Receptor Antagonist
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MCQ Base Clinical Pharmacology
MCQ Base Clinical Pharmacology Mechanism of drug action is explored by: A) pharmacokinetics B) pharmacogenetics C) pharmacoeconomics D) pharmacodynamics E) pharmacognosy Therapeutic window is the dosages of a medication (therapeutic serum concentrations ) between: A) TD50 curve and ED50 B) ED50 and T1/2 C) the amount that gives an effect (effective dose) and the amount that gives more adverse effects than desired effects D) the amount that gives minimal adverse effects and the amount that gives more adverse effects E) the amount that gives minimal effect and the amount that gives full therapeutic effect Therapeutic index is the ratio of: A) LD50 over the ED50 B) ED50over the LD50 C) bioavailability over drug dose D) apparent volume of distribution over elimination rate constant E) total clearance over nonrenal (extrarenal) clearance Therapeutic drug monitoring means: A) trough concentration under steady-state condition B) measurement of medication concentrations in blood C) the process of chemical alteration of drugs in the body D) amount of untoward effects following treatment E) development of expected desired effects Therapeutic dose is not related to: A) patient’s age B) rout of administration C) desired therapeutic effect D) organs of elimination E) treatment costs Mean therapeutic doses mentioned in manuals is obtained by the following way: A) calculation of pharmacokinetic features B) clinical investigations C) experimental investigations D) experimental data adopted for human body E) calculation of pharmacodynamic features Find -
Evidence-Based Guidelines for Treating Depressive Disorders with Antidepressants
JOP0010.1177/0269881115581093Journal of PsychopharmacologyCleare et al. 581093research-article2015 BAP Guidelines Evidence-based guidelines for treating depressive disorders with antidepressants: A revision of the 2008 British Association Journal of Psychopharmacology 2015, Vol. 29(5) 459 –525 for Psychopharmacology guidelines © The Author(s) 2015 Reprints and permissions: sagepub.co.uk/journalsPermissions.nav DOI: 10.1177/0269881115581093 jop.sagepub.com Anthony Cleare1, CM Pariante2 and AH Young3 With expert co-authors (in alphabetical order): IM Anderson4, D Christmas5, PJ Cowen6, C Dickens7, IN Ferrier8, J Geddes9, S Gilbody10, PM Haddad11, C Katona12, G Lewis12, A Malizia13, RH McAllister-Williams14, P Ramchandani15, J Scott16, D Taylor17, R Uher18 and the members of the Consensus Meeting19 Endorsed by the British Association for Psychopharmacology Abstract A revision of the 2008 British Association for Psychopharmacology evidence-based guidelines for treating depressive disorders with antidepressants was undertaken in order to incorporate new evidence and to update the recommendations where appropriate. A consensus meeting involving experts in depressive disorders and their management was held in September 2012. Key areas in treating depression were reviewed and the strength of evidence and clinical implications were considered. The guidelines were then revised after extensive feedback from participants and interested parties. A literature review is provided which identifies the quality of evidence upon which the recommendations -
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. -
First Part Examination Mock Exam
FIRST PART EXAMINATION MOCK EXAM This Mock Examination is prepared to provide candidates, tutors and their Supervisors of Training with information about the way the Examiners will assess the performance of candidates in the Examination. Example questions provided are to be used as a guide only as to what may be expected. Candidates should discuss the exam with their tutors so that they may prepare appropriately for future examinations. It should be read in conjunction with the Notes to Candidates document. WRITTEN EXAM GLOSSARY OF TERMS Calculate Work out or estimate using mathematical principles Classify Divide into categories; organise, arrange Compare Examine similarities and differences Define Give the precise meaning Describe Give a detailed account of Explain Make plain, interpret, and account for Interpret Explain the meaning or significance Outline Provide a summary of the important points Relate Show a connection between Understand Appreciate the details of; comprehend 1 FIRST PART EXAMINATION MOCK EXAM SHORT ANSWER QUESTIONS MORNING PAPER (A) Start each answer on a new page and indicate the question number. It is not necessary to rewrite the question in your answer book. (B) You should aim to allocate ten minutes to answer each SAQ. (C) The questions are worth equal marks. (D) Short Answer Questions with more than one part have the proportion of marks indicated for each part. (E) Record your candidate number and each question number on the cover of each book and hand in all answer books. 2 Please answer Questions 1 and 2 in the blue answer booklet 1. Describe the anatomy of the left subclavian vein. -
