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Pharmacology, Biochemistry, and Behavior Dec 2021Regular alcohol consumption is on the rise among older adults and has the potential of altering the subjective experience of pain and response to pain medications. This...
BACKGROUND
Regular alcohol consumption is on the rise among older adults and has the potential of altering the subjective experience of pain and response to pain medications. This study examined the cognitive, analgesic and side effect response to oxycodone in middle age and older adults with elevated levels of customary alcohol consumption in a human laboratory setting.
METHODS
After refraining from alcohol for one day, eligible participants underwent baseline assessment cognition and side effects by means of questionnaires that were repeated at three time points (90 min, 5 and 8 h) following administration of a 10 mg oral dose of oxycodone. Response to pain stimulus (Cold Pressor Test (CPT)), pupil size, and plasma oxycodone were also measured.
RESULTS
One hundred twenty-eight adults (age 35-85) completed the study day. Compared to those with lower customary alcohol consumption, participants with elevated alcohol consumption showed attenuated opioid-induced pupil constriction and cognitive decline on objective measures of working memory, sustained attention, inhibitory control, coordination on a simulated driving task, and subjective dysphoric effects with enhanced subjective euphoric effects. Oxycodone pharmacokinetics, pain tolerance to CPT, and Berg balance were impacted comparably between alcohol consumption groups. Women endorsed greater negative drug effects, whereas men endorsed positive drug effects.
CONCLUSION
Independent of subject's age, elevated customary alcohol consumption attenuates opioid central effects (i.e., pupil miosis, impaired cognition) and gender influences subjective drug effects. Clinicians should consider alcohol consumption and gender when prescribing opioid medications.
Topics: Adult; Age Factors; Aged; Aged, 80 and over; Alcohol Drinking; Analgesics, Opioid; Attention; Automobile Driving; Cognition; Ethanol; Female; Humans; Male; Memory, Short-Term; Middle Aged; Miosis; Oxycodone; Pain; Sex Factors; Surveys and Questionnaires
PubMed: 34742948
DOI: 10.1016/j.pbb.2021.173295 -
European Journal of Pharmaceutics and... Oct 2022Opioids are generally used as analgesics in pain treatment. Like many drugs, they have side effects when overdosed and can causeaddiction problems.Illegal drug use and... (Review)
Review
Opioids are generally used as analgesics in pain treatment. Like many drugs, they have side effects when overdosed and can causeaddiction problems.Illegal drug use and misuse are becoming a major concern for authorities worldwide; thus, it is critical to have precise procedures for detecting them in confiscated samples, biological fluids, and wastewaters. Routine blood and urine tests are insufficient for highly selective determinations and can cause cross-reactivities. For this purpose, nanomaterial-based biosensors are great tools to determine opioid intakes, continuously monitoring the drugs with high sensitivity and selectivity even at very low sample volumes.Nanobiosensors generally comprise a signal transducer nanostructure in which a biological recognition molecule is immobilized onto its surface. Lately, nanobiosensors have been extensively utilized for the molecular detection of opioids. The usage of novel nanomaterials in biosensing has impressed researchers who work on developing biosensors. Nanomaterials with a large surface area have been used to develop nanobiosensors with shorter reaction times and higher sensitivity than conventional biosensors. Colorimetric and fluorescence sensing methods are two kinds of optical sensor systems based on nanomaterials. Noble metal nanoparticles (NPs), such as silver and gold, are the most frequently applied nanomaterials in colorimetric techniques, owing to their unique optical feature of surface plasmon resonance. Despite the progress of an extensive spectrum of nanobiosensors over the last two decades, the future purpose of low-cost, high-throughput, multiplexed clinical diagnostic Lab-on-a-Chip instruments has yet to be fulfilled. In this review, a concise overview of opioids (such as tramadol and buprenorphine, oxycodone and fentanyl, methadone and morphine) is provided as well as information on their classification, mechanism of action, routine tests, and new opioid sensing technologies based on various NPs. In order to highlight the trend of nanostructure development in biosensor applications for opioids, recent literature examples with the nanomaterial type, target molecules, and their limits of detection are discussed.
