Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: UMLS:C0348321 (Haemophilus)
15,372 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Cefadroxil (Duricef, Mead Johnson and Company), resembles cephalexin and cephradine in spectrum of antibacterial activity but differs in human pharmacokinetic properties. Whether the latter are likely to affect activity in vivo was assessed by determining bactericidal activity against clinical isolates under conditions simulating the variation of drug concentration in the blood stream after an oral dose of 500 mg to adults. In this kinetic model, cefadroxil was more active than cephalexin or cephradine against Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, Proteus mirabilis, Haemophilus influenzae and one of two strains of Escherichia coli. The other strain of E. coli was virtually unaffected by the cephalosporins. S. pyogenes was equally susceptible to all three cephalosporins. Analysis of the results suggest that the pharmocokinetic properties of an antibiotic affect its activity in the blood stream, provided the susceptibility of the infecting organism is concentration-dependent within the range of drug concentration occurring in serum.
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PMID:Bactericidal activity of cefadroxil, cephalexin, and cephradine in an in vitro pharmacokinetic model. 54 Dec 65

We tested the efficacy of a single daily dose of ceftriaxone (active ingredient of Rocephin) for the treatment of severe bacteremic infections in 125 non-neutropenic adult patients. A single daily dose of ceftriaxone ranging from 1 to 4 g was given. Surgical procedures were performed if needed. Seventy-six (60.8%) were males and bacteremia was nosocomially acquired in 45 (36%). Microbiologically proven bacteremia was demonstrated in all patients. The most common microorganisms isolated were Escherichia coli (46 episodes), Streptococcus pneumoniae (17 episodes), Klebsiella pneumoniae, and Haemophilus influenzae, Serratia marcescens, Salmonella sp., and Staphylococcus aureus (9, 7, 6, 6, respectively). The urinary tract was the source of the bacteremia in 45 cases (36%), and the lower respiratory tract in 33 (26.4%). Mean duration of treatment was 10.8 days (range 3-21 days). One hundred and six patients (84.8%) recovered completely, 11 (8.8%) improved, but needed an alternative antibiotic treatment. An alternative treatment was also given to a patient whose condition had initially deteriorated. Seven patients (5.6%) died. Death was directly related to the infection in 2 cases. Three patients (2.4%) developed a superinfection, and 5 (4%) a severe (1 case) or mild (4 cases) adverse effect. In summary, a single daily dose of ceftriaxone proved to be useful for the treatment of selected severe bacteremic infections.
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PMID:Ceftriaxone monotherapy for severe bacteremic infections. Spanish Ceftriaxone Study Group. 261 37

The bactericidal quotient (BQ) assessed in the site of infection represents an essential parameter for evaluating the real bactericidal potency of an antibiotic in vivo. The assessment and knowledge of BQ values allow us to set up a more accurate and appropriate antibacterial therapy. The two drugs--ceftriaxone (Rocephin) and imipenem plus cilastatin (Tienam)--that have been taken into consideration in this study, having a similar antibacterial spectrum though with different kinetics, may have the same BQ values in bronchial secretion versus Haemophilus influenzae, Klebsiella pneumoniae and Streptococcus pneumoniae, when administered at different dosages, i.e. ceftriaxone 1 g (i.v.) every 24 h, imipenem 0.5 g (i.v.) every 8 h.
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PMID:Bactericidal effect of ceftriaxone versus imipenem plus cilastatin in bronchial secretion. 307 44

Twenty-six adults with acute bacterial meningitis were enrolled in an open randomized comparative study. The organisms isolated from CSF were Streptococcus pneumoniae, Staphylococcus epidermidis, Haemophilus influenzae, Escherichia coli and Salmonella typhi. 13 patients (group A) were treated once daily with intravenous ceftriaxone (Rocephin). The 13 patients in group B received ampicillin or ampicillin plus chloramphenicol in 4 doses/day. The mean duration of therapy in groups A and B was 9.9 and 12.3 days, respectively. This difference in the duration of therapy was statistically significant. All patients from group A showed clinical improvement and all were bacteriologically cured. In group B only 12 patients were clinically and bacteriologically cured; 1 patient had to be withdrawn from the therapy because CSF culture remained positive after 48 h of therapy. Ceftriaxone was well tolerated in all patients; ampicillin or ampicillin plus chloramphenicol were associated with diarrhea and skin rash in 6 patients.
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PMID:Ceftriaxone in the treatment of bacterial meningitis in adults. 307 45

The clinical efficacy of cefditoren pivoxil (CDTR-PI, ME 1207) was evaluated in 45 patients with various infections. CDTR-PI was administered after meals at a dose of 3 mg/kg t.i.d. to most patients. The clinical efficacy rate was 95.3%. As side effects, diarrhea occurred in 2 patients. Cefditoren showed excellent antibacterial activities against Haemophilus influenzae, Streptococcus pyogenes and Streptococcus pneumoniae, and was more effective against Staphylococcus aureus than other cephems.
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PMID:[A clinical study on cefditoren pivoxil granules in the pediatric field]. 837 93

