Inhibitors of acetylcholinesterase (often abbreviated AChEI ) or anti-cholinesterase are chemicals or drugs that inhibit the enzyme acetylcholinesterase from the breakdown of acetylcholine, thereby increasing both the level and duration of action of acetylcholine neurotransmitter. Acetylcholinesterase inhibitors are classified as reversible, irreversible, or quasi-irreversible (also called pseudo-irreversible).
Video Acetylcholinesterase inhibitor
Usage
Acetylcholinesterase Inhibitors:
- Occurs naturally as poison and poison
- Used as a weapon in the form of a nerve agent
- Used as an insecticide
- Used medically:
- To treat myasthenia gravis. In myasthenia gravis, they are used to increase neuromuscular transmission.
- To treat glaucoma
- To treat postural tachycardia syndrome
- As an anticholinergic toxicant antidote
- To reverse the non-depolarising muscle relaxant effect
- To treat symptoms of neuropsychiatric diseases such as Alzheimer's disease, especially apathy
- To increase the likelihood of lucid dreaming (by extending REM sleep)
- To treat Alzheimer's disease, Lewy's body dementia and Parkinson's disease. In this neurodegenerative condition AChEIs are mainly used to treat cognitive (memory and learner mostly) symptoms of dementia. These symptoms are attenuated because of the role of acetylcholine in cognition on CNS. There is some evidence to suggest that AChEIs may attenuate psychotic symptoms (especially visual hallucinations) in Parkinson's disease.
- To treat cognitive impairment in patients with schizophrenia. There is some evidence that demonstrates efficacy in treating positive, negative and affective symptoms.
- As a treatment for autism and to increase the percentage of rapid eye movements in autistic children, in line with the mechanisms that encourage them to dream clearly.
Maps Acetylcholinesterase inhibitor
Side effects
Some of the main effects of cholinesterase inhibitors are:
- Actions on the parasympathetic nervous system, (parasympathetic branch of the autonomic nervous system) can cause bradycardia, hypotension, hypersecretion, bronchoconstriction, GI channel hypermotility, and decreased intraocular pressure.
- SLUDGE syndrome.
- Action on the neuromuscular junction will result in prolonged muscle contraction.
Administration of reversible cholinoesterase inhibitors is contraindicated with those with urinary retention due to obstruction.
Titration phase
When used in the central nervous system to relieve neurologic symptoms, such as rivastigmine in Alzheimer's disease, all cholinesterase inhibitors require doses to be gradually increased over several weeks, and this is usually referred to as the titration phase . Many other types of drug treatments may require a titration or elevation phase. This strategy is used to build tolerance for side effects or to achieve the desired clinical effect. It also prevents accidental overdoses and is therefore recommended when starting treatment with very strong and/or toxic drugs (drugs with a low therapeutic index).
Example
Reversible inhibitor
Compounds that serve as competitive or noncompetitive inhibitors of reversible cholinesterase are the most likely to have therapeutic uses. These include:
- Some organophosphates are not listed under "Can not Be Fixed" below
- Karbamat
- Physostigmine
- Neostigmine
- Pyridostigmine
- Ambenonium
- Demecarium
- Rivastigmine
- Phenanthrene's derivatives
- Galantamine
- Caffeine - uncompetitive (also an Adenosine receptor antagonist)
- Rosmarinic acid - Caffeic acid ester. Found in plant species of Lamiaceae family.
- Alpha-Pinene - uncompetitive reversible
- Piperidine
- Donepezil
- Tacrine, also known as tetrahydroaminoacridine (THA ')
- Edrophonium
- Huperzine A
- Ladostigil
- Not Collapse
- Lactucopicrin
- Acotiamide
Comparison table
Pseudo inhibitor that can not be changed
Compounds that act as quasi-irreversible inhibitors of cholinesterase are the most likely to be used as chemical or pesticide weapons. These include:
See also
- Pesticide poisoning
References
External links
- Acetylcholinesterase inhibitor at the US National Library of Medicine's Medical Subject Headings (MeSH)
- Acetylcholinesterase: Enzyme cork-gorge Interesting article GDP structure in PDBe
Source of the article : Wikipedia
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