RECENTAD\ANCES

INCHEMOTHERAPY

Antimicrobial Section 2

Proceedings of the 14th International Congress of Chemotherapy, Kyoto, 1985

Edited by Joji Ishigami

UNIVERSITY OF TOKYO PRESS

Contents

§6. Cephem Antibiotics

New Aminothiazole Cephalosporins with 3-Pyridiniumthiomethyl SubstituentsT. Tsuruoka et al 877

In vitro and in vivo Antibacterial Activity of M 14643, a New SemisyntheticCephalosporin

H. Inaba et al 879In vitro and in vivo Antibacterial Activity of M 14638, a New SemisyntheticCephalosporin

H. Mochizuki et al 881Antibacterial Activity of CGP 31 523 A, a New Parenteral Cephalosporin

W. Tosch et al 883Chemotherapeutic Efficacy of CGP 31 523 A, a New Cephalosporin Antibiotic, in vivo

O.Zzk etal 885The in vitro and in vivo Antibacterial Activities of L-105, a New ParenteralCephalosporin

M. Otsuki etal 887Bactericidal Activity of L-105, a New Cephalosporin

M. Hikida etal 889Antimicrobial Activity and Pharmacokinetics of L-105, a New Cephem Antibiotic Agent

M. Tomisawa et al 891Pharmacokinetics of L-105 in Patients with Renal Insufficiency

A. Mizuno etal 893Laboratory and Clinical Studies on L-105, a New Cephem Antibiotic

Y. Shigeno etal 895In vitro Antibacterial Activity of L-105, a New Cephalosporin, against RespiratoryPathogenic Organisms, and Its Pharmacokinetic Properties

A. Takahashi et al 897L-105: In vitro Antimicrobial Activity and Therapeutic Efficacy on Lower RespiratoryInfections

A. Watanabe etal 899Fundamental and Clinical Studies of L-105 in Ophthalmologic Field

M. Ooishi etal 901Biliary Excretion, Tissue Concentration in Gallbladder, and Clinical Effects in PatientsTreated with L-105

N. Kobayashi etal 903Antimicrobial Activity and Clinical Efficacy of L-105

F. Miki etal .905Fundamental and Clinical Studies of L-105 in Obstetrics and Gynecology

N. Cho et al 907

vi CONTENTS

Safety and Pharmacokinetics of Intramuscularly Administered Cefpimizole(Ajinomoto-1370, Upjohn U-63196E) in Normal Human Volunteers

E. Novak etal 909Clinical Evaluation of AC-1370 in Complicated Urinary Tract Infections:A Double-blind Controlled Study with Cefoperazone

S. Nakamuta etal 910Antibacterial Activity of Cefpirome (HR 810) against Pathogens Involved in STDand Stability towards |3-Lactamases Produced by Neisseria gonorrhoeaeand Haemophilus ducreyi

E. Schrinner etal 912The in vitro Activity of HR 810 Compared with Four Other P-Lactam Antibiotics

E. Canton et al 914In vitro Activity of HR 810 Compared with Ceftazidime against AerobicGram-negative Bacteria

L. Steele-Moore and W. Holloway 916HR 810 and BMY-28142, Two New Cephalosporins with Broad-spectrum Activity:An in vitro Comparison with Other P-Lactam Antibiotics

A. M. Clarke etal 917Comparative in vitro Activity of BMY-28142 Alone and in Combination with Amikacinagainst Organisms Relatively Resistant to Gentamicin

D. Gerding et al. . 919Disposition of BMY-28142 in Cynomolgus Monkeys and Beagle Dogs

R. H. Barbhaiya etal. 921Antibacterial Activity of Cefodizime (HR 221)

W. Stille and S. Spieler 923The Interactions of Cefodizime with P-Lactamases

R. Labia etal '. . . 925In vitro Antibacterial Activity of a New Aminothiazolyl-oximino Cephalosporin:Cefodizime (HR 221) against 323 Gram-negative Rods Isolates:Comparison with Cefotiam, Cefoperazone, Cefotetan and Cefotaxime

P. Le Noc etal \ 927In vitro Antimicrobial Activity of Cefodizime (HR 221)

A. Raimondi et al 929Stimulation of Lymphocyte Cell Growth in vitro by the Cephalosporin-derivatives Cefodizime (HR 221) and Cefotaxime

W. E. G. Muller and G. Seibert 931Influence of Cefodizime (HR 221) on the Immune System

M. Limbert et al 933Bactericidal Activity of Cefodizime under Conditions Simulating SerumPharmacokinetic Parameters

P. M. Shah 935Cefodizime (HR 221): Pharmacokinetics in Healthy Volunteersafter 1 g i.v. Bolus, 1 g i.m.

G. Humbert etal 937Concentration of Cefodizime (HR 221), a New Cephalosporin in Urological Tissues

A. Hofstetter etal 939Cefodizime (HR 221), a New Aminothiazolyl Cephalosporin:First Clinical Results - Multicentric Study

P. Veyssier etal 941

CONTENTS vii

Comparative Therapeutic Effects of Cefodizime and Other Cephalosporinsin the Treatment of Experimentally Induced Pneumonia in Mice

N. Klesel etal 943A Comparative Study of Ceftazidime with Other Cephalosporins

Jia-Tai Li et al 945The Volume of Distribution of Ceftazidime in Normal, Fractured and Infected Bone

F. M. Anderson et al 947A Pharmacokinetic Study on Ceftazidime and Cefoperazone in HealthyChinese Volunteers

Jia-Tai Li et al 949Pharmacokinetics of Ceftazidime in Normal Subjects and Patients with Renal Failure

S. Vulterini etal 951Pharmacokinetics of Ceftazidime in Renal Insufficiency and during Haemodialysis

R. V. Dalen etal 953Pharmacokinetics and Clinical Use of Ceftazidime in Pediatrics

P. Begue etal 955Comparative Investigation of Serum Bactericidal Kinetics after Applicationof Ceftazidime and Ceftriaxone

U. Ullmann and M. Erttmann 957Comparative Randomized Blind Study on Ceftazidime vs Ceftazidime + Sisomicinvs Piperacillin + Sisomicin in Pseudomonas Pulmonary Exacerbations in Cystic Fibrosis

R. Padoan etal 959Treatment of Serious Infections in a Surgical Intensive Care Unit:Ceftazidime versus Cefotaxime and Piperacillin

E. Mueller etal 961Ceftazidime versus Cefazolin Plus Azlocillin in Therapy of NosocomialBronchopulmonary Infections

R. Serafin etal 963Clinical and Pharmacokinetic Study of Ceftazidime in the Treatment of PseudomonasInfections in Intensive-care Patients

R. Rondanelli etal \ 968Combined Action of Ceftazidime with Other Antibiotics and Inhibitionof Development of Secondary Resistance

C. Simon and M. Simon 970Pharmacokinetics of Intravenous Ceftazidime and Aztreonam in Crossover Studyin Humans

E. Yamaji etal 972Efficacy and Safety of Ceftazidime in the Treatment of Selected CancerPatients with Serious Infections

O. Quesada etal 974Evaluation of Ceftazidime in Pseudomonas Meningitis

C. Ezpeleta etal 976Ceftazidime in the Management of Severe Infections

A. Spantideas et al 978A Randomized Study of Ceftazidime Monotherapy versus Ceftazidimeand Cephalothin in Febrile Neutropenic Patients

R. S. G. Holdrinet etal 980Randomized Comparison of Ceftazidime versus Tobramycin Therapyfor Gram-negative Burn Wound Infection

H. G. Stiver etal 982

viii CONTENTS

Evaluation of Ceftriaxone Concentrations in Prostatic Adenoma Tissueafter Intravenous Single Dose Administration

R. Oertle etal 984Distribution of Ceftriaxone in Purulent Peritoneal Fluid, and in Lochiaduring Puerperium

D. A. Kafetzis etal 986Ceftriaxone Therapy of Osteomyelitis

A. D. Tice etal 988Pharmacokinetics of Ceftriaxone in Serum and Gynecological Tissues

P. De Grandi and J.-F. Bauen 990A Multicenter Trial on the Activity of Ceftriaxone in the Treatment of LowerRespiratory Tract Infections

C. Grassi 992Comparative Study between Two Third-generation Cephalosporins(Ceftriaxone-Cefoperazone) in the Treatment of Severe Infectious Dieases

J. P. Ducroix etal 994The Clinical Effectiveness and Compatibility of Ceftriaxone in Pediatric Surgery

A. F. Scharli and K. Briilhart 996Comparative Study of Ceftriaxone and Trimethoprim-Sulfamethoxazolefor the Treatment of Chancroid in Thailand

