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)

Cefuroxime axetil has been evaluated previously in the treatment of lower respiratory tract infections, but not specifically in the treatment of community-acquired pneumonia. In a multicentre, investigator-blinded clinical trial, 162 patients with community-acquired pneumonia were randomly assigned to receive orally either cefuroxime axetil 500 mg bid (n = 84) or amoxycillin/clavulanate 500 mg/125 mg tid (n = 78) for 10 days. Organisms were isolated from the pretreatment sputum specimens of 97 of 162 (60%) patients, the commonest isolates being Streptococcus pneumoniae (38%) and Haemophilus influenzae (18%). A satisfactory clinical outcome (cure or improvement) was achieved in 100% (55 of 55) and 96% (49 of 51) of the clinically evaluable patients treated with cefuroxime axetil or amoxycillin/clavulanate, respectively (P = 0.23). With respect to eradication of bacterial pathogens, a satisfactory outcome (cure, presumed cure or cure with colonization) was obtained in 94% (32 of 34) and 93% (37 of 40) of bacteriologically evaluable patients treated with cefuroxime axetil or amoxycillin/clavulanate, respectively (P = 1.00). Both treatment regimens used in this study were well tolerated. The most common drug-related adverse experiences were gastrointestinal events, reported by 8% and 4%, respectively, of the patients in the amoxycillin/clavulanate and cefuroxime axetil groups, a difference which was not statistically significant (P = 0.32). These results indicate that cefuroxime axetil twice a day is as effective as amoxycillin/clavulanate three times a day in the treatment of outpatients with mild to moderate community-acquired pneumonia.
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PMID:Comparison of oral cefuroxime axetil and oral amoxycillin/clavulanate in the treatment of community-acquired pneumonia. 918 12

The serum bactericidal activity of three oral cephalosporins was studied in 12 volunteers, after administration of single doses of cefuroxime axetil 250 mg, cefixime 200 mg, cefixime 400 mg and cefetamet pivoxil 500 mg. Serum bactericidal activity against clinical isolates of Streptococcus pyogenes, Streptococcus pneumoniae, Haemophilus influenzae and Klebsiella pneumoniae was measured by a standardized microdilution method. Cefuroxime axetil demonstrated the best bactericidal activity against Gram-positive organisms and cefixime was the most bactericidal against Gram-negative bacteria.
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PMID:Serum bactericidal activity of newer oral cephalosporins in healthy volunteers. 959 80

Cefuroxime is the first commercially-available second-generation cephalosporine to be widely used in therapy; it is a semi-synthetic cephalosporin obtained from the 7-cephalosporanic acid nucleus of cephalosporin C. Cefuroxime axetil is the acetoxyethyl ester of cefuroxime. The majority of micro-organisms associated with respiratory infections are highly sensitive to cefuroxime. These include Haemophilus influenzae, Streptococcus pneumoniae, Streptococcus pyogenes and the other streptococci (excluding group D streptococci), and Moraxella catarrhalis. Bacteria sensitive to cefuroxime include the enterobacteria (Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, and Salmonella and Shigella and Straphylococcus aureus (methicillin-sensitive strains). The pharmacokinetic studies show that the maximum plasma concentration of cefuroxime after oral administration of 250 mg and 500 mg of cefuroxime axetil after a meal are respectively 4.6 and 7.9 mg/l. The absolute bioavailability of tablets is 68% (extremes 63-73%) after oral administration of 500 mg cefuroxime axetil. The protein binding is 33+/-5.7%. Tissue diffusion was studied in the interstitial fluid, the bronchial mucosa, the tonsils, and the bronchial secretions. Cefuroxime axetil is available as capsule-shaped tablets containing 125, 250 or 500 mg. An oral suspension dosage form for paediatric purposes is also available as granules in multidose bottles and sachets. Constitution gives a suspension containing 125 mg or 250 mg cefuroxime (as cefuroxime axetil). Cefuroxime axetil is indicated for the treatment of infections caused by susceptible bacteria. Indications include: lower respiratory tract infections (e.g., acute and chronic bronchitis and pneumonia); upper respiratory tract infections (e.g., ear, nose and throat infections such as otitis media, sinusitis tonsillitis and pharyngitis); genito-urinary tract infections (e.g., pyelonephritis, cystitis and urethritis, gonorrhoea, acute uncomplicated gonococcal urethritis and cervicitis); and skin and soft tissue infections (e.g., furunculosis, pyoderma and impetigo). For most infections, a dose of 250 mg twice daily is appropriate. In some urinary tract infections, 125 mg twice daily has been shown to be effective. If pneumonia is suspected or in more severe lower respiratory tract infection, doses of 500 mg bd should be used. Uncomplicated gonorrhoea has been shown to respond to a single 1-g dose of cefuroxime axetil. Adverse reactions to cefuroxime have generally been mild and transient in nature (gastrointestinal disturbances, including diarrhoea, nausea and vomiting).
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PMID:Cefuroxime axetil. 1861 87

Cefuroxime axetil is widely used to treat respiratory tract infections. We are not aware of a population pharmacokinetic (PK) model for cefuroxime axetil. Our objectives were to develop a semiphysiological population PK model and evaluate the pharmacodynamic profile for cefuroxime axetil. Twenty-four healthy volunteers received 250 mg oral cefuroxime as a suspension after a standardized breakfast. Liquid chromatography-tandem mass spectrometry was used for drug analysis, NONMEM and S-ADAPT (results reported) were used for parametric population PK modeling, and NPAG was used for nonparametric population PK modeling. Monte Carlo simulations were used to predict the duration for which the non-protein-bound-plasma concentration was above the MIC (fT(>MIC)). A model with one disposition compartment, a saturable and time-dependent drug release from the stomach, and fast drug absorption from the intestine yielded precise (r > 0.992) and unbiased curve fits and an excellent predictive performance. The apparent clearance was 21.7 liters/h (19.8% coefficient of variation [CV]) and the volume of distribution 38.7 liters (18.3% CV). Robust (>or=90%) probabilities of target attainment (PTAs) were achieved by 250 mg cefuroxime given every 12 h (q12h) or q8h for MICs of <or=0.375 mg/liter or <or=0.5 mg/liter, respectively, for the bacteriostasis target fT(>MIC) of >or=40% and for MICs of <or=0.094 mg/liter or <or=0.375 mg/liter, respectively, for the near-maximal-killing target fT(>MIC) of >or=65%. For the >or=40% fT(>MIC) target, the PTAs for 250 mg cefuroxime q12h were >or=97.8% for Streptococcus pyogenes and penicillin-susceptible Streptococcus pneumoniae. Cefuroxime at 250 mg q12h or q8h achieved PTAs below 73% or 92%, respectively, for Haemophilus influenzae, Moraxella catarrhalis, and penicillin-intermediate S. pneumoniae for susceptibility data from various countries. Depending on the MIC distribution, 250 mg oral cefuroxime q8h instead of q12h should be considered, especially for more-severe infections that require near-maximal killing by cefuroxime.
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PMID:New semiphysiological absorption model to assess the pharmacodynamic profile of cefuroxime axetil using nonparametric and parametric population pharmacokinetics. 1952 78


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