Fundamental and Clinical PharmacologyThis is an RSS file. You can use it to subscribe to this data in your favourite RSS reader, such as GoogleReader, or to display this data on your own website or blog. Subscribe to this data using MyMedWorm.Subscribe to this data using GoogleReader.Subscribe to this data using Bloglines.Subscribe to this data using MyYahoo.

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Acute generalized exanthematous pustulosis (AGEP) induced by cefotaximeEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We report a case of acute generalized exanthematous pustulosis (AGEP) after cefotaxime use confirmed by a positive patch test. A 30-year-old woman received cefotaxime, fosfomycin and ciprofloxacin for sinusitis. Twelve days after drug initiation, she developed an extending pustular erythema associated with fever. Laboratory investigations showed marked leukocytosis. His blood chemistry was normal. The histological examination showed parakeratosis, spongiosis and nonfollicular intra-epidermal pustules consistent with AGEP. All medications were withdrawn. The symptoms resolved within 11 days after cefotaxime discontinuation....
Source: Fundamental and Clinical Pharmacology - November 18, 2009 Category: Drugs & Pharmacology Authors: Amel Chaabane, Karim Aouam, Lies Gassab, Leila Njim, Naceur A. Boughattas Source Type: journals

Serum brain-derived neurotrophic factor and platelet activation evaluated by soluble P-selectin and soluble CD-40-ligand in patients with acute myocardial infarctionEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The objective of this study was to evaluate the relationship between BDNF, functional parameters and biological markers associated with inflammatory processes and platelet activation. BDNF serum levels were assessed in patients with acute myocardial infarction (MI) (n = 20) or stable angina pectoris (SAP) (n = 20) who underwent coronary angiography. Serum levels of IL-6, MCP1, sVCAM, soluble CD-40-ligand (sCD40L) and soluble P-selectin (sP-selectin) were measured simultaneously by flux cytometry. Median BDNF levels were higher in the MI than in the SAP group (1730 vs. 877 pg/mL, respectively; P = 0.025). In MI patients, we...
Source: Fundamental and Clinical Pharmacology - November 10, 2009 Category: Drugs & Pharmacology Authors: Luc Lorgis, Sebastien Amoureux, Emmanuel de Maistre, Pierre Sicard, Yannick Bejot, Marianne Zeller, Catherine Vergely, Annabelle Sequeira-Le Grand, Anne-Cécile Lagrost, Juliane Berchoud, Yves Cottin, Luc Rochette Source Type: journals

Anxiolytic-like effect of Carvacrol (5-isopropyl-2-methylphenol) in mice: involvement with GABAergic transmissionEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Carvacrol (5-isopropyl-2-methylphenol) is a monoterpenic phenol present in the essencial oil of many plants. It is the major component of the essential oil fraction of oregano and thyme. This work presents the behavioral effects of carvacrol in animal models of elevated plus maze (EPM), open field, Rotarod and barbiturate-induced sleeping time tests in mice. Carvacrol (CVC) was administered orally, in male mice, at single doses of 12.5; 25 and 50 mg/kg while diazepam 1 or 2 mg/kg was used as standard drug and flumazenil (2.5 mg/kg) was used to elucidate the possible anxiolytic mechanism of CVC on the plus maze test. The re...
Source: Fundamental and Clinical Pharmacology - November 10, 2009 Category: Drugs & Pharmacology Authors: Francisca Helvira Cavalcante Melo, Edith Teles Venâncio, Damião Pergentino de Sousa, Marta Maria de França Fonteles, Silvânia Maria Mendes de Vasconcelos, Glauce Socorro Barros Viana, Francisca Cléa Florenço de Sousa Source Type: journals

Non-competitive interaction between raclopride and spiperone on human D2L-receptors in intact Chinese hamster ovary cellsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We recently investigated the binding properties of the antagonists [3H]-raclopride and [3H]-spiperone to intact Chinese hamster ovary cells expressing recombinant human D2long-dopamine receptors (CHO-D2L cells). Compared with saturation binding with [3H]-raclopride, raclopride reduced [3H]-spiperone binding with to low potency in competition binding experiments. The present findings illustrate the ability of spiperone to inhibit [3H]-raclopride binding non-competitively. While raclopride only decreases the apparent KD of [3H]-raclopride in saturation binding experiments, spiperone only decreases the number of sites to whic...
Source: Fundamental and Clinical Pharmacology - November 10, 2009 Category: Drugs & Pharmacology Authors: Ann Packeu, Jean-Paul De Backer, Georges Vauquelin Source Type: journals

Fatal liver injury associated with clopidogrelEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We report a serious liver injury with fatal outcome in a 63-year-old man developed 19 days after starting clopidogrel for percutaneous coronary stenting. (Source: Fundamental and Clinical Pharmacology)
Source: Fundamental and Clinical Pharmacology - November 6, 2009 Category: Drugs & Pharmacology Authors: Sarrah Kastalli, Sihem el Aïdli, Ahmed Zaïem, Hatem ben Abdallah, Riadh Daghfous Source Type: journals

