Acetylcholinesterase inhibitor: Difference between revisions

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** To treat [[myasthenia gravis]]. In myasthenia gravis, they are used to increase neuromuscular transmission.
** To treat [[myasthenia gravis]]. In myasthenia gravis, they are used to increase neuromuscular transmission.
** To treat [[glaucoma]]
** To treat [[glaucoma]]
** To treat [[Alzheimer's disease]]
** To treat [[Lewy Body Dementia]]
** To treat [[Postural Tachycardia Syndrome]]
** To treat [[Postural Tachycardia Syndrome]]
** As an [[antidote]] to [[anticholinergic]] poisoning
** As an [[antidote]] to [[anticholinergic]] poisoning
Line 23: Line 21:
** To treat [[Apathy]]
** To treat [[Apathy]]
** To increase chances of [[lucid dreaming]] (by prolonging [[REM sleep]])<ref>{{cite book |last= Yuschak|first= Thomas|title= Advanced Lucid Dreaming: The Power of Supplements|year= 2006|publisher= Lulu|isbn= 1430305428}}</ref>
** To increase chances of [[lucid dreaming]] (by prolonging [[REM sleep]])<ref>{{cite book |last= Yuschak|first= Thomas|title= Advanced Lucid Dreaming: The Power of Supplements|year= 2006|publisher= Lulu|isbn= 1430305428}}</ref>
** To treat [[Alzheimer's disease]], [[Lewy Body Dementia]] and [[Parkinson's disease]]. In these [[Neurodegenerative disorder|neurodegenerative conditions]] AChEIs are primarily used to treat the cognitive (memory and learning deficits mostly) symptoms of [[dementia]]. These symptoms are attenuate due to the role of acetylcholine in cognition in the [[Central Nervous System|CNS]]. There is some evidence to suggest that AChEIs may attenuate psychotic symptoms (especially visual hallucinations) in Parkinson's disease.<ref>{{cite isbn|9780470979693|page=520}}</ref>
** To treat cognitive impairments in patients with [[schizophrenia]]. There is some evidence to suggest efficacy in treating positive, negative and affective symptoms.<ref>{{cite journal|title=Acetylcholinesterase inhibitors for schizophrenia|journal=The Cochrane Database of Systematic Reviews|volume=1|pages=CD007967|date=January 2012|doi=10.1002/14651858.CD007967.pub2|pmid=22258978|author=Singh, J; Kour, K; Jayaram, MB|url=http://onlinelibrary.wiley.com/doi/10.1002/14651858.CD001257.pub2/pdf}}</ref><ref>{{cite journal|title=Adjunctive pharmacotherapy for cognitive deficits in schizophrenia: meta-analytical investigation of efficacy|journal=The British Journal of Psychiatry|volume=203|issue=3|pages=172-178|doi=10.1192/bjp.bp.111.107359|pmid=23999481|date=September 2013|author=Choi, KH; Wykes, T; Kurtz, MM}}</ref><ref>{{cite journal|title=Cholinesterase Inhibitors as Adjunctive Therapy in Patients with Schizophrenia and Schizoaffective Disorder A Review and Meta-Analysis of the Literature|journal = CNS Drugs|date=April 2010|volume=24|issue=4|pages=303-317|doi=10.2165/11530260-000000000-00000|pmid=20297855|author=Ribeiz, SR; Bassitt, DP; Arrais, JA; Avila, R; Steffens, DC; Bottino, CM}}</ref>


==Effects==
==Effects==

Revision as of 10:59, 25 October 2013

Not to be confused with ACE inhibitor.
Acetylcholine
Acetylcholinesterase
Acetylcholinesterase inhibition

An acetylcholinesterase inhibitor (often abbreviated AChEI) or anti-cholinesterase is a chemical that inhibits the acetylcholinesterase enzyme from breaking down acetylcholine, thereby increasing both the level and duration of action of the neurotransmitter acetylcholine. Reversible, quasi-irreversible (or pseudirreversible in some sources) and irreversible inhibitors exist.[1]

Uses

Acetylcholinesterase inhibitors:[2]

Effects

Potential side effects of acetylcholinesterase inhibitors[8][9]
mild – usually goes away potentially serious

Some major effects of cholinesterase inhibitors:

Administration of reversible cholinoesterase inhibitors is contraindicated with those that have urinary retention due to obstruction.

