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Related Concept Videos

Antiasthma Drugs: Muscarinic Receptor Antagonists01:20

Antiasthma Drugs: Muscarinic Receptor Antagonists

Muscarinic receptor antagonists, also known as antimuscarinic agents, are a class of bronchodilators used to treat asthma, although they are more commonly used to treat COPD. They work by inhibiting the action of acetylcholine (ACh), a neurotransmitter, on muscarinic receptors found in the airways.
Antimuscarinic agents compete with ACh for the same binding site on the muscarinic receptors. By binding to these receptors, they inhibit the downstream effects of ACh and block the parasympathetic...
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...
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...
Cholinergic Antagonists: Pharmacokinetics01:24

Cholinergic Antagonists: Pharmacokinetics

Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations,  while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and the conjunctiva.
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: Chemistry and Structure-Activity Relationship01:29

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship

Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic antagonists are called...

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In vitro Measurements of Tracheal Constriction Using Mice
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In vitro Measurements of Tracheal Constriction Using Mice

Published on: June 25, 2012

Muscarinic receptor antagonists: effects on pulmonary function.

Kalmia S Buels1, Allison D Fryer

  • 1Oregon Health and Science University, 3181 SW Sam Jackson Park Road, UHN67, Portland, OR 97239, USA. buelsk@ohsu.edu

Handbook of Experimental Pharmacology
|January 7, 2012
PubMed
Summary

Muscarinic receptors regulate lung functions like mucus secretion. In COPD and asthma, targeting these receptors with antagonists offers therapeutic potential for improving airflow.

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Area of Science:

  • Pulmonary Medicine
  • Pharmacology

Background:

  • Muscarinic receptors are crucial for regulating airway smooth muscle tone, mucus secretion, vasodilation, and inflammation in healthy lungs.
  • Cholinergic mechanisms are implicated in the pathophysiology of chronic obstructive pulmonary disease (COPD) and asthma, exacerbating bronchoconstriction and mucus production.

Purpose of the Study:

  • To review the sources of acetylcholine in the lung.
  • To examine the expression and function of M₁, M₂, and M₃ muscarinic receptor subtypes in lung physiology.
  • To discuss the role of parasympathetic nerves in asthma and the therapeutic applications of muscarinic antagonists in COPD and asthma.

Main Methods:

  • Literature review of neuronal and nonneuronal acetylcholine sources.
  • Analysis of muscarinic receptor subtype expression and function.
  • Evaluation of clinical evidence regarding parasympathetic nerve involvement in asthma.
  • Assessment of current and potential use of muscarinic receptor antagonists.

Main Results:

  • Acetylcholine is produced by both neuronal and nonneuronal sources in the lung.
  • M₁, M₂, and M₃ muscarinic receptor subtypes play distinct roles in lung physiology.
  • Evidence for the role of parasympathetic nerves in asthma is debated.
  • Muscarinic receptor antagonists are established treatments for COPD and show therapeutic potential for asthma.

Conclusions:

  • Understanding muscarinic receptor pathways is key to managing airway diseases.
  • Muscarinic antagonists represent a significant therapeutic strategy for COPD and asthma.
  • Further research may elucidate the precise role of parasympathetic innervation in asthma pathogenesis.