Pharmacological doses of vitamin A increase caspase-3 activity selectively in cerebral cortexEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Vitamin A exerts a wide range of physiological roles from embryonic to adulthood stages of the mammalian life. However, there is a great concern regarding the deleterious effects of vitamin A use even therapeutically. It was shown that vitamin A induces behavioral impairments, for instance, anxiety-like behavior and depression, in experimental animals and humans. Caspases are enzymes associated with cell death; however, there is a role for such enzymes also in synaptic plasticity. Then, based on previously published data, we have investigated the effects of vitamin A supplementation at clinical doses (1000[ndash]9000 IU/kg...
Source: Fundamental and Clinical Pharmacology - November 4, 2009 Category: Drugs & Pharmacology Authors: Marcos Roberto de Oliveira, Max William Soares Oliveira, José Cláudio Fonseca Moreira Source Type: journals

Toxicological evaluation of azumolene after repeated intraperitoneal administration in ratsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, Az is a safe compound for long-term administration, but does cause a mild, reversible reaction in skeletal muscle and kidney. (Source: Fundamental and Clinical Pharmacology)
Source: Fundamental and Clinical Pharmacology - November 3, 2009 Category: Drugs & Pharmacology Authors: Paula Lima do Carmo, Gisele Zapata-Sudo, Margarete Manhães Trachez, Maria das Graças Fernandes Sales, Roberto Takashi Sudo Source Type: journals

Thrombin-stimulated proliferation is mediated by endothelin-1 in cultured rat gingival fibroblastsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In this study, using cultured rat gingival fibroblasts, we investigated whether thrombin-induced proliferation of gingival fibroblasts is mediated by ET-1. Thrombin-induced proliferation (0.05[ndash]2.5 U/mL). Proliferation was also induced by a PAR1-specific agonist (TFLLR-NH2, 0.1[ndash]30 [mu]m), but not by a PAR2-specific agonist (SLIGRL-NH2). Thrombin (2.5 U/mL) induced an increase in immunoreactive ET-1 expression, which was inhibited by cycloheximide (10 [mu]g/mL), and an increase in preproET-1 mRNA expression, as assessed by reverse transcription polymerase chain reaction. TFLLR-NH2 increased ET-1 release into the ...
Source: Fundamental and Clinical Pharmacology - October 31, 2009 Category: Drugs & Pharmacology Authors: Nozomi Ohuchi, Kazuhiko Hayashi, Keishi Iwamoto, Katsuo Koike, Yasuo Kizawa, Michiyoshi Nukaga, Tomohito Kakegawa, Hajime Murakami Source Type: journals

The antinociceptive effect and adverse drug reactions of oxycodone in human experimental pain in relation to genetic variations in the OPRM1 and ABCB1 genesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The aim of this study was to search for a possible association between the variant allele of the single nucleotide polymorphisms A118G in the OPRM1 gene and C3435T and G2677T/A in the ABCB1 gene and altered antinociceptive effect and adverse drug reactions of oxycodone. Thirty-three healthy subjects exposed to experimental pain including electrical stimulation and the cold pressor test were included. A118G: We found that the variant G allele was associated with reduced antinociceptive effect as measured by pain tolerance thresholds to single electrical nerve stimulation (8% increase vs. 25% for the wild-type carriers, P = ...
Source: Fundamental and Clinical Pharmacology - October 20, 2009 Category: Drugs & Pharmacology Authors: Stine T. Zwisler, Thomas P. Enggaard, Lene Noehr-Jensen, Soeren Mikkelsen, Céline Verstuyft, Laurent Becquemont, Soeren H. Sindrup, Kim Brosen Source Type: journals

Perception of risk of adverse drug reactions: a 3-year follow-up of a cohort of medical studentsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Previous studies have pointed out the question of effective training and information to health professionals on pharmacovigilance. The lack of training is known to induce inadequate use of drugs and noncompliance of patients. Pharmacology teaching is performed in the third year of medical studies at the Toulouse Faculty of Medicine. The aim of the study was to investigate the perception of risk of adverse drug reactions (ADRs) by medical students at the end of the one year pharmacology course and two years later, after clinical training period. Sixty-seven students were interviewed in May 2005 and in October 2007. Visual a...
Source: Fundamental and Clinical Pharmacology - October 20, 2009 Category: Drugs & Pharmacology Authors: Geneviève Durrieu, C. Hurault, C. Damase-Michel, J.L. Montastruc Source Type: journals

Anti-arthritic effect of scopoletin, a coumarin compound occurring in Erycibe obtusifolia Benth stems, is associated with decreased angiogenesis in synoviumEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, scopoletin is capable of ameliorating clinical symptoms of rat adjuvant-induced arthritis, by reducing numbers of new blood vessels in the synovium and the production of important endogenous angiogenic inducers. Therefore, this compound may be a potential agent for angiogenesis-related diseases and could serve as a structural base for screening more potent synthetic analogs. (Source: Fundamental and Clinical Pharmacology)
Source: Fundamental and Clinical Pharmacology - October 20, 2009 Category: Drugs & Pharmacology Authors: Rong Pan, Xing-Hua Gao, Ying Li, Yu-Feng Xia, Yue Dai Source Type: journals

Reduced elimination clearance of micafungin in rats with cholestatic hyperbilirubinemiaEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We examined whether the pharmacokinetic disposition of micafungin (MCFG), an echinocandin class antifungal agent, is altered in hyperbilirubinemia using a rat model prepared by bile duct ligation (BDL). Serum bilirubin levels were increased depending upon the duration of BDL. The elimination rate constant and total body clearance (CLtot) of MCFG were reduced by 24% and 16%, respectively, after BDL for 1 h, but there was no significant change in the apparent volume of distribution at steady-state. The degree of reduction in the CLtot was much greater 7 days after BDL as compared with that 1 h after BDL (44% vs. 16%). Howeve...
Source: Fundamental and Clinical Pharmacology - October 20, 2009 Category: Drugs & Pharmacology Authors: Hiroki Konishi, Keizo Fukushima, Masatomo Sudo, Masaki Sumi, Tokuzo Minouchi, Ikumi Iga, Nobuhito Shibata, Kanji Takada, Akira Yamaji Source Type: journals