D. N. Taylor etal 998Serum Concentration and Elimination Half-life of Ceftriaxone inPatients with Severe Infections

F. Follath etal 1000Disposition of Ceftriaxone in Patients with Pleural Effusion

G. Benoni etal 1002Inpatient-outpatient Treatment of Serious Infections with a Single DailyDose of Ceftriaxone

L. Jauregui et al 1004A Comparative Trial of Ceftriaxone versus Cefamandole in the Therapyof Lower Respiratory Tract Infections in Elderly Men

W. C. Graham and R. B. Belshe 1006Cefonicid Pharmacokinetics in Normal Subjects and in Renal Insufficiency

J. P. Fillastre etal 1008Comparative Clinical Evaluation of Cefonicid in the Treatment of Urinary TractInfections Caused by Indole-positive Organisms

D. Ziv et al 1010In vitro Susceptibility of Various Species of Pseudomonas to Cefsulodin

G. Blandino etal 1012Cefsulodin/Tobramycin as Alternative Therapy for Serious Pseudomonas aeruginosaInfections Where a Penicillin Cannot Be Given

L. Crane etal ; 1014In vitro and Clinical Study of Cefsulodin against Pseudomonasand Opportunistic Bacteria

A. Limsuwan et al 1016Comparative Study of Cefsulodin and Conventional Anti-pseudomonal Therapyin the Treatment of Malignant External Otitis: A Retrospective Analysis

B. R. Meyers etal 1018

CONTENTS ix

Comparative Clinical Evaluation of Cefsulodin/Tobramycin andTicarcillin/Tobramycin in Serious Pseudomonas aeruginosa Infections

L. Crane etal 1020Cefpiramide: Antibacterial Activity, P-Lactamase Stability andDisk Diffusion Susceptibility Tests

A. L. Barry etal 1022Pharmacokinetics of Cefpiramide after Intravenous Administration

N. Nazari etal 1024Open Study of Intravenously Administered Cefpiramide in the Treatmentof Bacterial Infections in Hospitalized Patients

N. Nazari etal 1026Clinical Evaluation of Cefpiramide in Complicated Urinary Tract Infectionby Open Prospective Method

R. Sharifi etal 1028In vitro Study of the Susceptibility of Fresh Clinical Isolates to the Combinationof Cefoperazone Plus Sulbactam

D. Bechard etal 1030The Clinical and Experimental Study of the Biliary Excretion of Cefoperazonein Cases with External Biliary Fistula

H. Shimada etal 1032Elimination of Fecal Microflora by Cefoperazone Therapy in Patients

E. E. Ohnhaus etal 1034Cefoperazone versus Standard Combination Antibiotic Therapy for Gram-negativePneumonia and Nosocomial Aspiration Pneumonia

R. J. Mangi etal 1036Cefoperazone versus Clindamycin Plus Gentamicin for the Treatment of Obstetricand Gynecologic Infections

R. S. Gibbs etal 1038Outpatient Cefoperazone Therapy

L. J. Eron etal , 1040Studies on the Transfer of Cefotaxime into the Cerebrospinal Fluid in the Fieldof Neurosurgery

M. Sato and K. Echizenya 1042Studies on the Concentration of Cefotaxime in Tissues in the Field of Obstetricsand Gynecology

S. Hoshi etal 1044Concentrations of Cefotaxime and Desacetylcefotaxime in Synovial Fluid

A. Kazmierczak et al 1046Cefotaxime in Serious Infections Caused by Staphylococci

R. Blomer and K. Bruch 1048A Single-blind Comparative Study of Parenteral Cefotaxime and Oral Cefalexinin the Treatment of Patients with Uncomplicated, Non-obstructive Urinary TractInfections Caused by Susceptible Bacterias

O. Shobokshi and Y. Al-Saffi 1050Pharmacokinetic Studies of Cefmenoxime and Cefotaxime in Terms of Maternaland Fetal Plasma Concentrations, Placental Transfer, Protein Binding Rateand Tissue Concentration in Pelvic Organs

S. Tanaka et al 1053Dynamics of Cefmenoxime Ophthalmic Solution in Ocular Tissues andIts Clinical Application

K. Sasaki etal 1055

x CONTENTS

In vitro Antibacterial Activity of P-Lactam AntibioticsYu-kun Liu et al . 1057

A Laboratory Assessment of Eight P-Lactamase Stable CephalosporinsS. Esposito et al. 1059

Susceptibility of Haemophilus influenzae to First, Second, and Third GenerationCephalosporins

J. A. Daly etal 1061The Transfer of Cefmenoxime into Cerebrospinal Fluid: A Comparative Studybetween the Intravenous Bolus Injection and Intravenous Drip Infusion

S. Kashiwagi etal 1063Cefmenoxime — Pharmacokinetics in the Neonate

J. Sarangues et al 1065Pharmacokinetics of Cefmenoxime in Elderly Patients (60-90 Years Old)with a Normal Renal Function after 1.0 g i.v. Bolus

P. Veyssier etal 1067Comparative Studies on Bactericidal Activity, P-Lactamase Susceptibilityand Other in vitro Characteristics of Ceftizoxime

S. Selwyn and M. Bakhtiar 1069Bone Tissue Concentration of Ceftizoxime

T. Makiyama and T. Asai 1071The Comparative Efficacy of Ceftizoxime and Cefotaxime in Severe Infections

S. Segev etal 1073Activity of Cefmetazole Assessed by the Comparison of Timed Bacteriostaticand Bactericidal Concentrations

G. Masuda etal 1075Activity of Cefmetazole in Comparison to Cefoxitin and Cephalothin in vitroand in Treatment of Experimental Infections in Mice

R. V. Goering etal 1077Transference of Cefmetazole and Fosfomycin into Prostatic Tissues

S. Ra et al 1079Clinical Study of Cefmetazole in Respiratory Tract Infections

K. Nakagami et al 1081A Clinical Study with Cefmetazole

W. Holloway 1083Clinical Evaluation of Cefmetazole Alone in the Treatment of BacteremiaNot Responding to Other Antibiotics

C.-Y. Liu et al. 1085Clinical Evaluation of Cefmetazole in the Field of Urology

I. Miyagawa et al 1087Clinical Evaluation of Cefmetazole in Treatment of Complicated UrinaryTract Infection

T.-C. Tsai etal ; 1089Clinical Evaluation of Cefmetazole in Obstetrics and Gynecology

T. Chimura etal 1091Clinical Results with Cefmetazole in Gynecological and Obstetrical Infectionsand in Prophylactic Use after Surgery

M. Ozaki etal 1093Clinical Evaluation of Cefmetazole for Prophylaxis in Patients UndergoingGynecological Surgery

K. Fujiwara et al 1095

CONTENTS xi

Cefotetan and Cefmetazole Concentrations in the Tissue of Patientsat the Abdominal Operations

H. Furuhata etal 1097Biliary Pharmacokinetics and Gallbladder Bile Concentration ofCefotetan in Healthy Volunteers

A. Lanzini et al 1099Clinical Study on Penetration of Cefotetan into CSF

A. Hirayama et al 1101Comparative Study of Cefotetan versus Cefoxitin in the Treatment of AcuteBacterial Infections

H. K. Horsch 1103A Comparison of the Efficacy and Safety of Cefotetan with That of Moxalactamin the Treatment of Hospitalized Patients with Acute Lower RespiratoryTract Infections

T. M. Nolen etal 1104A Clinical Trial of Cefotetan in the Treatment of Severe Cervico-facial Infectionof Dental Origin

A. A. Quayle etal 1107Cefotetan in the Treatment of Anaerobic Infections: Clinical Efficacy and theComparison of Clinical Outcome with in vitro Susceptibility of Anaerobes

J. C. H. Lee and A. L. Barry 1109Comparative Pharmacokinetic Studies of Cefotetan and Other Cephamycin Antibiotics:Cefminox, Cefbuperazone, Cefmetazole, Cefoxitin, and Latamoxef

Y. Akieda etal 1111Pharmacokinetics of Patients with Serious Sepsis

S. D. Scott etal 1113Prophylactic Use of Cefotetan: A Long Acting Cephamycin for the Patientsunder Abdominal Surgery

M. Murata et al 1115The Use of Cefotetan in Surgical Prophylaxis

B. Mason et al. 1117Peritonitis, Septicaemia and Serious Intra-abdominal Infections:Research Experience with Cefotetan in a Surgical Controlled Clinical Trial

S. D. Scott etal 1119Cefotetan Concentration in Non-traumatic Joint Effusion

M. Bonadio etal 1121Clinical Evaluation of Cefotetan in Renourinary and Extraurinary Infections

G. F. Abbate etal 1123In vitro Activity, Pharmacokinetics, Safety and Therapeutic Efficacy of Cefotetanin Patients with Complicated Urinary Tract Infections

