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https://www.readbyqxmd.com/read/29142176/evaluation-of-the-human-relevance-of-the-constitutive-androstane-receptor-mediated-mode-of-action-for-rat-hepatocellular-tumor-formation-by-the-synthetic-pyrethroid-momfluorothrin
#1
Yu Okuda, Masahiko Kushida, Hiroko Kikumoto, Yoshimasa Nakamura, Hashihiro Higuchi, Satoshi Kawamura, Samuel M Cohen, Brian G Lake, Tomoya Yamada
High dietary levels of the non-genotoxic synthetic pyrethroid momfluorothrin increased the incidence of hepatocellular tumors in male and female Wistar rats. Mechanistic studies have demonstrated that the mode of action (MOA) for momfluorothrin-induced hepatocellular tumors is constitutive androstane receptor (CAR)-mediated. In the present study, to evaluate the potential human carcinogenic risk of momfluorothrin, the effects of momfluorothrin (1-1,000 µM) and a major metabolite Z-CMCA (5-1,000 µM) on hepatocyte replicative DNA synthesis and CYP2B mRNA expression were examined in cultured rat and human hepatocyte preparations...
2017: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/29137861/renal-replacement-therapy-in-severe-phenobarbital-poisoning-another-brick-in-the-wall
#2
A Bedet, A Alestra, D Vodovar, A Mekontso Dessap, N de Prost
No abstract text is available yet for this article.
November 11, 2017: Medicina Intensiva
https://www.readbyqxmd.com/read/29137095/differences-in-ugt1a1-gene-mutations-and-pathological-liver-changes-between-chinese-patients-with-gilbert-syndrome-and-crigler-najjar-syndrome-type-ii
#3
Lei Sun, Man Li, Liang Zhang, Xiaoying Teng, Xiangmei Chen, Xingang Zhou, Zhiyuan Ma, Liming Qi, Peng Wang
Diagnosis of Crigler-Najjar syndrome type II (CNS-II) and Gilbert syndrome (GS) based on the serum bilirubin concentration is difficult, because this parameter can fluctuate under certain conditions. The aim of this study was to explore differences in UGT1A1 gene mutations, which cause both CNS and GS, and pathological changes between CNS-II and GS.Ninety-five Chinese patients with hereditary unconjugated hyperbilirubinemia were enrolled in this study. Peripheral blood samples obtained from patients were used to evaluate bilirubin levels and for UGT1A1 gene testing...
November 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29131525/modified-dispersive-liquid-phase-microextraction-based-on-sequential-injection-solidified-floating-organic-drop-combined-with-hplc-for-the-determination-of-phenobarbital-and-phenytoin
#4
Arezou Amiri Pebdani, Shayesteh Dadfarnia, Ali Mohammad Haji Shabani, Saeid Khodadoust, Mohammad Sharif Talebianpoor
A modified dispersive liquid phase microextraction based on sequential injection solidified floating organic drop was developed for simultaneous separation/preconcentration of trace amounts of phenobarbital and phenytoin. The important factors affecting on the extraction recovery including pH, the volume of extraction solvent, ionic strength and the number of injections were investigated and optimized by Box-Behnken design and desirability function. Under the optimum experimental conditions, the calibration graph was linear in the concentration range of 1...
November 13, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/29128797/sotalol-enhances-the-anticonvulsant-action-of-valproate-and-diphenylhydantoin-in-the-mouse-maximal-electroshock-model
#5
Monika Banach, Monika Popławska, Kinga K Borowicz-Reutt
BACKGROUND: Sotalol as a drug blocking β-receptors and potassium KCNH2 channels may interact with different substances that affect seizures. Herein, we present interactions between sotalol and four conventional antiepileptic drugs: carbamazepine, valproate, phenytoin and phenobarbital. METHODS: Effects of sotalol and antiepileptics alone on seizures were determined in the electroconvulsive threshold test, while interactions between sotalol and antiepileptic drugs were estimated in the maximal electroshock test in mice...
May 11, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29117788/recurrent-admissions-for-hypothermia-from-concomitant-topiramate-and-phenobarbital-a-case-report
#6
Alisha M Mutch
INTRODUCTION: This article presents an additional case of concomitant topiramate and phenobarbital administration that resulted in 8 hospital admissions for hypothermia that resolved after discontinuation of phenobarbital. CASE: A 56-year-old white female with cerebral palsy and quadriplegia, epilepsy, and hypothyroidism was admitted to a community teaching hospital multiple times with documented hypothermia. These admissions followed a subsequent dose increase of topiramate in December 2014...
