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PubMed1986

Cefadroxil in the treatment of susceptible infections in infants and children.

The efficacy and safety of cefadroxil in the treatment of paediatric patients with a wide variety of infections were evaluated in a multicentre clinical trial. This study included 395 infants and children with Group A streptococcal pharyngitis, sinusitis, otitis media, bronchitis, pneumonia or bronchopneumonia, urinary tract infections and acute gastroenteritis. Cefadroxil was given as a suspension in a daily dose of 30 to 50 mg/kg in 2 divided doses every 12 hours to all but 76 patients; 50 patients with acute otitis media were given 100 mg/kg/day in 2 doses and 26 patients with urinary tract infections received 25 mg/day once daily. Of 317 patients with respiratory tract infections and 78 with urinary or gastrointestinal infections, 95 and 100%, respectively, were clinically cured following treatment with cefadroxil.

Adolescent↗
PubMed1988

Five versus ten days treatment of group A streptococcal pharyngotonsillitis: a randomized controlled clinical trial with phenoxymethylpenicillin and cefadroxil.

216 patients aged greater than or equal to 7 years with febrile group A streptococcal pharyngotonsillitis were randomly assigned to 3 treatment groups receiving either phenoxymethylpenicillin for 5 days followed by placebo for 5 days, phenoxymethylpenicillin for 10 days, or cefadroxil for 10 days. 209 patients completed treatment, 70 subjects in each phenoxymethylpenicillin group and 69 in the cefadroxil group. Within 1 week after completion of the antibiotic treatment significantly more recurrences with the same T-type as the initial streptococcal strain occurred in the 5-day treatment group (27%) as compared with the two 10-day groups (6% and 3%, respectively). The cumulative rate of recurrences (irrespective of T-type) within 2 months from the start of therapy was 55% among patients treated with phenoxymethylpenicillin for 5 days, 24% among those treated for 10 days with this drug and 19% among patients receiving cefadroxil. Obviously, one important factor to avoid recurrence of group A streptococcal pharyngotonsillitis is the length of antibiotic treatment and, in our opinion, it is not advisable to change the current recommendation of 10 days treatment.

Adolescent↗
PubMed1989

Cefadroxil as an alternative to metronidazole in the treatment of bacterial vaginosis.

A randomized single-blind study was performed to compare the efficacy of cefadroxil to that of metronidazole in the treatment of bacterial vaginosis. 22 women completed the study with follow-ups after 1 and 4 weeks. After completion of treatment 2/11 women receiving metronidazole still had bacterial vaginosis compared with 1/11 women receiving cefadroxil. At follow-up after 4 weeks 3/10 women treated with cefadroxil had recurrent bacterial vaginosis while the corresponding figures for metronidazole were 2/9.

Adult↗
PubMed1990

[Alteration of IgE production by cefadroxil].

The effect of two cephalosporins, cefadroxil and cefalexine, was in vitro studied by using two models of regulation of the IgE production in healthy humans, e.g. the induction of CD23-antigens on B-cells and the IgE synthesis in cell culture supernatants after stimulation by recombinant interleukin-4. Cefadroxil clearly inhibited CD23 membrane expression on normal human B-lymphocytes. In the same way, this cephalosporin blocked up to 90% of the in vitro interleukin-4-dependent IgE production by normal peripheral blood mononuclear cells. Cefalexine was unable to do the same. There results suggest that cefadroxil interplays with the regulation processes of the IgE production in humans.

Antigens, Differentiation, B-Lymphocyte↗
PubMed1989

Efficacy of cefadroxil in the treatment of bacterial dermatitis in dogs.

Cefadroxil was found to be an effective antibiotic for the treatment of canine bacterial pyoderma. Bacterial pyoderma was diagnosed in 30 dogs, which were treated with cefadroxil administered orally at 22 mg/kg of body weight, q 12 h, for 21 to 30 days. Dogs were reexamined at the conclusion of antibiotic treatment, and 29 were found to have good to excellent response. On the basis of this study, cefadroxil is a good choice in the treatment of canine pyoderma when cephalosporins are necessary. Efficacy, frequency of administration, cost, and veterinary approval are the major advantages.

