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Adamantane

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121. Peramivir (Rapivab)

in previously healthy adults. Zanamivir and oseltamivir are active against both influenza A and B viruses, but differ in pharmacokinetics, safety profiles, route of administration, approved age groups, and recommended dosages. Zanamivir is administered through oral inhalation by using a plastic device included in the medication package. Oseltamivir is available for oral administration in 30 mg, 45 mg, and 75 mg capsules and liquid suspension. The adamantanes are the other class of approved influenza (...) antiviral agents and include amantadine and rimantadine. Adamantanes are thought to interact with the viral M2 ion channel protein. When administered within 48 hours of illness onset, amantadine and rimantadine can reduce the severity and shorten the duration of acute uncomplicated influenza A illness among healthy adults; however, they have no activity against influenza B virus. In recent years, widespread adamantane resistance among influenza A virus strains (H3N2, H1N1pdm09) has made this class

2014 FDA - Drug Approval Package

122. Ebilfumin - oseltamivir

. The most effective way to prevent the disease or severe outcomes from the illness is vaccination. In addition, antiviral drugs for treatment and prevention of influenza are available. There are two classes of such medicines, 1) adamantanes (amantadine and remantadine), and 2) inhibitors of influenza neuraminidase (oseltamivir and zanamivir). Ebilfumin (oseltamivir), a neuraminidase inhibitor, ATC Code: J05AH02, is a generic of the originator product Tamiflu. The active metabolite is a selective

2014 European Medicines Agency - EPARs

123. Grand Rounds: Influenza Pandemic

reported a high proportion of patients placed on ECMO for adequate oxygenation. There were 39 documented cases of pulmonary hemorrhage. Pregnant women merit special commentary—five percent of them died from pandemic H1N1 (as compared to making up 1% of the general population), and the relative risk of hospitalization for a pregnant woman was 4.3 (versus those not pregnant). Initial strains of pandemic H1N1 were susceptible to NA inhibitors like oseltamivir but almost 100% resistant to adamantanes (...) -2011 circulating influenza viruses are susceptible to oseltamivir and zanamivir and resistant to the adamantanes. The ACIP (Advisory Committee on Immunization Practices) antiviral use guidelines recommend early empiric therapy with a neuramindase inhibitor for all patients with suspected/confirmed influenza who are hospitalized or severely ill, and for those with a chronic underlying medical condition as previously detailed which puts them at high risk for complications, no matter what

2010 Clinical Correlations

124. Risk of myocardial infarction in trials with Dipeptidyl Peptidase-4 inhibitors: Is duration of study a real issue?

Diabetology, Careggi Teaching Hospital, Florence, Italy. Electronic address: edoardo.mannucci@unifi.it. eng Letter Meta-Analysis 2015 02 24 Netherlands Int J Cardiol 8200291 0167-5273 0 Dipeptides 0 Dipeptidyl-Peptidase IV Inhibitors 0 Piperidines 56HH86ZVCT Uracil 9GB927LAJW saxagliptin JHC049LO86 alogliptin PJY633525U Adamantane IM Adamantane analogs & derivatives pharmacology Diabetes Mellitus, Type 2 drug therapy Dipeptides pharmacology Dipeptidyl-Peptidase IV Inhibitors pharmacology Humans Incidence

2015 International journal of cardiology

125. Genetic Characterization of H1N1 and H1N2 Influenza A Viruses Circulating in Ontario Pigs in 2012 (PubMed)

of the five Ontario H1N1 viruses had between one and four amino acid (aa) changes within five antigenic sites, while one Ontario H1N2 virus had two aa changes within two antigenic sites. Such aa changes in antigenic sites could have an effect on antibody recognition and ultimately have implications for immunization practices. According to aa sequence analysis of the M2 protein, Ontario H1N1 and H1N2 viruses can be expected to offer resistance to adamantane derivatives, but not to neuraminidase inhibitors.

