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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...
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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...
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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...
Phase II Reactions: Methylation Reactions01:17

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Methylation is a phase II biotransformation process involving the attachment of a methyl group to a substrate. Enzymes known as methyltransferases orchestrate this reaction.
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Modified-release dosage forms are designed to address the limitations of drugs with short biological half-lives. These forms maintain stable therapeutic drug concentrations over extended periods, reducing the need for frequent dosing. A consistent drug level helps minimize peak-trough fluctuations, which can reduce adverse effects, lower the risk of drug resistance, and improve overall treatment effectiveness.One common type of modified-release form is the extended-release (ER) formulation. ER...
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Continuous-release drug delivery systems offer a strategic approach to maintaining therapeutic drug levels over extended periods following oral administration. By modulating the release rate of active pharmaceutical ingredients, these systems minimize fluctuations in plasma concentrations, which enhances clinical efficacy and reduces the need for frequent dosing. Such characteristics make them particularly advantageous in managing chronic diseases where patient adherence and stable drug...

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Related Experiment Video

Updated: Jun 29, 2026

A General Method for Evaluating Deep Brain Stimulation Effects on Intravenous Methamphetamine Self-Administration
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Published on: January 22, 2016

Long acting methadone

N H Choulis, H Papadopoulos, M Choulis

    Die Pharmazie
    |July 1, 1976
    PubMed
    Summary

    Sustained release tablets were developed using matrix and eroding tablet concepts for controlled drug delivery. Optimized formulations provided prolonged analgesia for up to 60 hours in rats without adverse effects.

    Area of Science:

    • Pharmaceutical Sciences
    • Drug Delivery Systems
    • Pharmacology

    Background:

    • Sustained release formulations are crucial for improving therapeutic efficacy and patient compliance.
    • Traditional drug delivery methods often result in fluctuating plasma concentrations and potential side effects.
    • The matrix and eroding tablet concepts offer promising strategies for controlled drug release.

    Purpose of the Study:

    • To formulate and characterize sustained release tablets using different approaches.
    • To investigate the influence of formulation parameters on drug release kinetics.
    • To evaluate the in vivo efficacy and safety of optimized sustained release tablets.

    Main Methods:

    • Tablets were prepared using pan-coating, congealing, plasticization, and direct compression.

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  • Dissolution testing was performed using official methods.
  • Active ingredient analysis was conducted using gas-liquid chromatography (GLC).
  • In vivo analgesia was assessed in male albino rats.

    • Main Results:

    • Particle size of plastic material affected release rates from porous inert matrices, leading to incomplete drug release.
    • Three-layer slowly-eroding tablets with carbomer achieved quantitative drug release by adjusting gum proportion.
    • Linear drug release-time relationships were approximated in three-layer tablets with varying drug concentrations.
    • A 30 mg methadone tablet formulation provided analgesia for approximately 60 hours in rats.

    Conclusions:

    • Formulation strategies involving matrix and slowly-eroding concepts can effectively control drug release.
    • Optimized three-layer eroding tablets offer predictable and prolonged drug delivery.
    • Sustained release methadone tablets demonstrate significant analgesic potential with a favorable safety profile.