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At least 19 recordsLinked to original sources

PubMed1985

Concentrations of ampicillin and cefadroxil in human serum and mixed saliva following a single oral administration of talampicillin and cefadroxil, and relationships between serum and mixed saliva concentrations.

The concentrations of ampicillin (ABPC) from talampicillin (TAPC) and cefadroxil (CDX) in serum and mixed saliva were assayed by the thin layer disc plate method. Talampicillin and cefadroxil (500 mg) were given by a single oral administration. The relationships between serum and mixed saliva ampicillin and cefadroxil concentrations were evaluated in the paired specimens collected from 10 different persons, respectively. The means of concentration ratios of mixed saliva to serum ampicillin and cefadroxil were 0.006 +/- 0.003 and 0.025 +/- 0.010 (mean +/- SD), respectively. Significant correlation coefficients between mixed saliva and serum concentrations were found for both ampicillin and cefadroxil, which were r = 0.78, P less than 0.001, and r = 0.67, P less than 0.001, respectively.

Adult↗

PubMed1991

Dose-dependent absorption and elimination of cefadroxil in man.

The pharmacokinetic behaviour of cefadroxil was dose-dependent in healthy male volunteers following the oral administration of single doses of 5, 15, and 30 mg.kg-1. As the dose of cefadroxil increased from 5 to 15 and 30 mg.kg-1, the peak plasma concentrations, normalized to 5 mg.kg-1, decreased significantly from 15.1 to 10.7 and 7.6 mg.l-1, while the corresponding normalized areas under the plasma concentration-time curves from 0 to 2 h decreased significantly from 1258 to 946 and 801 min.mg.l-1. When the same subjects were given 5 mg.kg-1 of cefadroxil together with 45 mg.kg-1 of cephalexin, the absorption of cefadroxil was slowed to a similar or greater extent than with the high dose of cefadroxil. Although the absorption rate decreased as the dose increased, the systemic availability of cefadroxil was essentially complete at all doses, as judged by the 24 h urinary recoveries of the antibiotic. Kinetic analysis of the plasma concentration-time curves gave the best fit with a zero-order followed by a first-order absorption process, consistent with saturable intestinal absorption of cefadroxil. The elimination rate of cefadroxil was directly related to dose and plasma concentrations, and the clearance at the dose of 5 mg.kg-1 was significantly increased by the simultaneous administration of high-dose cephalexin. The renal clearance of cefadroxil ranged from 98 ml.min.l-1 at total plasma cephalosporin (cefadroxil + cephalexin) concentrations less than 2.5 mg.l-1 to 156 mg.l-1 at concentrations greater than 40 mg.l-1.(ABSTRACT TRUNCATED AT 250 WORDS)

Absorption↗

PubMed1992

Uptake of cefadroxil derivatives in rat intestinal brush-border membrane vesicles.

Uptake of cefadroxil and its two acetyl-derivatives, N-acetyl- and O-acetyl-cefadroxil, into the brush-border membrane vesicles (BBMV) was measured at [pH]o = 5.5, 7.4 and [pH]i = 7.4. Both acetyl-derivatives showed a significantly slower uptake than cefadroxil at [pH]o = 5.5 and 7.4. Cefadroxil and the two derivatives showed a higher uptake rate in the presence of an inward H+ gradient ([pH]o = 5.5, [pH]i = 7.4). At [pH]o = 5.5, uptake of cefadroxil into BBMV was inhibited by N-acetyl-, O-acetyl-, N-BOC-, and N-BOC-O-acetyl-cefadroxil, but not by cephalothin and cefuroxime. At [pH]o = 7.4, no inhibition of cefadroxil uptake was evident for any inhibitors. There were two different transporters responsible for the uptake of cefadroxil at pH 5.5 and 7.4. One is the H(+)-coupled dipeptide transport system, and the other is the neutral pH-preferring system. The alpha-amino group may be essential for the transport of cefadroxil by both transport systems. Although the phenolic group in the side chain is not an essential functional group of beta-lactam antibiotics, an additional derivation on the phenolic group of cefadroxil also inhibited both the H(+)-coupled dipeptide transport system and the neutral pH-preferring transport system.

Animals↗

PubMed1991

[The biological availability of cefadroxil given simultaneously with N-acetylcysteine].

