Designing Inhibitors Via Molecular Modelling Methods for Monoamine Oxidase Isozymes a and B Filiz Varnali Kadir Has Universit
Total Page:16
File Type:pdf, Size:1020Kb
Load more
Recommended publications
-
Studies on the Metabolism and Toxicity of Hydrazine in The~Rat~
STUDIES ON THE METABOLISM AND TOXICITY OF HYDRAZINE IN THE~RAT~ Andrew Michael Jenner, B.Sc. Submitted to the University of London for the examination of the degree for Doctor of Philosophy, 1992 Toxicology Department The School of Pharmacy Brunswick Square London ProQuest Number: U068521 All rights reserved INFORMATION TO ALL USERS The quality of this reproduction is dependent upon the quality of the copy submitted. In the unlikely event that the author did not send a com plete manuscript and there are missing pages, these will be noted. Also, if material had to be removed, a note will indicate the deletion. uest ProQuest U068521 Published by ProQuest LLC(2017). Copyright of the Dissertation is held by the Author. All rights reserved. This work is protected against unauthorized copying under Title 17, United States C ode Microform Edition © ProQuest LLC. ProQuest LLC. 789 East Eisenhower Parkway P.O. Box 1346 Ann Arbor, Ml 48106- 1346 ACKNOWLEDGEMENTS I would like to express my sincere appreciation to my supervisor Dr. John Timbrell for his invaluable advice, guidance and support. Many people have assisted the progress of my studies in a wide variety of ways, including everyone who has worked alongside me in the Toxicology Unit, both past and present. Particular thanks go to Simon (ET) for his critical eye and mutual, down to earth Yorkshire mentality and also to Cathy for her heartening encouragement. I would also like to thank Dr. Alan Boobis for his assistance in obtaining human liver samples and to the USAF for funding this project. Finally I would like to recognise Jacqui for her designs, Maria for her typing, Justina for her continuous care and support and to my mum and dad for their understanding and my much appreciated conveyance through life. -
Ayahuasca: Spiritual Pharmacology & Drug Interactions
Ayahuasca: Spiritual Pharmacology & Drug Interactions BENJAMIN MALCOLM, PHARMD, MPH [email protected] MARCH 28 TH 2017 AWARE PROJECT Can Science be Spiritual? “Science is not only compatible with spirituality; it is a profound source of spirituality. When we recognize our place in an immensity of light years and in the passage of ages, when we grasp the intricacy, beauty and subtlety of life, then that soaring feeling, that sense of elation and humility combined, is surely spiritual. The notion that science and spirituality are somehow mutually exclusive does a disservice to both.” – Carl Sagan Disclosures & Disclaimers No conflicts of interest to disclose – I don’t get paid by pharma and have no potential to profit directly from ayahuasca This presentation is for information purposes only, none of the information presented should be used in replacement of medical advice or be considered medical advice This presentation is not an endorsement of illicit activity Presentation Outline & Objectives Describe what is known regarding ayahuasca’s pharmacology Outline adverse food and drug combinations with ayahuasca as well as strategies for risk management Provide an overview of spiritual pharmacology and current clinical data supporting potential of ayahuasca for treatment of mental illness Pharmacology Terms Drug ◦ Term used synonymously with substance or medicine in this presentation and in pharmacology ◦ No offense intended if I call your medicine or madre a drug! Bioavailability ◦ The amount of a drug that enters the body and is able to have an active effect ◦ Route specific: bioavailability is different between oral, intranasal, inhalation (smoked), and injected routes of administration (IV, IM, SC) Half-life (T ½) ◦ The amount of time it takes the body to metabolize/eliminate 50% of a drug ◦ E.g. -
Strategies for Managing Sexual Dysfunction Induced by Antidepressant Medication
