PRIMAXIN (Imipenem and Cilastatin)
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Oral Presentations September 23Rd - Rooms 1,2 and 3
Oral Presentations September 23rd - Rooms 1,2 and 3 Presentation Date Abstract Authors Presenter´s name - Theme Title Code indicated by the author 18498 Thomas Smits; Femke Gresnigt; Thomas Smits Clinical Toxicology/drugs of PERFORMANCE OF AN IMMUNOASSAY Eric Franssen; Milly Attema-de abuse METHOD FOR GAMMA-HYDROXYBUTYRIC Jonge ACID (GHB) IN PATIENTS PRESENTED AT THE EMERGENCY DEPARTMENT, A PROSPECTIVE STUDY 18499 Thomas Smits; Femke Gresnigt; Thomas Smits Clinical Toxicology/drugs of DO WE NEED POINT-OF-CARE TESTING OF Milly Attema-de Jonge; Eric abuse GAMMA-HYDROXYBUTYRIC ACID (GHB) AT Fransse THE EMERGENCY DEPARTMENT? September 23 18730 Lilian H.J. Richter; Julia Menges; Lea Wagmann Clinical Toxicology/drugs of NEW PSYCHOACTIVE SUBSTANCES: Lea Wagmann; Simon D. Brandt; abuse METABOLIC FATE, ISOZYME-MAPPING, 13:30 - 14:45 Folker Westphal; Veit Flockerzi; AND PLASMA PROTEIN BINDING OF 5-APB- ROOM 1 Markus R. Meyer NBOME, 2C-B-FLY-NB2ETO5CL, AND 2C-B- FLY-NBOME 18985 Annelies Cannaert; Marie Annelies Cannaert Clinical Toxicology/drugs of HIDE AND SEEK: OVERCOMING THE Deventer; Melissa Fogarty; abuse MASKING EFFECT OF OPIOID Amanda L.A. Mohr; Christophe P. ANTAGONISTS IN ACTIVITY-BASED Stove SCREENING TESTS 18740 Souleiman El Balkhi ; Roland Souleiman El Balkhi Clinical Toxicology/drugs of METABOLIC INTERACTIONS BETWEEN Lawson; Franck Saint-Marcoux abuse OXYCODONE, BENZODIAZEPINES OR DESIGNER BENZODIAZEPINES PLAY AN IMPORTANT ROLE IN OXYCODONE INTOXICATIONS 19050 Brenda de Winter F de Velde; MN Brenda de Winter Anti-infective drugs POPULATION -
Critical Access COVID-19 Drugs Shortages (156-40)
Resilient Drug Supply Project: Critical Acute Drug List & Critical COVID-19 Drug List Drug Shortages Reported by ASHP & FDA Shortages as of 8/22/2021 UMN RDSP UMN RDSP ASHP FDA Drug Critical Acute Drugs Drug Category List of 156 List of 40 Drug Drug # Generic Name Critical Acute Critical Shortage Shortage Drugs COVID-19 List List Drugs 1 Cisatracurium Paralytic X X Yes 2 Rocuronium Paralytic X X Yes 3 Vecuronium Paralytic X X Yes Yes 4 Succinylcholine Paralytic X X 5 Atracurium Paralytic X 6 Propofol Sedation X X Yes Yes 7 Midazolam Sedation X X Yes Yes 8 Lorazepam Sedation X X Yes Yes 9 Dexmedetomidine Sedation/Anesthesia X X Yes Yes 10 Phenobarbital Sedation X 11 Ketamine Sedation/Anesthesia X X Yes Yes 12 Diazepam Sedation X 13 Lidocaine Local Anesthetic X Yes Yes 14 Bupivacaine Local Anesthetic X Yes Yes 15 Fentanyl Pain X X Yes Yes 16 Hydromorphone Pain X X Yes Yes 17 Morphine Pain X X Yes Yes 18 Oxycodone Pain X X 19 Acetaminophen Pain & Fever X 20 Ketorolac Pain X Yes Yes 21 Anakinra Pain X 22 Oxygen Medical Gas X X 23 Nitric Oxide Medical Gas X 24 Sevoflurane Medical Gas X 25 Albuterol Bronchodilator X X Yes 26 Ipratropium (Inhaler) Bronchodilator X 27 Azithromycin Anti-infective X X 28 Piperacillin-Tazobactam Anti-infective X X 29 Cefepime Anti-infective X X Yes 30 Ceftriaxone Anti-infective X 31 Vancomycin Anti-infective X X Yes 32 Doxycycline Anti-infective X 33 Meropenem Anti-infective X X 34 Cefazolin Anti-infective X X Yes Yes 35 Levofloxacin Anti-infective X 36 Linezolid Anti-infective X 37 Ampicillin-Sulbactam Anti-infective -
In Vitro and in Vivo Study of Fosfomycin in Methicillin-Resistant Staphylococcus Aureus Septicaemia