Cefditoren (formerly ME-1206), a new orally administered cephalosporin, was evaluated in vitro against 1249 recently isolated strains of Streptococcus pneumoniae (500 strains), Moraxella catarrhalis (250 strains), and Haemophilus influenzae (499 strains). Reference National Committee for Clinical Laboratory Standards methods were used and the strains were representative for the current rates of beta-lactamase production or penicillin resistance. Cefditoren had MIC50/MIC90 results for Moraxella catarrhalis and Haemophilus influenzae of 0.12/0.5 and < or = 0.008/0.015 microgram/mL, respectively. The pneumococci were consistently twofold to eightfold more susceptible to cefditoren than other oral cephalosporins or penicillins. The MIC90 for penicillin-resistant S. pneumoniae was only 2 micrograms cefditoren/mL, and the highest recorded MIC was 4 micrograms/mL. Cefditoren appears to be a very promising beta-lactam possessing the greatest potency and potential spectrum versus contemporary (1997) respiratory tract pathogens.
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PMID:In vitro evaluation of a novel orally administered cephalosporin (Cefditoren) tested against 1249 recent clinical isolates of Haemophilus influenzae, Moraxella catarrhalis, and Streptococcus pneumoniae. 976 98

Among Haemophilus influenzae isolated from children with respiratory tract infections, the evolution of ampicillin resistance was investigated during 1996 and 1997 in Japan. beta-Lactamase production was assessed and minimum inhibitory concentrations (MICs) of eight antimicrobial agents were determined using a broth microdilution method in Mueller-Hinton-lysed horse blood medium. Of 74 H. influenzae, 11 strains (14.9%) produce beta-lactamase and were thus highly resistant to ampicillin (MIC of >4.0 microgram/ ml). In addition, moderate resistance to ampicillin, defined as an MIC of >==1.0 microgram/ml, was noted in 44.4% of all beta-lactamase-negative isolates. These beta-lactamase-negative ampicillin-resistant (BLNAR) organisms were resistant to other cephalosporins such as cefpodoxime and cefdinir, while beta-lactamase-producing strains were susceptible to them. Cefditoren, cefteram, and minocycline were active against all strains studied, whereas cefaclor and clarithromycin were inactive against all H. influenzae isolates in this study. Results indicate that BLNAR strains have emerged among children with respiratory tract infections in Japan.
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PMID:Increasing prevalence of ampicillin- resistant, non-beta-lactamase-producing strains of Haemophilus influenzae in children in Japan. 987 5

Cefditoren, a third generation orally administered aminothiazolyl cephalosporin, has demonstrated bactericidal activity against many Gram positive and negative bacterial pathogens and stability against clinically important beta-lactamases. Cefditoren was compared to cefaclor, cefixime, and penicillins against 1 435 recently isolated strains of streptococci (312 Streptococcus pneumoniae, 165 viridans group streptococci, 142 beta-haemolytic streptococci), Haemophilus influenzae (521 strains), and Moraxella catarrhalis (295 strains). Streptococcus pneumoniae and viridans group streptococci had penicillin nonsusceptible rates of 37.8 and 35.8%, respectively. Cefditoren (MIC(90) in microg/ml/% susceptible) activity against all tested H. influenzae (0.03/100) and M. catarrhalis (0.06-0.5/100) was comparable to cefixime and significantly greater than cefaclor. Cefditoren (MIC(90), 0.5 microg/ml) was 4- to 128-fold more active than comparison beta-lactams against the pneumoococci and was the most potent beta-lactam (including penicillin) versus beta-haemolytic streptococci. Cefditoren pharmacokinetics demonstrate a T(1/2) of 1.5-2 h and C(max) values of 2.8 and 4.6 microg/ml, respectively with 200 or 400 mg doses of cefditoren pivoxil; plasma concentrations exceed 1 microg/ml for 4 to 6 hours (33-50% of dosing interval). Consequently, a susceptible MIC of </= 1 microg/ml or </= 2 microg/ml was proposed with zone diameter correlates of >/= 18 and >/= 15 mm (5-microg disk) for all cited fastidious species tested. Categorical agreement between MIC and disk tests was 94.6 to 100% with a correlation coefficient (r) range of 0.50 to 0.90 for streptococci. H. influenzae intermethod comparison results using the same interpretive criteria were in complete agreement, but exhibited a low r = 0.39. Cefditoren clearly possesses the most potent activity among currently studied oral cephalosporins or penicillin against commonly isolated bacterial pathogens causing bronchitis, pneumonia, sinusitis, or pharyngitis and was active against nearly all penicillin-resistant streptococci at </= 0.5 microg/ml. Expanded clinical investigations seem warranted.
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PMID:Antimicrobial activity and in vitro susceptibility test development for cefditoren against Haemophilus influenzae, Moraxella catarrhalis, and Streptococcus species. 1086 4

