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https://www.readbyqxmd.com/read/28729070/abc-transporters-in-the-liver-fluke-opisthorchis-felineus
#1
Viatcheslav A Mordvinov, Nikita I Ershov, Darya S Pirozhkova, Yuri V Pakharukov, Maria Y Pakharukova
ATP-binding cassette transporters (ABC transporters) are essential components of normal cellular physiological machinery in all eukaryotic and prokaryotic species, including parasites. Some ABC transporters, e.g., P-glycoproteins, are involved in the efflux of toxins and xenobiotics from the cell. At present, nothing is known about ABC transporter genes in epidemiologically important liver flukes from the Opisthorchiidae family, including European liver fluke Opisthorchis felineus. Opisthorchiasis caused by O...
July 17, 2017: Molecular and Biochemical Parasitology
https://www.readbyqxmd.com/read/28725143/pharmacy-malpractice-the-rate-and-prevalence-of-dispensing-high-risk-prescription-only-medications-at-community-pharmacies-in-saudi-arabia
#2
Thamir M Alshammari, Salman A Alhindi, Ahmed M Alrashdi, Imaan Benmerzouga, Mohamad Aljofan
OBJECTIVE: To assess the compliance of community pharmacies with the regulations that prohibit the dispensing of prescription-only medications in the absence of a physician prescription in Saudi Arabia. METHOD: A cross-sectional study was conducted in the period between October 2014 and January 2015. A list of 10 prescription-only medications were selected to be studied. 150 community pharmacies were visited across 6 major regions in Saudi Arabia to assess the prevalence of non-compliance among community pharmacies...
July 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28718527/evaluation-of-intralesional-injection-of-hyaluronic-acid-compared-with-verapamil-in-peyronie-s-disease-preliminary-results-from-a-prospective-double-blinded-randomized-study
#3
V Favilla, G I Russo, A Zucchi, G Siracusa, S Privitera, S Cimino, M Madonia, T Cai, G Cavallini, G Liguori, G D'Achille, M Silvani, G Franco, P Verze, A Palmieri, B Torrisi, V Mirone, G Morgia
Several intralesional therapeutic protocols have been proposed for the treatment of Peyronie's disease. Among all, hyaluronic acid (HA) and verapamil have been differently tested. We aimed to evaluate the efficacy of intralesional verapamil (ILVI) compared with intralesional HA in patients with early onset of Peyronie's disease (PD). This is a multi-centre prospective double-arm, randomized, double-blinded study comparing ILVI vs. intralesional HA after 12-weeks. Sexually active men, older than 18 years and affected by the acute phase of PD were eligible for this study...
July 2017: Andrology
https://www.readbyqxmd.com/read/28710081/use-of-a-next-generation-multi-durometer-long-guide-sheath-for-triaxial-access-in-flow-diversion-experience-in-95-consecutive-cases
#4
Li-Mei Lin, Matthew T Bender, Geoffrey P Colby, Narlin B Beaty, Bowen Jiang, Jessica K Campos, Judy Huang, Rafael J Tamargo, Alexander L Coon
BACKGROUND: Intracranial access techniques in modern neurointerventions have shifted towards more robust access platforms. The long guide sheath is one of the building blocks of triaxial systems used in intracranial embolizations. Here we present our experience with the AXS Infinity LS long sheath in the triaxial platform for the implantation of the Pipeline embolization device (PED). METHODS: We retrospectively identified patients who underwent PED Flex treatment with the AXS Infinity LS at a single institution...
July 14, 2017: Journal of Neurointerventional Surgery
https://www.readbyqxmd.com/read/28708754/the-effect-of-vasodilatory-medications-on-radial-artery-spasm-in-patients-undergoing-transradial-coronary-artery-procedures-a-systematic-review
#5
Elizabeth Curtis, Ritin Fernandez, Astin Lee
BACKGROUND: The uptake of percutaneous coronary procedures via the radial artery has increased internationally due to the decreased risk of complications and increased patient satisfaction. The increased susceptibility of the radial artery to spasm however presents a potential risk for procedural failure. Although most experts agree on the need for prophylactic medications to reduce radial artery spasm, currently there is inconsistency in literature regarding the most effective vasodilatory medication or combination of medications...