King’s Research Portal DOI: 10.1002/14651858.CD003382.pub3 Document Version Publisher's PDF, also known as Version of record Link to publication record in King's Research Portal Citation for published version (APA): Taylor, M. J., Rudkin, L., Bullemor-Day, P., Lubin, J., Chukwujekwu, C., & Hawton, K. (2013). Strategies for managing sexual dysfunction induced by antidepressant medication. Cochrane Database of Systematic Reviews, (5). https://doi.org/10.1002/14651858.CD003382.pub3 Citing this paper Please note that where the full-text provided on King's Research Portal is the Author Accepted Manuscript or Post-Print version this may differ from the final Published version. If citing, it is advised that you check and use the publisher's definitive version for pagination, volume/issue, and date of publication details. And where the final published version is provided on the Research Portal, if citing you are again advised to check the publisher's website for any subsequent corrections. General rights Copyright and moral rights for the publications made accessible in the Research Portal are retained by the authors and/or other copyright owners and it is a condition of accessing publications that users recognize and abide by the legal requirements associated with these rights. •Users may download and print one copy of any publication from the Research Portal for the purpose of private study or research. •You may not further distribute the material or use it for any profit-making activity or commercial gain •You may freely distribute the URL identifying the publication in the Research Portal Take down policy If you believe that this document breaches copyright please contact [email protected] providing details, and we will remove access to the work immediately and investigate your claim. -
The In¯Uence of Medication on Erectile Function
International Journal of Impotence Research (1997) 9, 17±26 ß 1997 Stockton Press All rights reserved 0955-9930/97 $12.00 The in¯uence of medication on erectile function W Meinhardt1, RF Kropman2, P Vermeij3, AAB Lycklama aÁ Nijeholt4 and J Zwartendijk4 1Department of Urology, Netherlands Cancer Institute/Antoni van Leeuwenhoek Hospital, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands; 2Department of Urology, Leyenburg Hospital, Leyweg 275, 2545 CH The Hague, The Netherlands; 3Pharmacy; and 4Department of Urology, Leiden University Hospital, P.O. Box 9600, 2300 RC Leiden, The Netherlands Keywords: impotence; side-effect; antipsychotic; antihypertensive; physiology; erectile function Introduction stopped their antihypertensive treatment over a ®ve year period, because of side-effects on sexual function.5 In the drug registration procedures sexual Several physiological mechanisms are involved in function is not a major issue. This means that erectile function. A negative in¯uence of prescrip- knowledge of the problem is mainly dependent on tion-drugs on these mechanisms will not always case reports and the lists from side effect registries.6±8 come to the attention of the clinician, whereas a Another way of looking at the problem is drug causing priapism will rarely escape the atten- combining available data on mechanisms of action tion. of drugs with the knowledge of the physiological When erectile function is in¯uenced in a negative mechanisms involved in erectile function. The way compensation may occur. For example, age- advantage of this approach is that remedies may related penile sensory disorders may be compen- evolve from it. sated for by extra stimulation.1 Diminished in¯ux of In this paper we will discuss the subject in the blood will lead to a slower onset of the erection, but following order: may be accepted. -
Download Download
J. Pharm. Tech. Res. Management Vol. 8, No. 1 (2020), pp.39–46 Vol. 7 | No. 2 | Nov 2019 Journal of Pharmaceutical Technology Research and Management Journal homepage: https://jptrm.chitkara.edu.in/ Ranitidine Induced Hepatotoxicity: A Review Amit Bandyopadhyay Banerjee1, Manisha Gupta2, Thakur Gurjeet Singh3, Sandeep Arora4 and Onkar Bedi5* Chitkara College of Pharmacy, Chitkara University, Punjab-140401, India [email protected] [email protected] [email protected] [email protected] 5*[email protected] (Corresponding Author) ARTICLE INFORMATION ABSTRACT Received: January 29, 2020 Background: Ranitidine (RAN) is one of the common drugs associated with idiosyncratic Revised: April 08, 2020 adverse drug reactions (IADRs) in humans. It was found to be associated with severe adverse drug Accepted: April 28, 2020 reactions due to the presence of contaminants such as N-Nitrosodimethylamine (NDMA) which Published Online: May 20, 2020 is claimed to be carcinogenic. As a consequence, on April 1, 2020, United States Food and Drug Keywords: Administration (USFDA) had decided to