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)

The safety and efficacy of two dose regimens of cefodizime (CAS 69739-16-8, HR 221) in hospitalized patients with lower respiratory tract infections were assessed in two consecutive studies. Sputum bacteriology, chest X-ray and a safety laboratory check were performed at baseline and after therapy. In order to compensate for the lack of a double-blind design the evaluation was conducted as a clinical intention-to-treat analysis. 32 patients (16 males, 16 females, mean age: 64 years) were admitted to study A and 42 subjects (30 males, 12 females, mean age: 66 years) to study B. The dosage regimens of cefodizime were 1 g b.i.d. (median 7 days) in study A and 2 g once daily (median 6 days) in study B. Parenchymal involvement was confirmed by chest X-ray in 56% of the patients in study A and 64% in study B, the remainder patients had acute exacerbations of chronic bronchitis with reasonable evidence of bacterial infection. The most frequent pathogens were Streptococcus pneumoniae and Haemophilus spp. The clinical cure rate was 97% in study A and 88% in study B. Eradication rates were 100% and 94%, respectively. No superinfection occurred. No adverse reactions were observed. In conclusion, a single daily injection of cefodizime 2 g achieved similar clinical and bacteriological cure rates to the standard dose regimen of 1 g b.i.d.
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PMID:Cefodizime given in single or divided doses for the treatment of lower respiratory tract infection. 910 49

Cefodizime (CAS 69739-16-8, HR 221) is a new third-generation cephalosporin with pharmacokinetic properties that make it suitable for once-daily administration in the treatment of lower respiratory tract infections (LRTI). Ninety-nine adult hospitalized patients (66 males, 33 females, median age 57.5 years) received a once-daily injection of 2 g cefodizime for LRTI. Median treatment duration was 8 days. Forty-two patients received cefodizime intravenously and 57 intramuscularly. Indications for treatment were as follows; primary lobar pneumonia (n = 36), bronchopneumonia (n = 14), secondary pneumonia (n = 3), aspiration pneumonia (n = 5), acute exacerbation of chronic bronchitis (n = 21), and of bronchiectasis (n = 9) and acute purulent bronchitis (n = 11). General condition was good in 29 patients and poor in 58; 12 patients were critically ill. The following pathogens were isolated at baseline (source: bronchial secretions, sputum or blood): S. pneumoniae (n = 47), Haemophilus spp. (n = 17), M. catarrhalis (n = 6), Streptococcus spp. (n = 9), Staphylococcus spp. (n = 5), Klebsiella spp. (n = 4), Pseudomonas spp. (n = 1), A. calcoaceticus (n = 1) and anaerobic organisms (n = 7). Fifty-nine patients were evaluable for bacteriological response and 82 for clinical response. Bacteriological outcome was satisfactory in 29/30 patients having LRTI with parenchymal involvement (97%) and in 29/29 patients without parenchymal involvement (100%). Clinical cure was achieved in 41/43 evaluable patients with parenchymal involvement (95%) and in 37/39 patients without parenchymal involvement (95%) in the per-protocol analysis and in 54/58 patients (93%) and 37/41 patients (93%), respectively, in the clinical intention-to-treat analysis. Three of the patients with an unsatisfactory clinical response died of infection during the study. Cefodizime was well tolerated. Adverse reactions--all of mild intensity--were tachycardia, lumbalgia and dizziness, each occurring in one patient. Cefodizime 2 g once daily either i.m. or i.v. was effective in the treatment of lower respiratory tract infections in hospitalized patients.
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PMID:Cefodizime once daily in the treatment of lower respiratory tract infections. 920 86

After 30 years of therapeutic use, thiamphenicol glycinate acetylcysteinate (CAS 20192-91-0) is still widely employed in the treatment of upper and lower respiratory tract infections. This is due to its particular characteristic to exert at pulmonary level, either the antibacterial activity of thiamphenicol (CAS 15318-45-3) and the mucolytic activity of N-acetylcysteine (CAS 616-91-1). The aim of this study was to evaluate the present pattern of susceptibility of several clinical isolates to thiamphenicol and the interference of N-acetylcysteine on this parameter. The studies have been performed in vitro. Equimolar concentrations of N-acetylcysteine and even higher concentrations did not interfere with the antibacterial activity of thiamphenicol against Streptococcus pneumoniae, Streptococcus pyogenes and Haemophilus influenzae. The spectrum of activity of thiamphenicol was similar to that observed in the past and was superior to that of erythromycin and amoxicillin. The activity of thiamphenicol was greater than that of erythromycin against H. influenzae and streptococci and equivalent versus Branhamella catarrhalis. In comparison with amoxicillin the activity of thiamphenicol was higher against H. influenzae and B. catarrhalis and slightly lower against streptococci. The results demonstrate that thiamphenicol maintains its therapeutic value confirming the importance of thiamphenicol glycinate acetylcysteinate in the treatment of respiratory tract infections.
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PMID:In vitro antibacterial activity of thiamphenicol glycinate acetylcysteinate against respiratory pathogens. 1041 71

