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Related Concept Videos

Drugs Acting on Autonomic Ganglia: Stimulants01:23

Drugs Acting on Autonomic Ganglia: Stimulants

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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...
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Cholinergic Receptors: Nicotinic01:15

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.
There are two types of nicotinic receptors: neuromuscular (NM/NM/N1) and neuronal (NN/NN/N2). The two families differ based on their location and selectivity to...
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Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

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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.
The direct-acting...
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Drugs Acting on Autonomic Ganglia: Blockers01:28

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 Antagonists: Chemistry and Structure-Activity Relationship01:29

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship

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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...
3.0K
CNS Depressants: Alcohol and Nicotine01:27

CNS Depressants: Alcohol and Nicotine

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Ethanol, a clear colorless alcohol, has been consumed by humans for millennia, but its effects on the body are far from benign. At lower doses, it induces decreased inhibitions and loquaciousness, leading to its social appeal. However, it can cause severe consequences at higher doses, such as coma and respiratory depression, due to its zero-order elimination kinetics. Chronic ethanol abuse wreaks havoc on multiple organ systems, particularly the CNS and the liver. Abrupt cessation of ethanol...
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Related Experiment Video

Updated: Mar 21, 2026

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

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Nicotine receptor partial agonists for smoking cessation.

Kate Cahill1, Nicola Lindson-Hawley, Kyla H Thomas

  • 1Nuffield Department of Primary Care Health Sciences, University of Oxford, Radcliffe Observatory Quarter, Woodstock Road, Oxford, UK, OX2 6GG.

The Cochrane Database of Systematic Reviews
|May 10, 2016
PubMed
Summary

Nicotine receptor partial agonists like varenicline and cytisine significantly increase smoking cessation success rates. Varenicline is more effective than bupropion or nicotine replacement therapy, with nausea being the most common side effect.

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Local Application of Drugs to Study Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices
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Probing Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices via Laser Flash Photolysis of Photoactivatable Nicotine
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Spectral Confocal Imaging of Fluorescently tagged Nicotinic Receptors in Knock-in Mice with Chronic Nicotine Administration
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Local Application of Drugs to Study Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices
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Probing Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices via Laser Flash Photolysis of Photoactivatable Nicotine
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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.
  • These medications act as both agonists and antagonists to nicotine receptors.

Purpose of the Study:

  • To review the efficacy of nicotine receptor partial agonists, specifically varenicline and cytisine, for smoking cessation.
  • Evaluate their effectiveness compared to placebo, bupropion, and nicotine replacement therapy (NRT).

Main Methods:

  • Conducted a systematic review of randomized controlled trials (RCTs) from the Cochrane Tobacco Addiction Group's register.
  • Included trials with a minimum six-month follow-up, comparing drugs against placebo, bupropion, or NRT.
  • Extracted data on participant characteristics, treatment details, and smoking abstinence rates, using meta-analysis for pooled risk ratios.

Main Results:

  • Cytisine showed a significant increase in smoking cessation compared to placebo (RR 3.98) and was effective compared to NRT (RR 1.43).
  • Varenicline (standard dose) demonstrated a 2- to 3-fold increase in sustained smoking cessation versus placebo (RR 2.24), outperforming bupropion (RR 1.39) and NRT (RR 1.25).
  • Nausea was the most common adverse effect of varenicline, usually mild to moderate. A slight increase in serious adverse events (SAEs) was observed (RR 1.25), though causality is often unclear. Concerns regarding neuropsychiatric events have not been confirmed by recent large trials.

Conclusions:

  • Cytisine improves quit rates, though absolute success rates are modest.
  • Varenicline significantly enhances long-term smoking cessation, with lower doses also effective and potentially reducing adverse events.
  • Varenicline demonstrated superior efficacy over bupropion and NRT, with nausea as the primary side effect. Concerns about serious neuropsychiatric events are not supported by current evidence.