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Dihydroetorphine: a potent analgesic: pharmacology, toxicology, pharmacokinetics, and clinical effects.

Dihydroetorphine (DHE) is one of the strongest analgesic opioid alkaloids known; it is 1000 to 12000 times more potent than morphine. Several in vitro and in vivo studies have shown that DHE is a selective mu-opioid receptor (OP(3)) agonist that also binds and activates all human recombinant mu-, delta-, and kappa-opioid receptors (OP(3), OP(1), and OP(2)). The onset of the analgesic effect of DHE in rodents is rapid, 5 to 15 min after parenteral administration; the duration of action is short, the analgesic effect disappears within 120 min after administration. By oral administration much hig

Strong opioids and non-cancer chronic pain in Catalonia. An analysis of the family physicians prescription patterns.

OBJECTIVE: To identify family doctor prescription patterns for strong opioids for chronic, non-cancer-related pain. MATERIALS AND METHODS: Design A descriptive study based on a self-administered email questionnaire. LOCATION: All primary health care centres in Catalonia. PARTICIPANTS: 3,602 family doctors, all members of the Catalan Society of Family and Community Medicine. INTERVENTIONS: Email survey of Catalan family doctors. MAIN MEASUREMENTS: Demographic data, number of patients treated with potent opioids for chronic non-cancer pain, type of opioid used and indications, prescribing p

Absorption, distribution, metabolism, and excretion of radiolabeled naldemedine in healthy subjects.

1. Naldemedine is a peripherally acting μ-opioid receptor antagonist for the treatment of opioid-induced constipation. 2. This phase 1 study investigated the absorption, distribution, metabolism and excretion of naldemedine, following a single oral 2-mg dose of [oxadiazole-14C]-naldemedine or [carbonyl-14C]-naldemedine to 12 healthy adult male subjects. Pharmacokinetic assessments were performed on blood, urine and fecal samples collected at defined intervals. 3. Naldemedine was the major circulating component in plasma with a median Tmax of approximately 0.8-0.9 h and a geometric mean t1/2,z …

Cancer Pain Management and Bone Metastases: An Update for the Clinician.

Breast cancer patients with bone metastases often suffer from cancer pain. In general, cancer pain treatment is far from being optimal for many patients. To date, morphine remains the gold standard as first-line therapy, but other pure μ agonists such as hydromorphone, fentanyl, or oxycodone can be considered. Transdermal opioids are an important option if the oral route is impossible. Due to its complex pharmacology, methadone should be restricted to patients with difficult pain syndromes. The availability of a fixed combination of oxycodone and naloxone is a promising development for the red

A Practical Narrative Review on the Role of Magnesium in Cancer Therapy.

Magnesium (Mg2+) has gained oncologists' attention due to its wide range of biological functions and frequent use as a complementary or inte … iency is associated with drug or chemotherapy-related hypomagnesemia, postoperative pain, cachexia, opioid-induced constipation, normal tissue protection from radiation damage, and prevention of nephrotoxicity. A balanced diet usually provides sufficient Mg2+, but supplementation may be necessary in some clinical settings.

Safety of enteral naloxone for the reversal of opiate-induced constipation in the intensive care unit.

BACKGROUND: Opiates are the mainstay of analgesia in the intensive care unit (ICU). Unfortunately, constipation is a common adverse effect associated with opioid use. Naloxone is a pure opiate antagonist that is frequently utilized in practice for the prophylaxis or treatment of opiate-induced constipation in the ICU. Despite extensive first pass metabolism in the liver there remains the potential for opiate reversal after oral administration. We sought to assess the safety of enteral naloxone in the ICU for the treatment of opiate-induced constipation. METHODS: Patients who were ordered ente

Bowel dysfunction after elective spinal surgery: etiology, diagnostics and management based on the medical literature and experience in a university hospital.

BACKGROUND: Bowel dysfunction after spinal surgery is often underestimated and if not treated in a timely manner can lead to undesirable sur … d bowel dysfunction, obstruction, postoperative ileus, spinal surgery, spinal fusion, constipation, opioid-induced constipation, colonic pseudo-obstruction, ischemic colitis, immobility-induced bowel changes, epidural anesthesia and diet. Relevant studies were chosen and included in the review. The treatment approach used in the spine center of a university hospital was incl …

Opioid-free anesthesia for patients with joint hypermobility syndrome undergoing craneo-cervical fixation: a case-series study focused on anti-hyperalgesic approach.

