The Efficacy of Ampicillin Compared with Ceftriaxone on Preventing
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In Vitro Susceptibilities of Escherichia Coli and Klebsiella Spp. To
Jpn. J. Infect. Dis., 60, 227-229, 2007 Short Communication In Vitro Susceptibilities of Escherichia coli and Klebsiella Spp. to Ampicillin-Sulbactam and Amoxicillin-Clavulanic Acid Birgul Kacmaz* and Nedim Sultan1 Department of Central Microbiology and 1Department of Microbiology, Faculty of Medicine, Gazi University, Ankara, Turkey (Received January 30, 2007. Accepted April 13, 2007) SUMMARY: Ampicillin-sulbactam (A/S) and amoxicillin-clavulanic acid (AUG) are thought to be equally efficacious clinically against the Enterobacteriaceae family. In this study, the in vitro activities of the A/S and AUG were evaluated and compared against Escherichia coli and Klebsiella spp. Antimicrobial susceptibility tests were performed by standard agar dilution and disc diffusion techniques according to the Clinical and Laboratory Standards Institute (CLSI). During the study period, 973 strains were isolated. Of the 973 bacteria isolated, 823 were E. coli and 150 Klebsiella spp. More organisms were found to be susceptible to AUG than A/S, regardless of the susceptibility testing methodology. The agar dilution results of the isolates that were found to be sensitive or resistant were also compatible with the disc diffusion results. However, some differences were seen in the agar dilution results of some isolates that were found to be intermediately resistant with disc diffusion. In E. coli isolates, 17 of the 76 AUG intermediately resistant isolates (by disc diffusion), and 17 of the 63 A/S intermediately resistant isolates (by disc diffusion) showed different resistant patterns by agar dilution. When the CLSI breakpoint criteria are applied it should be considered that AUG and A/S sensitivity in E. coli and Klebsiella spp. -
Orally Active Esters of Cephalosporin Antibiotics. Ii
VOL. XXXII NO. 11 THE JOURNAL OF ANTIBIOTICS 1155 ORALLY ACTIVE ESTERS OF CEPHALOSPORIN ANTIBIOTICS. II SYNTHESIS AND BIOLOGICAL PROPERTIES OF THE ACETOXYMETHYL ESTER OF CEFAMANDOLE WALTER E. WRIGHT, WILLIAM J. WHEELER, VERLE D. LINE, JUDITH ANN FROGGE' and DON R. FINLEY Lilly Research Laboratories, Eli Lilly and Company Indianapolis, Indiana 46206, U.S.A. (Received for publication August 29, 1979) The synthesis of the acetoxymethyl (AOM) ester of cefamandole (CM) is described. The sparingly soluble ester is shown to be well absorbed orally by mice, but only when administered in solution in a partially non-aqueous vehicle, 50°o propylene glycol. Neither the ester in aqueous suspension nor the sodium salt of CM in solution is well absorbed orally. The rate of oral absorption of the ester from solution is very rapid as shown by the early peak time and shape of the plasma level curve. Oral bioavailability from solution is at least 60% and is ap- parently limited only by hydrolysis or precipitation of a variable portion of the ester dose in the intestinal lumen prior to absorption. Esterification of the carboxyl group of penicillins and cephalosporins can result in significant improvement in the oral absorption of the parent drug. Pivampicillin1), bacampicillin2) and talampicil- lin3J are examples of such successful penicillin derivatives, and the acetoxymethyl ester of cephaloglycin4 and other cephalosporin derivatives') illustrate the applicability of this pro-drug principle to cephalo- sporins. Although the intact esters are biologically inactive, they can be hydrolyzed to the active parent drug either during passage through the intestinal wall or after absorption has occurred6). -
Ampicillin (Ampicillin Sodium) INJECTION, POWDER, FOR
