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Related Concept Videos

Opioid Analgesics: Synthetic and Semisynthetic Opioids01:15

Opioid Analgesics: Synthetic and Semisynthetic Opioids

Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...
Opioid Receptors: Overview01:22

Opioid Receptors: Overview

Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2, D-Pen5]-enkephalin or DPDPE for...
Opioid Analgesics: Morphine and Other Natural Cogeners01:20

Opioid Analgesics: Morphine and Other Natural Cogeners

Opioids are a class of drugs that mimic endogenous opioid peptides and act on opioid receptors, and help in pain relief. These compounds are classified as natural, synthetic, or semi-synthetic. Natural opioids, like morphine, codeine, and thebaine, are derived from the opium poppy plant (Papaver somniferum or Papaver album) and are termed opiates. Synthetic opioids are artificial, while semi-synthetic opioids combine natural and synthetic compounds. Morphine, a prototypical opioid, possesses a...
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.
Analgesia and Pain Management01:25

Analgesia and Pain Management

Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
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...

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Related Experiment Video

Updated: May 10, 2026

Investigating Drivers of Antireward in Addiction Behavior with Anatomically Specific Single-Cell Gene Expression Methods
09:29

Investigating Drivers of Antireward in Addiction Behavior with Anatomically Specific Single-Cell Gene Expression Methods

Published on: August 4, 2022

Opioid antagonists for smoking cessation.

Sean P David1, Tim Lancaster, Lindsay F Stead

  • 1Center for Education in Family & Community Medicine, Stanford University, Stanford, California, USA. spdavid@stanford.edu.

The Cochrane Database of Systematic Reviews
|June 8, 2013
PubMed
Summary
This summary is machine-generated.

Naltrexone, an opioid antagonist, was evaluated for smoking cessation. This meta-analysis found no significant difference in long-term smoking abstinence when using naltrexone alone or with nicotine replacement therapy (NRT).

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Area of Science:

  • Addiction Medicine
  • Pharmacology
  • Public Health

Background:

  • Nicotine's reinforcing effects are mediated by neurotransmitter release, leading to reported positive effects and relief from negative affect.
  • Opioid antagonists are investigated for their potential to reduce the rewarding effects of smoking.

Purpose of the Study:

  • To assess the effectiveness of opioid antagonists, specifically naloxone and naltrexone, in achieving long-term smoking cessation.
  • To analyze randomized controlled trials (RCTs) comparing opioid antagonists to placebo for smoking cessation outcomes.

Main Methods:

  • Systematic literature search of Cochrane Tobacco Addiction Group Register and MEDLINE for relevant trials up to April 2013.
  • Inclusion of RCTs reporting at least six months of smoking abstinence data; meta-analysis using Mantel-Haenszel fixed-effect model.
  • Extraction of data on study population, drug therapy, outcomes, randomization, and follow-up completeness; verification of abstinence using cotinine or carbon monoxide where available.

Main Results:

  • Eight naltrexone trials (1213 participants) met inclusion criteria for long-term cessation meta-analysis.
  • No significant difference in long-term smoking abstinence was found between naltrexone and placebo (RR 0.97; 95% CI 0.76 to 1.24).
  • Naltrexone as an adjunct to nicotine replacement therapy (NRT) also showed no significant benefit over placebo plus NRT (RR 0.95; 95% CI 0.70 to 1.30).

Conclusions:

  • Naltrexone, alone or with NRT, demonstrated no significant effect on long-term smoking abstinence in this meta-analysis.
  • The confidence intervals suggest that a clinically significant effect of naltrexone on smoking cessation is unlikely.
  • Further trials are unlikely to be resource-effective due to the current evidence and wide confidence intervals.