III. Mechanism

  1. Decreased cerebral Cholinergic activity in Alzheimer Disease, Lewy Body Dementia, Vascular Dementia
  2. Cholinergic inhibitors reversibly bind cholinesterase at Synapse between CNS Neurons
    1. Results in decreased acetylcholine degradation, and hence increased Cholinergic activity

IV. Efficacy

  1. Minimal clinical benefit, despite Statistically Significant improvement in cognitive function in trials
  2. Improve neuropsychiatric scores 7 points
    1. Seven point improvement equals ~1 year of decline
    2. Benefits may persist for 1-2 years
    3. Rogers (1998) Arch Intern Med 158:1021-31 [PubMed]
  3. Meta-analysis shows marginal benefit to risk ratio
    1. Where NNT is Number Needed to Treat
    2. NNT for global improvement: 10
    3. NNT for cognitive improvement: 12
    4. NNT for significant side effects to stop med: 16
    5. Lanctot (2003) CMAJ 169:557-64 [PubMed]

V. Adverse Effects

  1. No hepatotoxicity with newer agents (contrast with Tacrine, Cognex - the initial agent in class)
  2. Cardiovascular effects
    1. Atrioventricular Block
  3. Gastrointestinal effects
    1. Decreased appetite and anorexia
    2. Diarrhea
    3. Nausea or Vomiting
    4. Weight loss
  4. Neurologic effects
    1. Dizziness
    2. Headache

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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

Ontology: Central acetylcholinesterase inhibitor (C0594440)

Concepts Pharmacologic Substance (T121)
SnomedCT 323363000
English Central cholinesterase inhib, Central acetylcholinesterase inhibitor, Central acetylcholinesterase inhibitor (product), Central acetylcholinesterase inhibitor (substance)
Spanish inhibidor central de la acetilcolinesterasa (producto), inhibidor central de la acetilcolinesterasa (sustancia), inhibidor central de la acetilcolinesterasa