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Fundamental & Clinical Pharmacology

Wenting Ai, Min Wu, Lin Chen, Baozhou Jiang, Mian Mu, Lihua Liu, Zuyi Yuan
The effects of ghrelin, a peptide hormone, on atherogenesis are mainly beneficial. This study aimed to investigate whether ghrelin ameliorates atherosclerosis (AS) by preventing endoplasmic reticulum stress (ERS). AS was induced by a high-fat diet in ApoE(-/-) mice. AS lesions in aortas were detected by Oil-red O staining, and the inner diameter and intima-media thickness (IMT) of the abdominal aorta were analyzed by ultrasonography. The protein expression of the ERS markers 78-kDa glucose-regulated protein, C/EBP homologous protein, and active caspase-12 was detected by western blot analysis...
October 18, 2016: Fundamental & Clinical Pharmacology
Majid Motaghinejad, Manijeh Motevalian, Behnaz Shabab
Neurodegeneration induced by methylphenidate (MPH), as a central stimulant with unknown long-term consequences, in adult rats' brain and the possible mechanisms involved were studied. Rats were acutely treated with MPH in presence and absence of some receptor antagonists such as ketamine, topiramate, yohimibine and haloperidol. Motor activity and anxiety level in rats were monitored. Anti-oxidant and inflammatory parameters were also measured in isolated hippocampus and cerebral cortex. MPH treated groups (10 and 20 mg/kg) demonstrated anxiety-like behavior and increased motor activity...
October 14, 2016: Fundamental & Clinical Pharmacology
Sonia Goineau, Vincent Castagné
Gastric mucosa is frequently exposed to various gastric irritants and there is a continuing requirement to develop new gastro-protective agents. The present study compares the effects of three such agents, sucralfate, rebamipide and cimetidine in both in vivo and in vitro indomethacin-induced gastric damage models. For the in vivo approach, rats were orally administered sucralfate, rebamipide and cimetidine at 300 mg/kg before an acute dose of indomethacin (30 mg/kg). Gastric lesions were then macroscopically examined...
October 14, 2016: Fundamental & Clinical Pharmacology
Elham Kordijaz, Ali Moghimi, Masoud Fereidoni, Saeedeh Asadi, Ali Shamsizadeh, Ali Roohbakhsh
Convulsive seizures are due to abnormal synchronous and repetitive neuronal discharges in the central nervous system (CNS). Finding new therapeutics to overcome the side effects of the current drug therapies and to increase their effectiveness is ongoing. Orexin-A and orexin-B are brain neuropeptides originating from postero-lateral hypothalamic neurons. Studies show that orexins, through activation of OX1 and OX2 receptors, have excitatory effects in the CNS. Accordingly, the present study was designed to evaluate the effect of OX1 receptor antagonist (SB-334867) on seizure- and anxiety-related behaviors of pentylenetetrazol (PTZ) kindled rats...
October 14, 2016: Fundamental & Clinical Pharmacology
Olivier Colin, Sylvie Favrelière, Alexandre Quillet, Jean-Philippe Neau, Jean-Luc Houeto, Claire Lafay-Chebassier, Marie-Christine Pérault-Pochat
Progressive multifocal leukoencephalopathy (PML) is an often fatal demyelinating disease of the central nervous system. As effective treatment is unavailable, identification of all drugs that could be associated with PML is essential. The objective of this study was to investigate the putative association of reports of PML and drugs. We used the case/noncase method in the French PharmacoVigilance Database (FPVD). Cases were reports of PML in the FPVD between January 2008 and December 2015. Noncases were all other reports during the same period...
October 13, 2016: Fundamental & Clinical Pharmacology
Maud Pétrault, Sophie Gautier, Vincent Bérézowski, Thavarak Ouk, Michèle Bastide, Olivier Pétrault, Régis Bordet
Analgesics such as opioid agonists are usually not given during the post-operative phase of experimental stroke because they are susceptible to interfere with the evaluation of neuroprotective therapies. Here we investigate the potential of acetaminophen and nefopam, two non-opioid analgesic drugs, to exert an analgesic effect without inducing neuroprotection in a murine model of ischemic stroke. We demonstrate that acetaminophen (200 mg/kg, PO) induces a significant decrease in the infarct volume, particularly in the cortex (VEHICLE: 200...
September 30, 2016: Fundamental & Clinical Pharmacology
David Metsu, Patrick Seraissol, Pierre Delobel, Christel Cinq-Frais, Lise Cuzin, Jacques Izopet, Etienne Chatelut, Peggy Gandia
To date, therapeutic drug monitoring (TDM) is carried out with anti-retrovirals and is usually based on total concentrations (Ct). However, for some patients, TDM does not reflect efficacy or the avoidance of toxicity as is the case for atazanavir (ATV), a HIV protease inhibitor. As the unbound concentration (Cu) is the pharmacological active form, the aim of the study was to evaluate the value of Cu and the unbound fraction (fu, fu = Cu / Ct) for the TDM of ATV. The variability of Cu and the corresponding fu of ATV were explored in 43 patients treated with ATV for an average of 13...
