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European Journal of Pharmacology Dec 2015Opioids are are commonly used for the management of acute and chronic pain. Opioids have different physicochemical and pharmacokinetic characteristics, which explain the... (Review)
Review
Opioids are are commonly used for the management of acute and chronic pain. Opioids have different physicochemical and pharmacokinetic characteristics, which explain the profound changes in the clinical effect in several clinical conditions. Pharmacokinetics influences the opioid response affecting bioavailability, production of metabolites with residual clinical activity, and elimination. Generality of opioid metabolism and clinical implications for specific opioids in different clinical conditions were reviewed to bridge the gap between pharmacokinetics and clinical response. The knowledge of opioid metabolism is essential, particularly for older and complicated patients who receive multiple medications and may have impaired of renal and hepatic function. The recognition of possible metabolic problems and the consideration of adverse drug-drug interactions are fundamental to optimize the use of opioids in clinical practice.
Topics: Analgesics, Opioid; Humans; Metabolic Detoxication, Phase I; Metabolic Detoxication, Phase II
PubMed: 26522929
DOI: 10.1016/j.ejphar.2015.10.049 -
British Journal of Hospital Medicine... Jan 2024Adverse effects of perioperative opioids have led to the pursuit of 'opioid-free anaesthesia'. While early studies have shown that effective analgesia can be achieved...
Adverse effects of perioperative opioids have led to the pursuit of 'opioid-free anaesthesia'. While early studies have shown that effective analgesia can be achieved without using opioids, with some reduction in unwanted effects, further research is needed to elucidate which patients may benefit most and how.
Topics: Humans; Anesthesia; Anesthesiology; Analgesia; Analgesics, Opioid; Drug-Related Side Effects and Adverse Reactions
PubMed: 38300677
DOI: 10.12968/hmed.2023.0344 -
Pain Medicine (Malden, Mass.) Oct 2015To discuss the phenomenon of opioid induced hyperalgesia (OIH) and investigate the data and clinical recommendations available on this topic. (Review)
Review
OBJECTIVE
To discuss the phenomenon of opioid induced hyperalgesia (OIH) and investigate the data and clinical recommendations available on this topic.
DESIGN
A literature search on the topic of OIH was performed. Relevant studies pertaining to OIH were included in this review.
RESULTS
Existing studies and reviews on the pathophysiology, diagnosis, and clinical management of OIH are discussed with updated data and literature references.
CONCLUSION
As more opioids are prescribed, especially to treat chronic nonmalignant pain, OIH becomes more of a relevant and significant issue. Although the exact mechanisms of OIH are not clearly understood further research is required to broaden and develop our knowledge of this topic.
Topics: Analgesics, Opioid; Animals; Chronic Pain; Disease Models, Animal; Drug Tolerance; Humans; Hyperalgesia; Opioid-Related Disorders
PubMed: 26461074
DOI: 10.1111/pme.12914 -
Canadian Family Physician Medecin de... Mar 2018
Topics: Analgesics, Opioid; Chronic Pain; Humans; Opioid-Related Disorders; Physician-Patient Relations
PubMed: 29540394
DOI: No ID Found -
Archives of Toxicology Feb 2023Insights into the pathophysiology of many non-immune-mediated drug reactions referred to as toxicities, sensitivities, intolerances, or pseudoallergies have resulted... (Review)
Review
Insights into the pathophysiology of many non-immune-mediated drug reactions referred to as toxicities, sensitivities, intolerances, or pseudoallergies have resulted from research identifying the mastocyte-related G-protein-coupled receptor (GPCR) member X2 (MRGPRX2), a human mast cell receptor mediating adverse reactions without the involvement of antibody priming. Opioid-induced degranulation of mast cells, particularly morphine, provoking release of histamine and other preformed mediators and causing hemodynamic and cutaneous changes seen as flushing, headache and wheal and flare reactions in the skin, is an example of results of MRGPRX2 activation. Opioids including morphine, codeine, dextromethorphan and metazocine as well as endogenous prodynorphin opioid peptides activate MRGPRX2 at concentrations causing mast cell degranulation. Unlike the canonical opioid receptors, MRGPRX2 shows stereochemical recognition preference for dextro rather than levo opioid enantiomers. Opioid analgesic drugs (OADs) display a range of histamine-releasing potencies from the strong releaser morphine to doubtful releasers like hydromorphone and the non-releaser fentanyl. Whether there is a correlation between histamine release by individual OADs, MRGPRX2 activation, and presence or absence of adverse cutaneous effects is not known. To investigate the question, ongoing research with recently pursued methodologies and strategies employing basophil and mast cell tests resulting from MRGPRX2 insights should help to elucidate whether or not an opioid's histamine-releasing potency, and its property of provoking an adverse reaction, are each a reflection of its activation of MRGPRX2.
