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https://www.readbyqxmd.com/read/28777172/narcolepsy-and-other-central-hypersomnias
#1
Yves Dauvilliers, Lucie Barateau
PURPOSE OF REVIEW: This article focuses on the clinical presentation, pathophysiology, diagnosis, differential diagnosis, and management of narcolepsy type 1 and narcolepsy type 2, idiopathic hypersomnia, Kleine-Levin syndrome, and other central disorders of hypersomnolence, as defined in the International Classification of Sleep Disorders, Third Edition (ICSD-3). RECENT FINDINGS: In ICSD-3, the names of some central disorders of hypersomnolence have been changed: narcolepsy with cataplexy and narcolepsy without cataplexy have been renamed narcolepsy type 1 and narcolepsy type 2, respectively...
August 2017: Continuum: Lifelong Learning in Neurology
https://www.readbyqxmd.com/read/28490912/update-on-the-treatment-of-narcolepsy-clinical-efficacy-of-pitolisant
#2
REVIEW
Michael W Calik
Narcolepsy is a neurological disease that affects 1 in 2,000 individuals and is characterized by excessive daytime sleepiness (EDS). In 60-70% of individuals with narcolepsy, it is also characterized by cataplexy or a sudden loss of muscle tone that is triggered by positive or negative emotions. Narcolepsy decreases the quality of life of the afflicted individuals. Currently used drugs treat EDS alone (modafinil/armodafinil, methylphenidate, and amphetamine), cataplexy alone ("off-label" use of antidepressants), or both EDS and cataplexy (sodium oxybate)...
2017: Nature and Science of Sleep
https://www.readbyqxmd.com/read/28449891/the-european-medicines-agency-review-of-pitolisant-for-treatment-of-narcolepsy-summary-of-the-scientific-assessment-by-the-committee-for-medicinal-products-for-human-use
#3
Marta Kollb-Sielecka, Pierre Demolis, Joseph Emmerich, Greg Markey, Tomas Salmonson, Manuel Haas
On 31 March 2016, the European Commission issued a decision for a marketing authorisation valid throughout the European Union (EU) for pitolisant (Wakix) for the treatment of narcolepsy with or without cataplexy in adults. Pitolisant is an antagonist/inverse agonist of the human histamine H3 receptor. The dose should be selected using an up-titration scheme depending on individual patient response and tolerance and should not exceed 36 mg/day. The main evidence of efficacy of pitolisant was based on two Phase III clinical trials...
May 2017: Sleep Medicine
https://www.readbyqxmd.com/read/28443381/pharmacological-management-of-narcolepsy-with-and-without-cataplexy
#4
Ulf Kallweit, Claudio L Bassetti
Narcolepsy is an orphan neurological disease and presents with sleep-wake, motoric, neuropsychiatric and metabolic symptoms. Narcolepsy with cataplexy is most commonly caused by an immune-mediated process including genetic and environmental factors, resulting in the selective loss of hypocretin-producing neurons. Narcolepsy has a major impact on workableness and quality of life. Areas covered: This review provides an overview of the temporal available treatment options for narcolepsy (type 1 and 2) in adults, including authorization status by regulatory agencies...
June 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28424564/new-developments-in-the-management-of-narcolepsy
#5
REVIEW
Vivien C Abad, Christian Guilleminault
Narcolepsy is a life-long, underrecognized sleep disorder that affects 0.02%-0.18% of the US and Western European populations. Genetic predisposition is suspected because of narcolepsy's strong association with HLA DQB1*06-02, and genome-wide association studies have identified polymorphisms in T-cell receptor loci. Narcolepsy pathophysiology is linked to loss of signaling by hypocretin-producing neurons; an autoimmune etiology possibly triggered by some environmental agent may precipitate hypocretin neuronal loss...
2017: Nature and Science of Sleep
https://www.readbyqxmd.com/read/28129985/safety-and-efficacy-of-pitolisant-on-cataplexy-in-patients-with-narcolepsy-a-randomised-double-blind-placebo-controlled-trial
#6
RANDOMIZED CONTROLLED TRIAL
Zoltan Szakacs, Yves Dauvilliers, Vladimir Mikhaylov, Irina Poverennova, Sergei Krylov, Slavko Jankovic, Karel Sonka, Philippe Lehert, Isabelle Lecomte, Jeanne-Marie Lecomte, Jean-Charles Schwartz
BACKGROUND: Histaminergic neurons are crucial to maintain wakefulness, but their role in cataplexy is unknown. We assessed the safety and efficacy of pitolisant, a histamine H3 receptor inverse agonist, for treatment of cataplexy in patients with narcolepsy. METHODS: For this randomised, double-blind, placebo-controlled trial we recruited patients with narcolepsy from 16 sleep centres in nine countries (Bulgaria, Czech Republic, Hungary, Macedonia, Poland, Russia, Serbia, Turkey, and Ukraine)...
