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https://www.readbyqxmd.com/read/29665423/evaluation-of-four-calcium-channel-blockers-as-fluconazole-resistance-inhibitors-in-candida-glabrata
#1
Lina M Alnajjar, Nailya R Bulatova, Rula M Darwish
OBJECTIVES: In this study we aimed to evaluate the ability of four calcium channel blockers, verapamil, diltiazem, nicardipine and nifedipine to enhance sensitivity of Candida glabrata strains to fluconazole. METHODS: The synergistic antifungal effect was examined by checkerboard method; fractional inhibitory concentration index (FIC) was determined. Time-kill curve method was used for the most promising combination to further evaluate the synergetic effects. RESULTS: nicardipine showed additive effect with fluconazole against fluconazole-resistant and fluconazole-susceptible-dose-dependent strains (DSY565 and CBS138) known to express efflux pumps but not against fluconazole-sensitive strains...
April 14, 2018: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/29627171/comparison-of-nicardipine-with-clevidipine-in-the-management-of-hypertension-in-acute-cerebrovascular-diseases
#2
Zachary Rosenfeldt, Katelyn Conklen, Breck Jones, Don Ferrill, Maithili Deshpande, Fazeel M Siddiqui
BACKGROUND AND PURPOSE: In acute stroke, hypertension worsens outcomes. Guidelines do not mention a preferred antihypertensive agent. This present study aimed to compare the efficacy and safety of nicardipine and clevidipine in acute stroke. METHODS: This retrospective review compared nicardipine with clevidipine for hypertension in acute stroke patients from March 17, 2015 to December 23, 2016. Ischemic and hemorrhagic stroke types were evaluated. Patients were excluded if under 18 years, had traumatic brain injury, had intracranial neoplasm, were on dialysis, had both study drugs during the stroke admission, or the study drug was infused for less than 1 hour...
April 4, 2018: Journal of Stroke and Cerebrovascular Diseases: the Official Journal of National Stroke Association
https://www.readbyqxmd.com/read/29617905/microvascular-decompression-of-facial-nerve-and-pexy-of-the-left-vertebral-artery-for-left-hemifacial-spasm-3-dimensional-operative-video
#3
Chun-Yu Cheng, Rakshith Shetty, Vicente Martinez, Laligam N Sekhar
A 73-yr-old man presented with intractable left hemifacial spasm of 4 yr duration. Brain magnetic resonance imaging showed significant compression of left facial nerve by the left vertebral artery (VA) and anterior inferior cerebellar artery (AICA).The patient underwent a left retrosigmoid craniotomy and a microvascular decompression of the cranial nerve (CN) VII. Intraoperatively, we found that the distal AICA had a protracted subarcuate extradural course.1 This was relieved by intra/extradural dissection...
March 29, 2018: Operative Neurosurgery (Hagerstown, Md.)
https://www.readbyqxmd.com/read/29571761/a-new-technique-for-the-assessment-of-cerebral-vasodilatory-capacity-as-part-of-catheter-based-cerebral-angiography
#4
Adnan I Qureshi, Muhammad A Saleem, Nishath Naseem, Shawn S Wallery
BACKGROUND: Previous studies have demonstrated the value of cerebral vasodilatory capacity assessment for risk stratification in patients with extracranial arterial stenosis or occlusion. We describe a new method that assesses cerebral vasodilatory capacity as part of catheter-based cerebral angiography. METHODS: We assessed regional cerebral blood volume (rCBV) in the arterial distribution of interest using a controlled contrast injection through a diagnostic catheter placed in the common carotid or the subclavian artery...
March 20, 2018: Journal of Stroke and Cerebrovascular Diseases: the Official Journal of National Stroke Association
https://www.readbyqxmd.com/read/29569130/correlation-of-noninvasive-blood-pressure-and-invasive-intra-arterial-blood-pressure-in-patients-treated-with-vasoactive-medications-in-a-neurocritical-care-unit
#5
Ali A Saherwala, Sonja E Stutzman, Mohamed Osman, Junaid Kalia, Stephen A Figueroa, DaiWai M Olson, Venkatesh Aiyagari
BACKGROUND: The correlation between noninvasive (oscillometric) blood pressure (NBP) and intra-arterial blood pressure (IAP) in critically ill patients receiving vasoactive medications in a Neurocritical Care Unit has not been systematically studied. The purpose of this study is to examine the relationship between simultaneously measured NBP and IAP recordings in these patients. METHODS: Prospective observational study of patients (N = 70) admitted to a neurocritical care unit receiving continuous vasopressor or antihypertensive infusions...