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2015 PloS one

126. Study in Healthy Volunteers to Evaluate the Efficacy and Safety of CR6261 in an H1N1 Influenza Healthy Human Challenge Model

by 24-48 hours and reducing shedding in relatively healthy adults, as with vaccination, they have had limited effectiveness in high risk groups and those who have severe or complicated influenza infections. In addition, antiviral resistance has become very common in human influenza A viruses, as currently circulating H1N1 and H3N2 strains are resistant to the adamantane M2 channel blockers and many cases of neuraminidase inhibitor resistance have also been reported with strains of both subtypes

2015 Clinical Trials

127. A Novel Ranking System for Identifying Efficacious Anti-Influenza PB2 Inhibitors. (PubMed)

several neuraminidase inhibitors have been developed for the treatment of influenza virus infections, these have shown a limited window for treatment initiation, and resistant variants have been noted in the population. In addition, an older class of antiviral drugs for influenza, the adamantanes, are no longer recommended for treatment due to widespread resistance. There remains a need for new influenza therapeutic agents with improved efficacy as well as an expanded window for the initiation

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2015 Antimicrobial Agents and Chemotherapy

128. Soluble epoxide hydrolase activity regulates inflammatory responses and seizure generation in two mouse models of temporal lobe epilepsy. (PubMed)

, we investigated the involvement of sEH in neuroinflammation, seizure generation and subsequent epileptogenesis using two mouse models of temporal lobe epilepsy. Experimental epileptic seizures were induced by either pilocarpine or electrical amygdala kindling in both wild-type (WT) C57BL/6 mice and sEH knockout (sEH KO) mice. The sEH expression in the hippocampus was detected by immunohistochemistry and Western blot analysis. The effects of the sEH hydrolase inhibitors, 12-(3-adamantan-1-yl

2015 Brain, behavior, and immunity

129. Letter by Muskiet et al Regarding Article, "Heart Failure, Saxagliptin, and Diabetes Mellitus: Observations From the SAVOR-TIMI 53 Randomized Trial". (PubMed)

University Medical Center, Amsterdam, The Netherlands. Tonneijck Lennart L Diabetes Center, Department of Internal Medicine, VU University Medical Center, Amsterdam, The Netherlands. van Raalte Daniël H DH Diabetes Center, Department of Internal Medicine, VU University Medical Center, Amsterdam, The Netherlands. eng Letter Comment United States Circulation 0147763 0009-7322 0 Dipeptides PJY633525U Adamantane AIM IM Circulation. 2014 Oct 28;130(18):1579-88 25189213 Circulation. 2015 Aug 11;132(6):e121-2 (...) 26260506 Adamantane analogs & derivatives Diabetes Mellitus, Type 2 complications drug therapy Dipeptides adverse effects Female Heart Failure chemically induced complications Humans Male 2015 8 12 6 0 2015 8 12 6 0 2015 10 20 6 0 ppublish 26260505 CIRCULATIONAHA.114.013819 10.1161/CIRCULATIONAHA.114.013819

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2015 Circulation Controlled trial quality: uncertain

130. Response to Letter Regarding Article, "Heart Failure, Saxagliptin and Diabetes Mellitus: Observations From the SAVOR-TIMI 53 Randomized Trial". (PubMed)

Circulation 0147763 0009-7322 0 Dipeptides PJY633525U Adamantane AIM IM Circulation. 2014 Oct 28;130(18):1579-88 25189213 Circulation. 2015 Aug 11;132(6):e120 26260505 Adamantane analogs & derivatives Diabetes Mellitus, Type 2 complications drug therapy Dipeptides adverse effects Female Heart Failure chemically induced complications Humans Male 2015 8 12 6 0 2015 8 12 6 0 2015 10 20 6 0 ppublish 26260506 CIRCULATIONAHA.115.015511 10.1161/CIRCULATIONAHA.115.015511

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2015 Circulation Controlled trial quality: uncertain

