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PubMed1981

Disposition of cefadroxil administered orally to rabbits with experimentally induced renal impairment.

The pharmacokinetics of (6R,7R)-7-[(R)-2-amino-2-(p-hydroxyphenyl)-acetamido]-3-methyl-8-oxo-5-thia-1- azabicyclo-[4,2,0]-oct-2-ene-carbonic acid (cefadroxil) were studied in rabbits with normal renal function and with varying degrees of renal impairment induced experimentally by i.v. administration of uranyl nitrate at a dose of 4 mg/kg. All animals received a single oral dose of 50 mg/kg of cefadroxil. The serum, urinary and bile concentrations of the antibiotic were determined by a microbiological method. The antibiotic follows a single-compartment kinetic model. In rabbits with renal impairment a significant decrease in Ka and Ke occurred together with an increase in the values of tmax and (AUC)0 infinity, which are related to the serum creatinine concentrations, used as an index of the degree of renal function.

Animals↗
PubMed1980

[Therapeutical experience of cefadroxil against acute infectious diseases in the otorhinolaryngological field (author's transl)].

In the clinical studies on cefadroxil against acute infectious diseases in the otorhinolaryngological field, the following results were obtained: (1) In 10 cases of various infections, excellent was 2 cases and good was 8 cases, efficacy rate being 100%. (2) No side effects were observed subjectively, and no abnormal findings were demonstrated with laboratory tests. (3) Cefadroxil may be expected to be a highly effective and safe agent for the therapy of otorhinolaryngological infections.

Acute Disease↗
PubMedDate not supplied

Antibacterial activity of cefpodoxime in comparison with cefixime, cefdinir, cefetamet, ceftibuten, loracarbef, cefprozil, BAY 3522, cefuroxime, cefaclor and cefadroxil.

The new oral cephalosporins cefpodoxime, cefixime, cefdinir, cefetamet and ceftibuten demonstrate enhanced activity against Enterobacteriaceae susceptible to the established compounds as well (e.g. cefuroxime, cefaclor, cefadroxil). In addition, cefpodoxime, cefixime, cefdinir, cefetamet and ceftibuten include in their spectrum species hitherto resistant to oral cephalosporins (Proteus vulgaris, Providencia spp., Yersinia enterocolitica). Besides, the majority of these compounds demonstrate relevant activity (MIC50 equal to or below 2 mg/l) against Enterobacter spp., Citrobacter freundii, Serratia spp. and Morganella morganii. Ceftibuten is the most potent oral cephalosporin against most of the Enterobacteriaceae. Non-fermentative bacilli (Acinetobacter spp., Pseudomonas spp.) remain completely resistant to oral cephalosporins (except some Acinetobacter species against cefdinir and Pseudomonas cepacia against ceftibuten). Antistaphylococcal activity for oral cephalosporins is highest for cefdinir followed by BAY 3522, cefprozil, cefuroxime and cefpodoxime. Loracarbef, cefaclor and cefadroxil are about equally active, while the other compounds are only weakly active (cefixime) or inactive (cefetamet, ceftibuten). Enterococci are insensitive to new generation oral cephalosporins as they have been to established compounds. The most active oral cephalosporins against hemolytic streptococci are cefdinir and cefprozil. Streptococcus pneumoniae, Streptococcus milleri and Streptococcus mitior are most susceptible to cefpodoxime, cefdinir, cefuroxime and BAY 3522. Penicillin resistant pneumococci have to be regarded as resistant to all oral cephalosporins. Fastidious pathogens like Haemophilus spp., Moraxella catarrhalis and Neisseria gonorrhoeae are more susceptible to cefpodoxime, cefixime, cefdinir, cefetamet and ceftibuten than to the other oral cephalosporins. The activity of oral cephalosporins is only weak against Listeria spp., Helicobacter pylori and anaerobic pathogens (except BAY 3522). Bordetella pertussis remains resistant to all absorbable cephalosporins. Progress in antibacterial activity of oral cephalosporins was mainly achieved by cefpodoxime, cefixime, cefdinir, cefetamet and ceftibuten against Enterobacteriaceae and the fastidious pathogens and against staphylococci and the nonenterococcal streptococci by cefdinir, BAY 3522, cefprozil and cefpodoxime.

Bacteria↗
PubMed1980

Treatment of urinary infections with cefadroxil: controlled comparison of high-compliance oral dosage regimens.

