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Basic & Clinical Pharmacology & Toxicology

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https://www.readbyqxmd.com/read/28640946/physicians-non-uniform-approach-to-prescribing-drugs-to-older-patients-a-qualitative-study
#1
Line Due Christensen, Janne Petersen, Ove Andersen, Susanne Kaae
Multi-morbidity and polypharmacy are common in older patients and increase their susceptibility to adverse drug events and hospitalizations. Rational drug prescription is critical, however, little is known about physicians' perspectives on how to prescribe drugs for older patients. The aim of this study was to explore physicians' approach to prescribe drugs to older patients, including identifying the drugs that physicians perceive to be risk drugs for older patients and comparing them with established lists of potentially inappropriate medications...
June 22, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28639405/multiple-and-opposite-effects-of-angiotensin-ii-receptor-blockers-on-the-bioavailability-of-epoxyeicosatrienoic-acids
#2
LETTER
Jeremy Bellien, Matthieu Leuillier, Safa Louhichi, Thomas Duflot, Robinson Joannides
No abstract text is available yet for this article.
June 22, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28639402/reply-to-multiple-and-opposite-effects-of-angiotensin-ii-receptor-blockers-on-the-bioavailability-of-epoxyeicosatrienoic-acids
#3
LETTER
Asuna Senda, Yuji Mukai, Toru Hayakawa, Yuka Kato, Erik Eliasson, Anders Rane, Takaki Toda, Nobuo Inotsume
No abstract text is available yet for this article.
June 22, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28639436/a-high-hasbled-score-identifies-poor-warfarin-control-in-patients-treated-for-non-valvular-atrial-fibrillation-in-australia-and-singapore
#4
Nijole Bernaitis, Ching Chi Keong, Chen Liping, Hon Jin Shing, Teo Siew Chong, Tony Badrick, Andrew K Davey, Shailendra Anoopkumar-Dukie
Warfarin reduces stroke risk in atrial fibrillation (AF) patients. The quality of warfarin control, measured by time in therapeutic range (TTR), impacts outcomes and adverse events. One tool evaluating risk of adverse events and potential warfarin control would simplify risk-benefit assessment of warfarin. Recently, HASBLED was demonstrated effective for this purpose but this was in well-controlled patients with deep vein thrombosis. HASBLED as a predictor of warfarin control has not been validated in other populations including differing indications, warfarin control levels and ethnicities...
June 21, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28639431/decrease-in-oxidative-stress-parameters-after-post-ischaemic-recombinant-human-erythropoietin-administration-in-the-hippocampus-of-rats-exposed-to-focal-cerebral-ischaemia
#5
Jasenka Mršić-Pelčić, Kristina Pilipović, Goran Pelčić, Dinko Vitezić, Gordana Župan
Recombinant human erythropoietin (rhEpo) is a multifunctional drug with antioxidant potential. However, the underlying molecular mechanisms of its action are still unclear. The purpose of this study was to investigate the effects of rhEpo on the brain infarct volume as well as on the levels of the neuronal damage, oxidative stress parameters and active caspase-3, nuclear factor erythroid 2-related factor 2 (Nrf2) and hemeoxygenase-1 (HO-1) expressions in the hippocampi of rats exposed to the right middle cerebral artery occlusion (MCAO) for 1 hr...
June 21, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28639420/the-pharmacokinetics-of-enalapril-in-relation-to-ces1-genotype-in-healthy-danish-volunteers
#6
Claus Stage, Gesche Jürgens, Louise Schow Guski, Ragnar Thomsen, Ditte Bjerre, Laura Ferrero-Miliani, Yassine Kamal Lyauk, Henrik Berg Rasmussen, Kim Dalhoff
The present study investigated the influence of variations in the carboxylesterase 1 gene (CES1) on the pharmacokinetics of enalapril. Forty-three healthy, Danish, Caucasian volunteers representing different pre-defined genotypes each received 10 mg of enalapril. At specified time points, plasma concentrations of enalapril and the active metabolite enalaprilat were measured. The volunteers were divided into six different groups according to their genetic profile of CES1: Group 1 (controls, n=16) with two CES1 copies without non-synonymous SNPs in the exons; group 2 (n=5) with four copies of CES1; group 3 (n=6) harbouring the G143E polymorphism; group 4 (n=2) with three CES1 copies and increased transcriptional activity of the duplication (CES1A2); group 5 (n=4) harbouring the CES1A1c variant; and group 6 (n=10) with three CES1 copies and the common promoter with low transcriptional activity of the duplication...