Animals↗
PubMed1988

Once-daily cefadroxil versus oral penicillin in the pediatric treatment of streptococcal pharyngitis.

Thirty-two patients with pharyngitis were randomly assigned to receive either 30 mg/kg of cefadroxil every 24 hours orally or 15 mg/kg of penicillin V potassium every eight hours orally for ten days. Sera for antistreptolysin-O, streptozyme, and anti-DNAase were compared before and after treatment. Twenty patients finished the study and had a confirmed throat culture for the group A streptococcus and at least one fourfold antibody rise. Of these 20 patients, seven of eight in the penicillin group and all 12 in the cefadroxil group were cured at the end of therapy. One patient in the penicillin group had a positive culture at the end of therapy; one patient in each group was recolonized at follow-up culture 10 to 20 days after ending therapy. Seven other patients who finished the study had a positive throat culture but no antibody response and were presumed carriers; these included five in the penicillin and two in the cefadroxil group. One of these presumed carriers had a persistent infection and relapsed two days after the end of therapy. Both therapies appeared to be equally successful and no serious side effects occurred.

Adolescent↗
PubMed1984

Comparison of cefadroxil and ampicillin in the treatment of urinary tract infections in children.

The therapeutic efficacy of 25 mg/kg of cefadroxil administered once daily was compared with that of 50 mg/kg/day of ampicillin administered in four equal doses in the treatment of acute uncomplicated urinary tract infections (UTIs) in children. Nineteen girls and seven boys (mean age, 5.5 years) received cefadroxil, and 18 girls and eight boys (mean age, 5.9 years) received ampicillin. The clinical and bacteriological characteristics, as well as the demographic characteristics, of both populations were well matched. Patients with structural anomalies or with a history of hypersensitivity to cephalosporins or penicillins or abnormal hepatorenal function were excluded from the trial. Only patients with at least two consecutive positive cultures of a single pathogen, obtained in clean-catch midstream urine samples (greater than or equal to 10(5) colony-forming units per ml urine) and susceptible to the respective antibiotic, were admitted to the study. Urine cultures were repeated during the ten days of treatment and ten days after the completion of treatment. All patients in the cefadroxil group were evaluated as clinically and bacteriologically cured. Three (12%) of the patients in the ampicillin group had positive cultures in the immediate post-treatment period. The differences in the cure rates of the two groups were not statistically significant. No adverse effects of either antibiotic were observed.

Ampicillin↗
PubMed1980

[Studied on protein binding of cefadroxil and some other cephalosporins (author's transl)].

1. Human serum protein binding of cefadroxil and some other cephalosporins were determined by centrifugal ultrafiltration (U.F.) method and equilibrium dialysis (E.D.) method. The binding rates of cefadroxil were 28.1% by U.F. method and 3.8% (beta 1*), 11.6% (beta 2*) by E.D. method. 2. Protein binding of cefadroxil with sera of various animal species were also determined by E.D. method. The binding rates were low as well as that with human serum. 3. With two popular calculation formula for E.D. method, binding rate was considered on the alteration of the ratio of V2/V1.

Animals↗
PubMed1981

[Clinical results of cefadroxil in pediatric field (author's transl)].

Cefadroxil was administered at a daily dose of 50 mg/kg in 113 children including acute respiratory tract infections suspected to be a bacterial infection and other febrile diseases. Among 41 cases in which pharyngeal culture was made twice before and after administration or urine and feces cultures were made, 20 cases (48.8%) were good bacteriologically, 5 cases (12.2%) were poor, and 16 cases (39.0%) were unknown. Clinical efficacy was obtained in 105 cases (92.9%) out of 113 cases. Microbial substitution was noticed in 12 cases (29.3%) out of the cases of which pharyngeal culture was made after cefadroxil administration. Haemophilus influenzae was detected newly after the administration in 7 cases (58.3%) out of these 12 cases. Bacteriological efficacy was obtained in 5 cases of acute respiratory tract infection of which pathogen was considered to be Haemophilus influenzae. No microbial substitution was noticed in these 5 cases. As to the side effects of cefadroxil administration, only a slight diarrhea was observed in 2 cases.