A preliminary study revealed that similarly to the antibiotics amoxillin, thiamphenicol, erythromycin and doxycycline, the oral cephalosporin cefadroxil (CAS 66592-87-8) can be administered simultaneously with the mucolytic n-acetylcysteine (CAS 616-91-1). In the present study 12 healthy male volunteers received in a randomised cross-over design a single oral dose of 1000 mg cefadroxil or a single oral dose of 1000 mg cefadroxil (Bidocef) plus 200 mg n-acetylcysteine. The two study days were separated by a wash-out period of one week. To determine the pharmacokinetic profile of cefadroxil, plasma and sputum were analysed by HPLC at defined intervals. Regarding the bioavailability of cefadroxil, the free combination is bioequivalent to the individual component. After administration of cefadroxil plus n-acetylcysteine, a higher cefadroxil concentration was found in the sputum compared to an administration of cefadroxil alone. However, the difference was not statistically significant. According to the results, simultaneous administration of the oral cephalosporin cefadroxil and the mucolytic n-acetylcysteine is possible without changes in the bioavailability of cefadroxil being observed.

Acetylcysteine↗

PubMed1979

[General pharmacology of cefadroxil (author's transl)].

The general pharmacological properties of cefadroxil which is a new semisynthetized cephalosporin were examined and following results were obtained. 1) Cefadroxil had no appreciable influences on the central nervous system in mice and the EEG in cats. 2) Cefadroxil had no effects on the isolated smooth muscle organs. 3) Cefadroxil had no effects on the passage of charcoal meal in mice and the motility of the stomach in situ in rabbits. 4) Cefadroxil inhibited the gastric secretion in pylorus-ligated rats. 5) Cefadroxil induced no marked changes in the respiration, blood pressure, heart rate, electrocardiogram and femoral blood flow in anesthetized dogs. Cefadroxil had no effects on the isolated hearts and ear vessles of rabbits. 6) Cefadroxil decreased the urine volume and the excretion of electrolytes (Na+, K+ and Cl-) in first three hours in rats. 7) Cefadroxil increased the biliary secretion in rats. No significant effects of cefadroxil were found in the other pharmacological experiments.

Animals↗

PubMed1990

Cefadroxil kinetics and dynamics in a pediatric patient with acute osteomyelitis.

Cefadroxil has been used for the treatment of acute osteomyelitis. However, its pharmacokinetics and pharmacodynamics have not been studied in these patients. We evaluated the kinetics and dynamics of cefadroxil in a pediatric patient with osteomyelitis caused by Staphylococcus aureus. After initial clinical improvement on intravenous nafcillin, the patient received oral cefadroxil, 60 mg/kg every 12 h. Blood samples were collected at 0, 1, 2, 4, 6, 8 and 12 h; bactericidal titers were determined at 2 and 12 h. Cefadroxil was measured by an HPLC method. The peak and trough serum concentration of cefadroxil was 35.4 and 0.5 micrograms/ml, respectively. The oral clearance and elimination half-life were 11.5 ml/min/kg and 2.4 h, respectively. The peak bactericidal titer was 1:4 and the trough titer was less than 1:2 for the infecting organism. The child's finger appeared worse with an increase in swelling and erythema after 2 days of cefadroxil therapy. Cefadroxil was discontinued and the patient was treated successfully with intravenous nafcillin. The apparent failure of cefadroxil therapy can be explained by lower than recommended peak (greater than or equal to 1:8) and trough (greater than or equal to 1:2) titers for therapeutic success. Thus, an alternative dosage regimen of cefadroxil should be considered in the future studies.

Cefadroxil↗

PubMed1977

Comparative human oral clinical pharmacology of cefadroxil, cephalexin, and cephradine.

At equivalent oral doses, cefadroxil has a longer serum half-life, slower urinary excretion rate, greater area under the serum level versus time curve than cephalexin or cephradine, and peak serum concentrations that are 75 to 80% those of cephalexin. The calculated, apparent in vivo volume of distribution of cefadroxil is greater than that of cephalexin. These properties infer greater persistence of cefadroxil in serum and urine and more prolonged in vivo bacterial exposure to cefadroxil than to cephalexin or cephradine. Neither cefadroxil nor cephalexin demonstrates drug accumulation on repeated administration. The serum levels achieved by cefadroxil are unaffected by food. The pharmacokinetic properties of cefadroxil are supportive of the development of clinical efficacy data which could indicate that cefadroxil could be administered at 12-h intervals.

Adult↗

PubMed1989

Cefadroxil versus penicillin in the treatment of streptococcal tonsillopharyngitis.

