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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 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...
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 Receptors: Overview01:22

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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...
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Combined Effects of Drugs: Synergism

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Combining Laser Capture Microdissection and Microfluidic qPCR to Analyze Transcriptional Profiles of Single Cells: A Systems Biology Approach to Opioid Dependence
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[Opioid effects - galenics make the difference].

Kuno Güttler1

  • 1Uniklinik Köln. kuno.guettler@uk-koeln.de

Anasthesiologie, Intensivmedizin, Notfallmedizin, Schmerztherapie : AINS
|April 17, 2012
PubMed
Summary

Extended-release opioid formulations vary significantly in quality. Key parameters like peak-trough fluctuation, time to maximum concentration, and half-value duration demonstrate substantial differences, impacting therapeutic efficacy and substitution possibilities.

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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Combining Laser Capture Microdissection and Microfluidic qPCR to Analyze Transcriptional Profiles of Single Cells: A Systems Biology Approach to Opioid Dependence
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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

Area of Science:

  • Pharmacokinetics and Drug Delivery
  • Pharmaceutical Technology
  • Opioid Formulations

Context:

  • Extended-release opioid formulations exhibit considerable variability in their galenic properties.
  • Assessing the quality of these formulations is crucial for ensuring consistent therapeutic outcomes.
  • Current evaluation methods often prove insufficient for precise quality assessment.

Purpose:

  • To evaluate the galenic quality of extended-release opioids using key pharmacokinetic parameters.
  • To highlight the variability in drug release profiles among different opioid formulations.
  • To establish parameters for assessing the suitability of extended-release opioid substitution.

Summary:

  • The galenic quality of extended-release opioids can be assessed using Peak-Trough Fluctuation (PTF), time to maximum concentration (Tmax), and Half-Value Duration (HVD).
  • Significant variations exist in PTF, Tmax, and HVD values across different extended-release opioid products, influencing plasma level fluctuations and onset of action.
  • Jurnista® demonstrates a favorable profile with lower PTF and longer HVD compared to other formulations, suggesting superior controlled-release characteristics.

Impact:

  • Understanding these pharmacokinetic differences is essential for clinicians when prescribing and substituting extended-release opioids.
  • The observed variability challenges the concept of 'aut-idem' substitution for these critical medications.
  • This analysis provides a framework for a more rigorous evaluation of extended-release opioid formulations, potentially leading to improved patient safety and treatment efficacy.