Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0038454 (stroke)
 147,016 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Bacteriological and clinical evaluations of BRL 25000 (1 part clavulanic acid plus 2 parts amoxicillin) granules in the pediatric field have been performed. The MICs of BRL 25000 against 25 clinically isolated strains of S. aureus, 40 E. coli, and 14 K. pneumoniae were compared with those of AMPC. Against beta-lactamase non-producing strains of S. aureus and E. coli, the MICs of both drugs were nearly equal, however, against beta-lactamase producing strains of these species and K. pneumoniae, BRL 25000 was superior to AMPC. The blood levels of AMPC and CVA after single oral administration of approximately 15 mg/kg of BRL 25000 granules to fasted children were studied in 3 subjects. The mean levels of AMPC and CVA peaked about 1 hour after administration at values of 11.40 and 5.49 micrograms/ml, respectively, with half-lives of 0.91 and 1.02 hours, and AUCs of 23.52 and 12.66 hr X micrograms/ml, respectively. The 6-hour urinary recovery of AMPC ranged from 30.59% to 52.03% and for CVA from 16.31% to 45.18%. There was no significant difference between the blood level of AMPC following single oral administration of approximately 10 mg/kg AMPC granules and that of AMPC following single oral administration of approximately 15 mg/kg BRL 25000 granules to the same children. Clinical evaluation of BRL 25000 granules administered orally 3-4 times a day at total daily doses of between 42.9-52.9 mg/kg resulted in improvement, judged excellent or good, in all 7 cases of tonsillitis and 2 cases of pyelonephritis. In particular, the clinical effect was excellent in the case of tonsillitis where a beta-lactamase producing H. influenzae was isolated. In the total 11 cases treated, including 2 cases of mycoplasmal pneumonia excluded from the clinical evaluation, 1 case of rash and eosinophilia was observed. No other adverse reactions or abnormal laboratory findings were observed. The taste and flavor of the drug were well accepted by the children. It was concluded that BRL 25000 granules are promising new drug which should be markedly useful in the treatment of infections in pediatric outpatients.
 ...
PMID:[Bacteriological and clinical evaluation of BRL 25000 (clavulanic acid-amoxicillin) granules in the pediatric field]. 384 23

BRL 25000 granules (containing 2 parts amoxicillin and 1 part clavulanic acid) have been studied fundamentally and clinically. The MICs of BRL 25000 against strains of S. aureus, E. coli, K. pneumoniae which were resistant to CEZ and beta-lactamase producing strains of H. influenzae were determined. The MICs of BRL 25000 at an inoculum of 10(6) cells/ml were 1/4 to 1/128 of those of AMPC and, in particular, the MICs of BRL 25000 were especially reduced against the organisms for which those of AMPC were more than 100 micrograms/ml. The pharmacokinetics of BRL 25000 were studied in 46 children at dose levels of 7.5 mg (8 fasting children, 7 non-fasting children), 10 mg/kg (4 fasting, 4 non-fasting), 15 mg/kg (4 fasting, 4 non-fasting), 20 mg/kg (8 fasting, 7 non-fasting). The peak serum concentrations in fasting children were marginally higher than those in non-fasting subjects. Values for AMPC and CVA from BRL 25000, dosed at 7.5, 10, 15 and 20 mg/kg to fasting children, 0.5-1 hour after dosing were 4.86 and 2.36 micrograms/ml, 5.20 and 1.69 micrograms/ml, 7.50 and 3.27 micrograms/ml, 9.38 and 6.30 micrograms/ml, respectively. In non-fasting subjects, corresponding values were 2.84 and 1.01 micrograms/ml, 4.53 and 2.10 micrograms/ml, 7.29 and 4.08 micrograms/ml, 6.83 and 2.96 micrograms/ml, respectively. The biological half-lives of AMPC and CVA, following the administration of BRL 25000, show no significant difference between the fasting and non-fasting states. Values for AMPC and CVA in fasting children were 0.85-1.15 hours and 0.64-1.03 hours, and in non-fasting children, 1.18-1.79 hours and 0.78-1.02 hours, respectively. The time to reach the peak serum concentration and half-lives were similar for AMPC and CVA when dosed as BRL 25000. Peak urinary concentrations for BRL 25000 (AMPC and CVA) at dose levels of 7.5, 10, 15, 20 mg/kg to fasting children were 681.8 and 148.2 micrograms/ml, 247.1 and 66.3 micrograms/ml, 484.2 and 149.1 micrograms/ml, 1,796.5 and 372.0 micrograms/ml, whilst in the non-fasting state the values were 496.3 and 83.2 micrograms/ml, 991.1 and 156.7 micrograms/ml, 2,397.5 and 460.7 micrograms/ml, 1, 896.3 and 323.4 micrograms/ml, respectively. The peak urinary concentration in the fasting state was observed at 0-2 hours after dosing, and in non-fasting individuals it occurred at 2-4 hours after dosing.(ABSTRACT TRUNCATED AT 400 WORDS)
 ...
