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drug substitution

Ashlea F Dassanayake, Juan J Canales
There are currently no approved medications to effectively counteract the effects of methamphetamine (METH), reduce its abuse and prolong abstinence from it. Data accumulated in recent years have shown that a range of N-substituted benztropine (BZT) analogues possesses psychopharmacological features consistent with those of a potential replacement or "substitute" treatment for stimulant addiction. On the other hand, the evidence that antidepressant therapy may effectively prevent relapse to stimulant seeking is controversial...
February 13, 2018: Neuroscience Letters
Jason Grebely, Jordan J Feld, David Wyles, Mark Sulkowski, Liyun Ni, Joe Llewellyn, Heshaam M Mir, Nika Sajed, Luisa M Stamm, Robert H Hyland, John McNally, Diana M Brainard, Ira Jacobson, Stefan Zeuzem, Marc Bourlière, Graham Foster, Nezam Afdhal, Gregory J Dore
Background: Hepatitis C virus (HCV) direct-acting antiviral therapy is effective among people receiving opioid substitution therapy (OST), but studies are limited by small numbers of nongenotype 1 (GT1) patients. The aim of this study was to evaluate the treatment completion, adherence, SVR12, and safety of sofosbuvir-based therapies in HCV patients receiving and not receiving OST. Methods: Ten phase 3 studies of sofosbuvir-based regimens included ION (ledipasvir/sofosbuvir ± ribavirin for 8, 12, or 24 weeks in GT1), ASTRAL (sofosbuvir/velpatasvir for 12 weeks in GT1-6), and POLARIS (sofosbuvir/velpatasvir and sofosbuvir/velpatasvir/voxilaprevir in GT1-6)...
February 2018: Open Forum Infectious Diseases
Marleen Häring, Julio Rodríguez-López, Santiago Grijalvo, Markus Tautz, Ramon Eritja, Victor S Martin, David Díaz Díaz
In this work we demonstrated that the simple substitution of the 1,2,4-triazole moiety in 5-(4H-1,2,4-triazol-4-yl)isophthalic acid (5-TIA) by the 1H-1,2,3-triazol-5-yl unit enables the preparation of a hydrogelator (click-TIA). In sharp contrast to 5-TIA, its isostere click-TIA undergoes self-assembly in water upon sonication, leading to the formation of stable supramolecular viscoelastic hydrogels with a critical gelation concentration of 6 g/L. Hydrogels made of click-TIA as well as hybrid hydrogels made of the mixture click-TIA + 5-TIA (molar ratio 1:0...
February 15, 2018: Molecular Pharmaceutics
Clíona Ní Cheallaigh, Aisling O'Leary, Shay Keating, Aileen Singleton, Sheila Heffernan, Eamon Keenan, Lisa Robson, Jess Sears, John Moloney, Sanjeev Arora, Colm Bergin, Suzanne Norris
The Extension of Community Healthcare Outcomes (ECHO) project is a novel educational intervention designed in New Mexico to transfer subspecialty knowledge about hepatitis C virus (HCV) to primary care providers, thereby increasing patient access to HCV care. The ECHO model has been shown to deliver educational benefits and to result in good treatment outcomes for HCV-infected individuals in the USA; however, this approach has not been assessed in a European setting. We sought to evaluate the feasibility, acceptability and implementation of the ECHO model in Ireland using a pilot study...
July 2017: BMJ Innovations
Kathleen M Gura, Andrew E Mulberg, Paul D Mitchell, John Yap, Clara Y Kim, Minjun Chen, Alexis Potemkin, Mark Puder
BACKGROUND: Intestinal failure-associated liver disease (IFALD) is complex and diagnosed by concurrent use of parenteral nutrition, clinical presentation, and alterations in hepatic biomarkers exclusive of other causes of liver disease. In comparison with individual measures, composite biomarkers may provide a more effective means for assessing disease progression and response to treatment than single parameters. Since IFALD is considered by some to be a type of drug-induced liver injury (DILI), those diagnostic criteria could potentially be used in this population...
February 2018: JPEN. Journal of Parenteral and Enteral Nutrition
R Jayasree, K Madhumathi, Deepti Rana, Murugan Ramalingam, Rakesh P Nankar, Mukesh Doble, T S Sampath Kumar
Carbonated apatite has a chemical composition quite similar to biological apatite found in native bone. The incorporation of carbonate (CO2-3) ions groups into the apatitic crystal structure can tailor its crystallinity, solubility and biological activity that benefit the bone repair and regeneration. In this study, we report a simple and elegant method of synthesizing carbonated calcium deficient hydroxyapatite (ECCDHA) nanoparticles from egg shell wastes and its efficacy has been compared with synthetic calcium deficient hydroxyapatite (SCDHA) nanoparticles...