K. G. Naber etal 1125Cefotetan versus Moxalactam in the Treatment of Acute Bacterial LowerRespiratory Tract Infections

T. M. File etal 1127Clinical and Laboratory Studies of Cefbuperazone, a Long Acting Cephamycin,in a Suburban Community Hospital

T. Madhaven and D. Cunningham 1129Improved Outer Membrane Permeabilities of 6315-S and 2355-S in Escherichia coli

Y. Komatsu etal 1131

xii CONTENTS

Moxalactam in the Treatment of Nosocomial Infections: Clinical ExperienceP. Nikolaidis etal 1133

Chemistry and in vivo Activities of New Oral Prodrugs of a PotentAminothiazoloximino Cephalosporin

W. V. Curran etal 1135Antibiotic Activity of CL 118,673, a New Oral Cephalosporin

N. A. Kuck etal 1137Chemotherapeutic Efficacy and Pharmacokinetics of CGP 19 359,a New Oral Cephalosporin, in Experimental Animals

0 . Zak et al 1139Pharmacokinetics of CGP 19 359, a New Oral Cephalosporin

W. Tosch etal 1141Antibacterial Activities of FK 089, a New Oral Cephalosporin

T. Takaya etal 1143Pharmacokinetics of FK 089, a New Oral Cephalosporin, in Animals

Y. Mine etal 1145Pharmacokinetics and Safety of FK 089 in Healthy Volunteers

T. Suematsu et al 1147BMY 28100, a New Oral Cephalosporin: Synthesis and Structure-activityRelationships

T. Naito etal 1149Preliminary Laboratory Evaluation of BMY 28100

K. Tomatsu et al 1151BMY 28100, a New Oral Cephalosporin: Activity in vitro

F. Leitner etal 1153BMY 28100: Therapeutic Efficacy and Pharmacokinetics in Rodents

Y. H. Tsai etal 1155Clinical Studies of FK027, a New Oral Cephalosporin, in Respiratory TractInfections, and Its Pharmacokinetics

K. Konishi and M. Tamura 1157Treatment of Cholangitis Using New Orally Active Cephalosporin FK027:Its Basic Studies and Clinical Application

T. Shimizu et al 1159Experimental and Clinical Evaluation of FK027 Activity in the Treatmentof Urinary Tract Infections

H. Kishi etal 1161Clinical Usefulness of FKO27, a New Oral Cephalosporin, in the Treatmentof Urinary Tract Infections

K. Suzuki etal 1163Clinical Evaluation of FK027 on Urinary Tract Infections

Y. Ohi et al 1165Serum and Sputum Concentration and Clinical Results of FK027 on RespiratoryTract Infection

1. Hayashi 1167The in vitro and in vivo Antibacterial Activities of FK027, a New Orally ActiveCephalosporin

Y. Obana etal 1169Clinical and Experimental Study of FK027 for Otorhinolaryngological Infection

Y. Fujimaki etal 1171

CONTENTS xiii

Fundamental and Clinical Studies of FK027, a New Oral CephalosporinM. Yamamoto et al 1173

Clinical Study of FK027 in the Treatment of Respiratory Tract InfectionN. Aoki etal 1175

Antibacterial Activities of Ro 15-8074, a New Oral CephalosporinW. W. S. Ng et al 1177

T-2588, a Third-generation Oral Cephalosporin: Human PharmacokineticsJ. Shimada etal 1179

Clinical Study of a New Oral Antibiotic, T-2588 of the Cephems, in the Fieldof Internal Medicine

R. Soejima et al 1181Treatment of Urinary Tract Infections with T-2588, a New Oral Cephalosporin

Y. Kawada and T. Nishiura 1183Cefuroxime-axetil versus Augmentin: Pharmacokineties and Fecal Floraafter Multiple Doses over 8 Days

H. Langmaack et al 1185

§7. Penem and Penam Antibiotics

In vitro Antibacterial Activity of MK 0787 (iV-Formimidoylthienamycin), Aztreonam,Sultamicillin, Ceftazidime against Pseudomonas pseudomallei (Melioidosis)and Other Clinical Isolates

D. Tanphaichitra and S. Srimuang 1189The Superiority of Imipenem over Currently Available Anti-pseudomonal Antibioticsamong Community Hospital Clinical Pathogens of Resistant Pseudomonas aeruginosa

T. Madhavan and B. Fitzsimons 1191P-Lactamase Induction in Pseudomonas aeruginosa by Imipenem andIts Influence on Susceptibility Tests

D. M. Livermore 1193Penetration of Primaxin (iV-Formimidoylthienamycin and Cilastatin)into Human Cerebrospinal Fluid

D. H. Dealy etal 1195Penetration of Imipenem and Cilastatin into Cerebrospinal Fluid of Patientswith Bacterial Meningitis

J. Modai etal 1197Clinical and Microbiological Results of Treatment with Imipenem/Cilastatin

U. Hartenauer et al 1199Evaluation of Imipenem/Cilastatin in the Treatment of Severe Infectionsin Non-neutropenic Adult Patients

J. Garau etal 1201Comparative Efficacy of Imipenem (MK 787) Administered or in Combinationwith Cilastatin, a Dehydropeptidase Inhibitor (MK 791), in the Treatmentof Complicated Urinary Tract Infections

J. F. Acar etal 1203Imipenem (Thienamycin) Therapy of Perforated and Gangrenous Appendicitis

P. N. R. Heseltine etal 1205Bile and Tissue Concentrations and Clinical Efficacy of MK-0787/MK-0791in Surgical Infections

H. Tanimura etal 1207

xiv CONTENTS

Effect of Imipenem Prophylaxis on Colon Microflora in PatientsUndergoing Colorectal Surgery

L. Kager etal 1209Cilastatin-sensitive Lactamase Active on Carbapenem and Penem Antibioticsin the Lung of Rodents

R. Hajdu etal .1211Determination of Serum and Tissue Levels of Imipenem by HPLC

M. Erttmann etal 1213A Multiple Dose Pharmacokinetic and Treatment Study of Imipenem-Cilastatinin Patients with End-stage Renal Disease Undergoing Chronic Hemodialysis

S. Berman 1215Serum and Lung Tissue Concentrations of Imipenem

K. Unertl etal . . . . 1216Clinical Experience with Imipenem/Cilastatin in the Following of Surgical Treatment

P. Kempf et al 1218An Open Study on the Efficacy, Safety and Tolerance of an i.v. AdministeredImipenem/Cilastatin b.i.d. Regimen (2 X 1 g) in the Treatmentof Hospitalized Patients

M. Wenzel etal 1220Imipenem/Cilastatin Treatment of Multiresistant Pseudomonas aeruginosa LungInfection in Cystic Fibrosis

S. S. Pedersen etal 1223Imipenem in the Treatment of Septicemia

S. Breyer etal 1224Comparative in vitro Activity of SCH 34343 with 14 Antibiotics against100 Gram-negative Blood Isolates

H. Giamarellou etal 1226The in vitro Antibacterial Activity of SCH 34343 Compared with That ofOther P-Lactams

I. Phillips etal 1228Pharmacokinetics of SCH 34343 in Man

C. Lin et al 1230Comparison of the Efficacy and Safety of SCH 34343-Na with That of Cefamandolein the Treatment of Acute Lower Respiratory Tract Infection

L. A. Cone etal 1232A Comparison of the Efficacy and Safety of SCH 34343 and Cefamandole in theTreatment of Acute Respiratory Tract Infections

T. M. Nolen etal 1234Comparison of SCH 34343 with Cefotaxime in the Treatment of DifficultUrinary Tract Infections

C. E. Cox and D. L. Santomauro 1236Comparison of SCH 34343 with Cefoxitin in the Treatment of Skin and SkinStructure Infections

R. L. Nichols etal 1238Penem Antibiotic FCE 22891: Tissue and Body Fluid Distribution in Miceand Therapy of Experimental Diseases

D. Jabes etal 1240Activity of FCE 22101 on Gram-negative Bacteria Resistant to 3rd GenerationCephalosporins

C. Delia Bruna and A. Sanfilippo 1242

CONTENTS xv

Activity of the Penem FCE 22101 on Gram-negative Bacteria Induced for P-LactamaseA. Sanfilippo et al 1244

Susceptibility of Clinical Isolates to Temocillin, a Recently Introduced Penicillinwith Narrow Antimicrobial Spectrum

H. D. Heilmann and K. Kuhn 1246Clinical Evaluation of Temocillin in Serious Infections

P. D. Welsby etal 1248Temocillin Therapy of Patients with Hepatobiliary Infections

D. Tanphaichitra etal 1250The Activity of Temocillin, Amoxicillin/Clavulanic Acid and Ticarcillin/Clavulanic Acid: An Epidemiological Multicenter Survey in Eight Hospitals