call off all the RAN products from the market. The exact DILI, Ranitidine withdrawal, RAN induced cause of RAN associated idiosyncratic hepatotoxicity is not clear yet. hepatotoxicity Purpose: To summarize and analyze the reason behind the withdrawal of RAN products from the market and whether ranitidine will be available again in future or will FDA withdraw approvals of ranitidine National Drug Authority (NDA) and an abbreviated new drug application (ANDA)? Methods: We performed a systematic PubMed/MEDLINE search of studies investigating the reason behind the withdrawal of RAN products and explored the possible mechanism associated with RAN induced hepatotoxicity. -
Potentiation of the Mydriatic Effect of Norepinephrine in the Rabbit After
Reports Potentiation of the mydriatic effect of change.7 After topical application of the mono- norepinephrine in the rabbit after amine releaser Ro 4-1284 to the eyes of rabbits monoamine oxidase inhibition. BRENDA K. pretreated with these MAO inhibitors, however, COLASANTI AND ERNST H. BARANY. pupillary dilation ensued. As in the case of re- sponses of other peripheral tissues, the response Dose-response curves of pupillary dilation after topical of the iris to indirectly acting sympathomimetic administration of norepinephrine or methoxamine have agents has been shown to be potentiated in hu- been determined in rabbits after chronic inhibition of man subjects undergoing treatment with MAO in- ocular monoamine oxidase by treatment with pargyline hibitors.8 or pheniprazine. Eyes treated with either monoamine ox- In the present communication, we report a idase inhibitor showed an enhanced responsiveness to potentiation of the mydriatic response of the rab- the mydriatic effect of norepinephrine given either topi- bit eye to norepinephrine after prior treatment cally or intravenously. Increments in pupil size of the with MAO inhibitors. This increase in sensitivity treated and control eyes in response to methoxamine applied topically, on the other hand, were the same. of the iris contrasts with the unaltered responses of These results suggest that monoamine oxidase may play a other peripheral organs and tissues to directly act- 2 role in the iris as one factor influencing the concentration ing catecholamines after MAO inhibition. of norepinephrine at the receptors. Methods. Adult male albino rabbits weighing 2 to 3 kg were used in these experiments. Pheni- The principal mechanism for physiological inac- prazine (Draco, Lund and Merrell—National tivation of norepinephrine released from adren- Laboratories, Ohio) was applied topically by mi- ergic nerve endings for action on autonomic effec- crodrop to the right eyes of three groups of six tor organs involves reuptake into the prejunctional rabbits once daily for 7 days. -
Long-Lasting Analgesic Effect of the Psychedelic Drug Changa: a Case Report
CASE REPORT Journal of Psychedelic Studies 3(1), pp. 7–13 (2019) DOI: 10.1556/2054.2019.001 First published online February 12, 2019 Long-lasting analgesic effect of the psychedelic drug changa: A case report GENÍS ONA1* and SEBASTIÁN TRONCOSO2 1Department of Anthropology, Philosophy and Social Work, Universitat Rovira i Virgili, Tarragona, Spain 2Independent Researcher (Received: August 23, 2018; accepted: January 8, 2019) Background and aims: Pain is the most prevalent symptom of a health condition, and it is inappropriately treated in many cases. Here, we present a case report in which we observe a long-lasting analgesic effect produced by changa,a psychedelic drug that contains the psychoactive N,N-dimethyltryptamine and ground seeds of Peganum harmala, which are rich in β-carbolines. Methods: We describe the case and offer a brief review of supportive findings. Results: A long-lasting analgesic effect after the use of changa was reported. Possible analgesic mechanisms are discussed. We suggest that both pharmacological and non-pharmacological factors could be involved. Conclusion: These findings offer preliminary evidence of the analgesic effect of changa, but due to its complex pharmacological actions, involving many neurotransmitter systems, further research is needed in order to establish the specific mechanisms at work. Keywords: analgesic, pain, psychedelic, psychoactive, DMT, β-carboline alkaloids INTRODUCTION effects of ayahuasca usually last between 3 and 5 hr (McKenna & Riba, 2015), but the effects of smoked changa – The treatment of pain is one of the most significant chal- last about 15 30 min (Ott, 1994). lenges in the history of medicine. At present, there are still many challenges that hamper pain’s appropriate treatment, as recently stated by American Pain Society (Gereau et al., CASE DESCRIPTION 2014). -