September 24, 2016: Fundamental & Clinical Pharmacology
Alireza Partoazar, Sanaz Nasoohi, Sayed Mehdi Rezayat, Kambiz Gilani, Shahram Ejtemaei Mehr, Amir Amani, Nastaran Rahimi, Ahmad Reza Dehpour
Cyclosporin A (CsA) is known as a neuroprotective agent against cerebral ischemia/reperfusion (I/R) in animal models. However, the significant therapeutic effects of CsA have been observed in high systemic doses or manipulating the blood brain barrier (BBB), resulting in systemic side effects and toxicity. Since the liposome nanocarries have been developed for efficient delivery of peptide and proteins, liposomal CsA (Lipo-CsA) could improve cerebral (I/R) injuries. In this study, the liposomal CsA formulation (CsA at dose of 2...
September 12, 2016: Fundamental & Clinical Pharmacology
Amandine Gouverneur, Magali Rouyer, Angela Grelaud, Philip Robinson, Françoise Colombani, Eric Terrebonne, Denis Smith, Annie Fourrier-Réglat, Pernelle Noize
Metastatic colorectal cancer (mCRC) is frequent among elderly patients. However, in the era of new targeted therapies, little is known about real-life mCRC treatment in this population. This study aimed to describe elderly mCRC patients and the current real-life treatment practices. mCRC patients aged ≥65 years were identified using the registry of multidisciplinary team meetings, mandatory for all cancer patients, held between January 1, 2013 and June 30, 2014 at the Bordeaux University Hospital. Data were collected from medical records using a standardized questionnaire...
September 7, 2016: Fundamental & Clinical Pharmacology
Qian Chen, Hong-Jie Qian, Wei Wang, Meng-Qi Zhang, Dong-Ying Lu, Chuan Lu, Jie-Mei Jin, Chao-Ying Hu, Gang-Yi Liu, Jing-Ying Jia, Hong-Chao Zheng, Xue-Ning Li, Chen Yu, Yi-Ping Wang, Yun Liu
Sulcardine sulfate (Sul) is a novel anti-arrhythmic agent as a potential treatment for atrial fibrillation and ventricular arrhythmias. This study was conducted to investigate the pharmacokinetic profile, safety, and tolerability of Sul in healthy Chinese subjects. In this open-label, single-dose, randomized study, 10 healthy subjects were assigned to receive Sul doses of 200, 400, and 800 mg under fasting conditions (Cohorts A, B, and C, respectively) or 400 mg under fed conditions (Cohort D). The study incorporated a crossover design, separated by a seven-day washout period...
September 7, 2016: Fundamental & Clinical Pharmacology
Elodie Cartet-Farnier, Laetitia Goutelle-Audibert, Pascal Maire, Blandine De la Gastine, Sylvain Goutelle
The objectives of this study were to compare the estimations of renal function obtained with six equations, including the Cockcroft-Gault (CG), Modification of Diet in Renal Disease (MDRD), and Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) equations and to evaluate the implication of using other equations for drug dosing in elderly patients in place of CG. An observational prospective study was conducted over 6 months in two geriatric hospitals with inclusions of all hospitalized inpatients. A list of 36 drugs for which recommendations of dosage adjustment for renal function were mentioned in the manufacturer dosing guidelines was used to compare the implications of using the various equations for drug dosing...
September 7, 2016: Fundamental & Clinical Pharmacology
Hesham A Salem, Muhammad Y Al-Shorbagy
Levetiracetam (LEV) is an approved drug for the treatment of some epileptic disorders. With few and controversial reports addressing its possible pharmacodynamic interactions, the current study aimed at studying the effect of LEV on isolated rat duodenal strips to enlighten its possible intestinal adverse effects using the isolated smooth muscle strips of rat duodenum. LEV showed a dose-dependent inhibition in KCl (80 mm)-induced contractions in normal Tyrode's solution. Moreover, preincubation with LEV (3 mm) in K(+) -rich/Ca(2+) -free medium led to a significant decrease in the maximum contractions (Emax ) coupled to a right shift of the cumulative CaCl2 concentration curves implying a possible Ca(2+) channel blocking potential...
September 7, 2016: Fundamental & Clinical Pharmacology
Amélie Daveluy, Elisabeth Frauger, Hélène Peyrière, Christophe Moracchini, Françoise Haramburu, Joëlle Micallef
Addiction to illicit substances or medicines is influenced by cultural, religious, ethnic factors as well as local availability. The purpose of this study was to evaluate the profile of drug users and characteristics of the psychoactive substances used in French overseas territories, using data from the OPPIDUM survey. OPPIDUM is an annual, nationwide, multicentric, cross-sectional study based on specialized care centres that included subjects presenting a drug addiction or under opiate maintenance treatment...
