Current and Experimental Therapeutics of Insomnia
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Drugs Inducing Insomnia As an Adverse Effect
2 Drugs Inducing Insomnia as an Adverse Effect Ntambwe Malangu University of Limpopo, Medunsa Campus, School of Public Health, South Africa 1. Introduction Insomnia is a symptom, not a stand-alone disease. By definition, insomnia is "difficulty initiating or maintaining sleep, or both" or the perception of poor quality sleep (APA, 1994). As an adverse effect of medicines, it has been documented for several drugs. This chapter describes some drugs whose safety profile includes insomnia. In doing so, it discusses the mechanisms through which drug-induced insomnia occurs, the risk factors associated with its occurrence, and ends with some guidance on strategies to prevent and manage drug- induced insomnia. 2. How drugs induce insomnia There are several mechanisms involved in the induction of insomnia by drugs. Some drugs affects sleep negatively when being used, while others affect sleep and lead to insomnia when they are withdrawn. Drugs belonging to the first category include anticonvulsants, some antidepressants, steroids and central nervous stimulant drugs such amphetamine and caffeine. With regard to caffeine, the mechanism by which caffeine is able to promote wakefulness and insomnia has not been fully elucidated (Lieberman, 1992). However, it seems that, at the levels reached during normal consumption, caffeine exerts its action through antagonism of central adenosine receptors; thereby, it reduces physiologic sleepiness and enhances vigilance (Benington et al., 1993; Walsh et al., 1990; Rosenthal et al., 1991; Bonnet and Arand, 1994; Lorist et al., 1994). In contrast to caffeine, methamphetamine and methylphenidate produce wakefulness by increasing dopaminergic and noradrenergic neurotransmission (Gillman and Goodman, 1985). With regard to withdrawal, it may occur in 40% to 100% of patients treated chronically with benzodiazepines, and can persist for days or weeks following discontinuation. -
Mol.116.105981.Full.Pdf
Molecular Pharmacology Fast Forward. Published on September 13, 2016 as DOI: 10.1124/mol.116.105981 This article has not been copyedited and formatted. The final version may differ from this version. MOL #105981 CURRENT KNOWLEDGE AND PERSPECTIVES FOR HISTAMINE H1 AND H2 RECEPTOR PHARMACOLOGY. FUNCTIONAL SELECTIVITY, RECEPTOR CROSSTALK AND REPOSITIONING OF CLASSIC HISTAMINERGIC LIGANDS. Downloaded from Federico Monczor and Natalia Fernandez. Instituto de Investigaciones Farmacológicas, ININFA. Universidad de Buenos Aires—Consejo molpharm.aspetjournals.org Nacional de Investigaciones Científicas y Técnicas, CONICET. Buenos Aires, Argentina. at ASPET Journals on September 28, 2021 1 Molecular Pharmacology Fast Forward. Published on September 13, 2016 as DOI: 10.1124/mol.116.105981 This article has not been copyedited and formatted. The final version may differ from this version. MOL #105981 Running title: Current and perspectives for histamine receptors pharmacology. Corresponding author: Federico Monczor. Laboratorio de Farmacología de Receptores. Instituto de Investigaciones Farmacológicas, ININFA. Universidad de Buenos Aires—Consejo Nacional de Investigaciones Científicas y Técnicas, CONICET. Junin 956 (1113) Buenos Aires, Argentina. Tel:+54-11-5287-4856. e-mail: [email protected]. Total text pages: 41 Downloaded from Tables: 2 Figures: 1 References: 125 molpharm.aspetjournals.org Abstract words: 222 Abbreviations: AML, acute myeloid leukemia; ATP, adenosine triphosphate; GTP, guanosine triphosphate; AC, adenylyl cyclase; IP, inositol -
Sleep Inducing Toothpaste Made with Natural Herbs and a Natural Hormone
Sleep inducing toothpaste made with natural herbs and a natural hormone Abstract A toothpaste composition for inducing sleep while simultaneously promoting intraoral cleanliness, which includes toothpaste base ingredients and at least one sleep- inducing natural herb or hormone. The sleep-inducing natural herbs and hormone are selected from the group consisting of Chamomile, Lemon Balm, Passion Flower, and Valerian, and the hormone Melatonin. The sleep-inducing natural herbs are in a range of 0.25% to 18% by weight of the composition. Description of the Invention FIELD OF THE INVENTION The following natural herbs and natural hormone in combination with toothpaste is used at night to improve sleep. The expected dose of toothpaste