March 22, 2018: Neurocritical Care
https://www.readbyqxmd.com/read/29534916/metoclopramide-induced-pheochromocytoma-crisis
#6
James B Leonard, Kashif M Munir, Hong K Kim
Metoclopramide (MCP) is a commonly used anti-emetic in the emergency department (ED). Its use is generally well tolerated; although infrequent adverse reactions such as extrapyramidal reactions or tardive dyskinesia are reported. However, many ED providers are not familiar with the potentially life-threatening hypertensive emergency that can be precipitated by MCP administration in patients with pheochromocytoma. A previously healthy 36-year-old woman presented to the ED with headache and nausea. She developed acute hypertensive emergency (acute agitation, worsening headache, chest pain and wide complex tachycardia) when her blood pressure (BP) increased to 223/102mmHg (initial BP, 134/86mmHg) after receiving intravenous MCP...
March 5, 2018: American Journal of Emergency Medicine
https://www.readbyqxmd.com/read/29528115/a-role-for-focal-adhesion-kinase-in-facilitating-the-contractile-responses-of-murine-gastric-fundus-smooth-muscles
#7
Yeming Xie, Koon Hee Han, Nathan Grainger, Wen Li, Robert D Corrigan, Brian A Perrino
Smooth muscle contraction involves regulating myosin light chain phosphorylation and dephosphorylation by myosin light chain kinase and myosin light chain phosphatase. CPI-17 and MYPT1 are crucial for regulating gastrointestinal smooth muscle contraction by inhibiting myosin light chain phosphatase. Integrin signalling involves the dynamic recruitment of several proteins, including FAK, to focal adhesions. FAK tyrosine kinase activation is involved in cell adhesion to the extracellular matrix via integrin signalling...
March 12, 2018: Journal of Physiology
https://www.readbyqxmd.com/read/29519742/reduction-of-nicardipine-related-phlebitis-in-patients-with-acute-stroke-by-diluting-its-concentration
#8
Kei Kawada, Tsuyoshi Ohta, Koudai Tanaka, Norifumi Miyamoto
BACKGROUND: Nicardipine is frequently used in the treatment of hypertension for patients with acute stroke; however, its dosing is complicated by a high risk of phlebitis. In the present study, we examined whether restricting nicardipine concentration under a specific value could reduce the incidence of nicardipine-related phlebitis in patients with acute stroke. METHODS: Intravenous nicardipine-related phlebitis was retrospectively analyzed. From July 2015, a simple proposition was made to dilute maximum intravenous nicardipine concentration to lower than 130 µg/mL...
March 5, 2018: Journal of Stroke and Cerebrovascular Diseases: the Official Journal of National Stroke Association
https://www.readbyqxmd.com/read/29482112/role-of-voltage-gated-calcium-channels-on-striatal-dopamine-release-induced-by-inorganic-mercury-in-freely-moving-rats
#9
Lilian R Ferreira Faro, Miguel Alfonso, Vania Moraes Ferreira, Rafael Durán
The possible role of voltage-sensitive calcium channels (VSCC) activation on the HgCl2 -induced dopamine release was investigated using selective VSCC blockers and the dopamine levels were measured by HPLC from samples obtained by in vivo brain microdialysis. Infusion of HgCl2 in nicardipine (10 or 100 μM) or flunaricine (10 μM) pretreated animals had no significant effect on dopamine release induced by HgCl2 . Pretreatment with 100 μM flunaricine, 20 μM ω-conotoxin MVIIC, or ω-conotoxin GVIA significantly decreased the HgCl2 -induced dopamine release over 61%, 88%, and 99%, respectively...
February 12, 2018: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/29385292/advanced-continuous-flow-platform-for-on-demand-pharmaceutical-manufacturing
#10
Ping Zhang, Nopphon Weeranoppanant, Dale A Thomas, Kohei Tahara, Torsten Stelzer, Mary Grace Russell, Marcus O'Mahony, Allan S Myerson, Hongkun Lin, Liam P Kelly, Klavs F Jensen, Timothy F Jamison, Chunhui Dai, Yuqing Cui, Naomi Briggs, Rachel L Beingessner, Andrea Adamo
As a demonstration of an alternative to the challenges faced with batch pharmaceutical manufacturing including the large production footprint and lengthy time-scale, we previously reported a refrigerator-sized continuous flow system for the on-demand production of essential medicines. Building on this technology, herein we report a second-generation, reconfigurable and 25 % smaller (by volume) continuous flow pharmaceutical manufacturing platform featuring advances in reaction and purification equipment. Consisting of two compact [0...