June 21, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28639365/vascular-calcification-vitamin-k-and-warfarin-therapy-possible-or-plausible-connection
#7
Aino Siltari, Heikki Vapaatalo
Atherosclerosis is a pathological process underpinning many cardiovascular diseases; it is the main cause of global mortality. Atherosclerosis is characterized by an invasion of inflammatory cells, accumulation of lipids and the formation of fatty streaks (plaques) which subsequently allow accumulation of calcium and other minerals leading to a disturbance in the vascular endothelium and its regulatory role in arterial function. Vascular calcification is a different process, stringently regulated mainly by local factors, in which osteoblast-like cells accumulate in the muscular layer of arteries ultimately taking on the physiological appearance of bone...
June 21, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28627809/ivabradine-reduces-digitalis-induced-ventricular-arrhythmias
#8
Gerrit Frommeyer, Jan Weller, Christian Ellermann, Nils Bögeholz, Patrick Leitz, Dirk G Dechering, Simon Kochhäuser, Kristina Wasmer, Lars Eckardt
The I(f) channel inhibitor ivabradine is recommended for treatment of heart failure but also affects potassium currents and thereby prolongs ventricular repolarization. The aim of the present study was to examine the electrophysiological effects of ivabradine on digitalis-induced ventricular arrhythmias. Thirteen rabbit hearts were isolated and Langendorff-perfused. After obtaining baseline data, the digitalis glycoside ouabain was infused (0.2μM). Monophasic action potentials and ECG showed a significant abbreviation of QT interval (-34ms,p<0...
June 19, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28627804/the-effect-of-genetic-polymorphisms-in-slco2b1-on-the-lipid-lowering-efficacy-of-rosuvastatin-in-healthy-adults-with-elevated-low-density-lipoprotein
#9
Tae-Eun Kim, Dong-Seong Shin, Namyi Gu, Byung Hwa Jung, Jayoun Kim, Young Min Cho, Kyung-Sang Yu, Joo-Youn Cho
Rosuvastatin is an HMG-CoA reductase inhibitor widely used for treating hypercholesterolaemia. We investigated whether genetic polymorphisms in solute carrier organic anion transporter 2B1 (SLCO2B1) affect the lipid-lowering effect of rosuvastatin in healthy adults with elevated low-density lipoprotein (LDL). This study included 18 volunteers with LDL levels above 130 mg/dL. Rosuvastatin (20 mg) was administered once a day for 8 weeks. Blood samples were drawn before and after the 8-week treatment to measure changes in lipid levels...
June 19, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28627776/the-comt-val-108-158-met-genetic-polymorphism-can-not-be-recommended-as-a-biomarker-of-prediction-of-venlafaxine-efficacy-in-patients-treated-in-psychiatric-settings
#10
Adela Taranu, Khalil El Asmar, Romain Colle, Florian Ferreri, Mircea Polosan, Denis David, Laurent Becquemont, Emmanuelle Corruble, Céline Verstuyft
The antidepressant venlafaxine is known to increase the turn-over of cerebral monoamines, which are catabolized by the cathecol-O-methyltransferase (COMT). The COMT (Val108/158Met, rs4680) genetic polymorphism affects the cerebral COMT activity. But whether this genetic polymorphism is associated with response to venlafaxine remains unclear. We assessed the impact of the COMT Val(108/158)Met, rs4680 genetic polymorphism on the efficacy of venlafaxine in depressed patients. This study was nested in the METADAP cohort, a real-world naturalistic treatment study in psychiatric settings...
