548 Trimipramine for Refractory Panic Attacks
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Acute Extrapyramidal Symptoms Following Abrupt Discontinuation of Propranolol
Medical Journal of the Volume 14 Islamic Republic of Iran Number 3 Fall 1379 November 2000 ACUTE EXTRAPYRAMIDAL SYMPTOMS FOLLOWING ABRUPT DISCONTINUATION OF PROPRANOLOL A. ALAVIAN GHAVANINI From the Center Jor Research Consultation, School oj Medicine, Shiraz University ojMedical Sciences, Shiraz, I.R. Iran. ABSTRACT A case of acute extrapyramidal manifestations consisting of dystonia and akathisia following abrupt discontinuation of propranolol is reported. She re sponded well to oral propranolol and intramuscular diazepam. Extrapyramidal symptoms have commonly been associated with acute or chronic administration of neuroleptic drugs. There have been reports of a substantial number of cases with similar clinical characteristics associated with tricyclic antidepressants, monoamine oxidase inhibitors, and selective serotonin reuptake inhibitors. Al though it is known that beta-adrenoceptor antagonists are effective in the treat ment of extrapyramidal symptoms, especially akathisia, there has been no previ ous report of such symptoms induced by abrupt withdrawal of these drugs. Al though she had been on low dose amitriptyline and had discontinued this medica tion long before, prolonged use of amitriptyline may have had a predisposing role in the development of these symptoms. MJIRL Vol. 14, No.3, 305-306, 2000. Keywords: Propranolol; Extrapyramidal symptoms; Beta-adrenoceptor antagonists. INTRODUCTION She described a feeling of "being pulled down by gravity." She had never experienced such symptoms before. Thor Extrapyramidal symptoms include acute dystonias, ough physical examination with special focus on the ner akathisia, Parkinson's syndrome, and tardive dyskinesia. vous system was unremarkable except for the involuntary These symptoms are common manifestations of neurolep contraction of jaw muscles and a fine tremor in her ex tic drugs. -
Prevalence of Extrapyramidal Side Effects in Patients on Antipsychotics Drugs at a Tertiary Care Center
f Ps al o ych rn ia u tr o y J Kirgaval et al., J Psychiatry 2017, 20:5 Journal of Psychiatry DOI: 10.4172/2378-5756.1000419 ISSN: 2378-5756 Research Article Open Access Prevalence of Extrapyramidal Side Effects in Patients on Antipsychotics Drugs at a Tertiary Care Center5 Ramprasad Santhanakrishna Kirgaval1*, Srinivas Revanakar2 and Chidanand Srirangapattna2 1Department of Psychiatry, Shimoga Institute of Medical Sciences, Shimoga, Karnataka, India 2Department of Pharmacology, Shimoga Institute of Medical Sciences, Shimoga, Karnataka, India Abstract Background: Antipsychotic drugs are associated with adverse effects that can lead to poor medication adherence, stigma, distress and impaired quality of life. Among the various side effects of anti-psychotics extra pyramidal symptoms constitute one of the important side effects interfering with the compliance of the patients towards medication. Objective: Evaluation of extrapyramidal side effects by AIMS in patients who are on antipsychotics. Results: The extrapyramidal symptoms were more commonly seen in males (62.85%), the age of incidence of maximum in the age group of 34.28, Maximum was seen among the patients on the Risperidone (45.7%), Involvement of the extremities was common (42.85%) and 64.28% of individuals had moderate severity and 54.28% of individuals were aware of the extrapyramidal symptoms which provided mild distress. Conclusion: Extrapyramidal symptoms are one of the commonest side effect of the antipsychotics interfering with compliance of the patients towards adherence to medications, thereby decreasing the efficacy. Keywords: Extrapyramidal symptoms; Compliance; Antipsychotics; positive symptom of the psychosis but have some serious limitations AIMS. such as lack of efficacy against negative symptoms and adverse effects like extrapyramidal symptoms [7]. -
Treatment of Psychosis: 30 Years of Progress
