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David E Moody, Yueqiao Fu, Wenfang B Fang
The purpose of this study was to test the hypothesis that skeletal muscle relaxants could inhibit the in vitro metabolism of common comedications opioids buprenorphine, methadone and oxycodone. The compounds [solubility-limited concentration (μM) studied] were as follows: baclofen (1000), carisoprodol (200), its metabolite meprobamate (1000), chlorzoxazone (200), cyclobenzaprine (1000), metaxalone (50), methocarbamol (1000), orphenadrine (1000) and tizanidine (1000). Compounds were first incubated with human liver microsomes ± pre-incubation, screened with pathway-specific cDNA-expressed cytochrome P450s (rCYP), and then IC50 values determined using either 8-concentration tests for those where the rCYP screen suggested an IC50 was achievable, or a 3-concentration test with downward extrapolation if screen suggested 50% inhibition was not achievable...
March 5, 2018: Basic & Clinical Pharmacology & Toxicology
Minkyu Park, Tarun Anumol, Kevin D Daniels, Shimin Wu, Austin D Ziska, Shane A Snyder
Ozone oxidation has been demonstrated to be an effective treatment process for the attenuation of trace organic compounds (TOrCs); however, predicting TOrC attenuation by ozone processes is challenging in wastewaters. Since ozone is rapidly consumed, determining the exposure times of ozone and hydroxyl radical proves to be difficult. As direct potable reuse schemes continue to gain traction, there is an increasing need for the development of real-time monitoring strategies for TOrC abatement in ozone oxidation processes...
August 1, 2017: Water Research
Jasmien Obbels, Esmée Verwijk, Filip Bouckaert, Pascal Sienaert
BACKGROUND: A significant proportion of electroconvulsive therapy (ECT)-treated patients experience anxiety anticipating the treatment, often to such an extent that they refuse or discontinue a much-needed treatment. Despite its great impact on treatment adherence, anxiety in patients receiving ECT is underexposed in the scientific literature. OBJECTIVES: We aimed to review the prevalence and specific subjects of ECT-related anxiety and therapeutic interventions to reduce it...
December 2017: Journal of ECT
Aileen Lu, Karen S Scott, Aya Chan-Hosokawa, Barry K Logan
In 2013, the National Safety Council's Alcohol Drugs and Impairment Division added zolpidem and carisoprodol and its metabolite meprobamate to the list of Tier 1 drugs that should be tested for in all suspected drug impaired driving and motor vehicle fatality investigations. We describe the validation of an enzyme linked immunosorbent assays (ELISA) for both drugs in whole blood, and the utilization of the ELISA to assess their positivity in a sample of 322 suspected impaired driving cases that was retrospectively screened using the validated assays...
March 1, 2017: Journal of Analytical Toxicology
T A Lewandowski
Carisoprodol is a widely prescribed muscle relaxant and is also a drug known to be a subject to abuse. Despite the fact that carisoprodol has been available for prescription since 1959, a number of gaps in our knowledge of the toxicokinetics of this common drug exist. For example, the volume of distribution (Vd) for carisoprodol in humans has not been reported. A two-compartment pharmacokinetic model describing carisoprodol metabolism and that of the primary metabolite, meprobamate, was developed to better understand the pharmacokinetics of this drug...
August 2017: Human & Experimental Toxicology
Laszlo Prokai, Petr Fryčák, Vien Nguyen, Michael J Forster
We report the evaluation of several mass spectrometry-based methods for the determination of carisoprodol and meprobamate in samples obtained from the rat brain by in vivo intracranial microdialyis. Among the techniques that aspire to perform analyses without chromatographic separation and thereby increase throughput, chip-based nanoelectrospray ionization and the use of an atmospheric pressure solids analysis probe fell short of requirements because of insufficient detection sensitivity and hard ionization, respectively...
October 2016: Journal of Mass Spectrometry: JMS
J A Van Heerden, J R Burger, J J Gerber
BACKGROUND: Prescribing for older patients is a well-recognised problem, and inappropriate items are prescribed frequently. Several tools and criteria are available to promote rational prescribing in older patients. OBJECTIVE: To determine the prevalence of potentially inappropriate prescriptions (PIPs) in older South African patients. METHODS: A retrospective drug utilisation review was conducted using medicine claims data over a 1-year period...
