02... 

Woodruff-Pak DS, Vogel RW 3rd, Wenk GL. (2001) Galantamine Effect on nicotinic receptor binding, acetylcholinesterase inhibition, and learning. Proc Natl Acad Sci USA 98 2089-2094. 

Pharmacology Galantamine is a competitive and reversible inhibitor of acetylcholinesterase. While the precise mechanism of galantamine s action is unknown, it may exert its therapeutic effect by enhancing cholinergic function. Pharmacokinetics ... 

Galantamine (Razadyne) [Cholinesterase Inhibitor] Uses Alzheimer Dz Action Acetylcholinesterase inhibitor Dose 4 mg PO bid, T to 8 mg bid after 4 wk may T to 12 mg bid in 4 wk Caution [B, ] T Effect w/ suc-cinylcholine, amiodarone, dildazem, verapamil, NSAIDs, digoxin X- effect w/ anticholinergics, T risk of death vs placebo Contra Severe renal/hepadc impair Disp Tabs, soln SE GI disturbances, wt loss, sleep disturbances, dizziness, HA Interactions T Effects W/ amitriptyline, cimeddine, erythromycin, fluoxetine, fluvoxamine, ketoconazole, paroxetine, quinidine EMS Use succinylcholine w/ caudon, may need a reduced dose monitor ECG for induced conduction abnormalities OD May cause cholinergic Sxs (SLUDGE), muscle weakness, resp depression, and Szs atropine may be used as antidote... 

Galantamine, unlike the other anticholinesterases in clinical use, is derived from the alkaloids from the daffodil and snowdrop family. It is a reversible, competitive inhibitor of acetylcholinesterase with some inhibitory action on butyryl cholinesterase. It is also an agonist at nicotinic receptor sites. Although a clinically effective drug, galantamine frequently causes gastrointestinal side effects. 

Greenblatt HM, Kryger G, Lewis T, Sihnan I, Sussman JL (1999) Structure of acetylcholinesterase complexed with(-)-galantamine at 2.3 A resolution. FEBS Lett 463 321-326. 

Huang F, Fu Y (2010) A review of clinical pharmacokinetics and pharmacodynamics of galantamine, a reversible acetylcholinesterase inhibitor for the treatment of Alzheimer s disease, in healthy subjects and patients. Curr Clin Pharmacol 5 115-124... 

Keywords Acetylcholinesterase inhibitors Donepezil Rivastigmine Galantamine Tacrine... 

Galantamine REMINYL 2000 acetylcholinesterase Jansen Alkaloid 3 natural product (plant)... 

Arias, E. et al., Unequal neuroprotection afforded by the acetylcholinesterase inhibitors galantamine, donepezil, and rivastigmine in SH-SY5Y neuroblastoma cells role of nicotinic receptors, J. Pharmacol. Exp. Ther., 315, 1346, 2005. 

Novel galantamine derivatives with indole moiety have exhibited an activity against acetylcholinesterase up to 95 times higher than the parent compound, with one promising lead binding in a region close to the peripheral anionic site of the enzyme, where the Q-loop of amyloid beta peptide adheres [57]. 

Thomsen T, Kewitz H (1990) Selective inhibition of human acetylcholinesterase by galantamine in vitro and in vivo. Life Sci 46 1553... 

In the other work [63], semi-empirical, restricted Hartree-Fock (RHF) and DFT calculations were carried out to study the well-known acetylcholinesterase inhibitors tacrine (32), galantamine (33), donepezil (34), tacrine dimer (35), and physo-stigmine (36). Some electronic and structural properties were evaluated (Table 7.3),... 

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