Acetylcholinesterase donepezil

Alternatively, some studies used expert opinion to extrapolate the effectiveness of donepezil over a longer period (Neumann et al, 1999 O Brien et al, 1999). However, it is recognized that expert opinion can be the weakest source of evidence, which introduces considerable uncertainty into the analysis and interpretation of the results. In addition, the cost-effectiveness of acetylcholinesterase inhibitors depends heavily on the distribution of the cohort of patients across different severity states. O Brien s team found that the results of their model were very sensitive to this variable. In this context, the correct... 

Donepezil is a piperidine cholinesterase inhibitor, which reversibly and non-competitively inhibits centrally active acetylcholinesterase 34 This specificity is claimed to result in fewer peripheral side effects as compared to the other ChE inhibitors. 

Donepezil (Aricept) is a piperidine derivative with specificity for inhibition of acetylcholinesterase rather than butyrylcholinesterase. 

Pharmacology Donepezil enhances cholinergic function by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by acetylcholinesterase (AChE). Donepezil s effect may lessen as the disease process advances and fewer cholinergic neurons remain functionally intact. Pharmacokinetics ... 

V. Kaasinen, K. Nagren, T. Jarvenpaa, A. Roivainen, M. Yu, V. Oikonen, T. Kurki, J.O. Rinne, Regional effects of donepezil and rivastigmine on cortical acetylcholinesterase activity in Alzheimer s disease, J. Clin. Psychopharmacol. 22 (2002) 615-620. 

Donepezil is a selective, reversible inhibitor of acetylcholinesterase. Its long half-hfe allows for once-daUy dosing. Several stud-... 

Donepezil is currently approved worldwide as a first-line treatment for improving memory or at least slowing the rate of memory loss in Alzheimer s disease. It is a reversible, long-acting, selective piperidine inhibitor of acetylcholinesterase (AchE)... 

FIGURE 12—24. Icon for the cholinesterase inhibitor donepezil. This is the current first-line treatment for Alzheimer s disease, since it is a once daily agent without significant hepatotoxicity. It is a reversible agent, selective for acetylcholinesterase (AChE) over butyrylcholinesterase (BuChE), developed by American and Japanese companies. 

Donepezil hydrochloride (E2020) is the second drug approved by the US FDA for the treatment of mild to moderate Alzheimer s diseases (AD). It is a new class of acetylcholinesterase (AChE) inhibitor having an... 

Y.-F. Norio, F. Rie, T. Takenori, T. Tomonori, Determination of donepezil, an acetylcholinesterase inhibitor, in human plasma by high-performance liquid chromatography with ultraviolet absorbance detection, J. Chromatogr. B 768 (2002) 261-265. 

Donepezil is primarily a reversible inhibitor of acetylcholinesterase with a long elimination half-life. It lacks the hepatotoxicity of tacrine but frequently causes nausea, vomiting and diarrhoea. These side effects, together with occasional bradycardia, sycope and changes in the sleep architecture, are directly associated with a central and peripheral enhancement of cholinergic function. At the present time, donepezil is the most widely prescribed anticholinesterase in the United States and Europe. 

Q5 Donepezil is a reversible inhibitor of acetylcholinesterase, which is administered once daily. The starting dosage is 5 mg daily at bedtime, increasing if necessary after one month to 10 mg daily. 

An additive inhibitory effect of donepezil and neostigmine on acetylcholinesterase has been proposed to explain prolonged neuromuscular blockade during anesthesia in an 85-year-old woman taking donepezil (80). 

Sahin HA, Gurvit IH, Bilgic B, Hanagasi HA, Emre M. Therapeutic effects of an acetylcholinesterase inhibitor (donepezil) on memory in Wernicke-Korsakoff s disease. Clin Neuropharmacol 2002 25 16-20. 

Rivastigmine (1) was the second drug after donepezil in a class of second-generation acetylcholinesterase inhibitors to become commercially available. It is now marketed in over 60 countries worldwide, including those in Europe and South America and the United Kingdom. It has central selectivity, suggesting fewer peripheral adverse effects. These include nausea, vomiting, abdominal pain, and anorexia (2,3). Daily doses up to 12 mg were tolerated and produced improvement in patients with Alzheimer s disease (4). 

Donepezil has greater action on CNS acetylcholinesterase than on peripheral acetylcholinesterase... 

Of the acetylcholinesterase inhibitors, tacrine, methoxy-tacrine, metrifonate, donepezil hydrochloride, and rivastigmine are used in the treatment of Alzheimer s disease. In 12-30% of patients with Alzheimer s disease, tacrine causes an increase in hepatic transaminase activity. Abdominal adverse effects are very frequent, for example nausea, anorexia, diarrhea. The peripheral cholinomimetic effects of tacrine occur in a very high proportion of patients, probably the majority. The hepatic effects seem to be such that the use of these new (and in some cases still experimental) drugs would not be justified in... 

Donepezil acts primarily as a reversible inhibitor of acetylcholinesterase with a half-life of over 70 hours. Prolonged paralysis lasting several hours and requiring postoperative mechanical ventilation in the intensive care unit has been reported after the use of suxamethonium in a patient taking long-term donepezil (285). 

Friedhoff LT, Rogers SL. Correlation between the clinical efficacy of donepezil HCl (E2020) and red-blood cell (RBC) acetylcholinesterase (ACHE) inhibition in patients with Alzheimer s disease. Clin Pharmacol Ther 1997 61 177. 

---