Topics: Humans; Analgesics, Opioid; Histamine; Receptors, Neuropeptide; Hypersensitivity; Receptors, G-Protein-Coupled; Morphine Derivatives; Mast Cells; Cell Degranulation; Nerve Tissue Proteins
PubMed: 36344690
DOI: 10.1007/s00204-022-03402-2 -
Pharmacology Research & Perspectives May 2021Opioids are a commonly prescribed and efficacious medication for the treatment of chronic pain but major side effects such as addiction, respiratory depression,... (Review)
Review
Opioids are a commonly prescribed and efficacious medication for the treatment of chronic pain but major side effects such as addiction, respiratory depression, analgesic tolerance, and paradoxical pain hypersensitivity make them inadequate and unsafe for patients requiring long-term pain management. This review summarizes recent advances in our understanding of the outcomes of chronic opioid administration to lay the foundation for the development of novel pharmacological strategies that attenuate opioid tolerance and hypersensitivity; the two main physiological mechanisms underlying the inadequacies of current therapeutic strategies. We also explore mechanistic similarities between the development of neuropathic pain states, opioid tolerance, and hypersensitivity which may explain opioids' lack of efficacy in certain patients. The findings challenge the current direction of analgesic research in developing non-opioid alternatives and we suggest that improving opioids, rather than replacing them, will be a fruitful avenue for future research.
Topics: Analgesia; Analgesics, Opioid; Animals; Drug Hypersensitivity; Drug Tolerance; Humans; Pain; Receptors, Opioid; Signal Transduction
PubMed: 34096178
DOI: 10.1002/prp2.789 -
Molecules (Basel, Switzerland) May 2022A few neurotransmitter systems have fascinated the research community, as muchas the opioid system (i.e., opioid ligands and their receptors) [...].
A few neurotransmitter systems have fascinated the research community, as muchas the opioid system (i.e., opioid ligands and their receptors) [...].
Topics: Analgesics, Opioid; Drug Discovery; Ligands; Receptors, Opioid
PubMed: 35630616
DOI: 10.3390/molecules27103140 -
Anesthesiology Clinics Jun 2016Opioids prescribed for chronic cancer and noncancer pain have been embroiled in public policy debates as to effectiveness and potential for contributing to society's... (Review)
Review
Opioids prescribed for chronic cancer and noncancer pain have been embroiled in public policy debates as to effectiveness and potential for contributing to society's problem with misuse, addiction, and overdose mortality. The conundrum of opioid prescribing is to determine who will most likely benefit from opioids and how medical practitioners may safely provide chronic opioid therapy, while also identifying patients who are unlikely to benefit or could divert illicit pharmaceuticals into society. Risk assessment and monitoring are essential to meet the standard of care, as is compliance with federal controlled substances law as well as state regulations.
Topics: Analgesics, Opioid; Chronic Pain; Humans; Practice Guidelines as Topic
PubMed: 27208714
DOI: 10.1016/j.anclin.2016.01.002 -
Current Neuropharmacology 2023As a global health problem, chronic pain is one of the leading causes of disability, and it imposes a huge economic and public health burden on families and society.... (Review)
Review
As a global health problem, chronic pain is one of the leading causes of disability, and it imposes a huge economic and public health burden on families and society. Opioids represent the cornerstone of analgesic drugs. However, opioid tolerance caused by long-term application of opioids is a major factor leading to drug withdrawal, serious side effects caused by dose increases, and even the death of patients, placing an increasing burden on individuals, medicine, and society. Despite efforts to develop methods to prevent and treat opioid tolerance, no effective treatment has yet been found. Therefore, understanding the mechanism underlying opioid tolerance is crucial for finding new prevention and treatment strategies. Noncoding RNAs (ncRNAs) are important parts of mammalian gene transcriptomes, and there are thousands of unique noncoding RNA sequences in cells. With the rapid development of high-throughput genome technology, research on ncRNAs has become a hot topic in biomedical research. In recent years, studies have shown that ncRNAs mediate physiological and pathological processes, including chromatin remodeling, transcription, posttranscriptional modification and signal transduction, which are key regulators of physiological processes in developmental and disease environments and have become biomarkers and potential therapeutic targets for various diseases. An increasing number of studies have found that ncRNAs are closely related to the development of opioid tolerance. In this review, we have summarized the evidence that ncRNAs play an important role in opioid tolerance and that ncRNAs may be novel targets for opioid tolerance.
Topics: Animals; Humans; MicroRNAs; Analgesics, Opioid; Drug Tolerance; RNA, Untranslated; Signal Transduction; Mammals
PubMed: 36453497
DOI: 10.2174/1570159X21666221129122932 -
Postgraduate Medicine Jan 2017Opioids are the standard of care for treating moderate-to-severe pain; however, their efficacy can be limited by adverse events (AEs), including nausea and vomiting.... (Review)
Review
Opioids are the standard of care for treating moderate-to-severe pain; however, their efficacy can be limited by adverse events (AEs), including nausea and vomiting. Opioid-induced nausea and vomiting (OINV) is an inherent adverse effect of opioid treatment, exerting effects centrally and peripherally. Opioid-related AEs can impact treatment adherence and discontinuation, which can result in inadequate pain management. OINV may persist long-term, negatively affecting patient functional outcomes, physical and mental health, patient satisfaction, and overall costs of treatment. Multiple factors may contribute to OINV, including activation of opioid receptors in the chemoreceptor trigger zone, vestibular apparatus, and gastrointestinal tract. Prophylactic or early treatment with antiemetics may be appropriate for patients who are at high risk for OINV.
Topics: Analgesics, Opioid; Antiemetics; Humans; Nausea; Pain; Vomiting
PubMed: 27690715
DOI: 10.1080/00325481.2017.1243004