FROM MELANCHOLIA to DEPRESSION a HISTORY of DIAGNOSIS and TREATMENT Thomas A
1 FROM MELANCHOLIA TO DEPRESSION A HISTORY OF DIAGNOSIS AND TREATMENT Thomas A. Ban International Network for the History of Neuropsychopharmacology 2014 2 From Melancholia to Depression A History of Diagnosis and Treatment1 TABLE OF CONTENTS Introduction 2 Diagnosis and classifications of melancholia and depression 7 From Galen to Robert Burton 7 From Boissier de Sauvages to Karl Kahlbaum 8 From Emil Kraepelin to Karl Leonhard 12 From Adolf Meyer to the DSM-IV 17 Treatment of melancholia and depression 20 From opium to chlorpromazine 21 Monoamine Oxidase Inhibitors 22 Monoamine Re-uptake Inhibitors 24 Antidepressants in clinical use 26 Clinical psychopharmacology of antidepressants 30 Composite Diagnostic Evaluation of Depressive Disorders 32 The CODE System 32 CODE –DD 33 Genetics, neuropsychopharmacology and CODE-DD 36 Conclusions 37 References 37 INTRODUCTION Descriptions of what we now call melancholia or depression can be found in many ancient documents including The Old Testament, The Book of Job, and Homer's Iliad, but there is virtually 1 The text of this E-Book was prepared in 2002 for a presentation in Mexico City. The manuscript was not updated. 3 no reliable information on the frequency of “melancholia” until the mid-20th century (Kaplan and Saddock 1988). Between 1938 and 1955 several reports indicated that the prevalence of depression in the general population was below 1%. Comparing these figures, as shown in table 1, with figures in the 1960s and ‘70s reveals that even the lowest figures in the psychopharmacological era (from the 1960s) are 7 to 10 times greater than the highest figures before the introduction of antidepressant drugs (Silverman 1968). -
Phenelzine in the Treatment of Depressive Illness
Hull & East Riding Prescribing Committee Prescribing Framework for Phenelzine in the treatment of depressive illness Patients Name:…………………………………………………..… NHS Number: ……………… Patients Address:……………………………………………...……(Use addressograph sticker) GP’s Name:……………………………………………………….…….. Communication We agree to treat this patient within this Prescribing Framework Specialist Prescriber’s Name………………………………………… Prof Reg. No. ………… Specialist Prescriber’s Signature…………………………………… Date:……………………. Where prescriber is not a consultant: Consultant’s Name: ………………………………………………… GMC No ……………….. Consultant’s Signature ………………………….... ………………. Date:……………………. GP’s Signature:………………………………………………………… Date:…………………….. GP’s Name (if different from listed above)………………………….. The front page of this form should be completed by the specialist and the form sent to the patient’s general practitioner. The patient’s GP should sign and send back to specialist, to confirm agreement to enter into shared care arrangement. If the General Practitioner is unwilling to accept prescribing responsibility for the above patient the specialist should be informed within two weeks of receipt of this framework and specialist’s letter. Full copy of framework can also be found at : http://www.hey.nhs.uk/amber.htm Prescribing framework for Phenelzine Date approved by HERPC : March 2021 Review date: April 2024 Page 1 of 7 APPROVAL PROCESS Written by: Jackie Stark, Principal Pharmacist HFT Wendy Tucker, Pharmacist Reviewed by Karen Thompson , Specialist Pharmacist May 2017 Reviewed by Wendy Storey Feb -
Insights Into the Mechanisms of Action Ofthe MAO Inhibitors Phenelzine and Tranylcypromine
