Veterinary Science Animal Pathology and Clinical Aspects
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(12) United States Patent (10) Patent N0.: US 8,343,962 B2 Kisak Et Al
US008343962B2 (12) United States Patent (10) Patent N0.: US 8,343,962 B2 Kisak et al. (45) Date of Patent: *Jan. 1, 2013 (54) TOPICAL FORMULATION (58) Field of Classi?cation Search ............. .. 514/226.5, 514/334, 420, 557, 567 (75) Inventors: Edward T. Kisak, San Diego, CA (US); See application ?le fOr Complete Search history. John M. NeWsam, La Jolla, CA (US); _ Dominic King-Smith, San Diego, CA (56) References C‘ted (US); Pankaj Karande, Troy, NY (US); Samir Mitragotri, Goleta, CA (US) US' PATENT DOCUMENTS 5,602,183 A 2/1997 Martin et al. (73) Assignee: NuvoResearchOntano (CA) Inc., Mississagua, 6,328,979 2B1 12/2001 Yamashita et a1. 7,001,592 B1 2/2006 Traynor et a1. ( * ) Notice: Subject to any disclaimer, the term of this 7,795,309 B2 9/2010 Kisak eta1~ patent is extended or adjusted under 35 2002/0064524 A1 5/2002 Cevc U.S.C. 154(b) by 212 days. FOREIGN PATENT DOCUMENTS This patent is subject to a terminal dis- W0 WO 2005/009510 2/2005 claimer- OTHER PUBLICATIONS (21) APPI' NO‘, 12/848,792 International Search Report issued on Aug. 8, 2008 in application No. PCT/lB2007/0l983 (corresponding to US 7,795,309). _ Notice ofAlloWance issued on Apr. 29, 2010 by the Examiner in US. (22) Med Aug- 2’ 2010 Appl. No. 12/281,561 (US 7,795,309). _ _ _ Of?ce Action issued on Dec. 30, 2009 by the Examiner in US. Appl. (65) Prior Publication Data No, 12/281,561 (Us 7,795,309), Us 2011/0028460 A1 Feb‘ 3’ 2011 Primary Examiner * Raymond Henley, 111 Related U 5 Application Data (74) Attorney, Agent, or Firm * Foley & Lardner LLP (63) Continuation-in-part of application No. -
The Local Use of the Sulfonamide Drugs
THE LOCAL USE OF THE SULFONAMIDE DRUGS GEORGE CRILE Jr., M.D. Since the introduction of sulfanilamide and its derivatives, the reliance upon chemotherapy for the control of acute surgical infections has temporarily overshadowed the importance of sound surgical princi- ples and often has resulted in the administration of inefficient or inade- quate treatment. Too often, the physician fails to recognize the limita- tions of chemotherapy and vainly attempts to control the infection well beyond the optimum time for surgical intervention. Chemotherapy is very effective in controlling infections from hemo- lytic streptococcus; is moderately effective in controlling staphylococcic infections; but is of slight value when administered systemically in patients infected with the nonhemolytic streptococcus or colon bacillus. However, even in infections caused by the hemolytic streptococcus or the staphylococcus, sulfanilamide and sulfathiazole cannot replace surgery after suppuration has taken place and mechanical drainage of an abscess is required. It is in the treatment of lymphangitis and cellulitis, not in the treatment of abscesses, that chemotherapy has been of the greatest value. The work of Lockwood1 and others has indicated that the products of proteolysis in vitro interfere with the bacteriostatic and bacteriocidal powers of sulfanilamide. The presence of similar substances in undrained abscess cavities probably interferes with the destruction of the organ- isms by chemotherapy. Accordingly, the sulfonamide drugs should supplement rather than replace early and adequate surgical drainage, especially in the presence of suppuration. The local application of the sulfonamide drugs is based upon the principle that the local concentration of the drug in the tissues is ten to twenty times as high as that which can be obtained by any method of systemic administration. -
Xifaxan® (Rifaximin)