April 1, 2018: Journal of Nanoscience and Nanotechnology
Xiaonan Liu, Youkui Zhang, Kun Xiong, Minhao Yan
Bone repair microspheres have been widely studied due to their convenience during clinical operations. In this study, beta tricalcium phosphate/sodium alginate/poly(D,L-lactic acid) (β-TCP/SA/PDLLA) composite microspheres were successfully prepared using the liquid droplet method. Then, β-TCP/SA/PDLLA composite microspheres were soaked in simulated body fluids (SBF) for 7 days, and tested in an X-ray diffractometer (XRD). The results indicated that sodium alginate (SA) and poly(D,L-lactic acid) (PDLLA) are not limiting factors for the transformation of β-TCP to HA...
June 1, 2018: Journal of Nanoscience and Nanotechnology
Ilke Akpinar, Philip Jacobs, Tien Dat Tran
BACKGROUND: Economic evaluation helps policy makers and healthcare payers make decisions on drug listing, coverage, and reimbursement. When economic evaluations are conducted before a product launch, the prices of the pharmaceuticals have to be forecast. OBJECTIVE: The aim of this study was to examine the methods of establishing proxy prices and their accuracies compared with actual market prices after the product launch. METHODS: We searched the literature for evaluations for drugs that were licensed in the US between 2010 and 2015...
March 2017: PharmacoEconomics Open
Benedikt C Melzer, Jan G Felber, Franz Bracher
Highly-substituted isoquinolines are important scaffolds in syntheses of natural products and in drug development and hence, effective synthetic approaches are required. Here we present a novel method for the introduction of a methyl group at C1 of isoquinolines. This is exemplified by a new total synthesis of the alkaloid 7-hydroxy-6-methoxy-1-methylisoquinoline. Direct metalation of 7-benzyloxy-6-methoxyisoquinoline with Knochel-Hauser base, followed by cuprate-mediated methylation gives the target alkaloid directly, but separation from the educt is cumbersome...
2018: Beilstein Journal of Organic Chemistry
Allison Germann, Daniel Shin, Christina Kuhrau, Alexander Johnson, Alex S Evers, Gustav Akk
GABAA receptors activated by the transmitter GABA are potentiated by several allosterically acting drugs including the intravenous anesthetic propofol. Propofol can also directly activate the receptor, albeit at higher concentrations. Previous functional studies have identified amino acid residues whose substitution reduces potentiation of GABA-activated receptors by propofol while enhancing the ability of propofol to directly activate the receptor. One interpretation of such observations is that the mutation has specific effects on the sites or processes involved in potentiation or activation...
February 8, 2018: Molecular Pharmacology
Shilpy Aggarwal, Deepika Paliwal, Dhirender Kaushik, Girish Kumar Gupta, Ajay Kumar
BACKGROUND: Malaria, one of the most vital infectious diseases caused by protozoan parasites of the Plasmodium genus. As P. falciparum, the cause of most of the severe cases of malaria, is increasingly resistant to available drugs such as amodioquine, chloroquine, artemisinin, and antifolates, there is an urgent need of identify new targets for chemotherapy Objective: This study screened novel pyrazole derivatives carrying iminium & benzothiazole group for antimalarial potential against P...
February 12, 2018: Combinatorial Chemistry & High Throughput Screening
Chul Min Park, Yuki Kawasaki, Alaa Refaat, Hiroaki Sakurai
Cisplatin (CDDP) and doxorubicin (DOX) are chemotherapeutic drugs that trigger apoptosis by inducing DNA-damage. A previous study using breast cancer cells demonstrated the negative feedback modulation of the epidermal growth factor receptor (EGFR) and receptor tyrosine-protein kinase erbB-2 (ErbB2) via extracellular signal-regulated kinase (ERK)-mediated phosphorylation of conserved Thr-669 and Thr-677 residues, respectively, in the juxtamembrane domain. In addition, CDDP has been identified to cause negative feedback inhibition of activated EGFR in lung cancer cells...
February 2018: Oncology Letters
Takashi Nakaoku, Takashi Kohno, Mitsugu Araki, Seiji Niho, Rakhee Chauhan, Phillip P Knowles, Katsuya Tsuchihara, Shingo Matsumoto, Yoko Shimada, Sachiyo Mimaki, Genichiro Ishii, Hitoshi Ichikawa, Satoru Nagatoishi, Kouhei Tsumoto, Yasushi Okuno, Kiyotaka Yoh, Neil Q McDonald, Koichi Goto
Resistance to vandetanib, a type I RET kinase inhibitor, developed in a patient with metastatic lung adenocarcinoma harboring a CCDC6-RET fusion that initially exhibited a response to treatment. The resistant tumor acquired a secondary mutation resulting in a serine-to-phenylalanine substitution at codon 904 in the activation loop of the RET kinase domain. The S904F mutation confers resistance to vandetanib by increasing the ATP affinity and autophosphorylation activity of RET kinase. A reduced interaction with the drug is also observed in vitro for the S904F mutant by thermal shift assay...
