Article
Multidisciplinary Sciences
Md Tariqul Haque Tuhin, Dengpan Liang, Fang Liu, Hala Aldawod, Toufiq Ul Amin, Joshua S. Ho, Rasha Emara, Arjun D. Patel, Melanie A. Felmlee, Miki S. Park, James A. Uchizono, Mamoun M. Alhamadsheh
Summary: The study develops a drug delivery approach to limit the passage of small molecules across the blood-brain barrier, and also develops new potent analgesics that have a significant impact on the central nervous system.
NATURE COMMUNICATIONS
(2022)
Article
Clinical Neurology
Eric D. Shah, Bruce H. Chamberlain, Michelle Rhiner, Neil E. Slatkin, Nancy Stambler, Robert J. Israel
Summary: This study evaluated the efficacy and safety of subcutaneous methylnaltrexone for opioid-induced constipation in patients with and without active cancer. The results showed that a significantly higher proportion of patients treated with methylnaltrexone achieved a laxation response within 4 hours compared to placebo. The drug was well-tolerated and did not cause significant differences in pain scores. Therefore, subcutaneous methylnaltrexone is an effective and safe treatment for opioid-induced constipation.
JOURNAL OF PAIN RESEARCH
(2023)
Article
Clinical Neurology
Bruce H. Chamberlain, Michelle Rhiner, Neal E. Slatkin, Nancy Stambler, Robert J. Israel
Summary: Methylnaltrexone effectively reduces constipation time in advanced illness patients, regardless of active cancer status, while preserving pain control with opioid treatment.
JOURNAL OF PAIN RESEARCH
(2021)
Article
Obstetrics & Gynecology
Gary Peltz, Lauren M. Jansson, Susan Adeniyi-Jones, Carol Cohane, David Drover, Steven Shafer, Meiyue Wang, Manhong Wu, Balaji Govindaswami, Priya Jegatheesan, Cynthia Argani, Salwa Khan, Walter K. Kraft
Summary: Ondansetron treatment reduces the severity of symptoms in neonatal opioid withdrawal syndrome (NOWS) and may indicate a shortened length of stay.
JOURNAL OF PERINATOLOGY
(2023)
Article
Clinical Neurology
Neel Mehta, Neal E. Slatkin, Robert J. Israel, Nancy Stambler, Eric D. Shah
Summary: This study evaluated the safety and efficacy of methylnaltrexone in constipated patients and found that methylnaltrexone significantly improved rescue-free laxation. Abdominal pain was more common in patients receiving methylnaltrexone.
JOURNAL OF PAIN RESEARCH
(2023)
Review
Clinical Neurology
Ying-Ying Zhang, Rong Zhou, Wan-Jie Gu
Summary: The meta-analysis results indicate that methylnaltrexone is effective and safe in alleviating opioid-induced constipation, but caution should be taken regarding the safety of abdominal pain.
Article
Chemistry, Medicinal
Boshi Huang, Mengchu Li, Pornprom Klongkumnuankarn, Rolando E. Mendez, James C. Gillespie, David L. Stevens, William L. Dewey, Dana E. Selley, Yan Zhang
Summary: Opioid-induced constipation (OIC) is a common side effect of opioid analgesics. Peripherally acting mu opioid receptor antagonists (PAMORAs) can effectively treat OIC without affecting the analgesic effects. A new compound has shown promising results in improving intestinal motility and may be developed as an oral treatment for constipation.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Ehsan A. Habeeb, Lena K. Tran, Melanie Z. Goodberlet, Kenneth E. Lupi, Jeremy R. DeGrado, Kevin M. Dube
Summary: This study aimed to evaluate the efficacy of enteral naloxone (NLX) versus subcutaneous methylnaltrexone (MNTX) for opioid-induced constipation (OIC) in critically ill patients. The results showed that NLX had a shorter time to first bowel movement compared to MNTX. Both NLX and MNTX were effective in treating OIC without causing reversal of analgesia. Future controlled trials are needed to further validate these findings.
