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Mefloquine

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https://www.readbyqxmd.com/read/28333192/susceptibilities-of-mdr-mycobacterium-tuberculosis-isolates-to-unconventional-drugs-compared-with-their-reported-pharmacokinetic-pharmacodynamic-parameters
#1
Joseph S Cavanaugh, Ruwen Jou, Mei-Hua Wu, Tracy Dalton, Ekaterina Kurbatova, Julia Ershova, J Peter Cegielski
Background: The second-line drugs recommended to treat drug-resistant TB are toxic, expensive and difficult to procure. Given increasing resistance, the need for additional anti-TB drugs has become more urgent. But new drugs take time to develop and are expensive. Some commercially available drugs have reported anti-mycobacterial activity but are not routinely used because supporting laboratory and clinical evidence is sparse. Methods: We analysed 217 MDR M. tuberculosis isolates including 153 initial isolates from unique patients and 64 isolates from follow-up specimens during the course of treatment...
February 20, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28332319/piperazine-linked-4-aminoquinoline-chalcone-ferrocenyl-chalcone-conjugates-synthesis-and-anti-plasmodial-evaluation
#2
Amandeep Singh, Anu Rani, Jiri Gut, Philip J Rosenthal, Vipan Kumar
A series of piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates were prepared with a view to evaluate their activities against Plasmodium falciparum. The synthesized conjugates had in vitro IC50 values from 0.41-2.38 μM against chloroquine-resistant and mefloquine sensitive W2 strain of P. falciparum. The sub-micromolar activities of most of the synthesized conjugates suggest that such molecular frameworks can act as therapeutic templates for the design and synthesis of new antimalarials...
March 23, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28322482/progressive-multifocal-leukoencephalopathy-associated-with-fumaric-acid-esters-treatment-in-psoriasis-patients
#3
Deepak M W Balak, Enes Hajdarbegovic, Wichor M Bramer, Martino H A Neumann, H Bing Thio
BACKGROUND: Fumaric acid esters (FAEs) are a systemic treatment for psoriasis considered to have a favorable long-term safety profile without an increased risk for immunosuppression. However, progressive multifocal leukoencephalopathy (PML), a rare, opportunistic viral infection of the central nervous system, has been linked anecdotally to FAE treatment. OBJECTIVE: to assess clinical features and outcomes of FAE-associated PML cases. METHODS: Systematic literature search in multiple databases up to February, 25(th) 2016 for reports of PML in psoriasis patients treated with FAEs...
March 21, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/28302108/confirmation-of-plasmodium-falciparum-in-vitro-resistance-to-monodesethylamodiaquine-and-chloroquine-in-dakar-senegal-in-2015
#4
Silman Diawara, Marylin Madamet, Mame Bou Kounta, Gora Lo, Khalifa Ababacar Wade, Aminata Nakoulima, Raymond Bercion, Rémy Amalvict, Mamadou Wague Gueye, Bécaye Fall, Bakary Diatta, Bruno Pradines
BACKGROUND: In response to increasing resistance to anti-malarial drugs, Senegal adopted artemisinin-based combination therapy (ACT) as the first-line treatment for uncomplicated malaria in 2006. However, resistance of Plasmodium falciparum parasites to artemisinin derivatives, characterized by delayed parasite clearance after treatment with ACT or artesunate monotherapy, has recently emerged and rapidly spread in Southeast Asia. After 10 years of stability with rates ranging from 5.6 to 11...
March 16, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28288098/mefloquine-targets-the-plasmodium-falciparum-80s-ribosome-to-inhibit-protein-synthesis
#5
Wilson Wong, Xiao-Chen Bai, Brad E Sleebs, Tony Triglia, Alan Brown, Jennifer K Thompson, Katherine E Jackson, Eric Hanssen, Danushka S Marapana, Israel S Fernandez, Stuart A Ralph, Alan F Cowman, Sjors H W Scheres, Jake Baum
Malaria control is heavily dependent on chemotherapeutic agents for disease prevention and drug treatment. Defining the mechanism of action for licensed drugs, for which no target is characterized, is critical to the development of their second-generation derivatives to improve drug potency towards inhibition of their molecular targets. Mefloquine is a widely used antimalarial without a known mode of action. Here, we demonstrate that mefloquine is a protein synthesis inhibitor. We solved a 3.2 Å cryo-electron microscopy structure of the Plasmodium falciparum 80S ribosome with the (+)-mefloquine enantiomer bound to the ribosome GTPase-associated centre...
