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At least 19 recordsLinked to original sources
PubMed1994

Should probenecid be used to reduce the dicloxacillin dosage in orthopaedic infections? A study of the dicloxacillin-saving effect of probenecid.

Reduction in the dosage of dicloxacillin from 500 mg to 250 mg 3 times a day would mean lowering of costs and less side-effects in orthopaedic infections. In this cross-over study, the serum concentrations of dicloxacillin were measured in 9 patients after administration of dicloxacillin 500 mg 3 times a day (dicloxacillin 500 mg) and after co-administration of 250 mg dicloxacillin and 250 mg probenecid 3 times per day (dicloxacillin 250 mg+probenecid 250 mg). Concentrations were measured every hour after the tablet intake. The mean maximum serum concentrations of dicloxacillin were 17.1 micrograms/ml (dicloxacillin 500 mg) and 12.2 micrograms/ml (dicloxacillin 250 mg+probenecid 250 mg), respectively (P < 0.05). Serum concentrations above 3 micrograms/ml were obtained during 285 min. in both regimes, but the individual variations were biggest during in the dicloxacillin 250 mg+probenecid 250 mg treatment. Serum concentrations above 5 micrograms/ml were in mean measured during 228 min. (dicloxacillin 500 mg) and 190 min. (dicloxacillin 250 mg+probenecid 250 mg), respectively (P < 0.05). The clinical significance of these findings is being discussed. In theory, treatment with dicloxacillin 250 mg+probenecid 250 mg may be as sufficient as dicloxacillin 500 mg.

Administration, Oral↗
PubMed1996

Potential interaction between warfarin and dicloxacillin.

OBJECTIVE: To report a case and retrospective review of seven patients who experienced a decrease in prothrombin time during concomitant administration of warfarin and dicloxacillin. 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. Plasma collected for PT determinations was also used to measure trough warfarin R- and S- enantiomer concentrations. The PT and S- and R-warfarin concentrations decreased 17%, 25%, and 20%, respectively, on day 5 after initiation of dicloxacillin. For the retrospective review, the mean PT decreased 17.0% (range 10.5-25.9%) as soon as 4 days after the initiation of dicloxacillin. DISCUSSION: Our observations, which are consistent with those of two previously published reports, suggest a close temporal relationship between the administration of dicloxacillin and a decreased anticoagulant effect of warfarin. Limited data from our patient further suggest that this may result from declines in systemic warfarin concentrations. The time course of the fall of PTs appears to occur within 4-5 days; return of the PT to baseline after dicloxacillin administration is stopped appears to take up to 3 weeks. Until further controlled studies are conducted to confirm this interaction, clinicians should be aware that patients may be at risk for a decreased anticoagulant effect of warfarin when dicloxacillin is given concomitantly. CONCLUSIONS: Careful monitoring of international normalized ratios and titration of the warfarin dosage is recommended on initiation and for 3 weeks after discontinuation of dicloxacillin in patients receiving warfarin.

Adult↗
PubMedDate not supplied

Influence of sulfaethidole on the human pharmacokinetics of dicloxacillin.

In a five-patient crossover study, serum levels of dicloxacillin after intravenous administration of dicloxacillin in the absence and presence of sulfaethiodole were measured. Significantly greater serum concentrations of dicloxacillin were noted when dicloxacillin was administered with sulfaethidole. Pharmacokinetic evaluation of the data suggests that the higher serum concentrations were primarily the result of changes in the extravascular distribution for dicloxacillin in the presence of sulfaethidole. Although examination of the distribution rate constants for dicloxacillin in a two-compartment open model would suggest a lowering of serum concentrations, the experimental data clearly indicate that the serum and tissue compartment dicloxacillin concentrations increased in the presence of sulfaethiodle, indicating that protein binding in the central as well as extravascular compartments could be affected by sulfaethidole.

Adult↗
PubMed1998

The effect of dicloxacillin and fusidic acid on the extracellular and intracellular killing of Staphylococcus aureus.