September 1, 2016: Fundamental & Clinical Pharmacology
Lei Li, Xiaojiao Hou, Rongfang Xu, Menbayaer Tu, Chang Liu
Astragalus membranaceus Bunge has been used to treat numerous diseases for thousands of years. As the main active substance of Astragalus membranaceus Bunge, Astragaloside IV (AS-IV) also demonstrates the potent protective effect on focal cerebral ischemia/reperfusion, cardiovascular disease, pulmonary disease, liver fibrosis, and diabetic nephropathy. Based on studies published during the past several decades, the current state of AS-IV research and the pharmacological effects are detailed, elucidated, summarized...
August 27, 2016: Fundamental & Clinical Pharmacology
Xiaolei Hu, Xiaomei Zhang, Guoxi Jin, Zhaoming Shi, Weihua Sun, Fengling Chen
Renal pathology was a commonly seen complication in patients with diabetes. Geniposide (GPO) was previously demonstrated to modulate glucose metabolism in diabetes. This study was to investigate effects of GPO in streptozotocin (STZ) induced diabetic rats and its underlying mechanism. Renal function in diabetic rats was evaluated by levels of serum creatinine (Scr), blood urea nitrogen (BUN) and urinary albumin. Renal inflammation was appraised by inflammatory cells infiltration and pro-inflammatory cytokines production...
August 13, 2016: Fundamental & Clinical Pharmacology
Vitor Won-Held Rabelo, Taísa Fortes Santos, Luciana Terra, Marcos Vinícius Santana, Helena Carla Castro, Carlos Rangel Rodrigues, Paula Alvarez Abreu
CYP51 is an enzyme of sterol biosynthesis pathway present in animals, plants, protozoa and fungi. This enzyme is described as an important drug target that is still of interest. Therefore, in this work we reviewed the structure and function of CYP51 and explored the molecular modeling approaches for the development of new antifungal and antiprotozoans that target this enzyme. Crystallographic structures of CYP51 of some organisms have already been described in the literature, which enable the construction of homology models of other organisms enzymes and molecular docking studies of new ligands...
August 3, 2016: Fundamental & Clinical Pharmacology
Wenbin Ye, Siyuan Zhu, Congrui Liao, Jun Xiao, Qian Wu, Zhen Lin, Jianting Chen
Advanced oxidation production products (AOPPs) have been confirmed to accumulate in patients with rheumatoid arthritis (RA). Previous study demonstrated that AOPPs could accelerate cartilage destruction in rabbit arthritis model. However, the effect of AOPP stimulation on apoptosis of human chondrocyte and the underlying mechanisms remains unclear. This study demonstrated that exposure of chondrocyte to AOPPs resulted in cell apoptosis. AOPP stimulation triggered reactive oxygen species (ROS) production, which induced mitochondrial dysfunction and endoplasmic reticulum stress (ER stress) resulted in caspase activation...
August 2, 2016: Fundamental & Clinical Pharmacology
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...
August 1, 2016: Fundamental & Clinical Pharmacology
Anthony Aiudi, Benjamin Miller, Gopal Krishna, Adedayo Adedoyin, Alan Xiao
Ceftolozane/tazobactam, a novel antibacterial with potent activity against Gram-negative pathogens, was developed for treatment of complicated urinary tract infections, including pyelonephritis, and intra-abdominal infections. A phase 1 pharmacokinetic (PK) study of ceftolozane/tazobactam in healthy Japanese, Chinese, and white volunteers was conducted to assess the potential effect of ethnicity on PK. The PK of ceftolozane, tazobactam and tazobactam metabolite M1 were compared after single 1.5-g and 3-g intravenous doses of ceftolozane/tazobactam...
July 30, 2016: Fundamental & Clinical Pharmacology
Mahshid Tahamtan, Seyed Mostafa Shid Moosavi, Vahid Sheibani, Mohsen Nayebpour, Saeed Esmaeili-Mahani, Mohammad Shabani
Neurologic sequelae remain a common and destructive problem in patients with acute kidney injury. The objective of the present study was to evaluate the possible neuroprotective effect of erythropoietin (EPO) on motor impairments following bilateral renal ischemia (BRI) in two time points after reperfusion: short term (24h) and long term (1w). Male Wistar rats underwent BRI or sham surgery. EPO or saline administration was performed 30 min before surgery (1,000 U/kg, i.p.). Explorative behaviors and motor function of the rats were evaluated by open field, rotarod and wire gripe tests...
July 30, 2016: Fundamental & Clinical Pharmacology
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