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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...
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
Andrew J Faskowitz, Vladimir N Kramskiy, Gavril W Pasternak
To determine if recent observations of hypoglycemia in patients receiving high-dose methadone extended to an animal model, we explored the effects of methadone and other mu-opioids on blood glucose levels in mice. Methadone lowered blood glucose in a dose-dependent manner with 20 mg/kg yielding a nadir in average glucose levels to 55 ± 6 mg/dL from a baseline of 172 ± 7 mg/dL, an effect that was antagonized by naloxone and mu selective antagonists β-funaltrexamine and naloxonazine. The effect was stereoselective and limited to only the l-isomer, while the d-isomer was ineffective...
May 2013: Cellular and Molecular Neurobiology
Selena S Schattauer, Mayumi Miyatake, Haripriya Shankar, Chad Zietz, Jamie R Levin, Lee-Yuan Liu-Chen, Vsevolod V Gurevich, Mark J Rieder, Charles Chavkin
KOR activation of Gβγ dependent signaling results in analgesia, whereas the dysphoric effects of KOR agonists are mediated by a different pathway involving G protein receptor kinase and non-visual arrestin. Based on this distinction, a partial KOR agonist that does not efficiently activate arrestin-dependent biased signaling may produce analgesia without dysphoria. No KOR-selective partial agonists are currently available, and preclinical assessment is complicated by sequence differences between rodent (r) and human (h) KOR...
December 7, 2012: Journal of Biological Chemistry
Zsuzsanna Gyulai, Antal Udvardy, Attila Cs Bényei, Jakub Fichna, Katarzyna Gach, Martin Storr, Géza Tóth, Sándor Antus, Sándor Berényi, Anna Janecka, Attila Sipos
Novel 6-ketolevorphanol analogs with diverse substitution patterns at ring C were synthesized and their binding affinities at the μ,δ and κ opioid receptors were investigated. The in vitro activity of the new analogs was then evaluated in the functional assay based on the electrically-stimulated contractions of the mouse ileum. It was shown that analogs with Δ7,8 bond had no significant potency at any of the opioid receptor types. In contrast, analogs with the saturated ring C were either potent κ agonist or antagonist depending on the absence or presence of the hydroxyl group in position 14...
February 2013: Medicinal Chemistry
Vikhyat S Bebarta, Sasha Ramirez, Shawn M Varney
Spice is an herbal mixture smoked for euphoria and mixed with synthetic cannabinoids that are undetected on urine drug screens. Spice use has increased in the military because it is considered legal and is not detected on urine drug screen. The authors describe 3 cases of Spice use in military members. Case 1: 19-year-old male presented with paranoia, agitation, and visual hallucinations after smoking the "Space" brand of Spice. Urine thin-layer chromatography (TLC) and gas chromatography-mass spectrometry (GC-MS) were negative...
2012: Substance Abuse
Eric Prommer, Brandy Ficek
Pain is one of the symptoms most frequently encountered in elderly patients at the end of life. The management of pain in the elderly in general has been associated with undertreatment. The geriatric population has been identified as a challenging population with respect to pain management because of issues related to co-morbidities, polypharmacy and cognitive dysfunction. In the geriatric population, the assessment of pain requires measurement of pain intensity, delineation of opioid responsiveness, and clarification of the impact of pain on patients' psychological, social, spiritual and existential domains...
April 1, 2012: Drugs & Aging
Esther Berrocoso, Kazutaka Ikeda, Ichiro Sora, George R Uhl, Pilar Sánchez-Blázquez, Juan Antonio Mico
Most classical preclinical tests to predict antidepressant activity were initially developed to detect compounds that influenced noradrenergic and/or serotonergic activity, in accordance with the monoaminergic hypothesis of depression. However, central opioid systems are also known to influence the pathophysiology of depression. While the tail suspension test (TST) is very sensitive to several types of antidepressant, the traditional form of scoring the TST does not distinguish between different modes of action...
February 2013: International Journal of Neuropsychopharmacology
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