Adolescent↗
PubMed1981

[Clinical investigations of cefadroxil in the infections of children (author's transl)].

Clinical investigations were performed on clinical effects of cefadroxil, and the following results were obtained. 1. Cefadroxil was administered at a daily dose of 30 mg/kg divided into 3 times in 24 cases of acute tonsillitis and pharyngitis, and clinical results were obtained; remarkably excellent in 8 cases, good in 13 cases, and poor in 3 cases. 2. It was suggested, though the case numbers were limited, that higher efficacy may be obtained in urinary tract infection. 3. No noteworthy side effect was observed throughout all 29 cases, and cefadroxil will be expected to be administered safely in pediatric field.

Cefadroxil↗
PubMed1976

Treatment of skin and soft tissue infections with cefadroxil, a new oral cephalosporin.

Oral cefadroxil in doses of 0-6-1-8 g per day given on twice or three times daily schedules was effective in the treatment of thirty-six patients with infections such as abscesses, carbuncles, cellulitis, furunculosis and impetigo. Staphylococcus aureus strains and beta-haemolytic streptococci, alone or in combination, were cultured from lesions before treatment. In vitro studies with test discs showed that all the organisms were sensitive to cefadroxil, but twenty-three of twenty-nine S aureus strains and one of the seven streptococci strains were resistant to penicillin G. Pre- and post-treatment laboratory tests of renal, hepatic and haematopoietic functions produced no evidence of drug toxicity. The cefadroxil dosage effective in this study is lower than that recommended for currently available oral cephalosporins, which must be given on a four times daily schedule.

Adolescent↗
PubMed1998

Analysis of cefadroxil by micellar electrokinetic capillary chromatography: development and validation.

A method is developed and validated for analysis of the antibiotic cefadroxil using micellar electrokinetic capillary chromatography. It permits cefadroxil to be completely separated from ten of its known related substances within 15 min (including the washing procedure). The separation is performed in an acetate buffer (50 mM, pH 5.25) containing sodium dodecyl sulfate (SDS; 110 mM). The fused-silica capillary was 44 cm long (36 cm effective length), 50 microm ID; the voltage, 18 kV; temperature, 15 degrees C; and the detection wavelength; 254 nm. The influence of the type of buffer, buffer pH and concentration, and of the SDS concentration was investigated. The robustness of the method was examined by means of a full-fraction factorial design. The parameters for validation such as linearity, precision, limit of detection and limit of quantitation are also reported.

Cefadroxil↗
PubMed1981

Degradation kinetics and mechanism of aminocephalosporins in aqueous solution: cefadroxil.

The degradation kinetics and mechanism of a new, orally effective cephalosporin derivative, cefadroxil, in aqueous solution were investigated at pH 2.51-11.5 at 35 degrees and ionic strength 0.5. The degradation rates were determined by high=pressure liquid chromatography. At constant pH and temperature, the degradation followed first-order kinetics and a log k-pH profile was presented. The shape of the rate-pH profile resembled that for cephalexin or cephradine under the same conditions. Citrate and phosphate buffers enhanced general acid and base catalysis of the degradation. In aqueous solution, cefadroxil was shown to degrade by three parallel reactions: (a) intramolecular aminolysis by the C-7 side-chain amino group on the beta-lactam moiety, (b) water-catalyzed or spontaneous hydrolysis, and (c) beta-lactam cleavage by the nucleophilic attack of hydroxide ion. In neutral and weak alkaline solutions, the main degradation products were two piperazine-2, 5-diones and 3-hydroxy-4-methyl-2(5H)-thiophenone, the former being formed from Reaction a, while the latter arose via the degradation pathways of Reaction b and/or c.