Wednesday, October 14, 2015 4 p.m. Oklahoma Health Care Authority 4345 N. Lincoln Blvd. Oklahoma City, OK 73105 The University of Oklahoma Health Sciences Center COLLEGE OF PHARMACY PHARMACY MANAGEMENT CONSULTANTS MEMORANDUM TO: Drug Utilization Review Board Members FROM: Bethany Holderread, Pharm.D. SUBJECT: Packet Contents for Board Meeting – October 14, 2015 DATE: October 1, 2015 NOTE: The DUR Board will meet at 4:00 p.m. The meeting will be held at 4345 N Lincoln Blvd. Enclosed are the following items related to the October meeting. Material is arranged in order of the agenda. Call to Order Public Comment Forum Action Item – Approval of DUR Board Meeting Minutes – Appendix A Action Item – Vote on 2016 Meeting Dates – Appendix B Update on Medication Coverage Authorization Unit/Bowel Preparation Medication Post-Educational Mailing – Appendix C Action Item – Vote to Prior Authorize Tykerb® (Lapatinib), Halaven® (Eribulin), Ixempra® (Ixabepilone), Kadcyla® (Ado-Trastuzumab), Afinitor® (Everolimus), & Perjeta® (Pertuzumab) – Appendix D Action Item – Vote to Prior Authorize Orkambi™ (Lumacaftor/Ivacaftor) – Appendix E Action Item – Vote to Prior Authorize Savaysa® (Edoxaban) – Appendix F Action Item – Vote to Prior Authorize Epanova® (Omega-3-Carboxylic Acids), Praluent® (Alirocumab), & Repatha™ (Evolocumab) – Appendix G Annual Review of Constipation and Diarrhea Medications and 30-Day Notice to Prior Authorize Movantik™ (Naloxegol), Viberzi™ (Eluxadoline), & Xifaxan® (Rifaximin) – Appendix H 30-Day Notice to Prior Authorize Daraprim® (Pyrimethamine) – Appendix I Annual Review of Allergy Immunotherapies and 30-Day Notice to Prior Authorize Oralair® (Sweet Vernal, Orchard, Perennial Rye, Timothy, & Kentucky Blue Grass Mixed Pollens Allergen Extract) – Appendix J Annual Review of Non-Steroidal Anti-Inflammatory Drugs and 30-Day Notice to Prior Authorize Dyloject™ (Diclofenac Sodium) – Appendix K ORI-4403 • P.O. -
Chloroquinoxaline Sulfonamide (NSC 339004) Is a Topoisomerase II␣/ Poison1
[CANCER RESEARCH 60, 5937–5940, November 1, 2000] Advances in Brief Chloroquinoxaline Sulfonamide (NSC 339004) Is a Topoisomerase II␣/ Poison1 Hanlin Gao, Edith F. Yamasaki, Kenneth K. Chan, Linus L. Shen, and Robert M. Snapka2 Departments of Radiology [H. G., E. F. Y., R. M. S.]; Molecular Virology, Immunology and Medical Genetics [H. G., R. M. S.]; College of Medicine [H. G., E. F. Y., R. M. S., K. K. C.]; and College of Pharmacy [K. K. C.], Ohio State University, Columbus, Ohio 43210, and Abbott Laboratories, Abbott Park, Illinois 60064 [L. L. S.] Abstract Drugs and Enzymes. CQS (NSC 339004) was provided by Dr. R. Shoe- maker, National Cancer Institute. VM-26 (teniposide, NSC 122819) was Chloroquinoxaline sulfonamide (chlorosulfaquinoxaline, CQS, NSC obtained from the National Cancer Institute Division of Cancer Treatment, 339004) is active against murine and human solid tumors. On the basis of Natural Products Branch. DMSO was the solvent for all drug stocks. Purified  its structural similarity to the topoisomerase II -specific drug XK469, human topoisomerase II␣ was from TopoGen (Columbus, OH) and LLS ␣ CQS was tested and found to be both a topoisomerase-II and a topoi- (Abbott Laboratories, Abbott Park, IL). Purified topoisomerase II was a  somerase-II poison. Topoisomerase II poisoning by CQS is essentially gift of Dr. Caroline Austin (University of Newcastle, Newcastle upon Tyne, undetectable in assays using the common protein denaturant SDS, but United Kingdom). easily detectable with strong chaotropic protein denaturants. The finding Filter Assay for in Vitro Topoisomerase-DNA Cross-links. The GF/C that detection of topoisomerase poisoning can be so dependent on the filter assay for protein-SV40 DNA cross-links is used to measure topoisomer- protein denaturant used in the assay has implications for drug discovery ase poisoning in vitro with purified enzymes and DNA substrates (9). -
