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PubMedDate not supplied

Nonlinear pharmacokinetics of cefadroxil in the rat.

The pharmacokinetics and bioavailability of cefadroxil in the rat were examined after intravenous and oral administration at three doses (2.5, 10, and 15 mg). Cefadroxil disposition kinetics was clearly nonlinear, with an increase in plasma clearance as the dose increased (2.65 +/- 0.55, 3.17 +/- 0.48, and 3.82 +/- 0.39 ml/min for the three doses assayed). This phenomenon was attributed to a saturable renal tubular reabsorption of the antibiotic. After oral administration, the normalized Cmax was lower for the largest dose (4.6 +/- 0.7 micrograms/ml) than for the other two doses (5.5 +/- 0.5 and 5.4 +/- 0.7 micrograms/ml). Renal excretion of cefadroxil in the rat after intravenous and oral administration was investigated at two level doses (2.5 and 15 mg). No significant differences were found between doses or administration routes, and the mean percentage of dose recovered in the urine for the intravenous and oral routes was 80.7 +/- 6.1% and 76.4 +/- 3.7%, respectively. Cefadroxil bioavailability estimated from plasma levels or from the amounts of drug excreted in the urine was high and ranged from 90% to 100%.

Administration, Oral↗
PubMed1993

Pharmacokinetic and bacteriological study of cefadroxil-salicylate and josamycin-salicylate drug regimens.

Eye, nose, throat and bronchopulmonary infections are frequently associated with inflammatory symptoms. This often leads the clinician to prescribe a combination of an anti-inflammatory and an antibiotic. Cefadroxil and josamycin are among the antibiotics most frequently used in these infections, and they are often combined with acetylsalicylic acid in various pharmaceutical formulations. The study of possible pharmacokinetic and bacteriological interactions was performed in healthy volunteers who received in a crossover protocol each of the two antibiotics, either alone or combined with acetylsalicylic acid or lysine acetylsalicylate. No marked pharmacokinetic interaction was noted except an increase in the AUC for plasma concentrations of cefadroxil when combined with a salicylate. A greater uniformity of kinetic profiles was seen with cefadroxil than with josamycin. Lastly, with the exception of one strain, the salicylates did not alter the antibacterial activity of cefadroxil.

Adult↗
PubMed1979

Cefadroxil kinetics in patients with renal insufficiency.

Kinetic parameters and bioavailability of cefadroxil were studied in 20 subjects with differing renal function as measured by endogenous creatinine clearance (CCr). Two subjects were on hemodialysis. After an overnight fast, each subject ingested two 500-mg capsules of cefadroxil. The peak serum concentration was variable (12 to 57 mg/L) and correlated inversely with the CCr. All but one patient had maximum absorption within 4 hr of ingestion and in most patients the peak was reached within the 2-hr sample. Urinary recovery within 48 hr was 45% to 106% when CCr greater than 8 ml/min. Even in patients with the most severe renal failure (CCr less than 10 ml/min), urine concentrations of cefadroxil were adequate to treat susceptible bacteria. The rate of oral absorption ka, was not affected by the state of renal function and was 0.76 +/- 0.50 hr-1. The apparent distribution volume (V d ext) was 0.28 +/- 0.09 L/kg. The plasma elimination rate was dependent on CCr wih a small fraction of drug being removed by nonrenal routes. Except in advanced renal failure, tubular secretion was present since renal clearance of cefadroxil exceeded CCr. The data suggest that little drug accumulation will occur with the usual 8- to 12-hr dosing schedule except when the CCr is less than 25 ml/min.

Adult↗
PubMed1978

Clinical comparison of cefadroxil, new oral cephalosporin, and cephalexin in uncomplicated urinary tract infection.

Efficacy and safety of cefadroxil, a new oral cephalosporin, were compared with that of cephalexin in the treatment of 28 women with acute urinary tract infections. According to a randomized double-blind design, each patient received cefadroxil 1,000 mg. twice daily or cephalexin 500 mg. four times a day for ten days. Cures based on urine culture five to nine days post-treatment were obtained for all but 1 patient receiving cefadroxil; reinfection after eradication of the original pathogen was recorded for only 1 patient in each treatment group. No drug-related side effects or significant clinical laboratory abnormalities were observed during the study. Cefadroxil 1,000 mg. given twice daily was as effective and as well tolerated as cephalexin 500 mg. given four times daily. The significance of this dosage schedule advantage is discussed.

