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ketamine pharmacology

Solina Tith, Garinder Bining, Laurent Bollag
Background : Opioid use during pregnancy is a growing concern in the United States. Buprenorphine has been recommended by "The American College of Obstetrics and Gynecology" as an alternative to methadone to decrease risks associated with the use of illicit opioids during pregnancy. The partial μ-opioid agonists' unique pharmacology, including its long half time and high affinity to the μ-opioid receptor, complicates patient management in a highly kinetic, and often urgent field like obstetric anesthesia...
2018: F1000Research
Panos Zanos, Scott M Thompson, Ronald S Duman, Carlos A Zarate, Todd D Gould
Traditional pharmacological treatments for depression have a delayed therapeutic onset, ranging from several weeks to months, and there is a high percentage of individuals who never respond to treatment. In contrast, ketamine produces rapid-onset antidepressant, anti-suicidal, and anti-anhedonic actions following a single administration to patients with depression. Proposed mechanisms of the antidepressant action of ketamine include N-methyl-D-aspartate receptor (NMDAR) modulation, gamma aminobutyric acid (GABA)-ergic interneuron disinhibition, and direct actions of its hydroxynorketamine (HNK) metabolites...
March 7, 2018: CNS Drugs
Yonglai Zhang, Rui Sha, Kaiguo Wang, Hao Li, Bo Yan, Naibao Zhou
Tetrahydropalmatine exerts numerous pharmacological activities, including analgesic and narcotic effects; anti-arrhythmic, blood pressure lowering and cardioprotective effects; protective effects against cerebral ischemia-reperfusion injury; inhibition of platelet aggregation; prevention of ulcerative diseases and inhibition of gastric acid secretion; antitumor effects; and beneficial effects on the withdrawal symptoms associated with drug addiction. The present study aimed to investigate the protective effects of tetrahydropalmatine against ketamine‑induced learning and memory impairment in mice...
March 7, 2018: Molecular Medicine Reports
Logan J Voss, Sebastian Karalus, Vilhelm Englund, James W Sleigh
BACKGROUND: Ketamine is a general anesthetic thought to act by antagonizing N-methyl-D-aspartate receptors. However, ketamine acts on multiple channels, many of which are potential targets-including hyperpolarization-activated cyclic nucleotide-gated and potassium channels. In this study we tested the hypothesis that potassium leak channels contribute to the anesthetic action of ketamine. METHODS: Adult mouse cortical slices (400 µm) were exposed to no-magnesium artificial cerebrospinal fluid to generate seizure-like event activity...
March 6, 2018: Anesthesiology
Brian Wilkinson, James Garwood, Stephen Langford
OBJECTIVE: Patients can be transferred many hundreds of kilometers with acute mental health disturbance for specialist mental health services in Western Australia. METHODS: A retrospective notes review of Royal Flying Doctor Service Western Operations records was undertaken over a 4-month period. Patients were identified from the transfer database by mental health diagnosis. Benzodiazepine and antipsychotic doses were converted into a reference drug per class for comparison...
March 2018: Air Medical Journal
Caio Átila Prata Bezerra Souza, Breytiner Amaro de Oliveira, Sacha Aubrey Alves Rodrigues Santos, Francisco Lucas Alves Batista, Francisco Regivânio Nascimento Andrade, Eugênio Januário Ramos Neto, José de Maria Albuquerque de Melo Júnior, Francisco Rogenio da Silva Mendes, Lana Karine Vasconcelos Barroso, Kirley Marques Canuto, Francisco Ernani Alves Magalhães, Angelo Roncalli Alves E Silva, Wladimir Ronald Lobo Farias, Adriana Rolim Campos
This study aimed to evaluate the antinociceptive effect of sulphated polysaccharide from the marine algae Hypnea pseudomusciformis (PLS) using rodent models of orofacial pain. Acute pain was induced by formalin, capsaicin, cinnamaldehyde, acidified saline or glutamate (cutaneous modes) and hypertonic saline (corneal model). In one experiment, animals were pretreated with ruthenium red, glibenclamide, naloxone, L-NAME, methylene blue or ketamine to investigate the mechanism of antinociception. In another experiment, animals pretreated with PLS or saline were submitted to the temporomandibular joint formalin test...