July 2017: JBI Database of Systematic Reviews and Implementation Reports
https://www.readbyqxmd.com/read/28704741/outside-the-box-medications-worth-considering-when-traditional-antiepileptic-drugs-have-failed
#6
REVIEW
Adrian L Turner, M Scott Perry
PURPOSE: Review and discuss medications efficacious for seizure control, despite primary indications for other diseases, as treatment options in patients who have failed therapy with traditional antiepileptic drugs (AEDs). METHODS: Literature searches were conducted utilizing PubMed and MEDLINE databases employing combinations of search terms including, but not limited to, "epilepsy", "refractory", "seizure", and the following medications: acetazolamide, amantadine, bumetanide, imipramine, lidocaine, verapamil, and various stimulants...
June 27, 2017: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/28694398/renal-sympathetic-denervation-assisted-treatment-of-electrical-storm-due-to-polymorphic-ventricular-tachycardia-in-a-patient-with-cathecolaminergic-polymorphic-ventricular-tachycardia
#7
Tolga Aksu, Tümer Erdem Güler, Kazım Serhan Özcan, Serdar Bozyel, Kıvanç Yalın
Electrical storm (ES) is not a rare clinical entity. Sympathetic hyperactivity may play critical role in development and continuation of ES. Some recent reports have demonstrated that catheter-based renal sympathetic denervation (RSD) may reduce sympathetic activation and have a potential role in reducing arrhythmic burden. A 46-year-old man was admitted to clinic with frequent implantable cardioverter defibrillator shocks and ES related to catecholaminergic polymorphic ventricular tachycardia (VT). Tachycardia was unresponsive to administration of beta-blockers, verapamil, and flecainide...
July 2017: Türk Kardiyoloji Derneği Arşivi: Türk Kardiyoloji Derneğinin Yayın Organıdır
https://www.readbyqxmd.com/read/28680626/years-of-palpitations-and-a-heart-rate-of-213-beats-per-minute
#8
Kevin Lee, Joseph Banta, Matthew D'Ambrosio, Apostolos Voudouris, Antonios Tsompanidis
Belhassen tachycardia is the most common idiopathic ventricular tachycardia arising from the left ventricle, classically characterized by a right bundle branch block and left axis deviation. Vigilance for Belhassen tachycardia is essential as intravenous verapamil has proven to be highly efficacious for treating symptomatic patients with this underlying arrhythmia.
July 2017: Clinical Case Reports
https://www.readbyqxmd.com/read/28675836/natural-alkaloids-as-p-gp-inhibitors-for-multidrug-resistance-reversal-in-cancer
#9
REVIEW
Prashant Joshi, Ram A Vishwakarma, Sandip B Bharate
The biggest challenge associated with cancer chemotherapy is the development of cross multi-drug resistance to almost all anti-cancer agents upon chronic treatment. The major contributing factor for this resistance is efflux of the drugs by the p-glycoprotein pump. Over the years, inhibitors of this pump have been discovered to administer them in combination with chemotherapeutic agents. The clinical failure of first and second generation P-gp inhibitors (such as verapamil and cyclosporine analogs) has led to the discovery of third generation potent P-gp inhibitors (tariquidar, zosuquidar, laniquidar)...
June 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28675424/predicting-qrs-and-pr-interval-prolongations-in-humans-using-nonclinical-data
#10
L Bergenholm, J Parkinson, J Mettetal, N D Evans, M J Chappell, T Collins
BACKGROUND AND PURPOSE: Risk of cardiac conduction slowing (QRS/PR prolongations) is assessed prior to clinical trials using in vitro and in vivo studies. Understanding the quantitative translation of these studies to the clinical situation enables improved risk assessment in the nonclinical phase. EXPERIMENTAL APPROACH: Four compounds that prolong QRS and/or PR (AZD1305, flecainide, quinidine and verapamil) were characterised using in vitro (sodium/calcium channels), in vivo (guinea pigs/dogs) and clinical data...
