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Nicardipine

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https://www.readbyqxmd.com/read/27847440/gintonin-facilitates-catecholamine-secretion-from-the-perfused-adrenal-medulla
#1
Seung-Yeol Na, Ki-Hwan Kim, Mi-Sung Choi, Kang-Su Ha, Dong-Yoon Lim
The present study was designed to investigate the characteristics of gintonin, one of components isolated from Korean Ginseng on secretion of catecholamines (CA) from the isolated perfused model of rat adrenal gland and to clarify its mechanism of action. Gintonin (1 to 30 µg/ml), perfused into an adrenal vein, markedly increased the CA secretion from the perfused rat adrenal medulla in a dose-dependent fashion. The gintonin-evoked CA secretion was greatly inhibited in the presence of chlorisondamine (1 µM, an autonomic ganglionic bloker), pirenzepine (2 µM, a muscarinic M1 receptor antagonist), Ki14625 (10 µM, an LPA1/3 receptor antagonist), amiloride (1 mM, an inhibitor of Na(+)/Ca(2+) exchanger), a nicardipine (1 µM, a voltage-dependent Ca(2+) channel blocker), TMB-8 (1 µM, an intracellular Ca(2+) antagonist), and perfusion of Ca(2+)-free Krebs solution with 5mM EGTA (a Ca(2+)chelater), while was not affected by sodium nitroprusside (100 µM, a nitrosovasodialtor)...
November 2016: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/27824680/angiotensin-ii-receptor-blockers-following-intravenous-nicardipine-administration-to-lower-blood-pressure-in-patients-with-hypertensive-intracerebral-hemorrhage-a-prospective-randomized-study
#2
Joji Inamasu, Shunsuke Nakae, Kazuhide Adachi, Yuichi Hirose
BACKGROUND AND OBJECTIVE: In patients with hypertensive intracerebral hemorrhage (HICH), intravenous nicardipine is primarily used to lower blood pressure (BP). However, there are few studies investigating the role of oral antihypertensives administered after intravenous nicardipine to prevent BP from rising. Angiotensin II receptor blockers (ARBs) may be beneficial in HICH patients not only as antihypertensives but also by lowering plasma catecholamine levels. A prospective randomized study was conducted between January 2015 and March 2016 to comparatively evaluate the efficacy of two ARBs (azilsartan vs...
November 7, 2016: Blood Pressure Monitoring
https://www.readbyqxmd.com/read/27823932/n-and-l-type-calcium-channels-blocker-cilnidipine-ameliorates-neuropathic-pain
#3
Shohei Yamamoto, Yuma Suzuki, Hideki Ono, Kazuhiko Kume, Masahiro Ohsawa
Cilnidipine is a dihydropyridine derivative that inhibits N-type and L-type voltage-gated Ca(2+) channels (VDCCs). We recently reported that a selective N-type VDCC blocker attenuated the spinal long-term potentiation (LTP) of C-fiber-evoked field potentials recorded in the spinal dorsal horn of rats, which served as a model for examining synaptic function during central pain sensitization. In this study, we investigated the effects of cilnidipine on the changes related to neuropathic pain induced by nerve injury...
November 4, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27813130/p-glycoprotein-inhibition-sensitizes-human-breast-cancer-cells-to-proteasome-inhibitors
#4
Rahul R Deshmukh, Seongho Kim, Yasmine Elghoul, Q Ping Dou
Although effective for the treatment of hematological malignancies, the FDA approved proteasome inhibitors bortezomib and carfilzomib have limited efficacy in solid tumors including triple negative breast cancer (TNBC). Chemotherapy is the only option for treating TNBC due to the absence of specific therapeutic targets. Therefore, development of new TNBC therapeutic strategies has been warranted. We studied whether P-glycoprotein (P-gp) inhibition could sensitize TNBC cells to proteasome inhibitors. When verapamil, a P-gp inhibitor, was combined with the proteasome inhibitor MG132, bortezomib or carfilzomib, the cytotoxic effects and apoptosis in TNBC MDA-MB-231 cells were enhanced, compared to each treatment alone...
November 4, 2016: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/27757002/therapeutic-interchange-of-clevidipine-for-sodium-nitroprusside-in-cardiac-surgery
#5
Joseph E Cruz, Zachariah Thomas, David Lee, David M Moskowitz, Jeff Nemeth
BACKGROUND: Generic price inflation has resulted in rising acquisition costs for sodium nitroprusside (SNP), an agent historically described as the drug of choice for the treatment of perioperative hypertension in cardiac surgery. PURPOSE: To describe the implementation and cost avoidance achieved by utilizing clevidipine as an alternative to SNP in cardiac surgery patients at a 520-bed community teaching hospital that performs more than 300 cardiac surgeries each year...