G. Th. J. Fabius etal 1252Clinical Results and Pharmacokinetics of Temocillin in Surgical Patients

H. E. Klein etal 1254The Treatment of Gram-negative Infection with Temocillin lg 12-hourly

G. Lindsay etal 1256Miraxid® (Pivampicillin/Pivmecillinam) Evaluated: Four Clinical StudiesInvolving 794 Patients

E. C. Moorhouse etal 1258Therapy of Uncomplicated Gonococcal Urethritis with VD 2085

D. Tanphaichitra and O. Christensen 1260In vitro Synergistic Activity of Sulbactam and Cefoperazone against Aerobic Bacteria

D. N. Wright etal 1262Sulbactam-Ampicillin versus Moxalactam as an Adjunct to Surgeryin Acute Cholecystitis: A Preliminary Report

A. E. Yellin etal 1264Comparative Clinical Study of Sulbactam/Ampicillin and Clindamycin/Tobramycinin Polymicrobial Infections

B. V. Stromberg etal : 1266In vivo and in vitro Comparison of YTR 830 and Clavulanate Combined .with Amoxicillin against Staphylococcus aureus \

S. Aronoff et al 1268In vivo Comparison of YTR 830 and Clavulanate Combinedwith Amoxicillin against Citrobacter freundii and Proteus mirabilis

S. Aronoff etal 1270Inhibition of P-Lactamases, Binding to PBPs and MorphologicalChanges Affected by YTR 830, a New Penicillinate Sulphone

F. Moosdeen etal : . 1272YTR 830, a Novel P-Lactamase Inhibitor: Comparative in vitro and in vivo Studieswith Clavulanic Acid and Sulbactam

N. Ishida etal 1274Evaluation of New P-Lactamase Inhibitor YTR 830

M. D. Kitzis etal 1276Comparison of YTR 830, Sodium Clavulanate and Sulbactam Combinedwith Broad-spectrum Penicillins against P-Lactamase-producing Enterobacteriaceaeand Pseudomonas \

M. R. Jacobs etal . 1278Mutual Prodrugs of Ampicillin and 6P-Halopenicillanic Acids

W. von Daehne etal 1280

xvi CONTENTS

The Penetration of Amoxicillin and Clavulanic Acid into theCerebrospinal Fluid of Patients with Inflamed Meninges

J. S. Bakken etal 1282Clinical Evaluation of Augmentin Therapy in Anaerobic Infection of Skinand Soft Tissues

S. Balasubramaniam et al 1284Comparative in vitro Activity of Amoxicillin/Potassium Clavulanateand Imipenem/Cilastatin against Anaerobic Bacteria Isolated from Community Hospitals

E. J. C. Goldstein and D. M. Citron 1286Resistance to P-Lactam Antibiotics and to Combinations of Amoxicillin/ClavulanicAcid (Augmentin) and Ticarcillin/Clavulanic Acid (Timentin): Distributionof Phenotypes in Enterobacteriaceae

D. Sirot etal. ..'. 1288Pharmacokinetics of Augmentin and Timentin in Ear- and Eye-Fluids and in Serum

P. J. Federspil etal 1290Pharmacokinetic Studies on Clavulanate Potentiated Ticarcillin (Timentin)in Normal Subjects and Patients with Renal Insufficiency

P. Koeppe etal 1293Timentin: Pharmacokinetics and Clinical Results in Surgical Patients

R. R. Wittke and D. Adam 1295Comparison of Ticarcillin-Clavulinic Acid Combination with Cefazolinin the Treatment of Soft Tissue Infections

H. Katner etal 1297Timentin (BRL-28500) in the Treatment of Complicated Adult UrinaryTract Infections

R. Gebhart etal 1299Timentin: In vitro Efficacy against 712 Isolates of Aerobic-anaerobic Bacteria

M. B. Bansal etal 1301Comparative Evaluation of the in vitro Activity of Ticarcillin and Ticarcillin-ClavulanicAcid in Hospital Practice

V. Jarlier etal 1303Antibacterial Activity of Timentin according to Patterns of Susceptibilityto p-Lactam Antibiotics and Strain Origin

T. Fosse etal 1305Inttvitro Bactericidal Activity of Clavulanate/Ticarcillin Combinations

I. M. Gould etal 1308Pharmacokinetics of Antibiotis Combined with P-Lactamase Inhibitors in Patientswith Renal and/or Hepatic Dysfunctions

Y. Usuda etal 1310In vitro and Clinical Evaluation of Intravenous Timentin in Soft Tissue Infections

B. Rao et al 1312The Use of Timentin in the Treatment of Moderate and Severe Infections

J. D. Price etal 1314A Randomized Study Comparing Timentin with Piperacillin and TobramycinTreatment of Septicemia and Lower Respiratory Infections

D. Winslow and W. Holloway 1316Timentin: Clinical Experiences in German Hospitals

J. Johnsen et al 1318

CONTENTS xvii

Timentin Compared to Tobramycin-Piperacillin Combination as Empiric Therapyin Serious Infections in Hospitalized Patients

T. Madhavan etal 1320The Use of Clavulanate Potentiated Ticarcillin in Neonatal Sepsis

M. F. Smith etal 1323BRL 28500 (Ticarcillin + Clavulanic Acid) in the Pre- and Peri-operativeTreatment of Complicated Urinary Tract Infection

M. Westenfelder etal 1325Ticarcillin/Clavulanic Acid Treatment of Gynecological Infections with SpecialReference to the Blood and Tissue Concentrations

K. Gutschow etal 1327

§8. Monobactams

Pharmacokinetics of Carumonam in Patients with Renal InsufficiencyK. Stoeckel etal 1331

Kidney Tolerance of Monobactam (Ro 17-2301), Flucloxacillin and the Combinationof Both Using Parameters for Proximal and Distal Tubular Injury

A. W. Mondorf etal 1333Single Dose Pharmacokinetics and Absolute Bioavailability of the New MonocyclicP-Lactam Carumonam (Ro 17-2301, AMA-1080)

E. Weidekamm etal 1335In vitro Activity of the Monobactam Ro 17-2301 Compared with Aztreonamand Other P-Lactam Antibiotics

D. A. Bremner 1337An E. coli Strain Which Developed Resistance to Aztreonam But Not to Carumonam(Ro 17-2301): Resistance Development Kinetics and P-Lactamase

M. Arisawa etal 1339In vitro Activity of Ro 15-8074, SQ 82291 and Ro 17-2301 vs Other P-Lactams against300 Recent Nosocomial Pathogens

K. Kanellakopoulou et al 1341Comparative in vitro Evaluation of Ro 17-2301, a New Monobactam Antibiotic

J. LeFrock etal 1343Comparative Activity of Ro 17-2301, HR 810, Ceftazidime and Aztreonam for ResistantPseudomonas aeruginosa

S. M. Smith and R. H. K. Eng 1345In vitro Evaluation of Ro 17-2301, a New Monobactam Antibiotic

E. E. Stobberingh etal 1347The in vitro Activity of Ro 17-2301 against Pseudomonas Clinical Isolatesin Comparison to Aminoglycosides and Aztreonam

A. Georgopoulos et al 1349In vitro and Clinical Evaluation of Ro 17-2301, a New iV-Sulfo P-Lactam Antibiotic,in Severe Urinary Tract Infections

C. A. Barclay etal 1351Oral Monobactams. Chemistry of [(2-Oxo-l-azetidinyl)oxy]acetic Acidsand Prodrug Esters Thereof: An Overview

H. Breuer 1353Oral Monobactams: Comparative in vitro Activity of SQ 82,291and Other Antimicrobial Agents

A. G. Paradelis etal 1355

xviii CONTENTS

Penetration of Aztreonam into Tissues and Fluids of the Female GenitalTract in Patients Undergoing Surgery

D. Vernant et al 1359Concentrations of Aztreonam in Serum, Muscle, Fat and Renal Tissue

M. Westenfelder et al 1361Monobactam Metabolism in Patients with Biliary Tract Infection Relatedwith Its Fundamental and Clinical Study

T. Saito etal 1363In vitro and in vivo Effects of Aztreonam and Placebo on Platelet Functionand Bleeding Time in Normal Volunteers

T. A. Tartaglione et al 1365Aztreonam, an Alternative P-Lactam in Patients with Hypersensitivity to Penicillinsand Cephalosporins

W. Graninger etal 1367Clinical Experience with Aztreonam

J. Righter etal 1369Treatment of Gram-negative Septicaemia with Aztreonam

S. Lauwers et al 1371Therapeutic Effect of Aztreonam for Severe Infections Associatedwith Hematological Disorders

T. Masaoka etal 1373Evaluation of Aztreonam in an Implantable Drug Pump for the Treatmentof Gram-negative Osteomyelitis

C. R. Perry etal 1375Treatment of Acute Pelvic Inflammatory Disease with Aztreonam Plus Clindamycin

M. G. Dodson etal 1377Multicentre Comparative Study between Aztreonam (o.d.) and Gentamicin (b.i.d.)in Renal and Urinary Tract Infections Treatment