Drug reimbursement and GPs' prescribing decisions: a randomized case-vignette study about the pharmacotherapy of obesity associated with type 2 diabetes: how GPs react to drug reimbursementEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study sought to identify the effect of drug reimbursability [ndash] a decision made in France by the National Authority for Health [ndash] on physicians' prescribing practices for a diet drug such as rimonabant, approved for obese or overweight patients with type-2 diabetes. A cross-sectional survey of French general practitioners (GPs) presented a case-vignette about a patient for whom this drug is indicated in two alternative versions, differing only in its reimbursability, to two separate randomized subsamples of GPs in early 2007, before any decision was made about reimbursement. The results indicate that (i) more...
Source: Fundamental and Clinical Pharmacology - October 12, 2009 Category: Drugs & Pharmacology Authors: Pierre Verger, Sophie Rolland, Alain Paraponaris, Julien Bouvenot, Bruno Ventelou Source Type: journals

No effect of CYP450 and P-glycoprotein on hydroxyurea in vitro metabolismEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Our objectives were (1) to study the HU metabolism via human cytochromes and (2) to test if HU is a substrate of P-gp. HU metabolism was investigated by determining the appearance of urea and HU decreasing upon incubation with human liver microsomes. Quantification was determined using HPLC coupled with UV-detection at 449 nm. Our method was linear between 5 and 1000 [mu]m, precise (coefficients of variation ranging from 1.7 to 9.9%), accurate (97.7[ndash]103.9%). The limit of quantification was 7 [mu]m. The ATPase activity of human P-gp membranes was determined by measuring inorganic phosphate liberation. HU and urea meas...
Source: Fundamental and Clinical Pharmacology - October 8, 2009 Category: Drugs & Pharmacology Authors: Hind Sassi, Dora Bachir, Anoosha Habibi, Alain Astier, Frédéric Galactéros, Anne Hulin Source Type: journals

The challenge of polypharmacy in cardiovascular medicineEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Albeit great efforts in reducing the burden of cardiovascular diseases (CVD), their prevalence continues to grow worldwide. Among the causes for this rising burden, the upcoming pandemic of obesity and diabetes further enhances the estimates of CV mortality and healthcare costs over the next decades. Nevertheless, advances in CVD treatment has increased life-expectancy, and future perspectives announce a growing aging population, with increasing comorbid conditions predisposing to CVD. Despite the emphasis on primary prevention, CV risk factors are still poorly controlled and a further need for CV drugs is upcoming. In chr...
Source: Fundamental and Clinical Pharmacology - October 8, 2009 Category: Drugs & Pharmacology Authors: Massimo Volpe, Diana Chin, Francesco Paneni Source Type: journals

The evolving story of the RAAS in hypertension, diabetes and CV disease – moving from macrovascular to microvascular targetsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The phylogenetically old renin-angiotensin-system (RAS) was originally described as a circulating hormonal system and a main cardiovascular regulator. However, there also exist 'local RASs' which are situated in cardiovascular as well as non-cardiovascular tissues where they are involved in physiological and patho-physiological processes such as inflammation, fibrosis, proliferation or apoptosis. Local RASs are activated in diabetes, preferentially in organs affected by hyperglycaemic injury such as the kidney or the retina. Increased renal or retinal Ang II levels may contribute to diabetic tissue injury in two ways: (i) ...
Source: Fundamental and Clinical Pharmacology - October 8, 2009 Category: Drugs & Pharmacology Authors: Ulrike Muscha Steckelings, Franziska Rompe, Elena Kaschina, Thomas Unger Source Type: journals

The ultrastructural and biochemical evidences of the beneficial effects of chronic caffeic acid phenethyl ester and melatonin administration on brain and cerebellum of aged ratsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Nervous system is highly vulnerable to the deleterious effects of age-related oxidative stress. A large body of researches has consistently confirmed the implication of free radicals both in normal cerebral ageing and ageing-related pathologies. In the present study, in addition to the light and electron microscopic pictures of brain and cerebellum of young, old and antioxidant administered old Sprague[ndash]Dawley rats, pro-oxidant status was evaluated in terms of measurements of total glutathione, lipid peroxidation (malondialdehyde) and activities of superoxide dismutase, catalase and glutathione peroxidase. Taking the ...
Source: Fundamental and Clinical Pharmacology - October 8, 2009 Category: Drugs & Pharmacology Authors: Mukaddes Eşrefoğlu, Mehmet Gül, Burhan Ateş, İsmet Yılmaz Source Type: journals

The gastrointestinal effects that may follow the administration of theophylline reflect the pharmacodynamic profiles of both the parent drug and its metabolitesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, this study shows that the additive effect of the combined application of theophylline's major metabolites on the rabbit gastrointestinal tract plays a major role in the final response of the intestine, and a minor one in the final responses of the gastric regions, while both the parent drug and the metabolites contribute to the final responses of the oesophagus and LOS. (Source: Fundamental and Clinical Pharmacology)
Source: Fundamental and Clinical Pharmacology - September 23, 2009 Category: Drugs & Pharmacology Authors: Theophano A. Psarra, Georgios C. Batzias, Theo L. Peeters, Maria Koutsoviti-Papadopoulou Source Type: journals

