Cholinergic blocking drugs
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- See also: Anticholinergic
Added by PhloxBot
Added by PhloxBotAn acetylcholinesterase inhibitor or anti-cholinesterase is a chemical that inhibits the cholinesterase enzyme from breaking down acetylcholine, so increasing both the level and duration of action of the neurotransmitter acetylcholine.
Contents |
Uses
Edit
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
- as an antidote to anticholinergic poisoning
ExamplesEdit
reversible inhibitorEdit
Compounds which function as reversible competitive or noncompetitive inhibitors of cholinesterase are those most likely to have therapeutic uses. These include:
- Carbamates
- Phenanthrine derivatives
- Piperidines
- donepezil, also known as E2020
- Organophosphates
- Tacrine, also known as tetrahydroaminoacridine (THA')
- Edrophonium
- Phenothiazines
These need classifyingEdit
Comparison tableEdit
| Inhibitor | Duration[1] | Main site of action[1] | Clinical use[1] | Adverse effects[1] |
|---|---|---|---|---|
| edrophonium | short | neuromuscular junction | diagnosis of myasthenia gravis | |
| neostigmine | medium | neuromuscular junction |
| visceral |
| physiostigmine | medium | postganglionic parasympathetic | treat glaucoma (eye drops) | |
| pyridostigmine | medium | neuromuscular junction |
| |
| dyflos | long | postganglionic parasympathetic | historically to treat glaucoma (eye drops) | toxic |
| ecothiopate | long | postganglionic parasympathetic | treat glaucoma (eye drops) | systemic effects |
| parathion | long | none | toxic |
quasi-irreversible inhibitorEdit
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 (Supplements)Edit
EffectsEdit
Some major effects of anticholinesterases:
- Actions on the autonomic nervous system, that is parasympathetic nervous system will cause bradycardia, hypotension, hypersecretion, bronchoconstriction, GI tract hypermotility, and decrease intraocular pressure.
- SLUD syndrome.
- Actions on the neuromuscular junction will result in prolonged muscle contraction.
See also Edit
- Antiemetic drugs
- Antispasmodic drugs
- Cholinergic nerves
- Cholinomimetic drugs
- Hallucinogenic drugs
- Pesticide poisoning
- Phenothiazine derivatives
References Edit
- ↑ 1.0 1.1 1.2 1.3 Unless else specified n boxes, then ref is:Rang, H. P. (2003). Pharmacology, Edinburgh: Churchill Livingstone. Page 156
External linksEdit
Psychoanaleptics: anti-dementia drugs (N06D) | |
|---|---|
| Anticholinesterases | |
| Other | |
Parasympathomimetics (N07A) | |
|---|---|
| Anticholinesterases |
Stigmine (Neostigmine, Pyridostigmine, Distigmine) - Ambenonium |
| Choline esters | |
| Other parasympathomimetics | |
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