Ampicillin for Injection, USP Rx Only (For Intramuscular or Intravenous Injection) To reduce the development of drug-resistant bacteria and maintain the effectiveness of ampicillin and other antibacterial drugs, ampicillin should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria. DESCRIPTION Ampicillin for injection, USP the monosodium salt of [2S-[2α,5α,6β(S*)]]-6- [(aminophenylacetyl)amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, is a synthetic penicillin. It is an antibacterial agent with a broad spectrum of bactericidal activity against both penicillin-susceptible Gram-positive organisms and many common Gram-negative pathogens. Ampicillin for injection, USP is a white to cream-tinged, crystalline powder. The reconstituted solution is clear, colorless and free from visible particulates. Each vial of Ampicillin for injection, USP contains ampicillin sodium equivalent to 250 mg, 500 mg, 1 gram or 2 grams ampicillin. Ampicillin for injection, USP contains 65.8 mg [2.9 mEq] sodium per gram ampicillin. It has the following molecular structure: The molecular formula is C16H18N3NaO4S, and the molecular weight is 371.39. The pH range of the reconstituted solution is 8 to 10. CLINICAL PHARMACOLOGY Ampicillin for injection diffuses readily into most body tissues and fluids. However, penetration into the cerebrospinal fluid and brain occurs only when the meninges are inflamed. Ampicillin is excreted largely unchanged in the urine and its excretion can be delayed by concurrent administration of probenecid. Due to maturational changes in renal function, ampicillin half-life decreases as postmenstrual age (a sum of gestational age and postnatal age) increases for infants with postnatal age of less than 28 days. -
Guidelines on Urinary and Male Genital Tract Infections
European Association of Urology GUIDELINES ON URINARY AND MALE GENITAL TRACT INFECTIONS K.G. Naber, B. Bergman, M.C. Bishop, T.E. Bjerklund Johansen, H. Botto, B. Lobel, F. Jimenez Cruz, F.P. Selvaggi TABLE OF CONTENTS PAGE 1. INTRODUCTION 5 1.1 Classification 5 1.2 References 6 2. UNCOMPLICATED UTIS IN ADULTS 7 2.1 Summary 7 2.2 Background 8 2.3 Definition 8 2.4 Aetiological spectrum 9 2.5 Acute uncomplicated cystitis in pre-menopausal, non-pregnant women 9 2.5.1 Diagnosis 9 2.5.2 Treatment 10 2.5.3 Post-treatment follow-up 11 2.6 Acute uncomplicated pyelonephritis in pre-menopausal, non-pregnant women 11 2.6.1 Diagnosis 11 2.6.2 Treatment 12 2.6.3 Post-treatment follow-up 12 2.7 Recurrent (uncomplicated) UTIs in women 13 2.7.1 Background 13 2.7.2 Prophylactic antimicrobial regimens 13 2.7.3 Alternative prophylactic methods 14 2.8 UTIs in pregnancy 14 2.8.1 Epidemiology 14 2.8.2 Asymptomatic bacteriuria 15 2.8.3 Acute cystitis during pregnancy 15 2.8.4 Acute pyelonephritis during pregnancy 15 2.9 UTIs in post-menopausal women 15 2.10 Acute uncomplicated UTIs in young men 16 2.10.1 Pathogenesis and risk factors 16 2.10.2 Diagnosis 16 2.10.3 Treatment 16 2.11 References 16 3. UTIs IN CHILDREN 20 3.1 Summary 20 3.2 Background 20 3.3 Aetiology 20 3.4 Pathogenesis 20 3.5 Signs and symptoms 21 3.5.1 New-borns 21 3.5.2 Children < 6 months of age 21 3.5.3 Pre-school children (2-6 years of age) 21 3.5.4 School-children and adolescents 21 3.5.5 Severity of a UTI 21 3.5.6 Severe UTIs 21 3.5.7 Simple UTIs 21 3.5.8 Epididymo orchitis 22 3.6 Diagnosis 22 3.6.1 Physical examination 22 3.6.2 Laboratory tests 22 3.6.3 Imaging of the urinary tract 23 3.7 Schedule of investigation 24 3.8 Treatment 24 3.8.1 Severe UTIs 25 3.8.2 Simple UTIs 25 3.9 References 26 4. -
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. -
And Bacampicillin
SINGAPORE MEDICAL JOURNAL PROPULSIVE LOAD ADMINISTRATION AND BACAMPICILLIN T Bergan SYNOPSIS Propulsive load dosage for antibiotics is a temi applied to intermittent dosage which enables establishment of a better buffering capacity than continuous intravascular infusions. The major factors explaining why propulsive load dosing is effective are the antibacterial post -antibiotic effect (APAE), post -antibiotic leucocyte enhancement (PALE), post - antibiotic repressed adhesion (PARA), and pharmacokinetic extra - vascular persistence (PEP). These properties all apply to ampicillin, and its prodrug bacampicillin is preferable to other aminopenicillins for pharmacokinetic reasons. This prodrug produces particularly