Acetylcholinesterase rivastigmine

Corey-Bloom J, Anand R, Veach J, for the ENA 713 B352 Study Group (1998). A randomised trial evaluating the efficacy and safety of ENA 713 (rivastigmine tartrate), a new acetylcholinesterase inhibitor, in patients with mild and moderately severe Alzheimer s disease. IntJGeriatrPsychopharmacolX, 55-65. 

Anticholinesterase A drug that inhibits the enzyme acetylcholinesterase, which normally inactivates acetylcholine at the synapse. The effect of an anticholinesterase (or cholinesterase inhibitor) is thus to prolong the duration of action of the neurotransmitter. An example is rivastigmine, used in the treatment of Alzheimer s disease. 

Rivastigmine has central activity at acetylcholinesterase and butyrylcho-linesterase sites, but low activity at these sites in the periphery. 

Polinsky RJ, Cfinical pharmacology of rivastigmine, a new-generation acetylcholinesterase inhibitor for the treatment of Alzheimer s disease, Clin Ther 20 634-647, 1998. 

Rivastigmine Transdermal (Exelon Patch) [Cholinesterase Inhibitor/Anti-Alzheimer Agent] Uses MUd/mod Alzheimer and Parkinson Dz dementia Action Acetylcholinesterase inhibitor Dose Initial 4.6-mg patch/d applied to back, chest, upper arm, T 9.5 mg after 4 wk if tolCTated Caution [ ] Sick sinus synd, conduction defects, asthma, COPD, urinary obst, Sz Contra Hypersensitivity to rivastigmine, other carbamates Disp Transdermal patch 5 cm (4.6 mg/24 h), 10 cm (9.5 mg/24 h) SE NA /D EMS See Rivastigmine OD See Rivastigmine... 

The results with the recently introduced centrally acting inhibitors of acetylcholinesterase like tacrine and rivastigmine for the treatment of Alzheimer s disease are modest at best. 

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. 

Rivastigmine 40% 1.5 None anticipated Not hepatically metabolized (metabolized by hydrolysis and renally eliminated) Dual acetylcholinesterase and butyrylcholinesterase inhibitor... 

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). 

Gottwald MD, Rozanski RI. Rivastigmine, a brain-region selective acetylcholinesterase inhibitor for treating Alzheimer s disease review and current status. Expert Opin Invest Drugs 1999 8(10) 1673-82. 

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... 

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