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Fundamental & Clinical Pharmacology

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https://www.readbyqxmd.com/read/28322465/opioid-substitution-therapy-or-hidden-opioids-are-a-minefield-for-nalmefene-an-atypical-case-series-of-11-patients-in-lorraine
#1
Melissa Yéléhé-Okouma, Hervé Martini, Jérémie Lemarié, Pierre Labroca, Nadine Petitpain, Valérie Gibaja, François Paille, Pierre Gillet
Opioid antagonists such as naltrexone and nalmefene are used in drug therapy for alcoholism. Nalmefene, approved in Europe in February 2013 for the reduction of alcohol consumption is used in patients with alcohol dependence. We report 11 cases of opioid withdrawal syndrome after a single dose of nalmefene in patients usually treated with methadone, buprenorphine, but also with fentanyl or loperamide. Nalmefene is both a partial agonist and an antagonist of opioid receptors. Regarding to its opioid antagonist activity, nalmefene is contraindicated in patients with an opioid treatment...
March 21, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28322460/dapsone-induced-agranulocytosis-possible-involvement-of-low-activity-n-acetyltransferase-2
#2
Ines Potočnjak, Robert Likić, Iveta Šimić, Danica Juričić Nahal, Ivana Čegec, Lana Ganoci, Nada Božina
Dapsone-induced agranulocytosis is a rare but potentially fatal adverse drug reaction (ADR). A 45-year old male Caucasian patient developed agranulocytosis caused by dapsone (diamino-diphenyl sulfone) which he was prescribed for leukocytoclastic vasculitis. Patient's treatment consisted of termination of dapsone, antibiotic therapy, and granulocyte colony stimulating factor leading to prompt improvement of symptoms and normalization of laboratory blood values. Diagnostic evaluation revealed methemoglobinemia and excluded glucose-6-phosphate dehydrogenase (G6PD) deficiency...
March 21, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28299825/fingolimod-gilenya-%C3%A2-in-multiple-sclerosis-bradycardia-atrioventricular-blocks-and-mild-effect-on-the-qtc-interval-something-to-do-with-the-l-type-calcium-channel
#3
Sylvie Pilote, Chantale Simard, Benoit Drolet
Cardiac arrhythmias and ECG abnormalities including bradycardia, prolongation of the QT interval and atrioventricular (AV) conduction blocks have been extensively observed with fingolimod, the first marketed oral drug for treating the relapsing-remitting form of multiple sclerosis. The present study was aiming to further elucidate the effects of fingolimod on cardiac electrophysiology at three different levels; 1) in vitro, 2) ex vivo and 3) in vivo. 1) Patch-clamp experiments in whole cell configuration were performed on Cav 1...
March 16, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28299811/the-role-of-interleukin-1b-and-its-antagonist-diacerein-in-estradiol-benzoate-induced-endometrial-hyperplasia-and-atypia-in-female-rats
#4
Marwa M M Refaie, Maram El-Hussieny
Endometrial hyperplasia (EH) is a common gynecological condition and may progress to carcinoma. We investigated the effect of diacerein (DIA) on estradiol benzoate (EB)-induced EH and atypia. DIA (50mg/kg/day) was administered orally to rats for 4 weeks, in the presence or absence of EH induced by intramuscular (im) injection of EB (60μg/100g) 3 times per week for 4 weeks. We measured levels of serum total cholesterol, uterine tissue malondialdehyde (MDA), total nitrites (NOx ), superoxide dismutase (SOD) activity, caspase-3, interleukin-1b (IL-1b) immunoexpressions and histopathology...
March 16, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28295557/parachlorophenylalanine-induced-5-ht-depletion-alters-behavioural-and-brain-neurotransmitters-levels-in-6-hertz-psychomotor-seizure-model-in-mice
#5
Kausar Jahan, Krishna K Pillai, Divya Vohora
The present study was designed to investigate the role of serotonin and other neurotransmitters namely dopamine (DA), histamine, noradrenaline (NA), glutamate and γ-amino-butyric acid (GABA) in the 6-hertz (6 Hz) induced psychomotor seizures in Swiss albino mice. Parachlorophenylalanine (PCPA, 300 mg/kg/day, i.p for 3 days) treated mice were given 6 Hz stimulation. Sodium valproate (SVP) [200 mg/kg/day, p.o for 3 days] was used as a reference anti-epileptic drug. The behavioral changes induced by 6Hz including increased rearing and grooming, Straub's tail, behavioral arrest, stun position etc were amplified by PCPA...