PMID:[Experimental and clinical studies on BRL 25000 (clavulanic acid-amoxicillin) granules in the pediatric field]. 384 24

MICs of BRL 25000, a combination of a newly developed beta-lactamase inhibitor CVA and AMPC in the ratio of 1 to 2, were determined against a number of bacterial strains and compared with those of AMPC, CVA, CEX and CCL. The 98 bacterial strains tested included 2-S. aureus, 23-H. influenzae, 25-E. coli, 22-K. pneumoniae and 26-P. mirabilis. In pharmacokinetic studies, BRL 25000 medium granules were administered to groups of 3 male subjects, aged between 7 years 8 months and 9 years 5 months, at doses of 10, 15 and 20 mg/kg, 2 hours after a meal. The resultant serum and urine concentrations and drug recoveries were measured. Furthermore, BRL 25000 was administered to a total 43 patients (2-pharyngitis, 8-tonsillitis, 3-bronchitis, 2-pneumonia and 28-urinary tract infection) whom clinically evaluable. An average daily dosage of 45.3 mg/kg was given, in 3 or 4 divided doses, for a period of 8 days on average. Clinical and bacteriological effects as well as side effects were studied. In the microbiological studies on 98 clinical strains, including beta-lactamase negative bacteria, BRL 25000 showed MICs against the Gram-positive cocci (2-S. aureus) superior to the other 4 drugs at inoculum sizes of 10(8) and 10(6) cells/ml. For the Gram-negative bacilli, against H. influenzae at inoculum sizes of 10(8) and 10(6) cells/ml, BRL 25000 was inferior in the small MIC range but superior in the large MIC range to AMPC, and was superior to the other 3 drugs. Against E. coli at an inoculum of 10(8) cells/ml, BRL 25000 showed antibacterial activity next to AMPC and CCL whilst at an inoculum of 10(6) cells/ml, it was inferior in the small MIC range but superior in the large MIC range to AMPC and CEX and was inferior to CCL but superior to CVA. Against K. pneumoniae at an inoculum of 10(8) cells/ml, BRL 25000 was equal to AMPC, CVA and CEX but inferior to CCL, whilst at an inoculum of 10(6) cells/ml, it was inferior to CCL but superior to the other 3 drugs. Against P. mirabilis at inoculum sizes of 10(8) and 10(6) cells/ml, BRL 25000 was inferior in the small MIC range but equal or superior in the large MIC range to AMPC, and was superior to CVA and CEX.(ABSTRACT TRUNCATED AT 400 WORDS)
 ...