June 19, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28627771/clinical-experience-with-the-integrase-inhibitors-dolutegravir-and-elvitegravir-in-hiv-infected-patients-efficacy-safety-and-tolerance
#11
Purificación Cid-Silva, Josep María Llibre, Noelia Fernández-Bargiela, Luis Margusino-Framiñán, Vanesa Balboa-Barreiro, Berta Pernas-Souto, Isabel Martín-Herranz, Ángeles Castro-Iglesias, Eva Poveda-López
Two integrase inhibitors (INSTIs), Dolutegravir (DTG) and Elvitegravir/Cobicistat (EVG/COBI) have joined recently the pharmacotherapy arsenal against HIV. This study evaluated the efficacy and tolerability of these INSTIs in the last two years. A retrospective observational study in patients who started DTG or EVG/COBI from January 2015 to January 2017 at a reference hospital in Northwestern Spain was done. Epidemiological, clinical and immunovirological data were recorded. A statistical analysis was performed using SPSS software...
June 19, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28627763/suspected-methadone-toxicity-from-hospital-to-autopsy-bed
#12
Jaber Gharehdaghi, Asieh Takalloo-Bakhtiari, Hossein Hassanian-Moghaddam, Nasim Zamani, Mohammad-Javad Hedayatshode
High mortality rates have been reported for methadone in both adults and children. We aimed to determine the pattern of toxicity, possible underlying diseases and treatment challenges in patients referred to our center with early diagnosis of methadone toxicity and who later died. Medical files of all methadone-poisoned patients who had been admitted to a referral center of toxicology between March 2011 and March 2016, died during the hospital stay and sent for autopsy to Legal Medicine Organization were retrospectively evaluated...
June 19, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28627732/the-acute-effect-of-loperamide-on-ileostomy-output-a-randomized-double-blinded-placebo-controlled-cross-over-study
#13
Katrine Kristensen, Niels Qvist
High stoma output is a common problem in patients with ileostomy and can lead to dehydration and electrolyte disturbances. The first drug of choice to reduce stoma output is often loperamide. The aim was to assess the acute effect of loperamide on (a) ileostomy output in g/day, (b) gastrointestinal transit time and (c) patient-reported effects. A total of 12 patients completed this double-blinded, randomized, placebo-controlled, cross-over study, consisting of a 3-day treatment period with loperamide 12 mg/day or placebo followed by the reverse after a washout period of 5-7 days...
June 19, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28613449/study-of-the-cytotoxic-and-bactericidal-effects-of-sila-substituted-thioalkyne-and-mercapto-thionecompounds-based-on-1-2-3-triazole-scaffold
#14
Hanieh Mousazadeh, Mortaza Milani, Nosratollah Zarghami, Effat Alizadeh, Kazem D Safa
A series of sila-organosulfur compounds containing 1,2,3-triazole cores were screened for their cytotoxic activity on human breast cancer cell line MCF-7. Most of the tested compounds exhibited moderate to good activity against the cancer cells. Especially, the compound 4-((2-(trimethylsilyl)ethynylthio)methyl)-1-benzyl-1H-1,2,3-triazole 3a from series of sila-substituted thioalkyne 1,2,3-triazoles (STATs) and the compounds 3-(1-Benzyl-1H-1,2,3-triazol-4-yl)-1-mercapto-1,1-bis(trimethylsilyl)propane-2-thione 4a and 1-Mercapto-1,1-bis(trimethylsilyl)-3-(1-phenethyl-1H-1,2,3-triazol-4-yl)propane-2-thione 4e from series of sila-substituted mercapto-thione 1,2,3-triazoles (SMTTs)exhibited promising cytotoxicity against MCF-7 with IC50 values of 35...
June 14, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28612521/could-modafinil-prevent-psychostimulant-addiction-an-experimental-study-in-rats
#15
Verônica Tironi Dias, Luciana Taschetto Vey, Higor Zuquetto Rosa, Lívia Ferraz D'avila, Raquel Cristine Silva Barcelos, Marilise Escobar Burger
Addiction is a serious health problem which leads to general social impairment. The period of adolescence plays a significant role in drug abuse liability. Psychostimulants, such as modafinil (MOD), are majorly used by teenagers seeking improvements in cognition, which contributes to its indiscriminate use. The present study aimed to investigate the influence of MOD (64 mg/kg by gavage, once a day) treatment during adolescence (PND 28-42) on amphetamine (AMPH, 4 mg/kg i.p.) conditioned place preference (CPP) in early adulthood (PND 60)...
