Biochemical Pharmacology Lecture Slides
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Folic Acid Antagonists: Antimicrobial and Immunomodulating Mechanisms and Applications
International Journal of Molecular Sciences Review Folic Acid Antagonists: Antimicrobial and Immunomodulating Mechanisms and Applications Daniel Fernández-Villa 1, Maria Rosa Aguilar 1,2 and Luis Rojo 1,2,* 1 Instituto de Ciencia y Tecnología de Polímeros, Consejo Superior de Investigaciones Científicas, CSIC, 28006 Madrid, Spain; [email protected] (D.F.-V.); [email protected] (M.R.A.) 2 Consorcio Centro de Investigación Biomédica en Red de Bioingeniería, Biomateriales y Nanomedicina, 28029 Madrid, Spain * Correspondence: [email protected]; Tel.: +34-915-622-900 Received: 18 September 2019; Accepted: 7 October 2019; Published: 9 October 2019 Abstract: Bacterial, protozoan and other microbial infections share an accelerated metabolic rate. In order to ensure a proper functioning of cell replication and proteins and nucleic acids synthesis processes, folate metabolism rate is also increased in these cases. For this reason, folic acid antagonists have been used since their discovery to treat different kinds of microbial infections, taking advantage of this metabolic difference when compared with human cells. However, resistances to these compounds have emerged since then and only combined therapies are currently used in clinic. In addition, some of these compounds have been found to have an immunomodulatory behavior that allows clinicians using them as anti-inflammatory or immunosuppressive drugs. Therefore, the aim of this review is to provide an updated state-of-the-art on the use of antifolates as antibacterial and immunomodulating agents in the clinical setting, as well as to present their action mechanisms and currently investigated biomedical applications. Keywords: folic acid antagonists; antifolates; antibiotics; antibacterials; immunomodulation; sulfonamides; antimalarial 1. -
Pro-Oxidizing Metabolic Weapons ☆ ⁎ Etelvino J.H
Comparative Biochemistry and Physiology, Part C 146 (2007) 88–110 www.elsevier.com/locate/cbpc Review The dual face of endogenous α-aminoketones: Pro-oxidizing metabolic weapons ☆ ⁎ Etelvino J.H. Bechara a, , Fernando Dutra b, Vanessa E.S. Cardoso a, Adriano Sartori a, Kelly P.K. Olympio c, Carlos A.A. Penatti d, Avishek Adhikari e, Nilson A. Assunção a a Departamento de Bioquímica, Instituto de Química, Universidade de São Paulo, Av. Prof. Lineu Prestes 748, 05508-900, São Paulo, SP, Brazil b Centro de Ciências Biológicas e da Saúde, Universidade Cruzeiro do Sul, São Paulo, SP, Brazil c Faculdade de Saúde Pública, Universidade de São Paulo, São Paulo, SP, Brazil d Department of Physiology, Dartmouth Medical School, Hanover, NH, USA e Department of Biological Sciences, Columbia University, New York, NY, USA Received 31 January 2006; received in revised form 26 June 2006; accepted 6 July 2006 Available online 14 July 2006 Abstract Amino metabolites with potential prooxidant properties, particularly α-aminocarbonyls, are the focus of this review. Among them we emphasize 5-aminolevulinic acid (a heme precursor formed from succinyl–CoA and glycine), aminoacetone (a threonine and glycine metabolite), and hexosamines and hexosimines, formed by Schiff condensation of hexoses with basic amino acid residues of proteins. All these metabolites were shown, in vitro, to undergo enolization and subsequent aerobic oxidation, yielding oxyradicals and highly cyto- and genotoxic α-oxoaldehydes. Their metabolic roles in health and disease are examined here and compared in humans and experimental animals, including rats, quail, and octopus. In the past two decades, we have concentrated on two endogenous α-aminoketones: (i) 5-aminolevulinic acid (ALA), accumulated in acquired (e.g., lead poisoning) and inborn (e.g., intermittent acute porphyria) porphyric disorders, and (ii) aminoacetone (AA), putatively overproduced in diabetes mellitus and cri-du-chat syndrome. -
2019 National Library of Medicine Classification Schedules