January 1, 2017: Journal of Pharmacy Practice
https://www.readbyqxmd.com/read/29110630/genotoxicity-of-4-piperazin-1-yl-8-trifluoromethyl-pyrido-2-3-e-1-2-4-triazolo-4-3-a-pyrazine-a-potent-h4-receptor-antagonist-for-the-treatment-of-allergy-evidence-of-glyoxal-intermediate-involvement
#7
Mithat Gunduz, Amanda L Cirello, Peter Klimko, Jennifer L Dumouchel, Upendra A Argikar
BACKGROUND: 4-(piperazin-1-yl)-8-(trifluoromethyl)pyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazine (1) is small-molecule which demonstrated a sub-nM inhibitory potency toward the histamine H4 receptor (H4R). However, it was found to be mutagenic an in vitro Ames assay. Metabolic bioactivation of 1 could potentially arise from the piperazine moiety by forming reactive intermediates such as glyoxal, aldehyde-imine and/or iminium ion, which could all lead to genotoxicity. The aim was to investigate bioactivation of 1 to determine the potential causes of the genotoxicity and mitigate liabilities in this scaffold...
November 6, 2017: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29110561/efficacy-of-zonisamide-on-interictal-electroencephalography-in-familial-spontaneous-epileptic-cats
#8
Masayasu Ukai, Yuji Hamamoto, Yoshihiko Yu, Aki Fujiwara-Igarashi, Michio Fujita, Daisuke Hasegawa
Objectives The effectiveness of zonisamide (ZNS) against spontaneous epilepsy in cats has not yet been described. The purpose of this study was to investigate the effect of ZNS on interictal paroxysmal discharges (PDs) using scalp electroencephalography (EEG) in familial spontaneous epileptic cats (FSECs). Methods Eight FSECs were evaluated (six males and two females). Scalp EEG measurements were performed once a week for 3 weeks before ZNS administration (Pre-ZNS). Thereafter, administration of ZNS was started and an adjustment period was instituted until the drug in plasma achieved the steady state...
November 1, 2017: Journal of Feline Medicine and Surgery
https://www.readbyqxmd.com/read/29108398/blockade-of-p75-neurotrophin-receptor-reverses-irritability-and-anxiety-related-behaviors-in-a-rat-model-of-status-epilepticus
#9
Soraya Mehrabi, Mahyar Janahamdi, Mohammad Taghi Joghataie, Mahmood Barati, Mohsen Marzban, Mahmoudreza Hadjighassem, Maryam Farahmandfar
Background: Many recent epidemiological studies have shown that epileptic patients are more likely suffer from depression, anxiety, and irritability. However, the cellular mechanisms of epilepsy-induced psychotic behaviors are not fully elucidated. Neurotrophin receptors have been suggested to be involved in epilepsy and also in psychiatric disorders. Up-regulation of p75NTR expression and activation of p75NTR signalling cascades after the seizure have been shown, but the role of the p75 receptor in epilepsy-induced psychotic behaviors has not been documented so far...
November 7, 2017: Iranian Biomedical Journal
https://www.readbyqxmd.com/read/29097226/understanding-the-differences-between-cocrystal-and-salt-aqueous-solubilities
#10
Katie L Cavanagh, Chinmay Maheshwari, Naír Rodríguez-Hornedo
This work challenges the popular notion that pharmaceutical salts are more soluble than cocrystals. There are cocrystals that are more soluble than salt forms of a drug and vice-versa. It all depends on the interplay between the chemistry of both the solid and solution phases. Aqueous solubility, pHmax, and supersaturation index (SA =SCC or Ssalt/SD) of cocrystals and salts of a basic drug, Lamotrigine (LTG), were determined, and mathematical models that predict the influence of cocrystal/salt Ksp and Ka were derived...