October 2016: P & T: a Peer-reviewed Journal for Formulary Management
https://www.readbyqxmd.com/read/27753872/ish-aha-1-a-case-of-refractory-hypertension-controlled-by-repeated-renal-denervation-and-celiac-plexus-block-a-case-of-refractory-sympathetic-overload
#6
Chan Joo Lee, Yeongmin Woo, Byeong-Keuk Kim, Kyung Bong Yoon, Hae-Young Lee, Sungha Park
A 30-year-old woman was referred to our hospital due to high blood pressure, dizziness, headache and blurred vision. She had past history of preeclampsia and gestational hypertension 4 years ago but she had not taken antihypertensive medication in spite of remained hypertension after delivery. She was hospitalized for fever due to urinary tract infection and severe hypertension which was above 210/140 mmHg. Despite maximal medical treatment with telmisartan 80 mg, nifedipine 120 mg, carvedilol 50 mg, doxazocin 8 mg, chlorthalidone 50 mg, spironolactone 50 mg#2, isosorbide dinitrate 80 mg and intermittent intravenous administration of nicardipine and labetalol, her systolic blood pressure remained above 160 mmHg and repeatedly measured above 200 mmHg...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27729218/location-of-contact-residues-in-pharmacologically-distinct-drug-binding-sites-on-p-glycoprotein
#7
Rituparna Mittra, Megan Pavy, Nanditha Subramanian, Anthony M George, Megan L O'Mara, Ian D Kerr, Richard Callaghan
The multidrug resistance P-glycoprotein (P-gp) is characterised by the ability to bind and/or transport an astonishing array of drugs. This poly-specificity is imparted by at least four pharmacologically distinct binding sites within the transmembrane domain. Whether or not these sites are spatially distinct has remained unclear. Biochemical and structural investigations have implicated a central cavity as the likely location for the binding sites. In the present investigation, a number of contact residues that are involved in drug binding were identified through biochemical assays using purified, reconstituted P-gp...
October 8, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27726375/semi-empirical-rules-to-determine-drug-sensitivity-and-ionization-efficiency-in-sims-using-a-model-tissue-sample
#8
Jean-Luc Vorng, Anna M Kotowska, Melissa K Passarelli, Andrew West, Peter S Marshall, Rasmus Havelund, Martin P Seah, Colin T Dollery, Paulina D Rakowska, Ian S Gilmore
There is an increasing need in the pharmaceutical industry to reduce drug failure at late stage and so reduce the cost of developing a new medicine. Since most drug targets are intracellular this requires a better understanding of the drug disposition within a cell. Secondary ion mass spectrometry has been identified as a potentially important technique to do this as it is label-free and allows imaging in 3D with sub-cellular resolution and recent studies have shown promise for amiodarone. An important analytical parameter is sensitivity and we measure this in a bovine liver homogenate reference sample for twenty drugs representing important class-types relevant to the pharmaceutical industry...
October 11, 2016: Analytical Chemistry
https://www.readbyqxmd.com/read/27725386/molecular-mechanism-of-dihydropyridine-ca-2-channel-blockers-in-pulmonary-hypertension
#9
Aya Yamamura
 Idiopathic pulmonary arterial hypertension (IPAH) is a progressive and fatal disease of unidentified pathogenesis. IPAH is pathologically characterized as sustained vasoconstriction and vascular remodeling of the pulmonary artery. In pulmonary arterial smooth muscle cells (PASMCs), an increase in cytosolic Ca(2+) concentration ([Ca(2+)]cyt) triggers vasoconstriction and stimulates cell proliferation leading to vascular remodeling. However, dihydropyridine-type voltage-dependent Ca(2+) channel blockers are only effective in very few patients with IPAH (<10%)...
