The role of oxycodone/naloxone in pain management

Ból ◽  
2017 ◽  
Vol 17 (4) ◽  
pp. 26-40
Author(s):  
Magdalena Kocot-Kępska ◽  
Renata Zajączkowska ◽  
Anna Przeklasa-Muszyńska ◽  
Jan Dobrogowski

ABSTRACT: Strong opioid analgesics are essential for pain treatment of moderate to severe intensity, regardless of its etiology. An important factor limiting safety and efficacy of opioids are side effects, particularly gastrointestinal. Constipation as part of opioid induced bowel dysfunction is one of the most common reason for discontinuation of strong opioids. Introduction of novel oxycodone/naloxone formulation is an attempt to resolve the problem of opioid induced gastrointestinal side effects. On the basis of clinical trials from 2008-2016 the authors discuss the applicability of oxycodone/naloxone prolonged release in management of different pain syndromes in humans, in cancer patients, in neuropathic pain patients, in the elderly, in acute post-operative pain and other clinical indications for example restless leg syndrome. Presented data indicate comparable or in some cases even better analgesic efficacy of oxycodone with naloxone and lower risk of gastrointestinal side effects, especially constipation, when compared to other strong opioids. The introduction of oxycodone with naloxone significantly expands treatment options for chronic pain patients, likewise improving safety and thus the effectiveness of treatment with strong opioids.

2019 ◽  
Vol 32 (2) ◽  
pp. 108-110 ◽  
Author(s):  
E. Besserer-Offroy ◽  
P. Sarret

In the past few years, several biased ligands acting at the mu-opioid receptor were reported in the literature. These agonists are aimed at reducing pain while having fewer side effects than morphine, the gold standard of opioid analgesics. In this mini-review, we describe and discuss the recent advances in mu-biased ligands actually in preclinical and clinical development stages, including the latest U.S. Food and Drug Administration review of oliceridine, a biased mu-agonist for moderate to severe acute pain treatment developed by the company Trevena.


Lung ◽  
2020 ◽  
Vol 198 (2) ◽  
pp. 395-403 ◽  
Author(s):  
M. Drent ◽  
V. L. J. Proesmans ◽  
M. D. P. Elfferich ◽  
N. T. Jessurun ◽  
S. M. G. de Jong ◽  
...  

Abstract Background Clinical manifestations of sarcoidosis vary widely, depending on the intensity of the inflammation and the organ systems affected. So far, no curative treatment exists; the disease can only be suppressed. All treatment options cause side effects affecting quality of life. The aim of this study was to establish and rank the prevalence of self-reported gastrointestinal side effects of drugs used in the treatment of sarcoidosis. Methods A cross-sectional web-based anonymous survey about complaints and side effects was conducted among sarcoidosis patients in the Netherlands, United Kingdom, and United States of America. Results Of the participants, 70% were being treated with one or more drugs. The most important reported side effect was weight gain, associated with increased appetite among prednisone users (as monotherapy as well as in combination with other drugs). Methotrexate (MTX) users especially experienced nausea, with monotherapy as well as combination therapy. Vomiting and weight loss were most prominent among azathioprine and mycophenolate mofetil (MMF) users, whereas diarrhoea was frequently mentioned by MMF and MTX users. The reported side effects of hydroxychloroquine were generally rather mild. Conclusion The current study ranked the gastrointestinal side effects associated with pharmacotherapy in sarcoidosis patients. Pharmacotherapy does have multiple gastrointestinal side effects. The strongest association between a reported side effect and drug use was that of weight gain associated with increased appetite among prednisone users. It would therefore be useful for future research to look further into dietary interventions to counter these side effects and reduce their burden.