Ribavirin therapeutic drug monitoring: why, when and how?Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Recent studies suggest the potential interest of ribavirin therapeutic drug monitoring to improve sustain virological response rate in hepatitis C virus-infected patients. The present review details the pharmacokinetic properties of ribavirin, suggesting that it may be a good candidate for therapeutic drug monitoring, the different possible strategies and the analytical methods that could be employed. (Source: Fundamental and Clinical Pharmacology)
Source: Fundamental and Clinical Pharmacology - September 23, 2009 Category: Drugs & Pharmacology Authors: Françoise Stanke-Labesque, Véronique Loustaud-Ratti, Gérard Babany, Marie-Claude Gagnieu, Pierre Marquet Source Type: journals

Medicine or ecstasy? The importance of the logoEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Some pharmaceutical tablets have an appearance that resembles that of ecstasy (a logo and often a name referring to it, a given shape and/or a colour). These are sometimes sold in the street as 'ecstasy'. In order to assess the knowledge of this phenomenon, surveys were conducted among designer drug users (DDUsers), pharmacists and pharmaceutical firms. Three surveys were conducted: the first one was conducted among DDUsers by means of an anonymous questionnaire; the second one consisted of a 1-month postal survey within a network of 155 community pharmacies in the Aquitaine region, Southwestern France and the third one co...
Source: Fundamental and Clinical Pharmacology - September 15, 2009 Category: Drugs & Pharmacology Authors: Amélie Daveluy, Ghada Miremont-Salamé, Anne-Cécile Rahis, Jean-Michel Delile, Bernard Bégaud, Jean-Pierre Gachie, Françoise Haramburu Source Type: journals

Deletion of the inducible nitric oxide synthase gene reduces peripheral morphine tolerance in a mouse model of chronic inflammationEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The implication of inducible nitric-oxide synthase (iNOS) on peripheral tolerance to morphine was evaluated in wild-type (WT) and iNOS knockout mice. Chronic inflammation was induced by subplantar (s.p.) injection of Complete Freund's Adjuvant (CFA), and morphine tolerance by subcutaneous implantation of a 75 mg morphine-pellet. Withdrawal was assessed after the intraperitoneal injection of 2 mg/kg naloxone. Antinociception was assessed (Randall-Selitto test) 5 min after a fixed dose of s.p. morphine (16 [mu]g). In the absence of inflammation, s.p. morphine did not induce antinociception, while during CFA-inflammation prod...
Source: Fundamental and Clinical Pharmacology - September 14, 2009 Category: Drugs & Pharmacology Authors: Asunción Romero, Laura Hernández, Paula García-Nogales, Margarita M. Puig Source Type: journals

CHICAGO, PERISCOPE and PROactive: CV risk modification in diabetes with pioglitazoneEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Recent trials of intensive glycaemic control in patients with type 2 diabetes and its impact on cardiovascular disease have led to confusion and speculation amongst physicians. The Action to Control Cardiovascular Risk in Diabetes Study was terminated early because of a significant excess all-cause mortality in the intensively-treated group. Furthermore the ADVANCE and VADT trials did not demonstrate cardiovascular benefit with more intensive glycaemic control. Against this background, it is pertinent to re-visit and critically appraise the results of the PROactive study which examined the effects of the thiazolidinedione,...
Source: Fundamental and Clinical Pharmacology - September 9, 2009 Category: Drugs & Pharmacology Authors: D. John Betteridge Source Type: journals

The effect of nitroglycerin tolerance on oxidative stress and anaerobic sulfur metabolism in rat tissuesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, the results obtained in the liver and kidney confirm the involvement of oxidative stress in the pathomechanism of GTN tolerance, and reveal the diverse effects of this phenomenon on the [gamma]GT and GST activity and SNT level in both organs. We observed for the first time that GTN tolerance could be accompanied by the disruption of hepatic anaerobic cysteine metabolism, associated with sulfane sulfur and rhodanese activity. (Source: Fundamental and Clinical Pharmacology)
Source: Fundamental and Clinical Pharmacology - September 3, 2009 Category: Drugs & Pharmacology Authors: Magdalena Dudek, Anna Bilska, Marek Bednarski, Małgorzata Iciek, Inga Kwiecień, Maria Sokołowska-Jeżewicz, Barbara Filipek, Lidia Włodek Source Type: journals

Thioctic acid protects against carrageenan-induced acute inflammation in rats by reduction in oxidative stress, downregulation of COX-2 mRNA and enhancement of IL-10 mRNAEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In this study, the protective role of the known antioxidant, thioctic acid, in carrageenan-induced acute inflammation in rats was assessed and was compared to the reference non-steroidal anti-inflammatory drug (NSAID) indomethacin. In addition, the roles of oxidative stress, nitric oxide (NO), inducible cyclooxygenase isoform (COX-2) and interleukin (IL)-10 mRNA expressions in thioctic acid-induced effects were also investigated. Inflammation was induced by injection of 0.1 ml of 1.5% carrageenan into the plantar side of right hind paws of the rats. Thioctic acid (50, 100 or 200 mg/kg), indomethacin (10 mg/kg), DMSO and sa...
Source: Fundamental and Clinical Pharmacology - September 3, 2009 Category: Drugs & Pharmacology Authors: Nagla A. El-Shitany, Sanaa A. El-Masry, Mahmoud A. El-Ghareib, Karema El-Desoky Source Type: journals

