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Pharmacology

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https://www.readbyqxmd.com/read/28052289/the-pharmacokinetic-interaction-study-between-carvedilol-and-bupropion-in-rats
#1
Maria Bianca Abrudan, Dana Maria Muntean, Ana Maria Gheldiu, Maria Adriana Neag, Laurian Vlase
BACKGROUND/AIMS: The effects of multiple-dose bupropion on the pharmacokinetics of single-dose carvedilol were investigated in order to evaluate this possible drug-drug interaction. METHODS: A preclinical study was conducted among white male Wistar rats. Each rat was cannulated on the femoral vein prior to being connected to BASi Culex ABC®. During the reference period, each rat received an intravenous and an oral dose of 3.57 mg/kg body weight (b.w.) carvedilol, at 2 days distance...
January 5, 2017: Pharmacology
https://www.readbyqxmd.com/read/28049212/enhanced-hyperthermic-responses-to-lipopolysaccharide-in-mice-exposed-to-repeated-cold-stress
#2
Tomoyoshi Miyamoto, Yoshinori Funakami, Erika Kawashita, Shiori Tomita, Ai Nomura, Nanako Sugimoto, Haruka Saeki, Takaya Miyazakia, Maho Tsubota, Seiji Ichida, Atsufumi Kawabata
Lipopolysaccharide (LPS) induces hyperthermia accompanied by various other systemic inflammatory symptoms. The rodents exposed to repeated cold (RC) stress according to a specific schedule are useful as experimental models for autonomic imbalance or fibromyalgia. It is now proven that RC-stressed mice exhibit tolerance to LPS, we examined thermal responses to LPS challenge in RC-stressed mice by monitoring core temperature using the telemetry system. Systemic administration of LPS caused bimodal hyperthermic responses in RC-stressed and unstressed mice...
January 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/28049205/bufalin-inhibits-the-inflammatory-effects-in-asthmatic-mice-through-the-suppression-of-nuclear-factor-kappa-b-activity
#3
Zibierguli Zhakeer, Maierbati Hadeer, Zumulaiti Tuerxun, Kelibiena Tuerxun
Asthma is an inflammatory airway disease characterized by increased infiltration of inflammatory cells into the airways and poor respiratory function. Bufalin is one of the biological ingredients obtained from Chansu. Bufalin was found to possess various pharmacological properties including anti-inflammatory activities. However, the effect of bufalin treatment on asthma has not yet been reported. Therefore, this study aimed to investigate the inhibitory effect of bufalin on asthmatic response in a murine model...
January 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/28049198/mechanism-of-2-3-4-5-tetrahydroxystilbene-2-o-%C3%AE-d-glucoside-induced-upregulation-of-glutamate-transporter-1-protein-expression-in-mouse-primary-astrocytes
#4
Xiangfan Chen, Wenfeng Hu, Xu Lu, Bo Jiang, Jili Wang, Wei Zhang, Chao Huang
Glutamate transporter-1 (GLT-1), a major glutamate transporter expressed in astrocytes, takes up excess glutamate from the micro-environment in order to prevent excitotoxicity. Drugs that increase GLT-1 expression may have therapeutic effects in disorders associated with neuronal excitotoxicity. 2,3,4',5-tetrahydroxystilbene 2-O-β-D-glucoside (TSG), a monomer of stilbene from polygonummultiflorum, exerts neuroprotection in a range of experimental models such as Alzheimer's disease and brain ischemia. In this study, we evaluated the effect of TSG on GLT-1 protein expression in mouse primary-cultured astrocytes...
January 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/28049192/combined-memantine-and-donepezil-treatment-improves-behavioral-and-psychological-symptoms-of-dementia-like-behaviors-in-olfactory-bulbectomized-mice
#5
Yasushi Yabuki, Kazuya Matsuo, Koga Hirano, Yasuharu Shinoda, Shigeki Moriguchi, Kohji Fukunaga
Memantine, an uncompetitive N-methyl-D-aspartate receptor antagonist, and the cholinesterase inhibitor, donepezil, are approved in most countries for treating moderate-to-severe Alzheimer's disease (AD). These drugs have different molecular targets; thus, it is expected that the effects of combined treatment would be synergistic. Some reports do show memantine/donepezil synergy in ameliorating cognition in AD model animals, but their combined effects on behavioral and psychological symptoms of dementia (BPSD)-like behaviors have not been addressed...