2016: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/27643109/ish-aha-1-a-case-of-refractory-hypertension-controlled-by-repeated-renal-denervation-and-celiac-plexus-block-a-case-of-refractory-sympathetic-overload
#10
Chan Joo Lee, Yeongmin Woo, Byeong-Keuk Kim, Kyung Bong Yoon, Hae-Young Lee, Sungha Park
A 30-year-old woman was referred to our hospital due to high blood pressure, dizziness, headache and blurred vision. She had past history of preeclampsia and gestational hypertension 4 years ago but she had not taken antihypertensive medication in spite of remained hypertension after delivery. She was hospitalized for fever due to urinary tract infection and severe hypertension which was above 210/140 mmHg. Despite maximal medical treatment with telmisartan 80 mg, nifedipine 120 mg, carvedilol 50 mg, doxazocin 8 mg, chlorthalidone 50 mg, spironolactone 50 mg#2, isosorbide dinitrate 80 mg and intermittent intravenous administration of nicardipine and labetalol, her systolic blood pressure remained above 160 mmHg and repeatedly measured above 200 mmHg...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27636540/topical-vasodilators-in-microsurgery-what-is-the-evidence
#11
Jacob Rinkinen, Eric G Halvorson
Background Topical vasodilators are frequently used during free tissue transfer to prevent and treat vasospasm and microvascular thrombosis. A variety of agents have been studied and are available, yet most microsurgeons select an agent based on anecdotal evidence or personal training. Our aim was to review the literature on topical vasodilators so microsurgeons can make more informed decisions about which agent to use. Methods A systemic review of the literature was performed on PubMed, EMBASE, and Google Scholar using keywords "topical vasodilator," "antispasmodic," "vasospasm," "free flaps," and "microsurgery...
September 16, 2016: Journal of Reconstructive Microsurgery
https://www.readbyqxmd.com/read/27633557/calcium-homeostasis-and-protein-kinase-phosphatase-balance-participate-in-nicotine-induced-memory-improvement-in-passive-avoidance-task-in-mice
#12
Agnieszka Michalak, Grazyna Biala
Long-term potentiation (LTP) and long-term depression (LTD) depend on specific postsynaptic Ca(2+)/calmodulin concentration. LTP results from Ca(2+) influx through the activated NMDA receptors or voltage-gated calcium channels (VGCCs) and is linked with activation of protein kinases including mitogen-activated protein kinase (MAPK). Weaker synaptic stimulation, as a result of low Ca(2+) influx, leads to activation of Ca(2+)/calmodulin-dependent phosphatase (calcineurin - CaN) and triggers LTD. Interestingly, both memory formation and drug addiction share similar neuroplastic changes...
September 12, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27612699/cyclodextrin-polyhydrazine-degradable-gels-for-hydrophobic-drug-delivery
#13
Esmat Jalalvandi, Jaydee Cabral, Lyall R Hanton, Stephen C Moratti
An injectable and biocompatible hydrogel system was designed for hydrophobic drug delivery. This hydrogel consisted of degradable polymers with cyclodextrin (CD) moieties. CD groups were used to increase the solubility of a hydrophobic molecule (nicardipine) in an aqueous solution through the formation of the inclusion complex. Two sets of gels were prepared by mixing oxidized dextran (DA) and CD functionalized polyhydrazine (PH) at physiological conditions and different level of crosslinking via hydrazone bonds...
December 1, 2016: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/27556614/comparing-the-outcomes-of-different-agents-to-treat-vasospasm-at-microsurgical-anastomosis-during-the-papaverine-shortage
#14
Joseph A Ricci, Pieter G Koolen, Jinesh Shah, Adam M Tobias, Bernard T Lee, Samuel J Lin
BACKGROUND: Papaverine remains popular for treating intraoperative vasospasm, but the recent shortage has forced surgeons to trial antispasmodic agents unproven in microsurgery but commonly used in other body areas. During this shortage, the authors have used topical lidocaine and nicardipine to break intraoperative vasospasm. This study aims to analyze the outcomes of these medications on flap complications compared with papaverine. METHODS: All consecutive free flaps performed for breast reconstruction at a single institution were reviewed...
September 2016: Plastic and Reconstructive Surgery
https://www.readbyqxmd.com/read/27554460/-management-of-arterial-hypertension-before-20weeks-gestation-in-pregnant-women
#15
Florent Seguro, Béatrice Duly Bouhanick, Bernard Chamontin, Jacques Amar
In the first 6 months of pregnancy, the primary goal of antihypertensive treatment is to prevent the complications of severe hypertension. Initiation of antihypertensive drug treatment is recommended in pregnant women with severe hypertension (blood pressure>160/110mmHg). Initiation of antihypertensive drug treatment should also be considered in pregnant women at high cardiovascular risk (diabetes, chronic kidney disease, personal history of cardiovascular disease) with moderate hypertension (blood pressure between 140-159/90-109mmHg)...