National Library of Medicine Classification 2019 Schedule S-1 QS Human Anatomy Classify here general works on normal human anatomy. Works that treat men, women, or children separately are classed here. • Classify works on anatomy of a part of the body with the part. • Classify works on surgical anatomy in WO 101. • Classify works on artistic anatomy of human or animal in NC 760-783.8. • Classify works on anatomy of animals in QL or SF. QS 1-132 Anatomy QS 504-532 Histology QS 604-681 Embryology Anatomy Note that form numbers are also used under Histology (QS 504-539) and under Embryology (QS 604-681). QS 1 Organizations. Societies (General or not elsewhere classified) (Cutter from name of organization or society) (Table G) (Used for both monographs and serials) Includes membership lists issued serially or separately. Classify directories in QS 22. Classify annual reports, journals, etc., in W1. For academies and institutes, see QS 23-24. QS 4 General works Classify here works on regional anatomy. If written for the surgeon, classify in WO 101 Surgical anatomy. Classify material on comparative anatomy in QS 124. Collected works QS 5 By several authors QS 7 By individual authors QS 9 Addresses. Essays. Lectures QS 11 History (Table G) QS 11.1 General coverage (Not Table G) QS 13 Dictionaries. Encyclopedias QS 15 Classification. Terminology (Used for both monographs and serials) QS 16 Tables. Statistics. Surveys (Table G) (Used for both monographs and serials) QS 16.1 General coverage (Not Table G) (Used for both monographs and serials) QS 17 Atlases. -
NINDS Custom Collection II
ACACETIN ACEBUTOLOL HYDROCHLORIDE ACECLIDINE HYDROCHLORIDE ACEMETACIN ACETAMINOPHEN ACETAMINOSALOL ACETANILIDE ACETARSOL ACETAZOLAMIDE ACETOHYDROXAMIC ACID ACETRIAZOIC ACID ACETYL TYROSINE ETHYL ESTER ACETYLCARNITINE ACETYLCHOLINE ACETYLCYSTEINE ACETYLGLUCOSAMINE ACETYLGLUTAMIC ACID ACETYL-L-LEUCINE ACETYLPHENYLALANINE ACETYLSEROTONIN ACETYLTRYPTOPHAN ACEXAMIC ACID ACIVICIN ACLACINOMYCIN A1 ACONITINE ACRIFLAVINIUM HYDROCHLORIDE ACRISORCIN ACTINONIN ACYCLOVIR ADENOSINE PHOSPHATE ADENOSINE ADRENALINE BITARTRATE AESCULIN AJMALINE AKLAVINE HYDROCHLORIDE ALANYL-dl-LEUCINE ALANYL-dl-PHENYLALANINE ALAPROCLATE ALBENDAZOLE ALBUTEROL ALEXIDINE HYDROCHLORIDE ALLANTOIN ALLOPURINOL ALMOTRIPTAN ALOIN ALPRENOLOL ALTRETAMINE ALVERINE CITRATE AMANTADINE HYDROCHLORIDE AMBROXOL HYDROCHLORIDE AMCINONIDE AMIKACIN SULFATE AMILORIDE HYDROCHLORIDE 3-AMINOBENZAMIDE gamma-AMINOBUTYRIC ACID AMINOCAPROIC ACID N- (2-AMINOETHYL)-4-CHLOROBENZAMIDE (RO-16-6491) AMINOGLUTETHIMIDE AMINOHIPPURIC ACID AMINOHYDROXYBUTYRIC ACID AMINOLEVULINIC ACID HYDROCHLORIDE AMINOPHENAZONE 3-AMINOPROPANESULPHONIC ACID AMINOPYRIDINE 9-AMINO-1,2,3,4-TETRAHYDROACRIDINE HYDROCHLORIDE AMINOTHIAZOLE AMIODARONE HYDROCHLORIDE AMIPRILOSE AMITRIPTYLINE HYDROCHLORIDE AMLODIPINE BESYLATE AMODIAQUINE DIHYDROCHLORIDE AMOXEPINE AMOXICILLIN AMPICILLIN SODIUM AMPROLIUM AMRINONE AMYGDALIN ANABASAMINE HYDROCHLORIDE ANABASINE HYDROCHLORIDE ANCITABINE HYDROCHLORIDE ANDROSTERONE SODIUM SULFATE ANIRACETAM ANISINDIONE ANISODAMINE ANISOMYCIN ANTAZOLINE PHOSPHATE ANTHRALIN ANTIMYCIN A (A1 shown) ANTIPYRINE APHYLLIC -
Antibiotics and Antibacterials, General
B. Sulfamethoxydiazine (Sulfameter, Sulla) IX. TOXICITY AND SIDE EFFECTS: C. Sulfadimethoxine (Madribon) A. Fever D. Sulphormethoxine-Very long-acting; thera- B. Rash, urticaria peutic blood levels for 1 week. C. Cyanosis, methemoglobinemia D. Nausea, vomiting, diarrhea V. POORLY ABSORBED SULFONAMIDES: E. Hepatitis, jaundice for local use in the intestinal tract only. F. Hematuria, albuminuria, crystalluria, toxic A. Succinylsulfathiazole (Sulfasuxidine): nephritis. 1. Dosage-3.0 Gm q 4 h p.o. G. Headache, mental depression, psychosis, 2. Maximum effect usually not achieved un- peripheral neuritis. til 7th day of therapy. H. Leukopenia, agranulocytosis, purpura, aplas- B. Phthalylsulfathiazole (Sulfathalidine): tic anemia, hypoprothrombinemia, hemolytic ane- 1. Dosage-1.5 Gmq4hp.o. mia. 2. Double this dosage in the presence of I. Severe hypersensitivity reactions - anaphy- diarrhea. laxis, periarteritis nodosa and other collagen dis- 3. Effect produced in 5-7 days. eases, Stevens-Johnson syndrome. C. Para-nitrosulfathiazole (Nisulfazole): Used X. only for intrarectal instillation in treatment of PRECAUTIONS: proctitis or non-specific colitis. A. Keep careful record of urine output - try to maintain output of at least 1200-1500 ml/24 VI. TOPICAL SULFONAMIDES: hrs. B. Alkalinization of urine-sodium bicarbonate A. Mafenide (Sulfamylon): Used on skin as (12-15 Gm/day) may be used for this purpose 10% cream. Unlike other sulfonamides, effective when full systemic doses of sulfonamides are used, in presence of pus and necrotic tissue and does not when there is difficulty in being sure of adequate sensitize readily when used topically. Of value in fluid intake and output, and when such adjunctive prevention and therapy of burn infection due to therapy is not contraindicated. -