Administration, Oral↗
PubMed1978

Clinical pharmacology of cefadroxil in infants and children.

The pharmacokinetics of cefadroxil suspension were studied in 30 children, 13 months to 12 years of age (mean age, 5.7 years). Average peak concentrations in serum of 11 to 14 mug/ml and of 7 to 10 mug/ml after 15- and 10-mg/kg doses, respectively, were not substantially affected by the feeding status. The serum half-life values were 1.3 to 1.5 h. Cefadroxil was detected in saliva of all children 2 h after 15-mg/kg doses: the levels ranged from 0.17 to 2.6 mug/ml (mean, 0.46 mug/ml). The average concentrations in urine were 1,700 and 2,620 mug/ml at 0 to 2 and 2 to 4 h, respectively, after 15-mg/kg doses. In a randomized controlled study of 50 children with impetigo, cefadroxil was as effective as penicillin G in curing existing lesions and in preventing development of new lesions. Cefadroxil may be useful for therapy of mucocutaneous and urinary tract infections in infants and children.

Biological Availability↗
PubMed1979

Comparative pharmacokinetics of cephalexin, cefaclor, cefadroxil, and CGP 9000.

In a randomized crossover study, the pharmacokinetics of three new cephalosporin antibiotics, cefaclor, cefadroxil, and CGP 9000, in comparison to cephalexin, were determined after oral administration, by capsules, of 1,000 mg on an empty stomach in 12 normal subjects. Serum concentrations were measured during a period of 8 h, and urine recovery was measured during 24 h. The significant parameters of bioavailability of an orally administered substance were determined. The maximal serum concentrations (y(max)) for cephalexin, cefaclor, cefadroxil, and CGP 9000 (in milligrams per liter) were: 38.8 +/- 8.1; 34.6 +/- 7.8; 33.0 +/- 5.4; and 23.3 +/- 7.3, respectively. The areas under the curve (in hours x milligrams per liter) were: 93.0 +/- 14.8; 74.5 +/- 9.9; 70.1 +/- 9.0; and 108.5 +/- 18.4, respectively. In a further crossover study with six subjects, 1,000 mg of cephalexin and of cefadroxil were given during a standard breakfast. The y(max) of cephalexin decreased to 23.1 +/- 6.6 mg/liter, in contrast to cefadroxil, with an unchanged y(max) of 32.7 +/- 3.4 mg/liter.

Administration, Oral↗
PubMed1978

An overview of results of world-wide clinical trials with cefadroxil.

Céfadroxil, a new semisynthetic oral cephalosporin, is absorbed similarly by fasted and non-fasted subjects, produces sustained serum levels and is eliminated at a relatively slow rate. These pharmacokinetic properties permit less frequent and more convenient dosage scheduling than cephalexin and cephradine and consequently greater patient compliance. Cefadroxil was evaluated for safety in 1051 patients and for efficacy in 1030 patients. Overall it achieved a 91.8% rate of clinical success resulting from 881 complete cures and sixty-five clinical cures. Among 363 patients with respiratory tract infections and 471 patients with genito-urinary tract infections, cefadroxil treatment produced 97.5% and 84.5% clinical success, respectively. In the remaining infectious diseases treated, cefadroxil therapy resulted in 99.0% clinical success. Cefadroxil eradicated 87% of 1110 pathogens isolated, among which the most predominant pathogens were Staphylococcus aureus, beta-haemolytic streptococci, Streptococcus pneumoniae, Escherichia coli and Proteus mirabilis. Drug-related side-effects were reported in 7.2% of the patients.

Adolescent↗
PubMed2000

Comparative bioavailability of two cefadroxil formulations in healthy human volunteers after a single-dose administration.