Cancer ◽  
1989 ◽  
Vol 63 (11) ◽  
pp. 2284-2288 ◽  
Author(s):  
Russell K. Portenoy ◽  
Mathelyn Maldonado ◽  
Ronald Fitzmartin ◽  
Robert F. Kaiko ◽  
Ronald Kanner

2012 ◽  
Vol 30 (5_suppl) ◽  
pp. 170-170
Author(s):  
Jaclyn Lee Fong Bosco ◽  
Barbara Halpenny ◽  
Donna Lynn Berry

170 Background: Men diagnosed with localized prostate cancer (LPC) can choose from multiple treatment regimens and are faced with a decision in which medical factors and personal preferences are important. The Personal Patient Profile-Prostate (P3P) is a computerized decision aid for men with LPC that focuses on personal preferences. We determined the proportion of men with LPC who chose a concordant treatment approach by 6-months with self-reported, influential side effects by intervention or control group, and evaluated whether the intervention (versus control) group was more likely to choose a concordant treatment. Methods: English or Spanish-speaking men diagnosed with LPC (2007–2009) from four US cities were enrolled into a randomized trial and followed at 1- and 6-months via mailed or online questionnaire. Men were randomized to receive the P3P intervention or standard education plus links to reputable websites (control group). We classified concordance as men who were (a) concerned with urinary incontinence and/or erectile dysfunction and chose radiotherapy, (b) concerned with bowel dysfunction and chose prostatectomy, (c) concerned with all three side effects and chose watchful waiting, or (d) not concerned with any side effect and chose any treatment. We calculated the proportion of concordance by group. Using logistic regression, we calculated odds ratios (OR) and 95% confidence intervals (CI) for the association between the P3P intervention and concordance. Results: Of 448 men, most were <65 years, non-Hispanic white, and had multiple physician consultations prior to study enrollment. Only 43% of the sample chose a concordant treatment given concerns about potential side effects. There was no significant difference in concordance between the intervention (43%) and control (42%) group (OR=1.1; 95%CI=0.73, 1.7). Conclusions: The P3P intervention was not associated with concordance between potential side effects and treatment choice. Information and/or physician consultation immediately after diagnosis was likely to influence decisions despite concerns about side effects. The intervention may be more effective before the first treatment options consultation.


2019 ◽  
Vol 16 (3) ◽  
pp. 781-790
Author(s):  
Hayriye Baltaoğlu Alp

Research problem/aim: In a multicenter study of the World Health Organization, 22% of patients who applied to primary health care centers reported that their pain continued for 6 months. Multidisciplinary approach and empathy are important for patients with chronic pain. 20% of first-line outpatient referrals consist of chronic painful cases. When the analgesics are used correctly in the treatment of pain, sufficient pain control can be achieved in 85%. Non-steroidal and steroid analgesics may present with high doses of gastrointestinal side effects. Method: The sociodemographic characteristics of the participants were recorded on the forms prepared by the researchers. Finding: The mean age of the patients was 58.62 ± 10.72.Pain was found to affect sleep. (* p <0.05) Conclusion: The patient sector, which is far from rational drug use, can cause great harm to the country's economy. With the extensive studies to be carried out, the treatment method of the patients and the reasons why they prefer. It will be helpful for the chronic pain patients to get the right information from their doctors about the treatment options. For this reason, family physicians should be equipped with up-to-date information about all methods used in chronic pain treatment. Extended English summary is in the end of Full Text PDF (TURKISH) file.   Özet Araştırma problem/amaç: Dünya Sağlık Örgütünün çok merkezli yapılan bir araştırmasında birinci basamak sağlık merkezlerine başvuran hastaların %22’sinde ağrılarının 6 aydır devam ettiği belirtilmektedir. Kronik ağrısı olan hastalara multidispliner yaklaşım ve empati önemlidir. Birinci basamak poliklinik başvurularının %20’si kronik ağrılı olgulardan oluşmaktadır. Ağrı tedavisinde analjezikler doğru kullanıldığında %85’inde yeterli ağrı kontrolü sağlanabilmektedir. Non-steroid ve steroid analjezikler yüksek dozlarda gastrointestinal yan etkilerle karşımıza çıkabilmektedir. Metot: Katılımcıların sosyodemografik özellikleri araştırmacılar tarafından önceden hazırlanan formlara kaydedildi. Bulgular: Çalışmaya katılan hastaların ortalama yaşları 58.62±10.72 olarak tespit edildi. Ağrının uykuyu etkilediği bulunmuştur.(* p<0,05) Sonuçlar: Akılcı ilaç kullanımından uzak hasta kesimi ülke ekonomisine büyük zararlar verebilmektedir. Yapılacak geniş kapsamlı çalışmalar ile hastaların hangi tedavi yöntemini, neden tercih ettikleri konusu daha açığa kavuşacaktır. Kronik ağrı hastalarının tedavi seçenekleri hakkında doktorlarından doğru bilgi alması kendisine en uygun yöntemi seçmesi konusunda yol gösterici olacaktır. Bunun için de aile hekimlerinin kronik ağrı sağaltımında kullanılan tüm yöntemler hakkında güncel bilgilerle donanımlı olması gerekmektedir.