In a randomized multicentre study the efficacy of phenoxymethyl-penicillin and cefadroxil was tested in the treatment of acute tonsillopharyngitis caused by group A streptococci. These organisms were detected in 269 of the 300 children studied. Of the 239 patients in whom results could be evaluated, 121 received penicillin and 118 cefadroxil. After ten days of therapy the microbiological failure rate was 19% in the penicillin group and 6.8% in the cefadroxil group (p less than 0.01). Ten of 23 cases of microbiological failure in the penicillin group and two of eight in the cefadroxil group also had clinical symptoms of infection. All streptococcal isolates were sensitive to penicillin, cefadroxil and clindamycin with the exception of one strain with intermediate sensitivity to cefadroxil. Seven strains had intermediate sensitivity to erythromycin and one was resistant. No penicillin tolerance was observed. Patients in whom penicillin therapy failed more frequently had beta-lactamase producing staphylococci in the pharyngeal flora in comparison to successfully treated patients. The clinical and bacteriological results showed that cefadroxil was clearly superior to penicillin.

Adolescent↗

PubMed1986

Therapeutic efficacy of cefadroxil and cephalexin for pneumonia in a rat test model.

The therapeutic efficacies of cefadroxil and cephalexin were compared in a Streptococcus pyogenes-induced lung infection in rats. Although MICs, rates of in vitro killing in rat serum, and antibiotic serum levels after oral administration were similar for both drugs, cefadroxil was about eight times more effective than cephalexin in reducing the number of viable streptococci at the site of infection. This excellent in vivo bactericidal activity of cefadroxil in lung tissue and bronchial secretions was reflected in the 50% protective dose (PD50) after single or multiple oral treatments. A single treatment given 24 h after infection resulted in a PD50 of 2.8 mg of cefadroxil per kg, compared with 21 mg of cephalexin per kg. When treatment was administered three times, at 24, 27, and 30 h postinfection, the PD50s of cefadroxil and cephalexin were 0.7 and 8.0 mg/kg, respectively. In infected animals, treated 24 h postinfection, the area under the lung tissue concentration versus time curve for cefadroxil was significantly greater than that of cephalexin. This difference in pharmacokinetic behavior may account, at least in part, for the superior therapeutic results obtained with cefadroxil in this experimental pulmonary infection.

Animals↗

PubMed1977

Comparison of pharmacological and antimicrobial properties of cefadroxil and cephalexin.

Pharmacological and antimicrobial properties of cefadroxil, a new cephalosporin antibiotic, were compared with cephalexin. Absorption and excretion were studied in 20 healthy men. Peak concentrations of the drugs in serum were similar after ingestion of single 500-mg tablets. The concentration of cefadroxil in serum was more sustained than that of cephalexin. Levels of cefadroxil in serum after a dose of 1,000 mg were approximately twice those after a 500-mg dose through 6 h. Each drug administered in a dose of 500 mg every 6 h for 24 h resulted in concentrations in serum that were similar to a single dose without accumulation. Ninety-three percent of the cefadroxil and 85% of the cephalexin were excreted in urine after ingestions of single 500-mg tablets. The urine concentration of cefadroxil was more sustained than cephalexin. Minimal inhibitory and minimal bactericidal concentrations for clinical isolates were comparable with each drug. Cefadroxil compares favorably with cephalexin in this study. Sustained levels of cefadroxil in serum and urine suggest that this drug may be given at less frequent intervals than cephalexin.

Adult↗

PubMed1991

Synthesis and antimicrobial activities of some new tetrahydro-2H-1,3,5-thiadiazine-2-thione derivatives of cefadroxil.

Eleven new 7-[2-(dihydro-5-substituted-6-thioxo-2H-1,3,5-thiadiazine-3( 4H)-yl)-2- (4-hydroxyphenyl)acetamido]-3-methyl-3-cephem-4-carboxylic acid derivatives were synthesized by the reaction of cefadroxil monohydrate, formaldehyde and substituted potassium dithiocarbamate. Their structures have been elucidated by spectral data and elementary analysis. The title compounds were tested for antimicrobial activity in vitro against gram-positive bacteria (Staphylococcus aureus, Streptococcus faecalis), gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and yeast-like fungi (Candida albicans, C. parapsilosis, C. stellatoidea, C. pseudotropicalis) in comparison with cefadroxil monohydrate. The activity of compounds 1 and 10 against S. aureus (MBC: 37.5 micrograms/ml) and compound 1 against E. coli (MBC: 75 micrograms/ml) were found to be the same as cefadroxil monohydrate. Compounds 1 and 10 were more effective than cefadroxil monohydrate against S. faecalis with 25 and 37.5 micrograms/ml MBC values, respectively. None of the compounds and cefadroxil monohydrate proved to be effective against P. aeruginosa (MBC: greater than 100 micrograms/ml). While cefadroxil monohydrate had no activity against yeast-like fungi, compounds 9 and 10 were significantly effective against yeast-like fungi (MFC: 37.5 micrograms/ml).

