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Drug Research

Poonam Giri, Harilal Patel, Nuggehally R Srinivas
Avibactam, a potent non-β lactam β-lactamase inhibitor, was recently approved in the USA for combination use with ceftazidime, a cephalosporin antibiotic drug. The addition of avibactam potentiates the antimicrobial drug ceftazidime, which otherwise would have been susceptible to β-lactamases produced by variety of Gram negative pathogens. The focus of this review was to provide clinical pharmacokinetic data of avibactam to cover absorption, distribution, metabolism, and excretion aspects including any potential for avibactam to show drug-drug interactions in the clinic...
October 8, 2018: Drug Research
Eiji Kutoh, Jyunka Hayashi
This report describes the effect of administration (n=3) or withdrawal (n=2) of canagliflozin, a sodium-glucose co-transporters 2 (SGLT-2) inhibitor, on cardiac function in relation to ketone bodies. Three cases received and two cases discontinued canagliflozin. Changes of heart function with ultrasonography (EF: ejection fraction and %FS: functional shortening) and cardiometabolic parameters including ketone bodies (acetoacetate/beta-hydroxybutylate) were compared at 3 months. 69, 68 and 60 years old male patients A, B and C, respectively with moderately decreased heart function received canagliflozin 100 mg/day...
October 8, 2018: Drug Research
Khadeeja Khan, Abul Kalam Najmi, Mohd Akhtar
AIM: In the present study quercetin was studied for its role in inflammation, oxidative stress markers and 5-HT levels in unpredictable chronic mild stress (UCMS) animal model of depression. MATERIALS AND METHODS: The mice were randomized into different groups trained for UCMS protocol followed by different drug treatments. Treatments were started after 2 weeks from the start of UCMS protocol and continued up to 6 weeks. The behavioral tests such as modified forced swimming (MFST), tail suspension (TST) and open field tests were performed on week 6, at least 24 h after the last drug treatment...
October 8, 2018: Drug Research
Fatima Alaba Ibrahim, Lamidi Ajao Usman, Jubril Olayinka Akolade, Oluwafemi Ayodeji Idowu, Azeemat Titilola Abdulazeez, Aliyu Olalekan Amuzat
Citrus aurantifolia leaf essential oil was extracted via hydrodistillation, chemical composition of the oil was analyzed using gas chromatography-mass spectrometry and its antidiabetic potentials was assessed in alloxan-induced hyperglycaemic rats using metformin as the reference drug for comparison. Chemical analysis showed that D-limonene (57.84%) was the major constituent of the oil. Other notable compounds identified were neral (7.81%), linalool (4.75%), sulcatone (3.48%) and isogeraniol (3.48%). Intraperitoneal administration of C...
October 1, 2018: Drug Research
Aashiq Hussain Bhat, Khalid Bashir Dar, Mohammad Afzal Zargar, Akbar Masood, Showkat Ahmad Ganie
This study evaluates the ameliorative potential of Rheum spiciformis methanolic (RS-MeOH) extract in reducing oxidative stress and hyperglycemia in albino rats along with characterization of possible therapeutic compound(s). Groups treated with 50 and 100 mg/kg bw plant extract (RS-MeOH ) decrease blood glucose levels from 359.9±8.2 to 209.5±8.5 mg/dl (50 mg/kg bw) and 354.7±13.3 to 162.5±7.4 mg/dl (100 mg/kg bw) on the 0th and 14th day (P<0.001) respectively. This reduction in blood glucose was significant as compared to glibenclamide (20 mg/dl) which reduced glucose levels from 297...
September 12, 2018: Drug Research
Kannan Sridharan, Gowri Sivaramakrishnan
BACKGROUND: Vancomycin, metronidazole, fidaxomicin, teicoplanin, fusidic acid and bacitracin have been recommended for the treatment of Clostridium difficile infections (CDI). We conducted a Bayesian network meta-analysis comparing all the antimicrobial agents used in CDI. METHODS: Electronic databases were searched for randomized controlled trials comparing antimicrobial agents used for CDI. Risk of bias was assessed. Random effects model was used to derive the mixed treatment comparison estimates...
September 7, 2018: Drug Research
Xiumin Li, Yu Xue, Liang Pang, Zhaoshui ShangGuan, Yutian Pan
Obesity is a common and increasingly prevalent human condition due to unhealthy diet and less-exercise lifestyle. Development of obesity is associated with substantial modulation of adipose tissue structure. The expansion of adipose tissue is linked to the development of its vasculature, and modulation of angiogenesis may have the potential to impair adipose tissue development. In this study, we used obesity model of zebrafish fed by egg yolk to investigate the effect of Lysimachia capillipes on the obesity...