September 9, 2016: South African Medical Journal, Suid-Afrikaanse Tydskrif Vir Geneeskunde
Edson Baltazar Estrada-Arriaga, Juana Enriqueta Cortés-Muñoz, Arturo González-Herrera, César Guillermo Calderón-Mólgora, Ma de Lourdes Rivera-Huerta, Esperanza Ramírez-Camperos, Leticia Montellano-Palacios, Silvia Lucila Gelover-Santiago, Sara Pérez-Castrejón, Lina Cardoso-Vigueros, Alejandra Martín-Domínguez, Liliana García-Sánchez
Two full-scale biological nutrient removal systems upgraded with three physico-chemical processes (coagulation, chemical precipitation, and neutral Fenton) were evaluated in order to determine the removal of emerging pollutants (EPs) present in municipal wastewater from Mexico. Between 41 and 55 EPs were detected in the influents of two wastewater treatment plants (WWTPs), including personal care products (PPCPs), antibiotics, analgesics, antiepileptics, antilipidemics, antihypertensives, antiseptics, stimulants, and hormones...
November 15, 2016: Science of the Total Environment
Miguel Peña-López, Helfried Neumann, Matthias Beller
A general study of the iron-catalyzed reaction of urea with nucleophiles is here presented. The carbamoylation of alcohols allows for the synthesis of N-unsubstituted (primary) carbamates, including present drugs (Felbamate and Meprobamate), without the necessity to apply phosgene and related derivatives. Using amines as nucleophiles gave rise to the respective mono- and disubstituted ureas via selective transamidation reaction. These atom-economical transformations provide a direct and selective access to valuable compounds from cheap and readily available urea using a simple Lewis-acidic iron(II) catalyst...
August 23, 2016: ChemSusChem
Mandu Inyang, Riley Flowers, Drew McAvoy, Eric Dickenson
The removal of trace organic compounds (TOrCs) and their biotransformation rates, kb (LgSS(-)(1)h(-)(1)) was investigated across different redox zones in a biological nutrient removal (BNR) system using an OECD batch test. Biodegradation kinetics of fourteen TOrCs with initial concentration of 1-36μgL(-)(1) in activated sludge were monitored over the course of 24h. Degradation kinetic behavior for the TOrCs fell into four groupings: Group 1 (atenolol) was biotransformed (0.018-0.22LgSS(-)(1)h(-)(1)) under anaerobic, anoxic, and aerobic conditions...
September 2016: Bioresource Technology
Irene J Fisher, Patrick J Phillips, Kaitlyn M Colella, Shawn C Fisher, Tristen Tagliaferri, William T Foreman, Edward T Furlong
Coastal onsite wastewater disposal systems (OWDS) were inundated by Hurricane Sandy's storm tide. This study compares the shallow groundwater quality (nutrients, pharmaceuticals, and hormones) downgradient of OWDS before and after Hurricane Sandy, where available, and establishes a baseline for wastewater influence on groundwater in coastal communities inundated by Hurricane Sandy. Nutrients and contaminants of emerging concern (CECs) were detected in shallow groundwater downgradient of OWDS in two settings along the New Jersey and New York coastlines: 1) a single, centralized OWDS in a park; and 2) multiple OWDS (cesspools) in low-density residential and mixed-use/medium density residential areas...
June 30, 2016: Marine Pollution Bulletin
Yacine Lounis, Dominique Bonnet-Zamponi, Éric Pautas, Marie-Line Gaubert-Dahan
We have conducted in two nursing homes a survey to study the impact of meprobamate's withdrawal, at the beginning of 2012, in terms of extent of prescribing to others psychotropic drugs and occurrence of adverse events. After meprobamate's withdrawal, 65 % of residents did not receive alternative medication and within three months after meprobamate stopping, adverse events (drowsiness, falls and hospitalization) decreased while agitation did not increase.
March 2016: Soins. Gérontologie
Alexander Owen James, Timothy R Nicholson, Robert Hill, Jennifer Bearn
Meprobamate, a benzodiazepine-like drug, was commonly prescribed for anxiety in the 1960s and 1970s, but fell out of favour, at least in part, due to the risk of dependence, for which there is little published evidence to guide clinical management. We discuss a 70-year-old man with a 45-year history of meprobamate dependency and multiple failed previous withdrawal attempts who was successfully withdrawn from meprobamate using diazepam during a 2-week inpatient stay on a specialist Addictions ward. An appropriate diazepam dose was established using the Clinical Institute Withdrawal Assessment scale for benzodiazepines (CIWA-B)...