A. Albertazzi etal 1379Experience with Some New Antibiotics in Urinary Tract Infections

M. S. Sabbour etal 1381Well-controlled Comparative Study on Aztreonam and Cefoperazone in the Treatmentof Complicated Urinary Tract Infections

H. Ohmori etal 1383Randomized Comparison of the Efficacy and Safety of Aztreonam vs. Cefuroximein the Treatment of Serious Gram-negative Urinary Tract Infections and SerumPharmacokinetics of Aztreonam in Patients

G. Friman et al 1385Aztreonam: European Experience in the Treatment of Pediatric Patientswith Gram-negative Infections

D. Adam 1387Efficacy of Aztreonam in the Treatment of Gram-negative Rod Bacteremiaand Meningitis

P. McKellar 1390Studies of Aztreonam in Cancer Patients

G. Bodey etal 1392Sensitivity to Aztreonam in 2613 Strains of Enterobacteriaceaeat a Norwegian County Hospital

E. Holten 1394

CONTENTS xix

The P-Lactamase Stability and in vitro Activity of Aztreonam, with a Comparisonto 9 Other P-Lactam Antibiotics and Gentamicin

H. Friis etal 1396Clinical Evaluation of Aztreonam in Severe Urinary Tract Infections

P. J. Van Cangh etal 1398Aztreonam in the Therapy of Nosocomial Infections in High Risk Patients

P. Cristiano et al 1400

§9. Macrolide Antibiotics

In vitro Susceptibility of Streptococci and Staphylococci from Clinical Materialto a Novel Macrolide: RU 28965

E. Debbia etal 1405In vitro Activity of RU 28965 Evaluated by the Agar Dilution Methodsand MS-2-research System

P. Periti and P. Nicoletti 1407In vitro Activity of RU 28965, a New Macrolide, in Comparison with Erythromycinand Ampicillin against Haemophilus spp.

G. Nicoletti etal 1409In vitro Activity of RU 28965, a New Macrolide, against Chlamydia trachomatisand Ureaplasma urealyticum

R. Cevenini et al 1411In vitro Effect of RU 28965 and Other Macrolide Antibiotics on HumanNeutrophil Functions

A. Fietta etal 1413Synergy between RU 28965 and Human Neutrophils on Bactericidal Activity in vitro

M. T. Labro etal 1415Pharmacokinetic Properties of the New Macrolide RU 28965 in Animals

J. F. Chantot and A. Bryskier 1417In vitro Susceptibility of Ureaplasma urealyticum to RU 28965 Comparedto Erythromycin and Josamycin

C. Bebear etal 1419Influence of Food on the Absorption of RU 965, a New Macrolide Antibiotic,from Film-coated Tablets in Healthy Men

H. B. Lassman etal 1421Safety, Tolerance, and Pharmacokinetics of Single and Multiple Oral Doses ofRU 965, a New Macrolide Antibiotic, in Healthy Men

S. K. Puri etal. 1423Bacteriological Evaluation of a New Macrolide Antibiotic, Rokitamycin (TMS-19-Q)

T. Morohoshi et al 1425Metabolism of Rokitamycin (TMS-19-QJ, a New 16-Membered Macrolide Antibiotic,and Effects of Its Metabolites on Plasma Level as Total Activity

T. Suzuki etal 1427Formulation Design of Rokitamycin (TMS-19-Q) Tablet and Its Evaluation

M. Morishita etal 1429Clinical Effect of Rokitamycin (TMS-19-Q): Comparison of Different Formulations

K. Hara etal 1431In vitro Anti-mycoplasmal Activity of Miocamycin: MIC and Sub-MIC Study

P. M. Furneri etal 1433

xx CONTENTS

In vitro Antibacterial Activity of MiocamycinA. Yoshida etal 1435

The Activity of Miocamycin against Chlamydia trachomatis and Mycoplasmas in vitroG. L. Ridgway etal 1437

Anti-staphylococcal Activity of MiocamycinA. Repetto etal 1439

Effects of Miocamycin on Bacterial Surface and Its Relationship with AdherenceP. Mastroeni et al 1441

Miocamycin versus Professional Phagocytic CellsL. Bonina et al 1444

Plasma and Tissue Concentrations of Miocamycin in HumansF. Fraschini etal 1447

Absorption and Excretion of Miocamycin Tablets and Dry SyrupK. Fukaya etal 1450

Single and Multiple Dose Pharmacokinetics and Tolerance of Miocamycinin Healthy European Volunteers

S. W. Sanders etal 1452Miocamycin for the Management of Respiratory Tract Infections

R. Rimoldi etal 1454Efficacy and Tolerability of Miocamycin: A New Macrolide in Pediatrics

0 . Olivi 1457Results Obtained with Miocamycin in the Treatment of Pyodermas in Children

1. Obadia 1461Clinical Effect of Miocamycin on Whooping Cough

Y. Sakata etal. 1463Miocamycin in the Therapy of Pertussis, Scarlet Fever and Mycoplasma pneumoniaeInfections in Children

A. Ulivelli etal 1465Usefulness of Miocamycin in the Treatment of Surgical Infections

R. Germiniani \ 1467Miocamycin Treatment of Otorhinolaryngological Infections

G. Catalano etal 1470Susceptibility of Clinical Isolates to Josamycin, Erythromycin and Penicillin

A. Wildfeuer etal 1473Effect of Josamycin on the Phagocytic and Microbicidal Function of Leukocytes

G. Privitera etal 1476Activity of Josamycin in Human Tissue and Neutrophils

A. Wildfeuer etal 1478Influence of Josamycin on Caffeine Disposition in Human Healthy Volunteers

J. Descotes et al 1481Effects of Food on Bioavailability of Josamycin and Josamycin Propionate

C. Ikeda etal 1483Clinical Studies with Josamycin in Adults and Children

A. J. Moritz 1485Rational Basis of Antibiotic Therapy in Acute Pulmonary Infections in Children

M. Solbiati etal 1488Mycoplasma pneumoniae Pneumonia: Clinical Aspects and Therapeutical Problems

F. De Rosa etal 1490

CONTENTS xxi

Clinical Experience with Josamycin in the Therapy of Mycoplasma pneumoniaePneumonia

H. Kobayashi 1492In vitro Studies and Clinical Effect of Josamycin in Mycoplasma pneumoniae Pneumonia

S. Ogawa etal 1494Clinical Evaluation of Josamycin Treatment in Mycoplasmal pneumonia in Children

T. Fujimoto et al 1496Josamycin in the Treatment of Papulo Pustular Acne

E. Rampini et al 1498Prophylactic Josamycin for Traveller's Diarrhoea

J. P. Ghanassia etal 1500Josamycin and Host Defense

A. Wildfeuer 1502Efficacy of Josamycin in the Treatment of Infections of the Respiratoryand Ear, Nose and Throat Tracts

B. Wassmer etal 1505Spiramycin Half-life within Macrophages, Spleen, Thymus, and Liver Tissues in vivo

S. Kernbaum et al 1507In vivo Effects of Spiramycin on Non-specific and Specific Immunity

M. Levacher etal 1509Susceptibility of Anaerobic Bacteria to Eight Macrolides and Related Drugs

C. Quentin et al 1511

§10. Quinolone Antibacterials

In vitro Antibacterial Activity of AT-3295, a New Pyridonecarboxylic Acid DerivativeS. Nakamura et al 1515

In vivo Effect of AT-3295 against Experimental InfectionsA. Minami et al 1517

AT-3295, a New Pyridonecarboxylic Acid Derivative with Potent Antibacterial Activity:Synthesis and Structure-activity Relationships

J. Matsumoto et al 1519In vitro Evaluation of Two New 4-Quinolones: S25930 and S25932

D. Felmingham et al 1521Resistance Studies with Two New 4-Quinolones: S25930 and S25932

D. Felmingham etal 1523CI-934: A New Antistreptococcal Quinolone - In vitro and Chemotherapeutic Studies

E. L. Marcus and C. L. Heifftz 1525Evaluation of the Activity of A-56619 and A-56620, Two Novel QuinoloneAntimicrobial Agents, on Aerobic Microorganisms

B. Gordts etal 1527In vitro Evaluation of Two Quinolones, A-56619 and A-56620

A. L. Barry etal 1529Spectrum and Antibacterial Activity of Abbott A-56619 and A-56620 in Comparisonto Other Quinolones

P. M. Shah etal 1531In vitro Activity of A-56619 and A-56620 Compared to Ciprofloxacin, Norfloxacin,and Vancomycin

S. G. Kelley etal 1533

xxii CONTENTS

In vitro Antibacterial Activity of Aryl-fluoro Quinolones A-56619 and A-56620against Routine and Multi-resistant Clinical Isolates