March 13, 2017: Nature Microbiology
https://www.readbyqxmd.com/read/28287432/a-biologically-based-computational-approach-to-drug-repurposing-for-anthrax-infection
#6
Jane P F Bai, Theodore Sakellaropoulos, Leonidas G Alexopoulos
Developing drugs to treat the toxic effects of lethal toxin (LT) and edema toxin (ET) produced by B. anthracis is of global interest. We utilized a computational approach to score 474 drugs/compounds for their ability to reverse the toxic effects of anthrax toxins. For each toxin or drug/compound, we constructed an activity network by using its differentially expressed genes, molecular targets, and protein interactions. Gene expression profiles of drugs were obtained from the Connectivity Map and those of anthrax toxins in human alveolar macrophages were obtained from the Gene Expression Omnibus...
March 10, 2017: Toxins
https://www.readbyqxmd.com/read/28261884/modulation-of-antimalarial-activity-at-a-putative-bisquinoline-receptor-in-vivo-using-fluorinated-bisquinolines
#7
Alistar John Fielding, Valentina Lukinovic, Philip Evans, Said Alizadeh, Roger Bisby, Mike Drew, Alessio Del Casino, James Dunn, Laura Randle, Nicola Dempster, Nahar Lutfun, Sarker Satyajit, Fabián G Cantú Reinhard, Sam P de Visser, Mike Dascombe, Fyaz Ismail
Antimalarials can interact with heme covalently, by - interactions or hydrogen bonding. Consequently, the prototropy of 4-aminoquinolines and quinoline methanols was investigated using quantum mechanics. Calculations showed mefloquine protonated preferentially at the piperidine and was impeded at the endocyclic nitrogen due to electronic rather than steric factors. In gas phase calculations, 7-substituted mono- and bis-4-aminoquinolines were preferentially protonated at the endocyclic quinoline nitrogen...
March 6, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28231495/drug-induced-panic-attacks-analysis-of-cases-registered-in-the-french-pharmacovigilance-database
#8
Delphine Abadie, Anaïs Essilini, Virginie Fulda, Aurore Gouraud, Mélissa Yéléhé-Okouma, Joëlle Micallef, François Montastruc, Jean Louis Montastruc
BACKGROUND: The potential role of drugs in the onset of panic attacks (PAs) is poorly understood. AIM: The objective of our study was to characterize drug-induced PAs. METHOD: We performed an analysis of PAs registered in the French pharmacovigilance database between 01/01/1985 and 05/11/2014. RESULTS: Among the 163 recorded cases, 136 (83.4%) were directly related to drugs, mainly antidepressants (11.3%, mainly serotonin reuptake inhibitors), mefloquine (7...
February 9, 2017: Journal of Psychiatric Research
https://www.readbyqxmd.com/read/28223849/review-about-gabapentin-misuse-interactions-contraindications-and-side-effects
#9
REVIEW
Gabriel C Quintero
The current work is targeted to review the risks of gabapentin misuse, its potential interactions with other drugs, side effects and use contraindications. This review consists of a total of 99 biographical references (from the year 1983 to 2016). A publication search of PubMed was performed from January 1983 to December 2016. It included animal studies, clinical studies, case studies and reviews related to gabapentin misuse, potential interactions, side effects and use contraindications. The search terms were gabapentin, anticonvulsant and antiepileptic...
2017: Journal of Experimental Pharmacology
https://www.readbyqxmd.com/read/28199305/sterile-protection-against-human-malaria-by-chemoattenuated-pfspz-vaccine
#10
Benjamin Mordmüller, Güzin Surat, Heimo Lagler, Sumana Chakravarty, Andrew S Ishizuka, Albert Lalremruata, Markus Gmeiner, Joseph J Campo, Meral Esen, Adam J Ruben, Jana Held, Carlos Lamsfus Calle, Juliana B Mengue, Tamirat Gebru, Javier Ibáñez, Mihály Sulyok, Eric R James, Peter F Billingsley, K C Natasha, Anita Manoj, Tooba Murshedkar, Anusha Gunasekera, Abraham G Eappen, Tao Li, Richard E Stafford, Minglin Li, Phil L Felgner, Robert A Seder, Thomas L Richie, B Kim Lee Sim, Stephen L Hoffman, Peter G Kremsner
A highly protective malaria vaccine would greatly facilitate the prevention and elimination of malaria and containment of drug-resistant parasites. A high level (more than 90%) of protection against malaria in humans has previously been achieved only by immunization with radiation-attenuated Plasmodium falciparum (Pf) sporozoites (PfSPZ) inoculated by mosquitoes; by intravenous injection of aseptic, purified, radiation-attenuated, cryopreserved PfSPZ ('PfSPZ Vaccine'); or by infectious PfSPZ inoculated by mosquitoes to volunteers taking chloroquine or mefloquine (chemoprophylaxis with sporozoites)...