Tetracycline and Sulfonamide Antibiotics in Soils: Presence, Fate and Environmental Risks
processes Review Tetracycline and Sulfonamide Antibiotics in Soils: Presence, Fate and Environmental Risks Manuel Conde-Cid 1, Avelino Núñez-Delgado 2 , María José Fernández-Sanjurjo 2 , Esperanza Álvarez-Rodríguez 2, David Fernández-Calviño 1,* and Manuel Arias-Estévez 1 1 Soil Science and Agricultural Chemistry, Faculty Sciences, University Vigo, 32004 Ourense, Spain; [email protected] (M.C.-C.); [email protected] (M.A.-E.) 2 Department Soil Science and Agricultural Chemistry, Engineering Polytechnic School, University Santiago de Compostela, 27002 Lugo, Spain; [email protected] (A.N.-D.); [email protected] (M.J.F.-S.); [email protected] (E.Á.-R.) * Correspondence: [email protected] Received: 30 October 2020; Accepted: 13 November 2020; Published: 17 November 2020 Abstract: Veterinary antibiotics are widely used worldwide to treat and prevent infectious diseases, as well as (in countries where allowed) to promote growth and improve feeding efficiency of food-producing animals in livestock activities. Among the different antibiotic classes, tetracyclines and sulfonamides are two of the most used for veterinary proposals. Due to the fact that these compounds are poorly absorbed in the gut of animals, a significant proportion (up to ~90%) of them are excreted unchanged, thus reaching the environment mainly through the application of manures and slurries as fertilizers in agricultural fields. Once in the soil, antibiotics are subjected to a series of physicochemical and biological processes, which depend both on the antibiotic nature and soil characteristics. Adsorption/desorption to soil particles and degradation are the main processes that will affect the persistence, bioavailability, and environmental fate of these pollutants, thus determining their potential impacts and risks on human and ecological health. -
Transdermal Drug Delivery Device Including An
(19) TZZ_ZZ¥¥_T (11) EP 1 807 033 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61F 13/02 (2006.01) A61L 15/16 (2006.01) 20.07.2016 Bulletin 2016/29 (86) International application number: (21) Application number: 05815555.7 PCT/US2005/035806 (22) Date of filing: 07.10.2005 (87) International publication number: WO 2006/044206 (27.04.2006 Gazette 2006/17) (54) TRANSDERMAL DRUG DELIVERY DEVICE INCLUDING AN OCCLUSIVE BACKING VORRICHTUNG ZUR TRANSDERMALEN VERABREICHUNG VON ARZNEIMITTELN EINSCHLIESSLICH EINER VERSTOPFUNGSSICHERUNG DISPOSITIF D’ADMINISTRATION TRANSDERMIQUE DE MEDICAMENTS AVEC COUCHE SUPPORT OCCLUSIVE (84) Designated Contracting States: • MANTELLE, Juan AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Miami, FL 33186 (US) HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI • NGUYEN, Viet SK TR Miami, FL 33176 (US) (30) Priority: 08.10.2004 US 616861 P (74) Representative: Awapatent AB P.O. Box 5117 (43) Date of publication of application: 200 71 Malmö (SE) 18.07.2007 Bulletin 2007/29 (56) References cited: (73) Proprietor: NOVEN PHARMACEUTICALS, INC. WO-A-02/36103 WO-A-97/23205 Miami, FL 33186 (US) WO-A-2005/046600 WO-A-2006/028863 US-A- 4 994 278 US-A- 4 994 278 (72) Inventors: US-A- 5 246 705 US-A- 5 474 783 • KANIOS, David US-A- 5 474 783 US-A1- 2001 051 180 Miami, FL 33196 (US) US-A1- 2002 128 345 US-A1- 2006 034 905 Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations. -
Nitroaromatic Antibiotics As Nitrogen Oxide Sources
