Opioid Analgesics
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2021 ◽  
Vol 7 (3) ◽  
pp. 41-47
Alexander A. Spasov ◽  
Olesya Iu. Grechko ◽  
Natalya V. Eliseeva ◽  
Yuliya V. Lifanova ◽  
Angelina N. Aleksandrenkova

Introduction: Adjuvant medications can be used to increase the analgesic effect of opioid analgesics, reduce the manifestation of side effects, and also for premedication. This paper provides information on the effect of clonidine, haloperidol, metocloparmide, diazepam, midazolam on opioid analgesics: - morphine and the selective kappa-opioid agonist compound RU-1205. Materials and methods: A probable interaction between RU-1205, morphine and adjuvant drugs in pain behaviors was carried out on the model of somatogenic pain. 95 male mice received either RU-1205 (5 mg/kg, i.p.) and morphine (1 mg/kg, i.p.) separately or in combination with haloperidol (0.45 mg/kg, i.p.); midazolam (0.3 mg/kg, i.p.); diazepam (1 mg/kg, i.p.); metoclopramide (5 mg/kg, i.p.), and clonidine (1 mg/kg, i.p.). The analgesic effect was assessed by tail flick test. Registration of the latent period of the reaction was carried out 30, 60 and 90 minutes after the adjuvant drug administration. Results: When studying the interaction with morphine, it was found that clonidine, haloperidol and metoclopramide enhanced the effects; diazepam offset them, and midazolam had no affect on the analgesic properties. In the course of the studies, RU-1205 showed an increase in analgesic activity when combined with clonidine, a slight increase with midazolam, and a decrease when co-administered with diazepam. Haloperidol had no influence on the effect of RU-1205, while metoclopramide both potentiated and reduced the analgesic effect. Discussion: Pharmacodynamic and pharmacokinetic interactions of RU-1205 with an α2AR agonist, benzodiazepine receptor agonists, D2P antagonist, and σ-receptor blocker were established. Conclusion: The presented data make it possible to more accurately formulate ideas about the localization and action mechanism of the kappa-agonist of opioid receptors, the compound RU-1205.

2021 ◽  
Vol 41 ◽  
pp. 101135
Liang Zhao ◽  
Zhichuan Li ◽  
Lanyan Fang ◽  
Myong-Jin Kim ◽  
Srikanth C. Nallani ◽  

Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5448
Sandra Piras ◽  
Gabriele Murineddu ◽  
Giovanni Loriga ◽  
Antonio Carta ◽  
Enrica Battistello ◽  

Opioid analgesics are clinically used to relieve severe pain in acute postoperative and cancer pain, and also in the long term in chronic pain. The analgesic action is mediated by μ-, δ-, and κ-receptors, but currently, with few exceptions for k-agonists, μ-agonists are the only ones used in therapy. Previously synthesized compounds with diazotricyclodecane cores (DTDs) have shown their effectiveness in binding opioid receptors. Fourteen novel diazatricyclodecanes belonging to the 9-propionyl-10-substituted-9,10-diazatricyclo[,5]decane (compounds 20–23, 53, 57 and 59) and 2-propionyl-7-substituted-2,7-diazatricyclo[,8]decane (compounds 24–27, 54, 58 and 60) series, respectively, have been synthesized and their ability to bind to the opioid μ-, δ- and κ-receptors was evaluated. Five of these derivatives, compounds 20, 21, 24, 26 and 53, showed μ-affinity in the nanomolar range with a negligible affinity towards δ- and κ-receptors and high μ-receptor selectivity. The synthesized compounds showed μ-receptor selectivity higher than those of previously reported methylarylcinnamyl analogs.

Jordan T. Bateman ◽  
Erica S. Levitt

Respiratory depression is a potentially fatal side effect of opioid analgesics and major limitation to their use. G-protein-biased opioid agonists have been proposed as "safer" analgesics with less respiratory depression. These agonists are biased to activate G proteins rather than β-arrestin signaling. Respiratory depression has been shown to correlate with both G-protein bias and intrinsic efficacy, and recent work has refuted the role of β-arrestin signaling in opioid-induced respiratory depression. In addition, there is substantial evidence that G-proteins do, in fact, mediate respiratory depression by actions in respiratory-controlling brainstem neurons. Based on these studies, we provide the perspective that protection from respiratory depression displayed by newly developed G-protein biased agonists is due to factors other than G-protein versus arrestin bias.

