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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: 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...

Antipsychotic Drugs: Therapeutic Uses and Side Effects

Antipsychotic Drugs: Therapeutic Uses and Side Effects

Antipsychotic drugs primarily block dopamine and serotonin receptors and cholinergic, adrenergic, and histaminergic receptors, thereby reducing hallucinations and delusions in conditions like schizophrenia. However, they can trigger unwanted extrapyramidal effects such as dystonias, Parkinson-like symptoms, and tardive dyskinesia.
Despite these side effects, antipsychotics are used therapeutically for various purposes, including managing schizophrenia, preventing nausea and vomiting, curbing...

Cholinergic Antagonists: Therapeutic Uses

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: 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.

Anticholinesterase Agents: Poisoning and Treatment

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...

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Related Experiment Video

Updated: May 31, 2026

Detrusor Underactivity Model in Rats by Conus Medullaris Transection

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Published on: August 28, 2020

Antipsychotic-induced urinary dysfunction: anticholinergic effect or otherwise?

Sahoo Saddichha¹, Manoj Kumar

¹EMRI, Clinical Research, Hyderabad, Bhubaneswar, 500014, India.

BMJ Case Reports

|June 21, 2011

Summary

This summary is machine-generated.

Antipsychotics can cause urinary issues like incontinence and retention. In a bipolar patient, only aripiprazole effectively treated these urinary difficulties, suggesting unique mechanisms beyond anticholinergic or extrapyramidal effects.

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Published on: August 18, 2014

Area of Science:

Neuroscience
Psychiatry
Pharmacology

Background:

Urinary difficulties, including incontinence (UI) and retention (UR), are recognized side effects of antipsychotic medications.
Existing hypotheses attribute these urinary issues to anticholinergic or extrapyramidal side effects of antipsychotics.

Purpose of the Study:

To investigate the potential mechanisms behind antipsychotic-induced urinary difficulties.
To report a case study where aripiprazole demonstrated efficacy in managing urinary issues associated with antipsychotic use.

Main Methods:

Case report of a male patient with bipolar disorder experiencing urinary difficulties.
Review of antipsychotic medications, including typical and atypical agents.
Observation of treatment response to aripiprazole.

Main Results:

The patient experienced urinary difficulties (incontinence and retention) with various antipsychotics.
Aripiprazole was the only antipsychotic that effectively resolved the patient's urinary symptoms.
This suggests that the mechanisms of adverse urinary effects may differ from current hypotheses.

Conclusions:

Antipsychotic-induced urinary difficulties may involve mechanisms distinct from anticholinergic or extrapyramidal effects.
Aripiprazole may represent a therapeutic option for patients experiencing such urinary adverse events.
Further research is warranted to elucidate the specific neuropharmacological pathways involved.