Journal of Clinical Pharmacy and Therapeutics (2006) 31, 523–534 REVIEW ARTICLE Treatment of psychosis: 30 years of progress I. R. De Oliveira* MD PhD andM.F.Juruena MD *Department of Neuropsychiatry, School of Medicine, Federal University of Bahia, Salvador, BA, Brazil and Department of Psychological Medicine, Institute of Psychiatry, King’s College, University of London, London, UK phrenia. Thirty years ago, psychiatrists had few SUMMARY neuroleptics available to them. These were all Background: Thirty years ago, psychiatrists had compounds, today known as conventional anti- only a few choices of old neuroleptics available to psychotics, and all were liable to cause severe extra them, currently defined as conventional or typical pyramidal side-effects (EPS). Nowadays, new antipsychotics, as a result schizophrenics had to treatments are more ambitious, aiming not only to suffer the severe extra pyramidal side effects. improve psychotic symptoms, but also quality of Nowadays, new treatments are more ambitious, life and social reinsertion. We briefly but critically aiming not only to improve psychotic symptoms, outline the advances in diagnosis and treatment but also quality of life and social reinsertion. Our of schizophrenia, from the mid 1970s up to the objective is to briefly but critically review the present. advances in the treatment of schizophrenia with antipsychotics in the past 30 years. We conclude DIAGNOSIS OF SCHIZOPHRENIA that conventional antipsychotics still have a place when just the cost of treatment, a key factor in Up until the early 1970s, schizophrenia diagnoses poor regions, is considered. The atypical anti- remained debatable. The lack of uniform diagnostic psychotic drugs are a class of agents that have criteria led to relative rates of schizophrenia being become the most widely used to treat a variety of very different, for example, in New York and psychoses because of their superiority with London, as demonstrated in an important study regard to extra pyramidal symptoms. -
Dopamine D2 Receptor Occupancy by Perospirone: a Positron Emission Tomography Study in Patients with Schizophrenia and Healthy Subjects
Psychopharmacology (2010) 209:285–290 DOI 10.1007/s00213-010-1783-1 ORIGINAL INVESTIGATION Dopamine D2 receptor occupancy by perospirone: a positron emission tomography study in patients with schizophrenia and healthy subjects Ryosuke Arakawa & Hiroshi Ito & Akihiro Takano & Masaki Okumura & Hidehiko Takahashi & Harumasa Takano & Yoshiro Okubo & Tetsuya Suhara Received: 3 September 2009 /Accepted: 18 January 2010 /Published online: 27 March 2010 # Springer-Verlag 2010 Abstract striatum of healthy subjects was 74.8% at 1.5 h, 60.1% at Rationale Perospirone is a novel second-generation antipsy- 8 h, and 31.9% at 25.5 h after administration. chotic drug with high affinity to dopamine D2 receptor and Conclusion Sixteen milligrams of perospirone caused over short half-life of plasma concentration. There has been no 70% dopamine D2 receptor occupancy near its peak level, investigation of dopamine D2 receptor occupancy in patients and then occupancy dropped to about half after 22 h. The with schizophrenia and the time course of occupancy by time courses of receptor occupancy and plasma concentra- antipsychotics with perospirone-like properties. tion were quite different. This single dosage may be Objective We investigated dopamine D2 receptor occupan- sufficient for the treatment of schizophrenia and might be cy by perospirone in patients with schizophrenia and the useful as a new dosing schedule choice. time course of occupancy in healthy subjects. Materials and methods Six patients with schizophrenia Keywords Dopamine D2 receptor occupancy. taking 16–48 mg/day of perospirone participated. Positron Perospirone . Positron emission tomography . emission tomography (PET) scans using [11C]FLB457 were Schizophrenia . Time course performed on each subject, and dopamine D2 receptor occupancies were calculated. -
Modern Antipsychotic Drugs: a Critical Overview
Review Synthèse Modern antipsychotic drugs: a critical overview David M. Gardner, Ross J. Baldessarini, Paul Waraich Abstract mine was based primarily on the finding that dopamine ago- nists produced or worsened psychosis and that antagonists CONVENTIONAL ANTIPSYCHOTIC DRUGS, used for a half century to treat were clinically effective against psychotic and manic symp- a range of major psychiatric disorders, are being replaced in clini- 5 toms. Blocking dopamine D2 receptors may be a critical or cal practice by modern “atypical” antipsychotics, including ari- even sufficient neuropharmacologic action of most clinically piprazole, clozapine, olanzapine, quetiapine, risperidone and effective antipsychotic drugs, especially against hallucina- ziprasidone among others. As a class, the newer drugs have been promoted as being broadly clinically superior, but the evidence for tions and delusions, but it is not necessarily the only mecha- this is problematic. In this brief critical overview, we consider the nism for antipsychotic activity. Moreover, this activity, and pharmacology, therapeutic effectiveness, tolerability, adverse ef- subsequent pharmacocentric and circular speculations about fects