Topics: Analgesics, Opioid; Buprenorphine; Fentanyl; Gold; Illicit Drugs; Methadone; Oxycodone; Silver; Tramadol; Wastewater
PubMed: 36067954
DOI: 10.1016/j.ejpb.2022.08.017 -
Pakistan Journal of Medical Sciences 2023To investigate the effects of morphine hydrochloride sustained-release tablets and oxycodone hydrochloride sustained-release tablets on T-cell levels in advanced lung...
Effects of oxycodone hydrochloride sustained-release tablets and morphine hydrochloride sustained-release tablets on peripheral blood T cell levels in advanced lung squamous cell carcinoma with moderate to severe cancer pain.
OBJECTIVE
To investigate the effects of morphine hydrochloride sustained-release tablets and oxycodone hydrochloride sustained-release tablets on T-cell levels in advanced lung squamous cell carcinoma(LUSC) with moderate to severe cancer pain.
METHODS
A retrospective study was used, ninety-eight patients who were admitted to The First Affiliated Hospital of Hebei North University for treatment of advanced LUSC with moderate to severe cancer pain between January 2021 and December 2021 were randomized into two groups(n=49 each) using the sealed envelope system. The reference group was treated with morphine hydrochloride sustained-release tablets, while the experimental group received oxycodone hydrochloride sustained-release tablets to compare pain relief rates(PRRs), levels of T cells, pain intensity, et al. Blood samples were collected for lymphocyte levels by flow cytometry.
RESULTS
The experimental group had significantly higher level than the reference group(<0.05). Before administration, the two groups did not differ greatly in levels of T-cell subsets or pain scores on the visual analog scale(>0.05, respectively). At 15 days of administration, the Treg level in the experimental group was higher than in the reference group; T helper 17 and 22 cells were reduced in both groups, and the decrease was more pronounced in the experimental group. At seven and 15 days of administration, the experimental group had a VAS score significantly lower than the reference group(<0.05). The total adverse reaction rate was significantly lower in the experimental group as compared with the reference group(<0.05).
CONCLUSIONS
Oxycodone hydrochloride sustained-release tablets demonstrate desirable efficacy and safety in advanced LUSC with moderate to severe cancer pain by modulating T-cells in the body and improving the PRR.
PubMed: 37680811
DOI: 10.12669/pjms.39.5.6772 -
BMC Anesthesiology May 2023Management of acute postoperative pain is one of the major challenges in pediatric patients. Oral oxycodone has shown good pain relief in postoperative pain relief in... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Management of acute postoperative pain is one of the major challenges in pediatric patients. Oral oxycodone has shown good pain relief in postoperative pain relief in children, but no studies have investigated intravenous oxycodone in this context.
OBJECTIVE
whether oxycodone PCIA can provide adequate and safe postoperative pain relief, in comparison to tramadol as reference opioid drug.
DESIGN
a randomized, double-blind, parallel, multi-center clinical trial.
SETTING
five university medical centers and three teaching hospitals in China.
PARTICIPANTS
patients aged 3-month-old to 6-year-old undergoing elective surgery under general anesthesia.
INTERVENTION
patients were randomly allocated to either tramadol (n = 109) or oxycodone (n = 89) as main postoperative opioid analgesic. Tramadol or oxycodone were administered with a loading dose at the end of surgery (1 or 0.1 mg.kg, respectively), then with a parent-controlled intravenous device with fixed bolus doses only (0.5 or 0.05 mg.kg-1, respectively), and a 10-min lockout time.
OUTCOMES
the primary outcome was adequate postoperative pain relief, defined as a face, legs, activity, cry, and consolability (FLACC) score < 4/10 in the post-anesthesia care unit (PACU), with no need for an alternative rescue analgesia. FLACC was measured 10 min after extubation then every 10 min until discharge from PACU. Analgesia was currently conducted with the boluses of either tramadol or oxycodone if FLACC was ≥ 3, up to three bolus doses, after what rescue alternative analgesia was administered.
RESULTS
tramadol and oxycodone provided a similar level of adequate postoperative pain relief in PACU and in the wards. No significant differences were either noted for the raw FLACC scores, the bolus dose demand in PACU, the time between the first bolus dose and discharge from PACU, analgesic drug consumption, bolus times required in the wards, function activity score, or the parents' satisfaction. The main observed side effects in both groups were nausea and vomiting, with no difference between groups. However, patients in the oxycodone group showed less sedation levels and had a shorter stay in the PACU, compared with the tramadol group.