A Screening-Based Approach to Circumvent Tumor Microenvironment
JBXXXX10.1177/1087057113501081Journal of Biomolecular ScreeningSingh et al. 501081research-article2013 Original Research Journal of Biomolecular Screening 2014, Vol 19(1) 158 –167 A Screening-Based Approach to © 2013 Society for Laboratory Automation and Screening DOI: 10.1177/1087057113501081 Circumvent Tumor Microenvironment- jbx.sagepub.com Driven Intrinsic Resistance to BCR-ABL+ Inhibitors in Ph+ Acute Lymphoblastic Leukemia Harpreet Singh1,2, Anang A. Shelat3, Amandeep Singh4, Nidal Boulos1, Richard T. Williams1,2*, and R. Kiplin Guy2,3 Abstract Signaling by the BCR-ABL fusion kinase drives Philadelphia chromosome–positive acute lymphoblastic leukemia (Ph+ ALL) and chronic myelogenous leukemia (CML). Despite their clinical activity in many patients with CML, the BCR-ABL kinase inhibitors (BCR-ABL-KIs) imatinib, dasatinib, and nilotinib provide only transient leukemia reduction in patients with Ph+ ALL. While host-derived growth factors in the leukemia microenvironment have been invoked to explain this drug resistance, their relative contribution remains uncertain. Using genetically defined murine Ph+ ALL cells, we identified interleukin 7 (IL-7) as the dominant host factor that attenuates response to BCR-ABL-KIs. To identify potential combination drugs that could overcome this IL-7–dependent BCR-ABL-KI–resistant phenotype, we screened a small-molecule library including Food and Drug Administration–approved drugs. Among the validated hits, the well-tolerated antimalarial drug dihydroartemisinin (DHA) displayed potent activity in vitro and modest in vivo monotherapy activity against engineered murine BCR-ABL-KI–resistant Ph+ ALL. Strikingly, cotreatment with DHA and dasatinib in vivo strongly reduced primary leukemia burden and improved long-term survival in a murine model that faithfully captures the BCR-ABL-KI–resistant phenotype of human Ph+ ALL. -
Title 16. Crimes and Offenses Chapter 13. Controlled Substances Article 1
TITLE 16. CRIMES AND OFFENSES CHAPTER 13. CONTROLLED SUBSTANCES ARTICLE 1. GENERAL PROVISIONS § 16-13-1. Drug related objects (a) As used in this Code section, the term: (1) "Controlled substance" shall have the same meaning as defined in Article 2 of this chapter, relating to controlled substances. For the purposes of this Code section, the term "controlled substance" shall include marijuana as defined by paragraph (16) of Code Section 16-13-21. (2) "Dangerous drug" shall have the same meaning as defined in Article 3 of this chapter, relating to dangerous drugs. (3) "Drug related object" means any machine, instrument, tool, equipment, contrivance, or device which an average person would reasonably conclude is intended to be used for one or more of the following purposes: (A) To introduce into the human body any dangerous drug or controlled substance under circumstances in violation of the laws of this state; (B) To enhance the effect on the human body of any dangerous drug or controlled substance under circumstances in violation of the laws of this state; (C) To conceal any quantity of any dangerous drug or controlled substance under circumstances in violation of the laws of this state; or (D) To test the strength, effectiveness, or purity of any dangerous drug or controlled substance under circumstances in violation of the laws of this state. (4) "Knowingly" means having general knowledge that a machine, instrument, tool, item of equipment, contrivance, or device is a drug related object or having reasonable grounds to believe that any such object is or may, to an average person, appear to be a drug related object. -
AMEG Categorisation of Antibiotics
