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PubMed1990

A comparison of erythromycin and cefadroxil in the prevention of flare-ups from asymptomatic teeth with pulpal necrosis and associated periapical pathosis.

In a previous study by our group with patients having asymptomatic teeth with pulpal necrosis and an associated periapical radiolucent lesion (PN/PL), it was shown that prophylactic administration of penicillin V or erythromycin (high-dose, 1-day regimen) resulted in a low incidence of flare-up (mean = 2.2%) and a low incidence of swelling and pain not associated with flare-up. No hypersensitivity responses occurred, and gastrointestinal side effects were found primarily with the erythromycins. To ascertain whether a single-dose administration of a long-acting 1-gm tablet of the cephalosporin antibiotic cefadroxil would result in a similar outcome, the present study was undertaken with 200 patients having quiescent PN/PL. The patients were randomly given either cefadroxil or erythromycin (base or stearate). Evaluations of flare-up were done 1 day, 1 week, and 2 months after endodontic treatment. A 2.0% flare-up incidence was found, with no statistically significant differences for cefadroxil (1.0%), stearate (2.0%), or base (4.0%). No hypersensitivity responses occurred. Gastrointestinal side effects were found primarily with the erythromycins (19.0%). The results showed that a 1-gm, single-dose regimen of cefadroxil was as effective as erythromycin and penicillin in preventing flare-ups and serious sequelae. A comparative analysis of the data from our first study (no peritreatment antibiotics) and the pooled data from our last three investigations (including the current trial) showed that peritreatment antibiotic coverage significantly reduced flare-ups and serious sequelae after endodontic treatment of asymptomatic PN/PL (p less than 0.001).

Acute Disease↗
PubMed1991

Cefadroxil in the management of facial cellulitis of odontogenic origin.

The objectives of this prospective single-blind trial were to compare the efficacy and safety of cefadroxil, 1 gm/day, and cephalexin, 250 mg four times a day, in the treatment of facial cellulitis of odontogenic origin. One hundred sixteen patients were screened for sensitivity to the assigned antibiotic and then randomly assigned treatment groups. Fifty-eight (100%) of the cefadroxil-treated patients and 57 (98%) of the cephalexin-treated patients were considered cured. Adverse reactions were noted in only two cefadroxil-treated patients and one cephalexin-treated patient. One patient from each group discontinued therapy prematurely; the patient who discontinued cephalexin was the only treatment failure in this study. This study found that cefadroxil administered once a day was therapeutically equivalent to cephalexin given four times a day.

Adolescent↗
PubMed2006

Flow injection chemiluminescence determination of cefadroxil using potassium permanganate and formaldehyde system.

A simple, rapid and precise flow injection chemiluminescence (FI-CL) method is proposed for the determination of cefadroxil and is suitable for application to other antibiotics containing phenolic hydroxyl groups. A possible mechanism for this selectivity is suggested. The method is based on the CL-emitting reaction between cefadroxil and potassium permanganate in sulfuric acid medium, enhanced by formaldehyde (HCHO). Under the optimum conditions, calibration graphs over the ranges of 0.05-0.8 and 1.0-10.0 microg ml(-1) were obtained. The proposed method was successfully applied to the determination of cefadroxil in pharmaceutical formulations with no evidence of interference from common excipients. The detection limit (3sigma) of this method is 25 ng ml(-1) (6.9 x 10(-8) mol l(-1)). The relative standard deviation was less than 2% for 0.4 and 4.0 microg ml(-1) cefadroxil (n = 20). The sample throughput was found to be 120 h(-1).

Anti-Bacterial Agents↗
PubMed2003

Derivative spectrophotometry in the analysis of mixtures of cefotaxime sodium and cefadroxil monohydrate.