Review biomolecules Nitroaromatic Antibiotics as Nitrogen Oxide Sources Review Allison M. Rice, Yueming Long and S. Bruce King * Nitroaromatic Antibiotics as Nitrogen Oxide Sources Department of Chemistry and Biochemistry, Wake Forest University, Winston-Salem, NC 27101, USA; Allison M. Rice , Yueming [email protected] and S. Bruce (A.M.R.); King [email protected] * (Y.L.) * Correspondence: [email protected]; Tel.: +1-336-702-1954 Department of Chemistry and Biochemistry, Wake Forest University, Winston-Salem, NC 27101, USA; [email protected]: Nitroaromatic (A.M.R.); [email protected] antibiotics (Y.L.) show activity against anaerobic bacteria and parasites, finding * Correspondence: [email protected]; Tel.: +1-336-702-1954 use in the treatment of Heliobacter pylori infections, tuberculosis, trichomoniasis, human African trypanosomiasis, Chagas disease and leishmaniasis. Despite this activity and a clear need for the Abstract: Nitroaromatic antibiotics show activity against anaerobic bacteria and parasites, finding usedevelopment in the treatment of new of Heliobacter treatments pylori forinfections, these conditio tuberculosis,ns, the trichomoniasis, associated toxicity human Africanand lack of clear trypanosomiasis,mechanisms of action Chagas have disease limited and their leishmaniasis. therapeutic Despite development. this activity Nitroaro and a clearmatic need antibiotics for require thereductive development bioactivation of new treatments for activity for theseand this conditions, reductive the associatedmetabolism toxicity can convert -
Antibiotic Resistance and Trend of Urinary Pathogens in General Outpatients from a Major Urban City
Clinical Urology Resistance of Urinary Pathogens in Outpatients International Braz J Urol Vol. 33 (1): 42-49, January - February, 2007 Antibiotic Resistance and Trend of Urinary Pathogens in General Outpatients from a Major Urban City Carlos R. Kiffer, Caio Mendes, Carmen P. Oplustil, Jorge L. Sampaio Section of Microbiology, Fleury Institute, Sao Paulo, SP, Brazil ABSTRACT Objective: We assessed the antimicrobial resistance patterns of pathogens responsible for urinary tract infections (UTI) in outpatients in São Paulo, Brazil, as well as the Escherichia coli antimicrobial resistance trend. Materials and Methods: Outpatients urine cultures were collected from January 2000 to December 2003. Statistical analy- sis considered positive results for one bacterial species with colony count ≥ 100,000 CFU/mL. Stratification was done on age group and gender. Statistical tests used included chi-square and the chi-square test for trend to evaluate differences between susceptibility rates among age groups and ordering in the E. coli resistance rates per year, respectively. Results: There were 37,261 positive results with Enterobacteriaceae isolated in 32,530 (87.3%) and Gram-positive cocci in 2,570 (6.9%) cultures. E. coli had the highest prevalence (71.6%). Susceptibility tests were performed in 31,716 cultures. E. coli had elevated resistance rates (> 30%) to ampicillin, trimethoprim-sulfamethoxazole, and tetracycline. Significant differences between age groups and ordering among years were observed. Conclusions: The use of trimethoprim-sulfamethoxazole is precluded in the population studied due to elevated resistance rates (> 30%) among most prevalent pathogens. Significant resistance rate differences among age groups and years were observed, particularly for fluoroquinolones. Fluoroquinolones should be used with caution. -
1918 Serbian Sanitet 1914
