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Phenytoin

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https://www.readbyqxmd.com/read/29135699/phenytoin-induced-excessive-sedation-during-awake-craniotomy-an-unusual-observation
#1
Ankur Khandelwal, Navdeep Sokhal, Niraj Kumar, Shalendra Singh, Suman Sokhal
No abstract text is available yet for this article.
November 10, 2017: Journal of Neurosurgical Anesthesiology
https://www.readbyqxmd.com/read/29133240/prediction-of-human-cns-pharmacokinetics-using-a-physiologically-based-pharmacokinetic-modeling-approach
#2
Yumi Yamamoto, Pyry A Välitalo, Yin Cheong Wong, Dymphy R Huntjens, Johannes H Proost, An Vermeulen, Walter Krauwinkel, Margot W Beukers, Hannu Kokki, Merja Kokki, Meindert Danhof, Johan G C van Hasselt, Elizabeth C M de Lange
Knowledge of drug concentration-time profiles at the central nervous system (CNS) target-site is critically important for rational development of CNS targeted drugs. Our aim was to translate a recently published comprehensive CNS physiologically-based pharmacokinetic (PBPK) model from rat to human, and to predict drug concentration-time profiles in multiple CNS compartments on available human data of four drugs (acetaminophen, oxycodone, morphine and phenytoin). Values of the system-specific parameters in the rat CNS PBPK model were replaced by corresponding human values...
November 10, 2017: European Journal of Pharmaceutical Sciences
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
#3
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/29130833/changes-in-the-pharmacokinetics-of-phenytoin-in-dextran-sulfate-sodium-induced-ulcerative-colitis-in-mice
#4
Yoshiki Kusunoki, Yurika Kido, Yuichi Naito, Risako Kon, Nanaho Mizukami, Miho Kaneko, Nobuyuki Wakui, Yoshiaki Machida, Nobutomo Ikarashi
We previously demonstrated that the expression levels of drug-metabolizing enzymes, cytochrome P450 (CYP) enzymes, in the liver are significantly decreased in a murine model of ulcerative colitis (UC). In this study, we investigated changes in the pharmacokinetics of phenytoin, a CYP2C substrate drug, in the presence of UC. Colitis was induced by feeding male mice 3.5% dextran sulfate sodium (DSS) dissolved in drinking water for 10 days. The messenger RNA (mRNA) expression of CYP2C29 and CYP2C37 and the protein expression of CYP2C in the liver were evaluated via real-time reverse transcription-polymerase chain reaction and Western blotting, respectively...
January 1, 2017: International Journal of Toxicology
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/29125423/management-of-chronic-neuropathic-pain-with-single-and-compounded-topical-analgesics
#6
Nebojsa Nick Knezevic, Tatiana Tverdohleb, Farid Nikibin, Ivana Knezevic, Kenneth D Candido
The goal of our review was to emphasize important aspects that physicians should take into consideration when prescribing topical analgesics as part of chronic neuropathic pain treatment. We discuss the dermatopharmacokinetics and microstructural components of the skin, differences between topical and transdermal drug delivery, and topical medication effects on peripheral neuropathy and central sensitization. Even though the US FDA approved topical analgesics are 8%-capsaicin and 5%-lidocaine patches for treating postherpetic neuralgia, there are many other studies conducted on the efficacy of topical ketamine cream, clonidine gel, topical gabapentin, topical baclofen and topical phenytoin for peripheral neuropathic pain, either alone or in combination with other formulations...
November 10, 2017: Pain Management
https://www.readbyqxmd.com/read/29122665/in-vitro-screening-of-dual-flavonoid-combinations-for-reversing-p-glycoprotein-mediated-multidrug-resistance-focus-on-antiepileptic-drugs
#7
Ana Ferreira, Adriana O Santos, Amílcar Falcão, Gilberto Alves
The combined use of different P-glycoprotein (P-gp) inhibitors may be a relevant approach to the synergistic and safer inhibition of the P-gp-mediated drug efflux. Herein, we aimed to explore dual combinations of the flavonoids baicalein, (-)-epigallocatechin gallate, kaempferol, quercetin and silymarin to reverse the interference of P-gp on the intracellular accumulation of antiepileptic drugs (AEDs). The intracellular accumulation of rhodamine 123 (a classic P-gp substrate) and of several commonly used AEDs (carbamazepine, phenytoin, oxcarbazepine) or their metabolites (carbamazepine-10,11-epoxide and licarbazepine) was evaluated in MDCK-MDR1 cells in the presence and absence of individual flavonoids and their combinations...
November 6, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29114367/the-comparison-of-anti-seizure-and-tocolytic-effects-of-phenytoin-and-magnesium-sulphate-in-the-treatment-of-eclampsia-and-preeclampsia-a-randomised-clinical-trial
#8
Maryam Khooshideh, Majid Ghaffarpour, Sama Bitarafan
Background: To date, magnesium sulphate (MgSO4) is the treatment of choice for prevention of seizure in eclampsia and preeclampsia. However, there are some limitations in the administration of MgSO4 due to its tocolytic effects. The aim of this study was to compare the anticonvulsant and tocolytic effects of MgSO4 and another drug, phenytoin, in patients with eclampsia and preeclampsia. Methods: This clinical trial was conducted on pregnant women hospitalised with eclampsia or preeclampsia, during 2014-2016...