BACKGROUND: Patients with Ehlers-Danlos Syndrome/Hypermobility Type (EDS-HT/JHS) and Craneo-Cervical Instability frequently suffer from severe widespread pain which is difficult to control. Chronic neuroinflammation, opioid-induced hyperalgesia, and central sensitization may explain this painful condition. The aim of this study was to determine if opioid-free anesthesia plus the postoperative administration of lidocaine, ketamine and dexmedetomidine can reduce postoperative pain and the need of methadone rescues in comparison with opioid-based management in these patients undergoing Craneo-Cer

Anti-diarrheal drug loperamide induces dysbiosis in zebrafish microbiota via bacterial inhibition.

BACKGROUND: Perturbations of animal-associated microbiomes from chemical stress can affect host physiology and health. While dysbiosis induced by antibiotic treatments and disease is well known, chemical, nonantibiotic drugs have recently been shown to induce changes in microbiome composition, warranting further exploration. Loperamide is an opioid-receptor agonist widely prescribed for treating acute diarrhea in humans. Loperamide is also used as a tool to study the impact of bowel dysfunction in animal models by inducing constipation, but its effect on host-associated microbiota is poorly ch

Virtual reality as a non-pharmacologic analgesic for fasciotomy wound infections in acute compartment syndrome: a case report.

BACKGROUND: Fasciotomy is a life-saving procedure to treat acute compartment syndrome, a surgical emergency. As fasciotomy dramatically improves wound pain, it should be performed as soon as possible. Moreover, delays in the use of fasciotomy can increase the rate of wound infections. Once the fasciotomy wound is infected, pain control is achieved via the long-term use of opioids or anti-inflammatory analgesics. However, the administration of high doses of opioids may cause complications, such as respiratory depression, over-sedation, and constipation. Therefore, treatment methods other than n

Methadone associated long term hearing loss and nephrotoxicity; a case report and literature review.

BACKGROUND: Methadone is a long-acting opioid receptor agonist. Reported adverse effects of methadone include constipation, respiratory depression, dizziness, nausea, vomiting, itching, sweating, rhabdomyolysis, QT prolongation, and orthostatic hypotension. Hearing loss has been rarely reported following methadone use, and when reported, long term follow-up is rare. Herein we report a case of methadone poisoning with rhabdomyolysis, acute kidney injury, and persistent hearing loss documented by a 2 year follow up. CASE PRESENTATION: The patient was a 34 years old male who presented with a red

Impacts of genetic polymorphisms and cancer cachexia on naldemedine pharmacokinetics and bowel movements in patients receiving opioid analgesics.

BACKGROUND/OBJECTIVES: Clinical responses to naldemedine vary between individuals with advanced cancer. This is a prospective, single-center, observational study aimed to evaluate the influence of genetic polymorphisms and cachexia status on plasma naldemedine and clinical responses. METHODS: Forty-eight patients being treated with naldemedine for opioid-induced constipation under treatment of cancer pain were enrolled. Plasma naldemedine concentrations were determined on the fourth day or later after administration of naldemedine, and the associations with genotypes, cachexia status, and cli…

Response Rates to Methylnaltrexone in Hospitalized Cancer Patients.

Context: Methylnaltrexone is a peripherally-acting mu-opioid receptor antagonist studied in both cancer and non-cancer patients with opioid-induced constipation (OIC), but mostly in the outpatient setting. For adult hospitalized cancer patients with OIC, its effectiveness is unknown. Objectives: Describe the efficacy of methylnaltrexone for OIC in the inpatient setting, defined as bowel movement (BM) within 24 hours of methylnaltrexone administration. Methods: We performed a single-center, retrospective chart review of all hospitalized, adult patients with a cancer diagnosis who received methy…

Improved brain penetration of neurotensin(8-13) via blood-brain barrier shuttle conjugation underlies strong analgesia.

The development of non-opioid analgesics remains a major therapeutic priority. Although peptide-based drugs offer high target specificity, their clinical utility for brain disorders is limited by poor blood-brain barrier (BBB) permeability. The neurotensin (NT) peptide elicits potent antinociception via activation of the seven-transmembrane receptors NTS1 and NTS2; however, its therapeutic potential is constrained by rapid metabolic degradation and inadequate brain penetration. Here, we report the functional characterization of An2-NT(8-13), a conjugate linking the minimal active NT fragment t

Global Prevalence, Characterization, and Impact of Functional Bowel Disorders.

