Key words Streptococcus pneumoniae µ µ H F Cl H H N N H N F COOH O Fig.1. Sitafloxacinstructure.
I
γ S. pneumoniae Haemophilus influenzae
Table1. Observationandtestschedule Observation/Tests Informedconsent Patientbackground Symptoms Signs Adverseevent Bodytemperature ParanasalsinusX-ray/CT Bacteriologicaltests Laboratorytests required asneeded Testschedule Before Endof Day3 treatment treatment anytime 7daysafterend oftreatment S. pneumoniae β pbp1a pbpb pbpx pbp1a pbpb pbpx pbp1a pbpb pbp1a pbpx pbp b pbpx pbp1a pbpb pbpx mefa ermb mefa ermb mefa ermb H. influenzae β ftsi β H. influenzae β ftsi β H. influenzae β ftsi γ
II
Table. Patientprofiles Patients(%) Parameters Otitismedia Paranasal sinusitis Tonsilitis, Pharyngitis, Laryngitis Patientsinanalysis 9 7 116 Acuteotitismedia Chronicotitismedia 31(63.3) 18(36.7) 31(6.7) 18(15.5) Diagnosis Acuteparanasalsinusitis Chronicparanasalsinusitis Tonsilitis Peritonsilitis Peritonsilarabscess Pharyngitis,laryngitis Pharyngitis (89.) 5(1.6) 1(5.) 1(5.) 1(5.) 7(35.) 1(5.) (36.) 5(.3) 1(8.6) 1(.9) 1(.9) 7(6.) 1(.9) Severityofilness Moderate Severe 1(8.6) 35(71.) 8(59.6) 19(.) 15(75.) 5(5.) 57(9.1) 59(5.9) Sex Male Female (.9) 7(55.1) 17(36.) 3(63.8) 9(5.) 11(55.) 8(1.) 68(58.6) Age(yrs) 8±16 36±11 3±9 1±15 Bodyweight(kg) 57.5±9.6 58.5±11.6 6.7±15.5 58.8±11.6 Concomitantdrugs No Yes 9(59.) (.8) 3(7.3) 13(7.7) 15(75.) 5(5.) 78(67.) 38(3.8) Table3. Overalclinicaleficacyatendoftreatment Diagnosis Excelent Good Patients(%) Fair Poor Eficacy(%) Otitismedia Paranasalsinusitis Tonsilitis,Pharyngitis, Laryngitis 3(6.9) 7(57.) 1(7.) (.8) 15(31.9) 5(5.) 5(1.) (8.5) 1(5.) 1(.) 1(.1) 9 7 87.8 89. 95. 6(55.) (3.5) 1(8.6) (1.7) 116 89.7 Eficacy(%)= numberof(excelent+ Good)/numberof 1 Table. Clinicaleficacybydisease Diagnosis Excelent Good Patients(%) Fair Poor Eficacy(%) Otitismedia Acute Chronic (acuteexacerbation) 16(51.6) 7(38.9) 11(35.5) 9(5.) 3(9.7) (11.1) 1(3.) 31 18 87.1 88.9 Paranasalsinusitis Acute Chronic (acuteexacerbation) (57.1) 3(6.) 1(33.3) 1(.) 3(7.1) 1(.) 1(.) 5 9.5 8. Eficacy(%)= numberof(excelent+ Good)/numberof 1
Table5. Bacteriologicaleficacyatendoftreatment Diagnosis Otitismedia Paranasalsinusitis Tonsilitis,Pharyngitis, Laryngitis Eradication 3 36 13 83 Strains Persistence 5 Eradication(%)= numberoferadication/numberof 1 7 39 38 13 9 Eradication (%) 87. 9.7 1 9. Table6. Eradicationbypathogen(otitismedia) Strains Organism Eradication Persistence AerobicGram-positivebacteria 3 S.aureus 8 3 S.pneumoniae 1 AerobicGram-negativebacteria 1 M.(B.)catarhalis H.influenzae 7 P.aeruginosa 1 3 5 Eradication(%)= numberoferadication/numberof 1 5 11 1 1 7 3 39 Eradication (%) 88. 7.7 1 85.7 1 1 33.3 87. Table7. Eradicationbypathogen(paranasalsinusitis) Strains Organism Eradication Persistence AerobicGram-positivebacteria 19 S.aureus 7 S.pneumoniae 1 AerobicGram-negativebacteria 13 M.(B.)catarhalis 3 H.influenzae 1 Anaerobicbacteria P.micros P.oralis 1 P.asaccharolytica 1 36 Eradication(%)= numberoferadication/numberof 1 1 7 1 13 3 1 1 1 38 Eradication (%) 9.5 1 85.7 1 1 1 1 1 1 1 9.7 S. pneumoniae Staphylococcus aureus H. influenzae Moraxella Branhamella catarrhalis Pseudomonas aeruginosa S. aureus P. aeruginosa S. aureus µ µ µ P. aeruginosa µ µ S. pneumoniae
S. aureus H. influenzae MB catarrhalis Peptostreptococcus micros Prevotella oralis Porphyromonas asaccharolytica H. influenzae µ S. aureus Streptococcus pyogenes S. pneumoniae H. influenzae P. micros µ S. pneumoniae µ S. pneumoniae µ S. pneumoniae pbp S. pneumoniae mefa ermb mefa ermb mefa ermb µ ermb µ S. pneumoniae µ µ H. influenzae β ftsi H. influenzae III S. pneumoniae H. influenzae S. pneumoniae mefa ermb H. influenzae S. pneumoniae H. influenzae S. aureus P. aeruginosa S. pneumoniae H. influenzae S. aureus P. aeruginosa S. pneumoniae H. influenzae
Table8. ConcentrationofSTFXinmiddleear,maxilarysinus,ethmoidalsinus,palatinetonsil,andserum Mucousmembraneofmiddle ear Mucousmembraneof maxilarysinus Mucousmembraneof ethmoidalsinus Palatinetonsil Dose (mg) 1 1 1 5 Patients median min,max Patients median min,max Patients median min,max Patients median min,max Serum (μ g/ml) 1.59±.8.5.,1.8.58±.15.53.5,.79 6.6±.38.6.,1.18 1.38±.3.31.18,1. ConcentrationofSTFX Tissue(μ g/g) 9 a).8±.73.58.,1.81.56±.31.53.1,.97 6.96±.61.86.8,1.86 1.63±..56.35,.93 a) underdetectionlimitsoftissueconcentrationforhighdilutionbyshorttissueweightin1case b) underdetectionlimitsoftissueandserum concentrationin1additionalcase Penetrationratio (tissue/serum) 8 b) 1.±.7 1.3.3,.5 1.1±.8.9.,. 6 1.6±.5 1.6 1.,. 1 1.8±. 1.9.9,. S. pneumoniae µ H. influenzae µ S. aureus µ µ µ P. aeruginosa µ µ S. aureus µ µ S. pneumoniae H. influenzae µ µ
Streptococcus pneumoniae β β Haemophilus influenzae