Related Experiment Video
Updated: Feb 1, 2026
09:11
Use of MRI-ultrasound Fusion to Achieve Targeted Prostate Biopsy
Published on: April 9, 2019
22.4K
Advances in Achieving Opioid Analgesia Without Side Effects
Halina Machelska1, Melih Ö Celik1
1Department of Experimental Anesthesiology, Charité - Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, and Berlin Institute of Health, Berlin, Germany.
Frontiers in Pharmacology
|December 18, 2018
Summary
Developing safer opioids is crucial to combat the opioid crisis. Emerging strategies focus on targeted pain relief and reduced side effects, offering new hope for effective pain management.
Area of Science:
- Pharmacology
- Pain Management
- Drug Development
Background:
- Opioids are effective for severe pain but cause addiction and overdose deaths, fueling a global opioid crisis.
- There is an urgent need for the development of safer opioid analgesics with improved side effect profiles.
Purpose of the Study:
- To provide a critical overview of emerging opioid-based strategies for pain relief.
- To discuss novel approaches aimed at improving opioid side effect profiles.
Main Methods:
- Overview of biased agonism strategies.
- Targeting peripheral opioid receptors (e.g., nanocarriers, low pH-sensitive agonists).
- Exploration of heteromers, receptor splice variants, and endogenous opioid peptides.
Main Results:
- Pharmaceutical development of new opioids, including peripheral kappa-receptor agonists, is advancing.
- Treatments that augment endogenous opioid action have entered clinical trials.
- Numerous novel opioids show promise in preclinical studies.
Conclusions:
- Emerging opioid-based strategies offer potential for effective pain relief with reduced adverse effects.
- Further research and careful consideration of strategies like biased agonism are necessary for clinical translation.
Related Concept Videos
01:15Opioid Analgesics: Synthetic and Semisynthetic Opioids
1.1K
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...
1.1K
01:22Opioid Receptors: Overview
4.3K
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,...
4.3K
01:25Analgesia and Pain Management
1.6K
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...
1.6K
01:20Opioid Analgesics: Morphine and Other Natural Cogeners
1.0K
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...
1.0K
01:17Drugs Affecting GI Tract Motility: Opioids as Antidiarrheal Agents
675
Diarrhea, a condition marked by frequent loose or watery bowel movements, can be triggered by multiple factors such as viral or bacterial infections, food intolerances, anxiety, medications, and digestive disorders. Symptoms may include abdominal pain, bloating, nausea, and cramping. Severe or prolonged diarrhea can lead to complications like electrolyte imbalances, malnutrition, and dehydration if left untreated.
Opioids, widely used antidiarrheal agents, mitigate diarrhea by slowing down...
Opioids, widely used antidiarrheal agents, mitigate diarrhea by slowing down...
675
02:22Overview of Advanced Functional Groups
29.8K
Functional groups are groups of atoms with specific chemical properties that occur within organic molecules and are sometimes denoted as “R”. Functional groups can “functionalize” a compound by enabling it to adopt different physical and chemical properties.
Types of Advanced Functional Groups
The table below summarizes some of the major functional groups in organic chemistry.
29.8K