Title : Clinical pharmacology of rivastigmine: a new-generation acetylcholinesterase inhibitor for the treatment of Alzheimer's disease.

Pub. Date : 1998 Jul-Aug

PMID : 9737824






12 Functional Relationships(s)
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1 Clinical pharmacology of rivastigmine: a new-generation acetylcholinesterase inhibitor for the treatment of Alzheimer"s disease. Rivastigmine acetylcholinesterase (Cartwright blood group) Homo sapiens
2 Rivastigmine (ENA 713, or carbamoylatine) is an acetylcholinesterase (AChE) inhibitor with brain-region selectivity and a long duration of action. Rivastigmine acetylcholinesterase (Cartwright blood group) Homo sapiens
3 Rivastigmine (ENA 713, or carbamoylatine) is an acetylcholinesterase (AChE) inhibitor with brain-region selectivity and a long duration of action. Rivastigmine acetylcholinesterase (Cartwright blood group) Homo sapiens
4 Rivastigmine (ENA 713, or carbamoylatine) is an acetylcholinesterase (AChE) inhibitor with brain-region selectivity and a long duration of action. Rivastigmine acetylcholinesterase (Cartwright blood group) Homo sapiens
5 Rivastigmine (ENA 713, or carbamoylatine) is an acetylcholinesterase (AChE) inhibitor with brain-region selectivity and a long duration of action. Rivastigmine acetylcholinesterase (Cartwright blood group) Homo sapiens
6 Both preclinical studies and studies in human volunteers have shown that rivastigmine induces substantially greater inhibition of AChE in the central nervous system (CNS) compartment than in the periphery (40% inhibition of central AChE compared with 10% inhibition of plasma butylcholinesterase in healthy volunteers). Rivastigmine acetylcholinesterase (Cartwright blood group) Homo sapiens
7 Both preclinical studies and studies in human volunteers have shown that rivastigmine induces substantially greater inhibition of AChE in the central nervous system (CNS) compartment than in the periphery (40% inhibition of central AChE compared with 10% inhibition of plasma butylcholinesterase in healthy volunteers). Rivastigmine acetylcholinesterase (Cartwright blood group) Homo sapiens
8 Moreover, rivastigmine preferentially inhibits the G1 enzymatic form of AChE, which predominates in the brains of patients with Alzheimer"s disease (AD). Rivastigmine acetylcholinesterase (Cartwright blood group) Homo sapiens
9 Evidence from animal studies also suggests that rivastigmine is a more potent inhibitor of AChE in the cortex and hippocampus, the brain regions most affected by AD. Rivastigmine acetylcholinesterase (Cartwright blood group) Homo sapiens
10 The principal metabolite of rivastigmine has at least 10-fold lower activity against AChE compared with the parent drug. Rivastigmine acetylcholinesterase (Cartwright blood group) Homo sapiens
11 Distribution of rivastigmine into the CNS is extensive, and inhibition of AChE in the cerebrospinal fluid is detectable 1.2 hours after oral dosing in both healthy volunteers and patients with AD. Rivastigmine acetylcholinesterase (Cartwright blood group) Homo sapiens
12 Rivastigmine is inactivated during the process of interacting with and inhibiting AChE, and, in contrast to other AChE inhibitors, the hepatic cytochrome P-450 (CYP-450) system is not involved in the metabolism of rivastigmine. Rivastigmine acetylcholinesterase (Cartwright blood group) Homo sapiens