131. Comment on Udell et al. Saxagliptin and cardiovascular outcomes in patients with type 2 diabetes and moderate or severe renal impairment: observations from the SAVOR-TIMI 53 Trial. Diabetes Care 2015;38:696-705. (PubMed)

:696-705. e88-9 10.2337/dc15-0006 Kalra Sanjay S Bharti Hospital, Karnal, Haryana, India. Gupta Yashdeep Y Department of Medicine, Government Medical College & Hospital, Sector 32, Chandigarh, India yash_deep_gupta@yahoo.co.in. Baruah Manash P MP Excel Hospitals, Guwahati, Assam, India. Gupta Anu A Department of Neurology, Postgraduate Institute of Medical Education & Research, Chandigarh, India. eng Letter Comment United States Diabetes Care 7805975 0149-5992 0 Dipeptides PJY633525U Adamantane IM (...) Diabetes Care. 2015 Apr;38(4):696-705 25552421 Adamantane analogs & derivatives Cardiovascular Diseases epidemiology Diabetes Mellitus, Type 2 drug therapy epidemiology Diabetic Nephropathies drug therapy Dipeptides therapeutic use Female Humans Male Renal Insufficiency drug therapy 2015 5 23 6 0 2015 5 23 6 0 2015 10 3 6 0 ppublish 25998303 38/6/e88 10.2337/dc15-0006

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2015 Diabetes Care Controlled trial quality: uncertain

132. Diabetes Medications and Heart Failure: Recognizing the Risk. (PubMed)

-7322 0 Dipeptides 9GB927LAJW saxagliptin PJY633525U Adamantane AIM IM Circulation. 2014 Oct 28;130(18):1579-88 25189213 Adamantane adverse effects analogs & derivatives Diabetes Mellitus, Type 2 complications drug therapy Dipeptides adverse effects Female Heart Failure chemically induced complications Humans Male Editorials diabetes mellitus heart failure hospitalization treatment outcome 2014 9 6 6 0 2014 9 6 6 0 2014 12 30 6 0 ppublish 25189212 CIRCULATIONAHA.114.012883 10.1161/CIRCULATIONAHA

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2014 Circulation

133. Full-Genome Analysis of Avian Influenza A(H5N1) Virus from a Human, North America, 2013. (PubMed)

Full-Genome Analysis of Avian Influenza A(H5N1) Virus from a Human, North America, 2013. Full-genome analysis was conducted on the first isolate of a highly pathogenic avian influenza A(H5N1) virus from a human in North America. The virus has a hemagglutinin gene of clade 2.3.2.1c and is a reassortant with an H9N2 subtype lineage polymerase basic 2 gene. No mutations conferring resistance to adamantanes or neuraminidase inhibitors were found.

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2014 Emerging Infectious Diseases

134. Synthetically Modified l-Histidine-Rich Peptidomimetics Exhibit Potent Activity Against Cryptococcus neoformans (PubMed)

Synthetically Modified l-Histidine-Rich Peptidomimetics Exhibit Potent Activity Against Cryptococcus neoformans We describe the synthesis and antimicrobial evaluation of structurally new peptidomimetics, rich in synthetically modified L-histidine. Two series of tripeptidomimetics were synthesized by varying lipophilicity at the C-2 position of L-histidine and at the N- and C-terminus. The data indicates that peptides (5f, 6f, 9f and 10f) possessing highly lipophilic adamantan-1-yl group

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2014 Bioorganic & medicinal chemistry letters