Ethanol-induced relaxation of mouse esophagus: subcellular mechanismsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Ethanol (164 mm) produced reproducible relaxations in isolated mouse esophageal strips. Hexamethonium (10[ndash]500 [mu]m), a ganglionic blocking agent, and lidocaine (10[ndash]100 [mu]m), a local anesthetic agent, failed to affect the relaxations induced by ethanol in the mouse esophagus. Although verapamil (10[ndash]500 [mu]m), a selective blocker of L-type Ca2+ channels, failed to affect the relaxations to ethanol, ruthenium red (10[ndash]100 [mu]m), a selective blocker of ryanodine receptors (intracellular Ca2+ channels), and cyclopiazonic acid (1[ndash]10 [mu]m), a selective blocker of sarcoplasmic reticulum Ca2+ ATPa...
Source: Fundamental and Clinical Pharmacology - September 3, 2009 Category: Drugs & Pharmacology Authors: Naciye Yaktubay Döndaş, Derya Kaya, Mahir Kaplan, Peyman Ertuğ, Ergin Şingirik Source Type: journals

Effects of β-aminoisobutyric acid on leptin production and lipid homeostasis: mechanisms and possible relevance for the prevention of obesityEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
[beta]-Aminoisobutyric acid (BAIBA) is a catabolite of thymine and antiretroviral thymine analogues AZT and d4T. We recently discovered that this [beta]-amino acid is able to enhance fatty acid oxidation and reduce body weight in mice through an increased production of leptin by the white adipose tissue (WAT). Furthermore, BAIBA could have favourable effects on nonalcoholic steatohepatitis in a leptin-independent manner. In the present review, we shall recall the circumstances that led us to discover the effects of BAIBA on body fat mass and lipid homeostasis. In addition, we put forward several hypothetical mechanisms whe...
Source: Fundamental and Clinical Pharmacology - September 3, 2009 Category: Drugs & Pharmacology Authors: Karima Begriche, Julie Massart, Bernard Fromenty Source Type: journals

Relations between open-field, elevated plus-maze, and emergence tests in C57BL/6J and BALB/c mice injected with GABA- and 5HT-anxiolytic agentsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Two 5HT1A receptor agonists and chlordiazepoxide were examined in open-field, elevated plus maze, and emergence tests. At doses with no effect in the open-field, chlordiazepoxide increased open and open/total arm visits as well as open arm duration in the elevated plus maze, whereas 5HT1A receptor agonists showed an anxiolytic response on a single measure. The anxiolytic action of chlordiazepoxide was limited to the less active BALB/c strain. Unlike the 5HT1A receptor agonists, chlordiazepoxide was also anxiolytic in the emergence test, once again only in BALB/c and not C57BL/6J mice. Significant correlations were found be...
Source: Fundamental and Clinical Pharmacology - September 3, 2009 Category: Drugs & Pharmacology Authors: Robert Lalonde, Catherine Strazielle Source Type: journals

Evaluation of various gentamicin dosage regimens in geriatric patients: a simulation studyEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The aim of this simulation study was to evaluate the ability of three regimens proposed in official French recommendations for gentamicin to hit defined pharmacokinetic (PK) and pharmacodynamic targets in a population of elderly patients. The first drug regimen tested consisted of a loading dose of 1 mg/kg and a maintenance dose weighted by creatininemia, every 8 h. The second regimen consisted of a fixed dose of 1 mg/kg at various intervals of time, calculated from creatinine clearance. The last regimen was a fixed dose of 3 mg/kg once a day. All regimens were for 5 days. We used a bicompartmental PK model and implemented...
Source: Fundamental and Clinical Pharmacology - September 3, 2009 Category: Drugs & Pharmacology Authors: Laurent Bourguignon, Sylvain Goutelle, Julie Burdin De Saint-Martin, Pascal Maire, Michel Ducher Source Type: journals

Antithrombotic therapy for heart failure in sinus rhythmEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Although the risk of thromboembolism in chronic heart failure is high even in the absence of atrial fibrillation, the risk to benefit ratio of anticoagulation vs. antiplatelet therapy or no antithrombotic therapy is poorly defined in this population. Post hoc analysis of large therapeutic heart failure trials has estimated the risk of thromboembolism to be between 1 and 4.5%. However, most of these studies have included some patients with atrial fibrillation, and thromboembolism was not a predefined endpoint. At present, the evidence for either anticoagulation or antiplatelet therapy is limited and the results from current...
Source: Fundamental and Clinical Pharmacology - September 3, 2009 Category: Drugs & Pharmacology Authors: Veeran Subramaniam, Russell C. Davis, Eduard Shantsila, Gregory Y.H. Lip Source Type: journals

Gender differences in the treatment of chronic ischemic heart disease: prognostic implicationsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Despite the relatively high prevalence of coronary artery disease in women, there are little data on the investigation and treatment of ischemic heart disease in this population. In the last couple of decades authors have addressed health problems in minorities, including women. The great majority of these studies included the acute coronary syndrome population but most recent ones have focused on the management of stable angina from a gender perspective. Many of those studies showed that there are inequities between genders regarding the care of patients with ischemic heart disease. Although little is known about the prog...
Source: Fundamental and Clinical Pharmacology - August 30, 2009 Category: Drugs & Pharmacology Authors: Graciana Ciambrone, Juan Carlos Kaski Source Type: journals