Anti-Bacterial Agents↗

PubMedDate not supplied

A pharmacokinetic comparison of cephalexin and cefadroxil using HPLC assay procedures.

The pharmacokinetics of cephalexin and cefadroxil were compared following single 500 mg oral doses to 12 healthy male volunteers. Doses were administered after an overnight fast according to a crossover design. Plasma and urinary levels of both compounds were determined by HPLC procedures. Cephalexin was absorbed rapidly, achieving a mean peak plasma level of 17.5 micrograms ml-1 at 1 h, compared to 16 micrograms ml-1 at 1.8 h for cefadroxil. Elimination half-lives of cephalexin and cefadroxil were 0.7 and 1.1 h, respectively. The area under the cefadroxil plasma curve was significantly larger than that for cephalexin. However, after allowing for differences in elimination rate constants and assuming equal distribution volumes, plasma data indicated the compounds were equally well absorbed. Only 70 per cent of cefadroxil was recovered in urine compared to 87 per cent of cephalexin during the 12 h following drug administration. The therapeutic significance of the different pharmacokinetic characteristics of cephalexin and cefadroxil, if any, may be a function also of their pharmacologic activity and/or the sensitivity of the target organism.

Adult↗

PubMed1985

Cefadroxil in the horse: pharmacokinetics and in vitro antibacterial activity.

Sodium cefadroxil was administered as a single intravenous dose (25 mg/kg) to six healthy adult mares. Plasma samples were collected over a 24-h period and cefadroxil concentrations were measured by microbiological assay. The pharmacokinetic behavior of the drug was appropriately described in terms of a one-compartment open model. Values for the major pharmacokinetic terms were: extrapolated initial plasma concentration = 59.2 +/- 15.0 micrograms/ml; half-life = 46 +/- 20 min; apparent volume of distribution = 462 +/- 191 ml/kg; and body clearance = 7.0 +/- 0.6 ml/min.kg. In a subsequent study, a suspension of cefadroxil monohydrate was administered intragastrically (25 mg/kg) to the same six horses. Plasma concentrations of the drug peaked at 1-2 h but, in general, absorption was both poor and inconsistent. The data were unsuitable for determination of cefadroxil bioavailability from this oral dosage form. Ninety-nine isolates of eleven bacterial species obtained from clinically ill horses were tested for susceptibility to cefadroxil. All strains of Streptococcus equi, Streptococcus zooepidemicus, coagulase-positive staphylococci, Corynebacterium pseudotuberculosis and five out of six strains of Actinobacillus suis were highly susceptible to the drug (MIC less than 4 micrograms/ml). Escherichia coli, Klebsiella pneumoniae and Salmonella sp. showed intermediate susceptibility (MIC 4-16 micrograms/ml), while all isolates of Corynebacterium (Rhodococcus) equi, Enterobacter cloacae and Pseudomonas aeruginosa proved to be highly resistant to cefadroxil (MIC greater than 128 micrograms/ml).

Animals↗

PubMed1992

Evaluation of cefuroxime axetil and cefadroxil suspensions for treatment of pediatric skin infections.

A randomized, single-blind, multicenter study was conducted to evaluate the safety and efficacy of cefuroxime axetil and cefadroxil suspensions for the treatment of skin or skin structure infections in 287 children. Each drug was given at a dosage of 30 mg/kg of body weight per day in two divided doses. Staphylococcus aureus and Streptococcus pyogenes, or a combination of the two, were the primary pathogens isolated from infected skin lesions. A satisfactory bacteriological response (cure or presumed cure) was obtained in 97.1 and 94.3% of children in the cefuroxime axetil and cefadroxil groups, respectively (P greater than 0.05). Satisfactory clinical responses (cure or improvement) were more likely to occur in cefuroxime axetil recipients than in cefadroxil recipients (97.8 versus 90.3%; P less than 0.05). Both regimens were equally well tolerated, with adverse events occurring in 7.9 and 6.1% of cefuroxime axetil and cefadroxil recipients, respectively. There were more patients who refused to take cefuroxime axetil (7 of 189) than there were who refused to take cefadroxil (0 of 98), but the difference was not statistically significant (P = 0.1). In this study, cefuroxime axetil was at least as effective as cefadroxil in resolving skin and skin structure infections in children.

Cefadroxil↗

PubMed1988

Clinical comparison of once-daily cefadroxil and thrice-daily cefaclor in the treatment of streptococcal pharyngitis.