(DMT), Harmine, Harmaline and Tetrahydroharmine: Clinical and Forensic Impact
pharmaceuticals Review Toxicokinetics and Toxicodynamics of Ayahuasca Alkaloids N,N-Dimethyltryptamine (DMT), Harmine, Harmaline and Tetrahydroharmine: Clinical and Forensic Impact Andreia Machado Brito-da-Costa 1 , Diana Dias-da-Silva 1,2,* , Nelson G. M. Gomes 1,3 , Ricardo Jorge Dinis-Oliveira 1,2,4,* and Áurea Madureira-Carvalho 1,3 1 Department of Sciences, IINFACTS-Institute of Research and Advanced Training in Health Sciences and Technologies, University Institute of Health Sciences (IUCS), CESPU, CRL, 4585-116 Gandra, Portugal; [email protected] (A.M.B.-d.-C.); ngomes@ff.up.pt (N.G.M.G.); [email protected] (Á.M.-C.) 2 UCIBIO-REQUIMTE, Laboratory of Toxicology, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal 3 LAQV-REQUIMTE, Laboratory of Pharmacognosy, Department of Chemistry, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal 4 Department of Public Health and Forensic Sciences, and Medical Education, Faculty of Medicine, University of Porto, 4200-319 Porto, Portugal * Correspondence: [email protected] (D.D.-d.-S.); [email protected] (R.J.D.-O.); Tel.: +351-224-157-216 (R.J.D.-O.) Received: 21 September 2020; Accepted: 20 October 2020; Published: 23 October 2020 Abstract: Ayahuasca is a hallucinogenic botanical beverage originally used by indigenous Amazonian tribes in religious ceremonies and therapeutic practices. While ethnobotanical surveys still indicate its spiritual and medicinal uses, consumption of ayahuasca has been progressively related with a recreational purpose, particularly in Western societies. The ayahuasca aqueous concoction is typically prepared from the leaves of the N,N-dimethyltryptamine (DMT)-containing Psychotria viridis, and the stem and bark of Banisteriopsis caapi, the plant source of harmala alkaloids. -
Etiology, Classification, and Treatment of Urticaria
CONTINUING MEDICAL EDUCATION Etiology, Classification, and Treatment of Urticaria Kjetil Kristoffer Guldbakke, MD; Amor Khachemoune, MD, CWS GOAL To understand urticaria to better manage patients with the condition OBJECTIVES Upon completion of this activity, dermatologists and general practitioners should be able to: 1. Discuss the clinical classification of urticaria. 2. Recognize how to diagnose urticaria. 3. Identify treatment options. CME Test on page 50. This article has been peer reviewed and approved Einstein College of Medicine is accredited by by Michael Fisher, MD, Professor of Medicine, the ACCME to provide continuing medical edu- Albert Einstein College of Medicine. Review date: cation for physicians. December 2006. Albert Einstein College of Medicine designates This activity has been planned and imple- this educational activity for a maximum of 1 AMA mented in accordance with the Essential Areas PRA Category 1 CreditTM. Physicians should only and Policies of the Accreditation Council for claim credit commensurate with the extent of their Continuing Medical Education through the participation in the activity. joint sponsorship of Albert Einstein College of This activity has been planned and produced in Medicine and Quadrant HealthCom, Inc. Albert accordance with ACCME Essentials. Drs. Guldbakke and Khachemoune report no conflict of interest. The authors discuss off-label use of colchi- cine, cyclophosphamide, cyclosporine, dapsone, intravenous immunoglobulin, methotrexate, montelukast sodium, nifedipine, plasmapheresis, rofecoxib, sulfasalazine, tacrolimus, thyroxine, and zafirlukast. Dr. Fisher reports no conflict of interest. Urticaria is among the most common skin dis- autoimmune mechanisms are now recognized as a eases. It can be acute, chronic, mediated by a cause of chronic urticaria. A search of the PubMed physical stimulus, or related to contact with an database (US National Library of Medicine) for urticant. -
Safety Alert: Risks Associated with Ophthalmic Anesthetics
WRHA Pharmacy Program Health Sciences Centre MS-189 820 Sherbrook St. Winnipeg, Manitoba R3A 1R9 CANADA TEL: 204-787-7183 Fax: 204-787-3195 FAX: 204-787-3195 Safety Alert: Risks associated with Ophthalmic Anesthetics The self-administration of ophthalmic anesthetics by patients for the relief of eye pain should be avoided and they should not be given to patients to take home for pain relief. Vision threatening complications of topical anesthetic abuse are common. There is no indication for the use of ophthalmic anesthetics except for diagnostic and short term therapeutic purposes (the removal of a foreign body or ocular surgery) and therefore, these products should only be used under a physician’s supervision. Eye trauma resulting in a corneal abrasion (epithelial injury) is a common complaint in the Emergency department (1). A superficial corneal injury can cause intense pain causing a patient to seek medical help or immediate