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Valerie Le Rouzic, Ankita Narayan, Amanda Hunkle, Gina F Marrone, Zhigang Lu, Susruta Majumdar, Jin Xu, Ying-Xian Pan, Gavril W Pasternak
BACKGROUND: Levorphanol is a potent analgesic that has been used for decades. Most commonly used for acute and cancer pain, it also is effective against neuropathic pain. The recent appreciation of the importance of functional bias and the uncovering of multiple µ opioid receptor splice variants may help explain the variability of patient responses to different opioid drugs. METHODS: Here, we evaluate levorphanol in a variety of traditional in vitro receptor binding and functional assays...
April 11, 2018: Anesthesia and Analgesia
Amber R Watson, Ali Roberts
BACKGROUND: Levorphanol is a long-acting opioid analgesic that is an optical isomer of dextrorphan, a metabolite of the over-the-counter cough suppressant dextromethorphan. Providers prescribing levorphanol for pain management may need to assess compliance through urine drug testing, as this agent is subject to abuse. Therefore, it is important to differentiate between dextromethorphan and levorphanol ingestion. OBJECTIVES: This article is the first to report urine concentrations of levorphanol/dextrorphan and 3-hydroxymorphinan in human urine and assesses the need for an enantiomeric analysis to distinguish between dextromethorphan and levorphanol ingestion...
March 2018: Pain Physician
Akhila Reddy, Amy Ng, Tarun Mallipeddi, Eduardo Bruera
Neuropathic pain in cancer patients is often difficult to treat, requiring a combination of several different pharmacological therapies. We describe two patients with complex neuropathic pain syndromes in the form of phantom limb pain and Brown-Sequard syndrome who did not respond to conventional treatments but responded dramatically to the addition of levorphanol. Levorphanol is a synthetic strong opioid that is a potent N-methyl-d-aspartate receptor antagonist, mu, kappa, and delta opioid receptor agonist, and reuptake inhibitor of serotonin and norepinephrine...
January 29, 2018: Journal of Palliative Medicine
Charl Els, Tanya D Jackson, Diane Kunyk, Vernon G Lappi, Barend Sonnenberg, Reidar Hagtvedt, Sangita Sharma, Fariba Kolahdooz, Sebastian Straube
BACKGROUND: Chronic pain is common and can be challenging to manage. Despite increased utilisation of opioids, the safety and efficacy of long-term use of these compounds for chronic non-cancer pain (CNCP) remains controversial. This overview of Cochrane Reviews complements the overview entitled 'High-dose opioids for chronic non-cancer pain: an overview of Cochrane Reviews'. OBJECTIVES: To provide an overview of the occurrence and nature of adverse events associated with any opioid agent (any dose, frequency, or route of administration) used on a medium- or long-term basis for the treatment of CNCP in adults...
October 30, 2017: Cochrane Database of Systematic Reviews
Hai-Quyen Tran, Yoon Hee Chung, Eun-Joo Shin, The-Vinh Tran, Ji Hoon Jeong, Choon-Gon Jang, Seung-Yeol Nah, Kiyofumi Yamada, Toshitaka Nabeshima, Hyoung-Chun Kim
Dextromethorphan (DM) is a dextrorotatory isomer of levorphanol, a typical morphine-like opioid. When administered at supra-antitussive doses, DM produces psychotoxic and neurotoxic effects in humans. Although DM abuse has been well-documented, few studies have examined the effects of high-dose DM. The present study aimed to explore the effects of a single high dose of DM on mortality and seizure occurrence. After intraperitoneal administration with a high dose of DM (80mg/kg), Sprague-Dawley rats showed increased seizure occurrence and intensity...
November 1, 2017: Toxicology and Applied Pharmacology
S Nalamachu, J Gudin
No abstract text is available yet for this article.
April 2016: Journal of Pain: Official Journal of the American Pain Society
Jeffrey Gudin, Jeffrey Fudin, Srinivas Nalamachu
Levorphanol is a potent opioid analgesic that was first approved for use in the United States in 1953. Levorphanol is approved for use in moderate to severe pain where an opioid analgesic is appropriate. Levorphanol has a wide range of activities including mu opioid agonism, delta agonism, kappa1 and kappa3 receptor agonism, N-methyl-d-aspartate receptor antagonism and reuptake inhibition of both norepinephrine and serotonin. This multimodal profile might prove effective for pain syndromes that are refractory to other opioid analgesics, such as central and neuropathic pain and opioid-induced hyperalgesia...
