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https://www.readbyqxmd.com/read/27855360/benzyloxynitrostyrene-analogues-a-novel-class-of-selective-and-highly-potent-inhibitors-of-monoamine-oxidase-b
#1
Mietha M Van der Walt, Gisella Terre'Blanche, Jacobus P Petzer, Anél Petzer
This study examines a series of novel 3-benzyloxy-β-nitrostyrene analogues as a novel class of inhibitors of the monoamine oxidase (MAO) enzymes. MAO inhibitors are considered useful for the treatment of depression and Parkinson's disease, and have recently attracted attention as potential therapeutic agents for a range of disorders including Alzheimer's disease, prostate cancer and certain cardiomyopathies. This study shows that the 3-benzyloxy-β-nitrostyrene analogues are potent inhibitors of the MAO-B isoform with IC50 values in the nanomolar range (39-565 nM)...
November 9, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27853355/anticonvulsant-effects-of-isomeric-nonimidazole-histamine-h3-receptor-antagonists
#2
Bassem Sadek, Ali Saad, Johannes Stephan Schwed, Lilia Weizel, Miriam Walter, Holger Stark
Phenytoin (PHT), valproic acid, and modern antiepileptic drugs (AEDs), eg, remacemide, loreclezole, and safinamide, are only effective within a maximum of 70%-80% of epileptic patients, and in many cases the clinical use of AEDs is restricted by their side effects. Therefore, a continuous need remains to discover innovative chemical entities for the development of active and safer AEDs. Ligands targeting central histamine H3 receptors (H3Rs) for epilepsy might be a promising therapeutic approach. To determine the potential of H3Rs ligands as new AEDs, we recently reported that no anticonvulsant effects were observed for the (S)-2-(4-(3-(piperidin-1-yl)propoxy)benzylamino)propanamide (1)...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27803666/inhibitors-of-mao-a-and-mao-b-in-psychiatry-and-neurology
#3
REVIEW
John P M Finberg, Jose M Rabey
Inhibitors of MAO-A and MAO-B are in clinical use for the treatment of psychiatric and neurological disorders respectively. Elucidation of the molecular structure of the active sites of the enzymes has enabled a precise determination of the way in which substrates and inhibitor molecules are metabolized, or inhibit metabolism of substrates, respectively. Despite the knowledge of the strong antidepressant efficacy of irreversible MAO inhibitors, their clinical use has been limited by their side effect of potentiation of the cardiovascular effects of dietary amines ("cheese effect")...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27802242/effects-of-safinamide-on-pain-in-fluctuating-parkinson-s-disease-patients-a-post-hoc-analysis
#4
Carlo Cattaneo, Paolo Barone, Erminio Bonizzoni, Marco Sardina
BACKGROUND: Pain, a frequent non-motor symptom in Parkinson's Disease (PD), significantly impacts on quality of life. Safinamide is a new drug with dopaminergic and non-dopaminergic properties, approved in Europe as adjunct therapy to levodopa for the treatment of fluctuating PD patients. Results from two 24-month, double-blind, placebo-controlled studies demonstrated that safinamide has positive effects on both motor functions and quality of life in PD patients. OBJECTIVE: To investigate the effects of safinamide on pain management in PD patients with motor fluctuations using pooled data from studies 016 and SETTLE...
October 11, 2016: Journal of Parkinson's Disease
https://www.readbyqxmd.com/read/27713822/population-pharmacokinetic-and-pharmacodynamic-analyses-of-safinamide-in-subjects-with-parkinson-s-disease
#5
Luca Loprete, Chiara Leuratti, Carlo Cattaneo, Mita M Thapar, Colm Farrell, Marco Sardina
Safinamide is an orally administered α-aminoamide derivative with both dopaminergic and non-dopaminergic properties. Nonlinear mixed effects models for population pharmacokinetic (PK) and pharmacokinetic-pharmacodynamic (PKPD) analyses were developed using records from, respectively, 623 and 668 patients belonging to two Phase 3, randomized, placebo-controlled, double-blind efficacy studies. The aim was to estimate safinamide population PK parameters in patients with Parkinson's disease (PD) on stable levodopa therapy, and to develop a model of safinamide effect on the PD phase of normal functioning (ON-time)...