PMID:[Experimental and clinical trials of BRL 25000 (clavulanic acid-amoxicillin) granules in the field of pediatrics]. 389 76

Bacteriological, pharmacokinetic and clinical studies on SY5555 dry syrup (powder which is dissolved before use), a new penem antibiotic for oral use, were performed. The following results were obtained. 1. Antibacterial activities. MICs of SY5555, clavulanic acid/amoxicillin (CVA/AMPC), cefotiam (CTM), cefpodoxime (CPDX), cefaclor (CCL) and cefdinir (CFDN) were determined against clinically isolated Staphylococcus aureus, coagulase negative staphylococci, Streptococcus pneumoniae, Streptococcus pyogenes, Haemophilus influenzae, Moraxella catarrhalis, Escherichia coli and Enterobacter cloacae at a dose of 10(6) CFU/ml. MICs of SY5555 against S. aureus, CNS, S. pneumoniae, S. pyogenes, H. influenzae, M. catarrhalis, E. coli and E. cloacae were 0.2, 0.2, 0.2, < or = 0.025, 0.78, 0.2, 0.78 and 3.13 micrograms/ml, respectively, showing excellent antibacterial effects on these pathogens. Although the effects of SY 5555 against H. influenzae and E. coli were slightly inferior to those of CPDX and CFDN, the drug showed the most excellent antibacterial effect on other strains as compared with the control drugs. 2. Absorption and excretion In this study, plasma concentrations and urinary recovery rates were examined after administration of SY5555 at doses of 5 and 10 mg/kg (potency) after meals. With both 5 and 10 mg/kg doses, peak plasma concentrations were reached 1 hour after administration, at 0.25-2.61 micrograms/ml (mean 1.47 micrograms/ml) and 1.08-2.17 micrograms/ml (mean 1.74 micrograms/ml), respectively. The plasma levels rapidly decreased to 0.06-0.19 micrograms/ml (0.12 micrograms/ml) and 0.0503-0.0637 micrograms/ml) after 6 hours. The half-lives 1.12 hours in the 5 mg/kg group and 1.0 hour in the 10 mg/kg group. The urinary recovery rates were determined in the first 8 hours after administration in the 5 mg/kg and 6 hours in the 10 mg/kg group, and the values were as low as 1.05-12.3% and 1.6-4.33%, respectively. 3. Clinical results The clinical responses were examined in a total of 73 cases including 4 acute pneumonia, 13 acute bronchitis, 11 tonsillitis, 3 pharyngitis, 12 scarlet fever, 2 pertussis, 6 urinary tract infection, 6 otitis media, 7 lymphadenitis, 2 staphylococcal scalded skin syndrome, 2 phlegmon, 4 impetigo and 1 purulent parotitis. The treatment was effective or better in 66 of 70 cases with an efficacy rate of 94.3% (3 undeterminable cases were excluded). Bacteriological effects were examined during the clinical course for detected or suspected pathogens found before administration of SY5555. The effects were determined in 50 cases including 7 cases of polymicrobacterial infections, 57 strains in total. Eight strains, however, persisted, hence the overall eradication rate was 86.0%.(ABSTRACT TRUNCATED AT 400 WORDS)
 ...
PMID:[Bacteriological, pharmacokinetic and clinical studies of SY5555 dry syrup in the pediatric field]. 769 46

From January 1997 to July 1999, a total of 867 isolates of Haemophilus influenzae were recovered in the microbiology laboratory of Chiba Children's Hospital. The overall prevalence of beta-lactamase production was 12.8%. Ampicillin-MICs for all of the 111 beta-lactamase-producing isolates was > or =4 microg/ml. A total of 26 beta-lactamase-negative isolates (3.4% of all beta-lactamase-negative isolates and 3.0% of all isolates) were found to be resistant to ampicillin. The prevalence of beta-lactamase negative ampicillin-resistant strains (BLNAR) increased remarkably to 8.9% during the last 7-month period. It is noteworthy that the MICs not only of penicillins but also of cephems for BLNAR were significantly higher than those for ampicillin-susceptible isolates. Eight beta-lactamase-producing isolates of H. influenzae (7.2% of all beta-lactamase-producing isolates) were resistant to amoxicillin-clavulanate (AMPC/CVA). Consequently, the overall resistance to ampicillin was 15.8%, and that to AMPC/CVA was 3.0%. The results of this study corroborate the findings of previous investigators in the US (Doern et al., 1997) regarding the emergence of BLNAR and beta-lactamase-producing AMPC/CVA-resistant strains (BLPACR) of H. influenzae. Continued monitoring of susceptibility trends will be required to guide appropriate chemotherapy.