high peak area under the serum curve (PAUC), which is one decisive factor in establishing high extravascular concentrations of an antibiotic. Bacampicillin is subject to nearly complete absorption and high extravascular levels which are maintained longer than those in serum. Bacampicillin is thus an alternative preferable to ampicillin when the infecting microbe is ampicillin sensitive. INTRODUCTION By the term propulsive load dosing we understand intermittent dosage of antibiotics with high doses at time intervals rather than as continuous infusions. Load dosing applies to oral doses like tablets or intravenous rapid bolus doses. By the word propulsive, we convey the concept that load dosing enables optimal and good extravascular penetration of the antibiotic. At first impulse, one might think that maintenance of antibiotic concentrations constantly above a minimum inhibitory level (MIC) were ideal and that this were safer than dosage loads like tablets or injections given at certain time intervals. We shall expand on the reasons why intermittent administration, i.e. propulsive load dosing functions well. In tills context, we shall deal with the theoretical and practical explanations behind why intermittent dosage of antibiotics entails effective therapy. -
Treating Genitourinary and Pharyngeal Gonorrhoea with Single Dose Ceftriaxone
Genitourin Med: first published as 10.1136/sti.65.1.14 on 1 January 1989. Downloaded from Genitourin Med 1989;65:14-17 Treating genitourinary and pharyngeal gonorrhoea with single dose ceftriaxone J CHRISTOPHERSEN,* A C BOLLERUP,t E FROM,$ J 0 R0NNE-RASMUSSEN,§ K QUITZAUII From the *Department ofDermatovenereology, Gentofte Hospital, Hellerup; the tNeisseria Department, Statens Seruminstitut, Copenhagen; the tDepartment ofDermatovenereology, Marselisborg Hospital, Aarhus; the §Department ofDermatovenereology, Bispebjerg Hospital, Copenhagen; and the IlDepartment ofClinical Research, Roche, Denmark suMMARY The efficacy of ceftriaxone 250 mg given as a single intramuscular dose to treat genitourinary and pharyngeal gonorrhoea is compared with the outcome of the Danish standard treatment for uncomplicated genitourinary gonorrhoea, pivampicillin 1-4 g and probenecid 1 g, both given by mouth. The study comprised 327 patients for whom the diagnosis ofgonorrhoea was made by microscopy of a methylene blue stained smear at their first visit to the clinic and for whom the diagnosis was later confirmed by culture of Neisseria gonorrhoeae. One hundred and seventy patients with genitourinary gonorrhoea (18 with and 152 without concomitant pharyngeal infection) were treated with ceftriaxone. One hundred and fifty seven (17 with and 140 without concomitant pharyngeal infection) were treated with pivampicillin. One week after treatment N gonorrhoeae was isolated from none of 18, 1/152, (1%), 11/17 (65%), and 6/140 (4%) patients, respectively. At a second attendance two weeks after treatment no further treatment failure was found. During the study period, a further 52 patients with pharyngeal infection (with or without concomitant genitourinary infection) that was shown by culture only were treated with a single http://sti.bmj.com/ intramuscular injection of 250 mg ceftriaxone. -
Clinical Pharmacology of Ampicillin in Infants and Children
Central Journal of Drug Design and Research Bringing Excellence in Open Access Review Article *Corresponding author Gian Maria Pacifici,Associate professorof Pharmacology,via Sant’Andrea 32,56127 Pisa,Italy. Clinical Pharmacology of Email: [email protected] Submitted: 19 April 2021 Accepted: 25 April 2021 Ampicillin in Infants and Published: 27 April 2021 ISSN: 2379-089X Children Copyright © 2021 Pacifici GM Gian Maria Pacifici* OPEN ACCESS Associate professorof Pharmacology, Italy Keywords Abstract • Ampicillin • Dosing Ampicillin is an aminopenicillin and is more active than penicillin G. Ampicillin is destroyed by β-lactamase • Treatment and is co-formulated with sulbactam an inhibitor of β-lactamase. Ampicillin is bactericidal and it