February 19, 2018: Inflammopharmacology
Sebastiano Mercadante
BACKGROUND: Oral opioids or other pharmacological or non-pharmacological interventions are often suggested in the management of breakthrough cancer pain (BTcP). The aim of this systematic and critical review was to analyse and critically comment the evidence of any non-fentanyl therapies proposed for BTcP. METHODS: A systematic literature search was carried out to find studies providing clinical data on any treatment excluding fentanyl products. RESULTS: No data exist about the use of oral opioids...
February 2018: Critical Reviews in Oncology/hematology
Masami Sato, Hiroaki Yasumoto, Toshiyuki Arai
Anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis is an autoimmune disorder caused by production of anti-NMDAR antibodies that is often associated with ovarian teratoma and exhibits various manifestations including psychiatric symptoms, seizures, hypoventilation, and autonomic nerve instability. Patients with this disorder who receive early surgical tumor resection along with immunotherapy have better outcome than the rest of the patients. To establish an anesthetic plan, it is important to understand the pharmacological interaction between the anesthetic agents and the disabled NMDAR, because NMDAR is one of the major sites of action for commonly-used anesthetic agents...
2018: JA Clin Rep
Yan Yang, Yihui Cui, Kangning Sang, Yiyan Dong, Zheyi Ni, Shuangshuang Ma, Hailan Hu
The N-methyl-d-aspartate receptor (NMDAR) antagonist ketamine has attracted enormous interest in mental health research owing to its rapid antidepressant actions, but its mechanism of action has remained elusive. Here we show that blockade of NMDAR-dependent bursting activity in the 'anti-reward center', the lateral habenula (LHb), mediates the rapid antidepressant actions of ketamine in rat and mouse models of depression. LHb neurons show a significant increase in burst activity and theta-band synchronization in depressive-like animals, which is reversed by ketamine...
February 14, 2018: Nature
Atsushi Tsukamoto, Natsuko Niino, Mizuho Sakamoto, Risa Ohtani, Tomo Inomata
To achieve surgical anesthesia in animal experimentation, it is necessary to select the appropriate anesthetic protocol by considering its pharmacological properties and the surgical procedure to be performed. However, few studies have investigated the validity of anesthetic protocols under surgical conditions in small rodents. The present study aimed to clarify the pharmacological properties of 4 anesthetic protocols during the surgical procedure of castration in rats. Eight-week-old male Wistar rats were anesthetized with anesthetics, including the combination of ketamine and xylazine (K/X), the combination of medetomidine, midazolam, and butorphanol (M/M/B), and isoflurane, and sevoflurane...
February 14, 2018: Experimental Animals
Nobue Kitanaka, Junichi Kitanaka, F Scott Hall, Yoshiro Kubota, Yumi Mimura, Sayaka Ogura, Yukiya Okada, George R Uhl, Motohiko Takemura
A single administration of mice with memantine (1-amino-3,5-dimethyladamantane), a glutamatergic N-methyl-d-aspartate (NMDA) receptor antagonist, induced stereotyped behaviors in dose- and time-dependent manners. The predominant behavioral component of the stereotypy was a continuous, exaggerated sniffing which was accompanied by persistent locomotion. In contrast, a psychostimulant methamphetamine (METH) predominantly induced a stereotyped biting and other forms of intense stationary stereotypical behaviors...
April 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Robert Hofstetter, Georg M Fassauer, Andreas Link
On-line solid-phase supercritical fluid extraction (SFE) and chromatography (SFC) coupled to mass spectrometry (MS) has been evaluated for its usefulness with respect to metabolic profiling and pharmacological investigations of ketamine in humans. The aim of this study was to develop and validate a rapid, highly selective and sensitive SFE-SFC-MS method for the quantification of ketamine and its metabolites in miniature amounts in human urine excluding liquid-liquid extraction (LLE). Several conditions were optimized systematically following the requirements of the European Medicines Agency: selectivity, carry-over, calibration curve parameters (LLOQ, range and linearity), within- and between-run accuracy and precision, dilution integrity, matrix effect, and stability...
February 15, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Michael Gottlieb, Brit Long, Alex Koyfman
BACKGROUND: Acute agitation is a common occurrence in the emergency department (ED) that requires rapid assessment and management. OBJECTIVE: This review provides an evidence-based summary of the current ED evaluation and management of acute agitation. DISCUSSION: Acute agitation is an increasingly common presentation to the ED and has a broad differential diagnosis including metabolic, neurologic, infectious, toxicologic, and psychiatric etiologies...