The effect of dicloxacillin and fusidic acid used alone and in combination on the extracellular and intracellular killing of four isolates of Staphylococcus aureus in the presence of serum was studied. At the extracellular level, dicloxacillin (8 mg/L) had a bactericidal effect on all four isolates, whereas fusidic acid (64 mg/L) had a bacteriostatic effect on two isolates and no effect on the two other isolates. Fusidic acid significantly inhibited the extracellular bactericidal effect of dicloxacillin on two isolates. Intracellular killing was measured in human neutrophil granulocytes. Dicloxacillin (8 mg/L) significantly increased the intracellular killing of all four isolates, while fusidic acid (64 mg/L) significantly increased the intracellular killing of three isolates, but the killing was significantly lower than that of dicloxacillin. When the antibiotics were combined the intracellular killing of three of the isolates was significantly lower than that of dicloxacillin alone. The viability of the granulocytes and their ability to produce superoxide anion were not affected by the antibiotics. In conclusion, we found that the increased intracellular killing of S. aureus by dicloxacillin was inhibited by fusidic acid.

Adult↗
PubMed2005

Effect of the MDR1 C3435T variant and P-glycoprotein induction on dicloxacillin pharmacokinetics.

This study investigated 2 hypotheses about genotype-phenotype relationships for the efflux transporter, P-glycoprotein: (1) the presence of a synonymous C3435T variant in exon 26 of the MDR1 gene correlates to higher plasma concentrations of a P-glycoprotein substrate, dicloxacillin, and (2) the effects of genotypic differences decrease under conditions of P-glycoprotein induction by rifampin. Eighteen healthy volunteers received two 1-g doses of dicloxacillin, one on the 1st study day and the other on the 11th day of rifampin dosing (600 mg daily). Dicloxacillin and its 5-hydroxymethyl metabolite were analyzed using liquid chromatography/tandem mass spectrometry. 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. 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). Rifampin treatment increased the formation clearance, C(max), and AUC of the 5-hydroxymethyl metabolite by 135%, 119%, and 59%, respectively. The C3435T variant had no effect on dicloxacillin pharmacokinetics. The data suggested that rifampin induced intestinal P-glycoprotein and increased dicloxacillin metabolism.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed1976

Dicloxacillin and cloxacillin: pharmacokinetics in healthy and hemodialysis subjects.

Differences in the elimination, distribution, and absorption of dicloxacillin and cloxacillin were studied in a group of healthy individuals with the use of a 2-compartment model. In patients on chronic intermittent hemodialysis, only dicloxacillin was investigated and the results were compared with data obtained in earlier studies on cloxacillin and flucloxacillin. 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. Individual variation in bioavailability after oral administration was slightly lower for docloxacillin than for cloxacillin. The higher serum concentrations of dicloxacillin, as compared with cloxacillin, are also attributable to slower (renal) elimination (T 1/2: 42 and 33 min, respectively). 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. In hemodialysis patients the elimination rate of dicloxacillin (T 1/2: 129 min) corresponds with the extrarenal elimination rate in healthy subjects. The bioavailability after oral administration of 1 gm in patients is good (75.9% of the dose).

Administration, Oral↗
PubMedDate not supplied

Dicloxacillin and flucloxacillin: pharmacokinetics, protein binding and serum bactericidal titers in healthy subjects after oral administration.

The pharmacokinetics of dicloxacillin and flucloxacillin were studied in 12 healthy volunteers after oral administration. The participants received a single dose of either dicloxacillin (0.5 g, 0.75 g or 1.0 g) or flucloxacillin (0.75 g) in a cross-over fashion. Antibiotic concentrations were determined in serum and urine by bioassay and followed for 8 and 24 h, respectively. The three dicloxacillin dosages showed no significant differences for the serum elimination half-lives (t1/2 beta, median: 72 min). Comparing 0.75 g flucloxacillin with the same dose of dicloxacillin, no significant differences between the values of Cmax, t1/2 beta and AUC were found. Protein binding as determined by ultrafiltration in pooled serum was 94.7-96.2% for flucloxacillin and 96.4-97.2% for dicloxacillin. The serum bactericidal titers were similar for the two drugs. In conclusion, dicloxacillin and flucloxacillin showed similar pharmacokinetic behavior after 0.75 g doses in human volunteers.

Administration, Oral↗
PubMed1975

Enhanced renal excretion of dicloxacillin in patients with cystic fibrosis.