March 10, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28267871/effect-of-bucladesine-pentoxifylline-and-h-89-as-cyclic-adenosine-monophosphate-analog-phosphodiesterase-and-protein-kinase-a-inhibitor-on-acute-pain
#6
Forouz Salehi, Mahshid Sadat Hosseini-Zare, Haleh Aghajani, Yalda Seyedi, Maryam Sadat Hosseini-Zare, Mohammad Sharifzadeh
The aim of the present study was to determine the effects of Cyclic adenosine monophosphate (cAMP) and its dependent pathway on thermal nociception in a mouse model of acute pain. Here we studied the effect of H-89 (protein kinase A inhibitor), Bucladesine (Db-cAMP) (membrane permeable analog of cAMP) and pentoxifylline (PTX) (non-specific phosphodiesterase (PDE) inhibitor) on pain sensation. Different doses of H-89 (0.05, 0.1 and 0.5 mg/100g), PTX (5, 10 and 20 mg/100g), and Db-cAMP (50, 100 and 300 nM/mouse) were administered intraperitoneally (I...
March 7, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28258589/effect-of-dementia-on-receipt-of-influenza-vaccine-a-cohort-study-in-french-older-adults-using-administrative-data-2007-2012
#7
Adeline Gallini, Nicola Coley, Sandrine Andrieu, Maryse Lapeyre-Mestre, Virginie Gardette
Despite guidelines stating the vaccine benefit in this population, older adults with dementia may be less likely to receive influenza vaccine than cognitively intact older adults. But no study has yet reported on vaccine uptake in patients newly diagnosed with dementia or whether years since dementia diagnosis influence vaccine uptake. We conducted a cohort study in the French Health Insurance database (EGB) which contains hospital data and claims for a 1/97(th) random sample of the French population. Diseased subjects were ≥65 years and had a new record of dementia diagnosis between September 1 2007 and August 31 2008...
March 4, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28214375/anti-fatigue-effects-of-troxerutin-on-exercise-endurance-capacity-oxidative-stress-and-mmp-9-levels-in-trained-male-rats
#8
Mohammad Zamanian, Mohammad R Hajizadeh, Ali Esmaeili Nadimi, Ali Shamsizadeh, Mohammad Allahtavakoli
The aim of this study was to investigate effects of troxerutin (TRX) on endurance capacity, oxidative stress and MMP-9 levels in trained male rats. Forty male Wistar rats were divided into five groups. The control (Vehicle) and exercise training (5 days/week) with vehicle treatment (Exercise), exercise training with TRX treatment at 75 (Ex-TRX75), 150 (Ex-TRX150), and 300 mg/kg (Ex-TRX300). The treated groups received TRX by gavage every day while the other groups received water for 30 days. On the 30(th) day, rats were sacrificed immediately after exhaustive swimming test, and some biochemical parameters were measured...
February 18, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28199737/inhibition-of-trpv1-confers-neuroprotection-reduces-tnf-%C3%AE-and-increases-il-10-in-a-rat-stroke-model
#9
Elham Hakimizadeh, Ali Shamsizadeh, Ali Roohbakhsh, Mohammad Kazemi Arababadi, Mohammad Reza Hajizadeh, Mehdi Shariati, Mohammad Reza Rahmani, Mohammad Allahtavakoli
Stroke is a major cause of mortality and long-term disability in adults. TRPV1 plays a crucial role in neuroinflammation. In the current study, the effects of TRPV1 agonist (capsaicin) and antagonist (AMG9810) on cerebral ischemia were investigated. Forty male Wistar rats were assigned to the following experimental groups: sham, vehicle) ischemic), AMG9810 (selective TRPV1 antagonist, 0.5 mg/kg; 3 h after stroke), and capsaicin (1 mg/kg; 3 h after stroke). Stroke was induced by permanent middle cerebral artery occlusion and neurological deficits were evaluated 1, 3, and 7 days after stroke...
February 15, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28186665/dexmedetomidine-enhances-human-lung-fluid-clearance-through-improving-alveolar-sodium-transport
#10
Yong Cui, Yan Ding, Lei Chen, Yue Li, Yan Chun Li, Hongguang Nie
Accumulating evidence shows that dexmedetomidine can attenuate lung edema with acute lung injury in experimental mouse and rat models, but the mechanisms of dexmedetomidine on human alveolar fluid transport are still unknown. We measured the effects of dexmedetomidine on alveolar fluid clearance in human lung lobes ex vivo. Moreover, we measured the regulation of transepithelial Na(+) transport by dexmedetomidine in H441 cells by electrophysiological technique and western blot method. Our results showed that intratracheal instillation of dexmedetomidine markedly increased the re-absorption of 5% bovine serum albumin instillate (19...
