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Fundamental & Clinical Pharmacology

Joëlle Micallef, Julien Dupouey, Elisabeth Jouve, Romain Truillet, Bruno Lacarelle, Jack Taillard, Agnès Daurat, Colas Authié, Olivier Blin, Olivier Rascol, Pierre Philip, Daniel Mestre
Driving experiments in real conditions are considered as a "gold standard" to evaluate the effects of drugs on driving performance. Several constraints are difficult to manage in these conditions, so driving simulation appears as the best alternative. A preliminary comparison is crucial before being able to use driving simulation as a valid evaluation method. The aim of this study was to design a driving simulation method for assessing drugs effects on driving. We used cannabis (THC) as a positive control and assessed whether THC affects driving performance in simulation conditions and whether these effects are consistent with performance in real driving conditions...
May 12, 2018: Fundamental & Clinical Pharmacology
Mostafa M Hamdy, Mohamed M Elbadr, Ahmed Barakat
Fluoxetine, a commonly prescribed antidepressant, use in nociceptive pain management represent one of the unsettled issues of fluoxetine therapeutics. By reviewing the literature about fluoxetine's possible roles in this setting; those could be solitary antinociceptive effect, enhancement of acute morphine analgesia, blocking morphine tolerance development, and blocking dependence development and associated abstinence syndrome. In this study, we examined those four alleged roles of fluoxetine. Moreover, since effective alleviation of morphine tolerance, dependence, and abstinence syndrome represents one of the most challenging medical needs, we biochemically analyzed fluoxetine effect on these phenomena...
May 12, 2018: Fundamental & Clinical Pharmacology
Iat-Lon Leong, Tien-Yao Tsai, Kar-Lok Wong, Lian-Ru Shiao, Ka-Shun Cheng, Paul Chan, Yuk-Man Leung
Valproic acid (VA) is currently used to treat epilepsy and bipolar disorder. It has also been demonstrated to promote neuroprotection and neurogenesis. Although beneficial actions of VA on brain blood vessels have also been demonstrated, the effects of VA on brain endothelial cell (EC) Ca2+ signaling is hitherto unreported. In this report we examined the effects of VA on agonist-triggered Ca2+ signaling in mouse cortical bEND.3 EC. While VA (100 μM) did not cause an acute inhibition of ATP-triggered Ca2+ signaling, a 30-min VA treatment strongly suppressed ATP-triggered intracellular Ca2+ release; however, such treatment did not affect Ca2+ release triggered by cyclopiazonic acid, an inhibitor of SERCA Ca2+ pump, suggesting there was no reduction in Ca2+ store size...
May 12, 2018: Fundamental & Clinical Pharmacology
Lei Chen, Hongwen Cao, Chao Yu, Yigeng Feng
Lobaplatin is the third-generation platinum drug that has been shown promising antitumor activity in preclinical studies and clinical trials for multiple human cancers except prostate cancer. In the present study, we investigated the role of lobaplatin on prostate cancer progression and the underlying molecular mechanism. We treated a variety of prostate cancer cell lines with different doses of lobaplatin and examined cell cycle progression, cell apoptosis, cell proliferation and cell migration. Moreover, we also assessed the in vivo antitumor activity of lobaplatin by using xenograft mouse model...
May 7, 2018: Fundamental & Clinical Pharmacology
Johana Béné, Clémentine Rousselin, Haleh Bagheri, Thierry Vial, Sophie Gautier, Marc Lambert
Isolated arthralgia, without hemorrhagic side effect exists and is considered as a very rare adverse drug reaction according to vitamin K antagonists' (VKAs) summary of product characteristics. Up to now, there are no literature reports of isolated, non-hemorrhagic joint complications in patients receiving VKAs. Hence, the objective of this study was to describe cases of VKA-related non-hemorrhagic joint disorders (fluindione, warfarin, and acenocoumarol) reported in the French Pharmacovigilance Database (FPVD)...
May 5, 2018: Fundamental & Clinical Pharmacology
Nidhi Tiwari, Pankaj Bhatia, Amit Kumar, Amteshwar S Jaggi, Nirmal Singh
The present study investigates the potential of Carnosine a histamine precursor, in rat model of bilateral common carotid artery occlusion (BCCAo) induced vascular dementia (VaD). Wistar rats were subjected to BCCAo procedure under anesthesia to induce VaD. The rats were subjected to Morris water-maze (MWM) test (6th day onwards post-surgery). MWM test was employed to assess learning and memory of the animals whereby ELT (escape latency time), TSTQ (time spent in target quadrant) and Path length (distance travelled) taken as important parameters...