2017 ◽  
Vol 17 (1) ◽  
pp. 193-200 ◽  
Author(s):  
Vigdis Solhaug ◽  
Espen Molden

AbstractBackgroundAs pain is often a comorbid condition, many patients use opioid analgesics in combination with several other drugs. This implies a generally increased risk of drug interactions, which along with inherent pharmacogenetic variability and other factors may cause differences in therapeutic response of opioids.AimTo provide an overview of interactions and pharmacogenetic variability of relevance for individual differences in effect and tolerability of opioid analgesics, which physicians and other healthcare professionals should be aware of in clinical practice.MethodsThe article was based on unsystematic searches in PubMed to identify literature highlighting the clinical impact of drug interactions and pharmacogenetics as sources of variable response of opioid analgesics.ResultsCytochrome P450 (CYP)-mediated metabolism is an important process for both clinically relevant interactions and pharmacogenetic variability of several opioids. Concomitant use of CYP inhibitors (e.g. paroxetine, fluoxetine and bupropion) or inducers (e.g. carbamazepine, phenobarbital and phenytoin) could counteract the clinical effect or trigger side effects of analgesics in the same manner as genetically determined differences in CYP2D6-mediated metabolism of many opioids. Moreover, combination treatment with drugs that inhibit or induce P-glycoprotein (ABCB1), a blood-brain barrier efflux transporter, may alter the amount (‘dose’) of opioids distributed to the brain. At the pharmacodynamic level, it is crucial to be aware of the potential risk of interaction causing serotonergic syndrome when combining opioids and serotonergic drugs, in particular antidepressants inhibiting serotonin reuptake (SSRIs and SNRIs). Regarding pharmacogenetics at the receptor level of pain treatment, the knowledge is currently scarce, but an allelic variant of the μ1 opioid receptor (OPRM1) gene has been associated with higher dosage requirement to achieve analgesia.Conclusions and implicationsDrug interactions and pharmacogenetic differences may lead to therapeutic failure or serious side effects of opioid analgesics. Many interactions involve combinations with antidepressants and antiepileptics, which are highly relevant drugs in patients suffering from pain. To prevent unfavourable drug interactions it is important that clinicians pay close attention and use electronic drug interaction checkers when treatments are initiated or discontinued. For the management of issues related to pharmacogenetic differences, blood-based CYP genotyping is available as routine test at many laboratories, and provide a valuable tool for proper choice of drugs and doses for treatment of pain and other diseases.


2018 ◽  
Vol 4 (3) ◽  
pp. 163 ◽  
Author(s):  
George Colclough, MD ◽  
John T. McLarney, MD ◽  
Paul A. Sloan, MD ◽  
K. Todd McCoun, MD ◽  
Gregory L. Rose, MD ◽  
...  

Epidural opioids provide significant postoperative analgesia; however, their use is often limited by side effects such as nausea and pruritus, or they require the addition of epidural local anesthetics with possible side effects of motor block and hypotension. Adjuncts to epidural opioid analgesia would benefit pain management. There is evidence that epidural butyrophenones may enhance opioid analgesics and reduce side effects. The authors present the first reported use of epidural haloperidol to enhance epidural morphine analgesia in three individuals. Pharmacodynamic interactions of haloperidol, which may explain its analgesic efficacy, are summarized.