ANNALS OF PHARMACOTHERAPY
(2023)
Review
Gastroenterology & Hepatology
Karim Chamie, Vishnukamal Golla, Andrew T. Lenis, Patrick M. Lec, Siamak Rahman, Eugene R. Viscusi
Summary: PAMORAs, as peripherally acting mu-opioid receptor antagonists, have the potential to alleviate postoperative ileus and opioid-induced constipation by blocking peripheral effects of opioids in the gastrointestinal tract while maintaining their analgesic properties in the central nervous system. Further research is needed to explore the therapeutic potential of PAMORAs in the management of POI and postoperative OIC.
JOURNAL OF GASTROINTESTINAL SURGERY
(2021)
Article
Veterinary Sciences
Sarah Jepkes, Marie Josee-Lemoy, Heather Knych, Thiago de Lucena, Amir Ardeshir, Diane E. Stockinger
Summary: Opioids are commonly used in pain management for nonhuman primates, but they can cause adverse gastrointestinal effects. MNTX, a peripherally acting opioid receptor antagonist, can alleviate these GI effects without affecting central analgesia. We evaluated the pharmacokinetics of MNTX in serum and CSF of rhesus macaques and found that subcutaneous administration of MNTX can effectively block peripheral adverse effects of opioids while maintaining their central analgesic effects.
JOURNAL OF THE AMERICAN ASSOCIATION FOR LABORATORY ANIMAL SCIENCE
(2023)
Article
Medicine, Research & Experimental
W. Frank Peacock, Neal Slatkin, Patrick Gagnon-Sanschagrin, Jessica Maitland, Annie Guerin, George Joseph
Summary: Patients receiving OIC-Rx in the ED had decreased odds of hospitalization and fewer re-encounters in the 30-day post-discharge period, resulting in cost savings for insurance agencies and healthcare providers.
ADVANCES IN THERAPY
(2022)
Article
Neurosciences
Kim Juhani Blomqvist, Katarzyna Anna Dudek, Hanna Viisanen, Kert Matlik, Fredrik Harry Gustav Ahlstrom, Jouko Laitila, Eija Anneli Kalso, Pekka Veli Rauhala, Tuomas Olavi Lilius
Summary: Opioids are effective in managing severe pain, however, tolerance and adverse effects limit their use. The role of peripheral opioid receptors in analgesia and tolerance is still unclear. This study suggests that peripherally restricted opioid receptor antagonist, methylnaltrexone, may not prevent morphine tolerance and morphine tolerance is mediated by central opioid receptors in rats.
JOURNAL OF NEUROSCIENCE RESEARCH
(2022)
Article
Geriatrics & Gerontology
Solomon S. Liao, Neal E. Slatkin, Nancy Stambler
Summary: The study found that methylnaltrexone did not compromise opioid analgesia in older adults and was effective in relieving constipation with minimal side effects, regardless of age. Further research is needed to explore the impact of other factors on the safety and efficacy of methylnaltrexone.
Article
Biochemistry & Molecular Biology
Agata Szymaszkiewicz, Marcin Talar, Jakub Wlodarczyk, Mikolaj Swierczynski, Adrian Bartoszek, Julia Krajewska, Anna Mokrowiecka, Ewa Malecka-Wojciesko, Jakub Fichna, Marta Zielinska
Summary: Nearly 20% of elderly patients suffer from constipation, but the age-related changes in the gastrointestinal (GI) tract remain insufficiently elucidated. This study evaluated the alterations within the endogenous opioid system (EOS) as a potential cause of constipation in the elderly. The results showed that the age-related impairment of GI peristalsis may result from reduced MOP and DOP response to opioid agonists or alterations in EOS expression.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Medicinal
Ying-Ting Hsu, Shen-Ren Chen, Yung-Chiao Chang, Hsiao-Fu Chang, Teng-Kuang Yeh, Jian-Ying Chuang, Horace H. Loh, Hsing-Pang Hsieh, Shau-Hua Ueng, Shiu-Hwa Yeh
Summary: The demand for a non-addictive analgesic medication is increasing due to clinical misuse. Compound 14 is a dual agonist of the mu opioid receptor (MOR) and nociceptin-orphanin FQ opioid peptide (NOP) receptor, providing pain relief at very small doses and reducing unwanted side effects. Evaluating its effects in wild type and humanized mice can help develop a safer prescription analgesic drug.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)