SERBIAN SANITET 1914 – 1918 SERBIAN SANITET СРПСКИ САНИТЕТ 1914 – 1918. SERBIAN SANITET 1914 – 1918 Музеј града City museum 1914 – 1918. СРПСКИ САНИТЕТ Новог Сада of novi sad Музеј града City museum Новог Сада of novi sad Издавачи / Publishers Музеј града Новог Сада, Војни музеј, Београд, Народни музеј Шабац City Museum of Novi Sad, Military Museum Belgrade, National Museum Šabac За издавача / Editor-in-Chief МЅс Весна Јовичић / Vesna Jovičić,MSc Уредник / Publication Editor Др Мирко Пековић / Mirko Peković, PhD Аутори изложбе и каталога / Exhibition and Catalogue Authors Гордана Буловић, Мирко Пековић, Бранислав Станковић Gordana Bulović, Mirko Peković, Branislav Stanković Поставка изложбе / Exhibition Design Душан Пешић / Dušan Pešić Рецензенти / Consulting Editors Мр мед. Владимир Сакач, мр фар. Илија Савков, пуковник др Братомир Бркљача MD MSc Vladimir Sakač, MSc Pharm. Ilija Savkov, Colonel Dr Bratomir Brkljača Лектор / Proofreading Душица Милосављевић / Dušica Milosavljević Превод / Translation Зоран Протић / Zoran Protić Фотографија / Photography Феђа Киселички / Feđa Kiselički Конзервација / Conservation Тамина Кесић / Tamina Kesić Рестаурација / Restoration Саша Глишић, Александар Глишић / Saša Glišić, Aleksandar Glišić Техничка реализација / Tehnical support Данило Крушић / Danilo Krušić Припрема и штампа / Prepared and Printed by ЈП Службени гласник, Београд Official Gazette, Belgrade Тираж 300 primeraka / Circulation: 300 copies Пројекат је подржало Министарство културе и информисања Републике Србије This project is supported by the Ministry of Culture and Information, Republic of Serbia isBn 978-86-7637-087-0 Но ви Сад 2015 Транспорт првих рањеника при заузећу Кара-Тепеа и Плуче (јужне падине Кајмакчалана, кота 1900), 7. 8. 1916. године Transport of first wounded soldiers after taking over Kara Tepe and Pluča (southern slope of Kaymakchalan, cotta 1900), 07/08/1916 Срп ски са ни тет Serbian Medical Corps у Ве ли ком ра ту in the Great War 1914–1918. -
Gene-Drug Interactions and the Evolution of Antibiotic Resistance
Gene-Drug Interactions and the Evolution of Antibiotic Resistance The Harvard community has made this article openly available. Please share how this access benefits you. Your story matters Citation Palmer, Adam Christopher. 2012. Gene-Drug Interactions and the Evolution of Antibiotic Resistance. Doctoral dissertation, Harvard University. Citable link http://nrs.harvard.edu/urn-3:HUL.InstRepos:10436292 Terms of Use This article was downloaded from Harvard University’s DASH repository, and is made available under the terms and conditions applicable to Other Posted Material, as set forth at http:// nrs.harvard.edu/urn-3:HUL.InstRepos:dash.current.terms-of- use#LAA © - Adam Christopher Palmer All rights reserved. Professor Roy Kishony Adam Christopher Palmer Gene-drug interactions and the evolution of antibiotic resistance Abstract The evolution of antibiotic resistance is shaped by interactions between genes, the chemical environment, and an antibiotic's mechanism of action. This thesis explores these interactions with experiments, theory, and analysis, seeking a mechanistic understanding of how different interactions between genes and drugs can enhance or constrain the evolution of antibiotic resistance. Chapter 1 investigates the effects of the chemical decay of an antibiotic. Tetracycline resistant and sensitive bacteria were grown competitively in the presence of tetracycline and its decay products. Antibiotic decay did not only remove selection for resistance, but long- lived decay products favored tetracycline sensitivity by inducing costly drug efflux pumps in the resistant strain. Selection against resistance by antibiotic-related compounds may contribute to the coexistence of drug-sensitive and resistant bacteria in nature. Chapter 2 investigates how genetic interactions can favor particular combinations of resistance-conferring mutations. -
Antimicrobial and Anticancer Activity of Some Novel Fluorinated