October 2016: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/27665574/clinical-pharmacokinetics-and-pharmacodynamics-of-safinamide
#6
Thomas Müller, Paul Foley
The symptoms of Parkinson's disease (PD) reflect disruptions of a number of brain neurotransmitter systems of varying type and degree. Pharmacological agents with multiple neurochemical mechanisms of action are therefore promising candidates for countering these problems and providing comprehensive symptomatic relief for patients. The pharmacological profile of safinamide includes reversible monoamine oxidase B inhibition, blockage of voltage-dependent Na(+) channels, modulation of Ca(2+) channels, and inhibition of glutamate release...
September 24, 2016: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/27536120/emerging-approaches-in-parkinson-s-disease-adjunctive-role-of-safinamide
#7
REVIEW
Thomas Müller
Ongoing neuronal death in Parkinson's disease (PD) causes an altered neurotransmission of various biogenic amines, particularly dopamine. As these changes do not follow a distinct pattern, they vary individually, and are differently pronounced. As a result, a heterogeneous onset of motor and nonmotor features occurs in each patient with PD during the whole course of the disease. PD actually describes a set of distinct diseases that manifest themselves in clinical syndromes with certain similarities but also great differences...
2016: Therapeutics and Clinical Risk Management
https://www.readbyqxmd.com/read/26917951/adjuvant-therapies-for-parkinson-s-disease-critical-evaluation-of-safinamide
#8
REVIEW
Fabrizio Stocchi, Margherita Torti
Safinamide (SAF) is a new drug developed for the treatment of Parkinson's disease (PD). It is a benzylamino derivative with multiple mechanisms of action and antiparkinsonian, anticonvulsant, and neuroprotective properties. SAF inhibits monoamine oxidase B and dopamine reuptake and glutamate release, blocks voltage-dependent sodium channels, and modulates calcium channels. Although the antiparkinsonian effect can be ascribed in part to the inhibition of the monoamine oxidase B, which is complete at 50 mg, the enhanced benefit seen at the 100 mg dose is probably due to nondopaminergic mechanisms...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/26889632/safinamide-as-add-on-therapy-to-levodopa-in-mid-to-late-stage-parkinson-s-disease-fluctuating-patients-post-hoc-analyses-of-studies-016-and-settle
#9
Carlo Cattaneo, Marco Sardina, Ermino Bonizzoni
BACKGROUND: Studies 016 and SETTLE showed that safinamide was safe and effective as adjunct therapy in patients with advanced Parkinson's disease (PD) and motor fluctuations. The addition of safinamide to a stable dose of levodopa alone or with other antiparkinsonian medications significantly increased ON time with no/non-troublesome dyskinesia, decreased OFF time and improved Parkinson's symptoms. OBJECTIVE: To evaluate the clinical effects of safinamide 100 mg/day on motor fluctuations and cardinal Parkinson's symptoms in specific patient subgroups using pooled data from Studies 016 and SETTLE...
2016: Journal of Parkinson's Disease
https://www.readbyqxmd.com/read/26849427/the-safety-and-efficacy-of-safinamide-mesylate-for-the-treatment-of-parkinson-s-disease
#10
Santiago Perez-Lloret, Olivier Rascol
Safinamide (brand name Xadago®, Zambon S.p.A) is a third-generation reversible MAO-B inhibitor, which also blocks sodium voltage-sensitive channels and modulates stimulated release of glutamate. Safinamide was recently licensed by EMA for the treatment of PD as add-on therapy to a stable dose of levodopa alone or in combination with other PD medicinal products in mid-to advanced-stage fluctuating patients. It is also under review by the US FDA. Studies in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated monkeys and 6OHDA-lesioned rats suggest antiparkinsonian efficacy and antidyskinesic effects...