January 2016: Postgraduate Medicine
Thien C Pham, Jeffrey Fudin, Robert B Raffa
BACKGROUND: Methadone has been a stalwart pharmacologic option for the management of opioid drug dependence for many years. It substitutes for opioid agonists and possesses certain pharmacokinetic properties that confer characteristics preferable to those of other opioids for this application. Methadone is likewise used as an option for the treatment of pain, particularly chronic pain. It has a spectrum of pharmacodynamic activity, including contributions from non-opioid components, that translates to its specific clinical attributes as an analgesic...
September 2015: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
A Z DePriest, B L Puet, A C Holt, A Roberts, E J Cone
Opioid analgesics are commonly prescribed for acute and chronic pain, but are subject to abuse. Consequently, toxicology testing programs are frequently implemented for both forensic and clinical applications. Understanding opioid metabolism and disposition is essential for assessing risk of toxicity and, in some cases, providing additional information regarding risk of therapeutic failure. Opioids significantly metabolized by the cytochromeP450 (CYP450) enzyme system maybe subjectto drug-drug interactions, including codeine, hydrocodone, oxycodone, fentanyl, meperidine, methadone, buprenorphine, and tramadol...
July 2015: Forensic Science Review
Anna Bertaso, Giacomo Musile, Rossella Gottardo, Catia Seri, Franco Tagliaro
An enantioselective CE-based determination of methorphan and its main metabolites in blood is described. Enantiomeric separations were carried out in 50cm×50μm (ID) uncoated fused silica capillaries, using a background electrolyte composed of 150mM sodium phosphate pH 4.4 added with 5mM 2-(hydroxypropyl)-β-cyclodextrin and methanol 20% (v/v), at a constant voltage of 25kV. Sample injections were performed under field amplified sample stacking conditions. Detection was by recording UV absorbance at the wavelength of 200nm...
September 1, 2015: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Richard Brown, Robert Howard, Bridget Candy, Elizabeth L Sampson
BACKGROUND: Agitation is a common experience for people living with dementia, particularly as day-to-day function and cognition start to decline more. At the present time there are limited pharmacological options for relieving agitation and little is known about the safety and efficacy of opioid drugs in this setting. OBJECTIVES: To determine the clinical efficacy and safety of opioids for agitation in people with dementia. SEARCH METHODS: We searched ALOIS, the Cochrane Dementia and Cognitive Improvement Group Specialized Register, on 13 June 2014 using the terms: narcotic OR opioid OR opium OR morphine OR buprenorphine OR codeine OR dextromoramide OR diphenoxylate OR dipipanone OR dextropropoxyphene OR propoxyphene OR diamorphine OR dihydrocodeine OR alfentanil OR fentanyl OR remifentanil OR meptazinol OR methadone OR nalbuphine OR oxycodone OR papaveretum OR pentazocine OR meperidine OR pethidine OR phenazocine OR hydrocodone OR hydromorphone OR levorphanol OR oxymorphone OR butorphanol OR dezocine OR sufentanil OR ketobemidone...
May 14, 2015: Cochrane Database of Systematic Reviews
Eric Prommer
Levorphanol (levo-3-hydroxy-N-methylmorphinan) is a step 3 opioid first developed in the 1940s as an alternative to morphine. Levorphanol belongs to the morphinan opioid series. Levorphanol has greater potency than morphine and is a potent N-methyl-d aspartate (NMDA) antagonist. Levorphanol interferes with the uptake of norepinephrine and serotonin, which makes it potentially useful for neuropathic pain. Glucuronidation changes Levorphanol to Levorphanol-3-glucuronide with excretion by the kidney. Levorphanol has a long half-life and may accumulate with repeated dosing...
2014: Palliative Care
Katsuhisa Kurogi, Andriy Chepak, Michael T Hanrahan, Ming-Yih Liu, Yoichi Sakakibara, Masahito Suiko, Ming-Cheh Liu
The current study was designed to examine the sulfation of eight opioid drugs, morphine, hydromorphone, oxymorphone, butorphanol, nalbuphine, levorphanol, nalorphine, and naltrexone, in HepG2 human hepatoma cells and human organ samples (lung, liver, kidney, and small intestine) and to identify the human SULT(s) responsible for their sulfation. Analysis of the spent media of HepG2 cells, metabolically labeled with [35S]sulfate in the presence of each of the eight opioid drugs, showed the generation and release of corresponding [35S]sulfated derivatives...
