Disease relevance of dicloxacillin

• The inactivation of RTEM-2 beta-lactamase and of Bacillus cereus beta-lactamase I is accelerated in the presence of A type substrates such as dicloxacillin, quinacillin, and cefoxitin, which are thought to expand or loosen the conformation of these enzymes [1].
• In a mouse model, dicloxacillin-coated polyurethane catheters or control (uncoated) catheters were placed subcutaneously and then Staphylococcus aureus was inoculated at the time of insertion, 24 or 48 h later [2].
• The mechanism of synergistic activity of a combination of ampicillin and dicloxacillin was studied on beta-lactamase-producing Citrobacter freundii GN346 and its derived beta-lactamaseless mutant GN346/16 [3].
• We investigated the in vitro and in vivo effects of a combination of a beta-lactam (ceftazidime) and a beta-lactamase inhibitor (dicloxacillin) to synergistically kill a ceftazidime-resistant variant, Pseudomonas aeruginosa PA-48, which overproduces type Id cephalosporinase constitutively [4].
• The PAEs induced by ampicillin against E. coli and dicloxacillin against Staphylococcus aureus were not predictably dependent on the pH, whereas the PAEs induced by ciprofloxacin against S. aureus were longest at either end of the pH spectrum [5].

Psychiatry related information on dicloxacillin

• Growth of PA-48 cells in the presence of dicloxacillin (12.5 to 100 micrograms/ml) had no significant effect on the production rates or functional activity of the Id enzyme [4].

High impact information on dicloxacillin

• Analysis of serum concentrations after intravenous administration of 1 and 2 gm dicloxacillin to healthy subjects revealed concentration-dependent kinetics with respect ot renal elimination [6].
• In healthy volunteers the bioavailability after oral administration of 2 gm dicloxacillin or 2 gm cloxacillin amounted to 48.8% and 36.9% of the dose, respectively, when calculated from the area under the serum concentration-time curve, and to 74.1% and 48.5%, respectively, when calculated from the urinary excretion [6].
• Mechanism of synergistic action of a combination of ampicillin and dicloxacillin against a beta-lactamase-producing strain of Citrobacter freundii [3].
• These data support previous findings with dicloxacillin which show that patients with CF exhibit unusually rapid, active tubular secretion of certain penicillins that may necessitate use of larger doses of these drugs in treatment of infections [7].
• Biofilms formed in the presence of sub-MIC concentrations of dicloxacillin contained less biomass, and there were notable changes in the composition of the biofilm matrix [8].

Chemical compound and disease context of dicloxacillin

• After a single administration to patients in terminal renal failure a decrease in total oxacillin clearance from 279 to 159 ml/min/1.73 m2 and total dicloxacillin clearance from 249 to 43 ml/min/1.73 m2 was observed [9].
• Erythromycin and dicloxacillin are known to induce phlebitis frequently, as well as to exert toxic effects on cultured endothelial cells [10].
• Persistence of infection was recorded in one patient in the dicloxacillin group and superinfection in one patient in the azithromycin group [11].
• Extracellular and intracellular killing in neutrophil granulocytes of Staphylococcus aureus with rifampicin in combination with dicloxacillin or fusidic acid [12].
• A neonate treated initially with oxacillin intravenously for two weeks and who was receiving phenobarbital for a seizure disorder subsequently failed to achieve therapeutic levels of orally administered dicloxacillin, even when the dosage was as high as 175 mg/kg/day [13].

Biological context of dicloxacillin

• With the exception of a minor reduction in renal excretion, the pharmacokinetics of dicloxacillin showed no significant changes [9].
• The serum protein binding of dicloxacillin was similar in both groups of subjects [14].
• The time of occurrence of the peak serum concentration was similar in both groups and the total urinary recovery of dicloxacillin was normal or increased in the CF patients, suggesting that the intestinal absorption of the drug was unaffected by the disease [14].
• Following rifampin dosing, the mean dicloxacillin C(max) across genotypes decreased from 31.4 +/- 10.8 to 22.9 +/- 7.0 microg/mL (P < .05), whereas the mean oral clearance increased from 235 +/- 82 to 297 +/- 71 mL/min (P < .001), and the mean absorption time increased from 0.71 +/- 0.55 to 1.34 +/- 0.77 h (P < .05) [15].
• CASE SUMMARY: A 41-year-old man receiving warfarin 22 mg/wk with a final baseline prothrombin time (PT) of 20.7 sec was prescribed dicloxacillin 500 mg qid for 10 days [16].