is active • Trials against meningococci, Listeria monocytogenes, enterococci, and the co-administration with sulbactam markedly • Placental-transfer expands the spectrum of activity against Haemophilus influenzae, Escherichia coli, Proteus, and Bacillus fragilis. • Breast-milk Ampicillin may be administered intravenously and orally and the intravenous dose is 50 mg twice-daily and • Meningitis thrice-daily in preterm and term infants, respectively. The oral dose in children ranges from 125 to 500 mg 4 times-daily and increases with the chid age. Ampicillin has been found efficacy and safe in infants and children but may cause adverse-effects. In infants, the ampicillin elimination half-life ranges between 2.4 to 5.0 hours and decreases with infant maturation and in children it is about 0.8 hours. Ampicillin interacts with drugs, the treatment and the trials with ampicillin have been extensively studied in infants and children. This antibiotic freely crosses the human placenta but poorly migrates into the breast-milk. -
Ceftaroline Fosamil for the Treatment of Gram-Positive Endocarditis: CAPTURE Study Experience
International Journal of Antimicrobial Agents 53 (2019) 644–649 Contents lists available at ScienceDirect International Journal of Antimicrobial Agents journal homepage: www.elsevier.com/locate/ijantimicag Ceftaroline fosamil for the treatment of Gram-positive endocarditis: CAPTURE study experience ∗ Christopher J. Destache a, David J. Guervil b, Keith S. Kaye c, a School of Pharmacy and Health Professions, Creighton University, Omaha, NE, USA b Memorial Hermann-Texas Medical Center, Houston, TX, USA c Wayne State University and Detroit Medical Center, Detroit, MI, USA a r t i c l e i n f o a b s t r a c t Article history: Background: The clinical experience of ceftaroline fosamil (CPT-F) therapy for Gram-positive infective Received 3 October 2018 endocarditis is reported from CAPTURE, a retrospective study conducted in the USA. Accepted 27 January 2019 Methods: Data, including patient demographics, medical history, risk factors, microbiological aetiology and clinical outcomes, were collected by review of patient charts between September 2013 and February Editor: Professor Matthew Falagas 2015. Results: Patients ( n = 55) with Gram-positive endocarditis were treated with CPT-F. The most common Keywords: risk factors were intravascular devices (43.6%), diabetes mellitus (40.0%) and injection drug use (38.2%). Ceftaroline fosamil Gram-positive endocarditis The most commonly isolated pathogens were meticillin-resistant Staphylococcus aureus (MRSA; 80%), Meticillin-resistant Staphylococcus aureus meticillin-susceptible S. aureus (MSSA; 7.3%) and coagulase-negative staphylococci (7.3%). CPT-F was given Meticillin-susceptible Staphylococcus aureus as first-line therapy in 7.3% of patients and as second-line or later therapy in 92.7% of patients, and as CAPTURE study monotherapy in 41.8% of patients and as concurrent therapy in 58.2% of patients. -
EAU Guidelines on Urological Infections 2018
EAU Guidelines on Urological Infections G. Bonkat (Co-chair), R. Pickard (Co-chair), R. Bartoletti, T. Cai, F. Bruyère, S.E. Geerlings, B. Köves, F. Wagenlehner Guidelines Associates: A. Pilatz, B. Pradere, R. Veeratterapillay © European Association of Urology 2018 TABLE OF CONTENTS PAGE 1. INTRODUCTION 6 1.1 Aim and objectives 6 1.2 Panel composition 6 1.3 Available publications 6 1.4 Publication history 6 2. METHODS 6 2.1 Introduction 6 2.2 Review 7 3. THE GUIDELINE 7 3.1 Classification 7 3.2 Antimicrobial stewardship 8 3.3 Asymptomatic bacteriuria in adults 9 3.3.1 Evidence question 9 3.3.2 Background 9 3.3.3 Epidemiology, aetiology and pathophysiology 9 3.3.4 Diagnostic evaluation 9 3.3.5 Evidence summary 9 3.3.6 Disease management 9 3.3.6.1 Patients without identified risk factors 9 3.3.6.2 Patients with ABU and recurrent UTI, otherwise healthy 9 3.3.6.3 Pregnant women 10 3.3.6.3.1 Is treatment of ABU beneficial in pregnant women? 10 3.3.6.3.2 Which treatment duration should be applied to treat ABU in pregnancy? 10 3.3.6.3.2.1 Single dose vs. short course treatment 10 3.3.6.4 Patients with identified risk-factors 10 3.3.6.4.1 Diabetes mellitus 10 3.3.6.4.2 ABU in post-menopausal women 11 3.3.6.4.3 Elderly institutionalised patients 11 3.3.6.4.4 Patients with renal transplants 11 3.3.6.4.5 Patients with dysfunctional and/or reconstructed lower urinary tracts 11 3.3.6.4.6 Patients with catheters in the urinary tract 11 3.3.6.4.7 Patients with ABU subjected to catheter placements/exchanges 11 3.3.6.4.8 Immuno-compromised and severely -