Single oral doses of 6.25 mg/kg of dicloxacillin suspension were given to ten cystic fibrosis (CF) patients and eight normal subjects. Peak serum concentrations and areas under the concentration versus time curves for dicloxacillin were variable and, on average, were 2 1/2 times lower in the CF patients. 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. The low serum concentrations in the CF patients were caused by unusually high renal clearances of dicloxacillin which average 282 +/- 135 compared to 95 +/- 28 ml/min/1.73 sq m in the normal subjects. Creatinine clearances were also elevated in the CF patients by 55% on average, while urea clearances were normal. The serum protein binding of dicloxacillin was similar in both groups of subjects. Because the rapid excretion results in low and variable serum concentrations of the antibiotic, treatment of CF patients with dicloxacillin may warrant use of increased or more frequent doses and monitoring of serum antibiotic levels.

Adolescent↗
PubMed1985

A multicenter comparison of related pharmacologic features of cephalexin and dicloxacillin given for two months to young children with cystic fibrosis.

Twenty-one cystic fibrosis patients under 3 years of age were enrolled in an open multicenter study to assess the feasibility of the study design and to compare selected pharmacologic features of cephalexin or dicloxacillin administered orally for 2 months. Patient tolerance and compliance were significantly less for dicloxacillin (p less than .01 and p less than .001, respectively). Superficial Candida infections were more common in the cephalexin group (p = 0.02), however increased stool frequency and nonspecific diaper rashes were more prevalent in patients receiving dicloxacillin (p less than .05). Staphylococcus aureus was isolated from respiratory secretions after 2 months from two dicloxacillin and no cephalexin patients. Areas under the curve and peak serum concentrations were higher for cephalexin (p less than .05 and p = .02), but antistaphylococcal activity in serum was higher for dicloxacillin (p less than .05) due to a lower mean MIC compared to cephalexin. Deep pharyngeal plus routine throat culture yielded more pathogens than either method alone. Express mail and central processing of respiratory specimens was efficient for most organisms, however there was some loss of Streptococcus pneumoniae and Haemophilus influenzae. Cephalexin was associated with better patient acceptance and compliance despite higher rates of superficial fungal infections as compared to dicloxacillin. Cephalexin, routine bacteriologic throat swabs processed locally or centrally, mail-in urine compliance assessment and a multicenter design are feasible components for a long-term prospective evaluation of antibiotic prophylaxis in patients with cystic fibrosis.

Administration, Oral↗
PubMed1982

[Studies on the combination action of ampicillin and dicloxacillin (author's transl].

The combination action of ampicillin and dicloxacillin was studied in vitro. The following conclusions were obtained. 1) When both ampicillin and dicloxacillin were employed, an increase in antibacterial activity was observed against beta-lactamase producing E. coli No. 106 (clinical isolated strain). 2) A synergistic action of ampicillin and dicloxacillin was proved by chequer board dilution method for E. coli No. 106. 3) A same synergistic action of ampicillin and dicloxacillin was also proved by the growth curve for E. coli No. 106. 4) Dicloxacillin showed an inhibition in degradation of ampicillin brought about by beta-lactamase extracted from E. coli No. 106. 5) When the organisms of E. coli No. 106 were exposed to the combination of ampicillin and dicloxacillin, spheroplast-like structure and lysis were observed by scanning electron microscope.

Ampicillin↗
PubMed1989

Isolation of a Staphylococcus aureus beta-lactamase-dicloxacillin complex and kinetic studies on the reactivation of the enzyme.