and costs of individual modern agents versus older antipsy- altered dopaminergic function, have not led to a better un- chotic drugs. Because of typically minor differences between derstanding of the pathophysiology or causes of the several agents in clinical effectiveness and tolerability, and because of still idiopathic psychotic disorders, nor have they provided a growing concerns about potential adverse long-term health conse- non-empirical, theoretical basis for the design or discovery quences of some modern agents, it is reasonable to consider both of improved treatments for psychotic disorders. older and newer drugs for clinical use, and it is important to inform The neuropharmacodynamics of specific modern anti- patients of relative benefits, risks and costs of specific choices. -
Revision of Precautions Asenapine Maleate, Aripiprazole, Olanzapine
Published by Translated by Ministry of Health, Labour and Welfare Pharmaceuticals and Medical Devices Agency This English version is intended to be a reference material to provide convenience for users. In the event of inconsistency between the Japanese original and this English translation, the former shall prevail. Revision of Precautions Asenapine maleate, aripiprazole, olanzapine, quetiapine fumarate, clocapramine hydrochloride hydrate, chlorpromazine hydrochloride, chlorpromazine hydrochloride/promethazine hydrochloride/phenobarbital, chlorpromazine phenolphthalinate, spiperone, zotepine, timiperone, haloperidol, paliperidone, pipamperone hydrochloride, fluphenazine decanoate, fluphenazine maleate, brexpiprazole, prochlorperazine maleate, prochlorperazine mesilate, Pharmaceuticals and Medical Devices Agency Office of Safety I 3-3-2 Kasumigaseki, Chiyoda-ku, Tokyo 100-0013 Japan E-mail: [email protected] Published by Translated by Ministry of Health, Labour and Welfare Pharmaceuticals and Medical Devices Agency This English version is intended to be a reference material to provide convenience for users. In the event of inconsistency between the Japanese original and this English translation, the former shall prevail. propericiazine, bromperidol, perphenazine, perphenazine hydrochloride, perphenazine fendizoate, perphenazine maleate, perospirone hydrochloride hydrate, mosapramine hydrochloride, risperidone (oral drug), levomepromazine hydrochloride, levomepromazine maleate March 27, 2018 Non-proprietary name Asenapine maleate, -
Antipsychotics
The Fut ure of Antipsychotic Therapy (page 7 in syllabus) Stepp,,hen M. Stahl, MD, PhD Adjunct Professor, Department of Psychiatry Universityyg of California, San Diego School of Medicine Honorary Visiting Senior Fellow, Cambridge University, UK Sppyonsored by the Neuroscience Education Institute Additionally sponsored by the American Society for the Advancement of Pharmacotherapy This activity is supported by an educational grant from Sunovion Pharmaceuticals Inc. Copyright © 2011 Neuroscience Education Institute. All rights reserved. Individual Disclosure Statement Faculty Editor / Presenter Stephen M. Stahl, MD, PhD, is an adjunct professor in the department of psychiatry at the University of California, San Diego School of Medicine, and an honorary visiting senior fellow at the University of Cambridge in the UK. Grant/Research: AstraZeneca, BioMarin, Dainippon Sumitomo, Dey, Forest, Genomind, Lilly, Merck, Pamlab, Pfizer, PGxHealth/Trovis, Schering-Plough, Sepracor/Sunovion, Servier, Shire, Torrent Consultant/Advisor: Advent, Alkermes, Arena, AstraZeneca, AVANIR, BioMarin, Biovail, Boehringer Ingelheim, Bristol-Myers Squibb, CeNeRx, Cypress, Dainippon Sumitomo, Dey, Forest, Genomind, Janssen, Jazz, Labopharm, Lilly, Lundbeck, Merck, Neuronetics, Novartis, Ono, Orexigen, Otsuka, Pamlab, Pfizer, PGxHealth/Trovis, Rexahn, Roche, Royalty, Schering-Plough, Servier, Shire, Solvay/Abbott, Sunovion/Sepracor, Valeant, VIVUS, Speakers Bureau: Dainippon Sumitomo, Forest, Lilly, Merck, Pamlab, Pfizer, Sepracor/Sunovion, Servier, Wyeth Copyright © 2011 Neuroscience Education Institute. All rights reserved. Learninggj Objectives • Differentiate antipsychotic drugs from each other on the basis of their pharmacological mechanisms and their associated therapeutic and side effects • Integrate novel treatment approaches into clinical practice according to best practices guidelines • Identify novel therapeutic options currently being researched for the treatment of schizophrenia Copyright © 2011 Neuroscience Education Institute. -
Prolactin Levels in Schizophrenic Patients Receiving Perospirone in Comparison to Risperidone