February 10, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28186359/testosterone-supplementation-glucocorticoid-milieu-and-bone-homeostasis-in-the-ageing-male
#11
REVIEW
Vladimir Z Ajdžanović, Branko R Filipović, Branka T Šošić Jurjević, Verica Lj Milošević
Male ageing is entwined with a continuous fall in free testosterone levels, which contributes to the pathogenesis of bone loss. Glucocorticoid excess, either dependent on the ageing process or iatrogenically induced, was found to additionally impair the bone structure and metabolism. Cautious testosterone supplementation in this respect may positively affect the glucocorticoid milieu and bone homeostasis, while testosterone-induced changes in the glucocorticoid output could serve as a determinant of bone-related therapeutic outcome...
February 10, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28173624/evidence-for-the-role-of-histaminergic-pathways-in-neuroprotective-mechanism-of-ischemic-postconditioning-in-mice
#12
Indresh Kaur, Amit Kumar, Amteshwar S Jaggi, Nirmal Singh
The present study has been designed to investigate the possible role of histaminergic pathway in neuroprotective mechanism of ischemic postconditioning (iPoCo). Bilateral carotid artery occlusion (BCAO) for 12 min followed by reperfusion for 24 hr was employed to produce I/R induced cerebral injury in NIH mice. iPoCo involving three episodes of carotid artery occlusion and reperfusion of 10 sec each, was instituted immediately after BCAO just before prolonged reperfusion. Cerebral infarct size was measured using triphenyltetrazolium chloride staining...
February 7, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28107553/protective-effect-of-n-n-dimethylthiourea-against-stress-induced-gastric-mucosal-lesions-in-rats
#13
Yoshiji Ohta, Koji Yashiro, Takashi Kobayashi, Kazuo Inui, Junji Yoshino
In the present study, we examined the protective effect of N,N'-dimethylthiourea (DMTU), a scavenger of hydroxyl radical (•OH), against water-immersion restraint stress (WIRS)-induced gastric mucosal lesions in rats. When male Wistar rats fasted for 24 h were exposed to WIRS for 3 h, gastric mucosal lesions occurred with increases in the levels of gastric mucosal myeloperoxidase, an index of tissue neutrophil infiltration, pro-inflammatory cytokines (tumor necrosis factor alpha and interleukin 1beta), lipid peroxide, and NOx (nitrite/nitrate), an index of nitric oxide synthesis, and decreases in the levels of gastric mucosal non-protein SH and vitamin C and gastric adherent mucus...
January 20, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28107550/enhanced-trpc-channel-mediated-ca-2-influx-in-the-cells-with-phospholipase-c-%C3%AE-1-overexpression-its-possible-role-in-coronary-artery-spasm
#14
Kazuo Murakami, Tomohiro Osanai, Makoto Tanaka, Kimitaka Nishizaki, Takahiko Kinjo, Tomohiro Tanno, Yuji Ishida, Akiko Suzuki, Tomohide Endo, Hirofumi Tomita, Ken Okumura
We reported that coronary spasm was induced in the transgenic mice with the increased phospholipase C (PLC)-δ1 activity. We investigated the effect of enhanced PLC-δ1 on Ca(2+) influx and its underlying mechanisms. We used human embryonic kidney (HEK)-293 and coronary arteries-smooth-muscle cells (CASMC). Intracellular free Ca(2+) concentration ([Ca(2+) ]i ) (nM) was measured by fura-2, and Ca(2+) influx was evaluated by the increase in [Ca(2+) ]i after addition of extracellular Ca(2+) . Acetylcholine (ACh) was used to induce Ca(2+) influx...
January 20, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28103649/amlodipine-an-l-type-calcium-channel-blocker-protects-against-chlorpromazine-induced-neurobehavioural-deficits-in-mice
#15
Oluwafemi E Kale, Olufunsho Awodele, Temitope F Ogundare, Martins Ekor
This study investigated the modulatory and chemopreventive benefit of amlodipine (AML), a dihydropyridine calcium channel antagonist, against neurobehavioural abnormalities (NAs) associated with chlorpromazine (CPZ) toxicity in mice. Adult mice were divided into five groups of six animals/group. Group 1 (control) was administered saline (10 mL/kg i.p.). Group 2 received CPZ (2 mg/kg i.p.). Groups 3 and 4 received bromocriptine (BMC, 2.5 mg/kg s.c.) and AML (1 mg/kg s.c.), respectively, while group 5 received their combination...