The efficacy and tolerability of cefadroxil were assessed in a controlled comparison of high-compliance oral dosage regimens among 100 patients with urinary tract infections. Each patient was randomly assigned to one of three cefadroxil treatment groups: 2,000 mg. once daily, 1,000 mg. once daily, or 1,000 mg. twice daily. Urine cultures at five to nine days post-treatment revealed cures in 27 of 36 patients in the 2,000-mg. daily group, 32 of 36 patients in the 1,000-mg. daily group, and 27 of 28 patients taking 1,000 mg. twice daily. Recurrence rates were extremely low in all treatment groups, and only 3 patients had evidence of limited side effects. The benefits of a convenient and readily understood dosage schedule are discussed.

Administration, Oral↗
PubMedDate not supplied

Simultaneous liquid chromatographic analysis of the beta-lactam antibiotics cefazolin, cefadroxil, cephalexin, ampicillin, and cephradine in solution.

A liquid chromatographic method was developed for the determination of nanogram quantities of 5 broad-spectrum structurally related beta-lactam antibiotics (cefazolin, cefadroxil, cephalexin, cephradine, and ampicillin) in solution. The method uses a C18 reversed-phase column, UV absorption (240 nm) detection, and an aqueous mobile phase containing isopropyl alcohol and acetic acid. Relative resolution between the antibiotic peaks ranged from 1.7 to 5.9 for all peaks. Chromatographic retention times were 2.97, 3.92, 4.57, 5.37, and 6.56 min for cefazolin, cefadroxil, cephalexin, ampicillin, and cephradine, respectively. Accuracy, precision, linearity, and long term analytical reproducibility were determined by statistical analysis. Use of the proposed method to evaluate the degradation of cephradine solutions stored at room temperature illustrated its potential as a stability-indicating assay.

Anti-Bacterial Agents↗
PubMed1991

Effects of ethanol on the pharmacokinetics of cephalexin and cefadroxil in the rat.

Data are presented on the effect of ethanol on the intestinal absorption and excretion in rats of two beta-lactam antibiotics, cephalexin (CFX) and cefadroxil (CFD). A recirculating perfusion technique within an antibiotic concentration range of 0.5 to 50 mM was used. Ethanol was administered either in an acute form into the intestine or in a chronic form as a 15% drinking solution for 2 months. The results are normalized in relation to the metabolic body weight, intestinal length, and osmotic conditions. Acute ethanol treatment decreases the antibiotic absorption; biliary excretion of CFD is increased, while urinary excretion of CFX is lowered. Chronic treatment shows slight negative effects on the absorption of CFX and CFD. Results are interpreted on the basis of the effect of ethanol on biological membranes. Enhanced urinary excretion after acute ethanol treatment, as well as differences between transport mechanisms, are invoked to explain these effects.

Administration, Oral↗
PubMed1980

Influence of dose on the pharmacokinetics of cefadroxil.

The pharmacokinetics of Cefadroxil have been studied in a crossover study involving 20 experiments in four healthy volunteers (19--24 years), after oral administration of five individual doses of 250, 500, 750, 1000 and 1500 mg of the antibiotic in capsules to each person. Plasma and urine concentrations of the antibiotic were determined microbiologically by a plate diffusion method. The antibiotic followed an open, single-compartment kinetic model. The plasma half-life was not significantly influenced by dose; the average was 1.438 +/- 0.220 h. The percentage of the antibiotic excreted in urine, too, was not significantly affected by the dose, being close to 80% of the quantity originally administered within 24 h. The values of Cmax and (AUC) increased linearly with the administered dose.

Cefadroxil↗
PubMed1994

Automated column liquid chromatographic determination of amoxicillin and cefadroxil in bovine serum and muscle tissue using on-line dialysis for sample preparation.

A fully automated method is described for the determination of amoxicillin and cefadroxil in bovine serum and muscle tissue. The method is based on the on-line combination of dialysis and solid-phase extraction for sample preparation, and column liquid chromatography with ultraviolet detection. In order to enhance the UV detectability of the analytes, post-column addition of 0.1 M sodium hydroxide is performed. The method shows good linearity and repeatability for both analytes in serum as well as in muscle tissue; the limits of detection in these samples are 0.05 microgram/ml and 0.2 microgram/g, respectively. The method has a sample throughput of 30 samples per 24 h.

Amoxicillin↗
PubMed2004

Synthesis, characterization and electronic spectra of cefadroxil complexes of d-block elements.