June 14, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28609608/voriconazole-concentrations-in-plasma-and-epithelial-lining-fluid-after-inhalation-and-oral-treatment
#16
Charlotte U Andersen, Lene Dahl Sønderskov, Elisabeth Bendstrup, Nina Voldby, Lindsey Cass, John Ayrton, Ole Hilberg
Adverse effects can compromise oral voriconazole treatment of pulmonary aspergillosis. Inhaled low-dose voriconazole may be an alternative treatment. In this study, six patients inhaled 40 mg voriconazole b.i.d. for two days, and six patients ingested 400 and 200 mg orally b.i.d. on day one and two, respectively. Blood samples were collected after the first inhalation, and bronchial alveolar lavage fluids and blood samples were collected for measurements of voriconazole 12 hr after the last administration. The concentration of voriconazole in epithelial lining fluid (ELF) was calculated by the urea dilution method...
June 13, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28609587/chemogenetic-modulation-of-g-protein-coupled-receptor-signalling-in-visual-attention-research
#17
Søren H Jørgensen, Ciarán Martin Fitzpatrick, Ulrik Gether, David D P Woldbye, Andreas T Sørensen
Attention is a fundamental cognitive process involved in nearly all aspects of life. Abnormal attention control is a symptom of many neurological disorders, most notably recognized in ADHD (attention deficit hyperactivity disorder). Although attentional performance and its malfunction has been a major area of investigation, it has proven difficult to accurately associate specific neuronal projections, cell types, neurotransmitter systems and receptors with distinct phenotypes owing to its complexity. In this MiniReview, we present a recently invented technology known as Designer Receptors Exclusively Activated by Designer Drugs (DREADDs)...
June 13, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28561421/pharmacokinetics-of-transdermal-etofenamate-and-diclofenac-in-healthy-volunteers
#18
Sara Drago, Roger Imboden, Philipp Schlatter, Mirabel Buylaert, Stephan Krähenbühl, Juergen Drewe
Little is known about the course of the plasma concentration and the bioavailability of non-steroidal anti-inflammatory drugs (NSAIDs) contained in dermal patches. We compared an etofenamate prototype patch (patent EP 1833471) and a commercially available diclofenac epolamine patch regarding the bioavailability of the active ingredients relative to respective i.m. applications and regarding their plasma concentration-time course. Twenty-four healthy human volunteers were treated using a parallel group design (n=12 per group) with a single dermal patch (removed after 12 hr) followed (after a latency of 48 hr) by 8 consecutive dermal patches every 12 hr to reach steady-state conditions...
May 31, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28561324/curcumin-ameliorates-kidney-function-and-oxidative-stress-in-experimental-chronic-kidney-disease
#19
Badreldin H Ali, Suhail Al-Salam, Yousuf Al Suleimani, Jamila Al Kalbani, Shadia Al Bahlani, Mohammed Ashique, Priyadarsini Manoj, Buthaina Al Zhili, Nadia Al Abri, Heba T Naser, Javed Yasin, Abderrahim Nemmar, Mohamed Al Za'abi, Christina Hartmann, Nicole Schupp
Chronic kidney disease (CKD) is known to involve inflammation, oxidative stress and apoptosis. Here, we investigated the impact of curcumin (diferuloyl methane, a phenolic turmeric pigment), which has strong anti-oxidant, anti-inflammatory and anti-apoptotic activities on kidney structure and function in rats with adenine-induced CKD. Rats were treated for 5 weeks with adenine to induce CKD-like renal damage and combined with three doses of curcumin. Markers of kidney function and oxidative stress were quantified in plasma, urine, renal homogenates and on kidney tissue...
May 31, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28557265/pharmacokinetic-properties-of-memantine-following-a-single-intraperitoneal-administration-and-multiple-oral-doses-in-euploid-mice-and-in-the-ts65dn-mouse-model-of-down-s-syndrome
#20
Daniella B Victorino, Ilya R Bederman, Alberto C S Costa
Memantine is a drug approved for the treatment of moderate-to-severe Alzheimer's disease (AD), and there is ongoing research on the potential expansion of its clinical applicability. Published data on the pharmacokinetics of memantine in the mouse is still incomplete, particularly for chronic administration regimens and mouse models of specific genetic disorders. Down's syndrome (DS) is a genetic disorder known to affect multiple organs and systems, with the potential to alter significantly drug pharmacokinetics...
May 30, 2017: Basic & Clinical Pharmacology & Toxicology
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