12 December 2019 EMA/CVMP/CHMP/682198/2017 Committee for Medicinal Products for Veterinary use (CVMP) Committee for Medicinal Products for Human Use (CHMP) Categorisation of antibiotics in the European Union Answer to the request from the European Commission for updating the scientific advice on the impact on public health and animal health of the use of antibiotics in animals Agreed by the Antimicrobial Advice ad hoc Expert Group (AMEG) 29 October 2018 Adopted by the CVMP for release for consultation 24 January 2019 Adopted by the CHMP for release for consultation 31 January 2019 Start of public consultation 5 February 2019 End of consultation (deadline for comments) 30 April 2019 Agreed by the Antimicrobial Advice ad hoc Expert Group (AMEG) 19 November 2019 Adopted by the CVMP 5 December 2019 Adopted by the CHMP 12 December 2019 Official address Domenico Scarlattilaan 6 ● 1083 HS Amsterdam ● The Netherlands Address for visits and deliveries Refer to www.ema.europa.eu/how-to-find-us Send us a question Go to www.ema.europa.eu/contact Telephone +31 (0)88 781 6000 An agency of the European Union © European Medicines Agency, 2020. Reproduction is authorised provided the source is acknowledged. Categorisation of antibiotics in the European Union Table of Contents 1. Summary assessment and recommendations .......................................... 3 2. Introduction ............................................................................................ 7 2.1. Background ........................................................................................................ -
WSAVA List of Essential Medicines for Cats and Dogs
The World Small Animal Veterinary Association (WSAVA) List of Essential Medicines for Cats and Dogs Version 1; January 20th, 2020 Members of the WSAVA Therapeutic Guidelines Group (TGG) Steagall PV, Pelligand L, Page SW, Bourgeois M, Weese S, Manigot G, Dublin D, Ferreira JP, Guardabassi L © 2020 WSAVA All Rights Reserved Contents Background ................................................................................................................................... 2 Definition ...................................................................................................................................... 2 Using the List of Essential Medicines ............................................................................................ 2 Criteria for selection of essential medicines ................................................................................. 3 Anaesthetic, analgesic, sedative and emergency drugs ............................................................... 4 Antimicrobial drugs ....................................................................................................................... 7 Antibacterial and antiprotozoal drugs ....................................................................................... 7 Systemic administration ........................................................................................................ 7 Topical administration ........................................................................................................... 9 Antifungal drugs ..................................................................................................................... -
Antiprotozoal and Antitumor Activity of Natural Polycyclic Endoperoxides: Origin, Structures and Biological Activity
molecules Review Antiprotozoal and Antitumor Activity of Natural Polycyclic Endoperoxides: Origin, Structures and Biological Activity Valery M. Dembitsky 1,2,*, Ekaterina Ermolenko 2, Nick Savidov 1, Tatyana A. Gloriozova 3 and Vladimir V. Poroikov 3 1 Centre for Applied Research, Innovation and Entrepreneurship, Lethbridge College, 3000 College Drive South, Lethbridge, AB T1K 1L6, Canada; [email protected] 2 A.V. Zhirmunsky National Scientific Center of Marine Biology, 17 Palchevsky Str., 690041 Vladivostok, Russia; [email protected] 3 Institute of Biomedical Chemistry, 10 Pogodinskaya Str., 119121 Moscow, Russia; [email protected] (T.A.G.); [email protected] (V.V.P.) * Correspondence: [email protected]; Tel.: +1-403-320-3202 (ext. 5463); Fax: +1-888-858-8517 Abstract: Polycyclic endoperoxides are rare natural metabolites found and isolated in plants, fungi, and marine invertebrates. The purpose of this review is a comparative analysis of the pharmacological potential of these natural products. According to PASS (Prediction of Activity Spectra for Substances) estimates, they are more likely to exhibit antiprotozoal and antitumor properties. Some of them are now widely used in clinical medicine. All polycyclic endoperoxides presented in this article demonstrate antiprotozoal activity and can be divided into three groups. The third group includes endoperoxides, which show weak antiprotozoal activity with a reliability of up to 70%, and this group includes only 1.1% of metabolites. The second group includes the largest number of endoperoxides, Citation: Dembitsky, V.M.; which are 65% and show average antiprotozoal activity with a confidence level of 70 to 90%. Lastly, Ermolenko, E.; Savidov, N.; the third group includes endoperoxides, which are 33.9% and show strong antiprotozoal activity with Gloriozova, T.A.; Poroikov, V.V. -