March 2017: Lancet Neurology
https://www.readbyqxmd.com/read/28129984/wide-implications-of-a-trial-on-pitolisant-for-cataplexy
#7
Christian R Baumann
No abstract text is available yet for this article.
March 2017: Lancet Neurology
https://www.readbyqxmd.com/read/28087755/%C3%A2-pitolisant-for-narcolepsy
#8
(no author information available yet)
▼Pitolisant (Wakix-Bioprojet Pharma) is a new treatment for adults with narcolepsy with or without cataplexy. It was licensed for use in the EU in March last year and has orphan drug status.(1) Here, we consider the evidence for pitolisant for the treatment of narcolepsy in adults and how it fits with current management strategies.
January 2017: Drug and Therapeutics Bulletin
https://www.readbyqxmd.com/read/27902931/human-presynaptic-receptors
#9
REVIEW
Eberhard Schlicker, Thomas Feuerstein
Presynaptic receptors are sites at which transmitters, locally formed mediators or hormones inhibit or facilitate the release of a given transmitter from its axon terminals. The interest in the identification of presynaptic receptors has faded in recent years and it may therefore be justified to give an overview of their occurrence in the autonomic and central nervous system; this review will focus on presynaptic receptors in human tissues. Autoreceptors are presynaptic receptors at which a given transmitter restrains its further release, though in some instances may also increase its release...
November 27, 2016: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/27865546/french-consensus-management-of-patients-with-hypersomnia-which-strategy
#10
R Lopez, I Arnulf, X Drouot, M Lecendreux, Y Dauvilliers
Central hypersomnias principally involves type 1 narcolepsy (NT1), type 2 narcolepsy (NT2) and idiopathic hypersomnia (IH). Despite great progress made in understanding the physiopathology of NT1 with low cerebrospinal fluid hypocretin-1 levels, current treatment remains symptomatic. The same applies to NT2 and IH, for which the physiopathology is still largely unknown. Controlling excessive daytime sleepiness (EDS), cataplexy, hypnagogic hallucinations, sleep paralysis and disturbed night-time sleep are key therapeutic targets in NT1...
November 16, 2016: Revue Neurologique
https://www.readbyqxmd.com/read/27853355/anticonvulsant-effects-of-isomeric-nonimidazole-histamine-h3-receptor-antagonists
#11
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/27787717/role-of-the-histamine-h3-receptor-in-the-central-nervous-system
#12
Eberhard Schlicker, Markus Kathmann
The Gi/o protein-coupled histamine H3 receptor is distributed throughout the central nervous system including areas like cerebral cortex, hippocampus and striatum with the density being highest in the posterior hypothalamus, i.e. the area in which the histaminergic cell bodies are located. In contrast to the other histamine receptor subtypes (H1, H2 and H4), the H3 receptor is located presynaptically and shows a constitutive activity. In detail, H3 receptors are involved in the inhibition of histamine release (presynaptic autoreceptor), impulse flow along the histaminergic neurones (somadendritic autoreceptor) and histamine synthesis...
October 28, 2016: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/27568835/action-of-pitolisant-on-the-stimulant-and-rewarding-effects-of-cocaine-in-mice
#13
Christian Brabant, Yana Charlier, Maria Elisa Serrano Navacerrada, Livia Alleva, Ezio Tirelli
Previous studies have demonstrated that the histamine H3 receptor inverse agonist thioperamide potentiates the stimulant and rewarding effects of cocaine. However, these potentiating effects of thioperamide do not necessarily result from H3 receptor blockade since thioperamide is an imidazole-based compound capable of enhancing plasma cocaine concentrations by blocking cytochrome P450 activity. In contrast, Pitolisant is a non-imidazole H3 receptor inverse agonist that has already been tested in clinical trials but it remains to be determined whether this compound also potentiates the behavioral effects of cocaine...
November 15, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27568232/the-dual-acting-ache-inhibitor-and-h3-receptor-antagonist-uw-md-72-reverses-amnesia-induced-by-scopolamine-or-dizocilpine-in-passive-avoidance-paradigm-in-rats
#14
Bassem Sadek, Nadia Khan, Fouad H Darras, Steffen Pockes, Michael Decker
Both the acetylcholine esterase (AChE) and the histamine H3 receptor (H3R) are involved in the metabolism and modulation of acetylcholine release and numerous other centrally acting neurotransmitters. Hence, dual-active AChE inhibitors (AChEIs) and H3R antagonists hold potential to treat cognitive disorders like Alzheimer's disease (AD). The novel dual-acting AChEI and H3R antagonist 7-(3-(piperidin-1-yl)propoxy)-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one (UW-MD-72) shows excellent selectivity profiles over the AChE's isoenzyme butyrylcholinesterase (BChE) as well as high and balanced in-vitro affinities at both AChE and hH3R with IC50 of 5...