INTRODUCTION: Functional bowel disorders (FBDs) are common and have a profound impact on many aspects of life. However, little is known abou … symptoms, reduced quality of life, and increased healthcare utilization, most pronounced in IBS and opioid-induced constipation. Findings were similar across world regions and countries. The major contributor to lower Rome IV, vs Rome III, IBS prevalence (4.1% vs 10.1%) was the change in symptom frequency threshold for abdominal pain and/or discomfort. Minor alterations in I …

Tracking gastrointestinal transit of solids in aged rats as pharmacological models of chronic dysmotility.

BACKGROUND: Dysmotility in the gastrointestinal (GI) tract often leads to impaired transit of luminal contents leading to symptoms of diarrhea or constipation. The aim of this research was to develop a technique using high resolution X-ray imaging to study pharmacologically induced aged rat models of chronic GI dysmotility that mimic accelerated transit (diarrhea) or constipation. The 5-hydroxytryptamine type 4 (5-HT4 ) receptor agonist prucalopride was used to accelerate transit, and the opioid agonist loperamide was used to delay transit. METHODS: Male rats (18 months) were given 0, 1, 2, o

Application of trigger tools for detecting adverse drug events in older people: A systematic review and meta-analysis.

OBJECTIVE: To identify trigger tools applied to detect adverse drug events (ADEs) in older people and describe their utility and performance. METHODS: A systematic review was conducted in the PubMed, Lilacs, and Scopus databases (January 2024). Studies that developed, applied, or validated trigger tools and evaluated their utility and/or performance for detecting ADEs in older people were considered. Direct proportion meta-analyses using the inverse-variance method were performed for prevalence of ADEs and positive predictive value (PPV). RESULTS: Twenty-four studies (25 publications) were i

Research progress on the regulation of interstitial cell of Cajal autophagy and apoptosis crosstalk by traditional Chinese medicine in gastrointestinal motility disorders.

ETHNOPHARMACOLOGICAL RELEVANCE: Gastrointestinal motility disorders (GMD) severely impact quality of life, with rising global prevalence lin … oesophageal reflux disease (GERD), irritable bowel syndrome (IBS), functional constipation (FC) and opioid-induced constipation (OIC). Additionally, explore the underlying mechanisms involving autophagy, apoptosis, molecular crosstalk, and ICC dynamics. Investigate the potential therapeutic effects of herbal medicine, TCM compounds, bioactive phytocompounds, and external TCM …

Efficacy and Safety of Acupuncture Combined with Conventional Drug Therapy for the Treatment of Cancer-Induced Bone Pain: A Network Meta-Analysis of Randomized Controlled Trials.

BACKGROUND: Cancer-induced bone pain (CIBP) involves both nociceptive and neuropathic components, causing significant suffering in cancer patients. Acupuncture has shown beneficial effects on CIBP. However, given the diverse acupuncture techniques, their therapeutic efficacy may vary. OBJECTIVE: To evaluate the efficacy and safety of various acupuncture modalities integrated with conventional drug therapy for CIBP. METHODS: Randomized controlled trials (RCTs) of acupuncture combined with conventional analgesics for CIBP were searched across eight Chinese and English databases and clinical tr

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… Secondary outcomes included the incidence of opioid-induced constipation and nausea/vomiting. Each RCT should have a sample size per group of 20 or greater. Literature published from database inception to September 30, 2020, in Chinese or English. … Effects of electroacupuncture for opioid-induced constipation in patients with cancer in China: a randomized clinical trial. JAMA Network Open . 2023;6(2). doi: 10.1001/jamanetworkopen.2023.0310 14. Shen Y, Liu L, Chiang JS, et al. …

Agonist that activates the µ-opioid receptor in acidified microenvironments inhibits colitis pain without side effects.

OBJECTIVE: The effectiveness of µ-opioid receptor (MOPr) agonists for treatment of visceral pain is compromised by constipation, respiratory depression, sedation and addiction. We investigated whether a fentanyl analogue, (±)-N-(3-fluoro-1-phenethylpiperidine-4-yl)-N-phenyl propionamide (NFEPP), which preferentially activates MOPr in acidified diseased tissues, would inhibit pain in a preclinical model of inflammatory bowel disease (IBD) without side effects in healthy tissues. DESIGN: Antinociceptive actions of NFEPP and fentanyl were compared in control mice and mice with dextran sodium sul