- Opioid utilization in minimally invasive versus open inguinal hernia repair. [Journal Article]
- SSurgery 2019 Jun 19
- CONCLUSIONS: Postdischarge opioid utilization was clinically similar between patients undergoing open and minimally invasive surgery inguinal hernia repair and those requiring unilateral or bilateral repair. Given that more than one-third of patients required no opioids after discharge, 0 to 8 tablets of 5 mg oxycodone is sufficient for most opioid-naive patients undergoing inguinal hernia repair.
- Non-dopaminergic vs. dopaminergic treatment options in restless legs syndrome. [Journal Article]
- APAdv Pharmacol 2019; 84:187-205
- Two types of drugs have been extensively investigated for the treatment of restless legs syndrome (RLS)/Willis-Ekbom disease (WED): dopamine agonists and α2δ ligands to the α2δ subunit of calcium cha…
Two types of drugs have been extensively investigated for the treatment of restless legs syndrome (RLS)/Willis-Ekbom disease (WED): dopamine agonists and α2δ ligands to the α2δ subunit of calcium channels. Comparative studies show that both classes of drugs are similarly effective in treating RLS symptoms over the short- and long-term. While dopamine agonists are more effective in treating periodic limb movements (PLMs), α2δ ligands are more effective in consolidating sleep. However, given the fact that dopamine agonists cause high rates of augmentation of symptoms, recent international guidelines recommend that whenever possible the initial treatment of choice should be an α2δ ligand. In fact, the most effective preventive strategy involves not using dopaminergic agents unless absolutely necessary. Indeed, should dopaminergic treatment be needed to handle the symptoms effectively, then it is recommended that the dopaminergic load be reduced by using the lowest effective dose for the shortest possible period of time. However, it must be taken into account that the only α2δ ligand approved for RLS/WED is gabapentin enacarbil, which is not yet available in Europe. Furthermore, recent studies have also reported on the efficacy of opioids as a second-line treatment of RLS/WED, following treatment failure with dopamine agonists. Recent guidelines have taken these new data into account and highlight that a low dose of an opioid (prolonged-release oxycodone or methadone) may be considered in patients with very severe augmentation of symptoms. Alternative non-dopaminergic treatment concepts based on glutamatergic and adenosinergic mechanisms are currently in development, and are likely to provide encouraging therapeutic alternatives.
- Oxycodone concentrations in the central nervous system and cerebrospinal fluid after epidural administration to the pregnant ewe. [Journal Article]
- BCBasic Clin Pharmacol Toxicol 2019 Jun 21
- The main sites of the analgesic action of oxycodone are the brain and spinal cord. The present study describes the concentrations of oxycodone and its metabolites in the brain and spinal cord after e…
The main sites of the analgesic action of oxycodone are the brain and spinal cord. The present study describes the concentrations of oxycodone and its metabolites in the brain and spinal cord after epidural administration to the ewe. Twenty pregnant ewes undergoing laparotomy were randomised into two groups to receive epidural oxycodone; infusion group (n=10, 0.1 mg·kg-1 bolus followed by continuous infusion of 0.05 mg·kg-1 ·h-1 for five days) or repeated boluses group (n=10, 0.2+ 2x0.1 mg·kg-1 bolus followed by a 0.2 mg·kg-1 bolus every 12 hours for five days). After five days of oxycodone administration, arterial blood samples were collected, the sheep were euthanized, and a CSF sample and tissue samples from the cortex, thalamus, cerebellum and spinal cord were obtained for the quantification of oxycodone and its main metabolites. The median plasma and CSF concentration of oxycodone were 9.0 and 14.2 ng·mL-1 after infusion and 0.4 and 1.1 ng·mL-1 after repeated boluses. In the infusion group, the cortex, thalamus and cerebellum oxycodone concentration were 4-8-fold higher and in the spinal cord 1310-fold higher than in plasma. In the repeated boluses group, brain tissue concentrations were similar in the three areas, and in the spinal cord were 720-fold higher than in plasma. Oxymorphone was the main metabolite detected, which accumulated in the brain and spinal cord tissue. In conclusion, first, accumulation of oxycodone and oxymorphone in the CNS was observed, and second, high spinal cord concentrations suggest that epidural oxycodone may provide segmental analgesia. This article is protected by copyright. All rights reserved.
- Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors. [Journal Article]
- EJEur J Med Chem 2019 May 21; 178:571-588
- In order to obtain novel pharmacological tools and to investigate a multitargeting analgesic strategy, the CB1 and CB2 cannabinoid receptor agonist JWH-018 was conjugated with the opiate analgesic ox…
In order to obtain novel pharmacological tools and to investigate a multitargeting analgesic strategy, the CB1 and CB2 cannabinoid receptor agonist JWH-018 was conjugated with the opiate analgesic oxycodone or with an enkephalin related tetrapeptide. The opioid and cannabinoid pharmacophores were coupled via spacers of different length and chemical structure. In vitro radioligand binding experiments confirmed that the resulting bivalent compounds bound both to the opioid and to the cannabinoid receptors with moderate to high affinity. The highest affinity bivalent derivatives 11 and 19 exhibited agonist properties in [35S]GTPγS binding assays. These compounds activated MOR and CB (11 mainly CB2, whereas 19 mainly CB1) receptor-mediated signaling, as it was revealed by experiments using receptor specific antagonists. In rats both 11 and 19 exhibited antiallodynic effect similar to the parent drugs in 20 μg dose at spinal level. These results support the strategy of multitargeting G-protein coupled receptors to develop lead compounds with antinociceptive properties.
- Patient-Reported Outcomes After Arthroscopic Shoulder Surgery With Interscalene Brachial Plexus Nerve Block Using Liposomal Bupivacaine: A Prospective Observational Study. [Journal Article]
- STSurg Technol Int 2019 Jun 06; 35
- CONCLUSIONS: Our real-world observational findings suggest that multimodal postsurgical pain control using single-shot, ultrasound-guided ISBPNB with LB and postsurgical acetaminophen provides favorable pain control and limited need for postsurgical opioid rescue for seven days after shoulder surgery.
- Lower oxycodone prescription post caesarean section is associated with decreased inpatient opioid consumption. [Letter]
- IJInt J Obstet Anesth 2019 Apr 16
- Prospective Association of Serum Opioid Levels and Clinical Outcomes in Patients With Cancer Pain Treated With Intrathecal Opioid Therapy. [Journal Article]
- A&AAnesth Analg 2019 Jun 12
- CONCLUSIONS: ITT for cancer pain was associated with a marked reduction in serum opioid concentrations, with the majority of patients having undetectable serum levels. Reducing serum opioid concentrations in cancer patients may have implications with respect to restoring bowel function, improving fatigue, and promoting the integrity of antitumor immune function and warrants further study.
- The Current Practice of Opioid for Cancer Dyspnea: The Result from the Nationwide Survey of Japanese Palliative Care Physicians. [Journal Article]
- JPJ Pain Symptom Manage 2019 Jun 12
- CONCLUSIONS: Among Japanese palliative care physicians, using oxycodone for cancer dyspnea was relatively popular practice, while fentanyl was not. Oxycodone was the most preferred opioid for cancer dyspnea in the setting of renal insufficiency among Japanese palliative care physicians. We should conduct studies to confirm the safety and effectiveness of these opioid practices for cancer dyspnea.
- Multimodal opioid sparing postoperative pain regimen compared to the standard postoperative pain regimen in vaginal pelvic reconstructive surgery: a multicenter randomized controlled trial. [Journal Article]
- AJAm J Obstet Gynecol 2019 Jun 12
- CONCLUSIONS: The ICE-T multimodal pain regimen offers improved pain control the morning after surgery and 96 hours postoperatively compared to the Standard regimen with no differences in patient satisfaction and quality of recovery. ICE-T can significantly limit post-operative inpatient narcotic use and eliminate outpatient narcotic use in patients undergoing vaginal pelvic reconstructive surgery.
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- Cannabinoid modulation of opioid analgesia and subjective drug effects in healthy humans. [Journal Article]
- PPsychopharmacology (Berl) 2019 Jun 15
- CONCLUSIONS: This study indicates that dronabinol did not enhance the analgesic effects of oxycodone and increased abuse- and impairment-related subjective effects. These data suggest that dronabinol may not be an effective or appropriate opioid adjuvant; it could potentially increase opioid dose requirements, while increasing psychoactive opioid effects.