January 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/28049190/the-efficacy-of-rituximab-combined-with-131i-for-ophthalmic-outcomes-of-graves-ophthalmopathy-patients
#6
Jiagen Li, Zhangsheng Xiao, Xianjie Hu, Yun Li, Xing Zhang, Songze Zhang, Weikun Gong, Jianqiang Zhao, Xuemei Ye
PURPOSE: The purpose of this study is to examine the effectiveness of introducing both rituximab (RTX) and 131I for active Graves' ophthalmopathy (GO) with hyperthyroidism. METHODS: In total, 217 patients suffering from active GO with hyperthyroidism were included in this research. All subjects were randomly assigned to 3 groups. Patients in group A solely received 131I treatment; group B1 underwent a methylprednisolone treatment in combination with 131I treatment; and group B2 received an RTX in combination with 131I treatment...
January 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/27992867/dronedarone-modulates-m1-and-m3-muscarinic-receptors-with-subtype-selectivity-functional-selectivity-and-probe-dependence
#7
Gihan M Jayasuriya, Gwendolynne Elmslie, Ethan S Burstein, John Ellis
We have previously reported that amiodarone interacts with a novel allosteric site on muscarinic receptors. Amiodarone's most striking effect is to enhance the maximal response elicited by muscarinic agonists at the M1, M3, and M5 receptors. Furthermore, the quaternary analog N-ethylamiodarone (NEA) is inhibitory at these receptors and appears to compete with amiodarone at that allosteric site. In the present studies, we show that dronedarone also modulates Gq-mediated responses at M1 and M3, although in a more discriminating manner...
December 20, 2016: Pharmacology
https://www.readbyqxmd.com/read/27988509/rivaroxaban-induced-gastrointestinal-bleeding-presenting-as-acute-colon-obstruction
#8
Merav Cohen, Hadar Nevo, Dan Hershko, Alexander Becker
Rivaroxaban is a member of the novel target-specific oral anticoagulants (TSOACs) family of drugs recently approved for the prevention and treatment of venous thromboembolism events. A major drawback of the drug is its potential for causing severe hemorrhagic events, which may be difficult to treat in an emergency setting due to lack of effective antidote. Here, we describe a case of acute gastrointestinal (GI) hemorrhage leading to complete colon obstruction in a patient treated with rivaroxaban. Summary and Key Messages: The case presented here demonstrates a chain of events originating from an unprovoked intramural bleeding in a patient using rivaroxaban, leading to an organized giant clot formation, and to complete colon obstruction...
December 15, 2016: Pharmacology
https://www.readbyqxmd.com/read/27931022/hydrogen-sulfide-and-t-type-ca2-channels-in-pain-processing-neuronal-differentiation-and-neuroendocrine-secretion
#9
Kazuki Fukami, Fumiko Sekiguchi, Atsufumi Kawabata
BACKGROUND: Hydrogen sulfide (H2S), a gasotransmitter, is generated from L-cysteine by mainly 3 enzymes, cystathionine-γ-lyase (CSE), cystathionine-β-synthase, and 3-mercaptopyruvate sulfurtransferase in cooperation with cysteine aminotransferase. The H2S-forming enzymes, particularly CSE, are overexpressed under the pathological conditions such as inflammation, neuronal or neuroendocrine differentiation and cancer development. Given that Cav3.2 T-type Ca2+ channels mediate some of the biological activity of H2S, we focus on the role of the H2S/Cav3...
December 9, 2016: Pharmacology
https://www.readbyqxmd.com/read/27889779/tanshinone-iia-affects-autophagy-and-apoptosis-of-glioma-cells-by-inhibiting-phosphatidylinositol-3-kinase-akt-mammalian-target-of-rapamycin-signaling-pathway
#10
Lijuan Ding, Shudong Wang, Weiyao Wang, Peng Lv, Donghai Zhao, Feier Chen, Tianjiao Meng, Lihua Dong, Ling Qi
OBJECTIVE: To test the effects of Tanshinone IIA (Tan IIA) on cell viability, cycle, apoptosis, and autophagy of human glioma cell U251 by regulating phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) signal pathway. METHODS: Tan IIA and PI3K agonist (740 Y-P) were used to treat glioma cells U251. MTT assay was used to assess cell viability and flow cytometry was used to detect cell apoptosis and cell cycle. The expressions of apoptosis-related proteins (Bcl-2 and Bax), autophagy-related proteins (LC3B and Beclin 1) and PI3K/Akt/mTOR signal pathway-associated proteins (p-PI3K, p-Akt and p-mTOR) were evaluated by Western blotting...