is calculated at 2 grams. The ingredients have been assessed for range of daily dose for best effects, toxicity in normal range, recommended proportion of each, and water solubility of key constituents. BACKGROUND OF THE INVENTION It is an object of the present invention to provide a sleep-inducing toothpaste or mouth spray which includes sleep-inducing natural herbs and a natural hormone. It is a further object of the present invention to provide a sleep-inducing toothpaste which includes toothpaste base ingredients and natural herbs being Chamomile, Lemon Balm, Passion Flower, Valerian and the natural hormone Melatonin. SUMMARY OF THE INVENTION A toothpaste composition is provided for inducing sleep while simultaneously promoting intraoral cleanliness, which includes toothpaste base ingredients and at least one sleep-inducing natural herb or hormone. The sleep-inducing natural herbs and hormone are selected from the group consisting of the natural herbs Chamomile, Lemon Balm, Passion Flower, and Valerian, and the natural hormone Melatonin. -
THE USE of MIRTAZAPINE AS a HYPNOTIC O Uso Da Mirtazapina Como Hipnótico Francisca Magalhães Scoralicka, Einstein Francisco Camargosa, Otávio Toledo Nóbregaa
ARTIGO ESPECIAL THE USE OF MIRTAZAPINE AS A HYPNOTIC O uso da mirtazapina como hipnótico Francisca Magalhães Scoralicka, Einstein Francisco Camargosa, Otávio Toledo Nóbregaa Prescription of approved hypnotics for insomnia decreased by more than 50%, whereas of antidepressive agents outstripped that of hypnotics. However, there is little data on their efficacy to treat insomnia, and many of these medications may be associated with known side effects. Antidepressants are associated with various effects on sleep patterns, depending on the intrinsic pharmacological properties of the active agent, such as degree of inhibition of serotonin or noradrenaline reuptake, effects on 5-HT1A and 5-HT2 receptors, action(s) at alpha-adrenoceptors, and/or histamine H1 sites. Mirtazapine is a noradrenergic and specific serotonergic antidepressive agent that acts by antagonizing alpha-2 adrenergic receptors and blocking 5-HT2 and 5-HT3 receptors. It has high affinity for histamine H1 receptors, low affinity for dopaminergic receptors, and lacks anticholinergic activity. In spite of these potential beneficial effects of mirtazapine on sleep, no placebo-controlled randomized clinical trials of ABSTRACT mirtazapine in primary insomniacs have been conducted. Mirtazapine was associated with improvements in sleep on normal sleepers and depressed patients. The most common side effects of mirtazapine, i.e. dry mouth, drowsiness, increased appetite and increased body weight, were mostly mild and transient. Considering its use in elderly people, this paper provides a revision about studies regarding mirtazapine for sleep disorders. KEYWORDS: sleep; antidepressive agents; sleep disorders; treatment� A prescrição de hipnóticos aprovados para insônia diminuiu em mais de 50%, enquanto de antidepressivos ultrapassou a dos primeiros. -
Activation of 5-HT2C (But Not 5-HT1A) Receptors in the Amygdala Enhances Fear-Induced Antinociception: Blockade with Local 5-HT2C Antagonist Or Systemic fluoxetine
Neuropharmacology 135 (2018) 376e385 Contents lists available at ScienceDirect Neuropharmacology journal homepage: www.elsevier.com/locate/neuropharm Activation of 5-HT2C (but not 5-HT1A) receptors in the amygdala enhances fear-induced antinociception: Blockade with local 5-HT2C antagonist or systemic fluoxetine Lígia Renata Rodrigues Tavares a, b, Daniela Baptista-de-Souza a, c, * Azair Canto-de-Souza a, b, c, d, a Psychobiology Group, Department of Psychology/CECH- Federal University of Sao~ Carlos-UFSCar, Sao~ Carlos, Sao~ Paulo, 13565-905, Brazil b Joint Graduate Program in Physiological Sciences UFSCar/UNESP, Sao~ Carlos, Sao~ Paulo, 13565-905, Brazil c Neuroscience and Behavioral Institute-IneC, Ribeirao~ Preto, Sao~ Paulo, 14040-901, Brazil d Program in Psychology UFSCar, Sao~ Carlos, Sao~ Paulo, 13565-905, Brazil article info abstract Article history: It is well-known that the exposure of rodents to threatening environments [e.g., the open arm of the Received 17 August 2017 elevated-plus maze (EPM)] elicits pain inhibition. Systemic and/or intracerebral [e.g., periaqueductal gray Received in revised form matter, amygdala) injections of antiaversive drugs [e.g., serotonin (5-HT) ligands, selective serotonin 5 March 2018 reuptake inhibitors (SSRIs)] have been used to change EPM-open arm confinement induced anti- Accepted 6 March 2018 nociception (OAA). Here, we investigated (i) the role of the 5-HT and 5-HT receptors located in the Available online 13 March 2018 1A 2C amygdaloid complex on OAA as well as (ii) the effects of systemic pretreatment with fluoxetine (an SSRI) on the effects of intra-amygdala injections of 8-OH-DPAT (a 5-HT1A agonist) or MK-212 (a 5-HT2C agonist) Keywords: fi Amygdala on nociception in mice con ned to the open arm or enclosed arm of the EPM. -