Buffers↗
PubMed1987

Concentrations of phenoxymethylpenicillin and cefadroxil in tonsillar tissue and tonsillar surface fluid.

Thirty patients who underwent elective tonsillectomy were given phenoxymethylpenicillin (0.8 g) or cefadroxil (1 g) at different times before operation. The concentrations of the antibiotics were analysed in serum, tonsillar tissue, fluid from the surface of the tonsils, and mixed saliva. The concentrations in tonsillar tissue for both drugs were much lower than the corresponding serum concentrations. This apparently low tissue accessibility could be ascribed to the limited intracellular penetration of beta-lactam antibiotics. For both antibiotics the concentrations in the tonsillar surface fluid were higher than the levels in the tissue and well above the minimal inhibitory concentrations for streptococci. This was not due to antibiotics in saliva but probably a result of leakage from the interstitial fluid. Inability to reach active concentrations of phenoxymethylpenicillin or cefadroxil at the site of infection does not therefore seem to be a probable cause for relapse after treatment of streptococcal tonsillitis.

Adolescent↗
PubMedDate not supplied

Pharmacokinetic parameters and killing rates in serum of volunteers receiving amoxicillin, cefadroxil or cefixime alone or associated with niflumic acid or paracetamol.

Pharmacokinetic parameters and killing rates in serum of volunteers receiving amoxicillin, cefadroxil or cefixime alone or associated with niflumic acid or paracetamol were studied. Niflumic acid (250 mg) or analgesic and antipyretic drugs such as paracetamol (500 mg) are often combined with antibiotics to avoid inflammation and pain in acute ear, nose and throat diseases. Pharmacokinetic interactions between these two classes of drugs have been described in experimental models, and exceptionally in humans. The aim of the present investigation was to study the interactions of these two drugs with three antibiotics (amoxicillin 500 mg x 2, cefadroxil 500 mg x 2, cefixime 200 mg and one placebo capsule) on pharmacodynamic parameters and on rate of killing in the serum of six healthy volunteers receiving the antibiotic associated or not with the product in a randomized cross-over double-blind trial. The bacteria most often involved in sinusitis, bronchitis and otitis media (Haemophilus influenzae, Streptococcus pneumoniae, Staphylococcus aureus) three target diseases for oral cephalosporins and amoxicillin, were chosen for bacteriological study. Blood samples were obtained at 0.25, 0.50, 1, 1.5, 2, 4, 6 and 12 h after oral administration of antibiotics alone or associated with the drugs. There was a wash-out period of at least 1 week between the eleven sequences. Antibiotics were measured by two methods: bioassay and high performance liquid chromatography (HPLC). All serum samples obtained at peak level, 4 and 6 h were tested for killing rate. Area under the time kill curve was calculated by the trapezoidal rule method and relative bioactivity in percent was defined as follows: (AUC control - AUC test)/AUC control x 100. No pharmacokinetic interaction was found in the AUC and T1/2 of the plasma concentrations of the antibiotics or associated with the drugs, regardless of dose, as determined by HPLC or microbiological assay. For these beta-lactam antibiotics killing rate was found to be time-dependent. Bactericidal activity was improved on H. influenzae when cefixime was associated with niflumic acid and became concentration-dependent. A significant concentration relation was also found with niflumic acid or paracetamol associated with cefixime on Strep. pneumoniae.

Acetaminophen↗
PubMed1994

Cefadroxil concentrations in human serum, gingiva, and mandibular bone following a single oral administration.

Cefadroxil concentrations in human serum, gingiva, and mandibular bone were measured by a paper disk method following a single 500-mg oral dose. The mean peak concentrations in serum, gingiva, and mandibular bone occurred at the identical time, 3 hours, and were 12.92 micrograms/mL, 6.50 micrograms/g, and 2.67 micrograms/g, respectively. Mean cefadroxil concentration ratios of gingiva/serum and mandibular bone/serum at the peak time were 0.54 and 0.21, respectively. Mean concentrations in gingiva and mandibular bone at the peak time exceeded the minimum inhibitory concentrations for 90% of clinically isolated strains of a alpha-hemolytic streptococci.

