Cholinergic blocking drugs

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An 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 1 Uses 2 Examples 2.1 reversible inhibitor 3 These need classifying 3.1 Comparison table 3.2 quasi-irreversible inhibitor 3.3 Natural Compounds (Supplements) 4 Effects 5 See also 6 References 7 External links

[edit] 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
  • as an antidote to anticholinergic poisoning

[edit] Examples

[edit] reversible inhibitor

Compounds which function as reversible competitive or noncompetitive inhibitors of cholinesterase are those most likely to have therapeutic uses. These include:

• Carbamates
  • physostigmine
  • neostigmine
  • pyridostigmine
  • ambenonium
  • demarcarium
  • rivastigmine
• Phenanthrine derivatives
  • galantamine
• Piperidines
  • donepezil, also known as E2020
• Organophosphates
  • metrifonate
• Tacrine, also known as tetrahydroaminoacridine (THA')
• Edrophonium
• Phenothiazines

[edit] These need classifying

• Atropine
• Benactyzine
• Levodopa
• Nicotine
• Orphenadrine
• Scopalamine
• Trihexyphenidyl

[edit] Comparison table

Comparison of reversible acetylcholinesterase inhibitors

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	reverse neuromuscular block (intravenously) treat myasthenia gravis (orally)	visceral
physiostigmine	medium	postganglionic parasympathetic	treat glaucoma (eye drops)
pyridostigmine	medium	neuromuscular junction	treat myasthenia gravis (orally)
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

[edit] 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:

• Organophosphates
  • echothiophate
  • diisopropyl fluorophosphate
  • cyclosarin
  • sarin
  • soman
  • tabun
  • VX
  • VE
  • VG
  • VM
  • diazinon
  • malathion
  • parathion
• Carbamates
  • aldicarb
  • bendiocarb
  • bufencarb
  • carbaryl
  • carbendazim
  • carbetamide
  • carbofuran
  • chlorbufam
  • chloropropham
  • ethiofencarb
  • formetanate
  • methiocarb
  • methomyl
  • oxamyl
  • phenmedipham
  • pinmicarb
  • pirimicarb
  • propamocarb
  • propham
  • propoxur

[edit] Natural Compounds (Supplements)

• Huperzine A

[edit] Effects

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.

[edit] See also

• Antiemetic drugs
• Antispasmodic drugs
• Cholinergic nerves
• Cholinomimetic drugs
• Hallucinogenic drugs
• Pesticide poisoning
• Phenothiazine derivatives

[edit] References

1. ↑ ^{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

[edit] External links

• MeSH Acetylcholinesterase+inhibitors

v·d·e Pharmacology: enzyme inhibition
Class	Competitive inhibition - Uncompetitive inhibition - Non-competitive inhibition - Suicide inhibition - Mixed inhibition
Substrate	Acetylcholinesterase inhibitors - Aromatase inhibitors - Carbonic anhydrase inhibitors - Integrase inhibitor - Kinase inhibitors - Lipoxygenase inhibitor - Monoamine oxidase inhibitors - Reverse transcriptase inhibitors - Phosphodiesterase inhibitors - Protease inhibitors (ACE inhibitor, Trypsin inhibitor)

v·d·e Anticholinesterases (N06DA, N07AA)
Carbamates	Ambenonium - Demecarium - Stigmine (Neostigmine, Physostigmine, Pyridostigmine, Rivastigmine)
Other	Galantamine - Metrifonate - Donepezil - Tacrine - Edrophonium

v·d·e Psychoanaleptics: anti-dementia drugs (N06D)
Anticholinesterases	Tacrine - Donepezil - Rivastigmine - Galantamine
Other	NMDA receptor antagonist (Memantine) - Ginkgo biloba

v·d·e Parasympathomimetics (N07A)
Anticholinesterases	Stigmine (Neostigmine, Pyridostigmine, Distigmine) - Ambenonium
Choline esters	Carbachol - Bethanechol
Other parasympathomimetics	Pilocarpine - Choline alfoscerate

This page uses content from the English-language version of Wikipedia. The original article was at Anticholinergic. The list of authors can be seen in the page history. As with Psychology Wiki, the text of Wikipedia is available under the GNU Free Documentation License.