Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Indirect-Acting Cholinergic Agonists: Pharmacological Actions01:30

Indirect-Acting Cholinergic Agonists: Pharmacological Actions

Indirect-acting cholinergic agonists, also known as anticholinesterases, exert their pharmacological effects by enhancing cholinergic transmission in various body parts, including the neuromuscular junction, autonomic cholinergic synapses, and the brain.
At the neuromuscular junction, these agents work by inhibiting the breakdown of acetylcholine, allowing it to remain bound to the receptor and bind to nearby receptors. This process leads to repetitive firing of the endplate, causing muscle...
Indirect-Acting Cholinergic Agonists: Pharmacokinetics01:22

Indirect-Acting Cholinergic Agonists: Pharmacokinetics

Indirect-acting cholinergic agonists, or anticholinesterases, enhance the body's cholinergic activity by inhibiting acetylcholine's breakdown. They are categorized as reversible or irreversible agents based on their mechanism of action. They are further classified into short-acting, intermediate-acting, and long-acting agents based on their duration of action.
Reversible agents containing quaternary amines, such as neostigmine and edrophonium, are not easily absorbed orally because they are...
Anticholinesterase Agents: Poisoning and Treatment01:26

Anticholinesterase Agents: Poisoning and Treatment

Anticholinesterases, also known as cholinesterase inhibitors, work by blocking the breakdown of acetylcholine, leading to its accumulation in the synaptic cleft. This accumulation indirectly enhances both muscarinic and nicotinic actions. These agents are classified as reversible or irreversible based on their mechanism of action.     
Irreversible agents form a strong bond with the cholinesterase enzyme, making it inactive. The breakdown of the phosphorylated enzyme is slower than the...
Indirect-Acting Cholinergic Agonists: Mechanism of Action01:18

Indirect-Acting Cholinergic Agonists: Mechanism of Action

Indirect-acting cholinergic agonists work by interacting with an enzyme called acetylcholinesterase (AChE) in the synaptic cleft. They can be reversible or irreversible inhibitors and have different effects on the enzyme.
Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex, leading to...
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Cholinergic Antagonists: Pharmacological Actions01:28

Cholinergic Antagonists: Pharmacological Actions

Antimuscarinic drugs block muscarinic receptors in multiple systems, including the gut, eye, smooth muscles, respiratory tract, cardiovascular, and central nervous systems. They produce similar effects with varying selectivity depending on the specific agent and tissue. Here are the key pharmacological actions of antimuscarinics:
Gastrointestinal Effects: Antimuscarinics reduce gut contractions, increase gastric emptying, and slow intestinal transit. They partly inhibit gastric acid secretion...

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

[A Case Report of Cecal Cancer with Port Site Recurrence and Right Inguinal Lymph Node Metastasis after Laparoscopic Ileo‒Cecal Resection].

Gan to kagaku ryoho. Cancer & chemotherapy·2026
Same author

[Tuberculous Peritonitis Requiring Differentiation from Peritoneal Dissemination in a Case with Transverse Colon Cancer].

Gan to kagaku ryoho. Cancer & chemotherapy·2026
Same author

Frailty at 1 Month before ICU Admission Poses a Hospital Mortality Risk in Cancer Survivors whose Condition Has Deteriorated due to Medical Factors.

Acta medica Okayama·2025
Same author

Clinical characteristics, management strategies, and outcomes in patients with preoperative venous thromboembolism who underwent surgery: survey data from 2020 to 2022 by the Japanese Society of Anesthesiologists.

Journal of anesthesia·2025
Same author

Usefulness of Frameless Neuronavigation-Guided Stereotactic Biopsy for Brain Lesions Under Local Anesthesia: Surgical Outcomes and Feasibility for Molecular Diagnosis-Case Series.

Neurosurgery practice·2025
Same author

Clinical Experience of Using Remimazolam Instead of Volatile Anesthesia for Near-Infrared Photoimmunotherapy.

Cureus·2025

Related Experiment Video

Updated: May 13, 2026

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development
07:02

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development

Published on: February 11, 2019

[Anticholinesterases; peripheral and central effects].

Tetsufumi Sato1, Hideki Nakatsuka

  • 1Department of Anesthesiology and Intensive Care Medicine, National Cancer Center Tokyo 104-0045.

Masui. the Japanese Journal of Anesthesiology
|February 26, 2013
PubMed
Summary

Cholinesterase inhibitors, like donepezil, are used to treat Alzheimer's disease by increasing acetylcholine levels. These drugs also show potential in reversing opioid-induced respiratory depression, offering a dual therapeutic benefit.

More Related Videos

Subcutaneous Administration of Muscarinic Antagonists and Triple-Immunostaining of the Levator Auris Longus Muscle in Mice
07:09

Subcutaneous Administration of Muscarinic Antagonists and Triple-Immunostaining of the Levator Auris Longus Muscle in Mice

Published on: September 8, 2011

Functional Evaluation of Biological Neurotoxins in Networked Cultures of Stem Cell-derived Central Nervous System Neurons
15:05

Functional Evaluation of Biological Neurotoxins in Networked Cultures of Stem Cell-derived Central Nervous System Neurons

Published on: February 5, 2015

Related Experiment Videos

Last Updated: May 13, 2026

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development
07:02

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development

Published on: February 11, 2019

Subcutaneous Administration of Muscarinic Antagonists and Triple-Immunostaining of the Levator Auris Longus Muscle in Mice
07:09

Subcutaneous Administration of Muscarinic Antagonists and Triple-Immunostaining of the Levator Auris Longus Muscle in Mice

Published on: September 8, 2011

Functional Evaluation of Biological Neurotoxins in Networked Cultures of Stem Cell-derived Central Nervous System Neurons
15:05

Functional Evaluation of Biological Neurotoxins in Networked Cultures of Stem Cell-derived Central Nervous System Neurons

Published on: February 5, 2015

Area of Science:

  • Pharmacology
  • Neuroscience
  • Anesthesiology

Background:

  • Anticholinesterase drugs, such as neostigmine, were historically used for reversing neuromuscular block after surgery.
  • Neostigmine functions by increasing acetylcholine (ACh) at the neuromuscular junction but is ineffective for profound blocks and causes undesirable autonomic responses.
  • Donepezil, a specific anticholinesterase, targets central acetylcholinesterase, increasing brain ACh levels.

Purpose of the Study:

  • To explore the role of cholinesterase inhibitors in managing conditions beyond surgical reversal.
  • To highlight the application of donepezil and similar drugs in treating Alzheimer's disease.
  • To investigate the potential of donepezil in reversing opioid-induced respiratory depression.

Main Methods:

  • Review of the pharmacological actions of anticholinesterase agents, including neostigmine and donepezil.
  • Examination of the mechanism of action for cholinesterase inhibitors in Alzheimer's disease.
  • Analysis of donepezil's effect on opioid-induced respiratory depression.

Main Results:

  • Cholinesterase inhibitors increase acetylcholine levels by inhibiting acetylcholinesterase, benefiting cognitive function in Alzheimer's disease.
  • Donepezil demonstrates efficacy in treating Alzheimer's symptoms by enhancing cholinergic neurotransmission.
  • Donepezil has shown the capability to reverse opioid-induced respiratory depression.

Conclusions:

  • Cholinesterase inhibitors represent a key therapeutic strategy for Alzheimer's disease.
  • Donepezil offers a dual therapeutic profile, addressing both Alzheimer's symptoms and opioid-induced respiratory depression.
  • Further research into the broader applications of cholinesterase inhibitors is warranted.