January 31, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29383731/ca2-signalling-in-mouse-urethral-smooth-muscle-in-situ-role-of-ca2-stores-and-ca2-influx-mechanisms
#11
Bernard T Drumm, Benjamin E Rembetski, Caroline A Cobine, Salah A Baker, Gerard P Sergeant, Mark A Hollywood, Keith D Thornbury, Kenton M Sanders
Urethral smooth muscle cells (USMC) generate myogenic tone and contribute to urinary continence. Currently, little is known about Ca2+ signalling in USMC in situ, and therefore little is known about the source(s) of Ca2+ required for excitation-contraction coupling. We characterized Ca2+ signalling in USMC within intact urethral muscles using a genetically encoded Ca2+ sensor, GCaMP3, expressed selectively in USMC. USMC fired spontaneous intracellular Ca2+ waves that did not propagate cell-to-cell across muscle bundles...
January 31, 2018: Journal of Physiology
https://www.readbyqxmd.com/read/29290374/physical-compatibility-of-meropenem-and-vaborbactam-with-select-intravenous-drugs-during-simulated-y-site-administration
#12
James M Kidd, Lindsay M Avery, Tomefa E Asempa, David P Nicolau, Joseph L Kuti
PURPOSE: Meropenem/vaborbactam is a novel intravenous antibiotic combining the carbapenem, meropenem, with a novel β-lactamase inhibitor, vaborbactam. Meropenem/vaborbactam is administered as a 3-hour infusion given every 8 hours, thereby potentially restricting an intravenous line for 9 h/d. Intravenous medications may be given concurrently via Y-site when compatibility data are available. Herein, physical compatibility was determined for the identification which medications can be coadministered with meropenem/vaborbactam via Y-site...
February 2018: Clinical Therapeutics
https://www.readbyqxmd.com/read/29250113/encapsulation-of-nicardipine-hydrochloride-and-release-from-biodegradable-poly-d-l-lactic-co-glycolic-acid-microparticles-by-double-emulsion-process-effect-of-emulsion-stability-and-different-parameters-on-drug-entrapment
#13
Nopparuj Soomherun, Narumol Kreua-Ongarjnukool, Sorayouth Chumnanvej, Saowapa Thumsing
Poly(D,L-lactic-co-glycolic acid) (PLGA) is an important material used in drug delivery when controlled release is required. The purpose of this research is to design and characterize PLGA microparticles (PLGA MPs) implants for the controlled release of nicardipine hydrochloride (NCH) in vitro . This study used the water-in-oil-in-water (w1 /o/w2 ) double emulsion and solvent diffusion/evaporation approach to prepare PLGA MPs. Optimal processing conditions were found, such as polymer content, surfactant type, stabilizer concentration, inner and outer aqueous phase volumes, and stirring speed...
2017: International Journal of Biomaterials
https://www.readbyqxmd.com/read/29198152/development-of-sustained-release-gastro-retentive-tablet-formulation-of-nicardipine-hydrochloride-using-quality-by-design-qbd-approach
#14
Vijay S Chudiwal, Sadhana Shahi, Swapnil Chudiwal
The objective of the present study was to develop a sustained release gastro-retentive (SRGR) tablet formulation of nicardipine hydrochloride (HCl) for once-a-day dosing using the quality by design (QbD) approach. The quality target product profile of nicardipine HCl SRGR tablet formulation was defined, and critical quality attributes (CQAs) were identified. Potential risk factors were identified using a fish bone diagram and failure mode effect analysis (FMEA) tool and screened by the Plackett-Burman design, and finally nicardipine HCl SRGR tablet formulation was optimized using the Box-Behnken design...
May 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29192124/drugs-and-scaffold-that-inhibit-cytochrome-p450-27a1-in-vitro-and-in-vivo
#15
Morrie Lam, Natalia Mast, Irina A Pikuleva
Cytochrome P450 27A1 (CYP27A1) is a ubiquitous enzyme that hydroxylates cholesterol and other sterols. Complete CYP27A1 deficiency owing to genetic mutations is detrimental to human health, whereas 50% of activity retention is not and does not affect the whole body cholesterol levels. CYP27A1 is considered a potential therapeutic target in breast cancer and age-related neurodegenerative diseases; however, CYP27A1 inhibition should be ≤50%. Herein, 131 pharmaceuticals were tested for their effect on CYP27A1-mediated cholesterol 27-hydroxylation by in vitro enzyme assay...