Histamine Receptors
Tocris Scientific Review Series Tocri-lu-2945 Histamine Receptors Iwan de Esch and Rob Leurs Introduction Leiden/Amsterdam Center for Drug Research (LACDR), Division Histamine is one of the aminergic neurotransmitters and plays of Medicinal Chemistry, Faculty of Sciences, Vrije Universiteit an important role in the regulation of several (patho)physiological Amsterdam, De Boelelaan 1083, 1081 HV, Amsterdam, The processes. In the mammalian brain histamine is synthesised in Netherlands restricted populations of neurons that are located in the tuberomammillary nucleus of the posterior hypothalamus.1 Dr. Iwan de Esch is an assistant professor and Prof. Rob Leurs is These neurons project diffusely to most cerebral areas and have full professor and head of the Division of Medicinal Chemistry of been implicated in several brain functions (e.g. sleep/ the Leiden/Amsterdam Center of Drug Research (LACDR), VU wakefulness, hormonal secretion, cardiovascular control, University Amsterdam, The Netherlands. Since the seventies, thermoregulation, food intake, and memory formation).2 In histamine receptor research has been one of the traditional peripheral tissues, histamine is stored in mast cells, eosinophils, themes of the division. Molecular understanding of ligand- basophils, enterochromaffin cells and probably also in some receptor interaction is obtained by combining pharmacology specific neurons. Mast cell histamine plays an important role in (signal transduction, proliferation), molecular biology, receptor the pathogenesis of various allergic conditions. After mast cell modelling and the synthesis and identification of new ligands. degranulation, release of histamine leads to various well-known symptoms of allergic conditions in the skin and the airway system. In 1937, Bovet and Staub discovered compounds that antagonise the effect of histamine on these allergic reactions.3 Ever since, there has been intense research devoted towards finding novel ligands with (anti-) histaminergic activity. -
Melatonin Protects Against the Effects of Chronic Stress on Sexual Behaviour in Male Rats
MOTIVATION, EMOTION, FEEDING, DRINKING NEUROREPORT Melatonin protects against the effects of chronic stress on sexual behaviour in male rats Lori A. Brotto, Boris B. GorzalkaCA and Amanda K. LaMarre Department of Psychology, 2136 West Mall, Vancouver, BC, Canada V6T 1Z4 CACorresponding Author Received 9 July 2001; accepted 24 August 2001 The effects of chronic mild stress (CMS) on both sexual but not the effects on either spontaneous WDS or WDS in behaviour and wet dog shakes (WDS), a serotonergic type 2A response to the 5-HT2A agonist 1-(2,5-dimethoxy-4-iodophe- (5-HT2A) receptor-mediated behaviour, were explored in the nyl)-2-aminopropane, suggesting a mechanism of action other male rat. In addition, the possible attenuation of these effects than exclusive 5-HT2A antagonism. These results are the ®rst by chronic treatment with melatonin, a putative 5-HT2A to demonstrate that melatonin signi®cantly protects against the antagonist, was examined. The CMS procedure resulted in a detrimental effects of a chronic stressor on sexual behaviour. signi®cant increase in WDS and an overall decrease in all NeuroReport 12:3465±3469 & 2001 Lippincott Williams & aspects of sexual behaviour. Concurrent melatonin administra- Wilkins. tion attenuated the CMS-induced effects on sexual behaviour, Key words: Chronic mild stress; 5-HT2A receptors; Melatonin; Serotonin; Sexual behaviour INTRODUCTION vioural effect of melatonin is mediated via a reduction in The chronic mild stress (CMS) procedure, in which rats are 5-HT2A receptor activity rather than altered central 5-HT2A repeatedly exposed to a variety of mild stressors, is receptor density [8]. The demonstration that melatonin associated with behavioural and biochemical sequelae that reduces the concentration-dependent 5-HT2A receptor- are commonly associated with anhedonia [1]. -