J. Ilyg., Camb. (1980), 96, 419-423 419 Printed in Great Britain In vitro and in vivo study of fosfomycin in methicillin-resistant Staphylococcus aureus septicaemia BY W. Y. LAU, C. H. TEOH-CHAN,* S. T. FAN AND K. F. LAU* Government Surgical Unit, Queen Mary Hospital, and * Department of Microbiology, University of Hong Kong {Received 15 October 19S5; accepted 12 December 19S5) SUMMARY Five hundred strains of methicillin-resistant Staphylococcus aureus were tested against various anti-staphylococcal agents. Vancomycin, fusidic acid and fosfo- mycin were found to be the most effective. Only 1 strain out of 500 was resistant to fosfomycin. Three patients with methicillin-resistant Staphylococcus aureus septicaemia were successfully treated by fosfomycin. We conclude that fosfomycin could be the drug of choice for methicillin-resistant Staphylococcns aureus infection. INTRODUCTION Outbreaks of methicillin-resistant Staphylococcus aureus (MRSA) infection are causing increasing problems in centres all over the world (Thompson & Wenzel, 1982; Editorial, 1983). There has been a gradual increase in the incidence of MRSA in our hospital in Hong Kong from 317 in 1982 (18-7% of all S. aureus isolated) to 511 in 1983 (32-7%) and 833 in 1984 (34-9%). In vitro, resistance of MRSA is often demonstrated to many anti-staphylococcal agents including the penicillins, first-generation cephalosporins, aminoglycosides, erythromycin, clindamycin and chloramphenicol (Peacock et al. 1981). Second- and third-generation cephalosporins also have poor activity in vitro (Thompson, Fisher & Wenzel, 1982) though many MRSA strains have been found to be susceptible to rifampicin, trimethoprim- sulphamethoxazole and fusidic acid (Watanakunakorn, 1983). However, clinical experience of treating serious staphylococeal infection with rifampicin and trimethoprim-siilphamethoxazole is limited (Guenther & Wenzel, 1984) and fully resistant organisms may emerge rapidly after exposure to fusidic acid in vitro and in vivo (Watanakunakorn, 1983). -
Opposing Effects of Dehydroepiandrosterone And
European Journal of Endocrinology (2000) 143 687±695 ISSN 0804-4643 EXPERIMENTAL STUDY Opposing effects of dehydroepiandrosterone and dexamethasone on the generation of monocyte-derived dendritic cells M O Canning, K Grotenhuis, H J de Wit and H A Drexhage Department of Immunology, Erasmus University Rotterdam, The Netherlands (Correspondence should be addressed to H A Drexhage, Lab Ee 838, Department of Immunology, Erasmus University, PO Box 1738, 3000 DR Rotterdam, The Netherlands; Email: [email protected]) Abstract Background: Dehydroepiandrosterone (DHEA) has been suggested as an immunostimulating steroid hormone, of which the effects on the development of dendritic cells (DC) are unknown. The effects of DHEA often oppose those of the other adrenal glucocorticoid, cortisol. Glucocorticoids (GC) are known to suppress the immune response at different levels and have recently been shown to modulate the development of DC, thereby influencing the initiation of the immune response. Variations in the duration of exposure to, and doses of, GC (particularly dexamethasone (DEX)) however, have resulted in conflicting effects on DC development. Aim: In this study, we describe the effects of a continuous high level of exposure to the adrenal steroid DHEA (1026 M) on the generation of immature DC from monocytes, as well as the effects of the opposing steroid DEX on this development. Results: The continuous presence of DHEA (1026 M) in GM-CSF/IL-4-induced monocyte-derived DC cultures resulted in immature DC with a morphology and functional capabilities similar to those of typical immature DC (T cell stimulation, IL-12/IL-10 production), but with a slightly altered phenotype of increased CD80 and decreased CD43 expression (markers of maturity). -
