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  • 1
    ISSN: 1432-1076
    Keywords: Key words Ceftazidime ; Continuous infusion ; Cystic fibrosis ; Paediatrics ; Pseudomonas aeruginosa ; AbbreviationsCAZ ceftazidime ; CF cystic fibrosis ; CI continuous infusion ; FEV1 forced expiratory volume in one second ; FVC forced vital capacity ; MIC minimum inhibitory concentration ; PAE post-antibiotic effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Continuous infusion (CI) of β-lactam antibiotics provides a stable concentration which may result in a better activity against gram-negative bacteria if exceeding the minimum inhibitory concentration (MIC). Treatment outcome after 24 h CI of ceftazidime (CAZ) in cystic fibrosis (CF) children was compared with the bolus administration regimen. Fourteen CF children with chronic Pseudomonas aeruginosa pulmonary infection were treated during 14 days with the conventional CAZ thrice-a-day bolus infusion (regimen A), and few months later with 24 h CI of CAZ (regimen B) using a portable pump. Amikacin was added to both regimens. Clinical efficacy of treatment was assessed using pulmonary, inflammatory and nutritional variables. Bacteriological analyses and CAZ concentrations in serum and sputum were also measured. All patients improved clinically with both regimens. Among the parameters used to compare both regimens, only prealbumin values improved (regimen A: +0.08 g/l versus regimen B: +0.11 g/l, P=0.015). No clinically significant side-effects were noted. In regimen A, the mean predose (trough level) CAZ concentration in serum was highly variable (range 2.2–45.4 μg/ml) with some values (32% of samples) below the MIC of P. aeruginosa isolates found in the sputum of the patients. In regimen B, the serum CAZ level achieved was 28.5 ± 8.4 μg/ml without any value below the MIC. The mean sputum levels were comparable in both regimens. No CAZ resistant strains of P. aeruginosa appeared between and directly after the treatments. Conclusion The clinical outcome of children with cystic fibrosis treated with 24 h continuous infusion of ceftazidime was no different from that achieved with the conventional bolus infusion regimen. Continuous infusion provided a sustained serum ceftazidime level well above the P. aeruginosa minimum inhibitory concentration. Continuous infusion was well tolerated and appreciated by the children and this may promote home therapy for cystic fibrosis children.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The crude petroleum-ether extract of the root bark of Hypericum revolutum VAHL (Guttiferae) exhibited in vitro growth-inhibitory activity against the Co-115 human colon carcinoma cell line. Activity-guided fractionation of this extract resulted in the isolation of two new hyperforin derivatives 1 and 2. The structure of 1 (hyperevolutin A) was established by X-ray analysis as the 4-hydroxy-8-exo-methyl-5,7-exo-bis(3-methylbut-2-enyl)-1-(2-methyl-1-oxopropyl)-8-endo-(4-methylpent-3-enyl)bicyclo[3.3.1]non-3-ene-2,9-dione. The structure of the homologue 2 was deduced by comparison of its UV and 1H- and 13C-NMR spectra with those of 1.
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The crude petroleum-ether extract of the aerial parts of Hypericum calycinum L. (Guttiferae) exhibited in vitro growth-inhibitory activity against the Co-115 human colon carcinoma cell line. Bioassay-guided fractionation of this extract allowed the isolation of the cyclohexadienone derivatives 1-5, four of which are previously undescribed compounds. The structures of the known chinesin II (1) and of 2 (hypercalin A) were established by 1H- and 13C-NMR spectroscopy and were confirmed by X-ray analysis of their crystalline mixture which revealed the complete relative configuration of both compounds. The structure of 3 (hypercalin B) was elucidated by means of extensive 1D- and 2D-NMR experiments, including DQ-COSY, HETCOR and LR-HETCOR. The structure of compound 4 (hypercalin C) was established by 1H- and 13C-NMR spectroscopy and confirmed by X-ray analysis to be the 3,5-dihydroxy-4-{[(1R*,2S*, 5S*)-2-hydroxy-2-methyl-5-(1-methylethenyl)cyclopentyl]methyl}-6,6-bis-(3-methylbut-2-enyl)-2-(2-methylpropanoyl)cyclohexa-2,4-dien-1-one. The structures of the higher isomeric homologues 5a/5b were deduced by comparison of their UV, 1H-, and 13C-NMR spectra with those of 4. The isolated compounds appeared to be related to chinesin I and II previously isolated from Hypericum chinense L. and were responsible for the growth-inhibitory activity of the extract against the Co-115 human carcinoma cell line. Moreover, 1/2 and 3 showed molluscicidal activity against the schistosomiasis-transmitting snail Biomphalaria glabrata.
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
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