Insomnia Disorder a VA Clinician’S Guide to Managing Insomnia Disorder (2019) Contents Insomnia Disorder
Insomnia Disorder A VA Clinician’s Guide to Managing Insomnia Disorder (2019) Contents Insomnia Disorder .................................................................................................... 3 Risks in elderly patients and patients with dementia .................................15 Background ................................................................................................................ 3 Provider perceptions vs reality ............................................................................16 Figure 1. Stepped Care for Management of Insomnia Disorder .............. 3 Figure 5. Weighing the potential risks versus benefits of Table 1. Brief summary of the ISI ......................................................................... 4 medication use .........................................................................................................16 Figure 2. Acute Insomnia to Insomnia Disorder ............................................ 5 Doxepin ........................................................................................................................17 Clinical Pearl ............................................................................................................... 5 Figure 6. Doxepin Use .............................................................................................18 Figure 3. Common causes of sleep disturbance ........................................... 6 Ramelteon ...................................................................................................................18 -
Herbal Remedies and Sleep
HERBAL REMEDIES AND SLEEP • Some people use herbal remedies to treat sleep problems. They may choose this in preference to sleeping pills. • There have been studies on some of these herbs. However, not all of them have been conducted properly. For some herbs, there is virtually no evidence to show whether they are effective or not. • The most frequently studied herbs are Valerian, Kava, Hops, Chamomile, and Passionflower. However, there is little convincing evidence to suggest that they work well for improving sleep. • Some herbal remedies have been associated with adverse health effects. Note: All words that are underlined relate to topics in the Sleep Health Foundation Information Library at www.sleephealthfoundation.org.au 1. Why try herbs to help your sold by a specific manufacturer for a certain time-period. Trials testing effectiveness are expensive, and without a patent, companies may not sleep? be able to recover their costs through guaranteed sales, even if the herb has potential. However, there have been studies of some herbs About 40% of people use alternative or complementary medicines at used for insomnia and anxiety. Here we focus on herbs where least occasionally, and 4.5% use them to treat sleep problem. Some reasonable information exists from clinical research trials. people who are concerned about using sleeping pills will turn to herbal remedies to help them sleep (see our page on Sleeping Tablets). Melatonin is not a herbal remedy (for more information see Melatonin). 3. What does the evidence say about herbs helping sleep? 2. Has the effectiveness of herbs In the table below, we look at the effectiveness of eight herbal remedies in treating sleep problems as treatments of insomnia. -
Drug Information Update: Agomelatine Daniel Whiting,1 Philip J
SPECIAL ARTICLES Drug information update: agomelatine Daniel Whiting,1 Philip J. Cowen1 The Psychiatrist (2013), 37, 356-358, doi: 10.1192/pb.bp.113.043505 1University Department of Psychiatry, Summary Agomelatine is a new antidepressant, licensed for the treatment of Warneford Hospital, Oxford unipolar major depression, with a mode of action that combines activation of Correspondence to Philip Cowen melatonin receptors with blockade of 5-HT2C receptors. Agomelatine is notable for its ([email protected]) short duration of action in the body and modest side-effect burden; however, a First received 24 Mar 2013, final number of theoretical and practical challenges have limited its adoption into revision 3 Apr 2013, accepted 4 Apr 2013 mainstream treatment in the UK. Current meta-analyses show marginal clinical benefits of agomelatine relative to placebo and an association with occasional