Cefadroxil (CD) is an essential pharmaceutical drug used in curing many diseases. Due to its popular use in many pharmaceutical forms, attention is paid in this research to the synthesis and stereochemistry of new iron, cobalt, nickel, copper, and zinc complexes of this drug both in solution and the solid states. The spectra of these complexes in solution and the study of their stoichiometry refer to the formation of 1:1 and 1:2 ratios of metal (M) to ligand (L). The calculated stability constants (Kf) of these complexes (1.5x10(7) to 5x10(13)) and the change in free energy of formation (deltaGf=2.5-12.5 kcal mol(-1) degree(-1)) are indicative of their high stability. The stereo chemical structure of the solid complexes was studied on the basis of their analytical, spectroscopic, magnetic, and thermal data. Infrared spectra proved the presence of M-N and M-O bonds. Magnetic susceptibility and solid reflectance spectral measurements were used to infer the structure. The prepared complexes were found to have the general formulae [ML(OH)x(H2O)y](H2O)z-M: Fe(II), x=0, y=2, z=1; M: Fe(III) and Co(III), x=1, y=2, z=1; M: Co(II) and Zn(II), x=0, y=1, z=0; M: Ni(II) and Cu(II), x=1, y=0, z=1; L: CD. Octahedral and tetrahedral structures were proposed for these complexes depending upon the magnetic and reflectance data and were confirmed by detailed mass and thermal analyses comparative studies.

Anti-Bacterial Agents↗
PubMed2000

Study on electrooxidation of cefadroxil monohydrate and its determination by differential pulse voltammetry.

In this work electrooxidation of cefadroxil monohydrate was investigated using a glassy carbon electrode depending on pH and supporting electrolyte. It was shown that the direct determination of the substance from capsules and in oral suspension could be made by differential pulse voltammetry (DPV). UV and first derivative UV spectrophotometric methods are also proposed as comparative methods.

Cefadroxil↗
PubMed2001

In-vitro release kinetics of cefadroxil-loaded sodium alginate interpenetrating network beads.

This paper reports the development of new interpenetrating polymeric networks of sodium alginate with gelatin or egg albumin cross-linked with a common cross-linking agent, glutaraldehyde, for the in-vitro release of cefadroxil. The beads formed were characterized by Fourier transform infra-red spectroscopy, scanning electron microscopy and differential scanning calorimetry. Swelling/drying experiments were performed to compute the diffusion coefficients and the molecular mass between cross-links of the beads. The release results were evaluated using an empirical equation to understand the transport mechanism. The extent of cross-linking was studied in terms of the size and release characteristics of the beads. The experimental and derived quantities have been used to study their dependencies on the nature of the polymeric beads, transport mechanism, encapsulation efficiency and drug diffusion, as well as the cross-linking abilities of the polymers.

Albumins↗
PubMed1991

Determination of cefsulodin, cefmenoxime, and cefadroxil as residues on surfaces.

Cefsulodin, cefmenoxime, and cefadroxil are degraded instantaneously in aqueous sodium hypochlorite, sodium hypochlorite-detergent, or alkaline detergent solutions. These alkaline solutions are used to clean surfaces that have been exposed to the cephalosporins. The cleaned surfaces are monitored for residual drug levels (microgram) using a wet swab-dry swab technique. After extraction from the swabs, the content of the respective cephalosporin is determined in the solution by high-performance liquid chromatography. The limit of detection for each of the compounds is 0.1 microgram/ml. Recoveries from nonporous surfaces ranged from 56 to 102%.

Cefadroxil↗
PubMed1989

Spectrophotometric determination of certain cephalosporins using molybdophosphoric acid. Part II. Determination of cefadroxil, cefapirin, ceforanide and cefuroxime.

The use of molybdophosphoric acid as an oxidising agent for the spectrophotometric determination of four cephalosporin derivatives, viz., cefadroxil monohydrate (I), cefapirin sodium (II), ceforanide L-lysine (III) and cefuroxime sodium (IV), either in the pure form or in pharmaceutical formulations is described. Beer's law is obeyed up to 100 micrograms ml-1 for I, up to 60 micrograms ml-1 for II and IV and up to 80 micrograms ml-1 for III. The molar absorptivities were 4.58 X 10(3), 11.3 X 10(3), 9.8 X 10(3) and 10.9 X 10(3) l mol-1 cm-1 and the Sandell sensitivities were 83.3, 39.3, 53.0 and 41.0 ng cm-2 for I, II, III and IV, respectively. The slopes and intercepts of the equations of the regression line were calculated for each of these drugs with the following correlation coefficients: I, 0.9993; II, 0.9999; III, 1.000; and IV, 0.9999. These antibiotics were determined successfully both in the pure form and in pharmaceutical preparations. The results demonstrated that the proposed procedure is at least as accurate, precise and reproducible as the official methods, while being simpler and less time consuming. A statistical analysis indicated that there was no significant difference between the results obtained by the proposed procedure and those of the official methods.