November 26, 2016: Pharmacology
https://www.readbyqxmd.com/read/27832658/anaphylaxis-to-over-the-counter-flurbiprofen-in-a-child
#11
Mattia Giovannini, Lucrezia Sarti, Simona Barni, Neri Pucci, Elio Novembre, Francesca Mori
Non-steroidal anti-inflammatory drugs are suspected to cause drug hypersensitivity very frequently in paediatric patients. In this article, we describe the first case of anaphylaxis to flurbiprofen in a child and provide insight into the possibility of severe reactions and even anaphylaxis to over-the-counter flurbiprofen. Finally, the importance of a rigorous allergy work-up in reaching a confident diagnosis and providing the patient with a safe alternative is shown.
November 11, 2016: Pharmacology
https://www.readbyqxmd.com/read/27816979/evaluation-of-the-potential-pharmacokinetic-interaction-between-atomoxetine-and-fluvoxamine-in-healthy-volunteers
#12
Ioana Todor, Adina Popa, Maria Neag, Dana Muntean, Corina Bocsan, Anca Buzoianu, Laurian Vlase, Ana-Maria Gheldiu, Corina Briciu
BACKGROUND/AIMS: Attention deficit hyperactivity disorder (ADHD) is frequently associated with other psychiatric pathologies. Therefore, the present study investigated a possible pharmacokinetic interaction between atomoxetine (ATX), a treatment option for ADHD, and an antidepressant, namely, fluvoxamine (FVX). METHODS: Designed as an open-label, non-randomized clinical trial, the study included 2 periods. In period 1 (reference), each subject received ATX 25 mg (single-dose), whereas in period 2 (test), all subjects were given a combination of ATX 25 mg + FVX 100 mg, following a 6-day pretreatment regimen with the enzymatic inhibitor...
November 5, 2016: Pharmacology
https://www.readbyqxmd.com/read/27806372/generation-and-measurement-of-chlorine-dioxide-gas-at-extremely-low-concentrations-in-a-living-room-implications-for-preventing-airborne-microbial-infectious-diseases
#13
Norio Ogata, Koushirou Sogawa, Yasuhiro Takigawa, Takashi Shibata
BACKGROUND/AIMS: Preventing respiratory diseases caused by airborne microbes in enclosed spaces is still not satisfactorily controlled. At extremely low concentrations (about 30 parts per billion), chlorine dioxide (ClO2) gas can inactivate airborne microbes and prevent respiratory disease. It has no toxic effect on animals at this level. However, controversies still remain regarding how to measure concentrations of ClO2 gas at such low levels. It is therefore necessary to prove that measured gas concentrations are accurate and reproducible...
November 2, 2016: Pharmacology
https://www.readbyqxmd.com/read/27798943/effects-of-distigmine-on-electrical-field-stimulation-induced-contraction-of-mouse-urinary-bladder-smooth-muscles
#14
Keisuke Obara, Yurina Kobayashi, Daisuke Chino, Yoshio Tanaka
Distigmine bromide (distigmine), a reversible carbamate cholinesterase inhibitor, is used in Japan for treating detrusor underactivity, myasthenia gravis, and glaucoma. Although there is clinical evidence about the effectiveness of distigmine in the treatment of detrusor underactivity, mechanisms by which distigmine restores impaired urinary bladder smooth muscle (UBSM) contractility have not been fully investigated. The aims of this study were to investigate the potentiating effects of distigmine on UBSM contractions in response to parasympathetic nerve stimulation induced by electrical field stimulation (EFS) in mice...
November 1, 2016: Pharmacology
https://www.readbyqxmd.com/read/27788517/the-preventive-effect-of-the-traditional-japanese-herbal-medicine-hochuekkito-against-influenza-a-virus-via-autophagy-in-vitro
#15
Keita Takanashi, Katsuaki Dan, Sho Kanzaki, Hideki Hasegawa, Kenji Watanabe, Kaoru Ogawa
BACKGROUND: Hochuekkito (HKT), a traditional Japanese herbal medicine, enhances the immunity of elderly or weak individuals. It is also known to have preventive effects against influenza clinically. However, the detailed mechanisms of the preventive effects have not been clarified. We examined the relationship between the preventive effects of HKT and autophagy, a known stress response and quality control mechanism, using Madin-Darby canine kidney cells and influenza A/PR/8/34 (H1N1) virus...