CONCLUSIONS
an adequate postoperative analgesia can be achieved with intravenous oxycodone, this with less side effects than tramadol. It can therefore be a choice for postoperative pain relief in pediatric patients.
TRIAL REGISTRATION
The study was registered at www.chictr.org.cn (Registration number: ChiCTR1800016372; date of first registration: 28/05/2018; updated date:06/01/2023).
Topics: Humans; Child; Infant; Tramadol; Oxycodone; Prospective Studies; Analgesia, Patient-Controlled; Analgesics, Opioid; Pain, Postoperative; Double-Blind Method
PubMed: 37138225
DOI: 10.1186/s12871-023-02054-8 -
Supportive Care in Cancer : Official... Oct 2023Although opioids have been shown to be effective for cancer pain, opioid-induced adverse events (AEs) are common. To date, little is known about the differences in risks...
PURPOSE
Although opioids have been shown to be effective for cancer pain, opioid-induced adverse events (AEs) are common. To date, little is known about the differences in risks of AEs by opioid type. This study was performed to compare the prevalence of AEs across opioids commonly used for analgesic treatment in Japan.
METHODS
This study was conducted as a preplanned secondary analysis of a multicenter prospective longitudinal study of inpatients with cancer pain who received specialized palliative care for cancer pain relief. We assessed daily AEs until termination of follow-up. We rated the severity of AEs based on the Common Terminology Criteria for Adverse Events version 5.0. We computed adjusted odds ratios for each AE (constipation, nausea and vomiting, delirium, and drowsiness) with the following variables: opioid, age, sex, renal dysfunction, and primary cancer site.
RESULTS
In total, 465 patients were analyzed. Based on the descriptive analysis, the top four most commonly used opioids were included in the analysis: oxycodone, hydromorphone, fentanyl, and tramadol. With respect to the prevalence of AEs among all analyzed patients, delirium (n = 25, 6.3%) was the most frequent, followed by drowsiness (n = 21, 5.3%), nausea and vomiting (n = 19, 4.8%), and constipation (n = 28, 4.6%). The multivariate logistic analysis showed that no single opioid was identified as a statistically significant independent predictor of any AE.
CONCLUSION
There was no significant difference in the prevalence of AEs among oxycodone, fentanyl, hydromorphone, and tramadol, which are commonly used for analgesic treatment in Japan.
Topics: Humans; Analgesics, Opioid; Oxycodone; Hydromorphone; Cancer Pain; Tramadol; Prospective Studies; Japan; Prevalence; Longitudinal Studies; Fentanyl; Constipation; Nausea; Vomiting; Delirium
PubMed: 37843639
DOI: 10.1007/s00520-023-08099-2 -
Psychopharmacology Dec 2022Kratom derives from Mitragyna speciosa (Korth.), a tropical tree in the genus Mitragyna (Rubiaceae) that also includes the coffee tree. Kratom leaf powders, tea-like...
RATIONALE
Kratom derives from Mitragyna speciosa (Korth.), a tropical tree in the genus Mitragyna (Rubiaceae) that also includes the coffee tree. Kratom leaf powders, tea-like decoctions, and commercial extracts are taken orally, primarily for health and well-being by millions of people globally. Others take kratom to eliminate opioid use for analgesia and manage opioid withdrawal and use disorder. There is debate over the possible respiratory depressant overdose risk of the primary active alkaloid, mitragynine, a partial μ-opioid receptor agonist, that does not signal through ß-arrestin, the primary opioid respiratory depressant pathway.
OBJECTIVES
Compare the respiratory effects of oral mitragynine to oral oxycodone in rats with the study design previously published by US Food and Drug Administration (FDA) scientists for evaluating the respiratory effects of opioids (Xu et al., Toxicol Rep 7:188-197, 2020).
METHODS
Blood gases, observable signs, and mitragynine pharmacokinetics were assessed for 12 h after 20, 40, 80, 240, and 400 mg/kg oral mitragynine isolate and 6.75, 60, and 150 mg/kg oral oxycodone hydrochloride.