October 30, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29097018/antiepileptic-drugs-and-liver-disease
#11
REVIEW
Jorge Vidaurre, Satya Gedela, Shannon Yarosz
Acute, symptomatic seizures or epilepsy may complicate the course of hepatic disease. Choosing the most appropriate antiepileptic drug in this setting represents a difficult challenge, as most medications are metabolized by the liver. This article focuses on the acute and chronic treatment of seizures in patients with advanced liver disease and reviews the hepatotoxic potential of specific antiepileptic drugs. Newer antiepileptic drugs without, or with minimal, hepatic metabolism, such as levetiracetam, lacosamide, topiramate, gabapentin, and pregabalin should be used as first-line therapy...
September 22, 2017: Pediatric Neurology
https://www.readbyqxmd.com/read/29095046/molecular-spectroscopic-studies-examining-the-interactions-between-phenobarbital-and-human-serum-albumin-in-alcohol-consumption
#12
Sheng-Feng Cui, Wei Li, Cheng-He Zhou
BACKGROUND: Alcohol dependence is associated with a wide range of serious mental, physical, and social consequences and is one of the most common chronic diseases worldwide. Barbiturates, which are a first-line treatment in the clinic for alcohol withdrawal, may result in combined barbiturate and alcohol use. Their co-use abuse may promote synergistic effects between barbiturates and alcohol in vivo. OBJECTIVE: To investigate the effects of different alcohol concentrations on the synergistic effects of phenobarbital and alcohol...
November 2, 2017: American Journal of Drug and Alcohol Abuse
https://www.readbyqxmd.com/read/29071470/the-challenge-of-pharmacotherapy-in-children-and-adolescents-with-epilepsy-adhd-comorbidity
#13
REVIEW
Alberto Verrotti, Romina Moavero, Gianvito Panzarino, Claudia Di Paolantonio, Renata Rizzo, Paolo Curatolo
Epilepsy is common in children and adolescents where its prevalence is 3.2-5.5/1000. About one-third of patients also have attention deficit hyperactivity/impulsivity disorder (ADHD). The possible relationship between epilepsy and ADHD is still unclear, and ADHD symptoms (such as inattention, hyperactivity, behavioral disturbances) are frequently considered as adverse effects of antiepileptic drugs (AEDs). The literature was searched for data on the behavioral effects of AEDs. Phenobarbital is the most frequently reported medication to induce symptoms of ADHD, followed by topiramate and valproic acid...
October 25, 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/29067285/decreasing-total-medication-exposure-and-length-of-stay-while-completing-withdrawal-for-neonatal-abstinence-syndrome-during-the-neonatal-hospital-stay
#14
Lori A Devlin, Timothy Lau, Paula G Radmacher
INTRODUCTION: Neonatal abstinence syndrome (NAS) is a rapidly growing public health concern that has considerably increased health-care utilization and health-care costs. In an effort to curtail costs, attempts have been made to complete withdrawal as an outpatient. Outpatient therapy has been shown to prolong exposure to medications, which may negatively impact neurodevelopmental and behavioral outcomes. We hypothesized that the implementation of a modified NAS protocol would decrease total drug exposure and length of stay while allowing for complete acute drug withdrawal during the neonatal hospital stay...
2017: Frontiers in Pediatrics
https://www.readbyqxmd.com/read/29057572/simultaneous-analysis-by-quadrupole-orbitrap-mass-spectrometry-and-uhplc-ms-ms-for-the-determination-of-sedative-hypnotics-and-sleep-inducers-in-adulterated-products
#15
Ji Hyun Lee, Han Na Park, Ji Yeon Choi, Nam Sook Kim, Hyung-Joon Park, Seong Soo Park, Sun Young Baek
Adulterated products are continuously detected in society and cause problems. In this study, we developed and validated a method for determining synthetic sedative-hypnotics and sleep inducers, including barbital, benzodiazepam, zolpidem, and first-generation antihistamines, in adulterated products using Quadrupole-Orbitrap mass spectrometry and ultra high performance liquid chromatography with tandem mass spectrometry. In Quadrupole-Orbitrap mass spectrometry analysis, target compounds were confirmed using a combination of retention time, mass tolerance, mass accuracy, and fragment ions...
October 23, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/29054049/individual-variability-in-clinical-effect-and-tolerability-of-opioid-analgesics-importance-of-drug-interactions-and-pharmacogenetics
#16
REVIEW
Vigdis Solhaug, Espen Molden
BACKGROUND: As pain is often a comorbid condition, many patients use opioid analgesics in combination with several other drugs. This implies a generally increased risk of drug interactions, which along with inherent pharmacogenetic variability and other factors may cause differences in therapeutic response of opioids. AIM: To provide an overview of interactions and pharmacogenetic variability of relevance for individual differences in effect and tolerability of opioid analgesics, which physicians and other healthcare professionals should be aware of in clinical practice...