Investigating the Inhibition Mechanism of L,D-Transpeptidase 5 from Mycobacterium Tuberculosis Using Computational Methods
INVESTIGATING THE INHIBITION MECHANISM OF L,D-TRANSPEPTIDASE 5 FROM MYCOBACTERIUM TUBERCULOSIS USING COMPUTATIONAL METHODS BY: GIDEON FEMI TOLUFASHE 216076453 Submitted in fulfilment of the requirements for the degree of Doctor of Philosophy in Pharmaceutical Chemistry School of Health Sciences, College of Health Sciences, University of KwaZulu-Natal, Durban, South Africa. 2018 PREFACE The work described in this thesis was conducted at the Catalysis and Peptide Research Unit, Westville Campus, University of KwaZulu-Natal, Durban, South Africa, under the supervision of Dr Bahareh Honarparvar, Prof. H.G. Kruger and Dr G.E.M. Maguire. This work has not been submitted in any form for any degree or diploma to any institution, where use has been made of the work of others, it is duly acknowledged in the text. Supervisors: Dr B. Honarparvar Date 30/10/2018 Prof. H. G. Kruger________________ Date ___________ Dr. G.E.M Maguire_______________ Date ___________ As candidate’s supervisor I agree to the submission of this thesis. i DECLARATION DECLARATION I- PLAGIARISM I, Gideon Femi Tolufashe declare that (i). The research reports in this thesis, except where otherwise indicated, is my original work. (ii). This thesis has not been submitted for any degree or examination at any other university. (iii). This thesis does not contain other person’s data, pictures, graphs or other information, unless specifically acknowledged as being sourced from other persons. (iv). This thesis does not contain other person’s writing, unless specifically acknowledged as being sourced from other researchers. Where other written sources have been quoted, then: a. Their words have been re-written, but the general information attributed to them has been referenced. -
Tufts Health Unify 202 0 List of Covered Drugs (Formulary)
Tufts Health Unify 202 0 List of Covered Drugs (Formulary) Effective: 12/01/2020 Tufts Health Plan P.O. Box 9194 Watertown, MA 02471-9194 Phone: 855.393.3154 Seven days a week, from 8 a.m. to 8 p.m. TuftsHealthUnify.org Formulary ID: 20533 Version: 20 H7419_6507B Approved DISCRIMINATION IS AGAINST THE LAW Tufts Health Plan complies with applicable Federal civil rights laws and does not discriminate on the basis of race, color, national origin, age, disability, or sex. Tufts Health Plan does not exclude people or treat them differently because of race, color, national origin, age, disability, or sex. Tufts Health Plan: . Provides free aids and services to people with disabilities to communicate effectively with us, such as: — Written information in other formats (large print, audio, accessible electronic formats, other formats) . Provides free language services to people whose primary language is not English, such as: — Qualified interpreters — Information written in other languages If you need these services, contact Tufts Health Plan Member Services at 855.393.3154. If you believe that Tufts Health Plan has failed to provide these services or discriminated in another way on the basis of race, color, national origin, age, disability, or sex, you can file a grievance with: Tufts Health Plan Attention: Civil Rights Coordinator, Legal Dept. 705 Mount Auburn St. Watertown, MA 02472 Phone: 888.880.8699 ext. 48000, [TTY number— 711 or 800.439.2370] Fax: 617.972.9048 Email: [email protected] You can file a grievance in person or by mail, fax, or email. If you need help filing a grievance, the Tufts Health Plan Civil Rights Coordinator is available to help you. -