Pain Medicine ◽  
2021 ◽  
Connor Polson ◽  
Parker Siex ◽  
J Michael Anderson ◽  
Michael Weaver ◽  
Will Roberts ◽  

Abstract Objective We sought to determine whether author conflict of interest (disclosed or undisclosed) or industry sponsorship influenced the favorability of reporting of systematic reviews and meta-analyses investigating the use of opioid analgesics for the management of chronic non-cancer pain. Methods Our search included the MEDLINE (Ovid) and Embase (Ovid) databases. Study sponsorship was determined using the funding statement provided in each systematic review. Author COI information was extracted from the COI disclosure statement. This information was cross-referenced with information available on the CMS Open Payments Database, Dollars for Profs, Google Patents, the United States Patent and Trademark Office (USPTO), and previously published COI disclosures. Results Eight systematic reviews authored by 83 authors were included. Of these authors, 19 (23.0%) were found to have a COI, of which the majority (17/19; 89.5%) had at least one undisclosed COI. Despite nearly one-quarter of authors having a COI, we found no association between the presence of a COI and the favorability of results (p = 0.64) or conclusions (p = 0.07). Conclusion COI are common and frequently undisclosed among systematic review authors investigating opioid analgesics for the management of chronic non-cancer pain. Despite a high prevalence of COI, we did not find that these author-industry relationships had a significant influence on the favorability of results and conclusions; however, our findings should be considered a lower bound estimate of the true influence author COI have on outcomes of pain medicine systematic reviews secondary to the low sample size included in the present study.

2021 ◽  
Vol ahead-of-print (ahead-of-print) ◽  
Faiqa Naz ◽  
Kanwar Hamza Shuja ◽  
Muhammad Aqeel ◽  
Saima Ehsan ◽  
Atqa Noor ◽  

Purpose There is an ever-increasing number of patients suffering from various forms of acute and chronic pain and getting treatment for such ailments is a basic human right. Opioid analgesics remain one way of managing and attending to such patients. However, due to the prevalence of opiophobia, many doctors avoid prescribing opioid-based medicines, even at the cost of patients suffering leading to a hindrance in providing optimal health care. Up till now, there has been no reliable and valid instrument to measure the severity of opiophobia in doctors. For this reason, the purpose of this study is to represent the construction of a precise and reliable instrument for measuring opiophobia along with its validation for doctors in Pakistan. Design/methodology/approach Interviews and theoretical knowledge relating to opiophobia were used as the basis for the purpose of generating an item pool. The generated item pool was evaluated by subject matter experts for content validity and inter-rater reliability, followed by Velicer’s minimum average partial method and maximum likelihood factor analysis for establishing the factorial structure of the scale. As opiophobia in doctors prevails the most and causes a lower ratio of prescription of opioid analgesics. The present sample selected for the study was that of n = 100 doctors (men = 50; women = 50) from various hospitals, treating patients with chronic pain, in Rawalpindi and Islamabad. Findings A two-factor structure was suggested by Velicer’s minimum average partial method and maximum likelihood factor analysis, which were labeled as fear of opioid analgesics and justified acceptance of opioids. The developed opiophobia questionnaire along with its subscales displayed appropriate levels of reliability α = 0.733, α = 0.760 and α = 0.725, respectively, suggesting the scale to be reliable. Research limitations/implications Like any other study, this study also tried to address every essential aspect, but still lacked at some places which should be considered and catered for in future studies. In the first place the sample size was very limited which was due to the fact, the study was conducted during a pandemic and physically going for data collection was unavailable, thus leading to consequent sample size. It is recommended a correspondent study can be conducted with larger sample size, so they can get more reliable results with greater precision and power. Then, they will have the advantage of a small margin of error. The second limitation was the study involved only doctors as that was the main focus of the present study. However, other hospital staff such as nurses should also be incorporated to assess their level of opiophobia. The current scale suggests the severity of opiophobia with higher scores though no cutoff point has been suggested. Future studies should try and incorporate a cutoff point to assess the difference between doctors who have conventional levels of reservations against opioids and those suffering from opiophobia. Another limitation was that the present scale did not establish additional validities such as convergent and divergent validity. Future studies should collect data from a larger sample to establish these validities to further refine the scale. Practical implications This instrument can be immensely effective in identifying doctors who have concerns and fears about prescribing opioids to patients with chronic pain. The findings acquired on such a scale can help in developing appropriate academic and psychological interventions which can help such doctors to overcome their opiophobia. This can enable more doctors to prescribe appropriate medicine to their patients instead of letting them suffer from pain. Additionally, researchers can equally benefit from the instrument as it can enable them to investigate opiophobia with other possible variables. Social implications Developing such a scale about the fear faced by doctors while treating patients would be very useful as it is not possible to take such fear when it comes to a patient’s life. This fear is also common among patients where they have a fear about the undesirable effects, addiction of drugs and fear of dying. Better awareness should be given to them which will be helpful for successful and less painful treatment in hospitals. Originality/value This scale is an original work with the aim of accessing opiophobia among doctors toward (chronic) patients with severe pain. There was a lot of research work that has been done on opiophobia in developed countries and few Pakistani researchers have also worked on opiophobia and its impact on pain management but still, no scale has been developed to measure the extent or tendency of opiophobia among doctors or patients. This scale can be used globally on both men and women doctors to access the tendency of opiophobia among them.

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