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Indirect-Acting Cholinergic Agonists: Pharmacological Actions

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...

Cholinergic Antagonists: Therapeutic Uses

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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: Pharmacological Actions

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...

Direct-Acting Cholinergic Agonists: Therapeutic Uses

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.

Cholinergic Antagonists: Pharmacokinetics

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 Actions

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...

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Updated: Jul 11, 2026

Acetylcholine Re-Challenge After Intracoronary Nitroglycerine Administration

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Published on: April 4, 2022

Central anticholinergic syndrome: a case report.

Daniel D Moos¹

¹Kearney Anesthesia Associates PC, Kearney, NE, USA. moosd@charter.net

Journal of Perianesthesia Nursing : Official Journal of the American Society of Perianesthesia Nurses

|September 29, 2007

Summary

Postoperative central anticholinergic syndrome (CAS) is a reversible condition caused by medications blocking brain receptors. Early recognition and diagnosis are crucial for effective treatment and patient recovery.

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Area of Science:

Pharmacology
Neurology
Critical Care Medicine

Background:

Central anticholinergic syndrome (CAS) arises from medications crossing the blood-brain barrier.
These drugs block muscarinic cholinergic receptors, leading to diverse neurological symptoms.

Observation:

CAS presents with a broad spectrum of symptoms, from coma to agitation.
The syndrome can be underdiagnosed due to variable presentation and limited awareness.

Findings:

This case report highlights CAS in a young adult female patient.
Differential diagnosis for neurological changes must include CAS after excluding other causes.

Implications:

Increased awareness of CAS is vital for timely diagnosis and management.
Understanding CAS pathophysiology aids in preventing and treating postoperative neurological complications.