February 12, 2018: Nature Communications
Fangchao Bi, Shengli Ji, Henrietta Venter, Jingru Liu, Susan J Semple, Shutao Ma
3-Methoxybenzamide (3-MBA) derivatives have been identified as novel class of potent antibacterial agents targeting the bacterial cell division protein FtsZ. As one of isosteres for the amide group, 1,2,3-triazole can mimic the topological and electronic features of the amide, which has gained increasing attention in drug discovery. Based on these considerations, we prepared a series of 1H-1,2,3-triazole-containing 3-MBA analogues via isosteric replacement of the terminal amide with triazole, which had increased antibacterial activity...
February 2, 2018: Bioorganic & Medicinal Chemistry Letters
Guo-Ying Zuo, Cui-Xian Yang, Jun Han, Yu-Qing Li, Gen-Chun Wang
BACKGROUND: Clinical methicillin-resistant Staphylococcus aureus (MRSA) is a thorny problem in current anti-infective therapeutics and a challenge of new drug development. Plant prenylflavonoids possess anti-MRSA activity, but few of the prenylflavonoids have been reported the synergistic anti-MRSA effect when they are used in combination with conventional antibacterial agents. PURPOSE: This study deals with anti-MRSA activity of four prenylflavonoids from the root bark of Morus alba and their synergism with 11 conventional antibacterial agents...
January 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Tanzeela Abdul Fattah, Aamer Saeed, Pervaiz Ali Channar, Fayaz Ali Larik, Mubashir Hassan, Hussain Raza, Qamar Abbas, Sung-Yum Seo
The present article illustrated the synthesis and characterization of a novel series of (E)-4-(substituted-benzylideneamino)-2H-chromen-2-one derivatives 4A-4J: in good to excellent yields. The target compounds were synthesized by refluxing 4-aminocoumarin with aromatic aldehydes in ethanol. The structural confirmation was achieved by spectroscopic techniques such as (1H, 13C-NMR and FT-IR) and elemental analysis. The synthesized compounds were evaluated for carbonic anhydrase II (CA-II) inhibition and free radical scavenging activity...
February 12, 2018: Drug Research
N Viswanadh, Ganesh S Ghotekar, Mahesh B Thoke, R Velayudham, Aslam C Shaikh, M Karthikeyan, M Muthukrishnan
The chromanone scaffold is considered as a privileged structure in drug discovery. Herein, we report a highly efficient PhI(OAc)2 mediated regioselective, direct C-H hydroxylation of chromanones. This method offers easy access to substituted 6-hydroxy chromanones in moderate to good isolated yields, thus paving the way for their pharmaceutical studies.
February 12, 2018: Chemical Communications: Chem Comm
Heba A Ibrahim, Fadi M Awadallah, Hanan M Refaat, Kamilia M Amin
AIM: Computer-aided drug design techniques were adopted to design three series of 2-substituted-5-nitrobenzimidazole derivatives hybridized with piperzine 5a,b, oxadiazole 7a,b, 9, 14a-c and triazolo-thiadiazole moieties 12a-d, as VEGFR-2/c-Met kinase inhibitors. MATERIALS & METHODS: The designed compounds were synthesized adopting the chemical pathways outlined in schemes 1 and 2 to afford the desired three series followed by evaluating their inhibitory activities against VEGFR-2 and c-Met and in vitro anticancer activities...
February 12, 2018: Future Medicinal Chemistry
Wendy J Lynch, Andrea M Robinson, Jean Abel, Mark A Smith
Purpose of Review: This report provides an update on clinical and preclinical findings for the efficacy of exercise to prevent substance use disorder with a focus on recent evidence for sex differences and neurobiological mechanisms. Recent Findings: Exercise/physical activity is associated with decreased drug use in humans. Preclinical results further indicate that exercise decreases vulnerability to drug use and the development of features of substance use disorder, and suggest that females have an enhanced sensitivity to its reward-substitution effects...
December 2017: Current Addiction Reports
Lin Liu, Hong-Yu Yang, Yan Lou, Jing Miao, Xiao-Yang Lu, Qing-Wei Zhao, Rong-Rong Wang, Sai-Ping Jiang, Xing-Guo Zhang
Background and purpose: Off-label prescriptions for critically ill patients pose several ethical and legal dilemmas for intensive care unit (ICU) clinicians. Yet, few data are available on the prevalence of this practice in critical care environment in China. This nationwide survey was performed to evaluate the conditions of off-label prescriptions in ICU within China. Methods: The survey was performed at the scene of the national ICU conferences in 2016. ICU clinicians attending the congress from 23 provinces across the country were invited...
2018: Therapeutics and Clinical Risk Management
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