January 19, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28078787/targeting-nasopharyngeal-carcinoma-by-artesunate-through-inhibiting-akt-mtor-and-inducing-oxidative-stress
#16
Qin Li, Wei Ni, Zhifeng Deng, Minghe Liu, Lazhi She, Qiong Xie
Drug repurposing has become an alternative therapeutic strategy for cancer treatment given the known pharmacokinetics and toxicity. The inhibitory effects of artesunate have been reported in various cancers. In this work, we investigated the effects of artesunate in nasopharyngeal carcinoma (NPC). We demonstrate that artesunate significantly inhibits proliferation via arresting NPC cells at G2/M phase. It also induces apoptosis through caspase-dependent and mitochondria-independent pathways in multiple NPC cell lines...
January 11, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28078759/bufalin-a-bufanolide-steroid-from-the-parotoid-glands-of-the-chinese-toad-inhibits-l-type-ca-2-channels-and-contractility-in-rat-ventricular-myocytes
#17
Tao Song, Xi Chu, Xuan Zhang, Qiong Tao Song, Ying Zhang, Yuanyuan Zhang, Xue Han, Jianping Zhang, Li Chu
Bufalin is a bufanolide steroid compound in Chan Su. Chan Su is a traditional Chinese medicine prepared from the dried white secretion of the auricular and skin glands of toads, and has been used as an Oriental drug. However, the effect of bufalin on cardiac function and its underlying cellular mechanisms remain unclear. Here, we explore the cellular mechanisms of bufalin on myocardial protection via the whole-cell patch-clamp recording and video-based edge detection system. Exposure to bufalin resulted in a concentrated-dependent blockade of ICa-L , with the half-maximal inhibitory concentration (IC50 ) of 60 μM and the maximal inhibitory effect of 71...
January 11, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28036112/protocol-of-glucose-control-safety-and-efficacy-in-type-2-diabetes-a-network-meta-analysis-glucose-dinet-protocol-rational-and-design
#18
REVIEW
Guillaume Grenet, Audrey Lajoinie, Shams Ribault, Gia Bao Nguyen, Thomas Linet, Augustin Metge, Catherine Cornu, Michel Cucherat, Philippe Moulin, François Gueyffier
The aim of this study was to propose a ranking of the currently available antidiabetic drugs, regarding vascular clinical outcomes, in patients with type 2 diabetes, through a network meta-analysis approach. Randomized clinical trials, regardless of the blinding design, testing contemporary antidiabetic drugs, and considering clinically relevant outcomes in patients with type 2 diabetes mellitus will be included. The primary outcomes of this analysis will be overall mortality, cardiovascular mortality, and major cardiovascular events...
December 30, 2016: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28036099/can-drugs-induce-or-aggravate-sleep-apneas-a-case-non-case-study-in-vigibase-%C3%A2-the-who-pharmacovigilance-database
#19
Mélanie Linselle, Agnès Sommet, Emmanuelle Bondon-Guitton, Florence Moulis, Geneviève Durrieu, Justine Benevent, Vanessa Rousseau, Leila Chebane, Haleh Bagheri, François Montastruc, Jean-Louis Montastruc
The potential favorising role of drugs in Sleep Apnea Syndrome (SAS) is unknown. The present study investigates drugs associated with SAS in a pharmacovigilance database. SAS recorded as Adverse Drug Reactions (ADRs) in Vigibase(®) , the WHO pharmacovigilance database (more than 11 million reports), from 1978 to 2015 were selected. The risk of SAS reports was estimated using the case non-case method, with cases being SAS and non-cases all other recorded ADRs. During this 37-year period, 3,325 ADRs including the word SAS were registered (0...
December 30, 2016: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/27477928/what-tendon-pathology-is-seen-on-imaging-in-people-who-have-taken-fluoroquinolones-a-systematic-review
#20
REVIEW
Tina R Lang, Jill Cook, Ebonie Rio, James E Gaida
Fluoroquinolones (FQs) are highly effective broad-spectrum antibiotics. Clinical data reveal an increased incidence of tendon pain and rupture in those taking FQs, yet little is known about tendon structural changes. This review synthesises published data on tendon structural changes in people who have taken FQs. Eight databases were searched for potentially relevant articles (Medline, CINAHL, Biological Abstracts, AMED, Web of Knowledge, SCOPUS, SportDiscus and EMBASE) using MeSH and free-text searches. Inclusion and exclusion criteria determined which articles were used for this review...
February 2017: Fundamental & Clinical Pharmacology
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