Thiamphenicol-glycinate-acetylcysteinate (TGA; CAS 20192-91-0) is widely used for the treatment of infections of varied aetiology. The aim of this study was to compare the antibacterial activity of thiamphenicol-glycinate (TG; CAS 15318-45-3), TGA, amoxicillin (CAS 61336-70-7) plus clavulanic acid (CAS 58001-44-8), azithromycin (CAS 83905-01-5) and ceftriaxone (CAS 104376-79-6). Minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) were determined against Staphylococcus aureus, Klebsiella pneumoniae, Streptococcus pyogenes, Streptococcus pneumoniae, Moraxella catarrhalis and Haemophilus influenzae according to the National Committee for Clinical Laboratory Standards (NCCLS) methods. The effects of changes in assay conditions were also examined. The activity of TG and TGA was similar to that of amoxicillin plus clavulanic acid, with the exception of methicillin resistant S. aureus. Azithromycin and ceftriaxone were characterised by a limited activity against gram-positive cocci and methicillin resistant and cefinase-positive S. aureus, respectively. TG and TGA are characterized by a wide spectrum of activity, comparable to that of recent commercialized antibiotics for treatment of respiratory tract infections.
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PMID:Comparative in vitro activity of thiamphenicol-glycinate and thiamphenicol-glycinate-acetylcysteinate and other antimicrobials against respiratory pathogens. 1136 73

The palladium-catalyzed cross-coupling reaction of 5-(tributylstannyl)isoindoline and its 1- and 3-methyl derivatives with 6-fluoro or 6-unsubstituted 7-bromo-1-cyclopropyl-8-methoxy (or difluoromethoxy)-4-oxoquinoline-3-carboxylate afforded the corresponding 1-cyclopropyl-7-(5-isoindolinyl)-4-oxoquinoline-3- carboxylic acids: 6-fluoro, 1a-7a and 6-nonfluoro, 1b-7b. The in vitro antibacterial spectra of the newly synthesized quinolones were mostly characterized by excellent Gram-positive activity against Staphylococcus aureus and Streptococcus pneumoniae including quinolone-resistant strains, and also by significant Gram-negative activity comparable to 7-(1-piperazinyl)fluoroquinolones. Comparative examinations of the in vitro antibacterial profiles and the in vivo toxicity in terms of intravenous lethality, micronuclei-inducing potential and convulsive activity provided 6-nonfluorinated 1-cyclopropyl-8-(difluoromethoxy)-7-(1-methylisoindolin-5-yl)-4- oxoquinoline-3-carboxylic acid [(+/-)-5b] as the candidate for evaluation of the stereoisomers. The enantiomers (R)-5b and (S)-5b were synthesized via the Suzuki coupling reaction of (R)- and (S)-1-methyl derivatives of 2-(triphenylmethyl)isoindolin-5-boronic acid with the corresponding 7-bromo-8-(difluoromethoxy)-4- oxoquinoline-3-carboxylate. The (R)-5b stereoisomer proved to be 2- to 4-fold more active than the (S)-5b stereoisomer against the organisms tested, with the exception of an equal potency observed with S. pneumoniae IID553 and Haemophilus influenzae ATCC49247. A noticeable in vitro antibacterial profile of (R)-5b was that it is 16- and 64-fold more active than levofloxacin (CAS 100986-85-4) and ciprofloxacin (CAS 86393-32-0), respectively, against Mycoplasma pneumoniae IID813 (MIC of 0.0313 microgram/ml), and 4-fold more active than ciprofloxacin and levofloxacin against Mycobacterium tuberculosis M-4 (MIC of 0.0313 microgram/ml). Additional studies indicate that (R)-5b (T-3811, CAS 194804-75-6) exhibits excellent antibacterial activity against a wide range of organisms including anaerobes and common respiratory pathogens, while demonstrating a high selectivity against the mammalian homolog topoisomerases. The methane-sulfonate of (R)-5b (T-3811ME, CAS 223652-90-2) is now undergoing clinical testings.
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PMID:Synthesis, antibacterial activity, and toxicity of 7-(isoindolin-5-yl)-4-oxoquinoline-3-carboxylic acids. Discovery of the novel des-F(6)-quinolone antibacterial agent garenoxacin (T-3811 or BMS-284756). 1257 31