Articles: opioid.
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Neuroscience letters · Mar 2014
Opioid and noradrenergic contributions of tapentadol in experimental neuropathic pain.
Tapentadol is a dual action molecule with mu opioid agonist and norepinephrine (NE) reuptake blocking activity that has recently been introduced for the treatment of moderate to severe pain. The effects of intraperitoneal (i.p.) morphine (10mg/kg), tapentadol (10 or 30 mg/kg) or duloxetine (30 mg/kg), a norepinephrine/serotonin (NE/5HT) reuptake inhibitor, were evaluated in male, Sprague-Dawley rats with spinal nerve ligation (SNL) or sham surgery. Additionally, the effects of these drugs on spinal cerebrospinal fluid (CSF) NE levels were quantified. ⋯ This could be detected 30 min following tapentadol (30 mg/kg) in both sham and SNL groups. Surprisingly, while the dose of morphine studied reversed tactile hypersensitivity in nerve-injured rats, CSF NE levels were significantly reduced in both sham- and SNL rats. The data suggest that tapentadol elicits enhanced elevation in spinal NE levels in a model of experimental neuropathic pain offering a mechanistic correlate to observed clinical efficacy in this pain state.
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Randomized Controlled Trial
First clinical experience with TRV130: pharmacokinetics and pharmacodynamics in healthy volunteers.
TRV130 is a G protein-biased ligand at the µ-opioid receptor. In preclinical studies it was potently analgesic while causing less respiratory depression and gastrointestinal dysfunction than morphine, suggesting unique benefits in acute pain management. A first-in-human study was conducted with ascending doses of TRV130 to explore its tolerability, pharmacokinetics, and pharmacodynamics in healthy volunteers. ⋯ Marked pupil constriction was noted at 2.2, 4, and 7 mg doses. Nausea and vomiting observed at the 7 mg dose limited further dose escalation. These findings suggest that TRV130 may have a broad margin between doses causing µ-opioid receptor-mediated pharmacology and doses causing µ-opioid receptor-mediated intolerance.
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Moderate-to-severe postoperative pain is usually controlled using a multimodal approach, including opioids. Intravenously administered patient-controlled analgesia (IV PCA) with opioids, popular for over 40 years, enables patients to control their level of analgesia and has advantages over a nurse-administered approach, including more satisfied patients and improved pain relief. ⋯ Complicating IV PCA is the problem of commonly used compounds, morphine and hydromorphone, having significantly reduced brain/effector-site permeability and active metabolites, both of which create the risk of delayed adverse events. Novel patient-controlled modalities that incorporate rapid effector site-permeating opioids and non-invasive routes of administration offer great promise to enhance both patient and caregiver experiences with postoperative analgesia systems.
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Korean J Anesthesiol · Mar 2014
Antiemetic effect of propofol administered at the end of surgery in laparoscopic assisted vaginal hysterectomy.
Postoperative nausea and vomiting (PONV) commonly occur after general anesthesia, especially in women. In this study, we evaluated the antiemetic efficacy of propofol administered at the end of surgery in highly susceptible patients undergoing a laparoscopy-assisted vaginal hysterectomy. ⋯ The results of this study suggest that low-dose propofol administration at the end of surgery may effectively reduce the incidence of PONV within 2 hours postoperatively in highly susceptible women undergoing a laparoscopiy-assisted vaginal hysterectomy and receiving opioid-based PCA.
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Best Pract Res Clin Anaesthesiol · Mar 2014
Perioperative analgesia: ever-changing technology and pharmacology.
Our understanding of pain and its long-term implications have dramatically changed with the advent of advancements in molecular mechanisms involved in acute or postoperative pain and chronic pain. This better understanding has led to multiple pharmacologic advancements to better treat pain with minimal side effects. Currently, we are still struggling to find the right balance between all of the different modalities that we have at our leisure. ⋯ However, despite using a multimodal approach that includes newer technologies, we still have a long way to go before we can guarantee a pain-free postoperative course or a comfortable end for a terminally ill patient. These arms of anesthesiology are ever changing. Anesthesiologists have taken a leadership role in perioperative pain management and clinical research designed for the improvement of pain.