Derivative spectrophotometry (ratio-spectra 1st- and 2nd-derivative and zero-crossing 2nd-derivative techniques) was applied for the determination of some cephalosporins in two component mixtures. Cefotaxime sodium salt (C(16)H(16)O(7)N(5)S(2)Na) and cefadroxil monohydrate (C(16)H(17)N(3)O(5)S.H(2)O) were examined. In all procedures, the calibration plots are linear up to 43 microg/ml of each antibiotic, with r ranging from 0.9997 to 0.9999. In the ratio-spectra method, the measurements were taken at 239.5 and 291.5 nm (cefotaxime, 1st-derivative), 238 and 283 nm (cefadroxil, 1st-derivative), 284 and 303 nm (cefotaxime, 2nd-derivative), and 229.5 and 245.5 nm (cefadroxil, 2nd-derivative). Detection limits at P=0.05 level of significance, calculated by a statistical treatment of calibration data, ranged from 0.15 to 0.58 microg/ml. LOD and LOQ ranged, respectively, from 0.19 to 0.51 and from 0.63 to 1.70 microg/ml. By the zero-crossing 2nd-derivative method, lines of regression are linear at 257 and 279 nm (cefotaxime) and 242 and 296 nm (cefadroxil). Detection limits from 0.28 to 0.51 microg/ml. LOD and LOQ from 0.27 to 0.41 and from 0.90 to 1.37 microg/ml, respectively. All the samples were tested for stability in solution and in the course of actual analysis, up to 80 h from their preparation. The developed derivative spectrophotometric methods were applied to synthetic mixtures and the RSD values ranged between 0.05 and 1.35% (ratio-spectra technique) and 0.01 and 1.07% (zero-crossing technique). The methods were also applied to vials and tablets for these drugs. The recoveries obtained were between 100.9 and 102.4% (ratio-spectra) and between 99.8 and 102.0% (zero-crossing). The procedures are simple, rapid, and did not require any preliminary separation or treatment of the samples. Instrumentation commonly available was utilised. The cephalosporins analysed are frequently used antibiotics of relevant clinical and pharmacological importance; hence this work would be of interest for the readers of journals devoted to pharmaceutical and biomedical analysis.

Cefadroxil↗
PubMed1992

Erythromycin versus cefadroxil in the treatment of skin infections.

Erythromycin is often overlooked for the treatment of skin and skin structure infections. We evaluated the efficacy and safety of erythromycin particles in tablets and of cefadroxil in 164 patients with skin infections; both treatments were given as 500 mg twice daily. One hundred percent of erythromycin and 96% of cefadroxil patients were clinically cured or improved, and 98% of susceptible pathogens were eradicated in both groups. Only three erythromycin patients and one cefadroxil patient left the study early because of GI-related adverse events. Erythromycin, therefore, was as effective and safe as cefadroxil in the treatment of mild-to-moderate skin infections.

Adolescent↗
PubMed1982

Pharmacokinetics of cefadroxil after oral administration in humans.

The human oral pharmacokinetics of cefadroxil were studied in parallel at doses of 250, 500, and 1,000 mg in three groups of 10 healthy young male volunteers. Renal excretion of intact cefadroxil, accounted for 82, 79, and 77% of the above doses. Mean peak serum levels were dose linear: 9, 18, and 35 microgram/ml at 250, 500, and 1,000 mg, respectively. However, overall pharmacokinetics were linear only in the 250- to 500-mg dose range; apparent serum clearances were 10 liters/h, and true renal clearances were 9 and 8 liters/h at 250 and 500 mg. At 1,000 mg, apparent serum clearance dropped to about 7 liters/h, true renal clearance, dropped to 6 liters/h, and the area under the curve increased disproportionately. At 250 and 500 mg, mean half-life was about 1.2 h; at 1,000 mg, however, it was 1.6h. The nonlinear decrease in clearance could be related to saturation of active renal tubular secretion of cefadroxil between the 500- and 1,000-mg doses. Previous results indicating that cefadroxil has greater persistence than other oral cephalosporins such as cephalexin, cephradine, cefaclor were confirmed.

Administration, Oral↗
PubMed1991

Clinical comparison of cefuroxime axetil, cephalexin and cefadroxil in the treatment of patients with primary infections of the skin or skin structures.

This study was designed to compare the clinical and bacteriological efficacy of three oral cephalosporins, cefuroxime axetil, cephalexin and cefadroxil, in the treatment of patients with mild to moderate infections of the skin or skin structures. A total of 330 patients were enrolled at 10 centers and were randomly assigned to receive cefuroxime axetil 250 mg (n = 107), cephalexin 500 mg (n = 111) or cefadroxil 500 mg (n = 112), twice daily for 10 days. Patients were assessed for their clinical and bacteriological responses once during treatment (3-5 days) and twice after treatment (1-3 and 10-14 days). A total of 353 bacterial isolates were obtained: Staphylococcus aureus (41%), Staphylococcus epidermidis (33%) and Streptococcus pyogenes (5%). A satisfactory clinical outcome (cure or improvement) was achieved in 97% (89/92), 89% (80/90) and 94% (82/87) of the clinically evaluable patients treated with cefuroxime axetil, cephalexin or cefadroxil, respectively (p = 0.047, cefuroxime axetil vs. cephalexin). With respect to the eradication of the bacterial pathogens, a satisfactory outcome (cure or presumed cure) was obtained in 96% (69/72), 85% (60/71) and 93% (63/68) of bacteriologically evaluable patients treated with cefuroxime axetil, cephalexin and cefadroxil, respectively (p = 0.026, cefuroxime axetil vs. cephalexin). All three study drugs were well tolerated, with adverse events affecting the gastrointestinal system most commonly reported. There were no significant differences between treatment groups in the incidence of drug-related adverse events.