September 7, 2018: Drug Research
Xingang Li, Shusen Sun, Xiaowei Xu, Zhigang Zhao, Wei Li
BACKGROUND AND STUDY AIM: Genetic polymorphisms may play a role in muscular injury associated with simvastatin, but results were inconclusive. This study aimed to summarize evidence from the literature investigating the effects of genetic polymorphism on simvastatin-induced myopathy. METHODS: Studies regarding the association between genetic polymorphisms and simvastatin-induced myopathy were retrieved through electronic databases from February 1, 1990 to March 15, 2018...
September 7, 2018: Drug Research
Johsuke Hara, Kazuo Kasahara, Noriyuki Ohkura, Kenta Yamamura, Tamami Sakai, Miki Abo, Naohiko Ogawa, Keigo Saeki, Hayato Koba, Satoshi Watanabe, Yuka Uchida, Yuichi Tambo, Takashi Sone, Hideharu Kimura
OBJECTIVE: In Japan, most asthma deaths occur among the elderly. We should improve the control of asthma in elderly patients to reduce the number of deaths due to asthma. This retrospective study aimed to evaluate the efficacy of tiotropium RespimatⓇ (Tio-Res) in symptomatic, never-smoking, elderly asthmatics with irreversible airflow limitation despite the use of high-dose inhaled corticosteroids (ICS) plus long-acting β2 -adrenoceptor agonists (LABA). METHODS: The Asthma Control Test™ (ACT), pulmonary function tests, morning and evening peak flow (mPEF, ePEF, respectively, evaluated with an ASSESS® peak flow meter), and respiratory impedance (assessed with MostGraph® ) were measured before and after a minimum of one year of Tio-Res 5 µg/day administration...
September 7, 2018: Drug Research
Abhishek Dixit, Sadanand Rangnathrao Mallurwar, Suresh P Sulochana, Mohd Zainuddin, Ramesh Mullangi
A simple, sensitive and rapid assay method has been developed and validated as per regulatory guideline for the estimation of tofacitinib on mice dried blood spots (DBS) using liquid chromatography coupled to tandem mass spectrometry with electro spray ionization in the positive-ion mode. The method employs liquid extraction of tofacitinib from DBS disk of mice whole blood followed by chromatographic separation using 5 mM ammonium acetate (pH 6.5):acetonitrile (20:80, v/v) at a flow rate of 0.60 mL/min on an X-Terra Phenyl column with a total run time 2...
September 7, 2018: Drug Research
Poornima Devi, Abha Bishnoi, Krishna Srivastava, Sunil Kumar, Ankita Srivastava, Shaheen Fatma
A number of 5-oxo-1-phenyl-4-(substituted methyl) pyrrolidine-3-carboxylic acid derivatives bearing pyrrolidine ring and methylamino residues in their structure were synthesized as potential antibacterial drugs. The chemical structures of all the compounds were established by their UV-Vis absorption spectroscopy, IR, 1 H, 13 C NMR and mass spectroscopy. The in vitro antibacterial screening of all novel compounds was done against gram-positive Staphylococcus aureus, Bacillus subtilis and gram-negative Pseudomonas aeruginosa...
September 7, 2018: Drug Research
Hamed Nosrati, Hossein Hamzehei, Saeed Afroogh, Seyedeh Fatemeh Ashabi, Elahe Attari, Hamidreza Kheiri Manjili
In this study we reported the synthesis of L-phenyl alanine (Phe) & L-tyrosine (Tyr) Natural Amino acids coated iron oxide magnetic nanoparticles under one-pot and in situ reaction. Functionalized iron oxide magnetic nanoparticles were characterized by X-ray diffraction (XRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Vibrating Sample Magnetometer (VSM), Fourier transform infrared spectroscopy (FTIR), Scanning electron microscopy (SEM) and Transmission electron microscopy (TEM) techniques...
September 6, 2018: Drug Research
Ari Estuningtyas, Rianto Setiabudy, Pustika Amalia Wahidiyat, Hans-Joachim Freisleben
BACKGROUND: The leaves, fruit peels, and bark of mango trees (Mangifera indica L) contain mangiferin as an active compound with known anti-oxidative and iron chelating properties. This study aims to evaluate the benefits of mangiferin in the management of iron overload. METHODS: Thirty rats were divided into five groups: normal control, rats with iron overload, and rats with iron overload treated with oral mangiferin doses of 50, 100, or 200 mg/kg BW, respectively...