 ...
PMID:Antibiotic resistance among recent clinical isolates of Haemophilus influenzae in Japanese children. 1076 67

The positivity of beta-lactamase and antimicrobial susceptibility were determined in a total of 1,358 clinical isolates at 15 hospitals and clinics in four prefectures in southern Kyushu (Okinawa, Miyazaki, Kagoshima and Kumamoto) during the period from December 1999 to February 2000. The isolates collected comprised of 176 strains of S. aureus, 203 of H. influenzae, 102 of M. catarrhalis, 206 of E. coli, 153 of K. pneumoniae, 99 of E. cloacae, 95 of S. marcescens, 201 of P. aeruginosa, 79 of E. faecalis, and 44 of E. faecium. The frequency of CPDX resistance among E. coli in particular varied geographically, and was found to be higher in Kumamoto and Kagoshima. The strains of K. pneumoniae and E. cloacae resistant to common antimicrobial agents were particularly found in Kagoshima, and one strain of IPM-resistant E. cloacae was isolated in Miyazaki. Also, the geographical difference in the frequency of LVFX resistance among the isolates of E. cloacae was noted, the results indicating the higher prevalence in Okinawa and Kagoshima. Resistant isolates of P. aeruginosa were less common in Kagoshima, and four isolates of P. aeruginosa from Miyazaki were found to be resistant to CAZ and IPM. None of the isolates of S. aureus and Enterococcus spp. was resistant to VCM or TEIC at all. The isolates of E. faecalis resistant at high-level GM (500 micrograms/ml) and SM (1,000 micrograms/ml) were found in 27.8% and 22.8%, and those of E. faecium were 6.8% and 38.6%, respectively. Overall, the ratio of MRSA among S. aureus was 67.6%, and three isolates were resistant to ABK with no less than 8 micrograms/ml of MIC. The frequency of BLNAR (beta-lactamase-negative, ampicillin resistant) among H. influenzae isolated in Okinawa was markedly higher (isolation ratio, 37.9%) when compared with other prefectures, and the isolates of BLPACR (beta-lactamase-positive, AMPC/CVA resistant) were found only in Okinawa with a ratio of 41.6%. A total of 18 strains of ESBL defined by the NCCLS criteria (M100-S11) were isolated, eight strains of K. pneumoniae and 10 strains of E. coli. Of 18 isolates of ESBL, 13 were from Kagoshima and the remaining five were from Kumamoto.
 ...
PMID:[Antimicrobial susceptibility and prevalence of beta-lactamase producing clinical isolates in southern Kyushu. The results of collaborative study from 1999 to 2000]. 1259 33

Nasal sinusitis, tonsillitis, and pharyngolaryngitis typify upper respiratory tract infections, while bronchitis and pneumonia typify lower respiratory tract infections. Cases of paranasal sinusitis with severe suppuration are reportedly becoming less frequent, while those of chronic catarrhal paranasal sinusitis and edematous allergic paranasal sinusitis are becoming more so, The primary factor in paranasal sinusitis, a typical infectious disease encountered in otolaryngology, is bacterial infection. The main causative bacteria are Streptococcus pneumoniae, reported in 13.4% of cases, Haemophilus influenzae in 12.8% Moraxella catarrhalis in 5.5%, Staphylococcus aureus in 26.5%, Pseudomonas aeruginosa in 5.2%, and anaerobes. The incidence of strains resistant to antimicrobial agents has grown for S. pneumoniae, H. influenzae, and M. catarrhalis and decreased for S. aureus and P. aeruginosa. Acute exacerbation or severe suppuration in chronic paranasal sinusitis requires the administration of antimicrobial agents, with the same agent administered 2 weeks for maximal effect. First-line agents are AMPC/CVA, SBTPC, CDTR-PI, CFPN-PI, and GFLX for adults, with ASPC, SBPC, ACPC, CTRX, CMZ, FMOX, PAPM/BP, and MEPM injected in severe cases. Attention must be paid to strains that resist cephems and macrolides, such as PISP, PRSP, and BLNAR. In refractory chronic paranasal sinusitis, attention must also be paid to biofilms produced by S. aureus and P. aeruginosa. Suitable antimicrobial agents should be determined for treating of chronic paranasal sinusitis, in addition to the best procedure to ensure early recovery from inflammation, such as puncturing or irrigating the maxillary sinus, injecting a suitable agent, nebulization, and/or surgically widening the middle meatus.