Exposure of the beta-lactamase from Staphylococcus aureus to the slowly reacting substrates cloxacillin or dicloxacillin results in time-dependent inactivation of the enzyme. Methods for the rapid separation of a beta-lactamase-dicloxacillin complex from excess inhibitor, using centrifuged columns of Sephadex G-25 or DEAE-Sephadex G-25, are described. The enzyme-dicloxacillin complex releases active enzyme, with specific activity identical to that of untreated enzyme, after storage at pH 7.5 at 15 degrees C. Full reactivation was accompanied by the release of 0.8 eq of hydrolyzed dicloxacillin. The complex is stable for up to 40 h when stored at pH 3 at 4 degrees C. The reactivation process, which occurs with first-order kinetics at 15 degrees C and pH values between 4 and 8, displays a pH dependence with apparent pKa's of 4.6 and 8.5, and a limiting value of the reactivation rate constant of 0.022 min-1. Deviation from first-order kinetics at pH 9 is consistent with a competing irreversible inactivation of the enzyme at that pH. This behavior differs substantially from that of the similarly inactivated beta-lactamase I from Bacillus cereus, whose rate of reactivation is independent of pH, but which undergoes irreversible denaturation at acidic pH [A. L. Fink, K. M. Behner, and A. K. Tan (1987) Biochemistry 26, 4248-4258]. Addition of hydroxylamine to the S. aureus beta-lactamase-dicloxacillin, complex stimulates the rate of reactivation by a maximum of 35%. This effect is hyperbolically dependent on the concentration of hydroxylamine with half-maximal stimulation at 2.8 mM. The Km for ampicillin hydrolysis catalyzed by the partially reactivated enzyme is identical to that measured for catalysis by the untreated enzyme. We discuss our observations in relation to models for the transient inhibition process.

Dicloxacillin↗
PubMed1989

Resistance to dicloxacillin, methicillin and oxacillin in methicillin-susceptible and methicillin-resistant Staphylococcus aureus detected by dilution and diffusion methods.

A total of 54 Staphylococcus aureus strains of varying methicillin resistance were investigated for their resistance to methicillin, oxacillin and dicloxacillin by different diffusion tests. Inhibition zones were measured around locally prepared paperdiscs with 10 micrograms methicillin, 5 and 10 micrograms oxacillin, 5 and 10 micrograms dicloxacillin, PDM paperdiscs with 10 micrograms methicillin or oxacillin and Neo-sensitabs tablets with methicillin or oxacillin. All diffusion tests were performed both with Mueller-Hinton agar and Danish Blood agar as well as at 37 degrees C and 30 degrees C and read after overnight incubation. Differences in zone diameter under different conditions were found to be independent of the susceptibility level of the strains. Seventeen of the strains were detected as methicillin-resistant (MRSA) by two methods including high inoculum and prolonged incubation at 30 degrees C. The minimum inhibitory concentration (MIC) of the 54 strains was determined by a plate dilution method at 30 degrees C and 37 degrees C. A 10 micrograms locally prepared methicillin disc detected all MRSA strains with no false reactions either at 37 degrees C or 30 degrees C on Mueller-Hinton agar. Investigations with oxacillin discs had to be performed at 30 degrees C or with a 5 microgram disc in order to detect correctly. PDM paperdiscs gave reactions identical to the corresponding locally prepared discs. Methicillin Neo-sensitabs detected all MRSA strains but also included a few susceptible strains among the resistant ones. Addition of blood increased the number of not-detected MRSA strains. All 17 MRSA strains were susceptible to dicloxacillin by the dilution method, and the disc diffusion test showed similar results. Dicloxacillin discs therefore did not detect the presence of MRSA strains. The implications of replacement of the methicillin/oxacillin disc by a dicloxacillin disc are discussed.

Denmark↗
PubMed2000

Randomized comparison of linezolid (PNU-100766) versus oxacillin-dicloxacillin for treatment of complicated skin and soft tissue infections.

This randomized, double-blind, multicenter trial compared the efficacy and safety of linezolid, an oxazolidinone, with those of oxacillin-dicloxacillin in patients with complicated skin and soft tissue infections. A total of 826 hospitalized adult patients were randomized to receive linezolid (600 mg intravenously [i.v.]) every 12 h or oxacillin (2 g i.v.) every 6 h; following sufficient clinical improvement, patients were switched to the respective oral agents (linezolid [600 mg orally] every 12 h or dicloxacillin [500 mg orally] every 6 hours). Primary efficacy variables were clinical cure rates in both the intent-to-treat (ITT) population and clinically evaluable (CE) patients and microbiological success rate in microbiologically evaluable (ME) patients. Safety and tolerability were evaluated in the ITT population. Demographics and baseline characteristics were similar across treatment groups in the 819 ITT patients. In the ITT population, the clinical cure rates were 69.8 and 64.9% in the linezolid and oxacillin-dicloxacillin groups, respectively (P = 0.141; 95% confidence interval -1.58 to 11. 25). In 298 CE linezolid-treated patients, the clinical cure rate was 88.6%, compared with a cure rate of 85.8% in 302 CE patients who received oxacillin-dicloxacillin. In 143 ME linezolid-treated patients, the microbiological success rate was 88.1%, compared with a success rate of 86.1% in 151 ME patients who received oxacillin-dicloxacillin. Both agents were well tolerated; most adverse events were of mild-to-moderate intensity. No serious drug-related adverse events were reported in the linezolid group. These data support the use of linezolid for the treatment of adults with complicated skin and soft tissue infections.

