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Related Concept Videos

Drugs Acting on Autonomic Ganglia: Stimulants01:23

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...
CNS Depressants: Alcohol and Nicotine01:27

CNS Depressants: Alcohol and Nicotine

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...
Cholinergic Receptors: Nicotinic01:15

Cholinergic Receptors: Nicotinic

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...
Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
Drugs Acting on Autonomic Ganglia: Blockers01:28

Drugs Acting on Autonomic Ganglia: Blockers

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:
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

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

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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Related Experiment Video

Updated: Jul 17, 2026

Spectral Confocal Imaging of Fluorescently tagged Nicotinic Receptors in Knock-in Mice with Chronic Nicotine Administration
08:47

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.

K Cahill1, L F Stead, T Lancaster

  • 1Department of Primary Health Care, Old Road Campus, University of Oxford, Oxford, UK, OX3 7LF. kate.cahill@dphpc.ox.ac.uk

The Cochrane Database of Systematic Reviews
|January 27, 2007
PubMed
Summary

Varenicline, a nicotine receptor partial agonist, significantly increases long-term smoking cessation success rates threefold compared to unassisted attempts. While effective, nausea is a common side effect, and further research is needed for relapse prevention and comparisons with other therapies.

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Local Application of Drugs to Study Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices
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Local Application of Drugs to Study Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices

Published on: October 29, 2012

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Last Updated: Jul 17, 2026

Spectral Confocal Imaging of Fluorescently tagged Nicotinic Receptors in Knock-in Mice with Chronic Nicotine Administration
08:47

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

Published on: February 10, 2012

Local Application of Drugs to Study Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices
10:04

Local Application of Drugs to Study Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices

Published on: October 29, 2012

Area of Science:

  • Pharmacology
  • Addiction Medicine
  • Clinical Trials

Background:

  • Nicotine receptor partial agonists aim to aid smoking cessation by modulating dopamine levels, counteracting withdrawal symptoms, and reducing smoking satisfaction.
  • Varenicline, a partial agonist, was developed from cytisine, a smoking cessation drug used in Eastern Europe.
  • Early varenicline trial reports emerged in 2006, with ongoing research.

Purpose of the Study:

  • To evaluate the efficacy and tolerability of nicotine receptor partial agonists, specifically varenicline and cytisine, for smoking cessation.
  • To compare the effectiveness of these agents against placebo and bupropion.

Main Methods:

  • Systematic search of specialized registers and databases (MEDLINE, EMBASE, PsycINFO, CINAHL) for randomized controlled trials (RCTs).
  • Inclusion criteria: RCTs comparing treatment drugs with placebo or bupropion, with a minimum six-month follow-up.
  • Data extraction included participant details, dosage, outcomes, and randomization methods; primary outcome was continuous smoking abstinence at six months, with meta-analysis using a fixed-effect model.

Main Results:

  • Five varenicline trials (4924 participants) and one cytisine trial were included.
  • Varenicline demonstrated a pooled odds ratio (OR) of 3.22 (95% CI 2.43-4.27) for 12-month abstinence versus placebo and 1.66 (95% CI 1.28-2.16) versus bupropion.
  • Nausea was the primary adverse effect of varenicline, generally mild to moderate. Cytisine showed a two-year abstinence OR of 1.77 (95% CI 1.30-2.40) versus placebo.

Conclusions:

  • Varenicline approximately triples the odds of successful long-term smoking cessation compared to unassisted attempts and shows greater efficacy than bupropion in reported trials.
  • Nausea is the main side effect of varenicline, typically mild and transient.
  • Evidence for cytisine's efficacy is inconclusive, and further independent trials are needed for varenicline, particularly for relapse prevention and direct comparisons with nicotine replacement therapy.