October 28, 2016: Pharmacology
https://www.readbyqxmd.com/read/27771722/inhibitory-effects-of-antidepressants-on-acetylcholine-induced-contractions-in-isolated-guinea-pig-urinary-bladder-smooth-muscle
#16
Junji Uno, Keisuke Obara, Hiroko Suzuki, Satomi Miyatani, Daisuke Chino, Takashi Yoshio, Yoshio Tanaka
BACKGROUND/AIMS: To investigate the potential inhibitory effects of 18 clinically available antidepressants on acetylcholine (ACh)-induced contractions in guinea pig urinary bladder smooth muscle (UBSM) in order to predict whether they may induce voiding impairment. METHODS: Concentration-response curves for ACh-induced contractions in guinea pig UBSM strips were obtained in the absence or presence of selected antidepressants. When inhibitory effects indicated competitive antagonism, pA2 values against ACh were calculated and compared to plausible antidepressant blood concentrations...
October 22, 2016: Pharmacology
https://www.readbyqxmd.com/read/27756073/cardiovascular-profile-of-propranolol-after-multiple-dosing-in-infantile-hemangioma
#17
Patrizia Salice, Mario Giovanni Bianchetti, Alessandra Giavarini, Erica Gondoni, Riccardo Cavalli, Anna Maria Colli, Federico Lombardi
Propranolol is becoming the treatment of choice for complicated infantile hemangioma. We report here data on peripheral blood flow, O2-saturation, electrocardiographic PR-interval, left ventricular function, blood pressure and heart rate that were assessed before and during treatment for ≥4 weeks with propranolol 2 mg/kg of body weight daily in 67 infants <12 months of age in normal sinus rhythm and with structurally normal hearts. Management with propranolol was well tolerated in all and did not modify peripheral blood flow, O2-saturation, electrocardiographic PR-interval and left ventricular fractional shortening or ejection fraction...
October 19, 2016: Pharmacology
https://www.readbyqxmd.com/read/27756064/effects-of-allyl-isothiocyanate-acetaminophen-and-dipyrone-in-the-guinea-pig-ileum
#18
Josef Donnerer, Ingrid Liebmann
Allyl isothiocyanate (AITC, mustard oil, 50-200 µmol/l), depending on specific dosages, inhibited the cholinergic twitch response in the longitudinal muscle-myenteric plexus (LMMP) strip of the guinea-pig ileum. AITC also induced short-lasting contractile responses, and decreases of the basal tone of the LMMP strip at low concentrations and increases at high concentrations. Hexamethonium, a blocker of nicotinic ganglionic transmission, was able to prevent the AITC-evoked inhibitory effect, an effect that was also observed with the opioid antagonist naloxone...
October 19, 2016: Pharmacology
https://www.readbyqxmd.com/read/27736819/efficacy-of-fu-yuan-capsule-in-the-healing-of-fractures-of-the-lower-end-of-the-radius-in-a-rabbit-model
#19
Wei Wei, Biao-Fang Wei, Jian Cai, Wei He, Lin Wan, Ying Guan
OBJECTIVE: The aim of the study was to explore the efficacy of Fu-Yuan Capsule in the healing of fractures of the lower end of the radius in a rabbit model. METHODS: After establishing a rabbit fracture model, all animals were randomly divided into the model group (n = 24), the Fu-Yuan Capsule group (n = 24), and the Shenyang Hongyao group (n = 24). The X-ray was applied to observe the course of fracture healing at 2, 4, 6, and 8 weeks after treatment. Haematoxylin-eosin staining and immunohistochemical staining were used to determine the histological change and the expression of bone morphogenetic protein-2 (BMP-2)...
October 14, 2016: Pharmacology
https://www.readbyqxmd.com/read/27694752/nerve-growth-factor-facilitates-the-innervation-of-perivascular-nerves-in-tumor-derived-neovasculature-in-the-mouse-cornea
#20
Yoko Sone, Shingo Takatori, Eiko Ochi, Yoshito Zamami, Akiko Matsuyama, Satoko Fukuhara, Mitsuhiro Goda, Yoshihisa Kitamura, Hiromu Kawasaki
BACKGROUND: Tumor neovascular vessels are not innervated by perivascular nerves. This study was an investigation of the effects of the nerve growth factor (NGF) on the distribution of perivascular nerves and neovessel formation in tumor tissues. METHODS: A gel containing DU145 prostate carcinoma cells or HT1080 fibrosarcoma cells was implanted into mouse corneas. NGF was subcutaneously administered using an osmotic mini-pump. The distribution of perivascular nerves in mouse corneas and densities of CD31-immunopositive neovessels and smooth muscles (α-smooth muscle actin, α-SMA) in tumor tissues were quantified...
October 1, 2016: Pharmacology
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