View metadata, citation and similar papers at core.ac.uk brought to you by CORE provided by Springer - Publisher Connector Ghorab et al. Chemistry Central Journal (2017) 11:32 DOI 10.1186/s13065-017-0258-4 RESEARCH ARTICLE Open Access Antimicrobial and anticancer activity of some novel fuorinated thiourea derivatives carrying sulfonamide moieties: synthesis, biological evaluation and molecular docking Mostafa M. Ghorab1,2*, Mansour S. Alsaid1, Mohamed S. A. El‑Gaby3*, Mahmoud M. Elaasser4 and Yassin M. Nissan5 Abstract Background: Various thiourea derivatives have been used as starting materials for compounds with better biological activities. Molecular modeling tools are used to explore their mechanism of action. Results: A new series of thioureas were synthesized. Fluorinated pyridine derivative 4a showed the highest anti‑ microbial activity (with MIC values ranged from 1.95 to 15.63 µg/mL). Interestingly, thiadiazole derivative 4c and coumarin derivative 4d exhibited selective antibacterial activities against Gram positive bacteria. Fluorinated pyridine derivative 4a was the most active against HepG2 with IC50 value of 4.8 μg/mL. Molecular docking was performed on the active site of MK-2 with good results. Conclusion: Novel compounds were obtained with good anticancer and antibacterial activity especially fuorinated pyridine derivative 4a and molecular docking study suggest good activity as mitogen activated protein kinase-2 inhibitor. Keywords: Isothiocyanate, Sulfonamide, Fluorinated thiourea, Antimicrobial and anticancer activity Background the increased hydrophobicity, and (v) the second small- Fluorinated compounds are intriguing for the develop- est atomic radius of the fuorine atom. Tese factors are ment of pharmaceuticals, agrochemicals, and materials, operative singly or sometimes cooperatively to afect the and thus, much efort has been exerted to develop more pharmacological properties of the fuorinated molecules general and efcient approaches for introducing fuorine [5]. -
2-Amino-1,3,4-Thiadiazoles in Leishmaniasis
Review Future Prospects in the Treatment of Parasitic Diseases: 2‐Amino‐1,3,4‐Thiadiazoles in Leishmaniasis Georgeta Serban Pharmaceutical Chemistry Department, Faculty of Medicine and Pharmacy, University of Oradea, 29 Nicolae Jiga, 410028 Oradea, Romania; [email protected]; Tel: +4‐0756‐276‐377 Received: 22 March 2019; Accepted: 17 April 2019; Published: 19 April 2019 Abstract: Neglected tropical diseases affect the lives of a billion people worldwide. Among them, the parasitic infections caused by protozoan parasites of the Trypanosomatidae family have a huge impact on human health. Leishmaniasis, caused by Leishmania spp., is an endemic parasitic disease in over 88 countries and is closely associated with poverty. Although significant advances have been made in the treatment of leishmaniasis over the last decade, currently available chemotherapy is far from satisfactory. The lack of an approved vaccine, effective medication and significant drug resistance worldwide had led to considerable interest in discovering new, inexpensive, efficient and safe antileishmanial agents. 1,3,4‐Thiadiazole rings are found in biologically active natural products and medicinally important synthetic compounds. The thiadiazole ring exhibits several specific properties: it is a bioisostere of pyrimidine or benzene rings with prevalence in biologically active compounds; the sulfur atom increases lipophilicity and combined with the mesoionic character of thiadiazoles imparts good oral absorption and good cell permeability, resulting in good bioavailability. This review presents synthetic 2‐amino‐1,3,4‐thiadiazole derivatives with antileishmanial activity. Many reported derivatives can be considered as lead compounds for the synthesis of future agents as an alternative to the treatment of leishmaniasis. Keywords: 2‐amino‐1,3,4‐thiadiazole; neglected tropical diseases; protozoan parasites; Leishmania spp.; antileishmanial activity; inhibitory concentration 1.