FINDINGS
Oxycodone administration produced significant dose-related respiratory depressant effects and pronounced sedation with one death each at 60 and 150 mg/kg. Mitragynine did not yield significant dose-related respiratory depressant or life-threatening effects. Sedative-like effects, milder than produced by oxycodone, were evident at the highest mitragynine dose. Maximum oxycodone and mitragynine plasma concentrations were dose related.
CONCLUSIONS
Consistent with mitragynine's pharmacology that includes partial µ-opioid receptor agonism with little recruitment of the respiratory depressant activating β-arrestin pathway, mitragynine produced no evidence of respiratory depression at doses many times higher than known to be taken by humans.
Topics: Animals; Rats; Analgesics, Opioid; Mitragyna; Oxycodone; Plant Extracts; Receptors, Opioid; Secologanin Tryptamine Alkaloids
PubMed: 36308562
DOI: 10.1007/s00213-022-06244-z -
Addiction (Abingdon, England) Sep 2021To establish and quantify the association between abuse-deterrent formulation (ADF) oxycodone and 1-year risk of opioid-related harm.
AIM
To establish and quantify the association between abuse-deterrent formulation (ADF) oxycodone and 1-year risk of opioid-related harm.
DESIGN
Propensity score-matched cohort study of electronic medical records for years 2014-18, with patients followed up for 1 year after their index health-care visit.
SETTING
More than 70 million patients from 56 US health-care organizations.
PARTICIPANTS
Patients aged 18-64 years at index health-care visit with any indication for an oral opioid analgesic, with no past 12-month history of oral oxycodone use or substance use disorder, and who were alive at the end of the 1-year follow-up (new episode of prescription oral ADF oxycodone [OxyContin], n = 45 045; new episode of non-ADF oxycodone opioid preparation, n = 1 377 359).
MEASUREMENTS
International Classification of Diseases diagnoses of any opioid-related disorder or non-fatal opioid poisoning within 1 year of the index health-care visit. Pooled odds ratios (OR) with 95% confidence intervals (95% CI).
FINDINGS
After propensity score matching, 89 802 patients with a mean age of 44 [standard deviation (SD) = 11] years (62% women, 68% white) were included. During 1-year follow-up, 1445 diagnoses of opioid use disorder or opioid poisoning occurred in the ADF oxycodone cohort (34.8/1000 person-years) and 765 occurred in the non-ADF oxycodone cohort (18.2/1000 person-years). The odds of opioid-related adverse outcomes were increased in the ADF oxycodone cohort compared with the non-ADF oxycodone opioid cohort, including for opioid use disorders (OR = 2.02; 95% CI = 1.83, 2.23) and opioid poisoning (OR = 1.64 95% CI = 1.35, 1.99).
CONCLUSIONS
Patients with a new prescription of abuse-deterrent formulation oxycodone may be at increased risk of opioid-related harm.
Topics: Analgesics, Opioid; Child; Cohort Studies; Delayed-Action Preparations; Electronic Health Records; Female; Humans; Male; Opioid-Related Disorders; Oxycodone
PubMed: 33394528
DOI: 10.1111/add.15392 -
Frontiers in Pharmacology 2023The Department of Health and Human Services reports that prescription pain reliever (e.g., oxycodone) misuse was initiated by 4,400 Americans each day in 2019. Amid the...
The Department of Health and Human Services reports that prescription pain reliever (e.g., oxycodone) misuse was initiated by 4,400 Americans each day in 2019. Amid the opioid crisis, effective strategies to prevent and treat prescription opioid use disorder (OUD) are pressing. In preclinical models, the orexin system is recruited by drugs of abuse, and blockade of orexin receptors (OX receptors) prevents drug-seeking behavior. The present study sought to determine whether repurposing suvorexant (SUV), a dual OX receptor antagonist marketed for the treatment of insomnia, can treat two features of prescription OUD: exaggerated consumption and relapse. Male and female Wistar rats were trained to self-administer oxycodone (0.15 mg/kg, i. v., 8 h/day) in the presence of a contextual/discriminative stimulus (S) and the ability of SUV (0-20 mg/kg, p. o.) to decrease oxycodone self-administration was tested. After self-administration testing, the rats underwent extinction training, after which we tested the ability of SUV (0 and 20 mg/kg, p. o.) to prevent reinstatement of oxycodone seeking elicited by the S. The rats acquired oxycodone self-administration and intake was correlated with the signs of physical opioid withdrawal. Additionally, females self-administered approximately twice as much oxycodone as males. Although SUV had no overall effect on oxycodone self-administration, scrutiny of the 8-h time-course revealed that 20 mg/kg SUV decreased oxycodone self-administration during the first hour in males and females. The oxycodone S elicited strong reinstatement of oxycodone-seeking behavior that was significantly more robust in females. Suvorexant blocked oxycodone seeking in males and reduced it in females. These results support the targeting of OX receptors for the treatment for prescription OUD and repurposing SUV as pharmacotherapy for OUD.