V. Ackerman et al 1535Comparative in vitro and in vivo Potencies of A-56619, Ofloxacin, and Ciprofloxacin

P. B. Fernandes etal 1537Comparative in vitro and in vivo Potencies of A-56620, Ofloxacin, and Ciprofloxacin

D. Chu etal 1539Treatment of Experimental Pneumonia due to Pseudomonas aeruginosa in NeutropenicGuinea Pigs with a Quinolone (Abbott-56619)

J. Kapusnik et al 1541In vitro and in vivo Activity of Ciprofloxacin (BAY o9867): A New Quinoline Derivative,Alone and in Combination against Various E.coli, Mycobacterium and Salmonella Strains

M. Rosenfeld and J. K. Seydel 1543Ultrastructure and Reversion of Bacterial Filaments Produced with Ciprofloxacin

V. Lorian et al 1545Influence of Media and Method on the in vitro Susceptibility of Pseudomonas aeruginosaand Other Bacteria to Ciprofloxacin and Enoxacin

J. Blaser etal 1547In vivo Efficacy of Ciprofloxacin Compared with Cefbuperazone, Cefoperazoneand Cefoxitin in the Treatment of Experimental Intra-abdominal Abscess

M. B. Bansal etal 1549Comparative Efficacy of Ciprofloxacin, Azlocillin and Tobramycin Aloneand in Combination in Experimental Pseudomonas Sepsis

M. Johnson et al 1551Comparison of the Efficacy of Ciprofloxacin, BMY 28142 and Ceftazidimein the Therapy of Experimental Pseudomonas aeruginosa Endocarditis in the Rat:Importance of the Dosing Interval

M. J. Ingerman et al 1553Ciprofloxacin Alone and Combined with Azlocillin, Ceftizoxime, and Amikacin,against Gram-negative Bacilli in a Neutropenic Site Model

L. R. Peterson etal 1555Bactericidal Activity of Ciprofloxacin against Amikacin-resistant Gram-negativeBacilli and Methicillin-resistant Staphylococcus aureus

M. S. Simberkoff and J. J. Rahal, Jr 1557Comparative Activity of Ciprofloxacin (BAY o9867) with P-Lactam Antibioticsand Gentamicin, and the Effect of Inoculum Size, against Aerobic Gram-positiveand -negative Bacteria

K. E. Aldridge etal 1559Evaluation of Ciprofloxacin and Cefotaxime in the Treatment of ExperimentalSubcutaneous Abscess in Mice Due to Aerobes

H. Thadepalli etal 1561The Effect of Ciprofloxacin on the Viability and Morphology of Methicillin-resistantStaphylococcus aureus

S. M. Smith etal 1563Comparative in vitro Activity of Ciprofloxacin

A. Fernandez et al 1565In vitro Activity of Ciprofloxacin against Multi-resistant Staphylococciand Gram-negative Rods

C. Fernandes et al 1567

CONTENTS xxiii

In vitro Activity of Ciprofloxacin (BAY o9867) and Three Other Antibiotics againstMultiresistant Strains of Pseudomonas

G. S. R. Davies and J. Cohen 1569Antibacterial Activity of 19 Antimicrobial Agents and Kill Kinetics of CiprofloxacinPlus Ampicillin against Gentamicin-resistant and High-level-resistant Enterococci

H. Grimm 1571The Effects of Oral Ciprofloxacin on the Faecal Flora of Healthy Volunteers

H. A. Holt etal 1573Pharmacokinetics of Ciprofloxacin in Healthy Volunteers after Oraland Intravenous Administration

K. Borner etal 1575Ciprofloxacin Pharmacokinetics in Renal Failure

E. Singlas etal 1577Penetration of Ciprofloxacin into Bone Tissues

R. Braun etal 1579Ciprofloxacin Concentrations in Tonsils Following Single and Repeated Administration

N. Falser etal 1581Penetration of Ciprofloxacin into Nasal Secretions

U. Ullmann etal 1583Effect of the Gastric Emptying Time on Rate and Extent of the Systemic Availabilityof Ciprofloxacin (BAY o9867) in Humans

W. Wingender etal 1585A Clinical and Pharmacokinetic Study of Ciprofloxacin Administered Chronicallyas i.v. Bolus Doses to Young Healthy Volunteers

D. B. Jack etal 1587Biliary Elimination of Ciprofloxacin in Man: A Comparative HPLCand Microbiological Evaluation

J. M. Brogard etal 1589Excretion of Intravenous and Oral Ciprofloxacin in Biliary Disease

C. J. L. Strachan and B. T. Thorn 1591A Study of Ciprofloxacin Kinetics in Various Body-fluid Compartments

G. Petrikkos etal 1593Penetration of Ciprofloxacin into Female Genital Tract Tissues

E. Goormans et al 1595Ciprofloxacin Concentrations in the Female Genital Tract Organs

S. Segev etal 1597Ciprofloxacin Pharmacokinetics in Patients Undergoing Gastrointestinal Surgery

S. H. Silverman etal 1599Pharmacokinetics of Oral Ciprofloxacin, 100 mg Single Dose, in Volunteersand Elderly Patients

A. P. Ball etal 1601Multiple-dose Pharmacokinetics and Tissue Penetration of Ciprofloxacin,500 mg t.i.d.

M. LeBel etal 1603Interactions on the Gastrointestinal Absorption of Ciprofloxacin

G. Hoffken etal 1606Pharmacokinetic Properties of Ciprofloxacin in Intensive Care Patientswith Acute Renal Failure (Preliminary Data)

M. Dirksen etal 1608

xxiv CONTENTS

Diffusion of Ciprofloxacin in the Human Prostatic Tissue after Oraland Intravenous Administration

K. Schalkhauser et al 1610Tissue Distribution of Ciprofloxacin Following Oral and Intravenous Administration

H.- U. Eickenberg and A. Dalhoff 1612The Penetration of Ciprofloxacin after Single Oral Dose in Normal and Infected Bones

I. W. Fong,e< al 1614Ciprofloxacin Pharmacokinetics in Patients with Impaired Renal Function

D. B. Webb etal 1616Pharmacokinetics of Ciprofloxacin: Study of Its Distribution in the RespiratorySecretions

E. Bergogne-Berezin et al 1618Penetration of Ciprofloxacin into Human Lung Tissue Following a Single IntravenousAdministration

D. Schlenkhoffetal 1620Single Dose Pharmacokinetics of Oral Ciprofloxacin in Patients with Cystic Fibrosis

J. Goldfarb etal 1622Ciprofloxacin in Acute Exacerbations of Chronic Bronchitis

S. Klein etal 1624Ciprofloxacin in Purulent Exacerbations of Chronic Bronchitis:A Clinical, Microbiological and Pharmacokinetic Study

B. I. Davies etal 1626Non-comparative Study of Ciprofloxacin in Respiratory Tract Infection

S. Mehtar etal 1628Evaluation of the Clinical Efficacy and Safety of Ciprofloxacin (BAY o9867)in the Treatment of Respiratory Tract Infections

D. A. Campbell and R. M. du Bois 1630Ciprofloxacin in the Outpatient Treatment of Urinary Tract Infections

S. J. Childs 1632In vivo Efficacy of Ciprofloxacin Compared with Contrimoxazole in the Treatmentof Urinary Tract Infection in Hospital

A. H. Williams and R. N. Griineberg 1634Comparative Efficacy and Safety of Ciprofloxacin (Bay o9867) and Cotrimoxazolein the Treatment of Patients with Complicated Urinary Tract Infections

J. Boerema et al 1636Clinical Experience with Ciprofloxacin in the Treatment of Complicated Urinary 'Tract Infections

K. Schalkhauser and A. Dalhoff 1638Ciprofloxacin in the Treatment of Patients with Symptomatic and AsymptomaticUrinary Tract Infections: A Comparative Study of Single-dose Application versusThree-day Treatment Concerning Efficacy and Safety

F. Fischbach etal 1640Treatment of Uncomplicated Gonococcal Urethritis in Men with Ciprofloxacin250 mg and 500 mg in One Dose Orally in an Open Randomized Study

M. Tegelberg-Stassen et al 1642The in vitro Activity and Clinical Role of Ciprofloxacin: Observations duringTreatment of Patients with Systemic and Urinary Tract Infections Due toGram-negative Bacilli

M. F. Parry 1644

CONTENTS xxv

Treatment of Severe Complicated Urinary Tract and Tissue Infectionswith Ciprofloxacin