April 20, 2018: Fundamental & Clinical Pharmacology
Marwa Y Sallam, Sahar M El-Gowilly, Abdel-Galil A Abdel-Galil, Mahmoud M El-Mas
We have previously shown that cyclosporine (CSA) counteracts cardiovascular manifestations induced by endotoxemia (lipopolysaccharide, LPS) such as hypotension and cardiac autonomic dysfunction in conscious rats. In this study we investigated whether the facilitation of central γ-amino butyric acid (GABA) neurotransmission blunts these favorable influences of CSA. The LPS-CSA interaction was determined in the absence and presence of drugs that activate GABAA or GABAB receptors or elevate synaptic GABA levels in the central nervous system...
April 18, 2018: Fundamental & Clinical Pharmacology
Clément Boidin, Sophie Jenck, Laurent Bourguignon, Sejad Torkmani, Aurore Roussey-Jean, Stanislas Ledochowski, Lucie Marry, Nacim Ammenouche, Hervé Dupont, Frédéric Marçon, Bernard Allaouchiche, Julien Bohé, Alain Lepape, Sylvain Goutelle, Arnaud Friggeri
Amikacin antimicrobial effect has been correlated with the ratio of the peak concentration (Cmax) to the minimum inhibitory concentration. A target Cmax ≥ 60-80 mg/L has been suggested. It has been shown that such target is not achieved in a large proportion of critically ill patients in intensive care units. A retrospective analysis was performed to examine the determinants of Cmax ≥ 80 mg/L on the first peak in 339 critically ill patients treated by amikacin. The influence of available variables on Cmax target attainment was analyzed using a classification and regression tree (CART) and logistic regression...
April 16, 2018: Fundamental & Clinical Pharmacology
Régis Bouquié, Guillaume Deslandes, Hélène Mazaré, Marion Cogné, Julien Mahé, Matthieu Grégoire, Pascale Jolliet
Cannabis is a plant that has been used for centuries to relieve a wide range of symptoms. Since the 1960s, interest in medical research into this plant has grown steadily. Already very popular for recreational use, a growing number of consumers not accustomed to using cannabis for psychoactive purposes, have begun to use it as an alternative or complement to mainstream pharmaceutical medicines. The principal unsubstantiated or "social" uses of cannabis are based mainly on data that is at best controversial, but usually not scientifically proven...
April 16, 2018: Fundamental & Clinical Pharmacology
Amélie Daveluy, Lucie Sauvaget, Angela Bastien, Maryse Lapeyre-Mestre, Cédric Collin, Nathalie Richard, Françoise Haramburu
In France, prescription of narcotics must be written on a tamper-resistant prescription form with specific technical particularities. Dosage and daily dose of medicines shall be written out entirely in letters. These prescription forms are also mandatory for buprenorphine, clorazepate, clonazepam, tianeptine, buccal midazolam and zolpidem owing to traffic, abuse or diversion. In 2012, to assess the use of standard and tamper-resistant prescription forms and the acceptability of the generalization of the latter to all medicines, a national opinion survey was performed, with a postal questionnaire, within 3 randomized samples of 1,500 prescribers (physicians, dentists and midwives)...
March 27, 2018: Fundamental & Clinical Pharmacology
Xu Lu, Rong-Rong Yang, Jin-Lin Zhang, Peng Wang, Yu Gong, Wen-Feng Hu, Yue Wu, Min-Hui Gao, Chao Huang
Depression is a common psychiatric disorder with heavy economic and social burdens. Searching new agents with better antidepressant-like activities is of great significance for depression therapy. Tauroursodeoxycholic acid (TUDCA), a clinical drug for gallstone treatment, possesses neuroprotective effects in different brain disorders. However, whether it affects depression remains unclear. We addressed this issue by evaluating the effect of TUDCA on depression induced by chronic unpredictable stress (CUS). Results showed that TUDCA treatment at 200 but not 100 mg/kg prevented the 5 weeks of CUS-induced increases in the immobile time of C57BL6/J mice in the experiments of forced swimming test and tail suspension test as well as the CUS-induced decrease in sucrose intake and crossing numbers in the open-field test, and did not enhance the antidepressant-like effect of fluoxetine...
March 26, 2018: Fundamental & Clinical Pharmacology
Paula Regina Rodrigues Salgado, Diogo Vilar da Fonsêca, Cynthia Germoglio Farias de Melo, Fagner Carvalho Leite, Adriano Francisco Alves, Paula Benvindo Ferreira, Márcia Regina Piuvezam, Damião Pergentino de Sousa, Reinaldo Nóbrega de Almeida
Epoxy-carvone (EC) has chiral centers that allow generation of stereoisomers, including (+)-cis-EC and (-)-cis-EC, whose effects in the kindling tests have never been studied. Accordingly, this study aims to comparatively investigate the effect of stereoisomers (+)-cis-epoxy-carvone and (-)-cis-epoxy-carvone on behavioral changes measured in scores, in the levels of cytokines (IL-1β, IL-6 and TNFα) and neuronal protection in the face of continuous treatment with pentylenetetrazol. Swiss mice were divided into 5 groups (n = 10), receiving vehicle, (+) - cis-EC, (-) - cis-EC (both at the dose of 30 mg / kg) and diazepam (4 mg/kg)...
