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Drugs Acting on Autonomic Ganglia: Stimulants

Drugs Acting on Autonomic Ganglia: Stimulants

Ganglionic stimulants activate NM nicotinic receptors in autonomic ganglia, falling into two categories: nicotine mimetics [e.g., lobeline, dimethylpiperazine, tetramethylammonium] and muscarinic receptor agonists [e.g., muscarine, methacholine]. The first category's action is rapid and blocked by nicotinic receptor antagonists, while the second category's action is delayed and blocked by atropine-like agents. Nicotine, an alkaloid, affects the heart rate by stimulating sympathetic or...

Cholinergic Receptors: Nicotinic

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Nicotinic receptors are ligand-gated ion channels that are activated by acetylcholine and nicotine. Upon activation, they cause a rapid increase in the permeability of cells to K+, Na+, and Ca2+, followed by depolarization and excitation. They are in the autonomic ganglia, skeletal neuromuscular junction, CNS, and adrenal medulla.
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CNS Depressants: Alcohol and Nicotine

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Drug-Receptor Interaction: Agonist

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Drugs Acting on Autonomic Ganglia: Blockers

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Ganglionic blockers inhibit autonomic activity by blocking nicotinic receptors in the autonomic ganglia, suppressing impulse transmission. These blockers lack selectivity between sympathetic and parasympathetic ganglia and are ineffective as neuromuscular junction antagonists. They can be categorized into two groups:

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Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
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Related Experiment Video

Updated: Jun 4, 2026

Spectral Confocal Imaging of Fluorescently tagged Nicotinic Receptors in Knock-in Mice with Chronic Nicotine Administration

Spectral Confocal Imaging of Fluorescently tagged Nicotinic Receptors in Knock-in Mice with Chronic Nicotine Administration

Published on: February 10, 2012

Nicotine receptor partial agonists for smoking cessation.

Kate Cahill¹, Lindsay F Stead, Tim Lancaster

¹Department of Primary Health Care, University of Oxford, Rosemary Rue Building, Old Road Campus, Oxford, UK, OX3 7LF.

The Cochrane Database of Systematic Reviews

|February 18, 2011

Summary

Varenicline, a nicotine receptor partial agonist, significantly increases smoking cessation success rates compared to placebo and bupropion. While generally well-tolerated, nausea is a common side effect, and concerns about serious adverse events remain unsubstantiated.

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Area of Science:

Pharmacology
Addiction Medicine
Clinical Trials

Background:

Nicotine receptor partial agonists aid smoking cessation by managing dopamine levels and reducing smoking satisfaction.
Varenicline, derived from cytisine, is a key partial agonist developed for smoking cessation.
Ongoing research continues to explore the efficacy and safety of varenicline.

Purpose of the Study:

To evaluate the effectiveness and tolerability of nicotine receptor partial agonists, specifically varenicline and cytisine, for smoking cessation.
To compare the efficacy of varenicline against placebo, bupropion, and nicotine replacement therapy (NRT).

Main Methods:

Systematic review and meta-analysis of randomized controlled trials (RCTs) comparing varenicline or cytisine with placebo.
Searched major databases (Cochrane, MEDLINE, EMBASE, PsycINFO, CINAHL) up to September 2010.
Included RCTs with a minimum six-month follow-up, prioritizing biochemically validated abstinence rates.

Main Results:

Varenicline significantly increased continuous abstinence rates (RR 2.31) compared to placebo at six months.
Varenicline demonstrated higher efficacy than bupropion (RR 1.52 at one year) and comparable efficacy to NRT (RR 1.13).
One cytisine trial showed increased cessation rates compared to placebo (RR 1.61 at two years). Nausea was the most frequent adverse event for varenicline.

Conclusions:

Standard-dose varenicline is a highly effective smoking cessation aid, increasing success rates two- to threefold compared to unassisted attempts.
Lower varenicline doses are effective and may reduce adverse events; its efficacy surpasses bupropion.
While varenicline is generally safe, further research is needed to fully understand its long-term safety and efficacy in diverse populations.