J Pharmacol Sci 91, 259 – 262 (2003) Journal of Pharmacological Sciences ©2003 The Japanese Pharmacological Society Short Communication Prolactin Levels in Schizophrenic Patients Receiving Perospirone in Comparison to Risperidone Takashi Togo1,2,*, Eizo Iseki2, Mika Shoji1, Ikuo Oyama1, Akihiko Kase1, Hirotake Uchikado2, Omi Katsuse2 and Kenji Kosaka2 1Yokohama Maioka Hospital, Yokohama 244-0813, Japan 2Department of Psychiatry, Yokohama City University School of Medicine, Yokohama 236-0004, Japan Received November 21, 2002; Accepted January 9, 2003 Abstract. Serum prolactin levels were investigated in 41 patients with schizophrenia who were receiving clinically effective doses of perospirone or risperidone for more than 4 weeks. In order to determine baseline prolactin levels, blood samples were obtained in the morning, 10 – 14 h after antipsychotic medication. Median levels were within normal limits in both female and male patients receiving perospirone, while risperidone induced significant elevation. These results suggest that in contrast to risperidone, where baseline prolactin levels were elevated 5.3-fold in female and 4.2-fold in male patients, baseline prolactin levels are not elevated after treatment with perospirone. However, these results should be cautiously interpreted, because drug-by-time interaction has previously been reported in antipsychotic-induced hyperprolactinemia. Keywords: prolactin, perospirone, schizophrenia Hyperprolactinemia is a common side effect that may well as the adverse effects of perospirone have not been arise from the use of antipsychotic agents (1, 2). Before fully investigated. In the present study, we have investi- the introduction of clozapine, it was assumed that all gated the baseline serum prolactin levels in patients antipsychotics cause extrapyramidal side effects and treated with clinically effective doses of perospirone in elevate prolactin levels by antagonizing dopamine D2 comparison to risperidone. -
Efficacy and Tolerability of Aripiprazole Versus D2 Antagonists in the Early
www.nature.com/npjschz REVIEW ARTICLE OPEN Efficacy and tolerability of aripiprazole versus D2 antagonists in the early course of schizophrenia: a systematic review and meta-analysis David D. Kim1,2, Alasdair M. Barr1,2, Lulu Lian1, Jessica W. Y. Yuen1, Diane Fredrikson3, William G. Honer2,3, Allen E. Thornton2,4 and ✉ Ric M. Procyshyn 2,3 Early intervention is essential for favorable long-term outcomes in schizophrenia. However, there is limited guidance in the scientific literature on how best to choose between dopamine D2 receptor (D2R) partial agonists and D2R antagonists in early stages of schizophrenia. The aim of this meta-analysis was to directly compare D2R partial agonists with D2R antagonists for efficacy and tolerability, using randomized controlled trials (RCTs) that involved participants diagnosed with first-episode psychosis, schizophrenia, or related psychotic disorders with a duration of illness ≤5 years. Fourteen RCTs, involving 2494 patients, were included in the meta-analysis. Aripiprazole was the only identified D2R partial agonist, and was not significantly different from pooled D2R antagonists for overall symptom reduction or all-cause discontinuation. However, aripiprazole was more favorable than pooled D2R antagonists for depressive symptoms, prolactin levels, and triglyceride levels. Specifically, aripiprazole was more favorable than paliperidone for triglyceride levels and more favorable than risperidone and olanzapine, but less favorable than ziprasidone, for weight gain. In addition, aripiprazole was less favorable for akathisia compared with second-generation D2R 1234567890():,; antagonists, in particular olanzapine and quetiapine, and less favorable for discontinuation due to inefficacy than risperidone. Lastly, aripiprazole was more favorable than haloperidol for various efficacy and tolerability outcomes. -
United States Patent (10 ) Patent No.: US 10,660,887 B2 Javitt (45 ) Date of Patent: *May 26 , 2020