 ...
PMID:[Bacteria isolated from chronic upper and lower respiratory tract infections and the associated therapeutic strategies--in paranasal sinusitis]. 1651 20

An 80-year-old woman presenting with fever and cough was given a diagnosis of community-acquired pneumonia. She was hospitalized and treated with ampicillin/sulbactam (ABPC/SBT) and clarithromycin (CAM). Gram stain images and sputum culture results led us to believe that the causative agent was Haemophilus influenzae. Drug sensitivity testing indicated that the H. influenzae was a beta-lactamase-positive, ABPC-resistant (BLPAR) strain. Treatment with ABPC/SBT was not clinically effective. We considered the possibility of beta-lactamase-positive amoxicillin/clavulanate-resistant (BLPACR) strains. Further testing revealed that the MIC of ABPC was 128 microg/ml, that of SBT/ABPC was 8 microg/ml, and that of AMPC/CVA was 4 microg/ml. Furthermore, genetic analysis indicated the H. influenzae to be a BLPACR-I strain. The poor clinical course eventually led to a diagnosis of BLPACR. When beta-lactamase-producing H. influenzae is cultured, the possibility of a BLPACR strain resistant to ABPC/SBT and AMPC/CVA must be considered.
 ...
PMID:[Case of pneumonia caused by beta-lactamase-producing and amoxicillin/clavulanate resistant strains of H. influenzae]. 1893 21

We investigated the susceptibility to antibacterial agents of 197 strains of Haemophilus influenzae isolated from pediatric patients at medical facilities in Gifu and Aichi prefectures between 2009 and 2010. Those strains were also examined for the mutations of ftsI coding for penicillin-binding protein 3, presence of bla TEM-1, serotype and beta-lactamase producing ability. Among the 197 strains, the most prevalent serotype was non-typeable (89.8%), followed by serotype b (8.1%), e (1.5%) and f (0.5%). Based on the susceptibility among the 197 strains to antibacterial agents, beta-lactamase nonproducing ampicillin-susceptible H. influenzae (BLNAS) accounted for 27.4%, beta-lactamase nonproducing ampicillin-resistant H. influenzae (BLNAR) for 62.4%, beta-lactamase producing ampicillin-resistant H. influenzae (BLPAR) for 6.1% and beta-lactamase producing amoxicillin/ clavulanic acid-resistant H. influenzae (BLPACR) for 4.1%. According to PCR-based genotyping, the strains were classified into 6 categories: gBLNAS, gLow-BLNAR, gBLNAR, gBLPAR, gBLPACR-I and gBLPACR-II. The incidences of each resistant class were 17.3% for gBLNAS, 6.6% for gLow-BLNAR, 66.0% for gBLNAR, 5.6% for gBLPAR and 4.6% for gBLPACR-II. The combined incidence of gLow-BLNAR and gBLNAR was 72.6%, which was higher than that of BLNAR (62.4%). The MIC90s of antibacterial agents against the 197 strains were as follows; 0.0156 microg/mL for tosufloxacin and garenoxacin, 0.0313 microg/mL for levofloxacin and pazufloxacin, 0.0625 microg/mL for norfloxacin, 0.25 microg/mL for tazobactam/piperacillin (TAZ/PIPC) and ceftriaxone, 0.5 microg/mL for TAZ/PIPC (1:8) and cefditoren, 1 microg/mL for piperacillin, cefteram, cefotaxime, meropenem, tebipenem and minocycline, 2 microg/mL for doripenem, 4 microg/mL for cefcapene, imipenem and azithromycin, 8 microg/mL for sulbactam/ampicillin, clavulanic acid/amoxicillin (1:2, CVA/AMPC) and cefdinir, 16 microg/mL for CVA/AMPC (1:14), flomoxef and clarithromycin, 32 microg/mL for ampicillin. Although there was no rapid increase in the antibacterial resistance, the prevalence of BLNAR was still over 50%. In order to ensure the appropriate chemotherapy, it is important to continue the surveillance of susceptibility among H. influenzae.