2016: Expert Review of Neurotherapeutics
https://www.readbyqxmd.com/read/26825389/mitochondrial-permeability-transition-pore-a-promising-target-for-the-treatment-of-parkinson-s-disease
#11
Md Zeeshan Rasheed, Heena Tabassum, Suhel Parvez
Among the neurodegenerative diseases (ND), Parkinson's disease affects 6.3 million people worldwide characterized by the progressive loss of dopaminergic neurons in substantia nigra. The mitochondrial permeability transition pore (mtPTP) is a non-selective voltage-dependent mitochondrial channel whose opening modifies the permeability properties of the mitochondrial inner membrane. It is recognized as a potent pharmacological target for diseases associated with mitochondrial dysfunction and excessive cell death including ND such as Parkinson's disease (PD)...
January 29, 2016: Protoplasma
https://www.readbyqxmd.com/read/26744740/safinamide-for-symptoms-of-parkinson-s-disease
#12
REVIEW
T Müller
Chronic and slow progression of neuronal death in Parkinson's disease is responsible for an altered neurotransmission of various biogenic amines, such as dopamine. Therefore, an individually different pronounced heterogeneity of motor and nonmotor symptoms characterizes each Parkinson's disease patient. Ideal candidates for the balance of these neurotransmitter deficits are compounds like safinamide with broad mechanisms of action such as reversible monoamine oxidase type B inhibition, blockage of voltage-dependent sodium channels, modulation of calcium channels and of glutamate release...
November 2015: Drugs of Today
https://www.readbyqxmd.com/read/26587996/clinical-pharmacology-review-of-safinamide-for-the-treatment-of-parkinson-s-disease
#13
REVIEW
Margherita Fabbri, Mario M Rosa, Daisy Abreu, Joaquim J Ferreira
Safinamide (Xadago™) is an oral α-aminoamide derivative marketed for the treatment of Parkinson's disease (PD). The drug has both dopaminergic properties, namely highly selective and reversible inhibition of monoamine oxidase B, and nondopamimetic properties, namely selective sodium channel blockade and calcium channel modulation, with consequent inhibition of excessive glutamate release. In 2014, safinamide was approved in the European Economic Area, as "an add-on therapy to stable dose levodopa, alone or in combination with other PD therapies in mid- to late-stage-fluctuating PD patients...
December 2015: Neurodegenerative Disease Management
https://www.readbyqxmd.com/read/26406127/long-term-effects-of-safinamide-on-dyskinesia-in-mid-to-late-stage-parkinson-s-disease-a-post-hoc-analysis
#14
MULTICENTER STUDY
Carlo Cattaneo, R La Ferla, Erminio Bonizzoni, Marco Sardina
BACKGROUND: Safinamide is a novel α-aminoamide with dopaminergic and non-dopaminergic properties developed as adjunctive therapy for patients with PD. Results from a 24-month double-blind controlled study suggested that as add-on to levodopa (and other PD medications) the benefits of safinamide on dyskinesia may be related to severity of dyskinesia at baseline. OBJECTIVE: This post-hoc analysis further characterized the effects of safinamide on dyskinesia in mid- to late-stage PD patients...
2015: Journal of Parkinson's Disease
https://www.readbyqxmd.com/read/26300398/neuroprotection-by-safinamide-in-the-6-hydroxydopamine-model-of-parkinson-s-disease
#15
Mona Sadeghian, Gizem Mullali, Jennifer M Pocock, Thomas Piers, Arthur Roach, Kenneth J Smith
AIMS: Current therapies in Parkinson's disease mainly treat symptoms rather than provide effective neuroprotection. We examined the effects of safinamide (monoamine oxidase B and sodium channel blocker) on microglial activation and the degeneration of dopaminergic neurons in a rat model of PD in vivo, and on microglia in vitro. METHODS: Rats received unilateral stereotaxic injection of 6-hydroxydopamine into the medial forebrain bundle on day 0: The contralateral side served as control...
August 2016: Neuropathology and Applied Neurobiology
https://www.readbyqxmd.com/read/26293004/new-treatments-for-levodopa-induced-motor-complications
#16
REVIEW
Olivier Rascol, Santiago Perez-Lloret, Joaquim J Ferreira
Levodopa (l-dopa)-induced motor complications, including motor fluctuations and dyskinesia, affect almost all patients with Parkinson's disease (PD) at some point during the disease course, with relevant implications in global health status. Various dopaminergic and nondopaminergic pharmacological approaches as well as more invasive strategies including devices and functional surgery are available to manage such complications. In spite of undisputable improvements during the last decades, many patients remain significantly disabled, and a fully satisfying management of l-dopa-induced motor complications is still an important unmet need of PD therapy...