The efficacy of cefadroxil once daily and cefaclor given 3 times daily was compared in 250 pediatric patients with group A beta-hemolytic streptococcal pharyngitis. The duration of the therapy was 10 days. Therapeutic response was based on clinical responses at 24 h and 10 days and throat cultures on days 14, and 21 or 28. Five (5%) cefadroxil-treated patients and 12 (12%) cefaclor-treated patients were still culture-positive on day 14. When the patients were stratified according to major differences between treatment groups observed at baseline, a significant difference between the treatment groups in favor of cefadroxil was found on day 14 (p = 0.020) and days 21-28 (p = 0.043). These data were confirmed by the clinical findings; failure or clinical recurrence occurred in 4.6% of cefadroxil-treated patients versus 22.1% of cefaclor-treated patients. The patients complied with the recommended drug regimen, and none experienced any significant drug-related adverse reactions. The results of this study indicate that cefadroxil given once daily for streptococcal pharyngitis is an effective and well-tolerated antimicrobial agent, and suggest that the desirable pharmacokinetic properties of cefadroxil contribute to this efficacy.

Administration, Oral↗

PubMed1978

Clinical experience with cefadroxil in upper and lower respiratory tract infections.

Cefadroxil is a new semisynthetic oral cephalosporin with a broad spectrum of activity against both Gram-positive and Gram-negative organisms. Absorption of cefadroxil is unaffected by food, its serum levels are prolonged and it is excreted in the urine at a relatively slow rate compared to cephalexin. In the treatment of 108 patient with upper or lower respiratory tract infections, cefadroxil effected 93% complete cures. Fifty-five of the patients had upper respiratory tract infections and fifty-three had lower respiratory tract infections; among them cefadroxil acheived clinical success rates of 100% and 96%, respectively. Cefadroxil was clinically successful in eight (89%) out of nine patients whose infections were caused by mixed aetiologies. The principal causative agents were Staphylococcus aureus, beta-haemolytic streptococci, Streptococcus pneumoniae and Klebsiella pneumoniae. Overall bacterial eradication produced by cefadroxil was 112 (91%) of 123 organisms isolated from 108 patients. Reports of mild and transient side-effects in only 3.7% of the patients showed that the drug was well tolerated.

Adolescent↗

PubMed1990

Randomised double-blind study of norfloxacin and cefadroxil in the treatment of acute pyelonephritis.

In a coordinated, double-blind multi-centre trial, adults with symptoms of acute pyelonephritis were randomly assigned to receive a two-week course of oral treatment with either 400 mg norfloxacin twice daily or 1 g cefadroxil twice daily. Of 197 patients enrolled in the study, 140 could be evaluated for drug efficacy and 193 for drug safety. Norfloxacin gave a significantly higher bacteriological cure rate than cefadroxil, both at 3 to 10 days (98% versus 65%; p less than 0.0001; 95% confidence interval (CI) for difference in proportions 21-46%) and up to eight weeks (87% versus 48%; p less than 0.0001; 95% CI 25-54%) after cessation of treatment. The differences between the two regimens were most pronounced in men and in patients with complicating factors such as diabetes mellitus and urinary tract abnormalities. The clinical response during treatment did not differ between the two groups, but symptomatic recurrences at follow-up were more common in the cefadroxil group (28% versus 3%; p less than 0.0001; 95% CI 14-36%). Adverse events were more often reported by patients receiving cefadroxil (39% versus 22%; p = 0.011; 95% CI 4-30%) and consisted mainly of gastrointestinal disturbances and vulvo-vaginitis. In terms of bacteriological and clinical efficacy and safety, a two-week course of norfloxacin was superior to a two-week course of cefadroxil for oral treatment of community-acquired acute pyelonephritis.

Acute Disease↗

PubMed1985

Transport of cefadroxil, an aminocephalosporin antibiotic, across the small intestinal brush border membrane.

The transport characteristics of cefadroxil, an aminocephalosporin antibiotic, across the brush border membrane of rat small intestine were investigated by a rapid filtration technique. The uptake of cefadroxil was not affected by Na+ gradient, suggesting the absence of a cotransport system between cefadroxil and Na+ in the brush border membrane. The uptake was slightly inhibited by HgCl2 pretreatment and stimulated by the countertransport effect, where cyclacillin played a role as an elicitor. These results suggest the existence of a carrier-mediated transport system for cefadroxil in the brush border membrane, which is shared with cyclacillin. Papain treatment increased the specific transport activities for the antibiotic. This may be the first step of purification of the cefadroxil transport carrier.

Animals↗