Adolescent↗
PubMed1986

A comparison of cefadroxil and penicillin V in the treatment of streptococcal pharyngitis in children.

The efficacy of cefadroxil, an orally administered broad spectrum cephalosporin, was compared with that of penicillin V in several studies comprising more than 550 children with group A beta-haemolytic streptococcal (GABHS) pharyngitis. Both drugs alleviated clinical signs and symptoms and eradicated GABHS from the upper respiratory tract within 18 to 24 hours of the initiation of therapy. Approximately 8% of the patients treated with either cefadroxil or penicillin V had strains of GABHS isolated from 1 of their follow-up throat cultures which were identical to the strains isolated from their initial throat cultures, and were considered bacteriological treatment failures. Compliance was greater than 90% with all of the regimens used, but was significantly better with cefadroxil given as a 30 mg/kg dose once daily than with penicillin V given 3 times daily. There were no serious adverse reactions with either drug. Thus, cefadroxil was shown to be well tolerated and as effective as the standard agent, oral penicillin V, in the treatment of GABHS pharyngitis in children.

Cefadroxil↗
PubMed1986

Cefadroxil compared with cefaclor in the treatment of streptococcal pneumonia in adults.

103 young male Black African gold-miners with pneumococcal pneumonia confirmed by culture or serology were randomly assigned to receive the long acting oral cephalosporin cefadroxil 1 g every 12 hours or cefaclor 500 mg every 8 hours for 10 days. Clinical cures were obtained in 94% of the group who received cefadroxil and in 94% of the cefaclor group. Similarly, the causative organism S. pneumoniae was eradicated in 98% and 96% of patients who received cefadroxil and cefaclor, respectively. Minimal side effects occurred in both groups, although 1 patient withdrew from therapy with cefaclor because of severe diarrhoea. Thus, cefadroxil and cefaclor both displayed effective antimicrobial activity with low toxicity in the treatment of pneumococcal pneumonia.

Adult↗
PubMedDate not supplied

Cefadroxil in skin and skin-structure foot infections: a retrospective review.

The efficacy and safety of cefadroxil in eradicating localized skin and skin-structure infections of the foot were investigated in a retrospective chart review of 222 consecutive patients from two private practices seen over a 10-year period. Of the 189 patients for whom follow-up data were available, 187 (99%) received cefadroxil 500 mg twice daily, and 2 patients (1%) received 250 mg twice daily. The duration of therapy was 2 weeks or less in 87% of patients, with a median duration of therapy of 11.4 days (range, 5 to 35 days). Of the 189 clinically evaluable patients, 179 (95%) achieved a favorable clinical response to treatment; of the 57 patients with microbiologic cultures, 54 (95%) experienced a satisfactory bacteriologic response to therapy; no adverse events related to cefadroxil therapy were identified during the review. The overall results from this retrospective study suggest that cefadroxil is an effective agent with a favorable safety profile for the treatment of skin and skin-structure infections of the foot.

Adolescent↗
PubMed1989

A randomised, prospective, single-blind comparison of cefadroxil and amoxycillin in the treatment of acute exacerbations of chronic bronchitis.

Cefadroxil 1 g twice daily and amoxycillin 500 mg three times a day were compared in 111 patients suffering from acute exacerbations of chronic bronchitis. Treatment was for seven days. Excellent or good clinical responses were found in 85 per cent of cases receiving cefadroxil and 81 per cent of patients taking amoxycillin. However, residual symptoms of cough and rhonchi were present to a statistically significantly greater extent in the amoxycillin group. Tolerance of both drugs was good with mild to moderate side effects reported in seven of 54 patients in the cefadroxil group and six of 56 patients taking amoxycillin. Severe nausea and vomiting in two cases in the amoxycillin group resulted in discontinuation of therapy. Microbiological examination of sputum samples showed pathogenic bacteria in 16 per cent, principally Haemophilus influenzae. Amoxycillin 500 mg tds and cefadroxil 1 g bd were equally effective in the treatment of acute exacerbations of chronic bronchitis.

Adolescent↗
PubMed1980

[Bacteriological study on cefadroxil in vitro. Correlation between diameter of inhibition zone and inhibitory concentration (author's transl)].