OBJECTIVE: To compare the bioavailability of two cefadroxil capsule (500 mg) formulations (Cefadroxila from Eurofarma Laboratórios Ltd, Brazil, as test formulation and Cefamox from Bristol-Myers Squibb, Brazil S.A. as reference formulation) in 24 volunteers of both sexes. MATERIAL AND METHODS: The study was conducted open with randomized two-period crossover design and a 1-week washout period. Plasma samples were obtained over a 12-h interval. Cefadroxil concentrations were analysed by combined reversed-phase liquid chromatography and tandem mass spectrometry (LC-MS-MS) with positive ion electrospray ionization using a selected ion monitoring method. From the cefadroxil plasma concentration versus time curves the following pharmacokinetic parameters were obtained: AUC(last), AUC(0-infinity) and C(max). RESULTS: Geometric mean of Cefadroxila/Cefamox 500 mg individual percent ratio was 103.97% for AUC(last), 104.08% for AUC(0-infinity) and 95.23% for C(max). The 90% confidence intervals (CI) were 98.14-110.16%, 98.37-110.12%, and 85.59-105.96%, respectively. CONCLUSION: Since the 90% CI for C(max), AUC(last) and AUC(0-infinity) were within the 80-125% interval proposed by the Food and Drug Administration, it was concluded that the Cefadroxila 500 mg capsule was bioequivalent to the Cefamox 500 mg capsule, according to both the rate and extent of absorption.

Adolescent↗
PubMedDate not supplied

Comparative effects of cefadroxil and phenoxymethylpenicillin on the normal oropharyngeal and intestinal microflora.

The ecological effects on the commensal microflora in saliva and stool samples were studied during administration of two commonly used antibiotics: cefadroxil 500 mg b.i.d. for 10 days and phenoxymethylpenicillin 1 g b.i.d. for 10 days. Twenty healthy volunteers participated in the study. In the oropharyngeal microflora the aerobic microflora was significantly suppressed during administration of cefadroxil while no significant changes were noticed in the anaerobic microflora. Administration of phenoxymethylpenicillin caused a strong decrease in the number of viridans streptococci and an overgrowth of Neisseria cocci. The total numbers of anaerobic oropharyngeal microorganisms were suppressed during phenoxymethylpenicillin administration. In the intestinal microflora the variation in numbers of aerobic and anaerobic microorganisms was minor in both groups. The microflora became normalised 2 weeks after withdrawal of the drugs. It was concluded that peroral administration of cefadroxil to healthy volunteers resulted in minor ecological disturbances in the oropharyngeal and intestinal microflora, which were in the same range as for phenoxymethylpenicillin.

Adult↗
PubMed1991

Double-blind randomized study of oral temafloxacin and cefadroxil in patients with mild to moderately severe bacterial skin infections.

A randomized, double-blind, multicenter study was conducted in 374 patients to evaluate the safety and efficacy of a 7-10-day regimen of oral temafloxacin (600 mg b.i.d.) or oral cefadroxil (500 mg b.i.d.) in the treatment of mild to moderate staphylococcal or streptococcal infection of the skin or skin structure. Specimens from the infected skin lesion were obtained for culture. A dermatologic assessment was made within 48 hours of starting therapy, 0-48 hours post-treatment, and once during the 5-9 days following the last dose of study drug. The most common diagnoses were abscess, superficial skin infection, cellulitis, and infection of the hair follicle/sweat gland. Clinical response rates exceeded 95% in both the temafloxacin and cefadroxil groups. A higher bacterial eradication rate was demonstrated in the temafloxacin-treated patients (91%) than in those receiving cefadroxil (84%). This was statistically significant in the subset of infections caused by Staphylococcus epidermidis (100% versus 81%, respectively; p = 0.032). Both regimens were well tolerated. These results indicate that temafloxacin is useful in the treatment of mild to moderate skin and skin structure infections caused by staphylococci or streptococci.

Adolescent↗
PubMed2006

Chiral separation of cefadroxil by capillary electrochromatography.