October 15, 2016: Physiology & Behavior
https://www.readbyqxmd.com/read/27549768/management-of-narcolepsy
#15
REVIEW
Lucie Barateau, Régis Lopez, Yves Dauvilliers
Narcolepsy type 1 (NT1) and type 2 (NT2) are two rare neurological diseases, classified as central disorders of hypersomnolence. The pathophysiology of NT1 is well known; it is caused by the selective destruction of hypocretin (Hcrt) neurons, by a highly suspected autoimmune process. On the contrary, little is known about NT2 etiology, sharing with NT1 somnolence and signs of dysregulation of rapid eye movement (REM) sleep, but not cataplexy. Management strategies are rather codified, at least in adults, with a lifelong treatment required in NT1, whereas no pharmacological study focused only on NT2 patients, with sometimes spontaneous improvement or disappearance of their symptoms...
October 2016: Current Treatment Options in Neurology
https://www.readbyqxmd.com/read/27538329/-management-of-central-hypersomnias
#16
Yves Dauvilliers, Régis Lopez
Central hypersomnias include narcolepsy type 1, type 2 and idiopathic hypersomnia with daytime sleepiness excessive in the foreground of the clinical symptoms. Despite major advances in our understanding of the mechanisms of the narcolepsy type 1 with a low level of hypocretin-1 in cerebrospinal fluid, its current management is only symptomatic. The current management is also only symptomatic for type 2 narcolepsy and idiopathic hypersomnia with an unknown pathophysiology. Treatment options may vary from a single drug targeting several symptoms or several drugs treating a specific symptom...
June 2016: La Revue du Praticien
https://www.readbyqxmd.com/read/27438291/pitolisant-first-global-approval
#17
REVIEW
Yahiya Y Syed
Pitolisant (Wakix™) is an inverse agonist of the histamine H3 receptor that is being developed by Bioproject. Oral pitolisant is approved in the EU for the treatment of narcolepsy with or without cataplexy in adults. Pitolisant has received a Temporary Authorization of Use in France for this indication in case of treatment failure, intolerance or contraindication to currently available treatment. Pitolisant has orphan drug designation in the EU and the USA. In the pivotal HARMONY I trial, pitolisant significantly decreased excessive daytime sleepiness versus placebo in adults with narcolepsy with or without cataplexy (primary endpoint)...
September 2016: Drugs
https://www.readbyqxmd.com/read/27363923/histamine-h3-receptor-as-a-potential-target-for-cognitive-symptoms-in-neuropsychiatric-diseases
#18
REVIEW
Bassem Sadek, Ali Saad, Adel Sadeq, Fakhreya Jalal, Holger Stark
The potential contributions of the brain histaminergic system in neurodegenerative diseases, and the possiblity of histamine-targeting treatments is attracting considerable interests. The histamine H3 receptor (H3R) is expressed mainly in the central nervous system, and is, consequently, an attractive pharmacological target. Although recently described clinical trials have been disappointing in attention deficit hyperactivity disorder (ADHD) and schizophrenia (SCH), numerous H3R antagonists, including pitolisant, demonstrate potential in the treatment of narcolepsy, excessive daytime sleepiness associated with cognitive impairment, epilepsy, and Alzheimer's disease (AD)...
October 1, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27303254/multiple-targeting-approaches-on-histamine-h3-receptor-antagonists
#19
REVIEW
Mohammad A Khanfar, Anna Affini, Kiril Lutsenko, Katarina Nikolic, Stefania Butini, Holger Stark
With the very recent market approval of pitolisant (Wakix®), the interest in clinical applications of novel multifunctional histamine H3 receptor antagonists has clearly increased. Since histamine H3 receptor antagonists in clinical development have been tested for a variety of different indications, the combination of pharmacological properties in one molecule for improved pharmacological effects and reduced unwanted side-effects is rationally based on the increasing knowledge on the complex neurotransmitter regulations...
2016: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/27223666/exploratory-phase-ii-trial-to-evaluate-the-safety-and-the-antiepileptic-effect-of-pitolisant-bf2-649-in-refractory-partial-seizures-given-as-adjunctive-treatment-during-3-months
#20
MULTICENTER STUDY
Pierre Collart Dutilleul, Philippe Ryvlin, Philippe Kahane, Laurent Vercueil, Franck Semah, Arnaud Biraben, Jean-Charles Schwartz, Jérôme De Seze, Edouard Hirsch, Nicolas Collongues
BACKGROUND: Pitolisant (BF2.649) is a nonimidazole histamine 3 receptor antagonist. In previous animal studies, it has been shown that pitolisant might be helpful in chronic seizure treatment of both partial and generalized epilepsies. The present study is a multicenter, national, pragmatic, noncomparative, open-label, exploratory phase II trial. It is the first reported study of the clinical effects of pitolisant in human epilepsy. OBJECTIVE: The goal of this trial was to explore the antiepileptic effect of 3 different doses of pitolisant (20, 30, and 40 mg once daily) in patients presenting partial seizure onset despite therapy with adequate dose of 1 to 3 appropriate antiepileptic drugs...
July 2016: Clinical Neuropharmacology
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