There are only slight differences between the geometrical means of minimum inhibitory concentrations of (6R,7R)-7-[(R)-2-amino-2-2(p-hydroxyphenyl)-acetamido]-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (cefadroxil, Bidocef) and cefalexin against gram-positive and gram-negative bacteria freshly isolated from clinical material. Enterococci are more susceptible to cefadroxil. Considering the different break point, cefadroxil is on the whole more effective than cefalexin, in particular so against Proteus mirabilis, Enterobacter, Citrobacter and Escherichia coli. With the aid of the described regression analysis a meaningful interpretation of the results of the cefadroxil agar diffusion test is possible.

Bacteria↗
PubMed1980

[Microbiological assay method of cefadroxil in biological specimens (author's transl)].

A microbiological method for quantitative determination of cefadroxil in biological specimens is described. This method is essentially a cylinder-plate or a paper-disc method using Micrococcus luteus ATCC 9341 as the test organism grown in the tryptosoya broth added with 1.5% agar. Cefadroxil standard calibration curves are prepared in pooled human serum, moni-trol I or consera for the determination of serum level of human, and 0.1 M phosphate buffer (pH 6.0) to determine urine level. Cefadroxil in human serum and urine specimens can be measured by cylinder-plate method as low as 0.16 approximately 0.31 micrograms/ml and 0.08 approximately 0.16 micrograms/ml, respectively. Further, any active metabolites of cefadroxil were not detected on human and rat urine specimens by bioautography.

Animals↗
PubMed1981

[Fundamental and clinical studies on cefadroxil dry syrup in children (author's transl)].

Fundamental and clinical studies were made on cefadroxil, a new oral cephalosporin, and the following results were obtained. (1) Antibacterial activity of the drug against S. aureus, S. epidermidis, E. coli, Klebsiella, Salmonella and P. mirabilis was almost equal to that of cephalexin. The MIC of indole positive Proteus. Enterobacter, Citrobacter, S. marcescens and P. aeruginosa to cefadroxil was higher than 100 microgram/ml in almost all strains. (2) Serum concentrations following an oral administration of 10.0 to 14.3 mg/kg of cefadroxil dry syrup was highest at 2 hours in 2 cases and 1 hour in 1 case, respectively, which were 13.4 to 17.1 microgram/ml, and 1.8 to 6.8 microgram/ml at 4 hours with an T 1/2 of 1.04 to 1.62 hours and apparently longer continuation of serum concentration than that of cephalexin. Urinary recovery rate was 75-96% up to 6 hours. (3) Fourteen patients, i.e., 6 with tonsillitis and 8 with urinary tract infection, were treated with a daily oral dose of 30-50 mg/kg divided in 4 doses except 1 case divided in 3 doses. The overall efficacy rate was 100%, i.e., excellent in 13, good in 1 and no failure. Causative organisms disappeared in all cases. (4) Adverse reactions, such as diarrhea and skin rash, were not noted at all and 1 case presented a mild elevation of GOT and GPT. (5) Taste and flavor of the drug was well palatable to children. (6) Based on the above results, it is concluded cefadroxil dry syrup is a new potent cephalosporin for oral use in the treatment of acute bacterial infection in children. Daily dose of 40 mg/kg in 3-4 divided doses appeared to be appropriate.

Administration, Oral↗
PubMed1981

[Clinical experience with cefadroxil dry syrup in pediatric infections (author's transl)].

Cefadroxil was administered to 16 pediatric patients at dose levels ranging from 27 to 56 mg/kg daily for 5-9 consecutive days. Of 16 patients, 9 had urinary tract infections including 5 cases with nephrotic syndromes, 4 had respiratory tract infections including 2 cases with nephrotic syndromes, 3 had skin infections including 2 cases of pyoderma and 1 case of suppurative gingivitis, including 1 case with nephrotic syndrome. Clinical results obtained were 9 'excellent', 4 'effective' and 3 'ineffective' showing an efficacy ratio of 81%. Of 9 urinary tract infections, 5 patients exhibited bacteriuria and 3 had original pathogens persisting after treatment. In respiratory tract, skin and gingival infections, cefadroxil was either 'excellent' or 'effective' in all 7 patients. The above results demonstrate a distinctive feature of cefadroxil that attains a good cutaneous distribution after oral administration. The absorption of the drug was not adversely affected by a food intake. No significant side effects were observed in all 16 patients. Judging from our clinical results, cefadroxil is considered one of the valuable cephalosporin antibiotics in the treatment of pediatric infections.

Cefadroxil↗
PubMed1995

Experimental studies on the influence of surfactants on intestinal absorption of drugs. Cefadroxil as model drug and sodium lauryl sulfate as model surfactant: studies in rat duodenum.