February 29, 2016: BMJ Case Reports
Manish Kumar, Glenn H Dillon
Meprobamate is a schedule IV anxiolytic and the primary metabolite of the muscle relaxant carisoprodol. Meprobamate modulates GABAA (γ-aminobutyric acid Type A) receptors, and has barbiturate-like activity. To gain insight into its actions, we have conducted a series of studies using recombinant GABAA receptors. In αxβzγ2 GABAA receptors (where x=1-6 and z=1-3), the ability to enhance GABA-mediated current was evident for all α subunit isoforms, with the largest effect observed in α5-expressing receptors...
March 15, 2016: European Journal of Pharmacology
Matthew H Slawson, Kamisha L Johnson-Davis
Carisoprodol and meprobamate are centrally acting muscle relaxant/anxiolytic drugs that can exist in a parent-metabolite relationship (carisoprodol → meprobamate) or as a separate pharmaceutical preparation (meprobamate aka Equanil, others). The monitoring of the use of these drugs has both clinical and forensic applications in pain management applications and in overdose situations. LC-MS/MS is used to analyze urine or plasma/serum extracts with deuterated analogs of each analyte as internal standards to ensure accurate quantitation and control for any potential matrix effects...
2016: Methods in Molecular Biology
Philipe de Souto Barreto, Maryse Lapeyre-Mestre, Philippe Cestac, Bruno Vellas, Yves Rolland
BACKGROUND: Benzodiazepines and "Z drugs" are often prescribed in residents of nursing homes (NH) despite their well-known deleterious effects. We aimed to investigate if a general intervention on quality of care led to discontinuation of benzodiazepine, and to examine which NH-related factors were associated in change of benzodiazepines use. METHODS: IQUARE is a quasi-experimental study, investigating the impact of an intervention based on a geriatric education with NH staff on several quality indicators of care (including appropriate prescriptions)...
April 2016: British Journal of Clinical Pharmacology
O O Ogunlaja, W J Parker
The efficacy of three different wastewater treatment configurations, conventional activated sludge (CAS), nitrifying activated sludge (NAS) and biological nutrient removal (BNR) for removal of selected micropollutants from authentic wastewater was investigated. The processes were also characterized based on their proficiency to reduce the estrogenic activity of the influent wastewater using the in vitro recombinant yeast assay. The removal efficiency of trimethoprim improved with the complexity of the three treatment process configurations...
2015: Water Science and Technology: a Journal of the International Association on Water Pollution Research
Tarun Anumol, Massimiliano Sgroi, Minkyu Park, Paolo Roccaro, Shane A Snyder
This study investigated the applicability of bulk organic parameters like dissolved organic carbon (DOC), UV absorbance at 254 nm (UV254), and total fluorescence (TF) to act as surrogates in predicting trace organic compound (TOrC) removal by granular activated carbon in water reuse applications. Using rapid small-scale column testing, empirical linear correlations for thirteen TOrCs were determined with DOC, UV254, and TF in four wastewater effluents. Linear correlations (R(2) > 0.7) were obtained for eight TOrCs in each water quality in the UV254 model, while ten TOrCs had R(2) > 0...
June 1, 2015: Water Research
Bahadir Demir, Yasemin Demir, Ihsan Aksoy, Osman Hasan Tahsin Kilic, Volkan Gucyetmez, Haluk A Savas
Phenprobamate (3-phenylpropylcarbamate) is a centrally acting muscle relaxant with mild sedative and anticonvulsant effects. Muscle relaxants can enhance and prolong the effect of narcotic drugs and enable to obtain same effect with a smaller amount of alcohol or illicit substance. Almost all of the centrally acting muscle relaxants have varying sedative effects on which their abuse potential mainly depends. Data related to abuse of carisoprodol, meprobamate, baclofen takes place in the literature. However, to our knowledge this is the first case report about abuse of and tolerance to phenprobamate...
June 2015: Addictive Behaviors
Dilipkumar Pal, Upal Kanti Mazumder
Mikania scandens, a twining herb that grows as a weed in India and Bangladesh is used as vegetables and is a good source of vitamin A, C, B complex, mikanin, sesquiterpenes, betasitosterin, stigmasterol and friedelin. The present communication reports CNS depressant activities with special emphasis to brain biogenic amines in mice. Ethanol extract of leaves of M. scandens (EEMS) was prepared by Soxhalation and analyzed chemically. EEMS potentiated sleeping time induced by pentobarbitone, diazepam and meprobamate and showed significant reduction in the number of writhes and stretches...
December 2014: Indian Journal of Experimental Biology
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