Abbreviations: ABPC, Ampicillin
Agric. Biol. Chem., 44 (11), 2689•`2693, 1980 2689 Supersensitivity of Escherichia coli Cells to Several -Lactam Antibiotics Caused by Rod- MorphologyƒÀ Mutations at the mrd Gene Cluster Shigeo TAMAKI, Hiroshi MATSUZAWA,* Sadayo NAKAJIMA-IIJIMA and Michio MATSUHASHI Institute of Applied Microbiology, and *Department of Agricultural Chemistry, The University of Tokyo, Bunkyo-ku, Tokyo 113, Japan Received June 13, 1980 Two kinds of spherical mutants, mrdA and mrdB mutants, have been isolated from Escherichia coli strain K12. The mrdA mutants have thermosensitive penicillin-binding protein 2, while the mrdB mutants have normal penicillin-binding proteins. Both kinds of mutants form spherical cells at 42•Ž and are resistant to the amidinopenicillin, mecillinam, at the same temperature. The two mutations have been mapped very close to lip at 14.2 min (revised chromosome linkage map, 1980) on the E. coli chromosome. Both mutations cause supersensitivities of cell growth to various ƒÀ-lactam antibiotics, such as ampicillin, cephalexin, cefoxitin and nocardicin A at 42•Ž. There are several reports that mutations 14.4•`14.5 min on the new E. coli chromosome in penicillin-binding proteins (PBPs) in map.8) Mutation in PBP-2 is known to cause Escherichia coli can cause supersensitivity of formation of spherical cells.3,7) The gene which the cells to ƒÀ-lactam antibiotics. Mutations in is simultaneously responsible for the for PBP-l Bs caused supersensitivity to almost all mation of PBP-2 and rod shaped cells has been penicillins and cephalosporins -
Amoxicillin/Clavulanate Potassium Tablets
NDA 50-564/S-049 NDA 50-720/S-022 Page 3 AC:AL10 PRESCRIBING INFORMATION Amoxicillin/Clavulanate Potassium Tablets To reduce the development of drug-resistant bacteria and maintain the effectiveness of amoxicillin/clavulanate potassium and other antibacterial drugs, amoxicillin/clavulanate potassium should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria. DESCRIPTION Amoxicillin/clavulanate potassium is an oral antibacterial combination consisting of the semisynthetic antibiotic amoxicillin and the β-lactamase inhibitor, clavulanate potassium (the potassium salt of clavulanic acid). Amoxicillin is an analog of ampicillin, derived from the basic penicillin nucleus, 6-aminopenicillanic acid. The amoxicillin molecular formula is C16H19N3O5S•3H2O, and the molecular weight is 419.46. Chemically, amoxicillin is (2S,5R,6R)-6-[(R) (-)-2-Amino-2-(p-hydroxyphenyl)acetamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2 carboxylic acid trihydrate and may be represented structurally as: Clavulanic acid is produced by the fermentation of Streptomyces clavuligerus. It is a β-lactam structurally related to the penicillins and possesses the ability to inactivate a wide variety of β-lactamases by blocking the active sites of these enzymes. Clavulanic acid is particularly active against the clinically important plasmid-mediated β-lactamases frequently responsible for transferred drug resistance to penicillins and cephalosporins. The clavulanate potassium molecular formula is C8H8KNO5, and the molecular weight is 237.25. Chemically, clavulanate potassium is potassium (Z) (2R,5R)-3-(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo[3.2.0]-heptane-2-carboxylate, and may be represented structurally as: Inactive Ingredients: Colloidal silicon dioxide, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, sodium starch glycolate, and titanium dioxide.