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. Many other types drug treatments may require a titration or stepping up phase. This strategy is used to build tolerance to adverse events or to reach a desired clinical effect. [10]

Examples

Reversible inhibitor

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

Comparison table

Comparison of reversible acetylcholinesterase inhibitors
Inhibitor Duration Main site of action Clinical use Adverse effects
Edrophonium short (10 min.)[16] neuromuscular junction[16] diagnosis of myasthenia gravis[16]
Neostigmine medium (1–2 hrs.)[16] neuromuscular junction[16] visceral[16]
Physostigmine medium (0.5-5 hrs.)[16] postganglionic parasympathetic[16] treat glaucoma (eye drops)[16]
Pyridostigmine medium (2–3 hrs.)[16] neuromuscular junction[16]
Dyflos long[16] postganglionic parasympathetic[16] historically to treat glaucoma (eye drops)[16] toxic[16]
Ecothiopate (irreversible) long[16] postganglionic parasympathetic[16] treat glaucoma (eye drops)[16] systemic effects[16]
Parathion (irreversible) long[16] none[16] toxic[16]

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: Template:MultiCol

| class="col-break " |

Template:EndMultiCol

Natural Compounds

See also

References

  1. ^ Pohanka, M (2012). "Acetylcholinesterase inhibitors; a patent review (2008–present)". Expert Opinion on Therapeutic Patents. 22 (8): 871–886. doi:10.1517/13543776.2012.701620. PMID 22768972.
  2. ^ Colovic, MB; Krstic, Danijela Z.; Lazarevic-Pasti, Tamara D.; Bondzic, Aleksandra M.; Vasic, Vesna M. (2013). "Acetylcholinesterase Inhibitors: Pharmacology and Toxicology". Current Neuropharmacology. 11 (3): 315–335. doi:10.2174/1570159X11311030006.
  3. ^ Yuschak, Thomas (2006). Advanced Lucid Dreaming: The Power of Supplements. Lulu. ISBN 1430305428.
  4. ^ Template:Cite isbn
  5. ^ Singh, J; Kour, K; Jayaram, MB (January 2012). "Acetylcholinesterase inhibitors for schizophrenia". The Cochrane Database of Systematic Reviews. 1: CD007967. doi:10.1002/14651858.CD007967.pub2. PMID 22258978.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  6. ^ Choi, KH; Wykes, T; Kurtz, MM (September 2013). "Adjunctive pharmacotherapy for cognitive deficits in schizophrenia: meta-analytical investigation of efficacy". The British Journal of Psychiatry. 203 (3): 172–178. doi:10.1192/bjp.bp.111.107359. PMID 23999481.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  7. ^ Ribeiz, SR; Bassitt, DP; Arrais, JA; Avila, R; Steffens, DC; Bottino, CM (April 2010). "Cholinesterase Inhibitors as Adjunctive Therapy in Patients with Schizophrenia and Schizoaffective Disorder A Review and Meta-Analysis of the Literature". CNS Drugs. 24 (4): 303–317. doi:10.2165/11530260-000000000-00000. PMID 20297855.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  8. ^ Consumer Reports; Drug Effectiveness Review Project (May 2012). "Evaluating Prescription Drugs Used to Treat: Alzheimer's Disease Comparing Effectiveness, Safety, and Price" (Document). Consumer Reports. p. 2. {{cite document}}: Unknown parameter |accessdate= ignored (help); Unknown parameter |url= ignored (help); Unknown parameter |work= ignored (help)CS1 maint: postscript (link), which claims Alzheimer’s Association guidance as a source
  9. ^ Template:Cite PMID
  10. ^ Inglis, F (2002). "The tolerability and safety of cholinesterase inhibitors in the treatment of dementia". International journal of clinical practice. Supplement (127): 45–63. PMID 12139367.
  11. ^ Eubanks LM, Rogers CJ, Beuscher AE; et al. (2006). "A molecular link between the active component of marijuana and Alzheimer's disease pathology". Mol. Pharm. 3 (6): 773–7. doi:10.1021/mp060066m. PMC 2562334. PMID 17140265. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  12. ^ Karadsheh, N; Kussie, P; Linthicum, DS (1991). "Inhibition of acetylcholinesterase by caffeine, anabasine, methyl pyrrolidine and their derivatives". Toxicology letters. 55 (3): 335–42. doi:10.1016/0378-4274(91)90015-X. PMID 2003276.
  13. ^ Bauer, Brent A. Alzheimer's disease. mayoclinic.com
  14. ^ Wang, BS; Wang, H; Wei, ZH; Song, YY; Zhang, L; Chen, HZ (2009). "Efficacy and safety of natural acetylcholinesterase inhibitor huperzine A in the treatment of Alzheimer's disease: an updated meta-analysis". Journal of neural transmission (Vienna, Austria : 1996). 116 (4): 457–65. doi:10.1007/s00702-009-0189-x. PMID 19221692.
  15. ^ Rhee IK, I (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. doi:10.1248/bpb.27.1804. PMID 15516727. {{cite journal}}: Unknown parameter |coauthors= ignored (|author= suggested) (help)
  16. ^ a b c d e f g h i j k l m n o p q r s t u v w x y Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 156

External links

Template:Nootropics

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