January 29, 2018: Journal of Emergency Medicine
Sergio Terracina, Chiara Robba, Anna Prete, Paola G Sergi, Federico Bilotta
BACKGROUND AND OBJECTIVE: In the last decades, in developed countries, spine procedures (surgical and percutaneous) had the highest absolute increase in case volume trend. Optimal approach to prevent and treat postoperative pain is continuously evolving. This systematic literature review presents evidence on safety and efficacy of pharmacological and non-pharmacological therapies to prevent and treat postoperative pain after lumbar spine procedures. DATABASES AND DATA TREATMENT: Publications listed in PUBMED and EMBASE were considered to identify randomized clinical trials suitable for inclusion in this systematic review...
February 2, 2018: Pain Practice: the Official Journal of World Institute of Pain
Frank Birklein, Violeta Dimova
Complex regional pain syndrome (CRPS) was described for the first time in the 19th century by Silas Weir Mitchell. After the exclusion of other causes, CRPS is characterised by a typical clinical constellation of pain, sensory, autonomic, motor, or trophic symptoms which can no longer be explained by the initial trauma. These symptoms spread distally and are not limited to innervation territories. If CRPS is not improved in the acute phase and becomes chronic, the visible symptoms change throughout because of the changing pathophysiology; the pain, however, remains...
November 2017: Pain Reports (Baltimore, Md.)
Vitor Silva Pereira, Vinícius Antonio Hiroaki-Sato
OBJECTIVE: Although monoaminergic-targeted drugs have prompted great advances in the development of treatments for depression, the need for new options persists, since these drugs still have a delayed clinical effect and most patients do not respond properly to them. Recently, the observation of the antidepressant effects of ketamine brought on a new wave of studies regarding the comprehension of the neurobiology of depression and the development of new and more effective antidepressant drugs...
February 1, 2018: Acta Neuropsychiatrica
Haiying Tang, Daniel Kukral, Yu-Wen Li, Matthew Fronheiser, Harold Malone, Adrienne Pena, Rick Pieschl, Kurex Sidik, Gabriel Tobon, Patrick L Chow, Linda J Bristow, Wendy Hayes, Feng Luo
Major depressive disorder is a leading cause of disability globally. Improvements in the efficacy of antidepressant therapy are needed as a high proportion (>40%) of individuals with major depressive disorder fail to respond adequately to current treatments. The non-selective N-methyl-D-aspartate receptor channel blocker, (±)-ketamine, has been reported to produce a rapid and long-lasting antidepressant response in treatment-resistant major depressive disorder patients, which provides a unique opportunity for investigation of mechanisms that mediate its therapeutic effect...
January 1, 2018: Journal of Psychopharmacology
Bernhard Wünsch, Louisa Temme, Dirk Schepmann, Julian A Schreiber, Bastian Frehland
Since only a few studies investigated the affinity and functional activity of NMDA receptor open channel blockers under same assay conditions, a comparative study of common open channel blockers is of major interest. The pharmacological activity of MK-801, phencyclidine, dexoxadrol, etoxadrol, (S)- and (R)-ketamine, dextromethorphan, memantine and amantadine was analyzed under same uniform assay conditions. The affinity towards the PCP and ifenprodil binding sites was recorded in radioligand binding assays...
January 27, 2018: ChemMedChem
Martin Holtkamp
Patients with prolonged seizures that do not respond to intravenous benzodiazepines and a second-line anticonvulsant suffer from refractory status epilepticus and those with seizures that do not respond to continuous intravenous anesthetic anticonvulsants suffer from super-refractory status epilepticus. Both conditions are associated with significant morbidity and mortality. A strict pharmacological treatment regimen is urgently required, but the level of evidence for the available drugs is very low. Refractory complex focal status epilepticus generally does not require anesthetics, but all intravenous non-anesthetizing anticonvulsants may be used...
January 24, 2018: Drugs
Amir H Rezvani, Yousef Tizabi, Susan Slade, Bruk Getachew, Edward D Levin
Smoking cessation strategies are of prime medical importance. Despite availability of various pharmacological agents in combating addiction to nicotine, more effective medications are needed. Based on recent findings, the glutamatergic system in the brain may provide novel targets. Here, we evaluated the effects of acute administration of sub-anesthetic doses of ketamine, an NMDA receptor antagonist, in both male and female Sprague-Dawley rats trained to self-administer nicotine. Animals were injected subcutaneously with 5, 7...
January 12, 2018: Neuroscience Letters
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