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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: May 23, 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.

Kate Cahill1, Lindsay F Stead, Tim Lancaster

  • 1Department of Primary Care Health Sciences, University of Oxford, Oxford, UK. kate.cahill@phc.ox.ac.uk.

The Cochrane Database of Systematic Reviews
|April 20, 2012
PubMed
Summary

Nicotine receptor partial agonists like cytisine and varenicline (varenicline) can help individuals quit smoking. Varenicline significantly increases cessation success compared to placebo and bupropion, though nausea is a common side effect.

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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

Related Experiment Videos

Last Updated: May 23, 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 of addiction treatment
  • Clinical trial methodology
  • Public health interventions

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 evaluate the efficacy and tolerability of nicotine receptor partial agonists for smoking cessation.
  • Key drugs assessed include cytisine, dianicline, and varenicline.

Main Methods:

  • Systematic review and meta-analysis of randomized controlled trials.
  • Searched specialized databases for trials comparing drugs with placebo, bupropion, or nicotine patches.
  • Included trials with a minimum six-month follow-up period.

Main Results:

  • Cytisine demonstrated a significant increase in smoking cessation rates compared to placebo (RR 3.98).
  • Varenicline (standard dose) increased long-term smoking cessation by 2-3 times versus placebo (RR 2.27) and was more effective than bupropion (RR 1.52).
  • Nausea was the most common adverse event for varenicline, usually mild to moderate; potential serious psychiatric or cardiovascular events require further investigation.

Conclusions:

  • Cytisine and varenicline are effective smoking cessation aids, with varenicline showing significant benefits over placebo and bupropion.
  • Lower varenicline doses may reduce adverse events while maintaining efficacy.
  • Further research is needed on extended varenicline regimens and potential serious adverse events.