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anesthetic pharmacology

Jukka Kortelainen, Eero Väyrynen, Usko Huuskonen, Jouko Laurila, Juha Koskenkari, Janne T Backman, Seppo Alahuhta, Tapio Seppänen, Tero Ala-Kokko
BACKGROUND: Slow waves (less than 1 Hz) are the most important electroencephalogram signatures of nonrapid eye movement sleep. While considered to have a substantial importance in, for example, providing conditions for single-cell rest and preventing long-term neural damage, a disturbance in this neurophysiologic phenomenon is a potential indicator of brain dysfunction. METHODS: Since, in healthy individuals, slow waves can be induced with anesthetics, the authors tested the possible association between hypoxic brain injury and slow-wave activity in comatose postcardiac arrest patients (n = 10) using controlled propofol exposure...
October 5, 2016: Anesthesiology
Srivishnu Vardhan Yallapragada, Nagendra Nath Vemuri, Mastan Saheb Shaik
CONTEXT: The purpose of adding an adjuvant to local anesthetic in a central neuraxial blockade is to augment the desirable pharmacological actions of the agent and/or to minimize its undesirable pharmacological effects. Clonidine is an alfa-2 receptor agonist which has gained popularity in recent times as an adjuvant in spinal anesthesia. AIMS: To evaluate the influence of clonidine on the hemodynamic stability and the duration of anesthesia when added to intrathecal hyperbaric bupivacaine...
September 2016: Anesthesia, Essays and Researches
Amit Agrawal, Veena Asthana, J P Sharma, Vineeta Gupta
BACKGROUND: Subarachnoid block is the preferred technique for providing anesthesia for patients undergoing cesarean section. Various pharmacological agents in added to local anesthetics (LA) modify their original effects in terms of block characteristics and quality of analgesia. However, there is ongoing debate about this practice of using adjuncts with LA. We tested whether addition of lipophilic versus lipophobic opioids to LA gives any clinical benefits to maternal and fetal outcome when used in these patients requiring spinal anesthesia...
September 2016: Anesthesia, Essays and Researches
Maximilian H Beck, Jens K Haumesser, Johanna Kühn, Jennifer Altschüler, Andrea A Kühn, Christoph van Riesen
Abnormally enhanced beta oscillations have been found in deep brain recordings from human Parkinson's disease (PD) patients and in animal models of PD. Recent correlative evidence suggests that beta oscillations are related to disease-specific symptoms such as akinesia and rigidity. However, this hypothesis has also been repeatedly questioned by studies showing no changes in beta power in animal models using an acute pharmacologic dopamine blockade. To further investigate the temporal dynamics of exaggerated beta synchrony in PD, we investigated the reserpine model, which is characterized by an acute and stable disruption of dopamine transmission, and compared it to the chronic progressive 6-hydroxydopamine (6-OHDA) model...
October 12, 2016: Experimental Neurology
Yoshiro Tomimatsu, Diana Cash, Motohisa Suzuki, Kazunori Suzuki, Michel Bernanos, Camilla Simmons, Steven C R Williams, Haruhide Kimura
TAK-063 is a selective phosphodiesterase 10A (PDE10A) inhibitor that produces potent antipsychotic-like and pro-cognitive effects at 0.3mg/kg (26% PDE10A occupancy in rats) or higher in rodents through the balanced activation of the direct and indirect pathways of striatal medium spiny neurons (MSNs). In this study, we evaluated the specific binding of TAK-063 using in vitro autoradiography (ARG) and the modulation of brain activity using pharmacological magnetic resonance imaging (phMRI) and electroencephalography (EEG)...
October 8, 2016: Neuroscience
Lourdes Dias, Mariana A P Rodrigues, Bruna R Inoue, Renata L Rodrigues, André L Rennó, Valéria B de Souza, Frank D Torres-Huaco, Norma C Sousa, Alessandra Stroka, Anibal R Melgarejo, Stephen Hyslop
In this work, we examined some mechanisms involved in the hypotension caused by Lachesis muta (South American bushmaster) venom in anesthetized rats. Venom (1.5 mg/kg, i.v.) caused immediate hypotension that was maximal after 5 min and gradually returned to baseline over 60 min. Pretreatment of rats with the non-selective nitric oxide synthase (NOS) inhibitor N(ω)-nitro-L-arginine methyl ester (L-NAME) did not attenuate the early phase of venom-induced hypotension, but abolished the recovery phase and resulted in rapid death; a similar effect was observed with the soluble guanylate cyclase (sGC) inhibitor ODQ...