July 6, 2017: Iranian Journal of Neurology
https://www.readbyqxmd.com/read/29114270/trigeminal-neuralgia
#9
REVIEW
Yad Ram Yadav, Yadav Nishtha, Pande Sonjjay, Parihar Vijay, Ratre Shailendra, Khare Yatin
Trigeminal neuralgia (TN) is a sudden, severe, brief, stabbing, and recurrent pain within one or more branches of the trigeminal nerve. Type 1 as intermittent and Type 2 as constant pain represent distinct clinical, pathological, and prognostic entities. Although multiple mechanism involving peripheral pathologies at root (compression or traction), and dysfunctions of brain stem, basal ganglion, and cortical pain modulatory mechanisms could have role, neurovascular conflict is the most accepted theory. Diagnosis is essentially clinically; magnetic resonance imaging is useful to rule out secondary causes, detect pathological changes in affected root and neurovascular compression (NVC)...
October 2017: Asian Journal of Neurosurgery
https://www.readbyqxmd.com/read/29097018/antiepileptic-drugs-and-liver-disease
#10
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/29095797/influence-of-renal-function-on-pharmacokinetics-of-antiepileptic-drugs-metabolized-by-cyp3a4-in-a-patient-with-renal-impairment
#11
Yoshiaki Yamamoto, Naotaka Usui, Takuji Nishida, Miho Mori, Yukitoshi Takahashi, Katsumi Imai, Yoshiyuki Kagawa, Yushi Inoue
BACKGROUND: Several studies have demonstrated that renal impairment not only decreases renal clearance, but also hepatic clearance of medications that are CYP3A4 substrates. We evaluated the influence of renal function on the pharmacokinetics of antiepileptic drugs (AEDs) metabolized by CYP3A4. METHODS: We retrospectively calculated the concentration/dose ratio (CD ratio) for topiramate and clobazam in an epilepsy patient with renal impairment. In addition, we determined the CD ratio of perampanel in 17 patients with normal renal function and compared it with that in the patient with renal impairment...
October 31, 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/29093341/effects-of-the-antiepileptic-drugs-phenytoin-gabapentin-and-levetiracetam-on-bone-strength-bone-mass-and-bone-turnover-in-rats
#12
Junkichi Kanda, Nobuo Izumo, Yoshiko Kobayashi, Kenji Onodera, Taketoshi Shimakura, Noriaki Yamamoto, Hideaki E Takahashi, Hiroyuki Wakabayashi
Long-term treatment with antiepileptic drugs (AEDs) is accompanied by reduced bone mass that is associated with an increased risk of bone fractures. Although phenytoin has been reported to adversely influence bone metabolism, little is known pertaining to more recent AEDs. The aim of this study was to evaluate the effects of gabapentin or levetiracetam on bone strength, bone mass, and bone turnover in rats. Male Sprague-Dawley rats were orally administered phenytoin (20 mg/kg), gabapentin (30 or 150 mg/kg), or levetiracetam (50 or 200 mg/kg) daily for 12 weeks...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29078132/the-predictive-performances-of-equations-used-to-estimate-unbound-phenytoin-concentrations-in-a-medical-icu-population-and-the-impact-of-exogenous-albumin-administration
#13
Labdhi Parikh, Robert MacLaren
PURPOSE: This study evaluated the predictive performances of four equations (Sheiner-Tozer [ST], Kane-modified ST, Anderson-modified ST, and Cheng-modified ST) used to estimate free phenytoin concentrations in a medical intensive care unit (MICU) and assessed the impact of exogenously administered albumin. METHODS: Thirty MICU subjects receiving phenytoin were retrospectively evaluated. Predictive performances were assessed by mean absolute error (MAE), mean prediction error (MPE), and root mean squared error (RMSE); linear regression of predicted vs...
October 20, 2017: Journal of Critical Care
https://www.readbyqxmd.com/read/29076187/the-association-of-hla-b-15-02-allele-and-stevens-johnson-syndrome-toxic-epidermal-necrolysis-induced-by-aromatic-anticonvulsant-drugs-in-a-south-indian-population
#14
Keerankulangara Devi
BACKGROUND: The presence of HLA-B*15:02 allele is considered a risk factor for development of Stevens-Johnson syndrome/toxic epidermal necrolysis (SJS/TEN) in patients taking aromatic anticonvulsant drugs like carbamazepine and phenytoin. The genetic association is ethnicity specific. Testing for HLA-B*15:02 allele is suggested as a prerequisite before starting carbamazepine in certain ethnic groups. There are only a few/no studies from south India on HLA association of SJS/TEN. AIMS: To identify any association between HLA-B*15:02 allele and SJS/TEN induced by carbamazepine/phenytoin among native population...
