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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 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...
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...
Combined Effects of Drugs: Synergism01:27

Combined Effects of Drugs: Synergism

Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
Agonism and Antagonism: Quantification01:14

Agonism and Antagonism: Quantification

When drugs are administered, they can elicit either an agonist or antagonist effect on the body. Agonism occurs when a drug activates a specific receptor, triggering a biological response. On the other hand, antagonism happens when a drug binds to the same receptors but blocks their activation, thereby preventing a biological response.
To quantify these effects, researchers use a dose-response curve, which provides valuable information about the potency and efficacy of a drug. Potency refers to...

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Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities
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Published on: July 29, 2014

Evidence from basic research for opioid combinations.

Mellar P Davis1

  • 1Taussig Cancer Institute, Case Western Reserve University, Lerner School of Medicine, Cleveland Clinic, Palliative Medicine and Supportive Oncology Services, Cleveland, OH 44195, USA. davism6@ccf.org

Expert Opinion on Drug Discovery
|April 4, 2012
PubMed
Summary
This summary is machine-generated.

Opioid combinations show promise for better pain relief and fewer side effects in animal studies. Further research is needed to optimize dosing and understand effects on different pain types and side effects.

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Area of Science:

  • Pharmacology
  • Pain Management
  • Drug Development

Background:

  • Single opioid analgesics have limited efficacy and significant side effects.
  • Adjuvant analgesics are used to enhance opioid therapy.
  • Basic science research suggests opioid combinations may improve the therapeutic index and prevent tolerance.

Purpose of the Study:

  • To review opioid receptor pharmacology and its implications for combination therapy.
  • To explore the potential of opioid combinations for improved analgesia and reduced side effects.
  • To provide a rationale for clinical trials of opioid combinations.

Main Methods:

  • Review of opioid receptor genetics and downstream signaling.
  • Discussion of functional selectivity and ligand-biased responses in opioid pharmacodynamics.
  • Examination of preclinical evidence for opioid combinations (agonist-agonist, agonist-antagonist).

Main Results:

  • Opioid combinations (e.g., morphine with antagonists, oxycodone, fentanyl, methadone) improved analgesia in animal models.
  • Combinations demonstrated potential in blunting physical and psychological dependence markers.
  • Preclinical data support the rationale for clinical trials of opioid combinations.

Conclusions:

  • Opioid combinations offer a potential strategy to enhance analgesia and mitigate dependence.
  • Further research is required to determine optimal dosing, schedules, and ratios for clinical use.
  • Pain phenotype and side effect profiles of opioid combinations warrant close investigation in future trials.