Absorption↗
PubMed1997

The pharmacokinetics of cefadroxil over a range of oral doses and animal ages in the foal.

To evaluate the effect of foal age on the pharmacokinetics of cefadroxil, five foals were administered cefadroxil in a single intravenous dose (5 mg/kg) and a single oral dose (10 or 20 mg/kg) at ages of 0.5, 1, 2, 3 and 5 months. Pharmacokinetic parameters of terminal elimination rate constant (beta(po)), oral mean residence time (MRTpo), mean absorption time (MAT), rate constant for oral absorption (Ka), bioavailability F, peak serum concentrations (Cmax) and time of peak concentration (tmax), were evaluated in a repeated measures analysis over dose. Across animal ages, parameters for the intravenous dose did not change significantly over animal age (P > or = 0.05). Mean values +/- SEM were: beta(IV) = 0.633 +/- 0.038 h-1; Cl = 0.316 +/- 0.010 L/kg/h; Vc = 0.196 +/- 0.008 L/kg; Varea = 0.526 +/- 0.024 L/kg; VSS = 0.374 +/- 0.014 L/kg; MRTiv = 1.22 +/- 0.07 h; Kel = 1.67 +/- 0.08 h-1. Following oral administration, drug absorption became faster with age (P < 0.05), as reflected by MRTpo, MAT, Ka and tmax. However, oral bioavailability (+/- SE) declined significantly (P < 0.05) from 99.6 +/- 3.69% at 0.5 months to 14.5 +/- 1.40% at 5 months of age. To evaluate a dose effect on the pharmacokinetic parameters, a series of oral doses (5, 10, 20 and 40 mg/kg) were administered to these foals at 1 month of age. beta(po) (0.548 +/- 0.023 h-1) and F (68.26 +/- 2.43%) were not affected significantly by the size of the dose. Cmax was approximately doubled with each two-fold increase in dose: 3.15 +/- 0.15, 5.84 +/- 0.48, 12.17 +/- 0.93 and 19.71 +/- 2.19 micrograms/mL. Dose-dependent kinetics were observed in MRTpo, MAT, Ka and tmax.

Administration, Oral↗
PubMed1990

The in-vitro activity of ceftibuten against 475 clinical isolates of gram-negative bacilli, compared with cefuroxime and cefadroxil.

The in-vitro activity of ceftibuten was compared with cefuroxime and cefadroxil against 475 clinically-significant, epidemiologically-distinct isolates of Gram-negative bacilli: 170 from blood, 212 from urine and 93 from a supplementary collection of multiply-resistant strains known to have resistance plasmids, to have caused sporadic or epidemic nosocomial infection, or both. Ceftibuten MICs ranged from 0.003 to greater than 32 mg/l, with a modal MIC of 0.01 mg/l: 95% of all isolates had ceftibuten MIC values of less than or equal to 8 mg/l, the sensitivity breakpoint suggested by the manufacturer. Ninety per cent of isolates had MICs of less than or equal to 1 mg/l and 49% had MICs of less than or equal to 0.03 mg/l. All isolates of Klebsiella, Serratia, Proteus and Providencia spp., and Morganella morganii had MIC values of 8 mg/l or less. Only two of 124 isolates of Escherichia coli tested, and only one of 23 Citrobacter spp., had MICs of greater than 8 mg/l (16, 16 and greater than 32 mg/l respectively). Resistance MIC greater than 16 mg/l) was more frequent among Enterobacter and Acinetobacter spp. Thirteen of 52 Enterobacter spp., and seven of 18 Acinetobacter calcoaceticus had MICs of at least 32 mg/l. MIC ranges, modal MICs and MIC90s indicated that ceftibuten was, with the exception of only two strains, consistently more active in-vitro than cefuroxime, which was in turn more active than cefadroxil.

Bacterial Infections↗