March 25, 2018: Fundamental & Clinical Pharmacology
Jonaz Font, Mathilda Simeon, Christophe Simard, Stéphane Allouche, Anne-Flore Plane, Virginie Ferchaud, Marie Brionne, René Rouet, Marie Nowoczyn, Alain Manrique, Paolo Emilio Puddu, Paul Milliez, Joachim Alexandre
Whether oral anticoagulants, vitamin K antagonists (VKAs), and nonvitamin K oral anticoagulant (NOACs) frequently prescribed to atrial fibrillation (AF) patients, do themselves have a pro- or anti-arrhythmic effect have never been addressed. Transmembrane action potentials were recorded in an acute rabbit model of superfused pulmonary veins (PVs) sleeves preparations using standard microelectrode technique. Fluindione 10 μm (n = 6) increased the AP (action potential) duration (APD), induced a significantly Vmax depression (from 95 ± 14 to 53 ± 5 V/s, P < 0...
March 11, 2018: Fundamental & Clinical Pharmacology
Iman Fatemi, Sara Heydari, Ayat Kaeidi, Ali Shamsizadeh, Elham Hakimizadeh, Amin Khaluoi, Mohammad Allahtavakoli
Metformin (Met) has been shown to have pleiotropic effects such as neuroprotective, antioxidant, and anti-inflammatory properties making that a potential candidate for the treatment of central nervous system (CNS) disorders. This study was designed to investigate the possible effect of Met on the d-galactose (d-gal)-induced aging in ovariectomized mice. The female mice underwent bilateral ovariectomy. d-gal was administered orally at a dose of 500 mg/kg, and Met was administrated orally at doses of 1 and 10 mg/kg for 6 weeks...
March 7, 2018: Fundamental & Clinical Pharmacology
Gokhan Zengin, Devina Lobine, Adriano Mollica, Marcello Locatelli, Simone Carradori, Mohamad Fawzi Mahomoodally
The ethyl acetate, methanolic, and water extracts of Fibigia eriocarpa were assessed for a panoply of bioactivities. Total phenolic and flavonoid content were quantified as well as individual phenolic compounds by HPLC-DAD. The in vitro antioxidant and enzyme (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, α-amylase, and α-glucosidase) inhibitory potential of the extracts were evaluated. In silico molecular docking was used to investigate possible interaction between dominant compounds and selected enzymes...
March 5, 2018: Fundamental & Clinical Pharmacology
Joseph Rwagitinywa, Maryse Lapeyre-Mestre, Robert Bourrel, Jean-Louis Montastruc, Agnès Sommet
Adherence to antiretroviral (ARV) is crucial to achieve viral load suppression in HIV-infected patients. This study aimed to compare adherence to generic multi-tablet regimens (MTR) vs. brand MTR likely to incorporate ARV drugs without breaking fixed-dose combinations (FDC) and brand single-tablet regimens (STR) likely to incorporate generics by breaking the FDC. Patients aged of 18 years or over exposed to one of the generic or the brand of lamivudine (3TC), zidovudine/lamivudine (AZT/TC), nevirapine (NVP), or efavirenz (EFV), or the brand STR of efavirenz/emtricitabine/tenofovir (EFV/FTC/TDF)...
March 5, 2018: Fundamental & Clinical Pharmacology
Saeed Mehrzadi, Manijeh Motevalian, Mozhgan Rezaei Kanavi, Iman Fatemi, Habib Ghaznavi, Mansoor Shahriari
Diabetic retinopathy (DR) is one of the most common and serious microvascular complications of diabetes. The aim of this study was to evaluate the effects of melatonin (MEL) on retinal injury in diabetic rats. In this study, 21 rats were randomly divided into three groups: control, diabetic, and diabetic + MEL. Streptozotocin was used to induce diabetes at a dose of 50 mg/kg, i.p., and blood glucose was measured to choose the diabetic rats for the study. MEL (20 mg/kg) was given orally for 7 weeks in diabetic rats starting 1 week after induction of diabetes...
March 1, 2018: Fundamental & Clinical Pharmacology
Paul Carrier, Véronique Loustaud-Ratti
No abstract text is available yet for this article.
April 2018: Fundamental & Clinical Pharmacology
Liselotte Pochard, Julie Dupouy, Elisabeth Frauger, Adeline Giocanti, Joëlle Micallef, Maryse Lapeyre-Mestre
Pregnancy can be a motivation for decrease in drug abusing but may also represent a period of high vulnerability for relapse. We aimed to assess psychoactive substance use among women with substance use disorders followed in addiction care centers in France. We analyzed data from women aged 15-44 years included in the 'Observation of illegal drugs and misuse of psychotropic medication (OPPIDUM) survey', an annual cross-sectional survey collecting details on psychoactive substances used. Characteristics of women included in 2005-2012 yearly surveys were compared depending on their pregnant or not pregnant status...
April 2018: Fundamental & Clinical Pharmacology
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