D. A. Leigh and F. X. S. Emmanuel 1646Ciprofloxacin versus Placebo in the Treatment of Acute Bacterial Diarrhoea

H. Pichler etal 1648Ciprofloxacin in the Treatment of Chronic Salmonella Carriers

G. Diridl etal 1650Ciprofloxacin Treatment of Infections Caused by Gram-negative Bacilli orStaphylococcus aureus

R. N. Greenberg etal 1652Clinical Efficacy and Safety of Oral Ciprofloxacin

R. J. Fass 1654The Efficacy and Safety of Ciprofloxacin in Patients with Serious Infectionsof Selected Tissues

T. M. Nolen etal 1656Efficacy of Ciprofloxacin in the Treatment of Tissue Infections: An Open,Prospective Study

C. R. Meji'a etal 1658Clinical and in vitro Evaluation of Ciprofloxacin in the Treatment of Multi-resistantGram-negative Infections

S. Mehtar etal 1660Distribution Kinetics of Ciprofloxacin for Evaluation of Therapeutic Efficacy inPseudomonas Bronchopneumonia in Cystic Fibrosis Patients

S. W. Bender etal 1662Therapy of Infections with Ciprofloxacin

L. J. Eron etal 1664Ciprofloxacin Therapy in Patients with Pseudomonas Infections

F. Follath etal 1666Ciprofloxacin in the Treatment of Soft Tissue Infections and Osteomyelitis:Pharmacokinetics, Safety and Efficacy

D. E. Nix et al .\ 1668Ciprofloxacin: in vitro Activity and Clinical Use in Osteomyelitis Due to ResistantOrganisms

E. S. Johnson etal 1670Pilot Study of Ciprofloxacin in the Treatment of Pseudomonas aeruginosaInfection in Cystic Fibrosis

M. E. Hodson etal 1673Pseudomonas aeruginosa Infections Treated with Ciprofloxacin

G. A. Pankey etal 1675Evaluation of Ciprofloxacin in the Treatment of Severe Infections in Non-neutropenicPatients

F. Parras etal 1677Treatment of Pneumonia with Ciprofloxacin

H. Bassaris et al 1679RTI Patients Treated with Ciprofloxacin or Cefalexin: A Randomized Comparison

N. Vetter etal 1681Ciprofloxacin: Efficacy in Eradicating Campylobacter from Marmosetsand Pharmacokinetic Data

L. J. Goodman etal 1683

xxvi CONTENTS

The Efficacy and Tolerability of Ciprofloxacin in Geriatric Plurimorbid PatientsSuffering from Urinary Tract Infection

J. P. Cassiers etal 1685Ciprofloxacin in the Treatment of Non-complicated Gonococcal Urethritis

L. Belli etal 1687Intravenous Treatment of Urinary Tract Infections with Ciprofloxacin and Mezlocillinby a Comparative Clinical Study

H. J. Peters 1689Ciprofloxacin in the Treatment of Urinary Tract Infections Caused by Pseudomonasaeruginosa and Multiresistant Strains: Initial Report

C. H. Ramirez-Ronda etal 1691Clinical Efficacy of Ciprofloxacin in Difficult-to-treat Outpatients Sufferingfrom Urinary Tract Infections and Prostatitis

C. Zamfirescu and V. Chysky 1693Efficacy and Safety of Ciprofloxacin vs Bactrim (SMZ/TMP) in the Treatment of UTI(PN) Patients: A Randomized Study

R. Schmicker et al 1695Clinical, Microbiological and Pharmacokinetic Aspects of Ciprofloxacin in Therapyof Wound Infections after Vascular Surgery

B. Steckmeier et al 1697Clinical Evaluation of Ciprofloxacin in Bacterial Ocular Infections

M. Ooishi etal 1699Ciprofloxacin (BAY o9867): A Clinical Evaluation and Assessment of Its Effecton the Faecal Flora

M. Whitby etal 1701In vitro Activity of Pefloxacin Alone or in Combination on Multi-resistantStaphylococcus aureus Strains

C. J. Soussy etal 1703In vitro Bactericidal Activity as a Function of Time of Combinations of Pefloxacinwith Aminoglycosides and Pefloxacin with P-Lactam Antibiotics

A. Thabaut etal 1706Pefloxacin Concentrations in Sputum and Blood in Patients with Chronic ObstructiveBronchitis

I. Zimmermann et al 1708Penetration of Pefloxacin in Human Heart Valves

N. Brion etal 1711The in vitro Activity of Pefloxacin Compared with Three Quinolones, ThreeAminoglycosides and Three Cephalosporins against 500 Clinical Isolates

Y. J. Drabu etal 1713Pefloxacin Inhibits Multiplication of Legionella pneumophila within Human Macrophages

J. L. Vilde etal 1715Pefloxacin as a Substitute for Conventional Therapy in Uncontrolled Staphylococcusaureus Infections

C. J. L. Brian Buisson et al 1717Treatment of Chronic Osteomyelitis Due to Staphylococcus spp. or Gram-negativeBacteria with a New Quinolone: Pefloxacin

N. Desplaces etal 1719Single Dose Prophylaxis with Pefloxacin: Serum and Tissue Pharmacokineticsand Clinical Effect in Women Undergoing Hysterectomy

E. E. Petersen etal 1721

CONTENTS xxvii

Pefloxacin for Treatment of Experimental LegionellosisE. Dournon etal 1723

Evaluation of Enoxacin Activity against Recent Clinical IsolatesI. Covelli etal 1725

In vitro and in vivo Elimination of Plasmid-borne Antibiotic Resistance by EnoxacinS. A. Sonstein etal 1727

Enoxacin: Chemotherapeutic Evaluation as a Parenteral and Oral Agent againstHospital-derived Bacteria

C. L. Heifetz etal 1729Enoxacin vs. Vancomycin Treatment of Methicillin-resistant Staphylococcus aureusExperimental Endocarditis

J. A. Boscia etal 1731Effect of Food on the Oral Absorption of a Single 400 mg Dose of Enoxacin in Men

A. Somogyi et al 1733Pharmacokinetics and Penetration of Enoxacin into Sputum

B. R. Dobbs etal 1735Enoxacin Concentration in Human Prostatic Tissue after Oral Administration

S. Rannikko and A.-S. Malmborg 1737Evaluation of Biliary Pharmacokinetics of Oral Enoxacin, a New Quinolone Antibiotic

A. Flowerdew etal 1739An Open Study of the Safety and Efficiency of Enoxacin (CI919) in ComplicatedUrinary Tract Infections

G. Williams etal 1741Clinical and Bacteriological Experiences with Enoxacin Treatment in Urinary TractInfections in Elderly Patients and Patients under 65 Years

M. Huttunen et al 1743Enoxacin for the Treatment of Urinary Tract Infection

R. R. Bailey and B. A. Peddie 1745Enoxacin in the Treatment of Urinary Tract Infections

R. N. Wyndham etal 1747Enoxacin: Pharmacokinetics and Therapy of Urological Patients with ComplicatedUrinary Tract Infections

K. G. Naber etal 1749A Comparison of Enoxacin and Cephalexin in the Treatment of Patientswith Skin and Skin Structure Infections

L. E. King, Jr. and C. G. Vire 1751Enoxacin in Bacterial Skin Infection: A Bacteriologically Controlled Clinical Study

H. Mensing 1753Enoxacin Clinical and Pharmacokinetic Studies in Ear, Nose, and Throat Infections

P. J. Federspil etal 1755In vitro Efficacy of Ofloxacin against Gram-negative Upper RespiratoryTract Pathogens

D. Isaacson et al 1757Bactericidal Activity of Ofloxacin in Human Blood

P. M. Shah and C. Juttner 1759Comparative in vitro Activity of Ofloxacin (DL-8280) and Other AntimicrobialAgents against Enteric and Miscellaneous Bacteria

S. Wongwanich et al 1761Interpretive Criteria for the Agar Diffusion Susceptibility Test with Ofloxacin

K. Grimm and H. Grimm 1763

xxviii CONTENTS

Pharmacokinetics of Ofloxacin in Serum and Skin BlisterT. Kalager etal 1765

The Concentration of Ofloxacin in Human Prostatic Tissue and FluidH. Kumon etal 1767

Absorption and Excretion of Ofloxacin in Patients with Impaired Renal FunctionM. Tsugaya et al 1769

Ofloxacin: in vitro Activity and Concentrations in Plasma, Urine and ProstaticAdenoma Tissue in Elderly Patients

K. G. Naber etal 1771Ofloxacin: Bactericidal Effect in an in vitro Pharmacokinetic Model

L. Xerri et al. 1773In vivo Studies with Ofloxacin

W. Ritzerfeld etal 1775Ofloxacin: Efficacy in Renal and Subcutaneous Abscess Models in Mice

M. Sato etal 1777Comparative in vitro Activity of Ofloxacin, Cefotaxime, Ceftazidime, Gentamicin,and Netilmicin against 3,965 Clinical Isolates