PubMed: 37180716
DOI: 10.3389/fphar.2023.1127735 -
Pharmacology Research & Perspectives Feb 2022Tapentadol is a centrally acting analgesic with a dual mechanism of action. It acts as an agonist at the µ receptor and inhibitor of noradrenaline reuptake. Clinical... (Comparative Study)
Comparative Study
Tapentadol is a centrally acting analgesic with a dual mechanism of action. It acts as an agonist at the µ receptor and inhibitor of noradrenaline reuptake. Clinical trials suggest similar analgesic efficacy of tapentadol, oxycodone, and morphine in acute and chronic pain. Given the limited information about the molecular actions of tapentadol at the µ receptor, we investigated the intrinsic efficacy of tapentadol and compared it with other opioids. β-chlornaltrexamine (β-CNA, 100 nM, 20 min) was used to deplete spare receptors in AtT20 cells stably transfected with human µ receptor wild-type (WT). Opioid-mediated changes in membrane potential were measured in real-time using a membrane potential-sensitive fluorescent dye. Using Black and Leff's operational model, intrinsic efficacy relative to DAMGO was calculated for each opioid. Tapentadol (0.05 ± 0.01) activated the GIRK channel with lesser intrinsic efficacy than morphine (0.17 ± 0.02) and oxycodone (0.16 ± 0.02). We further assessed the signaling of tapentadol in the common µ receptor variants (N40D and A6V) which are associated with altered receptor signaling. We found no difference in the response of tapentadol between these receptor variants.
Topics: Analgesics, Opioid; Animals; Cell Line, Tumor; Humans; Mice; Morphine; Oxycodone; Receptors, Opioid, mu; Tapentadol
PubMed: 35084120
DOI: 10.1002/prp2.921 -
The American Journal of Hospice &... Oct 2022Opioids are known to induce delirium, but few studies have closely investigated differences in incidence of delirium among different opioids.
BACKGROUND
Opioids are known to induce delirium, but few studies have closely investigated differences in incidence of delirium among different opioids.
OBJECTIVES
To determine whether there is a clinically significant difference in the incidence of delirium between oral opioids in previously opioid-naive patients.
METHODS
Subjects were 259 opioid-naive in-patients with cancer who were started on morphine sulfate, oxycodone hydrochloride, or tapentadol hydrochloride extended-release tablets at our hospital between August 1, 2014, and September 30, 2018. The incidence of delirium during the first week of treatment was compared between the drugs.
RESULTS
The incidence of delirium was 4.8% (n = 83) for morphine sulfate, 6.9% (n = 131) for oxycodone hydrochloride, and 6.7% (n = 45) for tapentadol hydrochloride. The incidence did not significantly differ between oxycodone hydrochloride (OR = .69, 95% CI = .20-2.30, [Fisher's exact test] = .77) or tapentadol hydrochloride (OR = .71, 95% CI = .15-3.32, [Fisher's exact test] = .70) and morphine sulfate (reference group). Moreover, the incidence did not significantly differ between tapentadol hydrochloride (OR = 1.03, 95% CI = .27-3.00, [Fisher's exact test] = 1.00) and oxycodone hydrochloride (reference group).
CONCLUSION
The incidence of delirium in previously opioid-naive patients did not differ significantly among morphine sulfate, oxycodone hydrochloride, and tapentadol hydrochloride extended-release tablets, suggesting similar risk of delirium in opioid-naive patients among these oral opioids.
Topics: Analgesics, Opioid; Delirium; Humans; Incidence; Morphine; Oxycodone; Tapentadol
PubMed: 35045754
DOI: 10.1177/10499091211065171