US010660887B2 United States Patent (10 ) Patent No.: US 10,660,887 B2 Javitt (45 ) Date of Patent : *May 26 , 2020 (54 ) COMPOSITION AND METHOD FOR (56 ) References Cited TREATMENT OF DEPRESSION AND PSYCHOSIS IN HUMANS U.S. PATENT DOCUMENTS 6,228,875 B1 5/2001 Tsai et al. ( 71 ) Applicant : Glytech , LLC , Ft. Lee , NJ (US ) 2004/0157926 A1 * 8/2004 Heresco - Levy A61K 31/198 514/561 (72 ) Inventor: Daniel C. Javitt , Ft. Lee , NJ (US ) 2005/0261340 Al 11/2005 Weiner 2006/0204486 Al 9/2006 Pyke et al . 2008/0194631 Al 8/2008 Trovero et al. ( 73 ) Assignee : GLYTECH , LLC , Ft. Lee , NJ (US ) 2008/0194698 A1 8/2008 Hermanussen et al . 2010/0069399 A1 * 3/2010 Gant CO7D 401/12 ( * ) Notice : Subject to any disclaimer, the term of this 514 / 253.07 patent is extended or adjusted under 35 2010/0216805 Al 8/2010 Barlow 2011/0207776 Al 8/2011 Buntinx U.S.C. 154 ( b ) by 95 days . 2011/0237602 A1 9/2011 Meltzer This patent is subject to a terminal dis 2011/0306586 Al 12/2011 Khan claimer . 2012/0041026 A1 2/2012 Waizumi ( 21 ) Appl. No.: 15 /650,912 FOREIGN PATENT DOCUMENTS CN 101090721 12/2007 ( 22 ) Filed : Jul. 16 , 17 KR 2007 0017136 2/2007 WO 2005/065308 7/2005 (65 ) Prior Publication Data WO 2005/079756 9/2005 WO 2011044089 4/2011 US 2017/0312275 A1 Nov. 2 , 2017 WO 2012/104852 8/2012 WO 2005/000216 9/2013 WO 2013138322 9/2013 Related U.S. Application Data (63 ) Continuation of application No. -
Pharmacology Review(S)
CENTER FOR DRUG EVALUATION AND RESEARCH APPLICATION NUMBER: 200603 PHARMACOLOGY REVIEW(S) Tertiary Pharmacology/Toxicology Review From: Paul C. Brown, Ph.D., ODE Associate Director for Pharmacology and Toxicology, OND IO NDA: 200603 Agency receipt date: 12/30/2009 Drug: Lurasidone hydrochloride Applicant: Sunovion Pharmaceuticals (Originally submitted by Dainippon Sumimoto Pharma America, Inc.) Indication: schizophrenia Reviewing Division: Division of Psychiatry Products Background: The pharm/tox reviewer and team leader concluded that the nonclinical data support approval of lurasidone for the indication listed above. Reproductive and Developmental Toxicity: Reproductive and developmental toxicity studies in rats and rabbits revealed no evidence of teratogenicity or embryofetal toxicity. The high doses in the rat and rabbit embryofetal toxicity studies were 3 and 12 times, respectively, the maximum recommended human dose (80 mg) based on a body surface area comparison. Carcinogenicity: Lurasidone was tested in 2 year rat and mouse carcinogenicity studies. These studies were reviewed by the division and the executive carcinogenicity assessment committee. The committee concluded that the studies were adequate and that there was a drug-related increase in mammary carcinomas in female rats at doses of 12 mg/kg and higher and a drug-related increase in mammary carcinomas and adenoacanthomas and pituitary pars distalis adenomas in female mice. The applicant also provided data from various studies showing that lurasidone significantly increases prolactin in several different species including rats and mice. Conclusions: I agree with the division pharm/tox conclusion that this application can be approved from a pharm/tox perspective. The division recommends that lurasidone be labeled with pregnancy category B. -
Antipsychotic Tolerance: Evaluating the Behavioural Effects of Continuous Versus Intermittent Haloperidol Exposure
Antipsychotic Tolerance: Evaluating the Behavioural Effects of Continuous Versus Intermittent Haloperidol Exposure. by Laura Schulze A thesis submitted in conformity with the requirements for the degree of Master of Science Institute of Medical Science University of Toronto © Copyright by Laura Schulze (2014) Antipsychotic Tolerance: Evaluating the Behavioural Effects of Continuous Versus Intermittent Haloperidol Exposure. Laura Schulze Master of Science Institute of Medical Science University of Toronto 2014 Abstract There are several lines of investigation, both preclinical and clinical, that suggest antipsychotic drug (APD) tolerance may occur. Using a behavioural animal model, the present study examined whether the amount of APD exposure (i.e. continuous versus intermittent) significantly impacts APD efficacy. More specifically, it was investigated whether continuous haloperidol (an APD) exposure, in comparison to intermittent, would lead to a decrease in response over time. Catalepsy, locomotor activity, and exploratory behaviour were assessed weekly, over the course of 21 days, in rats receiving haloperidol continuously or intermittently. Our findings are consistent with earlier preclinical reports that have implicated chronic and continuous APD therapy in reduced drug effect. This line of investigation has immediate and direct implications in terms of current guidelines regarding maintenance antipsychotic treatment. ii Moving forward, we are in a position to translate these results to clinical studies that can further examine this issue in humans. iii Acknowledgments Thank you to my fellow colleagues Melanie Guenette, Patrick McCormick, and Steve Mann for your infinite wisdom, guidance, and support. Melanie, you have become a great friend and I am indebted to you for mentoring me throughout this experience. You are one of the most generous people that I have met, and I thank you for taking me under your wing.