In this paper, the chiral separation of cefadroxil was studied by capillary electrochromatography. Monolithic capillary column was prepared for the separation of cefadroxil enantiomers. The optimum buffer contained 28.5 mmol/L sodium acetate, 0.95% (v/v) acetic acid, 19 mmol/L beta-cyclodextrin (beta-CD) and 5% (v/v) isopropanol in formamide solution (pH 7.0), with the running voltage of 12 kV, the UV detector wavelength of 254 nm, the sample injected time of 8s and the temperature of 25 degrees C. Under these conditions, the column efficiency of cefadroxil enantiomers were N1=5324 and N2=23,768 with a selectivity factor (alpha) of 1.056 and resolution (Rs) of 0.978. The effect of buffer pH value, beta-CD concentration, organic modifier (isopropanol) concentration and voltage was also investigated for the separation by CEC.

Anti-Bacterial Agents↗
PubMed2000

Clathration-induced asymmetric transformation of cefadroxil.

[structure: see text] The cephalosporin antibiotic Cefadroxil can be epimerized at the alpha-carbon of its amino acid side chain using pyridoxal as the mediator. By clathration with 2,7-dihydroxynaphthalene, the desired diastereomer can be selectively withdrawn from the equilibrating mixture of epimers. In this way, an asymmetric transformation of Cefadroxil can be accomplished. This opens the possibility of the production of Cefadroxil starting from racemic p-hydroxyphenylglycine, in contrast to the current industrial synthesis that employs the D-amino acid in enantiopure form.

Cefadroxil↗
PubMed2002

PepT1 mRNA expression is induced by starvation and its level correlates with absorptive transport of cefadroxil longitudinally in the rat intestine.

PURPOSE: To establish how closely intestinal transport activity for beta-lactam antibiotics is correlated with PepT1 expression, absolute expression level of PepT1 mRNA and transport activity were determined longitudinally in the small intestine of fed and starved rats. METHODS: For evaluation of absolute expression levels of PepTl mRNA, quantitative RT-PCR by LightCycler was used. The transport function was determined by quantifying the absorptive transport of cefadroxil across intestinal tissue sheets in a Ussing chamber. RESULTS: PepT1 mRNA expression was highest at the lower region and lowest at the upper region in the fed rats. The value of PepT1 was about 1/5-1/6 of that of GAPDH. The expression level in the starved rats was increased in all segments, but more profoundly in the upper region. Cefadroxil transport across intestinal tissue was higher in the lower region and lower in the upper region in fed rats, and increased in the upper region in starved rats. An excellent correlation was observed between expression levels and the permeability coefficients (r2 = 0.859, p < 0.05). CONCLUSIONS: The intestinal transport of cefadroxil is directly proportional to PepT1 expression, suggesting that the PepT1 expression level in the rat small intestine is the major determinant of the absorption of peptide-like compounds.

Animals↗
PubMed1987

The in-vitro activity of cefadroxil, and the interpretation of disc-susceptibility testing.

Minimum inhibitory concentrations (MICs) of cefadroxil were determined for 749 defined clinically-significant bacteria isolated in a London teaching hospital and for 63 strains from an international collection of Gram-negative bacilli. Assuming a breakpoint of 16 mg/l, for the hospital isolates 81.8% of Gram-negative bacilli and 83.4% of Gram-positive cocci were sensitive. No significant difference between in-patient, out-patient or community-acquired isolates was found. Ninety-five and a half per cent of Escherichia coli, Klebsiella aerogenes (including gentamicin-resistant strains), Proteus mirabilis, and (with the exception of Streptococcus faecalis and methicillin-resistant Staphylococcus aureus) all Gram-positive cocci were sensitive. Of 41 strains of Enterobacter spp., were resistant. Most indole-positive Proteus, and all Serratia and Acinetobacter spp. were resistant, including 36 additional strains taken from an international collection. Of 30 strains of Haemophilus influenzae, only six had MICs of 16 mg/l or less. For disc susceptibility testing, the standard disc containing 30 micrograms of cefadroxil reliably gave zones of greater than 17 mm for organisms with MICs of less than 16 mg/l. A zone of less than 14 mm corresponded to MICs of greater than 64 mg/l. Despite a lack of controlled clinical trials, the results of this study (taken with favourable pharmacokinetics) suggest that cefadroxil has potential as an oral cephalosporin in hospital practice in the U.K.