September 15, 2015: Movement Disorders: Official Journal of the Movement Disorder Society
https://www.readbyqxmd.com/read/26164425/defining-the-role-of-the-monoamine-oxidase-b-inhibitors-for-parkinson-s-disease
#17
REVIEW
Daphne Robakis, Stanley Fahn
Inhibitors of monoamine oxidase-B (MAO-B) occupy an important place in the treatment of Parkinson's disease. Selegiline was the first MAO-B to be used therapeutically, while rasagiline is a second-generation drug with higher potency and selectivity. Safinamide is an investigational MAO-B inhibitor with non-dopaminergic properties that may provide advantages over its predecessors. As a class, MAO-B inhibitors are safe and well tolerated and provide symptomatic benefit both as monotherapy and in combination with other antiparkinsonian medications from early to late stages of disease...
June 2015: CNS Drugs
https://www.readbyqxmd.com/read/25968563/impact-of-pharmacotherapy-on-quality-of-life-in-patients-with-parkinson-s-disease
#18
REVIEW
Pablo Martinez-Martin, Carmen Rodriguez-Blazquez, Maria João Forjaz, Monica M Kurtis
Quality of life (QoL) is a patient-reported outcome frequently included in Parkinson's disease (PD) clinical trials as a secondary or tertiary endpoint. However, QoL is an important variable that reflects the impact of disease and treatment from the patients' perspective. In a chronic, neurodegenerative disease such as PD, with a wide range of complex symptoms, QoL provides valuable and comprehensive information on the patients' health status. This narrative review aims to evaluate the effect of specific PD treatments currently in use on patients' QoL measured with the Parkinson's Disease Questionnaire, 39-item (PDQ-39) or 8-item (PDQ-8) version...
May 2015: CNS Drugs
https://www.readbyqxmd.com/read/25851099/safinamide-first-global-approval
#19
REVIEW
Emma D Deeks
Safinamide (Xadago(®)) is an oral α-aminoamide derivative developed by Newron for the treatment of Parkinson's disease (PD). The drug has both dopaminergic properties (highly selective and reversible inhibition of monoamine oxidase-B) and non-dopaminergic properties (selective sodium channel blockade and calcium channel modulation, with consequent inhibition of excessive glutamate release). Safinamide is approved in the EU, Iceland, Lichtenstein and Norway, as an add-on therapy to stable-dose levodopa, alone or in combination with other PD therapies in mid- to late-stage fluctuating PD patients; regulatory submissions have also been filed in the USA and Switzerland for its use in this indication...
April 2015: Drugs
https://www.readbyqxmd.com/read/25711470/1-2-4-benzyloxyphenoxy-ethyl-imidazole-inhibits-monoamine-oxidase-b-and-protects-against-neuronal-loss-and-behavioral-impairment-in-rodent-models-of-parkinson-s-disease
#20
Jin Yong Chung, Ji Won Lee, Choon Ho Ryu, Hye Kyung Min, Yeo Jin Yoon, Mi Jung Lim, Cheol Hyoung Park
Monoamine oxidase B (MAO-B) is well known as a therapeutic target for Parkinson's disease (PD). MAO-B inhibitors retain antiparkinsonism abilities to improve motor function and prevent neuronal loss by decreasing dopamine metabolism and oxidative stress in the brain. From the study to find novel antiparkinsonism drugs that can inhibit MAO-B activity, neuronal loss, and behavioral deficits in the mouse model of PD, we identified that 1-[2-(4-benzyloxyphenoxy)ethyl]imidazole (BPEI) or safinamide strongly and selectively inhibited MAO-B activities in a dose-dependent manner (IC50 of BPEI and safinamide for MAO-B were 0...
August 2015: Journal of Neuroscience Research
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