Insights into the Mechanisms of Action of the MAO Inhibitors Phenelzine and Tranylcypromine: A Review Glen B. Baker, Ph.D., Ronald T. Coutts, Ph.D., D.Sc., Kevin F. McKenna, M.D., and Rhonda L. Sherry-McKenna, B.Sc. Neurochemical Research Unit, Department of Psychiatry and Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta Submitted: July 10, 1992 Accepted: October 7, 1992 Although the non-selective monoamine oxidase inhibitors phenelzine and tranylcypromine have been used for many years, much still remains to be understood about their mechanisms of action. Other factors, in addition to the inhibition of monoamine oxidase and the subsequent elevation of brain levels of the catecholamines and 5-hydroxytryptamine, may contribute to the overall pharma- cological profiles ofthese drugs. This review also considers the effects on brain levels of amino acids and trace amines, uptake and release of neurotransmitter amines at nerve terminals, receptors for amino acids and amines, and enzymes other than monoamine oxidase, including enzymes involved in metabolism of other drugs. The possible contributions of metabolism and stereochemistry to the actions of these monoamine oxidase inhibitors are discussed. Key Words: amino acids, monoamine oxidase, neurotransmitter amines, phenelzine, tranylcypromine, uptake Despite the fact that the non-selective monoamine oxidase nerve endings (Baker et al 1977; Raiteri et al 1977) and/or (MAO) inhibitors phenelzine (PLZ) and tranylcypromine may act as neuromodulators through direct actions on recep- (TCP) (see Fig. 1) have been used clinically for many years, tors for the catecholamines and/or 5-HT (Jones 1983; much remains to be learned about theirmechanisms ofaction. -
Les Femmes Peuvent Prendre Du Viagra * Achat De Viagra En
Viagra est indiquée pour le traitement de la dysfonction érectile masculine. >>> ORDER NOW <<< Les femmes peuvent prendre du viagra Tags: cialis ou viagra acheter vrai ou faux viagra risques avec viagra acheter du viagra sans ordonnance en suisse danger du faux viagra comment bien prendre viagra le prix du viagra en pharmacie au maroc les effets indesirable du viagra que ce que viagra de gaulle contre le viagra achat viagra internet doctissimo commande viagra belgique peut on avoir du viagra en pharmacie sans ordonnance comment prendre sildenafil pfizer nitrates and viagra interaction ordonnance ou pas pour viagra notice demballage viagran quels sont les effets du viagra quelle quantité de viagra prendre peut on acheter viagra en pharmacie sans ordonnance comment avoir le viagra site sur achat viagra nitrates viagra can deadly combination Recession quest ce qui peut remplacer le viagra review am astonishingly forgetful. Some things said caffeine was fine to consume (in drinks, food, etc) while on the med, others said caffeine decreased the effects of the med. Features of this disorder include dysphonia, dysarthria, and loss of pain and temperature over the ipsilateral face and contralateral body. Jeg vil også erklære, at du forlader soap ud. If you feel very bored when waiting for something or someone (a bus, your friend, your kids), distract yourself with a book, magazine, or crossword puzzle. The celexa is longer acting and must build in the system over time in order to work for anxiety. Medscape is the leading online destination for healthcare professionals seeking clinical information. Paxil over time increased my appetite but i think that is because les femmes peuvent prendre du viagra made me tired and lethargic, they did not increase appetite, in fact in the first few months they curbed it right down. -
(12) Patent Application Publication (10) Pub. No.: US 2011/0136742 A1 Mickle Et Al
US 20110136742A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2011/0136742 A1 Mickle et al. (43) Pub. Date: Jun. 9, 2011 (54) ANTIDEPRESSANT PRODRUGS A 6LX 3/5.375 (2006.01) A 6LX 3/553 (2006.01) (76) Inventors: Travis Mickle, Coralville, IA (US); A6II 3/42 (2006.01) Wendy Hirschelman Severs, A6II 3/44 (2006.01) Blacksburg, VA (US) A6II 3/42 (2006.01) A6II 3/405 (2006.01) (21) Appl. No.: 12/280,190 A63L/36 (2006.01) A63/4985 (2006.01) (22) PCT Fled: Feb. 22, 2007 A6II 3/4409 (2006.01) A6II 3/554 (2006.01) A6II 3/405 (2006.01) S371 (c)(1), A6IP 25/24 (2006.01) (2), (4) Date: Sep. 14, 2010 A6IP 25/22 (2006.01) Related U.S. Application Data A6IP 25/18 (2006.01) (52) U.S. Cl. ........ 514/17.6: 514/564: 514/321; 514/217; (60) Provisional application No. 60/776,216, filed on Feb. 514/237.8: 514/211.13: 514/378: 514/354; 24, 2006. 514/376; 514/.424; 514/239.2: 514/.466; 514/250; 514/423: 514/419 Publication Classification (57) ABSTRACT (51) Int. Cl. A6 IK 38/06 (2006.01) The invention provides antidepressant prodrugs comprising A6 IK 38/05 (2006.01) an antidepressant conjugated to one or more amino acids. The A 6LX 3L/95 (2006.01) invention also relates to pharmaceutical compositions com A6 IK 3L/4525 (2006.01) prising an antidepressant prodrug, and to methods of prepar A6 IK3I/55 (2006.01) ing and using the same.