Acetamides↗
PubMed1970

Flucloxacillin, a new isoxazolyl penicillin, compared with oxacillin, cloxacillin, and dicloxacillin.

Flucloxacillin, a new isoxazole penicillin, is active against penicillinase-producing strains of Staphylococcus aureus and is well absorbed in man after oral and intramuscular administration. Compared with isoxazole penicillins in current clinical use-namely, oxacillin, cloxacillin, and dicloxacillin-flucloxacillin has proved as active against Gram-positive cocci, including penicillin-resistant staphylococci. The extent of binding of flucloxacillin to the protein of human serum was similar to that of oxacillin and cloxacillin and less than that of dicloxacillin. In man flucloxacillin given orally produced total and free serum levels higher than those obtained with oxacillin and cloxacillin; total serum levels similar to those of dicloxacillin, and free levels greater than those of dicloxacillin. Similarly, after intramuscular injection the free serum levels of flucloxacillin were higher than those of oxacillin, cloxacillin, and dicloxacillin.

Administration, Oral↗
PubMed1989

In vitro activity of dicloxacillin against methicillin-susceptible and methicillin-resistant Staphylococcus-aureus.

A total of 54 strains of Staphylococcus aureus, 37 methicillin-susceptible (MSSA) and 17 methicillin-resistant (MRSA), were investigated for their susceptibility to dicloxacillin as compared to methicillin and oxacillin by agar plate dilution at two different temperatures of incubation (30 degrees C and 37 degrees C). Against MSSA strains we found a slight but significant increase (0-2 dilution steps) in minimal inhibitor concentrations (MICs) for all three antibiotics with decrease in incubation temperature. Against MRSA strains methicillin and oxacillin showed a 3-6 fold increase in median MIC with decrease incubation temperature. For dicloxacillin, in contrast, there were no significant differences in median MICs (i.e. 0.4 mg/l) against MSSA strains at 30 degrees C or MRSA strains at either incubation temperature. Population-analysis of the MRSA strains revealed, however, that a highly dicloxacillin-resistant subpopulation appeared with a frequency of 10(-6) to 10(-7). Such heterogenous resistance of MRSA strains to dicloxacillin probably prohibits the use of dicloxacillin against serious infections caused by these pathogens.

Dicloxacillin↗
PubMed1987

Stability of dicloxacillin sodium oral suspension stored in polypropylene syringes.

The stability of dicloxacillin sodium in oral suspension stored in clear polypropylene oral syringes was studied. Commercially available dicloxacillin sodium powder for oral suspension from a single lot was reconstituted according to the manufacturer's instructions and drawn into 5-mL clear polypropylene oral syringes. The syringes were divided into groups and stored at -20, 4, 25, 40, 60 or 80 degrees C. Two additional lots were similarly reconstituted, repackaged, and stored at 80 degrees C only to assess interlot variability. Powder in the original containers was similarly reconstituted according to the manufacturer's instructions, and the containers were divided into groups and stored with the syringes. Immediately after reconstitution and at specified times during storage, three syringes and the original containers at each storage temperature were removed, and their contents were analyzed for dicloxacillin sodium concentration using the Standard USP Iodometric Assay. Dicloxacillin sodium follows a first-order rate of degradation at temperatures of 40, 60, and 80 degrees C. The rate of degradation changes to a zero-order process at temperatures of 25, 4, and -20 degrees C. At all temperatures, degradation occurred more rapidly when the drug was repackaged into unit dose polypropylene oral syringes than in the manufacturer's original container. Dicloxacillin sodium reconstituted from powder as oral suspension and repackaged in clear polypropylene syringes was stable for no longer than 7, 10, and 21 days when stored under ambient, refrigerated, and frozen conditions, respectively.

Administration, Oral↗