relief from available over the counter remedies. In Canada, only two topical ophthalmic anesthetic drugs are available commercially as single entities, proparacaine (proxymetacaine) and tetracaine (available in bottle and minim forms). Benoxinate (oxybuprocaine) is only available in combination with fluorescein (3). Lidocaine is also used in ophthalmic surgical procedures however, it is not available in the Canadian market as an ophthalmic preparation. Topical ophthalmic anesthetics function by blocking nerve conduction when applied to the cornea and conjunctiva. The ocular surface is innervated by the multiple branches of the trigeminal nerve. The cornea is supplied by the long and short ciliary nerves, the nasociliary nerve and the lacrimal nerve (4). Topical anesthetics reduce sodium permeability preventing generation and conduction of nerve impulses, increasing excitation threshold, and slowing the nerve impulse propagation. -
Recovery from Tachyphylaxis of TRPV1 Coincides with Recycling to the Surface Membrane
Recovery from tachyphylaxis of TRPV1 coincides with recycling to the surface membrane Quan Tiana,1, Juan Hua,1, Chang Xiea,1, Kaidi Meia, Cuong Phamb, Xiaoyi Moa, Régine Heppb, Sylvia Soaresb, Fatiha Nothiasb, Yuanyuan Wanga, Qiang Liua, Fen Caia, Bo Zhonga, Dongdong Lib,2, and Jing Yaoa,2 aHubei Key Laboratory of Cell Homeostasis, College of Life Sciences, Wuhan University, Wuhan, 430072 Hubei, China; and bSorbonne Université, Institut de Biologie de Paris-Seine, Neuroscience Paris Seine, CNRS UMR8246, INSERM U1130, 75005 Paris, France Edited by Francisco Bezanilla, The University of Chicago, Chicago, IL, and approved January 31, 2019 (received for review November 20, 2018) The transient receptor potential vanilloid-1 (TRPV1) ion channel is and regulates TRPV1 recycling via distinct routes mediated by essential for sensation of thermal and chemical pain. TRPV1 synaptotagmin 1 and 7, respectively. These results suggest the + activation is accompanied by Ca2 -dependent desensitization; contribution of TRPV1 trafficking to the establishment of acute desensitization reflects rapid reduction in channel activity tachyphylaxis. during stimulation, whereas tachyphylaxis denotes the diminution in TRPV1 responses to repetitive stimulation. Acute desensitization Results has been attributed to conformational changes of the TRPV1 chan- Whole-Cell Tachyphylaxis Is Stimulation Strength Dependent. TRPV1 + nel; however, the mechanisms underlying the establishment of tachyphylaxis is a Ca2 -dependent process and has been induced tachyphylaxis remain to be defined. Here, we report that the de- by saturated doses of capsaicin (1, 4, 9). We applied different gree of whole-cell TRPV1 tachyphylaxis is regulated by the doses of capsaicin to induce desensitization in TRPV1-expressing strength of inducing stimulation. -
Histamine and Antihistamines Sites of Action Conditions Which Cause Release Aron H
Learning Objectives I Histamine Pharmacological effects Histamine and Antihistamines Sites of action Conditions which cause release Aron H. Lichtman, Ph.D. Diagnostic uses Associate Professor II Antihistamines acting at the H1 and H2 receptor Pharmacology and Toxicology Pharmacological effects Mechanisms of action Therapeutic uses Side effects and drug interactions Be familiar with the existence of the H3 receptor III Be able to describe the main mechanism of action of cromolyn sodium and its clinical uses Histamine Pharmacology First autacoid to be discovered. (Greek: autos=self; Histamine Formation akos=cure) Synthesized in 1907 Synthesized in mammalian tissues by Demonstrated to be a natural constituent of decarboxylation of the amino acid l-histidine mammalian tissues (1927) Involved in inflammatory and anaphylactic reactions. Local application causes swelling redness, and edema, mimicking a mild inflammatory reaction. Large systemic doses leads to profound vascular changes similar to those seen after shock or anaphylactic origin Histamine Stored in complex with: Heparin Chondroitin Sulfate Eosinophilic Chemotactic Factor Neutrophilic Chemotactic Factor Proteases 1 Conditions That Release Histamine 1. Tissue injury: Any physical or chemical agent that injures tissue, skin or mucosa are particularly sensitive to injury and will cause the immediate release of histamine from mast cells. 2. Allergic reactions: exposure of an antigen to a previously sensitized (exposed) subject can immediately trigger allergic reactions. If sensitized by IgE antibodies attached to their surface membranes will degranulate when exposed to the appropriate antigen and release histamine, ATP and other mediators. 3. Drugs and other foreign compounds: morphine, dextran, antimalarial drugs, dyes, antibiotic bases, alkaloids, amides, quaternary ammonium compounds, enzymes (phospholipase C). -
Guidance on the Use of H2 Antagonists for the Prevention and Management of Hypersensitivity