October 1, 2014: European Journal of Pharmaceutical Sciences
Hsin-Yu Wu, Brian T Cunningham
We demonstrate an approach for detection, identification, and kinetic monitoring of drugs flowing within tubing, through the use of a plasmonic nanodome array (PNA) surface. The PNA structures are fabricated using a low-cost nanoreplica molding process upon a flexible plastic substrate that is subsequently integrated with a flow cell that connects in series with ordinary intravenous (IV) drug delivery tubing. To investigate the potential clinical applications for point-of-care detection and real-time monitoring, we perform SERS detection of ten pharmaceutical compounds (hydrocodone, levorphanol, morphine, oxycodone, methadone, phenobarbital, dopamine, diltiazem, promethazine, and mitoxantrone)...
May 21, 2014: Nanoscale
J Brachet, N Six
1 In vivo treatment with RNase considerably increases (80%) the RNA content of anucleate and nucleate fragments as well as of whole algae (Acetabularia mediterranea). A parallel increase in the incorporation of phenylalanine into proteins is observed. 2 Prolonged actinomycin (30 \gmg/ml) treatment (7\2-15 days) results in a decrease in the amount of RNA in whole algae and in anucleate apical fragments. This is not, however, the case for the basal anucleate fragments of the stalk. The fact that RNA synthesis in this region resists such treatment with actinomycin seems to bear some relation to the extreme limitation of their morphogenetic capacities...
September 1966: Planta
Timothy J Atkinson, Jeffrey Fudin, Abhinetri Pandula, Maira Mirza
BACKGROUND: By 2030, the US population of adults aged ≥65 years will increase by >80%, and these adults will account for nearly 20% of the US population. In this population, the decline of multiple physiologic processes and diseases collectively influence treatment options. Physiologic changes, drug-drug interactions resulting from polypharmacy, and drug-disease interactions combine to make elderly patients more sensitive to the adverse events (AEs) associated with medications, all of which must be considered in drug selection...
November 2013: Clinical Therapeutics
Jack P McNulty
In the United States the most common cancers of the head and neck are those of the oral cavity and pharynx. In 2007, oral cancer will be diganosed in more than 37,000 Americans and will claim more than 7,500 lives. The report presented here describes a case of extrarodinary pain in a woman with metastatic adenocarcinoma of the hard palate. At the time of her referral for hospice care, she was experiencing excruciating, unremitting, chronic pain graded 10 of 10 on a standard pain scale. Her analgesic treatment consisted of opioids prescribed in increasingly higher doses until they were ineffective, the effects of treatment could not be tolerated, or she could not swallow the quantity or oral medication needed to provide relief...
May 2007: International Journal of Pharmaceutical Compounding
Jack P McNulty
The search for an effective and affordable treatment for severe chronic pain, particularly neuropathic pain, has been elusive. The reluctance of many physicians to prescribe strong opioids for pain when other modalities have failed has resulted in the undertreatment of many patients. Levorphanol is 1 of 2 opioids that block N-methyl-D-aspartate receptors. In this article, the mechanism of N-methyl-D-aspartate receptor activation is described, the efficacy of levorphanol in the treatment of severe chronic pain is examined, and the properties and clinical applications of that agent are reviewed...
May 2007: International Journal of Pharmaceutical Compounding
Jack P McNulty
No abstract text is available yet for this article.
March 2006: International Journal of Pharmaceutical Compounding
Jane Vail
For former National Football League player Kerry Schmidt, BA,MBA, chronic pain is a part of everyday life. To repair sports-related trauma sustained during his 6-year career as a defensive back, Schmidt has undergone 24 major orthopedic surgeries over the past three decades and will undergo two or three additional procedures to repair his lower back. Now a sports reporter, a syndicated sports columnist, and a business owner, Schmidt says his pain at times has rated a 10-plus on a 10-point pain scale. Schmidt recently took control of his constant discomfort...
January 2006: International Journal of Pharmaceutical Compounding
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