Cefditoren, a broad-spectrum orally administered cephalosporin ester, has documented in vitro efficacy against many Gram-positive and -negative pathogens and stability against clinically important beta-lactamases. We have reviewed the microbiology and the pharmacokinetic/pharmacodynamic literature regarding the spectrum and potency of this newer agent against the major etiologic agents of community-acquired respiratory infection, (Streptococcus pneumoniae, Hemophilus influenzae and Moraxella catarrhalis), as well as the Enterobacteriaceae and non-enteric Gram-negative bacilli, staphylococci, and other aerobic and anaerobic Gram-positive cocci. The level of cefditoren activity against S. pneumoniae (MIC(90,) 0.5 microg/mL) was superior to all marketed oral cephalosporins and at least equal to amoxicillin +/- clavulanate. H. influenzae (MIC(90,) 0.016-0.03 microg/mL) and M. catarrhalis (MIC(90,) 0.06-0.5 microg/mL) were also very susceptible to cefditoren. In contrast to cefixime and ceftibuten, cefditoren was active against oxacillin-susceptible staphylococci (MIC(90,) < or = 1 microg/mL) at a level comparable to cefuroxime axetil, cefaclor or cefprozil. Enterococci, Pseudomonas aeruginosa and most anaerobes (Gram-negative) were not cefditoren-susceptible, but most Enterobacteriaceae, beta-haemolytic and viridans group streptococci were highly susceptible. Furthermore, an overview of key in vitro susceptibility testing methods and issues including disk diffusion testing and Etest (AB BIODISK, Solna, Sweden) method accuracy, interpretive criteria, and pharmacodynamic considerations for the selection of a breakpoint concentration are provided. The rapid bactericidal nature of the antibacterial activity of cefditoren, its post antibiotic effect, penicillin binding protein targets, and extent of beta-lactamase stability are all favorable qualities. In conclusion, this orally administered (BID) beta-lactam possesses promise for use against commonly isolated problematic respiratory tract pathogens such as penicillin-non-susceptible pneumococci and beta-lactamase-positive M. catarrhalis or H. influenzae. Success in the clinical trials will further define the role of cefditoren in this era of emerging resistant bacterial pathogens.
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PMID:Cefditoren in vitro activity and spectrum: a review of international studies using reference methods. 1168 8

Cefditoren pivoxil is an orally absorbed prodrug that is rapidly hydrolysed by intestinal esterases to the microbiologically active cephalosporin cefditoren. Cefditoren has a broad spectrum of activity against Gram-positive and Gram-negative bacteria, including common respiratory and skin pathogens. Cefditoren has shown excellent in vitro activity against the Gram-positive pathogens penicillin-susceptible and -intermediate Streptococcus pneumoniae, S. pyogenes and methicillin-susceptible Staphylococcus aureus. Cefditoren was inactive against methicillin-resistant S. aureus. Of the important Gram-negative pathogens, cefditoren had potent antibacterial effects against beta-lactamase-positive and -negative Haemophilus influenzae, H. parainfluenzae and beta-lactamase-positive and -negative Moraxella catarrhalis. Cefditoren does not have antibacterial activity against Pseudomonas aeruginosa or atypical respiratory pathogens and has only variable activity against anaerobes. In healthy volunteers, single doses of cefditoren pivoxil 200 and 400mg achieved maximal plasma concentrations of 2.6 to 3.1 mg/L and 3.8 to 4.6 mg/L, respectively. Cefditoren penetrates rapidly into bronchopulmonary and tonsillar tissue as well as inflammatory and noninflammatory blister fluid. In two, randomised, double-blind trials involving patients with acute exacerbations of chronic bronchitis (AECB), cefditoren 200 and 400mg twice daily for 10 days produced clinical cure rates of 88 to 89% within 48 hours of treatment completion. Clinical cure rates in patients with AECB were similar to those of either clarithromycin 500mg twice daily or cefuroxime axetil 250mg twice daily. In patients with streptococcal pharyngitis, a 10-day course of cefditoren pivoxil 200mg twice daily produced clinical cure rates of 94% at 4 to 7 days after treatment, which were similar to those observed for phenoxymethylpenicillin potassium 250 mg four times daily. In uncomplicated skin and skin structure infections, a 10-day course of cefditoren pivoxil 200 or 400mg twice daily produced the same clinical cure rate of 89% within 48 hours of treatment completion. These cefditoren pivoxil dosage regimens were as effective as a 10-day course of either cefadroxil 500 mg twice daily or cefuroxime axetil 250mg twice daily in treating uncomplicated skin and skin structure infections, including those caused by S. aureus and S. pyogenes. The most common adverse events associated with therapeutic doses of cefditoren pivoxil are diarrhoea, nausea, headache, abdominal pain and vaginal candidiasis.
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PMID:Cefditoren pivoxil. 1181 76


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