Tuberculosis Medicines Technology and Market Landscape
2014 Tuberculosis Medicines Technology and Market Landscape OCTOBER 2014 2014 Tuberculosis Medicines Technology and Market Landscape UNITAID Secretariat World Health Organization Avenue Appia 20 CH-1211 Geneva 27 Switzerland T +41 22 791 55 03 F +41 22 791 48 90 [email protected] www.unitaid.org UNITAID is hosted and administered by the World Health Organization © 2014 World Health Organization (acting as the host organization for the Secretariat of UNITAID) The designations employed and the presentation of the material in this publication do not imply the expression of any opinion whatsoever on the part of the World Health Organization concerning the legal status of any country, territory, city or area or of its authorities, or concerning the delimitation of its frontiers or boundaries. The mention of specific companies or of certain manufacturers’ products does not imply that they are endorsed or recommended by the World Health Organization in preference to others of a similar nature that are not mentioned. All reasonable precautions have been taken by the World Health Organization to verify the information contained in this publication. However, the published material is being distributed without warranty of any kind either expressed or implied. The responsibility and use of the material lies with the reader. In no event shall the World Health Organization be liable for damages arising from its use. Overall coordination of this report was undertaken by Janet Ginnard. Components of this report were prepared by Patrick Aylward, Philippa Crompton, Colleen Daniels, Janet Ginnard, Erica Lessem and Megan Paterson with support from UNITAID. All reasonable precautions have been taken by the authors to verify the information contained in this publication. -
Insights of Taste Masking from Molecular Interactions and Microstructures of Microspheres
Insights of Taste Masking from Molecular Interactions and Microstructures of Microspheres Item Type Thesis Authors Guo, Zhen Publisher University of Bradford Rights <a rel="license" href="http://creativecommons.org/licenses/ by-nc-nd/3.0/"><img alt="Creative Commons License" style="border-width:0" src="http://i.creativecommons.org/l/by- nc-nd/3.0/88x31.png" /></a><br />The University of Bradford theses are licenced under a <a rel="license" href="http:// creativecommons.org/licenses/by-nc-nd/3.0/">Creative Commons Licence</a>. Download date 17/11/2019 12:36:58 Link to Item http://hdl.handle.net/10454/17420 Insights of Taste Masking from Molecular Interactions and Microstructure of Microspheres Zhen Guo Submitted for the Degree of Doctor of Philosophy Institute of Cancer Therapeutics, Faculty of Life Sciences, University of Bradford 2017 Abstract Zhen Guo Insights of Taste Masking from Molecular Interactions and Microstructures of Microspheres Keywords: Taste Masking, Cyclodextrin, Lipid Microspheres, Kinetics, Synchrotron Radiation, Surface Plasmon Resonance Imaging, High Performance Affinity Chromatography The effects of taste masking are determined by interactions between drug and excipients as well as the microstructures of the particulate drug delivery systems (DDS). Cyclodextrin (CD) is a widely used taste masking agent, to which the relationship between kinetic parameters (Ka and Kd) of a drug and taste masking remains unexplored, which is investigated for the first time in this study. A data base of the kinetic parameters for drug-CD was established by Surface Plasmon Resonance Imaging (SPRi) and High Performance Affinity Chromatography (HPAC). Combined with the electronic tongue, Ka and Kd based models for the taste masking effect of HP-β-CD were successfully established and applied to the prediction of taste masking effects.