135. Increases in Levels of Epoxyeicosatrienoic and Dihydroxyeicosatrienoic Acids (EETs and DHETs) in Liver and Heart in Vivo by 2,3,7,8-Tetrachlorodibenzo-p-Dioxin (TCDD) and in Hepatic EET:DHET Ratios by Cotreatment with TCDD and the Soluble Epoxide Hydrolas (PubMed)

heart lacks arachidonic acid-metabolizing activity, the latter findings suggest that arachidonic acid metabolites may travel from their site of production to a distal organ, i.e., heart. To determine if the TCDD-arachidonic acid-metabolite profile could be altered pharmacologically, chick embryos were treated with TCDD and the soluble epoxide hydrolase inhibitor 12-(3-adamantan-1-yl-ureido)-dodecanoic acid (AUDA). Cotreatment with AUDA increased hepatic EET-to-DHET ratios, indicating

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2014 Drug Metabolism and Disposition

136. Ordered, adherent layers of nanofibers enabled by supramolecular interactions (PubMed)

Ordered, adherent layers of nanofibers enabled by supramolecular interactions Aligned nanofibrous substrates can be created by electrospinning, but methods for creating multilamellar structures of aligned fibers are limited. Here, apposed nanofibrous scaffolds with pendant β-cyclodextrin (CD) were adhered together by adamantane (Ad) modified hyaluronic acid, exploiting the guest-host interactions of CD and Ad for macroscopic assembly. Stable user-defined multi-layered scaffolds were formed

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2014 Journal of materials chemistry. B, Materials for biology and medicine

137. Easily Accessible Polycyclic Amines that Inhibit the Wild-Type and Amantadine-Resistant Mutants of the M2 Channel of Influenza A Virus (PubMed)

Easily Accessible Polycyclic Amines that Inhibit the Wild-Type and Amantadine-Resistant Mutants of the M2 Channel of Influenza A Virus Amantadine inhibits the M2 proton channel of influenza A virus, yet most of the currently circulating strains of the virus carry mutations in the M2 protein that render the virus amantadine-resistant. While most of the research on novel amantadine analogues has revolved around the synthesis of novel adamantane derivatives, we have recently found that other

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2014 Journal of medicinal chemistry

138. Pharmacological Targeting of the Pseudokinase Her3 (PubMed)

that covalent modification of Her3 inhibits Her3 signaling but not proliferation in some Her3-dependent cancer cell lines. Subsequent derivatization with a hydrophobic adamantane moiety demonstrates that the resultant bivalent ligand (TX2-121-1) enhances inhibition of Her3-dependent signaling. Treatment of cells with TX2-121-1 results in partial degradation of Her3 and serendipitously interferes with productive heterodimerization between Her3 with either Her2 or c-Met. These results suggest that small

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2014 Nature chemical biology

139. [The SAVOR-TIMI 53 study]. (PubMed)

[The SAVOR-TIMI 53 study]. 25072417 2014 10 10 2014 07 30 1827-6806 15 6 2014 Jun Giornale italiano di cardiologia (2006) G Ital Cardiol (Rome) [The SAVOR-TIMI 53 study]. 335-9 10.1714/1582.17270 Di Lenarda Andrea A Candido Riccardo R Cioffi Giovanni G Bossi Antonio C AC ita Journal Article Randomized Controlled Trial Lo studio SAVOR-TIMI 53. Italy G Ital Cardiol (Rome) 101263411 1827-6806 0 Dipeptides 0 Hypoglycemic Agents 9GB927LAJW saxagliptin PJY633525U Adamantane IM Adamantane analogs

2014 Giornale italiano di cardiologia (2006) Controlled trial quality: uncertain

140. Memantine ratiopharm

6.1 of the SmPC. The product is available in Alu/Alu blisters or HDPE bottles as described in section 6.5 of the SmPC. 2.2.2. Active substance The active substance memantine (as hydrochloride) or 1-Amino-3,5-dimethyl tricycle (3,3,1,1 3,7 ) decane hydrochloride, 3,5-Dimethyl-1-adamantamine HCl, 1-Amino-3,5-dimethyl adamantane HCl is a white, crystalline powder, soluble in water and methanol, practically insoluble in acetone. It is a non-hygroscopic substance. Memantine contains two stereocenters

2013 European Medicines Agency - EPARs

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