Everyone Healthy medication library
Anticholinesterase Drug Class
Medicines in this drug class are grouped together in the Everyone Healthy medication database. This page is educational only and should not be used as personal prescribing advice.
Drug class overview
Anticholinesterase overview
Acetylcholinesterase inhibitor
Uses
Acetylcholinesterase inhibitors:
- Occur naturally as venoms and poisons
- Are used as weapons in the form of nerve agents
- Are used medicinally:
- To treat myasthenia gravis. In myasthenia gravis, they are used to increase neuromuscular transmission.
- To treat Alzheimer's disease
- To treat Lewy Body Dementia
- As an antidote to anticholinergic poisoning
Examples
Reversible inhibitor
Compounds which function as reversible competitive or noncompetitive inhibitors of cholinesterase are those most likely to have therapeutic uses. These include:
- Organophosphates
- Metrifonate (irreversible)
- Carbamates
- Phenanthrene derivatives
- Piperidines
- Donepezil, also known as E2020
- Tacrine, also known as tetrahydroaminoacridine (THA')
- Edrophonium
- Huperzine A
- Ladostigil
- Ungeremine[1]
Comparison table
Inhibitor  |
Duration[2] |
Main site of action[2] |
Clinical use[2] |
Adverse effects[2] |
|---|---|---|---|---|
| Edrophonium | short (10 min.) | neuromuscular junction | diagnosis of myasthenia gravis | |
| Neostigmine | medium (1-2 hrs.) | neuromuscular junction |
|
visceral |
| Physostigmine | medium (0.5-5 hrs.) | postganglionic parasympathetic | treat glaucoma (eye drops) | |
| Pyridostigmine | medium (2-3 hrs.) | neuromuscular junction |
|
|
| Dyflos | long | postganglionic parasympathetic | historically to treat glaucoma (eye drops) | toxic |
| Ecothiopate | long | postganglionic parasympathetic | treat glaucoma (eye drops) | systemic effects |
| Parathion (irreversible) | long | none | toxic |
Quasi-irreversible inhibitor
Compounds which function as quasi-irreversible inhibitors of cholinesterase are those most likely to have use as chemical weapons or pesticides. These include:
Natural Compounds
Effects
Some major effects of cholinesterase inhibitors:
- Actions on the autonomic nervous system, that is parasympathetic nervous system will cause bradycardia, hypotension, hypersecretion, bronchoconstriction, GI tract hypermotility, and decrease intraocular pressure.
- SLUDGE syndrome.
- Actions on the neuromuscular junction will result in prolonged muscle contraction.
Titration phase
When used in the central nervous system to alleviate neurological symptoms, such as rivastigmine in Alzheimer's disease, all cholinesterase inhibitors require doses to be increased gradually over several weeks, and this is usually referred to as the titration phase.[3]
See also
References
- ^ Rhee IK, I; Appels N, Hofte B, Karabatak B, Erkelens C, Stark LM, Flippin LA, Verpoorte R (November 2004). "Isolation of the Acetylcholinesterase Inhibitor Ungeremine from Nerine bowdenii by Preparative HPLC Coupled On-Line to a Flow Assay System". Biological & Pharmaceutical Bulletin 27 (11): 1804-1809. http://www.jstage.jst.go.jp/article/bpb/27/11/1804/_pdf.
- ^ a b c d Unless else specified n boxes, then ref is:Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 156
- ^ Inglis F. “The tolerability and safety of cholinesterase inhibitors in the treatment of dementia.” Int J Clin Pract. 2002;(127):45-63. PMID 12139367
External links
Structured database notes
Drug class attributes
These are structured notes stored against this drug class in the EH database. They should be interpreted cautiously and reviewed by a qualified clinician or pharmacist.
Class-level safety links
Possible class-level side effects / symptoms
These links come from the EH drug-class side-effect tables. They do not prove that every medicine in the class causes the symptom, or that the class caused a symptom in any individual person.
Class-level condition links
Conditions linked to this drug class
These are condition relationships stored against the drug class in the EH database. They are educational browsing links, not treatment recommendations.
Linked medicines