October 5, 2016: Toxicon: Official Journal of the International Society on Toxinology
Keith L Shelton
Inhalants are a loosely organized category of abused compounds defined entirely by their common route of administration. Inhalants include volatile solvents, fuels, volatile anesthetics, gasses, and liquefied refrigerants, among others. They are ubiquitous in modern society as ingredients in a wide variety of household, commercial, and medical products. Persons of all ages abuse inhalants but the highest prevalence of abuse is in younger adolescents. Although inhalants have been shown to act upon a host of neurotransmitter receptors, the stimulus effects of the few inhalants which have been trained or tested in drug discrimination procedures suggest that their discriminative stimulus properties are mediated by a few key neurotransmitter receptor systems...
October 7, 2016: Current Topics in Behavioral Neurosciences
John R Richards, Erik G Laurin, Nabil Tabish, Richard A Lange
BACKGROUND: Topical cocaine is sometimes used for the treatment of epistaxis, as it has both potent anesthetic and vasoconstrictive properties. Cocaine has unpredictable cardiovascular effects, such as sudden hypertension, tachycardia, coronary arterial vasoconstriction, and dysrhythmia. CASE REPORT: We report a case of acute iatrogenic cardiovascular toxicity from the use of topical cocaine in a 56-year-old man presenting to the Emergency Department with profound epistaxis...
September 29, 2016: Journal of Emergency Medicine
Olga A Lyubashina, Sergey S Panteleev, Alexey Y Sokolov
Electrical stimulation of the greater occipital nerve (GON) has recently shown promise as an effective non-pharmacological prophylactic therapy for drug-resistant chronic primary headaches, but the neurobiological mechanisms underlying its anticephalgic action are not elucidated. Considering that the spinal trigeminal nucleus (STN) is a key segmental structure playing a prominent role in pathophysiology of headaches, in the present study we evaluated the effects of GON electrical stimulation on ongoing and evoked firing of the dura-sensitive STN neurons...
September 27, 2016: Journal of Neural Transmission
Masoumeh Nazari, Alireza Komaki, Iraj Salehi, Abdolrahman Sarihi, Siamak Shahidi, Hamidreza Komaki, Ahmad Gangi
Long-term potentiation (LTP), a form of synaptic plasticity, is considered to be a critical cellular mechanism that underlies learning and memory. Cannabinoid CB1 and metabotropic GABAB receptors display similar pharmacological effects and co-localize in certain brain regions. In this study, we examined the effects of co-administration of the CB1 and GABAB antagonists AM251 and baclofen, respectively, on LTP induction in the rat dentate gyrus (DG). Male Wistar rats were anesthetized with urethane. A stimulating electrode was placed in the lateral perforant path (PP), and a bipolar recording electrode was inserted into the DG until maximal field excitatory postsynaptic potentials (fEPSPs) were observed...
September 20, 2016: Brain Research
Akbar Ahmad, Csaba Szabo
Hydrogen sulfide (H2S) exerts beneficial as well as deleterious effects in various models of critical illness. Here we tested the effect of two different pharmacological interventions: (a) inhibition of H2S biosynthesis using the cystathionine-beta-synthase (CBS)/cystathionine-gamma-lyase (CSE) inhibitor aminooxyacetic acid (AOAA) and the mitochondrially targeted H2S donor [10-oxo-10-[4-(3-thioxo-3H-1,2-dithiol-5-yl)phenoxy]decyl]triphenyl-phosphonium (AP39). A 30% body surface area burn injury was induced in anesthetized mice; animals were treated with vehicle, AOAA (10mg/kg i...
September 14, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Badri Prasad Das, Anil Prasad Singh, Ram Badan Singh
INTRODUCTION: Underdevelopment of the lung parenchyma associated with abnormal growth of pulmonary vasculature in neonates with congenital diaphragmatic hernia results in pulmonary hypertension which mandates smooth elective mechanical ventilation in postoperative period, for proper alveolar recruitment and oxygenation, allowing lungs to mature enough for its functional anatomy and physiology. Dexmedetomidine is sympatholytic, reduces pulmonary vascular resistance and exerts sedative and analgesic property to achieve stable hemodynamics during elective ventilation...
June 2016: Anesthesiology and Pain Medicine
Martín Galvalisi, José Pedro Prieto, Marcela Martínez, Juan Andrés Abin-Carriquiry, Cecilia Scorza
Oral, intraperitoneal, or intravenous have been the common routes of administration used to study the behavioral and neurochemical pharmacology of caffeine, one of the most widely used psychoactive substances worldwide. We have reported that caffeine is an active adulterant frequently found in coca-paste (CP)-seized samples, a highly addictive form of smokable cocaine. The role of caffeine in the psychostimulant and neurochemical effects induced by CP remains under study. No preclinical animal studies have been performed so far to characterize the effects of caffeine when it is administered through the pulmonary inhalation route...
