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Related Concept Videos

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...
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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...
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...
Drug Delivery Systems: Different Types01:27

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Conventional oral drug products, termed immediate-release (IR) formulations, are engineered to promptly release their active pharmaceutical ingredient (API) upon ingestion, typically in tablets or capsules. This rapid release often results in swift drug absorption and consequent pharmacodynamic effects, although the timing and intensity can vary depending on the drug's properties. Prodrugs within these formulations require metabolic conversion to activate their pharmacodynamic effects,...
Prescription, Nonprescription and Orphan Drugs01:02

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Prescription drugs require a prescription from a medical practitioner and can only be obtained from a pharmacy. They have many applications, including treating pain, anxiety, and hypertension.
The misuse and addiction to prescription drugs is a growing problem that can affect people of all age groups, specifically teenagers. This can happen when prescription medications are used in ways not intended by the prescriber, such as taking someone else's prescription or using medication for...
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Oral drug delivery is the most common route of administration due to its convenience, cost-effectiveness, and high patient compliance. It enables precise formulation to ensure proper drug dosage and bioavailability. The development of oral dosage forms considers drug properties such as solubility, stability, and absorption to optimize therapeutic efficacy.Tablets, capsules, liquids, and chewable formulations enhance drug stability, mask undesirable tastes, and improve patient experience.

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Opioid formulations designed to resist/deter abuse.

Robert B Raffa1, Joseph V Pergolizzi

  • 1Department of Pharmaceutical Sciences, Temple University School of Pharmacy, Philadelphia, Pennsylvania 19140, USA. robert.raffa@temple.edu

Drugs
|August 25, 2010
PubMed
Summary

New opioid formulations aim to deter abuse in chronic pain patients. While innovative, their effectiveness against resourceful individuals remains undetermined, requiring further study.

Area of Science:

  • Pharmacology
  • Pain Management
  • Drug Abuse Prevention

Background:

  • Opioid analgesics are prescribed for chronic pain, but abuse is a significant concern.
  • Abuse ranges from misuse to diversion for profit.
  • Innovative formulations are being developed to resist or deter abuse.

Purpose of the Study:

  • To examine novel opioid formulations designed to deter abuse.
  • To review clinical studies on the safety and effectiveness of these new products.

Main Methods:

  • Review of three abuse-deterrent opioid formulations: Embeda (extended-release morphine with sequestered naloxone), Remoxy (controlled-release oxycodone in a high-viscosity capsule), and Acurox with niacin (immediate-release oxycodone with subtherapeutic niacin).
  • Examination of the specific abuse-resistance mechanisms of each formulation.

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  • Analysis of reported clinical safety and effectiveness data.
  • Main Results:

    • Embeda utilizes sequestered naltrexone released upon tablet compromise.
    • Remoxy's capsule design resists needle extraction.
    • Acurox with niacin incorporates a gel-forming agent and niacin to deter inhalation/injection and excessive intake.

    Conclusions:

    • These abuse-deterrent formulations represent important innovations in pain management.
    • Their ultimate effectiveness in preventing abuse by resourceful individuals is yet to be determined.
    • Further research is warranted to assess their role in clinical practice.