Thienamycin (Imipenem)
1520 THE JOURNAL OF ANTIBIOTICS OCT. 1989 CONVERSION OF OA-6129 B2 INTO OA-6129 B2, a fermentation carbapenem product, (5i?,6^)-6-[(i?)- l -FLUOROETHYL]-7- into optically active 88617, an 8-fluorinated OXO- 3 -[(7V,Ar,Ar-TRIM ETHYL- carbapenem derivative which improved antimicro- CARBAMIMIDOYL)METHYL]THIO- bial activity and dehydropeptidase-I stability. l -AZABICYCLO[3.2.0]HEPT-2-ENE- Treatment of OA-6129B2 sodium salt 1 with 2-CARBOXYLIC ACID (88617)t /7-nitrobenzyl (PNB) bromide or pivaloyloxymethyl chloride in DMFgave /?NB ester 2 or pivaloyl- Takeo Yoshioka, AzumaWatanabe, oxymethyl (POM) ester 3 of OA-6129 B2 (Fig. 1). Noritaka Chida and Yasuo Fukagawa The two hydroxyl groups in the pantoyl moiety of OA-6129B2 were protected by isopropylidena- Central Research Laboratories, tion for differentiation from the C-8 hydroxyl Sanraku Incorporated, 4-9-1 Johnan, Fujisawa 251, Japan group. The protected compound4 or 5 was allowed to (Received for publication May 25, 1989) react with 1.2 equiv of diethylaminosulfur trifluoride (DAST)11} at -68°C in methylene chloride for 10 minutes. After the reaction mixture was diluted with Since the epoch-making discovery of thienamy- methylene chloride and washed with a saturated cin2), a numberof extensive studies have been carried aqueous sodium bicarbonate solution, silica gel out on the development of clinically useful car- column chromatography of the organic layer pro- bapenem compounds. As a result, formimidoyl- vided the desired fluorinated compound 6 or 7 thienamycin (imipenem) has recently been put on having a fluorine atom in the R configuration at C-8 the market as a combination drug (Primaxin)3) in 43 or 49% yield, respectively. -
Block of GABAA Receptor Ion Channel by Penicillin: Electrophysiological and Modeling Insights Toward the Mechanism
Molecular and Cellular Neuroscience 63 (2014) 72–82 Contents lists available at ScienceDirect Molecular and Cellular Neuroscience journal homepage: www.elsevier.com/locate/ymcne Block of GABAA receptor ion channel by penicillin: Electrophysiological and modeling insights toward the mechanism Alexey V. Rossokhin ⁎, Irina N. Sharonova, Julia V. Bukanova, Sergey N. Kolbaev, Vladimir G. Skrebitsky Research Center of Neurology, Russian Academy of Medical Sciences, 105064 Moscow, Russia article info abstract Article history: GABAA receptors (GABAAR) mainly mediate fast inhibitory neurotransmission in the central nervous system. Dif- Received 5 June 2014 ferent classes of modulators target GABAAR properties. Penicillin G (PNG) belongs to the class of noncompetitive Revised 29 September 2014 antagonists blocking the open GABAAR and is a prototype of β-lactam antibiotics. In this study, we combined elec- Accepted 7 October 2014 trophysiological and modeling approaches to investigate the peculiarities of PNG blockade of GABA-activated Available online 8 October 2014 currents recorded from isolated rat Purkinje cells and to predict the PNG binding site. Whole-cell patch-сlamp Keywords: recording and fast application system was used in the electrophysiological experiments. PNG block developed after channel activation and increased with membrane depolarization suggesting that the ligand binds within GABAA receptor Penicillin the open channel pore. PNG blocked stationary component of GABA-activated currents in a concentration- Isolated neurons dependent manner with IC50 value of 1.12 mM at −70 mV. The termination of GABA and PNG co-application Patch clamp was followed by a transient tail current. Protection of the tail current from bicuculline block and dependence Molecular modeling of its kinetic parameters on agonist affinity suggest that PNG acts as a sequential open channel blocker that pre- Monte-Carlo energy minimization vents agonist dissociation while the channel remains blocked. -