February 15, 2017: Nature
https://www.readbyqxmd.com/read/28192434/adverse-effects-of-mefloquine-for-the-treatment-of-uncomplicated-malaria-in-thailand-a-pooled-analysis-of-19-850-individual-patients
#11
Sue J Lee, Feiko O Ter Kuile, Ric N Price, Christine Luxemburger, François Nosten
Mefloquine (MQ) has been used for the treatment of malaria since the mid-1980s, first as monotherapy or as fixed combination with sulfadoxine-pyrimethamine (MSP) and since the mid-1990s in combination with artesunate. There is a renewed interested in MQ as part of a triple therapy for the treatment of multi-drug resistance P. falciparum malaria. The widespread use of MQ beyond south-East Asia has been constrained by reports of poor tolerability. Here we present the side effect profile of MQ for the treatment of uncomplicated malaria on the Thai-Myanmar/Cambodia borders...
2017: PloS One
https://www.readbyqxmd.com/read/28134928/blocking-microglial-pannexin-1-channels-alleviates-morphine-withdrawal-in-rodents
#12
Nicole E Burma, Robert P Bonin, Heather Leduc-Pessah, Corey Baimel, Zoe F Cairncross, Michael Mousseau, Jhenkruthi Vijaya Shankara, Patrick L Stemkowski, Dinara Baimoukhametova, Jaideep S Bains, Michael C Antle, Gerald W Zamponi, Catherine M Cahill, Stephanie L Borgland, Yves De Koninck, Tuan Trang
Opiates are essential for treating pain, but termination of opiate therapy can cause a debilitating withdrawal syndrome in chronic users. To alleviate or avoid the aversive symptoms of withdrawal, many of these individuals continue to use opiates. Withdrawal is therefore a key determinant of opiate use in dependent individuals, yet its underlying mechanisms are poorly understood and effective therapies are lacking. Here, we identify the pannexin-1 (Panx1) channel as a therapeutic target in opiate withdrawal...
March 2017: Nature Medicine
https://www.readbyqxmd.com/read/28080063/optimization-of-2-anilino-4-amino-substituted-quinazolines-into-potent-antimalarial-agents-with-oral-in-vivo-activity
#13
Paul R Gilson, Cyrus Tan, Kate E Jarman, Kym N Lowes, Joan M Curtis, William Nguyen, Adrian E Di Rago, Hayley E Bullen, Boris Prinz, Sandra Duffy, Jonathan B Baell, Craig A Hutton, Helene Jousset Subroux, Brendan S Crabb, Vicky M Avery, Alan F Cowman, Brad E Sleebs
Novel antimalarial therapeutics that target multiple stages of the parasite lifecycle are urgently required to tackle the emerging problem of resistance with current drugs. Here, we describe the optimization of the 2-anilino quinazoline class as antimalarial agents. The class, identified from publicly available antimalarial screening data, was optimized to generate lead compounds that possess potent antimalarial activity against P. falciparum parasites comparable to the known antimalarials, chloroquine and mefloquine...
February 9, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28077744/neuropsychiatric-outcomes-after-mefloquine-exposure-among-u-s-military-service-members
#14
Angelia A Eick-Cost, Zheng Hu, Patricia Rohrbeck, Leslie L Clark
Mefloquine was widely prescribed to U.S. military service members until 2009 when use was limited to personnel with contraindications to doxycycline and no contraindications to mefloquine. The need to estimate the occurrence of neuropsychiatric outcomes (NPOs) in service members prescribed mefloquine warranted a comprehensive evaluation of this issue. Active component service members filling a prescription for mefloquine, doxycycline, or atovaquone/proguanil (A/P) between January 1, 2008 and June 30, 2013, were included in the analysis...
January 11, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28068604/2-8-bis-trifluoromethyl-quinoline-analogs-show-improved-anti-zika-virus-activity-compared-to-mefloquine
#15
COMPARATIVE STUDY
Giselle Barbosa-Lima, Adriana M Moraes, Adriele da S Araújo, Emerson T da Silva, Caroline S de Freitas, Yasmine R Vieira, Andressa Marttorelli, José Cerbino Neto, Patrícia T Bozza, Marcus V N de Souza, Thiago Moreno L Souza
Zika virus (ZIKV), an arthropod-born Flavivirus, has been associated with a wide range of neurological diseases in adults, foetuses and neonates. Since no vaccine is available, repurposing of antiviral drugs currently in medical use is necessary. Mefloquine has confirmed anti-ZIKV activity. We used medicinal chemistry-driven approaches to synthesize and evaluate the ability of a series of new 2,8-bis(trifluoromethyl)quinoline derivatives to inhibit ZIKV replication in vitro, in order to improve the potency of mefloquine...
