Cholinesterase Inhibitor

Aka: Cholinesterase Inhibitor, Anticholinesterase, Acetylcholinesterase Inhibitor

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II. Indications

  1. Alzheimer's Disease
    1. Increased Cholinergic Activity by Anticholinesterases crossing the blood brain barrier may reduce Dementia related symptoms
    2. Central Cholinesterase Inhibitor examples include Aricept (Donepezil), Rivastigmine (Exelon), Galantamine (Reminyl)
  2. Glaucoma
    1. Increased Cholinergic Activity the iris sphincter Muscle (Miosis)
    2. Pupil Constriction pulls the iris away from canal of schlemm, increasing Aqueous Humor outflow (decreases Intraocular Pressure)
  3. Myasthenia Gravis
    1. Peripheral Anticholinesterases (e.g. neostigmine) prolong Acetylcholine activity at the Neuromuscular Junction
    2. Overcomes the myasthenia autoantibody binding of Neuromuscular JunctionNicotinic Receptors

III. Mechanism

  1. Acetylcholine
    1. Neurotransmitter for autonomic preganglionic Neuron Synapses (CNS to autonomic Ganglion)
      1. Acetylcholine mediates both preganglionic sympathetic and Parasympathetic Systems
    2. Acetylcholine is Neurotransmitter for parasympathetic postganglionic Neurons (autonomic Ganglion to target organ)
      1. Acts at muscarinic and nictonic Acetylcholine receptors
    3. Acetylcholine is the Neurotransmitter at the Neuromuscular Junction
      1. Muscle Contraction is triggered by release of Acetylcholine into the synaptic cleft
  2. Acetylcholinesterase
    1. Acetylcholinesterase cleaves and deactivates Acetylcholine at the synaptic cleft, leading to a short AcetylcholineHalf-Life
  3. Cholinesterase Inhibitor (Anticholinesterase)
    1. Inhibit Acetylcholinesterase activity, thereby resulting in prolonged Acetylcholine activity within the Synapse
  4. Images
    1. parasympatheticNervousSystem.jpg
    2. autonomicSynapse.png

IV. Types

  1. Carbamyl Ester Inhibitors
    1. Inhibition of Acetylcholinesterase via competitively binding the Acetylcholine site
    2. On cleaving the Carbamyl Ester link, Acetylcholinesterase is carbamylated
    3. Acetylcholinesterase is deactivated for minutes to hours until it is reactivated by decarbamylation
    4. Examples include agents used in Dementia, Myasthenia Gravis and Glaucoma
  2. Organophosphorus Inhibitors (Organophosphates)
    1. High affinity binding to the Acetylcholine site renders Acetylcholinesterase permanently inactivated
    2. Acetylcholinesterase must be regenerated over days to weeks to Restore activity at the Synapse
    3. Examples include OrganophosphatePesticides and Nerve Agents

V. Medications: Central Nervous System Agents

  1. Central Cholinesterase Inhibitor for Dementia Management
    1. Aricept (Donepezil)
    2. Rivastigmine (Exelon)
    3. Galantamine (Reminyl)
  2. Physostigmine
    1. Carbamyl Ester Inhibitor administered IM/IV for reversal of AnticholinergicOverdose

VI. Medications: Peripheral Nervous System Agents (Myasthenia Gravis)

  1. Neostigmine (Prostigmine)
  2. Pyridostigmine (Mestinon)
  3. Ambenonium (Mytelase)
    1. Prolonged activity

VII. Medications: Ocular Topical Agents (Glaucoma)

  1. See Intraocular Parasympathomimetic
  2. Demacarium (Humorsol)
  3. Echothiophate (Phosphate Iodide)

VIII. References

  1. Olson (2020) Clinical Pharm, Medmaster, Miami, p. 26-7

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Related Studies

Ontology: Acetylcholinesterase Inhibitors (C0001046)

