Cholinesterase inhibitor


Cholinesterase inhibitors, also known as anti-cholinesterase, are chemicals that prevent the breakdown of the neurotransmitter acetylcholine or butyrylcholine. This increases the amount of the acetylcholine or butyrylcholine in the synaptic cleft that can bind to muscarinic receptors, nicotinic receptors and others. This group of inhibitors are divided into two subgroups, acetylcholinesterase inhibitors and butyrylcholinesterase inhibitors.
They may be used as drugs for Alzheimer's and myasthenia gravis,. Side effects when used as drugs may include loss of appetite, nausea, vomiting, loose stools, vivid dreams at night, dehydration, rash, bradycardia, peptic ulcer disease, seizures, weight loss, rhinorrhea, salivation, muscle cramps, fasciculations.
Cholinesterase inhibitors are indirect-acting parasympathomimetic drug.

Medical use

While 4 cholinesterase inhibitors are approved in the United States only three are available commercially. The three available are rivastigmine, donepezil, and galantamine while tacrine is not.
They are generally used to treat Alzheimer's disease and dementia. If a benefit occurs this is generally at two to third month after starting.
It's difficult to determine which cholinesterase inhibitor has greater efficacy due to design flaws in head-to-head comparison study.

Cholinesterase inhibitor toxicity

Common Side effects include insomnia, nausea and vomiting, accidental injury, headache, dizziness, bradycardia, hypotension, ecchymosis, sleep disturbance

Binding affinity

Acetylcholinesterase inhibitors

, phenserine, huperzine A, and BW284c51 are selective AChE inhibitors.

Butyrylcholinesterase inhibitor

Tetra pyrophosphoramide and ethopropazine are selective BChE inhibitors.

AChE & BChE inhibitor

and rivastigmine are both acetylcholinesterase inhibitor and butyrylcholinesterase inhibitor.
USFDA's Administration Adverse Event Reporting System database compared rivastigmine to the other cholinesterase inhibiting drugs donepezil and galantamine found that rivastigmine was associated with a higher frequency of reports of death as an adverse event.

Acetylcholinesterase inhibitors & nicotinic receptor modulator">Allosteric_modulator">modulator

might be less well tolerated than donepezil and rivastigmine.

History

Given the cognitive-enhancing property of nicotine and higher-than-expected overlap in cigarette smoking in people with ADHD regardless of age, researchers believe there exists a link between nicotine and ADHD. Afterwards, the transdermal nicotine has proved reducing ADHD symptoms in adolescents and adults, which in turn contributed to their cessation of smoking. ABT-418 and ABT-089 are the leading candidate agents.