Effect of two oral doses of 17β-estradiol associated with dydrogesterone on thrombin generation in healthy menopausal women: a randomized double-blind placebo-controlled studyEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Oral hormone therapy is associated with an increased risk of venous thrombosis. Drug agencies recommend the use of the lowest efficient dose to treat menopausal symptoms for a better risk/ratio profile, although this profile has not been totally investigated yet. The aim of the study was to compare the effect of the standard dose of 17[beta]-estradiol to a lower one on thrombin generation (TG). In a 2-month study, healthy menopausal women were randomized to receive daily 1mg or 2 mg of 17[beta]-estradiol (E1, n = 24 and E2, n = 26; respectively) with 10 mg dydrogesterone or placebo (PL, n = 22). Plasma levels factors VII, ...
Source: Fundamental and Clinical Pharmacology - August 29, 2009 Category: Drugs & Pharmacology Authors: Alexandra Rousseau, Annie Robert, Grigoris Gerotziafas, Dahlia Torchin, Faiez Zannad, Karine Lacut, Christian Libersa, Eric Dasque, Jean-Louis Démolis, Ismail Elalamy, Tabassome Simon Source Type: journals

Correlation of seizures and biochemical parameters of oxidative stress in experimentally induced inflammatory rat modelsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The role of oxidative stress in the pathogenesis of various conditions including epilepsy, inflammatory bowel disease and rheumatoid arthritis is evolving. The aim of this study was to find out the correlation between various inflammatory models with seizures and antioxidant parameters. Fifty-four male rats were divided into three groups of colitis, adjuvant arthritis and cotton wool granuloma (CWG). Each group had three subgroups of control, model and treatment. Thalidomide was used as treatment in colitis and arthritis group, whereas etoricoxib was used in CWG group. In colitis and arthritis groups, thalidomide was admin...
Source: Fundamental and Clinical Pharmacology - August 29, 2009 Category: Drugs & Pharmacology Authors: Ramya S. Rao, Bikash Medhi, Krishan Lal Khanduja, Promila Pandhi Source Type: journals

Adaptive designs for Phase I dose-finding studiesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This article discusses the current atmosphere and attitude towards adaptive designs and focuses on the influence of Bayesian approaches. (Source: Fundamental and Clinical Pharmacology)
Source: Fundamental and Clinical Pharmacology - August 23, 2009 Category: Drugs & Pharmacology Authors: Yinghui Zhou Source Type: journals

Stereoselective renal tubular secretion of cetirizine enantiomers – initial plasma and urine data analysis may hold the keyEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
(Source: Fundamental and Clinical Pharmacology)
Source: Fundamental and Clinical Pharmacology - August 20, 2009 Category: Drugs & Pharmacology Authors: Nuggehally R. Srinivas Source Type: journals

Protective effect of quercetin, a polyphenolic compound, on mouse corpus cavernosumEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Flavonoids are plant-based phenolic compounds, and quercetin is the most abundant dietary member of this family. One of the most important characteristics of quercetin is its antioxidant property. The aim of this study was to investigate antioxidant effects of quercetin on corpora cavernosa of mice. Corpora cavernosa were isolated in organ baths, precontracted with phenylephrine (0.5 [mu]m) and relaxant responses were mediated by acetylcholine (0.1[ndash]1 [mu]m), electrical field stimulation (EFS, 1[ndash]16 Hz, 0.5 ms, 30 V) or acidified sodium nitrite (a NaNO2, 0.5 mm). Superoxide anion generators; pyrogallol (50 [mu]m)...
Source: Fundamental and Clinical Pharmacology - August 20, 2009 Category: Drugs & Pharmacology Authors: Peyman U. Ertuğ, Anil A. Olguner, Nuran Öğülener, Ergin Şingirik Source Type: journals

Lactation stage-dependent expression of transporters in rat whole mammary gland and primary mammary epithelial organoidsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion our study augments existing data on transporter expression in the lactating mammary gland. These data should facilitate investigations into lactation-stage dependent changes in drug or nutrient milk-to-serum concentration ratios, the potential for drug[ndash] or disease[ndash]transporter interactions, and mechanistic studies of transporter function in the lactating mammary gland. (Source: Fundamental and Clinical Pharmacology)
Source: Fundamental and Clinical Pharmacology - August 20, 2009 Category: Drugs & Pharmacology Authors: Samuel E. Gilchrist, Jane Alcorn Source Type: journals

Authors' replyEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
(Source: Fundamental and Clinical Pharmacology)
Source: Fundamental and Clinical Pharmacology - August 20, 2009 Category: Drugs & Pharmacology Authors: Margherita Strolin Benedetti, Christian Otoul Source Type: journals

Paroxetine inhibited the relaxations induced by EFS in mice corpus cavernosum: is it a NOS inhibition?Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Selective serotonin reuptake inhibitors are used in the treatment of psychiatric disorders but are associated with high incidence of sexual dysfunction such as ejaculation disorders by sertraline and fluoxetine, erection disorders by paroxetine. The aim of this study is to evaluate the effects of paroxetine, sertraline and fluoxetine on relaxation of smooth muscle of corpus cavernosum on the basis of nitric oxide (NO). Male mice were killed by cervical dislocation and their penile tissues were immediately removed. The tissues were incubated in organ baths containing Krebs solution at 37°C and bubbled with 95% O2 and 5% CO...
Source: Fundamental and Clinical Pharmacology - August 20, 2009 Category: Drugs & Pharmacology Authors: Mine Kadioglu, Efnan Muci, Rasin Ozyavuz, Ersin Yaris, Murat Kesim, Nuri I. Kalyoncu Source Type: journals