Guidance on the use of H2 antagonists for the prevention and management of hypersensitivity To guide for members on the prevention and management of hypersensitivity in situations where H2 antagonists are in short supply or unavailable www.bopa.org.uk Version 1.0 3rd June 2020 Contents 1. Scope ........................................................................................................................................ 3 2. Introduction ................................................................................................................................ 3 3. Approach ................................................................................................................................... 3 4. Guidance ................................................................................................................................... 4 5. Table 1: H2 Antagonists ............................................................................................................. 6 6. References ................................................................................................................................ 7 7. Acknowledgements ................................................................................................................... 8 8. Document control ...................................................................................................................... 8 Guidance on the use of H2 antagonists for the prevention and management of hypersensitivity Page 2 of 8 1. Scope 1.1 This guidance -
Histamine H2 Antagonist (Oral Route, Injection Route, Intravenous Route)
Histamine H2 Antagonist (Oralvisited Route, Injectionon 8/21/2015 Route, Intravenous Route)... Page 1 of 7 Request an Appointment Log in to Patient Search Mayo Clinic Find a Doctor Account Find a Job Translated Content Give Now PATIENT CARE & DEPARTMENTS & RESEARCH EDUCATION FOR MEDICAL PRODUCTS & GIVING TO HEALTH INFO CENTERS PROFESSIONALS SERVICES MAYO CLINIC Drugs and Supplements Print Histamine H2 Antagonist (Oral Route, Injection Route, Intravenous Route) Proper Use Advertisement Description and Brand Names Drug information provided by: Micromedex Before Using For patients taking the nonprescription strengths of these Proper Use medicines for heartburn, acid indigestion, and sour stomach: Precautions • Do not take the maximum daily dosage continuously for more than 2 weeks, unless directed to do so by your doctor. Side Effects • If you have trouble in swallowing, or persistent abdominal pain, see your doctor promptly. These may be signs of a Products and services serious condition that may need different treatment. For patients taking the prescription strengths of these medicines for more serious problems: • One dose a day—Take it at bedtime, unless otherwise Mayo Clinic is a not-for-profit organization. directed. Proceeds from website advertising help • Two doses a day—Take one in the morning and one at support our mission. Mayo Clinic does not endorse non-Mayo products and services. bedtime. • Several doses a day—Take them with meals and at bedtime Advertising & Sponsorship for best results. Policy Opportunities It may take several days before this medicine begins to relieve stomach pain. To help relieve this pain, antacids may be taken Mayo Clinic Store with the H2-blocker, unless your doctor has told you not to use them. -
Npp2013281.Pdf
Neuropsychopharmacology (2013) 38, S435–S593 & 2013 American College of Neuropsychopharmacology. All rights reserved 0893-133X/13 www.neuropsychopharmacology.org Poster Session III-Wednesday participants indicated their ongoing experience of the Wednesday, December 11, 2013 intensity of heartbeat and breathing sensations by rotating a dial. Discrimination was measured by a positive dial deflection above baseline during an infusion trial. Accuracy W2. Interoceptive Awareness in Meditators During was measured via maximum cross correlation between each Cardiorespiratory Deviations in Body Arousal subject’s dial ratings and their corresponding heart rate Sahib Khalsa*, David Rudrauf, Richard Davidson, response. After each infusion participants also traced the Daniel Tranel body locations where they had felt heartbeat sensations, on a manikin template. UCLA Semel Institute for Neuroscience and Human Results: Bolus isoproterenol infusions elicited equivalent Behavior, Los Angeles, California increases in heart rate in both groups (Repeated measures ANOVA; F(1, 5) ¼ 50.1, po0.0001). There were no signifi- Background: Attention directed towards internal body cant group (F(1, 28) ¼ 1.27, p ¼ 0.27) or group x dose sensations is commonly practiced in many meditation interactions (F(1, 5) ¼ 0.04, p ¼ 0.998). There were also no traditions, and is a core skill cultivated when learning group differences in adrenergic sensitivity as measured by mindfulness. This practice is commonly proposed to CD25 (dose required to elevate heart rate by 25 beats per