February 15, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28063022/identification-of-a-syndrome-class-of-neuropsychiatric-adverse-reactions-to-mefloquine-from-latent-class-modeling-of-fda-adverse-event-reporting-system-data
#16
Remington L Nevin, Jeannie-Marie Leoutsakos
INTRODUCTION: Although mefloquine use is known to be associated with a risk of severe neuropsychiatric adverse reactions that are often preceded by prodromal symptoms, specific combinations of neurologic or psychiatric reactions associated with mefloquine use are not well described in the literature. This study sought to identify a distinct neuropsychiatric syndrome class associated with mefloquine use in reports of adverse events. METHODS: Latent class modeling of US Food and Drug Administration Adverse Event Reporting System (FAERS) data was performed using indicators defined by the Medical Dictionary for Regulatory Activities neurologic and psychiatric high-level group terms, in a study dataset of FAERS reports (n = 5332) of reactions to common antimalarial drugs...
March 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28057491/mefloquine-inhibits-voltage-dependent-nav1-4-channel-by-overlapping-the-local-anaesthetic-binding-site
#17
Bertin Paiz-Candia, Angel A Islas, Alfredo Sánchez-Solano, Claudia Mancilla-Simbro, Thomas Scior, Lourdes Millan-PerezPeña, Eduardo M Salinas-Stefanon
Mefloquine constitutes a multitarget antimalaric that inhibits cation currents. However, the effect and the binding site of this compound on Na(+) channels is unknown. To address the mechanism of action of mefloquine, we employed two-electrode voltage clamp recordings on Xenopus laevis oocytes, site-directed mutagenesis of the rat Na(+) channel, and a combined in silico approach using Molecular Dynamics and docking protocols. We found that mefloquine: i) inhibited Nav1.4 currents (IC50 =60μM), ii) significantly delayed fast inactivation but did not affect recovery from inactivation, iii) markedly the shifted steady-state inactivation curve to more hyperpolarized potentials...
January 3, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28044042/influence-of-the-pfmdr1-gene-on-in-vitro-sensitivities-of-piperaquine-in-thai-isolates-of-plasmodium-falciparum
#18
Mathirut Mungthin, Ekularn Watanatanasup, Naruemon Sitthichot, Nantana Suwandittakul, Rommanee Khositnithikul, Stephen A Ward
Piperaquine combined with dihydroartemisinin is one of the artemisinin derivative combination therapies, which can replace artesunate-mefloquine in treating uncomplicated falciparum malaria in Thailand. The aim of this study was to determine the in vitro sensitivity of Thai Plasmodium falciparum isolates against piperaquine and the influence of the pfmdr1 gene on in vitro response. One hundred and thirty-seven standard laboratory and adapted Thai isolates of P. falciparum were accessed for in vitro piperaquine sensitivity...
January 2, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28039388/efficacy-and-safety-of-artesunate-mefloquine-therapy-for-treating-uncomplicated-plasmodium-falciparum-malaria-systematic-review-and-meta-analysis
#19
REVIEW
Henry Maia Peixoto, Paola Barbosa Marchesini, Maria Regina Fernandes de Oliveira
INTRODUCTION: The present study is a systematic review of the literature on the efficacy and safety of the treatment of uncomplicated Plasmodium falciparum infections with artesunate-mefloquine (ASMQ) compared to other artemisinin-based combination therapies (ACTs), designed to assist decision makers in Brazil. METHODS: Twenty-four randomized controlled trials (RCTs) were selected in four electronic databases and in complementary sources. Meta-analyses were performed to evaluate the efficacy expressed by relative risks (RR) obtained from treatment failure confirmed by the PCR...
December 29, 2016: Transactions of the Royal Society of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28035111/comparison-of-who-mark-iii-and-hrp-ii-elisa-for-in-vitro-sensitivity-of-plasmodium-falciparum
#20
Supriya Sharma, Neelima Mishra, Neena Valecha, Anupkumar R Anvikar
BACKGROUND & OBJECTIVES: Antimalarial drug resistance is a serious challenge to malaria control worldwide. In vitro sensitivity assays provide an early indication of emerging drug resistance. In vitro susceptibility of field and culture adapted Plasmodium falciparum isolates to different antimalarials was compared using two Methods: World Health Organization (WHO) micro-test (MARK III) and histidine rich protein II (HRP II) based enzyme- linked immunosorbent assay (ELISA). METHODS: In total, 50 P...
October 2016: Journal of Vector Borne Diseases
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