February 2018: Molecular Pharmacology
https://www.readbyqxmd.com/read/29159314/vasoconstriction-triggered-by-hydrogen-sulfide-evidence-for-na-k-2cl-cotransport-and-l-type-ca-2-channel-mediated-pathway
#16
Sergei N Orlov, Svetlana V Gusakova, Liudmila V Smaglii, Svetlana V Koltsova, Svetalana V Sidorenko
Objectives: This study examined the dose-dependent actions of hydrogen sulfide donor sodium hydrosulphide (NaHS) on isometric contractions and ion transport in rat aorta smooth muscle cells (SMC). Methods: Isometric contraction was measured in ring aortas segments from male Wistar rats. Activity of Na+ /K+ -pump and Na+ ,K+ ,2Cl- cotransport was measured in cultured endothelial and smooth muscle cells from the rat aorta as ouabain-sensitive and ouabain-resistant, bumetanide-sensitive components of the86 Rb influx, respectively...
December 2017: Biochemistry and Biophysics Reports
https://www.readbyqxmd.com/read/29159148/endovascular-treatment-of-symptomatic-vasospasm-after-aneurysmal-subarachnoid-hemorrhage-a-three-year-experience
#17
Eun-Sung Park, Dae-Won Kim, Sung-Don Kang
Objective: The cause of severe clinical vasospasm after aneurysmal subarachnoid hemorrhage remains unknown, despite extensive research over the past 30 years. However, the intra-arterial administration of vasodilating agents and balloon angioplasty have been successfully used in severe refractory cerebral vasospasm. Materials and Methods: We retrospectively analyzed the data of 233 patients admitted to our institute with aneurysmal subarachnoid hemorrhage (SAH) over the past 3 years...
September 2017: Journal of Cerebrovascular and Endovascular Neurosurgery
https://www.readbyqxmd.com/read/29129208/augmented-gene-expression-triggered-by-na-k-atpase-inhibition-role-of-ca-2-i-mediated-and-independent-excitation-transcription-coupling
#18
Larisa V Smolyaninova, Svetlana V Koltsova, Svetlana V Sidorenko, Sergei N Orlov
In rat vascular smooth muscle cells (RVSMC), 3-h Na+ ,K+ -ATPase inhibition by ouabain or in K+ -free medium resulted in the inversion of the [Na+ ]i /[K+ ]i ratio and elevation up to 7-fold the content of Egr1, Atf3, Nr4a1 and Ptgs2 mRNAs. Ouabain increased the rate of 45Ca2+ influx by 2-fold that was abolished by L-type voltage-gated Ca2+ channel blocker nicardipine, but it was resistant to Na+ /Ca2+ exchanger inhibitor KB-R7943. To study the role of Ca2+ -mediated signaling in the expression of Na+ i /K+ i -sensitive genes we used intracellular Ca2+ chelator BAPTA and incubated RVSMC in Ca2+ -free medium...
December 2017: Cell Calcium
https://www.readbyqxmd.com/read/29092768/continuous-infusion-labetalol-vs-nicardipine-for-hypertension-management-in-stroke-patients
#19
Jason P Hecht, Patrick G Richards
BACKGROUND: Labetalol and nicardipine are antihypertensives commonly used in the management of elevated blood pressure (BP) following an acute stroke, but there is limited evidence to suggest which agent as a continuous infusion should be used preferentially in this setting. OBJECTIVE: This study aimed to compare the safety, efficacy, and ease of administration of continuous-infusion labetalol with continuous-infusion nicardipine following an acute stroke. METHODS: This retrospective cohort study of patients with acute ischemic stroke or intracerebral hemorrhage included patients if they received either study agent within 24 hours of admission...
February 2018: Journal of Stroke and Cerebrovascular Diseases: the Official Journal of National Stroke Association
https://www.readbyqxmd.com/read/29067537/posterior-reversible-encephalopathy-syndrome-pres-induced-by-pazopanib-a-multi-targeting-tyrosine-kinase-inhibitor-in-a-patient-with-soft-tissue-sarcoma-case-report-and-review-of-the-literature
#20
Shoichi Deguchi, Koichi Mitsuya, Yoko Nakasu, Nakamasa Hayashi, Hirohisa Katagiri, Hideki Murata, Junji Wasa, Mitsuru Takahashi, Masahiro Endo
Posterior reversible encephalopathy syndrome (PRES) is a clinical entity characterized by acute neurological symptoms such as severe headache, seizures, and visual disturbance, and by typical reversible lesion on brain magnetic resonance (MR) images. Since PRES is thought to be caused by vascular endothelial injury due to cytotoxic agents or acute systemic hypertension, the number of reports on PRES associated with angiogenesis inhibitors has been increasing. Although five cases that developed PRES due to pazopanib for renal cell carcinoma have already been reported, none of PRES due to pazopanib for soft-tissue sarcoma has been reported thus far...
October 25, 2017: Investigational New Drugs
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