2018 ◽  
Vol 5 (3) ◽  
pp. 145 ◽  
Author(s):  
Peter Holzer, PhD ◽  
Sam H. Ahmedzai, BSc, MBChB, FRCP ◽  
Norbert Niederle, MD ◽  
Petra Leyendecker, PhD ◽  
Michael Hopp, MD ◽  
...  

Opioids are the mainstay of management for patients with cancer-related pain. Although the analgesic efficacy of opioid therapy is well documented, the recent European Pain in Cancer survey demonstrated that the management of moderate-to-severe pain in patients with cancer is far from optimal. Bowel dysfunction, and importantly constipation, is a common side effect and has a significant impact on the patient’s morbidity and quality of life. Nonpharmacological strategies and laxatives are often not effective in the management of opioid-induced constipation (OIC), making it necessary to search for new strategies for the treatment of opioid-induced bowel dysfunction. One promising strategy is the prevention of OIC with peripherally acting opioid antagonists that specifically target the underlying cause of this condition, without affecting centrally mediated analgesia. In recent studies, the novel combination of prolonged-release oral oxycodone and prolonged-release oral naloxone provided effective analgesia with improved bowel function in patients suffering from severe cancer-related and noncancer-related pain. The combination has the potential to improve the quality of pain management significantly in these patients.


2018 ◽  
Vol 25 (32) ◽  
pp. 3895-3916 ◽  
Author(s):  
Andrea Bedini ◽  
Santi Spampinato

Background: Chronic pain states are clinically relevant and yet unsolved conditions impacting on quality of life and representing an important social and economic burden; these diseases are poorly treated with the currently available drugs, being urgent the need of innovative analgesics. In this frame, novel analogues of endomorphin-1 and dermorphin emerge as promising starting points to develop innovative, more effective analgesics to treat neuropathic pain. Methods: An extensive and structured search of bibliographic databases for peer-reviewed research literature was undertaken using focused review questions; all the retrieved papers were published on prestigious international journals by the experts of the field and were carefully analyzed to collect all the information and data necessary to the conceptual framework of this review. Results: One hundred papers were included in this review; forty-one defined the up-to-date findings on neuropathic pain etiopathogenesis and its currently available treatment options. Thirty-five papers described all the advantages and drawbacks of using endomorphin-1 (23) or dermorphin (12) in the frame of neuropathic pain and outlined the most relevant advances in developing endomorphin-1 and dermorphin analogs useful as potential, innovative analgesics. Twenty-four papers provided the latest insights into exploiting biased agonism at opioid receptor as an innovative strategy to develop more effective and safer analgesics. Conclusion: This review reports that innovative opioid peptides will be of great help in better understanding the multifaceted scenario of neuropathic pain treatment, providing very interesting opportunities for the identification of novel and more effective opioid analgesics to be employed as medications.


2014 ◽  
Vol 32 (16) ◽  
pp. 1671-1676 ◽  
Author(s):  
Sebastiano Mercadante ◽  
Giampiero Porzio ◽  
Vittorio Gebbia

Despite the skilled use of opioid analgesics, which is crucial to the relief of cancer pain, there is a lack of evidence to support many aspects of current clinical practice. Therefore, there is a significant need for more effective treatment options. New opioids have been marketed in the past years, including hydrocodone and oxymorphone. Moreover, mixed opioids with combined mechanisms of action have been developed; one such agent, tapentadol, is a centrally acting oral analgesic that possesses a combined mechanism of action: μ-opioid receptor activation with norepinephrine reuptake inhibition. Drug development strategies involving naloxone have been initiated to reduce peripheral opioid-related adverse effects. The rationale is based on the local antagonist activity of naloxone in intestinal opioid receptors and the negligible oral bioavailability of naloxone, particularly in a prolonged-release formulation. New delivery systems have been developed to provide rapid analgesia with potent opioid drugs such as fentanyl. Despite the upcoming availability of these new drugs and technologies that will add to existing types of opioid medication, their benefits and liabilities will ultimately need to be determined by the individual physician and individual patient experiencing pain.


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