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Related Concept Videos

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...
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...
Pain01:20

Pain

Pain serves as a critical warning signal that alerts the body to potential or actual harm. When mechanical pressure on the skin is intense, such as from a sharp pinch, the sensation transitions from touch to pain. Similarly, extreme temperatures, like a hot pot handle, convert the sensation of heat into pain. Pain can also result from overstimulation of other senses, such as blinding light, loud noise, or the intense heat from habañero peppers. This ability to sense pain is essential for...
Nociception01:44

Nociception

Nociception—the ability to feel pain—is essential for an organism’s survival and overall well-being. Noxious stimuli such as piercing pain from a sharp object, heat from an open flame, or contact with corrosive chemicals are first detected by sensory receptors, called nociceptors, located on nerve endings. Nociceptors express ion channels that convert noxious stimuli into electrical signals. When these signals reach the brain via sensory neurons, they are perceived as pain. Thus, pain helps the...

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Intracranial Pharmacotherapy and Pain Assays in Rodents
02:26

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Published on: April 9, 2019

Opioid peptides in peripheral pain control.

Anna Lesniak1, Andrzej W Lipkowski

  • 1Mossakowski Medical Research Centre Polish Academy of Sciences, Warsaw, Poland. alesniak.imdik@gmail.com.

Acta Neurobiologiae Experimentalis
|April 19, 2011
PubMed
Summary

Classical opioids treat pain via central nervous system receptors. Novel peripheral opioid receptor analogs offer targeted pain relief with fewer side effects, aiding chronic pain management.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Pain Management

Background:

  • Opioids are widely used for pain relief, acting on central nervous system (CNS) opioid receptors.
  • Opioid receptors are also present in the periphery, offering potential for localized analgesia.
  • Current opioid therapies can have significant side effects due to central nervous system activation.

Purpose of the Study:

  • To explore the therapeutic potential of peripheral opioid receptors for pain management.
  • To investigate novel peptidic opioid receptor analogs for analgesia.
  • To develop pain therapies with reduced central side effects.

Main Methods:

  • Review of existing literature on opioid receptors and endogenous opioid peptides.
  • Analysis of the role of peripheral opioid receptors in pain pathways.

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  • Discussion of novel peptidic analogs with limited blood-brain barrier penetration.

    • Main Results:

    • Peripheral opioid receptors represent a promising target for non-central analgesia.
    • Endogenous opioid peptides modulate pain signaling, offering opportunities for drug development.
    • Peptidic opioid analogs with restricted CNS access may enable safer, prolonged pain treatment.

    Conclusions:

    • Targeting peripheral opioid receptors can provide effective pain relief with potentially fewer CNS-related adverse effects.
    • Novel opioid analogs offer a promising avenue for developing safer and more effective analgesics for chronic pain.
    • Further research into peripheral opioid receptor modulation is warranted for advanced pain therapy.