Cefadroxil↗
PubMed1986

Efficacy of a twice-daily regimen of cefadroxil in the treatment of respiratory tract infections.

This multicentre open study evaluated the responses of 474 adult and paediatric patients with upper or lower respiratory tract infections to treatment with cefadroxil (25 to 50 mg/kg in children and 500 mg to 1 g in adults) twice daily for 10 to 30 days. Complete or partial cures seen in 81% to 100% of all patients correlated with the eradication of 87% to 100% of the causative pathogens, most commonly beta-haemolytic streptococci, S. aureus or S. pneumoniae. Mild, transient side effects, usually gastrointestinal disturbances or hypersensitivity reactions, were reported in 4.8% of patients. Thus, the safety and efficacy of this oral cephalosporin recommends its use in the treatment of infections of the respiratory tract.

Cefadroxil↗
PubMed1985

Cefadroxil once daily for three or seven days versus amoxycillin for seven days in uncomplicated urinary tract infections in women.

The cure rate of acute uncomplicated urinary tract infection in general practice using 3 different treatment regimens, was studied in a randomized, multicenter trial. Patients were assigned to receive either cefadroxil 1 g once daily for 3 or 7 days or amoxycillin 375 mg t.i.d. for 7 days. 310 patients entered the study, of whom 230 could be evaluated according to the protocol. Two thirds of the cases were due to infections with Escherichia coli and about one fourth to Staphylococcus saprophyticus. No statistically significant differences in cure rates between the 3 regimens could be demonstrated neither at 1 week nor at 5 weeks of follow-up. The frequency of adverse reactions was low and similar in each treatment group.

Amoxicillin↗
PubMed1987

[The frequency of group A beta-hemolytic Streptococcus in acute tonsillopharyngitis and therapy with cefadroxil, clavulanic acid-amoxicillin combination and erythromycin in patients unresponsive to procaine penicillin therapy].

In January, February and March 1987, the frequency of Group A beta hemolytic streptococcus among 468 patients with acute tonsillopharyngitis who admitted to Dr. Sami Ulus Children's Hospital was % 41. Ten day procaine penicillin therapy was not successful in the % 29.5 patients. Cefadroxil (Duricef), clavulanic acid-amoxicillin combination (Augmentin) and erythromycin were tried in these patients. While the success rate of Duricef therapy was % 55, the results of other drug therapies were not been successful.

Acute Disease↗
PubMed1983

[Double-blind comparison of cefadroxil and cephalexin granules in the treatment of impetigo].

A double-blind clinical comparison of cefadroxil granules (CDX) and a long-acting preparation of cephalexin granules (L-CEX) was conducted in the treatment of impetigo in children. The long-acting cephalexin preparation was composed of 3 parts of granules soluble in the stomach and 7 parts of those soluble in the intestine. Drugs were administered at 3 different doses depending on the body weight of patients (Group I: less than 10 kg, Group II: between 10 kg and 20 kg, Group III: over 20 kg). Overall clinical evaluation by attending doctors: CDX group scored slightly better but not statistically significant results. Evaluation of usefulness: CDX group scored slightly better but not statistically significant results. Partially standardized evaluation: CDX scored statistically significantly higher points in the evaluation of total cases and Group II on Day 5, and Group II on Day 7. Cumulative points through Day 5 and Day 7 were not statistically significant. Follow-up evaluation by attending doctors: CDX group got a better result in total cases and Group II on day 3, and in total cases on days 5 and 7. Otherwise there was no statistically significant difference. Incidence of side effects was not significantly different between the 2 drug groups. As shown in Fig. 1, CDX was administered on rising in the morning, after lunch, and at bed time whereas L-CEX was given on rising and at bed time when the patients were relatively in fasting condition. This may have reduced the expected merit of L-CEX and some reserve is required in the interpretations of the results shown herein.

Adolescent↗