increases in liver transaminases. Theoretically it is not clear whether agomelatine does block brain 5-HT2C receptors in humans at therapeutic doses and the optimum daily timing of administration in depression has not been clearly established. However, agomelatine’s novel mode of action justifies further study, perhaps with the eventual aim of matching its use in depression to patients with specific disturbances in circadian rhythm. Declaration of interest P.J.C. has been a paid member of advisory boards for Eli Lilly, Lundbeck and Servier. The melatonin analogue, agomelatine, is the first anti- timed administration of melatonin has the capacity to shift depressant approved by the European Medicines Agency circadian rhythms, and melatonin is used for this purpose, which is not monoaminergic. -
Corticosterone Regulation of 5-HT2A Receptor-Mediated Behaviors: Attenuation by Melatonin
Physiology & Behavior, Vol. 67, No. 3, pp. 439–442, 1999 © 1999 Elsevier Science Inc. Printed in the USA. All rights reserved 0031-9384/99/$–see front matter PII S0031-9384(99)00096-7 Corticosterone Regulation of 5-HT2A Receptor-Mediated Behaviors: Attenuation by Melatonin BORIS B. GORZALKA,1 LORI A. BROTTO AND JANIE J. HONG Department of Psychology, The University of British Columbia, Vancouver, British Columbia, Canada, V6T 1Z4 Received 15 February 1999; Accepted 26 April 1999 GORZALKA, B. B., L. A. BROTTO AND J. J. HONG. Corticosterone regulation of 5-HT2A receptor-mediated behav- iors: Attenuation by melatonin. PHYSIOL BEHAV 67(3) 439–442, 1999.—The effects of chronic corticosterone treatment on sexual behavior and on wet-dog shakes (WDS), a serotonergic type 2A (5-HT2A) receptor-mediated behavior, were explored in the male rat. In addition, the effects of acute melatonin treatment, both alone and in combination with corticosterone, were investigated. Chronic injections of corticosterone resulted in an overall decrease in consummatory measures of sexual behav- ior, and an increase in WDS. Furthermore, although an acute injection of melatonin alone had no effect on any recorded be- havior, it attenuated the effects of corticosterone on sexual behavior and WDS. The data suggest that in the context of 5-HT2A receptor-mediated behaviors, melatonin has possible implications as a 5-HT2A antagonist. © 1999 Elsevier Science Inc. Melatonin Corticosterone Serotonin 5-HT2A receptor Sexual behavior IN the male rat, serotonergic type 2A (5-HT2A) receptor ac- some regulatory effects on the 5-HT2A receptor. Chronic cor- tivity has been reliably found to modulate an inhibition of sex- ticosterone treatment has been demonstrated to significantly ual behavior (15). -
Insomnia in Adults
New Guideline February 2017 The AASM has published a new clinical practice guideline for the pharmacologic treatment of chronic insomnia in adults. These new recommendations are based on a systematic review of the literature on individual drugs commonly used to treat insomnia, and were developed using the GRADE methodology. The recommendations in this guideline define principles of practice that should meet the needs of most adult patients, when pharmacologic treatment of chronic insomnia is indicated. The clinical practice guideline is an essential update to the clinical guideline document: Sateia MJ, Buysse DJ, Krystal AD, Neubauer DN, Heald JL. Clinical practice guideline for the pharmacologic treatment of chronic insomnia in adults: an American Academy of Sleep Medicine clinical practice guideline. J Clin Sleep Med. 2017;13(2):307–349. SPECIAL ARTICLE Clinical Guideline for the Evaluation and Management of Chronic Insomnia in Adults Sharon Schutte-Rodin, M.D.1; Lauren Broch, Ph.D.2; Daniel Buysse, M.D.3; Cynthia Dorsey, Ph.D.4; Michael Sateia, M.D.5 1Penn Sleep Centers, Philadelphia, PA; 2Good Samaritan Hospital, Suffern, NY; 3UPMC Sleep Medicine Center, Pittsburgh, PA; 4SleepHealth Centers, Bedford, MA; 5Dartmouth-Hitchcock Medical Center, Lebanon, NH Insomnia is the most prevalent sleep disorder in the general popula- and disease management of chronic adult insomnia, using existing tion, and is commonly encountered in medical practices. Insomnia is evidence-based insomnia practice parameters where available, and defined as the subjective perception of difficulty with sleep initiation, consensus-based recommendations to bridge areas where such pa- duration, consolidation, or quality that occurs despite adequate oppor- rameters do not exist.