Involvement of a Proton ‐Coupled Organic Cation Antiporter in the Blood‐Brain Barrier Transport of Amantadine
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - May 3, 2016 Category: Drugs & Pharmacology Authors: Toyofumi Suzuki, Takahiko Aoyama, Naoto Suzuki, Masaru Kobayashi, Toshiro Fukami, Yoshiaki Matsumoto, Kazuo Tomono Tags: Original Paper Source Type: research

Involvement of a Proton‐Coupled Organic Cation Antiporter in the Blood‐Brain Barrier Transport of Amantadine
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 31, 2016 Category: Drugs & Pharmacology Authors: Toyofumi Suzuki, Takahiko Aoyama, Naoto Suzuki, Masaru Kobayashi, Toshiro Fukami, Yoshiaki Matsumoto, Kazuo Tomono Tags: Original Paper Source Type: research

Intrathecal rimantadine induces motor, proprioceptive, and nociceptive blockades in rats
Publication date: 8 April 2016 Source:Neuroscience Letters, Volume 618 Author(s): Jann-Inn Tzeng, Jieh-Neng Wang, Jhi-Joung Wang, Yu-Wen Chen, Ching-Hsia Hung The purpose of the experiment was to evaluate the local anesthetic effect of rimantadine in spinal anesthesia. Rimantadine in a dose-dependent fashion was constructed after intrathecally injecting the rats with four different doses. The potency and duration of rimantadine were compared with that of the local anesthetic lidocaine at producing spinal motor, nociceptive, and proprioceptive blockades. We demonstrated that intrathecal rimantadine dose-depend...
Source: Neuroscience Letters - March 10, 2016 Category: Neuroscience Source Type: research

Intravirion cohesion of matrix protein M1 with ribonucleocapsid is a prerequisite of influenza virus infectivity.
Abstract Influenza virus has two major structural modules, an external lipid envelope and an internal ribonucleocapsid containing the genomic RNA in the form of the ribonucleoprotein (RNP) complex, both of which are interlinked by the matrix protein M1. Here we studied M1-RNP cohesion within virus exposed to acidic pH in vitro. The effect of acidification was dependent on the cleavage of the surface glycoprotein HA. Acidic pH caused a loss of intravirion RNP-M1 cohesion and activated RNP polymerase activity in virus with cleaved HA (HA1/2) but not in the uncleaved (HA0) virus. The in vitro acidified HA1/2 ...
Source: Virology - March 4, 2016 Category: Virology Authors: Zhirnov OP, Manykin AA, Rossman JS, Klenk HD Tags: Virology Source Type: research

Meeting report: 4th ISIRV antiviral group conference: Novel antiviral therapies for influenza and other respiratory viruses
Publication date: May 2016 Source:Antiviral Research, Volume 129 Author(s): Jennifer L. McKimm-Breschkin, Alicia M. Fry The International Society for Influenza and other Respiratory Virus Diseases (isirv) held its 4th Antiviral Group Conference at the University of Texas on 2–4 June, 2015. With emerging resistance to the drugs currently licensed for treatment and prophylaxis of influenza viruses, primarily the neuraminidase inhibitor oseltamivir phosphate (Tamiflu) and the M2 inhibitors amantadine and rimantadine, and the lack of effective interventions against other respiratory viruses, the 3-day programme focus...
Source: Antiviral Therapy - February 23, 2016 Category: Virology Source Type: research

Meeting report: 4th ISIRVAntiviral Group Conference: Novel Antiviral Therapies for Influenza and Other Respiratory Viruses
Publication date: Available online 9 February 2016 Source:Antiviral Research Author(s): Jennifer L. McKimm-Breschkin, Alicia Fry The International Society for Influenza and other Respiratory Virus Diseases (isirv) held its 4th Antiviral Group Conference at the University of Texas on 2-4 June, 2015. With emerging resistance to the drugs currently licensed for treatment and prophylaxis of influenza viruses, primarily the neuraminidase inhibitor oseltamivir phosphate (Tamiflu) and the M2 inhibitors amantadine and rimantadine, and the lack of effective interventions against other respiratory viruses, the 3-day programm...
Source: Antiviral Therapy - February 10, 2016 Category: Virology Source Type: research

Meeting report: 4(th) ISIRVAntiviral Group Conference: Novel Antiviral Therapies for Influenza and Other Respiratory Viruses.
Abstract The International Society for Influenza and other Respiratory Virus Diseases (isirv) held its 4(th) Antiviral Group Conference at the University of Texas on 2-4 June, 2015. With emerging resistance to the drugs currently licensed for treatment and prophylaxis of influenza viruses, primarily the neuraminidase inhibitor oseltamivir phosphate (Tamiflu) and the M2 inhibitors amantadine and rimantadine, and the lack of effective interventions against other respiratory viruses, the 3-day programme focused on the discovery and development of inhibitors of several virus targets and key host cell factors i...
Source: Antiviral Research - February 9, 2016 Category: Virology Authors: McKimm-Breschkin JL, Fry A Tags: Antiviral Res Source Type: research