September 6, 2018: Drug Research
Wojciech Danysz, Kang Jinlai, Fugang Li
"Browning" i. e. the transformation of white adipose tissue into brown-like adipose tissue could induce efficient burning of excess fat reserves via induction of non-shivering thermogenesis. For example, activation of ß3 adrenergic receptors has been show to induce such changes, however, it is still not clear, how long after termination of such a treatment, beneficial effects might be maintained. To address this question, we treated rats s.c. for 2 weeks with the ß3 agonist CL-316,243 at 1 mg/kg and assessed interscapular brown fat and inguinal white fat pads weight, UCP-1 (a marker for the brown-like fat phenotype) using immunohistochemistry and H&E staining, at different intervals after treatment termination...
September 6, 2018: Drug Research
Bijan Ghorbanpour Oskouei, Soheil Abbaspour-Ravasjani, Seyed Jamal Musavinejad, Seyed Ahmad Salehzadeh, Alireza Abdolhosseinzadeh, Hamed Hamishehkar, Kazem Ghahremanzadeh, Behrooz Shokouhi
No abstract text is available yet for this article.
August 24, 2018: Drug Research
Neli Vilhelmova-Ilieva, Rémi Jacquet, Denis Deffieux, Laurent Pouységu, Tahiri Sylla, Stefan Chassaing, Ivanka Nikolova, Stéphane Quideau, Angel S Galabov
Anti-herpes simplex virus (HSV-1) activity of 9 ellagitannins, including 6 natural compounds (castalin, vescalin, acutissimin A, epiacutissimins A and B, mongolicain) and 3 vescalagin synthetic derivatives (VgSBuSH, VgSOctSH, VgOMe), and 13 gallotannin-type compounds [Gal-01A, Gal-01B, Gal-02A, Gal-02B, Gal-03M, Gal-04A, Gal-04B, Gal-05M, Gal-07, Gal-08, Gal-09, Gal-11M (tannic acid), as well as Gal-12 (gallic acid), Gal-13 and Gal-14 (ellagic acid)] were examined in MDBK monolayer cell culture. Their antiviral activity was determined by the cytopathic effect (CPE) inhibition test and their cytotoxicity was evaluated through the neutral red uptake assay...
August 22, 2018: Drug Research
Budi Prasaja, M Maulana Syabani, Endah Sari, Uci Chilmi, Prawitasari Cahyaningsih, Theresia Weliana Kosasih
Sevelamer carbonate is a cross-linked polymeric amine; it is the active ingredient in Renvela® tablets. US FDA provides recommendation for demonstrating bioequivalence for the development of a generic product of sevelamer carbonte using in-vitro equilibrium binding study. A simple UV-vis spectrophotometry method was developed and validated for quantification of free phosphate to determine the binding parameter constant of sevelamer. The method validation demonstrated the specificity, limit of quantification, accuracy and precision of measurements...
November 2018: Drug Research
Prasun Mukherjee, Asish R Das, Raghwendra Mishra, Shovonlal Bhowmick, Achintya Saha
We have evaluated the LDH inhibitory property of novel pyrazolo[4',3':5,6][1,4]oxathiino[2,3-b]pyrazine derivatives which have been synthesized from easily available starting materials through a one-pot protocol that offers the use of elemental sulfur as the sulfur source. These newly synthesized compounds may aid to drug development for neoplastic and non-neoplastic diseases characterized by increased glucose metabolism. Additionally, they may act as suitable starting materials which can be further structurally modified for the development of new LDH inhibitors with higher efficacy and specificity...
November 2018: Drug Research
Fauzul Husna, Franciscus D Suyatna, Wawaimuli Arozal, Erni H Poerwaningsih
AIM AND OBJECTIVE: The present study aims to investigate whether the antihyperglycemic effect of Murraya koenigii is mediated by antioxidant properties and insulin mimetic effect. METHODS: Thirty Spraque - Dawley rats were induced hyperglycemia by streptozotocin and nicotinamide (STZ-NA). The STZ-NA diabetic rats were treated with an ethanolic extract of Murraya koenigii 200 mg/kg b.w and 400 mg/kg b.w. One group was treated with glibenclamide (1 mg/kg b.w)...
November 2018: Drug Research
Franziska G Leifer, Donna M Konicek, Kuan-Ju Chen, Adam J Plaunt, Dany Salvail, Charles E Laurent, Michel R Corboz, Zhili Li, Richard W Chapman, Walter R Perkins, Vladimir S Malinin
Treprostinil (TRE), a prostanoid analogue approved in the USA for the treatment of pulmonary arterial hypertension, requires continuous infusion or multiple dosing sessions per day for inhaled and oral routes of administration due to its short half-life. The inhaled drug is known to induce adverse systemic and local effects including headache, nausea, cough, and throat irritation which may be due at least in part to transiently high drug concentrations in the lungs and plasma immediately following administration [1]...
November 2018: Drug Research
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