Pharmacogenetic of response efficacy to antipsychotics in schizophrenia: pharmacodynamic aspects. Review and implications for clinical researchEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We present this gene-by-gene approach while detailing the features of the polymorphisms being studied (functionality, linkage disequilibrium) and the features of the studies (studied treatment(s), prospective/retrospective study, pharmacological dosage). We discuss the heterogeneity of the results and their potential clinical implications and extract methodological suggestions for the future concerning phenotype characterization, genotypes variants studied and methodological and statistical approach. (Source: Fundamental and Clinical Pharmacology)
Source: Fundamental and Clinical Pharmacology - August 20, 2009 Category: Drugs & Pharmacology Authors: Olivier Blanc, Georges Brousse, Alexandre Meary, Marion Leboyer, Pierre-Michel Llorca Source Type: journals

Unravelling the complex dissociation of [3H]-rimonabant from plated CB1 cannabinoid receptor-expressing cellsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The dissociation profile of the antagonist [3H]-rimonabant from recombinant CB1 cannabinoid receptors expressed in plated HEK293 cells followed a complex pattern when measured in medium only. After a rapid decline, the specific binding levelled off at about 20% below the initial value. To unravel the responsible mechanism(s), we examined the relative contribution of binding to cells and walls of the culture wells respectively. Washout was also performed in the presence of an excess of unlabelled ligand and/or bovine serum albumin (BSA). The findings suggest that dissociated [3H]-rimonabant molecules not only undergo rebind...
Source: Fundamental and Clinical Pharmacology - August 20, 2009 Category: Drugs & Pharmacology Authors: M. Wennerberg, A. Balendran, J.C. Clapham, Georges Vauquelin Source Type: journals

Quercitrin, a bioflavonoid improves glucose homeostasis in streptozotocin-induced diabetic tissues by altering glycolytic and gluconeogenic enzymesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The present study is an investigation into the role of quercitrin on carbohydrate metabolism in normal and streptozotocin (STZ)-induced diabetic rats. Administration of STZ leads to a significant increase (P < 0.05) in fasting plasma glucose and a decrease in insulin levels. The content of glycogen is significantly decreased (P < 0.05) in liver and muscle, but increased in the kidney. The activity of hexokinase decreased whereas the activities of glucose 6-phosphatase and fructose 1,6-bisphosphatase significantly increased (P < 0.05) in the tissues. Oral administration of quercitrin (30 mg/kg) to diabetic rats for a period...
Source: Fundamental and Clinical Pharmacology - August 17, 2009 Category: Drugs & Pharmacology Authors: Ranganathan Babujanarthanam, Purushothaman Kavitha, Moses Rajasekara Pandian Source Type: journals

Selecting healthy volunteers in specific populations: a retrospective analysis of clinical and laboratory screeningEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Healthy volunteers must undergo a medical examination before enrolment in a clinical trial. An increasing number of trials include specific populations designed to match the target populations of the drugs tested. Our study aimed at evaluating which investigations are the most appropriate in different sub-populations of healthy volunteers. Data from 350 healthy volunteers who attended our Research Center from 1997 to 2004 were retrospectively analysed. Volunteers were distributed into five sub-populations: young men, senior men, overweight men, young women, postmenopausal women. The screening procedure comprised a review o...
Source: Fundamental and Clinical Pharmacology - August 16, 2009 Category: Drugs & Pharmacology Authors: Clarisse Roux, Hugues Chevassus, Anne Farret, Françoise Costa, Pierre Petit, Florence Galtier Source Type: journals

Pre-medication and renal pre-conditioning: a role for alprazolam, atropine, morphine and promethazineEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study suggested a protective effect of these pre-medication drugs on I/R injury. Although obvious studies are required, these findings may lead to effective therapies against I/R injury. (Source: Fundamental and Clinical Pharmacology)
Source: Fundamental and Clinical Pharmacology - August 16, 2009 Category: Drugs & Pharmacology Authors: Hamid Reza Pazoki-Toroudi, Marjan Ajami, Rouhollah Habibey Source Type: journals

Antihypertensive drugs and risk of venous thromboembolism: results from the EDITH case–control studyEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This report from a hospital-based case[ndash]control study included 785 cases with confirmed unprovoked VTE and their 785 age- and sex-matched controls. Cases and controls were asked for drug exposure in a one-to-one standardized interview using the same questionnaire. Drug exposure was defined as current use of drugs at admission with onset at least 1 week ago. Three hundred and eighty-four out of 785 cases (48.9%) and 379 out 785 controls (48.3%) reported that they were currently using at least one antihypertensive drug. Among all antihypertensive therapies, only angiotensin II receptor blockers were significantly associ...
Source: Fundamental and Clinical Pharmacology - August 16, 2009 Category: Drugs & Pharmacology Authors: F.Z. Belattar, A. Delluc, G. Le Gal, C. Leroyer, D. Mottier, E. Oger, K. Lacut Source Type: journals

