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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 3, 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 Health Care, University of Oxford, Rosemary Rue Building, Old Road Campus, Oxford, UK, OX3 7LF. kate.cahill@dphpc.ox.ac.uk

The Cochrane Database of Systematic Reviews
|July 23, 2008
PubMed
Summary

Varenicline and cytisine are nicotine receptor partial agonists that aid smoking cessation. Varenicline significantly increases quit 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: Jul 3, 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 and Addiction Medicine
  • Clinical Trials and Evidence Synthesis

Background:

  • Nicotine receptor partial agonists, like varenicline and cytisine, aim to reduce withdrawal symptoms and smoking satisfaction.
  • Varenicline, developed from cytisine, is a key pharmaceutical intervention for smoking cessation.
  • Ongoing research continues to explore the efficacy and safety of these agents.

Purpose of the Study:

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

Main Methods:

  • Systematic review of randomized controlled trials (RCTs) including varenicline and cytisine.
  • Searches conducted across multiple databases (Cochrane, MEDLINE, EMBASE, PsycINFO, CINAHL) up to March 2008.
  • Meta-analysis used to calculate pooled risk ratios for continuous abstinence at six months or longer.

Main Results:

  • Varenicline demonstrated a pooled risk ratio (RR) of 2.33 (95% CI 1.95 to 2.80) for continuous abstinence versus placebo.
  • Varenicline showed superior efficacy compared to bupropion (RR 1.52) and NRT (RR 1.31) at one year.
  • Cytisine showed a RR of 1.61 (95% CI 1.24 to 2.08) for smoking cessation versus placebo at two years; varenicline's main side effect was mild to moderate nausea.

Conclusions:

  • Varenicline significantly increases long-term smoking cessation rates compared to placebo and bupropion.
  • Evidence for cytisine's efficacy is promising but currently inconclusive; further independent trials are needed for both agents.
  • Ongoing safety reviews are investigating potential links between varenicline and serious adverse events like depressed mood and suicidal ideation.