Definition (NCI) Any substance that inhibits acetylcholinesterase (AchE), an enzyme that breaks down acetylcholine (Ach) in the synaptic cleft. Inhibition of acetylcholinesterase results in an increase in the level and duration of action of acetylcholine.
Concepts Pharmacologic Substance (T121)
MSH D002800
English Inhibitors, Acetylcholinesterase, Acetylcholinesterase Inhibitor, ACETYLCHOLINESTERASE INHIB, Acetylcholine Hydrolase Inhibitor, AcCholE Inhibitor, Acetylcholinesterase Inhibitors, acetylcholinesterase inhibitor, acetylcholinesterase inhibitors
Portuguese Inibidores da Acetilcolinesterase
Spanish Inhibidores del Acetilcolinesterasa
French Inhibiteurs de l'acétylcholinesterase
German Acetylcholinesteraseinhibitoren
Italian Inibitori della acetilcolinesterasi
Czech inhibitory acetylcholinesteráz
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Cholinesterase Inhibitors (C0008425)

Definition (MSH) Drugs that inhibit cholinesterases. The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract and urinary bladder, the eye, and skeletal muscles; they are also used for their effects on the heart and the central nervous system.
Definition (CSP) any substance or agent which suppresses, prevents or opposes the action of cholinesterase resulting in the potentiation of the action of endogenously released acetylcholine at cholinergic synapses; cholinesterase inhibition is associated with a variety of acute symptoms such as nausea, vomiting, blurred vision, stomach cramps, and rapid heart rate.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D002800
SnomedCT 52761007, 372765004
English Agents, Anticholinesterase, Anticholinesterase Agents, Cholinesterase Inhibitors, Inhibitors, Cholinesterase, cholinesterase inhibitor, Anti Cholinesterases, Anti-Cholinesterases, Anticholinesterases, Anticholinesterase Drugs, Drugs, Anticholinesterase, Anticholinest. parasympath., CHOLINESTERASE INHIB, anticholinesterase agents (medication), anticholinesterase agents, Cholinesterase Inhibitor, anticholinesterases, anticholinesterase, anti cholinesterase, cholinesterase inhibitors, Anticholinesterase parasympathomimetics, Cholinesterase inhibitors, Anticholinesterase, Anticholinesterase parasympathomimetic, Cholinesterase inhibitor drug, Anticholinesterase agent (substance), Anticholinesterase agent, Anticholinesterase drug (product), Anticholinesterase drug, Anticholinesterase drug, NOS, Anticholinesterase drug (substance)
French Anticholinestérases, Anti-cholinestérasiques, Anti-cholinestérases, Médicaments anticholinestérasiques, Inhibiteurs de la cholinestérase, Anticholinestérasiques
Swedish Kolinesterashämmare
Finnish Koliiniesteraasin estäjät
Italian Agenti anticolinesterasi, Anticolinesterasi, Farmaci anticolinesterasi, Inibitori della colinesterasi
Russian ANTIKHOLINESTERAZNYE AGENTY, ATSETILKHOLINESTERAZY INGIBITORY, KHOLINESTERAZY INGIBITORY, АНТИХОЛИНЭСТЕРАЗНЫЕ АГЕНТЫ, АЦЕТИЛХОЛИНЭСТЕРАЗЫ ИНГИБИТОРЫ, ХОЛИНЭСТЕРАЗЫ ИНГИБИТОРЫ
Japanese 抗コリンエステラーゼ物質, コリンエステラーゼ阻害薬, アセチルコリンエステラーゼ阻害剤, コリンエステラーゼ阻害剤
Croatian KOLINESTERAZIJSKI INHIBITORI
Polish Inhibitory cholinoesterazy
Norwegian Kolinesterasehemmere
Czech cholinesterasa - inhibitory, inhibitory cholinesteráz
Spanish agente anticolinesterasa (sustancia), agente anticolinesterasa, droga anticolinesterasa (producto), droga anticolinesterasa (sustancia), droga anticolinesterasa, droga inhibidora de la colinesterasa, Agentes Anticolinesterasa, Inhibidores de la Colinesterasa
German Anticholinesterasemittel, Cholinesteraseinhibitoren
Portuguese Agentes Anticolinesterase, Inibidores da Colinesterase
Derived from the NIH UMLS (Unified Medical Language System)

Related Topics in Pharmacology

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