Subject Index to Abstracts
003 1-3998/84/1804-429ASO2.00 PEDIATRIC RESEARCH Vol. 18 No. 4, 1984 Copyright 0 1984 International Pediatric Research Foundation, Inc. Prinled in U.S.A. Subject Index to Abstracts Abortion 767 Adenosine 2 15, 389 Aminoglycoside 342, 1140 Arachidonic acid 295, 925, 1125, Absorption, gastrointestinal 7 15 Adenosine deaminase deficiency Aminonucleoside nephrosis 1598 1 139, 1254 Absorption, passive 706 888 Aminophylline 137 1, 1853 Arginine 134 1 Abstinence 140 1 Adenosine triphosphate 839 Aminopyrine 388 Arginine vasopressin 234,235,249 Abuse 24, 28, 37, 105 Adenovirus 542, 1044, 1073, 1133 Ammonia 1 397, 1707 Argininosuccinicaciduria 78 1 Abuse, sexual 1085 Adenylate kinase 1648 Amnesia 825 Argininosuccinate 742, 1 166 Abuse, substance 62 Adipocytes 44 1 Amniotic fluid 229, 618, 779, Arrhythmia 179, 195, 222, 223, Acanthosis 12 17 Adipose tissue 23 1, 69 1 1304, 1535 377,857,9 13, 1796 Accidents 5 1 1, 5 18 Adiposity 673 Amniotic leak, prolonged 1739 Arteriohepatic dysplasia 1642 Accretion 300 Admissions 825 Amoxicillin 8 19 Artery 1753 Acetaldehyde 777 Adolescence 1, 3, 4, 9, 10, 12, 16, Amphotericin 900, 1350, 1369 Artery, carotid 20 1 Acetaminophen 282, 297, 38 1, 19, 22, 24, 25 Ampicillin 11 14, 1147 Artery, mesenteric 372 390 Adrenal 14, 315,405,413,446 Amrinone 175,345 Artery, pulmonary 186, 2 17, 328, Acetylcholine 277 Adrenal hormones 18 Androgen 14,449, 465, 12 17 5 10 Acetyl-CoA 1200 Adrenal medulla 270 Anemia 20, 140, 143, 500, 545, Arthritis 1 167 N-Acetyl-P-D-glucosaminidase Adrenarche 4 13, 502 816, 835, 846, 888, 896, 904, -
Profile Profile Profile Uses and Administration
Gramicidin/lmipenem 309 Graneodin N; Graneodin; Gripaben Caramelos; Kenacomb; t Incompatibility and stability. Intipenem is unstable at Nasomicina; Neo Coltirot; Pantometilt; Proetztotal; Tosedrin �-�P.�.�� ����---········································································· alkaline or acidic pH and the commercially available injec (details are given in Volume B) NF; Austral.: Kenacomb; Neosporint; Otocomb Otic; Otodex; ProprielaryPreparations tion of intipenem with cilastatin sodium for intravenous Sofradex; Soframycint; Austria: Volon A antibiotikahaltigt; V alpeda. use is buffered to provide, when reconstituted, a solution Belg. : Mycolog; Polyspectran Granticidinet; Braz.: Fonergin; Single-ingredient Preparations. UK: with pH 6.5 to 7.5. Licensed product information advises Londerm-Nt; Mud; Neolon D; Omcilon-A M; Oncibel; Oncileg; against mixing with other antibacterials. Onciplust; Canad.: Ak Spor; Antibiotic Cream; Antibiotic Plus; Complete Antibiotic Ointment; Diosporint; Neosporin; Opti lbafloxacin (BAN, USAN, r/NN) References. cort; Optimyxin Plus; Optimyxin; Polysporin Complete; Poly 1. Bigley FP, et al. Compatibility of imipenem-dlastatin sodium with Am Hosp Phann 1986; 43: 2803- sporin For Kids; Polysporin Plus Pain Relief; Polysporin Triple commonly used intravenous solutions. 9. J Antibiotic; Polysporin; Polytopic; ratio-Tria comb; Sofracort; 2. Smith GB, et al. Stability and kinetics of degradation of imipenem in Soframycin; Soframycin; Triple Antibiotic Ointment; Viaderm Pharm 1990; 79: 732-40. aqueous -
Radical Sam Enzymes in Thienamycin Biosynthesis