 ...
PMID:[Antibacterial susceptibility surveillance of Haemophilus influenzae isolated from pediatric patients in Gifu and Aichi prefectures (2009-2010)]. 2338 33

As a special drug use investigation, we monitored and assessed trends in antibacterial activity of clavulanic acid/amoxicillin (1:14) (hereafter, "CVA/AMPC (1:14)") and other antimicrobial agents for clinical isolates from pediatric patients with otitis media or respiratory, skin, and urinary tract infections. Against Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis isolated and identified from otorrhea, epipharynx and rhinorrhea of pediatric patients with otitis media, the MIC90s of CVA/AMPC (1:14) in five years between 2006-2010 were 1 microg/mL for S. pneumoniae and 8 microg/mL for H. influenzae and 0.25-0.5microg/mL for M catarrhalis. The changes of MIC90s of CVA/AMPC (1:14) for penicillin-resistant S. pneumoniae (PRSP) and beta-lactamase non-producing H. influenzae were two times, and no decrease in drug susceptibility was found in the period of the present investigation. In addition, the MIC changes of other antimicrobial agents for these three organisms were approximately two to four times as well. Against organisms isolated and identified from pus, sputum, pharynx, skin and urine of pediatric patients with respiratory, skin, and urinary tract infections, the MIC90s of CVA/AMPC (1:14) in four years between 2008-2011 were 1 microg/mL for S. pneumoniae, < or =0.06microg/mL for penicillin susceptible S. pneumoniae (PSSP) without any change, 0.5-1 microg/mL for penicillin intermediate resistant S. pneumoniae (PISP) with a twofold change and 1 microg/mL for PRSP with no change. The MIC90s of CVA/AMPC (1:14) were 2-8 microg/mL for S. aureus with a fourfold change, 2 microg/mL for methicillin-sensitive S. aureus without any change, 4-8 microg/mL for H. influenzae with a twofold change. Against beta-lactamase non-producing H. influenzae, MIC90s of CVA/AMPC (1:14) were 1 microg/mL for beta-lactamase negative ampicillin susceptible (BLNAS), 8 microg/mL for beta-lactamase negative ampicillin resistant (BLNAR), showing no change. Neither Streptococcus pyogenes or Klebsiella pneumoniae demonstrated any change and M. catarrhalis and Escherichia coli showed twofold changes of MIC90s of CVA/AMPC (1: 14). In the present investigation conducted to monitor annual changes in antibacterial activity intended for pediatric patients with otitis media or other infections, there was no significant change in antibacterial activity of CVA/AMPC (1: 14).
 ...
PMID:[Antibacterial activity for clinical isolates from pediatric patients of clavulanic acid/amoxicillin (1: 14) -outcomes of special drug use investigation on antibacterial activity (annual changes)]. 2416 43


1 2 Next >>