July 3, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28670363/verapamil-suppresses-cardiac-alternans-and-ventricular-arrhythmias-in-acute-myocardial-ischemia-via-ryanodine-receptor-inhibition
#11
Yu-Lei Deng, Jun-Yan Zhao, Ji-Hua Yao, Qiang Tang, Le Zhang, Hong-Lian Zhou, Cun-Tai Zhang, Jia-Gao Lv, Xiao-Qing Quan
T-wave alternans (TWA) is a potent arrhythmia substrate under the conditions of acute myocardial ischemia. Abnormal intracellular calcium cycling contributes to the genesis of cardiac alternans. Ryanodine receptor (RyR) is a pivotal Ca(2+) cycling protein central to Ca(2+) signaling in the heart. Here, we investigated the potential role of RyR in cardiac alternans and ventricular arrhythmias in acute myocardial ischemia. Transmembrane action potentials were simultaneously recorded from epicardium and endocardium together with a transmural ECG and isometric contraction force in the arterially perfused left ventricular wedge preparations...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28669723/the-jak2-inhibitors-cep-33779-and-nvp-bsk805-have-high-p-gp-inhibitory-activity-and-sensitize-drug-resistant-cancer-cells-to-vincristine
#12
J I Hyun Cheon, Kyeong Seok Kim, Mihyun Kim, Hyung Sik Kim, Sungpil Yoon
P-glycoprotein (P-gp) is overexpressed in cancer cells in order to pump out chemotherapeutic drugs, and is one of the major mechanisms responsible for multidrug resistance (MDR). It is important to identify P-gp inhibitors with low toxicity to normal cells in order to increase the efficacy of anti-cancer drugs. Previously, a JAK2 inhibitor CEP-33779 demonstrated inhibitory actions against P-gp and an ability to sensitize drug-resistant cancer cells to treatment. In the present study, we tested another JAK2 inhibitor NVP-BSK805 for P-gp inhibitory activity...
June 29, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28669009/neuroprotective-effects-of-at1-receptor-antagonists-after-experimental-ischemic-stroke-what-is-important
#13
Juraj Culman, Toni Jacob, Sven O Schuster, Kjell Brolund-Spaether, Leonie Brolund, Ingolf Cascorbi, Yi Zhao, Peter Gohlke
The present study conducted in rats defines the requirements for neuroprotective effects of systemically administered AT1 receptor blockers (ARBs) in acute ischaemic stroke. The inhibition of central effects to angiotensin II (ANG II) after intravenous (i.v.) treatment with candesartan (0.3 and 3 mg/kg) or irbesartan and losartan (3 and 30 mg/kg) was employed to study the penetration of these ARBs across the blood-brain barrier. Verapamil and probenecid were used to assess the role of the transporters, P-glycoprotein and the multidrug resistance-related protein 2, in the entry of losartan and irbesartan into the brain...
July 2, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28668684/high-incidence-of-fluoroquinolone-resistance-and-effect-of-efflux-pump-inhibitors-on-moxifloxacin-resistance-among-mycobacterium-tuberculosis-isolates-causing-urinary-tract-infection-in-taiwan
#14
Jung-Yien Chien, Chong-Jen Yu, Po-Ren Hsueh
In this study, we explored the prevalence of urinary tract tuberculosis (UTB) and whether the activation of efflux pump account for resistance to moxifloxacin in Taiwan. Of the 3,034 patients with culture-confirmed TB from 2005 to 2012, 47 (1.5%) with UTB were included. Minimum inhibitory concentrations (MICs) of moxifloxacin were determined in the presence or absence of efflux pump inhibitors (EPIs), including verapamil, reserpine and carbonyl cyanide 3-chlorophenylhydrazone and EPIs responders were defined as at least a 4-fold reduction in MICs...
June 28, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28666572/rare-diagnosis-of-telethoninopathy-lgmd2g-in-a-turkish-patient
#15
Elena Ikenberg, Ivan Karin, Birgit Ertl-Wagner, Angela Abicht, Stefanie Bulst, Krause Sabine, Benedikt Schoser, Peter Reilich, Maggie C Walter
Telethoninopathy is one of the rarest forms of Limb-girdle muscular dystrophy (LGMD). So far, only a small number of LGMD type 2 G (LGMD2G) patients have been described, mostly patients from Brazil. Here we present a 35-year-old female patient of Turkish ethnicity with LGMD2G due to a novel homozygous frame-shift mutation c.90_91del (p.Ser31Hisfs*11) in the telethonin gene, probably leading to truncated protein or nonsense mediated decay. Myalgia and walking on tiptoes were the first symptoms starting in early childhood, around age 22 proximal, later distal leg muscles became affected...
June 1, 2017: Neuromuscular Disorders: NMD
https://www.readbyqxmd.com/read/28665551/mechanistic-differences-in-the-uptake-of-salicylic-acid-glucose-conjugates-by-vacuolar-membrane-enriched-vesicles-isolated-from-arabidopsis-thaliana
#16
Elizabeth Vaca, Claire Behrens, Tiju Theccanat, Jun-Yong Choe, John V Dean
Salicylic acid (SA) is a plant hormone involved in a number of physiological responses including both local and systemic resistance of plants to pathogens. In Arabidopsis, SA is glucosylated to form either SA 2-O-β-D-glucose (SAG) or SA glucose ester (SGE). In the present study, we show that SAG accumulates in the vacuole of Arabidopsis, while the majority of SGE was located outside the vacuole. The uptake of SAG by vacuolar membrane-enriched vesicles isolated from Arabidopsis was stimulated by the addition of MgATP and was inhibited by both vanadate (ABC transporter inhibitor) and bafilomycin A1 (vacuolar H(+) -ATPase inhibitor), suggesting that SAG uptake involves both an ABC transporter and H(+) -antiporter...