Anatomical context of dicloxacillin

• In contrast, dicloxacillin, gentamicin, and cephalothin had no significant effect on the number of intracellular staphylococci in normal or CGD neutrophils [17].
• Less marked binding of dicloxacillin to iris and sclera was noted [18].
• The membranes of this tolerant bacilli contained at least five proteins with different affinities for the radiotracer or Dicloxacillin [19].
• We treated 18 patients undergoing major lower limb amputation due to ischemia by intravenous administration of 1 g dicloxacillin either 0, 3, or 6 hours before surgery followed by a similar dose 8 hours after the first dose [20].
• The kinetics of dicloxacillin protein binding was studied in three umbilical cord serum, three adult plasma specimens and in human serum albumin [21].

Associations of dicloxacillin with other chemical compounds

• In vivo half-lives of inhibitory activity for clindamycin and dicloxacillin were 5.6 and 17.7 h, respectively, with apparent first-order kinetics [22].
• Effects of mezlocillin on the pharmacokinetics of oxacillin and dicloxacillin [9].
• An open, randomized, multicentre study was undertaken to compare a three-day regimen of azithromycin with a seven-day course of dicloxacillin or flucloxacillin in the treatment of 118 children (aged 2-12 years) with clinically diagnosed acute skin and skin-structure infections [23].
• A comparative study of the efficacy, safety and tolerance of azithromycin, dicloxacillin and flucloxacillin in the treatment of children with acute skin and skin-structure infections [23].
• Although the Leishmania ulceration healed after a second course of meglumine antimoniate, and despite three oral dicloxacillin or pristinamycin courses, the otochondritis extended and an abscess developed [24].

Gene context of dicloxacillin

• RESULTS: Dicloxacillin and trimethoprim are substrates of P-gp (B-->A/A-->B ratios in MDR1-MDCK cells are 32 and 50, respectively) [25].
• DESIGN: MSSA was always/usually sensitive to dicloxacillin, amoxicillin/clavulanate, cephalosporins, imipenem, quinolones, and erythromycin, whereas MRSA was always/usually resistant [26].
• Exposure of the beta-lactamase from Staphylococcus aureus to the slowly reacting substrates cloxacillin or dicloxacillin results in time-dependent inactivation of the enzyme [27].
• Mean dicloxacillin C(max) measurements were 30.5 +/- 13.5, 33.3 +/- 4.7, and 31.1 +/- 12.8 mug/mL in individuals with the CC, CT, and TT genotype at position 3435 in exon 26 of the MDR1 gene [15].
• The economical outpatient antibiotics of choice for CFI are penicillin plus dicloxacillin; the former is needed to cover Eikenella corrodens and the latter to cover Staphylococcus aureus, both common in these wounds [28].

Analytical, diagnostic and therapeutic context of dicloxacillin

• In hemodialysis patients the elimination rate of dicloxacillin (T 1/2: 129 min) corresponds with the extrarenal elimination rate in healthy subjects [6].
• Dicloxacillin and its 5-hydroxymethyl metabolite were analyzed using liquid chromatography/tandem mass spectrometry [15].
• In a five-patient crossover study, serum levels of dicloxacillin after intravenous administration of dicloxacillin in the absence and presence of sulfaethiodole were measured [29].
• Application of ion-exchange cartridge clean-up in food analysis III. Determination of benzylpenicillin, phenoxymethyl-penicillin, oxacillin, cloxacillin, nafcillin and dicloxacillin in bovine liver and kidney by liquid chromatography with ultraviolet detection [30].
• Effects of hip arthroplasty and peroperative dicloxacillin prophylaxis on renal function [31].

References