October 17, 2017: Scandinavian Journal of Pain
https://www.readbyqxmd.com/read/29053702/the-effects-of-adding-prophylactic-phenobarbital-to-therapeutic-hypothermia-in-the-term-equivalent-hypoxic-ischemic-rat
#17
Sushma Krishna, Alexandra Hutton, Eric Aronowitz, Holly Moore, Susan J Vannucci
BackgroundHypoxic-ischemic encephalopathy (HIE) is a major cause of neonatal morbidity and mortality. Therapeutic hypothermia (TH) is the only available intervention, but neuroprotection is incomplete and variable. Seizures are common in infants with HIE undergoing TH and may worsen outcome. Phenobarbital is sometimes added, although use of prophylactic phenobarbital is controversial in the neonate. We hypothesize that prophylactic phenobarbital (PB) will not reduce, and may enhance, the neuroprotective effects of TH on brain injury and motor outcomes in the postnatal-day 10 (P10) hypoxic-ischemic (HI) rat...
October 20, 2017: Pediatric Research
https://www.readbyqxmd.com/read/29042836/evaluation-of-the-effects-of-extracorporeal-membrane-oxygenation-on-antiepileptic-drug-serum-concentrations-in-pediatric-patients
#18
Nicholas O Dillman, Mindl M Messinger, Kimberly N Dinh, Jennifer L Placencia, Brady S Moffett, Milenka Cuevas Guaman, Jennifer C Erklauer, Jeffrey R Kaiser, Angus A Wilfong
OBJECTIVES: Patients supported on extracorporeal membrane oxygenation (ECMO) have an increased incidence of seizures. Phenobarbital (PB) and fosphenytoin (fos-PHT) are common antiepileptic drugs (AEDs) used to manage seizures in the pediatric population; however, it is unknown what effect ECMO has on the serum concentrations of AEDs. The purpose of this study is to evaluate the effect of ECMO on AED serum concentrations. METHODS: A retrospective, matched-cohort study was performed in patients younger than 18 years who received ECMO and were treated with intravenous (IV) PB or fos-PHT at Texas Children's Hospital between 2004 and 2014...
September 2017: Journal of Pediatric Pharmacology and Therapeutics: JPPT: the Official Journal of PPAG
https://www.readbyqxmd.com/read/29037435/feline-epilepsy
#19
REVIEW
Heidi Barnes Heller
Seizures occur commonly in cats and can be classified as idiopathic epilepsy, structural epilepsy, or reactive seizures. Pursuit of a diagnosis may include a complete blood count, serum biochemistry, brain MRI, and cerebrospinal fluid analysis as indicated. Antiepileptic drugs should be considered if a cat is having frequent seizures, or any 1 seizure longer than 5 minutes. Phenobarbital is often the drug of choice; however, levetiracetam may be more useful for certain types of epilepsy in cats. Long-term prognosis depends on the underlying diagnosis and response to therapy...
October 13, 2017: Veterinary Clinics of North America. Small Animal Practice
https://www.readbyqxmd.com/read/29031875/soluble-epoxide-hydrolase-inhibition-with-t-tucb-alleviates-liver-fibrosis-and-portal-pressure-in-carbon-tetrachloride-induced-cirrhosis-in-rats
#20
Chi-Hao Zhang, Lei Zheng, Liang Gui, Jia-Yun Lin, Yi-Ming Zhu, Wen-Sheng Deng, Meng Luo
BACKGROUND/AIMS: Fibrosis and increased intrahepatic vascular resistance are the hallmarks of chronic inflammatory disorders of the liver and cirrhosis. Inhibitors of the enzyme soluble epoxide hydrolase reduce fibrosis in several disease models. The present study aimed at investigating the effects of soluble epoxyhydrolase inhibition with t-TUCB in tetrachloride-induced cirrhosis in rats. METHODS: The models were established by CCl4 (2ml/kg) given subcutaneously for 14 weeks...
October 11, 2017: Clinics and Research in Hepatology and Gastroenterology
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