The effect of sodium lauryl sulfate (CAS 151-21-3) on the duodenal absorption of cefadroxil (CAS 50370-12-2) has been investigated with the aid of a classical rat gut in situ preparation. Both compounds were entirely compatible in working solutions. Cefadroxil was found to be very stable and only slightly solubilized in the micellar phase. The apparent first-order absorption rate constants for the free antibiotic fraction were determined in free solution, and in the presence of variable surfactant concentration in luminal fluid. A functional interpretation of these data, based both on the law of mass action and the complete noncompetitive transport inhibition equations, showed that the surfactant acts as a nonspecific inhibitor of the carrier-mediated absorption of the antibiotic, but also as an enhancer of its passive absorption component. The net result was an outstanding reduction in the absorption capacity of cefadroxil when it was perfused at 0.1 mg/ml, i.e. far from its carrier saturation (from 3.0 h-1 in free solution to 2.0(-1) at high surfactant concentration, with a minimum of about 1.4 h-1 in the presence of the surfactant at 0.5 mg/mg in duodenal fluid). When cefadroxil was perfused at 10.0 mg/ml, i.e. with its carrier-mediated transport beyond the saturation, the net result was a progressively enhanced absorption (ranging from about 0.9 h-1 in free solution to 2.0 h-1 at high surfactant concentration).(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1995

Experimental studies on the influence of surfactants on intestinal absorption of drugs. Cefadroxil as model drug and sodium lauryl sulfate as model surfactant: studies in rat colon.

The effect of the anionic surfactant, sodium lauryl sulfate (CAS 151-21-3), on the absorption of cefadroxil (CAS 50370-12-2) as model antibiotic in colon has been studied by means of an in situ rat gut technique, as a previous step to investigate the influence of the surfactant on the intestinal, carrier-mediated absorption of the antibiotic. Microbial degradation tests were initially performed, which demonstrated that cefadroxil disappearance from luminal content was only due to absorption. Micelle solubilization of cefadroxil was also previously assessed through dialysis tests in order to adequately correct absorption rate constant values found in the presence of the surfactant at supramicellar concentration. Micelle solubilization was minimal, although statistically significant. Apparent passive absorption rate constants, ka(h-1), were determined in the presence of variable concentrations of lauryl sulfate in perfusion fluids. Results showed that ka values greatly increased as surfactant luminal concentration increased until an asymptotic value (about 7-fold higher than cefadroxil alone) was obtained; this was assumed to be due to a direct effect of the surfactant on membrane polarity. Moreover, the results were satisfactorily adjusted using a functional hyperbolic-type equation, as occurs with many other saturable processes. This was supposed to be indicative that the surfactant effect is due to an adsorption process of the surfactant ions or molecules to the intestinal absorbent membrane.

Animals↗
PubMed1994

Transport of cefadroxil in rat kidney brush-border membranes is mediated by two electrogenic H+-coupled systems.

The transport characteristics of the aminocephalosporin [3H]cefadroxil have been studied in brush-border membrane vesicles (BBMV) of rat kidney cortex by a rapid filtration technique and by use of a potential sensitive fluorescent dye. Influx of [3H]cefadroxil (0.25 microM) into BBMV as a function of time displayed a pronounced overshoot phenomenon in the presence of a transmembrane pH gradient (pHin > pHout). Evidence for an electrogenic cefadroxil/H+-symport in the presence of an inwardly directed proton gradient is provided by the demonstration of: 1) reduced uptake in the presence of a protonophore; 2) reduced uptake under voltage clamp conditions; and 3) increased uptake in the presence of a valinomycin-induced inside negative K+-diffusion potential. pH-gradient dependent uptake of [3H]cefadroxil as a function of substrate concentration revealed the presence of multiple carrier systems. By kinetic analysis, a high-affinity carrier system (Km, 8.8 +/- 1.3 microM) and a low-affinity system (Km, 2.62 +/- 0.80 mM) could be resolved. The high-affinity transport system was found to be very specific for substrates (cephalosporins and di- and tripeptides) carrying an alpha-amino group. By use of a potential sensitive fluorescent dye 3,3'-dipropylthiadicarbocyanine iodide, the low-affinity transport system was characterized with respect to its driving force and its kinetic features. This transporter was found also to be electrogenic in nature, representing a second cefadroxil/H+-symport system. In summary, our studies demonstrate for the first time uphill transport of cefadroxil in kidney BBMV mediated by multiple carrier systems. Transport is rheogenic, energized by the proton motive force and shared by other aminocephalosporins as well as di- and tripeptides.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