How Do Central Acetylcholinesterase Inhibitors Work?

Central acetylcholinesterase (AChE) inhibitors also known as cholinesterase inhibitors are drugs that prevent the breaking down of acetylcholine (ACh) and increase the duration of action and levels of ACh in the nerve endings called synapses. These drugs are used to treat Alzheimer’s disease and associated abnormalities such as:

• Dementia
• Confusion
• Aggression
• Psychosis

ACh is an essential neurotransmitter released into space between two neurons (synaptic cleft) by the presynaptic neuron. It carries out various functions at neuromuscular junctions at synapses in the ganglia of the visceral motor system within the central nervous system (the brain and spinal cord). Some important functions of ACh in the central nervous system include:

• Memory
• Attention
• Arousal
• Motivation
• Learning

AChE is concentrated in the synaptic cleft and hydrolyzes ACh into acetate and choline, decreasing ACh levels before it reaches the postsynaptic neuron. Centrally acting AChE inhibitors are selective and reversible inhibitors of AChE

Central AChE inhibitors are used to treat:

• Behavioral and cognitive effects of Alzheimer’s disease
• Severe Alzheimer’s disease
• Alzheimer dementia
• Vascular dementia

Side effects of central AChE inhibitors include:

• Dizziness
• Nausea and vomiting
• Diarrhea
• Excess mucus secretion in the respiratory tract
• Trouble breathing
• Loss of appetite
• Abdominal pain
• Weakness
• Muscle and joint pains
• Trouble sleeping
• Tremors
• Syncope
• Vertigo (spinning sensation)
• Anxiety

Other serious side effects of central AChE inhibitors include:

• Liver failure
• Arrhythmia (irregular heartbeats)
• Seizures
• Anaphylaxis (life-threatening allergic reaction)
• Stevens-Johnson syndrome (severe skin reaction where the skin and mucous membranes are damaged)

The information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of central AChE inhibitors include:

• Donepezil (Aricept, Aricept ODT)
• Donepezil transdermal (Pending Food and Drug Administration approval)
• Galantamine (Razadyne)
• Memantine/donepezil (Namzaric)
• Rivastigmine (Exelon, Exelon Patch)