M. Steinbakk etal 1780Antibacterial Activity of Ofloxacin (DL 8280), a New Quinoline Derivative, againstGram-negative and Gram-positive Bacteria

G. Ravizzola et al 1781Pharmacokinetics of Ofloxacin in Humans after Various Single Oral Doses

S. Flor etal 1783Pharmacokinetics of Ofloxacin in Humans after a Single 100 mg Doseand during Multiple 300 mg b.i.d. Administration

S. Flor etal 1785Pharmacokinetics of Ofloxacin in Healthy Volunteers after Oral Administration

G. Humbert etal 1787Pharmacokinetics of Ofloxacin in Normal Subjects and in Patients with Mildto Moderate Renal Insufficiency

E. Arosio etal 1789Ofloxacin: Clinical and Pharmacokinetic Study in Health and Disease(Preliminary Data)

S. Vulterini etal 1791An Appraisal of Ofloxacin Level in Semen

H. Mizoguchi etal 1793Diffusion of Ofloxacin into Human Lung Tissue

L. Couraud et al 1795Clinical Experience with Ofloxacin in Severe Hospital Infections

M. Solbiati etal 1797Clinical Usefulness of Ofloxacin for the Outpatient with Chronic RespiratoryTract Infection

Y. Taguchi etal 1799Randomized, Comparative Studies of Ofloxacin and Other Standard Treatmentsof Urinary and Respiratory Infections

J. Kosmidis et al 1801Clinical Evaluation of Ofloxacin in Respiratory and Urinary. Tract Infections

A. Lechi etal 1803

CONTENTS xxix

Clinical Experience with Ofloxacin in the Treatment of Various Gram-negativeInfections

J. Tsagarakis et al 1805Efficacy and Safety of Ofloxacin in the Treatment of Urinary Tract Infectionsin Comparison with Cotrimoxazole and Amoxicillin + Clavulanic Acid

H. Knothe etal 1807Comparison of Ofloxacin with Co-trimoxazole and Nitrofurantoin in UrinaryTract Infections

P. Porpaczy 1809Efficacy of Ofloxacin on Biliary Tract Infections Compared with Other Drugs

K. Maruyama et al 1811Efficacy and Tolerance of Ofloxacin in the General Practice

P. M. Shah and W. Stille 1813Efficacy and Safety of Ofloxacin in the Treatment of Urinary Tract Infection

R. Wittenberger et al 1815Clinical Evaluation of Ofloxacin in Treatment of Non-gonococcal Urethritis

I. Saito 1817Results of Comparative Multicenter Studies with Ofloxacin in Europe

R. Blomer etal 1819•Influence of Sub-minimal Inhibitory Concentrations of Norfloxacin on both Adhesionto Uro-epithelial Cells and Haemagglutinating Activity of Escherichia coliStrains Isolated from Urine

G. Chabanon etal 1821A Study of Plasmid Stability in the Presence of Subinhibitory Concentrationsof Norfloxacin and Novobiocin

A. C. Graham etal 1823Antibacterial Activity of Norfloxacin and Induction of Resistant Strains

G. Ravizzola etal 1825Norfloxacin: Worldwide Preclinical Susceptibility Experience of UrinaryTract Pathogens

D. L. Shungu etal 1827Interaction of Norfloxacin with Nine Other Antibacterial Agents in vitro

B. A. Pelak etal 1829Efficacy of Norfloxacin in Experimental Models of Urinary Tract and SystemicInfections in Normal and Diabetic Mice: A Comparative Study

R. A. Fromtling etal 1831Pharmacokinetics of Norfloxacin in Renal Failure

J. P. Fillastre etal 1833Pharmacokinetic Studies of Norfloxacin in Healthy Volunteers and Effecton the Faecal Flora

D. A. Leigh etal 1835Experience with Norfloxacin in Oral Treatment of Severe and Complicated UrinaryTract Infections

W. Bischoff 1837Treatment of Acute Bacterial Gastroenteritis with Norfloxacin

J. Sabbaj etal 1839Efficacy and Tolerance of Norfloxacin in the Treatment of Patients with ComplicatedUrinary Tract Infections

M. Westenfelder etal 1841

xxx CONTENTS

Randomized Comparison of Single-dose vs. Short-term Norfloxacin Therapyin Acute Urinary Tract Infection

E. W. Rugendorff and H.-J. Schneider 1843Therapeutic Concept with Norfloxacin: Long-term Prophylaxis in RecurrentCystitis Infections

W. Bischoff 1845Therapeutic Concept with Norfloxacin: Single Shot Therapy in Acute Cystitis

W. Bischoff 1847Compassionate Treatments with Norfloxacin

K. Brown and M. Corrado 1849Pirfloxacin, a New Florurate Agent

N. Simonetti et al 1851Efficacy of New Quinolone Compound against Urinary Tract Pathogens

J. Dubois and V. Fontaine 1855Susceptibility of Campylobacter spp. to Quinolone Antibacterial Agents

J. Dubois and V. Fontaine 1857Ciprofloxacin and Enoxacin Activity vs. Nalidixic Acid, Amionoglycoside-resistantGram-negative Isolates Alone and with Amikacin or Newer P-Lactams

K. H. Mayer and J. A. Ellal 1859Activity of the 4-Quinolone Antibacterials at Physiological pH Values

J. T. Smith and N. T. Ratcliffe 1861In vitro Activity of 4-Quinolones against Difficult-to-treat Organisms and Developmentof Resistance to These Drugs

F. H. Kayser and G. Morenzoni 1863Research for a Hierarchy in the Acquisition of Resistance to the Quinolones

H. B. Drugeon etal 1865Growth Deficiency of Quinolone-resistant Mutants

P. Courvalin etal 1867Quantitative Analysis of Spontaneous Mutations in Serratia marcescens Which AffectSusceptibility to Quinolones in Different Ways

I. Haller 1869Bactericidal Activity of Ciprofloxacin, Norfloxacin and Ofloxacin in Serumand Urine after Oral Administration in Healthy Volunteers

H.-J. Zeiler etal 1871In vitro Antibacterial Activities of Seven Quinolones

K. T. Luh etal 1873Comparative Activities of Ciprofloxacin, Ticarcillin, and Tobramycin againstExperimental Pseudomonas aeruginosa Pneumonia

J. Pennington et al 1875Comparative Activities of Five Antimicrobial Agents in Experimental ProteusPyelonephritis

P. G. H. Peerbooms and D. M. MacLaren 1877Comparative Activities of AM-833, Norfloxacin, Ciprofloxacin and Ofloxacinagainst Various Experimental Infections

K. Hirai etal 1879Antimicrobial Activity of Quinolone Antibiotics in Urine

T. Kumada etal 1881Susceptibility to Quinolones in Relation to Other Antimicrobial Agents

M. S. M. Daniels 1883

CONTENTS xxxi

In vitro Activity of Ciprofloxacin, Pefloxacin and Ofloxacin against LegionellaA. Bure etal 1885

Susceptibility of Amikacin-resistant Strains of Pseudomonas to Ciprofloxacinand Norfloxacin

C. R. Rivera-Vazquez etal. 1887Isolation of Mutants of Pseudomonas aeruginosa PA01 Resistant to Ciprofloxacin,Norfloxacin and Ofloxacin and Incomplete Cross-resistance with Nalidixic Acid

P. Campos etal 1889The Pharmacokinetics and Saliva Penetration of Ofloxacin, Norfloxacin, Enoxacinand Pipemidic Acid

M. Uematsu etal 1891A Comparison of the Pharmacokinetics and Tissue Penetration of Ciprofloxacin(Oral and i.v.) and Ofloxacin (Oral) Administered to Volunteers,and Comparison with in vitro Activity

R. Wise etal 1893

Contents of Antimicrobial Section 1Special Lecture 1Symposia 11§ 1. New Antimicrobial Agents, Microbiology and Biochemistry 235§ 2. Diagnostics and Susceptibility 431§ 3. Pharmacokinetics 623§ 4. Experimental Infection 747§ 5. Immunology 789

Contents of Antimicrobial Section 3§ 11. Miscellaneous Antimicrobial Agents 1895§ 12. Internal Medicine and Pediatrics 1979§ 13. Urology 2185§ 14. Surgery, Gynecology and Obstetrics 2319§ 15. Miscellaneous Infections 2525§ 16. Adverse Side Effects 2595§ 17. Antibiotic Policy 2677Workshop Summaries 2701Author Index 2793Subject Index 2829Disease/Pathogen Index 2834Compound Index 2838Abbreviations of Antimicrobial Agents 2843