October 26, 2017: International Journal of Dermatology
https://www.readbyqxmd.com/read/29074381/drug-solubilization-by-means-of-a-surface-modified-edible-biopolymer-enabled-by-hot-melt-extrusion
#15
Hwee Jing Ong, Rodolfo Pinal
A formulation/processing combination approach for increasing the solubility of poorly-soluble drugs using solid dispersions (SDs) is presented, whereby the API retains its crystalline state. The approach utilizes a biopolymer naturally produced as dendrimeric nanoparticles that has been surface-modified to act as a solubilizing agent. The solubilizing agent is enabled by hot melt extrusion to produce the SDs. Four APIs, phenytoin (PHT), griseofulvin (GSF), ibuprofen (IBU) and loratadine (LOR) were used as model compounds to evaluate solubility enhancement...
October 23, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29073585/evaluation-of-phenytoin-serum-levels-following-a-loading-dose-in-the-acute-hospital-setting
#16
Olga Selioutski, Katherine Grzesik, Olga N Vasilyeva, Ágúst Hilmarsson, A James Fessler, Lynn Liu, Robert A Gross
PURPOSE: Due to the complex pharmacokinetic profiles of phenytoin (PHT) and fosphenytoin (FOS), achieving sustained, targeted serum PHT levels in the first day of use is challenging. METHODS: A population based approach was used to analyze total serum PHT (tPHT) level within 2-24h of PHT/FOS loading with or without supplementary maintenance or additional loading doses among PHT-naïve patients in the acute hospital setting. Adequate tPHT serum level was defined as ≥20μg/mL...
October 16, 2017: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/29071470/the-challenge-of-pharmacotherapy-in-children-and-adolescents-with-epilepsy-adhd-comorbidity
#17
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/29070779/effects-of-the-antiepileptic-drugs-topiramate-and-lamotrigine-on-bone-metabolism-in-rats
#18
Junkichi Kanda, Nobuo Izumo, Yoshiko Kobayashi, Kenji Onodera, Taketoshi Shimakura, Noriaki Yamamoto, Hideaki E Takahashi, Hiroyuki Wakabayashi
Long-term treatment with antiepileptic drugs (AED) is associated with an elevated risk of bone fracture due to decreased bone mineral density (BMD). Phenytoin has been shown to affect bone metabolism adversely, whereas newly developed AEDs have not been studied. This study evaluated the effects of topiramate and lamotrigine on bone metabolism in rats. Five-week-old male Sprague-Dawley rats were treated orally with phenytoin (20 mg/kg), topiramate (5 or 20 mg/kg), or lamotrigine (2 or 10 mg/kg) daily for 12 weeks...
2017: Biomedical Research
https://www.readbyqxmd.com/read/29061822/in-vitro-effects-of-bromoalkyl-phenytoin-derivatives-on-regulated-death-cell-cycle-and-ultrastructure-of-leukemia-cells
#19
Katarzyna Śladowska, Małgorzata Opydo-Chanek, Teodora Król, Wojciech Trybus, Ewa Trybus, Anna Kopacz-Bednarska, Jadwiga Handzlik, Katarzyna Kieć-Kononowicz, Lidia Mazur
BACKGROUND/AIM: To search for new antileukemic agents, the chemical structure of phenytoin was modified. A possible cytotoxic activity of three bromoalkyl phenytoin analogs, methyl 2-(1-(3-bromopropyl)-2,4-dioxo-5,5-diphenylimidazolidin-3-yl) propanoate (PH2), 1-(3-bromopropyl)-3-methyl-5,5-diphenylimidazolidine-2,4-dione (PH3) and 1-(4-bromobutyl)-3-methyl-5,5-diphenylimidazolidine-2,4-dione (PH4) on regulated cell death, the cell cycle and cell ultrastructure was assessed. MATERIALS AND METHODS: The experiments were performed in vitro on HL-60 and U937 cells, using flow cytometry and electron microscopy methods...
November 2017: Anticancer Research
https://www.readbyqxmd.com/read/29058998/liquid-chromatography-tandem-mass-spectrometry-lc-ms-ms-and-dried-blood-spot-sampling-applied-to-pharmacokinetics-studies-in-animals-correlation-of-classic-and-block-design
#20
Matías N Baldo, Emmanuel Angeli, Natalia C Gareis, Gabriel A Hunzicker, Marcelo C Murguía, Hugo H Ortega, Gustavo J Hein
A relative bioavailability study (RBA) of two phenytoin (PHT) formulations was conducted in rabbits, in order to compare the results obtained from different matrices (plasma and blood from dried blood spot (DBS) sampling) and different experimental designs (classic and block). The method was developed by liquid chromatography tandem-mass spectrometry (LC-MS/MS) in plasma and blood samples. The different sample preparation techniques, plasma protein precipitation and DBS, were validated according to international requirements...
January 1, 2017: Laboratory Animals
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