Differential Binding of Rimantadine Enantiomers to Influenza A M2 Proton Channel
Journal of the American Chemical SocietyDOI: 10.1021/jacs.5b13129 (Source: Journal of the American Chemical Society)
Source: Journal of the American Chemical Society - January 28, 2016 Category: Chemistry Authors: Anna K. Wright, Paratchata Batsomboon, Jian Dai, Ivan Hung, Huan-Xiang Zhou, Gregory B. Dudley and Timothy A. Cross Source Type: research

Amantadine resistance among highly pathogenic avian influenza viruses (H5N1) isolated from India
Publication date: Available online 27 November 2015 Source:Microbial Pathogenesis Author(s): Aron Jacob, Richa Sood, Kh.Victoria Chanu, Sandeep Bhatia, Rekha Khandia, A.K. Pateriya, S. Nagarajan, U. Dimri, D.D. Kulkarni Emergence of antiviral resistance among H5N1 avian influenza viruses is the major challenge in the control of pandemic influenza. Matrix 2 (M2) inhibitors (amantadine and rimantadine) and neuraminidase inhibitors (oseltamivir and zanamivir) are the two classes of antiviral agents that are specifically active against influenza viruses and are used for both treatment and prophylaxis of i...
Source: Microbial Pathogenesis - November 27, 2015 Category: Infectious Diseases Source Type: research

Influenza Antiviral Expenditures and Outpatient Prescriptions in the United States, 2003–2012
ConclusionInfluenza antivirals totaled $3.74 billion in the United States from 2003 to 2012, with the majority in 2009 and from community pharmacies. Influenza antivirals constituted a small proportion of total medication expenditures, but unforeseen pandemics resulted in unusually high use and expenditures. Influenza antiviral prescriptions dispensed from community pharmacies were associated with ILI and drug expenditures. (Source: Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy)
Source: Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy - November 23, 2015 Category: Drugs & Pharmacology Authors: Katie J. Suda, Robert J. Hunkler, Linda M. Matusiak, Glen T. Schumock Tags: Original Research Article Source Type: research

Investigation of the free energy profiles of amantadine and rimantadine in the AM2 binding pocket.
Abstract The purpose of this work was to study the mechanism of drug resistance of M2 channel proteins by analyzing the interactions between the drugs amantadine and rimantadine and M2 channel proteins (including the wild type and the three mutants V27A, S31N, and G34A) and the drug binding pathways, by use of a computational approach. Our results showed that multiple drug-binding sites were present in the M2 channel, and the trajectory of the drugs through the M2 channel was determined. A novel method was developed to investigate of free energy profiles of the ligand-protein complexes. Our work provides a...
Source: European Biophysics Journal : EBJ - September 21, 2015 Category: Physics Authors: Van Nguyen H, Nguyen HT, Le LT Tags: Eur Biophys J Source Type: research

Viruses, Vol. 7, Pages 4929-4944: Clinical Implications of Antiviral Resistance in Influenza
Influenza is a major cause of severe respiratory infections leading to excessive hospitalizations and deaths globally; annual epidemics, pandemics, and sporadic/endemic avian virus infections occur as a result of rapid, continuous evolution of influenza viruses. Emergence of antiviral resistance is of great clinical and public health concern. Currently available antiviral treatments include four neuraminidase inhibitors (oseltamivir, zanamivir, peramivir, laninamivir), M2-inibitors (amantadine, rimantadine), and a polymerase inhibitor (favipiravir). In this review, we focus on resistance issues related to the use of neuram...
Source: Viruses - September 14, 2015 Category: Virology Authors: Timothy LiMartin ChanNelson Lee Tags: Review Source Type: research

New small-molecule drug design strategies for fighting resistant influenza A
Publication date: Available online 6 September 2015 Source:Acta Pharmaceutica Sinica B Author(s): Zuyuan Shen, Kaiyan Lou, Wei Wang Influenza A virus is the major cause of seasonal or pandemic flu worldwide. Two main treatment strategies–vaccination and small molecule anti-influenza drugs are currently available. As an effective vaccine usually takes at least 6 months to develop, anti-influenza small molecule drugs are more effective for the first line of protection against the virus during an epidemic outbreak, especially in the early stage. Two major classes of anti-influenza drugs currently available are adm...
Source: Acta Pharmaceutica Sinica B - September 7, 2015 Category: Cancer & Oncology Source Type: research

Broad range of inhibiting action of novel camphor-based compound with anti-hemagglutinin activity against influenza viruses in vitro and in vivo
Publication date: Available online 10 June 2015 Source:Antiviral Research Author(s): V.V. Zarubaev , A.V. Garshinina , T.S. Tretiak , V.A. Fedorova , A.A. Shtro , A.S. Sokolova , O.I. Yarovaya , N.F. Salakhutdinov Influenza virus continues to remain one of the leading human respiratory pathogens causing significant morbidity and mortality around the globe. Due to short-term life cycle and high rate of mutations influenza virus is able to rapidly develop resistance to clinically available antivirals. This makes necessary the search and development of new drugs with different targets and mechanisms of activity. H...
Source: Antiviral Therapy - June 12, 2015 Category: Virology Source Type: research