RADICAL SAM ENZYMES IN THIENAMYCIN BIOSYNTHESIS by Daniel Roe Marous A dissertation submitted to The Johns Hopkins University in conformity with the requirements for the degree of Doctor of Philosophy Baltimore, Maryland December, 2015 ©Daniel Roe Marous 2015 All rights reserved Abstract Despite its broad anti-infective activity, the biosynthesis of the paradigm carbapenem antibiotic, thienamycin, remains largely unknown. Apart from the first two biosynthetic steps shared with a simple carbapenem, the pathway sharply diverges to the more structurally complex members of this class of β-lactam antibiotics like thienamycin. Existing evidence points to three putative cobalamin-dependent, radical S- adenosylmethionine (RS) enzymes, ThnK, ThnL and ThnP, potentially being responsible for assembly of the ethyl side chain at C6, bridgehead epimerization at C5, installation of the C2-thioether side chain and C2/3-desaturation. The C2 substituent has been demonstrated to be derived from stepwise truncation of coenzyme A, but the timing of these events with respect to C2—S bond formation is not known. Using in vitro reactions with synthetically-accessed substrates, we show that ThnK of the three apparent cobalamin-dependent RS enzymes performs sequential methylations to build out the C6- ethyl side chain in a stereocontrolled manner. This enzymatic reaction produced the expected RS methylase coproducts S-adenosylhomocysteine (SAH) and 5’- deoxyadenosine (5’-dA) by LC-MS and was also found to require cobalamin. For double methylation to occur, the carbapenam substrate must bear a coenzyme A-derived C2- thioether side chain, implying the activity of a prior sulfur insertion by an unidentified enzyme. Heterologous expression of thienamycin biosynthetic enzymes in Streptomyces combined with a competition bioassay now implicates ThnL in attachment of the thioether. -
Computational Antibiotics Book
Andrew V DeLong, Jared C Harris, Brittany S Larcart, Chandler B Massey, Chelsie D Northcutt, Somuayiro N Nwokike, Oscar A Otieno, Harsh M Patel, Mehulkumar P Patel, Pratik Pravin Patel, Eugene I Rowell, Brandon M Rush, Marc-Edwin G Saint-Louis, Amy M Vardeman, Felicia N Woods, Giso Abadi, Thomas J. Manning Computational Antibiotics Valdosta State University is located in South Georgia. Computational Antibiotics Index • Computational Details and Website Access (p. 8) • Acknowledgements (p. 9) • Dedications (p. 11) • Antibiotic Historical Introduction (p. 13) Introduction to Antibiotic groups • Penicillin’s (p. 21) • Carbapenems (p. 22) • Oxazolidines (p. 23) • Rifamycin (p. 24) • Lincosamides (p. 25) • Quinolones (p. 26) • Polypeptides antibiotics (p. 27) • Glycopeptide Antibiotics (p. 28) • Sulfonamides (p. 29) • Lipoglycopeptides (p. 30) • First Generation Cephalosporins (p. 31) • Cephalosporin Third Generation (p. 32) • Fourth-Generation Cephalosporins (p. 33) • Fifth Generation Cephalosporin’s (p. 34) • Tetracycline antibiotics (p. 35) Computational Antibiotics Antibiotics Covered (in alphabetical order) Amikacin (p. 36) Cefempidone (p. 98) Ceftizoxime (p. 159) Amoxicillin (p. 38) Cefepime (p. 100) Ceftobiprole (p. 161) Ampicillin (p. 40) Cefetamet (p. 102) Ceftoxide (p. 163) Arsphenamine (p. 42) Cefetrizole (p. 104) Ceftriaxone (p. 165) Azithromycin (p.44) Cefivitril (p. 106) Cefuracetime (p. 167) Aziocillin (p. 46) Cefixime (p. 108) Cefuroxime (p. 169) Aztreonam (p.48) Cefmatilen ( p. 110) Cefuzonam (p. 171) Bacampicillin (p. 50) Cefmetazole (p. 112) Cefalexin (p. 173) Bacitracin (p. 52) Cefodizime (p. 114) Chloramphenicol (p.175) Balofloxacin (p. 54) Cefonicid (p. 116) Cilastatin (p. 177) Carbenicillin (p. 56) Cefoperazone (p. 118) Ciprofloxacin (p. 179) Cefacetrile (p. 58) Cefoselis (p. 120) Clarithromycin (p. 181) Cefaclor (p.