Cefadroxil↗
PubMed1990

In-vitro enhancement of leukotriene B4 receptor expression on human neutrophils by cefadroxil.

The influence of cefadroxil on LTB4-receptor expression of polymorphonuclear leucocytes (PMNs) was studied. Furthermore, the effect of cefadroxil on the leukotriene generation from PMNs and the lymphocyte, monocyte and basophil (LMB) containing cell fraction as well as on the synthesis of 12-hydroxyeicosatetraenoic acid (12-HETE) from human platelets was analysed. Antibiotic concentrations ranged from 50 to 5 micrograms/10(7) cells. Analysis of the generated leukotrienes was performed by high performance liquid chromatography (HPLC). Significant augmentation of the LTB4-receptor expression in human PMNs (range 190%-220%) was observed at concentrations of 50 and 25 micrograms/10(7) cells. The calcium-ionophore A23187 induced LTB4 generation from PMNs as well as 12-HETE synthesis from platelets was not significantly modulated in the presence of cefadroxil. Preincubation of the human LMB fraction led to slight suppression of the ionophore induced LTB4 generation up to 20%.

12-Hydroxy-5,8,10,14-eicosatetraenoic Acid↗
PubMed1992

Utility of mixture of commercially available polymers as constituents of sustained-release microcapsules containing cefadroxil or theophylline.

Hydroxy propyl methyl cellulose acetate succinate high grade (AS-HG) and ethyl cellulose (EC) mixture microcapsules containing cefadroxil or theophylline were prepared by a solvent evaporation method in liquid paraffin dissolved sorbitan tri-stearate as a dispersing agent, and their sustained-release properties were evaluated. The microcapsules prepared with AS-HG:EC (in a 2:5 weight ratio) mixture containing 20% of cefadroxil or theophylline exhibited apparent zero-order releasing pattern in pH 6 to 8, at 50 rpm and 37 degrees C (paddle method). These microcapsules were administered orally to beagle dogs and the plasma concentrations of cefadroxil or theophylline were measured periodically. As a result of in vivo investigation, a satisfactory sustained-release plasma pattern and an apparent zero-order process in the gastrointestinal absorption were confirmed by deconvolution analysis of both drugs.

Administration, Oral↗
PubMed2006

Determination of cefadroxil by sequential injection with spectrophotometric detector.

A sequential injection analysis (SIA) spectrophotometric procedure for cefadroxil determination has been developed. The SIA instrumentation was modified to achieve the desired function and operations by using the software developed to interface the PC with the conventional SIA system. The method is based on the measurement of a red, water-soluble product formed by the reaction between cefadroxil and 4-aminoantipyrine in the presence of alkaline potassium hexacyanoferrate(III) at 510 nm. Optimum conditions for determining the drug were investigated. Beer's law was obeyed over the concentration ranges of 1 - 10 mg L(-1) and 10 - 50 mg L(-1) with a detection limit (3 sigma) of 0.17 mg L(-1) and a limit of quantification (10 sigma) of 0.56 mg L(-1). The relative standard deviations of 1.98% and 1.93% for 5 mg L(-1) and 30 mg L(-1) of the drug, respectively (n = 11) are obtained. The proposed method has been applied satisfactorily to the determination of cefadroxil in commercial pharmaceutical formulations with a sampling rate of 100 h(-1). Results obtained were in good agreement with those obtained by the official HPLC method at the 95% confidence level.

Ampyrone↗
PubMed1986

Penetration and concentration of cefadroxil in sputum, lung and pleural fluid.

The penetrability of cefadroxil in sputum, pleural fluid and lung tissue was examined in patients with acute respiratory infections, or who were undergoing thoracic surgery. The concentration of antibiotic in these tissues after single doses of 500 mg or 1 g was approximately half of that seen in serum, but persisted longer. In all biological matter studied, the concentration of cefadroxil was sufficient to inhibit pathogens such as S. aureus, S. pneumoniae and S. pyogenes, shown to be common causes of respiratory illnesses. Thus, cefadroxil should be a useful agent in the treatment of such infections.

Adolescent↗