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Related Concept Videos

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...
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...
Direct-Acting Cholinergic Agonists: Pharmacological Actions00:59

Direct-Acting Cholinergic Agonists: Pharmacological Actions

Direct-acting cholinergic agonists exert their pharmacological actions by mimicking the effects of acetylcholine on postsynaptic muscarinic receptors to generate parasympathetic responses. These agents elicit a range of physiological responses, including cardiovascular effects. For example, activation of muscarinic receptors induces bradycardia, decreased cardiac output, reduced peripheral resistance, and consequent hypotension. In the eye, stimulation of M3 receptors leads to smooth muscle...
Cholinergic Antagonists: Therapeutic Uses01:26

Cholinergic Antagonists: Therapeutic Uses

Antimuscarinic drugs have various therapeutic applications by inhibiting parasympathetic stimulation in different systems. Here are the key therapeutic uses of antimuscarinics:    
Respiratory Tract: Ipratropium, aclidinium, and tiotropium treat asthma, chronic bronchitis, and chronic obstructive pulmonary disease (COPD). They protect against bronchoconstriction caused by irritants like cigarette smoke, sulfur dioxide, and ozone. They also help reduce nasopharyngeal secretions in common...
Direct-Acting Cholinergic Agonists: Pharmacokinetics01:31

Direct-Acting Cholinergic Agonists: Pharmacokinetics

Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...
Direct-Acting Cholinergic Agonists: Therapeutic Uses01:11

Direct-Acting Cholinergic Agonists: Therapeutic Uses

Direct-acting cholinergic agonists have many therapeutic uses in various medical fields. Choline esters, including acetylcholine, have limited clinical utility due to their non-selectivity and short duration of action. Still, acetylcholine and carbachol are applied topically during ophthalmologic surgery to induce miosis. Pilocarpine, a muscarinic and ganglionic stimulator, effectively treats open-angle glaucoma and alleviates xerostomia and dry mouth caused by radiotherapy or Sjögren syndrome.

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Updated: May 27, 2026

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

Anticholinergics for overactive bladder therapy: central nervous system effects.

Michael Chancellor1, Timothy Boone

  • 1Oakland University William Beaumont School of Medicine, Department of Urology, William Beaumont Hospital, Royal Oak, MI 48073, USA. Michael.chancellor@beaumont.edu

CNS Neuroscience & Therapeutics
|November 11, 2011
PubMed
Summary
This summary is machine-generated.

Anticholinergic drugs for overactive bladder (OAB) can cause central nervous system (CNS) side effects. Hydrophilic drugs like trospium chloride are less likely to cross the blood-brain barrier, reducing CNS risks compared to lipophilic options.

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Bladder Smooth Muscle Strip Contractility as a Method to Evaluate Lower Urinary Tract Pharmacology
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Related Experiment Videos

Last Updated: May 27, 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

Bladder Smooth Muscle Strip Contractility as a Method to Evaluate Lower Urinary Tract Pharmacology
10:26

Bladder Smooth Muscle Strip Contractility as a Method to Evaluate Lower Urinary Tract Pharmacology

Published on: August 18, 2014

Area of Science:

  • Pharmacology
  • Neuroscience
  • Geriatrics

Background:

  • Overactive bladder (OAB) is commonly treated with anticholinergic medications.
  • Muscarinic receptors in the brain are crucial for cognitive functions.
  • Antimuscarinic OAB drugs carry a risk of adverse central nervous system (CNS) effects.

Purpose of the Study:

  • To review the physicochemical and pharmacokinetic properties of OAB antimuscarinics.
  • To assess their propensity to cause adverse CNS effects.
  • To guide the selection of OAB medications with reduced CNS risks.

Main Methods:

  • Literature search of PubMed/MEDLINE for OAB and anticholinergic drugs.
  • Inclusion of preclinical and clinical trials in adults.
  • Focus on US-approved OAB antimuscarinics.

Main Results:

  • Lipophilic tertiary amines (e.g., oxybutynin) more readily cross the blood-brain barrier (BBB) than hydrophilic quaternary amines (e.g., trospium chloride).
  • Trospium chloride has significantly fewer reported adverse CNS effects.
  • Oxybutynin's US product label includes warnings for potential anticholinergic CNS events.

Conclusions:

  • Drug properties influencing BBB penetration are key to CNS side effect profiles.
  • Hydrophilic antimuscarinics like trospium chloride may be preferable for minimizing CNS risks.
  • Careful drug selection is advised, especially in the elderly, to preserve cognitive function and independence.