September 8, 2016: Neurotoxicity Research
Raffael Vorberg, Nils Trapp, Daniel Zimmerli, Björn Wagner, Holger Fischer, Nicole A Kratochwil, Manfred Kansy, Erick M Carreira, Klaus Müller
The modulation of pharmacologically relevant properties of N-alkyl-piperidine-2-carboxamides was studied by selective introduction of 1-3 fluorine atoms into the n-propyl and n-butyl side chains of the local anesthetics ropivacaine and levobupivacaine. The basicity modulation by nearby fluorine substituents is essentially additive and exhibits an exponential attenuation as a function of topological distance between fluorine and the basic center. The intrinsic lipophilicity of the neutral piperidine derivatives displays the characteristic response noted for partially fluorinated alkyl groups attached to neutral heteroaryl systems...
October 6, 2016: ChemMedChem
Jingkao Chen, Yunling Dou, Xiaoke Zheng, Tiandong Leng, Xiaofang Lu, Ying Ouyang, Huawei Sun, Fan Xing, Jialuo Mai, Jiayu Gu, Bingzheng Lu, Guangmei Yan, Jun Lin, Wenbo Zhu
The melastatin-like transient receptor potential 7 (TRPM7) has been implicated in proliferation or apoptosis of some cancers, indicating the potential of TRPM7 as an anti-anaplastic target. Here, we identified the characteristic TRPM7 channel currents in human malignant glioma MGR2 cells, which could be blocked by a pharmacologic inhibitor Gd(3+). We mined the clinical sample data from Oncomine Database and found that human malignant glioma tissues expressed higher TRPM7 mRNA than normal brain ones. Importantly, we identified a widely used clinical anesthetic midazolam as a TRPM7 inhibitor...
September 14, 2016: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
Vanessa Orsini, Stefan Zurbruegg, Monika Pikiolek, Jan S Tchorz, Nicolau Beckmann
RATIONALE AND OBJECTIVES: The study aimed to validate magnetic resonance imaging (MRI)-based liver volumetry as a quantitative measure of hepatic regeneration in mice subjected to partial hepatectomy, in view of routine in vivo pharmacologic studies characterizing compounds aiming to accelerate liver regeneration. MATERIALS AND METHODS: Partial hepatectomy was performed in male B6 mice (n = 47). Images were acquired in 14.5 minutes from anesthetized and spontaneously respiring animals, without any gating and without administration of contrast material...
August 29, 2016: Academic Radiology
Aiwei Li, Vivian Man Ying Yuen, Sophie Goulay-Dufay, Philip Chi Lip Kwok
Dexmedetomidine is an alpha 2-adrenoceptor agonist and has been used as a general anesthetic, sedative, and analgesic for about thirty years. The aim of this paper is to review the pharmacokinetics and pharmacodynamics of dexmedetomidine, evaluate physiological factors that may affect the pharmacokinetics of dexmedetomidine, and summarize the pharmacodynamics of dexmedetomidine at different plasma levels. The pharmacokinetic parameters reported in previous studies according to non-compartmental analyses or population modeling results are compared...
September 5, 2016: Drug Development and Industrial Pharmacy
Heidi L Lujan, Joshua P Rivers, Stephen E DiCarlo
Mice may now be the preferred animal model for biomedical research due to its anatomical, physiological, and genetic similarity to humans. However, little is known about accentuated antagonism of chronotropic and dromotropic properties in conscious mice. Accordingly, we describe the complex and interacting influence of the autonomic nervous system on cardiac electrophysiology in conscious mice. Specifically, we report the effects of single and combined cardiac autonomic blockade on measurements of pulse interval (heart rate), atrio-ventricular interval, sinus node recovery time (SNRT), SNRT corrected for spontaneous sinus cycle, and Wenckebach cycle length in conscious mice free of the confounding influences of anesthetics and surgical trauma...
August 29, 2016: Autonomic Neuroscience: Basic & Clinical
C Boiteux, T W Allen
Sodium channels are chief proteins involved in electrical signaling in the nervous system, enabling critical functions like heartbeat and brain activity. New high-resolution X-ray structures for bacterial sodium channels have created an opportunity to see how these proteins operate at the molecular level. An important challenge to overcome is establishing relationships between the structures and functions of mammalian and bacterial channels. Bacterial sodium channels are known to exhibit the main structural features of their mammalian counterparts, as well as several key functional characteristics, including selective ion conduction, voltage-dependent gating, pore-based inactivation and modulation by local anesthetic, antiarrhythmic and antiepileptic drugs...
2016: Current Topics in Membranes
B S Zhorov, D B Tikhonov
Voltage-gated sodium channels are targets for many toxins and medically important drugs. Despite decades of intensive studies in industry and academia, atomic mechanisms of action are still not completely understood. The major cause is a lack of high-resolution structures of eukaryotic channels and their complexes with ligands. In these circumstances a useful approach is homology modeling that employs as templates X-ray structures of potassium channels and prokaryotic sodium channels. On one hand, due to inherent limitations of this approach, results should be treated with caution...
2016: Current Topics in Membranes
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