June 30, 2017: Physiologia Plantarum
https://www.readbyqxmd.com/read/28652884/drug-absorption-related-nephrotoxicity-assessment-on-an-intestine-kidney-chip
#17
Zhongyu Li, Wentao Su, Yujuan Zhu, Tingting Tao, Dong Li, Xiaojun Peng, Jianhua Qin
Drug absorption in the intestine is tightly related to drug-induced nephrotoxicity, which is a relatively common side effect in clinical practice. It highlights a great need to develop predictive models with high accuracy in the early stage during new drug discovery and development. Herein, we presented a novel intestine-kidney chip, which recapitulated drug absorption in the intestine and its resultant drug toxicity on the kidney. This work aims to provide an integrated tool for accurate assessment of drug absorption-related nephrotoxicity in vitro...
May 2017: Biomicrofluidics
https://www.readbyqxmd.com/read/28650628/synthesis-and-evaluation-of-new-fluorine-18-labeled-verapamil-analogs-to-investigate-the-function-of-p-glycoprotein-in-the-blood-brain-barrier
#18
Renske M Raaphorst, Gert Luurtsema, Robert C Schuit, Esther J M Kooijman, Philip H Elsinga, Adriaan A Lammertsma, Albert D Windhorst
P-glycoprotein is an efflux transporter located in the blood-brain barrier. (R)-[(11)C]Verapamil is widely used as a PET tracer to investigate its function in patients with epilepsy, Alzheimer's disease, and other neurodegenerative diseases. Currently it is not possible to use this successful tracer in clinics without a cyclotron, because of the short half-life of carbon-11. We developed two new fluorine-18 labeled (R)-verapamil analogs, with the benefit of a longer half-life. The synthesis of (R)-N-[(18)F]fluoroethylverapamil ([(18)F]1) and (R)-O-[(18)F]fluoroethylnorverapamil ([(18)F]2) has been described...
July 10, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28648081/in-silico-and-in-vitro-screening-for-p-glycoprotein-interaction-with-tenofovir-darunavir-and-dapivirine-an-anti-retroviral-drug-combination-for-topical-prevention-of-colorectal-hiv-transmission
#19
Magda Swedrowska, Shirin Jamshidi, Abhinav Kumar, Charles Kelly, K Miraz Rahman, Ben Forbes
The aim of the study was to use in-silico and in vitro techniques to evaluate whether a triple formulation of antiretroviral drugs (tenofovir, darunavir and dapivirine) interacted with p-glycoprotein (P-gp) or exhibited any other permeability-altering drug-drug interactions in the colorectal mucosa. Potential drug interactions with P-gp were screened initially using molecular docking, followed by molecular dynamics simulations to analyse the identified drug-transporter interaction more mechanistically. The transport of tenofovir, darunavir and dapivirine was investigated in the Caco-2 cells models and colorectal tissue and their apparent permeability coefficient (Papp), efflux ratio (ER) and the effect of transporter inhibitors were evaluated...
June 25, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28638869/reducing-toxicity-and-increasing-efficiency-aconitine-with-liquiritin-and-glycyrrhetinic-acid-regulate-calcium-regulatory-proteins-in-rat-myocardial-cell
#20
Yuyan Zhang, Li Yu, Weifeng Jin, Hongjing Fan, Min Li, Tianmei Zhou, Haitong Wan, Jiehong Yang
BACKGROUND: Compatibility of Radix Aconiti Carmichaeli and Liquorice is known to treat heart diseases such as heart failure and cardiac arrhythmias. This work answers the question that whether the active components (Aconitine, Liquiritin and Glycyrrhetinic Acid) of Radix Aconiti Carmichaeli and Liquorice could result in regulating intracellular calcium homeostasis and calcium cycling, and thereby verifies the therapeutic material basis. MATERIALS AND METHODS: The myocardial cells were divided into twelve groups randomly as control group, Aconitine group, nine different dose groups that orthogonal combined with Aconitine, Liquiritin and Glycyrrhetinic Acid, and Verapamil group...
2017: African Journal of Traditional, Complementary, and Alternative Medicines: AJTCAM
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