Statins, fibrates, nicotinic acid, cholesterol absorption inhibitors, anion-exchange resins, omega-3 fatty acids: which drugs for which patients?Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Classes of lipid lowering drugs differ strongly with respect to the types of lipids or lipoproteins they predominantly affect. Statins inhibit the de-novo synthesis of cholesterol. Consequently, the liver produces less VLDL, and the serum concentration primarily of LDL cholesterol (but, to a lesser extent, also of triglycerides) is lowered. Further, statins somewhat increase HDL cholesterol. There is abundant evidence that statins lower the rate of cardiovascular events. Cardiovascular risk reduction is the better, the lower the LDL cholesterol values achieved with statin therapy are. Some evidence is available that anion ...
Source: Fundamental and Clinical Pharmacology - August 13, 2009 Category: Drugs & Pharmacology Authors: Heinz Drexel Source Type: journals

Haplotype structure and allele frequencies of CYP2B6 in Spaniards and Central AmericansEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study was aimed to investigate the potential differences in allele frequencies of the CYP2B6 gene between Spaniards and Central Americans. Three single nucleotide polymorphisms of the CYP2B6 gene 516 G>T, 785 A>G and 1459 C>T were assayed by a polymerase chain reaction in 180 Spaniards and 182 Central Americans. The allele frequencies for CYP2B6*1, CYP2B6*4, CYP2B6*5, CYP2B6*6, CYP2B6*9 in Spaniards and Central Americans were 0.593 and 0.642, 0.062 and 0.073, 0.113 and 0.030, 0.215 and 0.230, 0.014 and 0.023, respectively. CYP2B6*5 was less prevalent among Central Americans than in Spaniards (P < 0.001). In comparison...
Source: Fundamental and Clinical Pharmacology - August 13, 2009 Category: Drugs & Pharmacology Authors: Izaskun Arenaz, Jorge Vicente, Ana Fanlo, Patricia Vásquez, Juan Carlos Medina, Blanca Conde, Fabricio González-Andrade, Blanca Sinués Source Type: journals

Protective effect of p-methoxyl-diphenyl diselenide in lethal acute liver failure induced by lipopolysaccharide and d-galactosamine in miceEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In this study, no alteration in ascorbic acid levels was observed in livers of mice exposed to LPS/d-GalN. Glutathione-S-transferase (GST) activity was stimulated by LPS/d-GalN exposure and p-methoxyl-diphenyl diselenide, at all doses, protected against this alteration. p-Methoxyl-diphenyl diselenide was effective in ameliorating inhibition of catalase activity induced by LPS/d-GalN exposure. Histological data showed that sections of livers from LPS/d-GalN-treated mice presented massive hemorrhage, inflammatory cells and necrosis. p-Methoxyl-diphenyl diselenide significantly attenuated LPS/d-GalN-induced hepatic histopatho...
Source: Fundamental and Clinical Pharmacology - August 13, 2009 Category: Drugs & Pharmacology Authors: E.A. Wilhelm, C.R. Jesse, C.W. Nogueira Source Type: journals

Effect of chronic pre-treatment with angiotensin converting enzyme inhibition on skeletal muscle mitochondrial recovery after ischemia/reperfusionEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Impaired skeletal muscle energetic participates in peripheral arterial disease (PAD) patient's morbidity and mortality. Angiotensin converting enzyme inhibition (ACEi), cornerstone for pharmacologic risk factor management in PAD patients, might also be interesting by protecting skeletal muscle energetic. We therefore determined whether chronic ACEi might reduce ischemia-induced mitochondrial respiratory chain dysfunction in the frequent setting of hindlimb ischemia[ndash]reperfusion. Ischemic legs of rats submitted to 5 h ischemia induced by a rubber band tourniquet applied on the root of the hindlimb followed by reperfusi...
Source: Fundamental and Clinical Pharmacology - August 13, 2009 Category: Drugs & Pharmacology Authors: Fabien Thaveau, Joffrey Zoll, Jamal Bouitbir, Benoît N'Guessan, Philippe Plobner, Nabil Chakfe, Jean-Georges Kretz, Ruddy Richard, François Piquard, Bernard Geny Source Type: journals

Combined therapy in the treatment of dyslipidemiaEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This systematic review analyses the efficacy, tolerability and safety of combinations of different medicines used to treat dyslipidemias in clinical practice. A PubMed search up to January 2009, was conducted to identify relevant studies. Criteria used to identify studies included (1) English language, (2) published studies with original data or meta-analyses in peer-reviewed journals. Although statin treatment is a mainstay of dyslipidemia management today, complementary effects of other lipid-lowering and/or HDL-cholesterol-raising therapies might substantially increase the clinical benefits not only in the small minorit...
Source: Fundamental and Clinical Pharmacology - August 13, 2009 Category: Drugs & Pharmacology Authors: Željko Reiner Source Type: journals

Lasting reduction of postsurgical hyperalgesia after single injection of botulinum toxin type A in ratEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A single injection of low doses of botulinum toxin type A (3.5 U/kg) completely abolished secondary mechanical hyperalgesia throughout its duration in a model of post surgical pain after gastrocnemius incision in rat. (Source: Fundamental and Clinical Pharmacology)
Source: Fundamental and Clinical Pharmacology - August 13, 2009 Category: Drugs & Pharmacology Authors: Boris Filipović, Lidija Bach-Rojecky, Zdravko Lacković Source Type: journals