July 2016: La Presse Médicale
https://www.readbyqxmd.com/read/27498589/comprehensive-evaluation-of-liver-microsomal-cytochrome-p450-3a-cyp3a-inhibition-comparison-of-cynomolgus-monkey-and-human
#16
Zuzana E Haarhoff, Melissa A Kramer, Tatyana A Zvyaga, Jun Zhang, Priyadeep Bhutani, Murali Subramanian, A David Rodrigues
1. Members of the cytochrome P450 3A (CYP3A) subfamily metabolize numerous compounds and serve as the loci of drug-drug interactions (DDIs). Because of high amino acid sequence identity with human CYP3A, the cynomolgus monkey has been proposed as a model species to support DDI risk assessment. 2. Therefore, the objective of this study was to evaluate 35 known inhibitors of human CYP3A using human (HLM) and cynomolgus monkey (CLM) liver microsomes. Midazolam was employed as substrate to generate IC50 values (concentration of inhibitor rendering 50% inhibition) in the absence and presence of a preincubation (30 mins) with NADPH...
August 8, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/27453704/use-of-continuous-infusion-hydralazine-in-a-pediatric-patient-on-mechanical-circulatory-support
#17
Nicholas O Dillman, Marc M Anders, Brady S Moffett
Hydralazine is a direct peripheral arterial vasodilator used for acute hypertension. Usually administered as a bolus dose, continuous infusion has been described during pregnancy for preeclampsia and eclampsia and in limited reports in cardiac surgeries for afterload reduction. This case describes the use of continuous infusion hydralazine for afterload reduction in an infant receiving extracorporeal membrane oxygenation (ECMO) post-cardiac surgery. Postsurgery, the patient's mean arterial pressures (MAPs) could not be controlled despite escalating doses of vasodilatory medications including nitroprusside, nicardipine, and milrinone; hence, continuous infusion hydralazine was initiated...
May 2016: Journal of Pediatric Pharmacology and Therapeutics: JPPT: the Official Journal of PPAG
https://www.readbyqxmd.com/read/27423368/risk-factors-of-nicardipine-related-phlebitis-in-acute-stroke-patients
#18
Kei Kawada, Tsuyoshi Ohta, Koudai Tanaka, Naoto Kadoguchi, Souichi Yamamoto, Masanori Morimoto
BACKGROUND AND PURPOSE: Intravenous nicardipine is generally used to treat hypertension in acute stroke patients but is associated with frequent phlebitis. We aimed to identify the incidence and risk factors of phlebitis in such patients. METHODS: The incidence and risk factors of phlebitis were investigated in 358 acute stroke patients from July 2014 to June 2015. RESULTS: In total, 138 patients received intravenous nicardipine. Of 45 (12...
October 2016: Journal of Stroke and Cerebrovascular Diseases: the Official Journal of National Stroke Association
https://www.readbyqxmd.com/read/27352538/-regulation-mechanism-of-ginkgo-dipyridamolum-for-calcium-homeostasis-on-cardioprotective-effect-during-ischemia-reperfusion-injury
#19
Jing Wang, Hai-hua Wang, Ping-ping Zhou, Yu-xin Jiang
OBJECTIVE: To explore regulatory mechanism of Ginkgo-dipyridamolum (GD) for calcium homeostasis on cardioprotective effect during ischemia reperfusion injury in the isolated rat heart. METHODS: 40 male SD-rats were randomly divided into five groups (n = 8): normal control group (NC), ischemia reperfusion group (IR), GD precondition group (GD + IR), Nicardipine and GD precondition group( Nic + GD + IR), and LaCl3 and GD precondition group (LaCl, + GD +IR). The hearts of rats were isolated after anesthesia and performed to profuse with Langendorff equipment...
December 2015: Zhong Yao Cai, Zhongyaocai, Journal of Chinese Medicinal Materials
https://www.readbyqxmd.com/read/27346708/systematic-approach-to-optimize-a-pretreatment-method-for-ultrasensitive-liquid-chromatography-with-tandem-mass-spectrometry-analysis-of-multiple-target-compounds-in-biological-samples
#20
Kazutaka Togashi, Kuninori Mutaguchi, Setsuko Komuro, Makoto Kataoka, Hiroshi Yamazaki, Shinji Yamashita
In current approaches for new drug development, highly sensitive and robust analytical methods for the determination of test compounds in biological samples are essential. These analytical methods should be optimized for every target compound. However, for biological samples that contain multiple compounds as new drug candidates obtained by cassette dosing tests, it would be preferable to develop a single method that allows the determination of all compounds at once. This study aims to establish a systematic approach that enables a selection of the most appropriate pretreatment method for multiple target compounds without the use of their chemical information...
August 2016: Journal of Separation Science
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