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PubMed1989

Non-linear intestinal absorption kinetics of cefadroxil in the rat.

Absorption of cefadroxil in a selective intestinal absorption area (the proximal third of the small intestine) of the anaesthetized rat, at seven initial perfusion concentrations, ranging from 0.01 to 10.0 mg mL-1, is shown to be a non-linear transport mechanism. With the aid of computer-fitting procedures based on differential and integrated forms of Michaelis-Menten equation, Vm and Km values of 36.7-37.3 mg h-1 and 12.0-13.0 mg, respectively, were found. The statistical parameters were better than those obtained both for first-order and for combined Michaelis-Menten and first-order kinetics. There is no evidence for substantial passive diffusion processes. The results reported here, together with allometric considerations and literature data analysis, may help to explain some particular non-linear features of plasma level curves associated with the administration of fairly high oral doses of cefadroxil to humans.

Animals↗
PubMed1982

Pharmacokinetics of cefadroxil and cefaclor during an eight-day dosage period.

The concentrations of cefadroxil and cefaclor in serum were studied in eight healthy volunteers receiving 1,000 mg of both substances three times per day for 8 days. Intraindividual comparisons showed an increase in peak serum levels of cefadroxil from days 1 to 8 in seven of eight volunteers. Cefaclor peak concentrations did not rise during the 8 days.

Adult↗
PubMed1983

Comparison of cefadroxil and cephalexin in the treatment of community-acquired pneumonia.

Thirty-four patients with community-acquired acute pneumonias were treated in a prospective, randomized trial with either cefadroxil, 500 mg twice daily, or cephalexin, 250 mg four times daily. In both groups of patients, the presence of chronic illnesses predisposing to pneumonia was common. Streptococcus pneumoniae was isolated from 65% of the initial sputum specimens, and most illnesses were of mild to moderate severity. All 19 cases treated with cefadroxil and all 15 cases treated with cephalexin were clinically cured, and adverse reactions to the medications were minimal. The success of these regimens suggests that outpatient use of oral cephalosporin therapy may be an appropriate treatment of patients with mild or moderate community-acquired pneumonia.

Adult↗
PubMed1989

Comparison of cefadroxil and cephalothin disk susceptibility test results.

Diffusion susceptibility tests with 30-micrograms cefadroxil disks and 30-micrograms cephalothin disks were evaluated. For both agents, the same zone size interpretive criteria were recommended (less than or equal to 14 mm for resistance and greater than or equal to 18 mm for susceptibility). Tests were performed with 904 bacterial isolates, and the data were examined to determine whether the two cephalosporins might be used interchangeably for purposes of in vitro susceptibility testing. When Haemophilus influenzae, Listeria monocytogenes, and methicillin-resistant staphylococci were evaluated, the two agents differed significantly. For testing other species, a cephalothin disk or cephalothin MIC could be used for predicting susceptibility or resistance to cefadroxil.

Bacteria↗
PubMed1980

Serum levels and urinary excretion in humans of BL-S 578 (cefadroxil), a new semisynthetic cephalosporin.

Single doses of 250 and 500 mg of BL-S 578 (cefadroxil), a new semisynthetic cephalosporin, were orally administered to 13 normal, healthy volunteers and serum levels determined at timed intervals for 7 h. Peak concentration was obtained at 1 1/2 h after administration of 250 mg (8.981 micrograms/ml) or 500 mg (17.861 micrograms/ml). Urniary excretion levels within 24 h after ingestion of single doses of 250 and 500 mg of cefadroxil were 89.92 and 86.34%, respectively.

Adult↗
PubMed1986

Cefadroxil-induced ampicillin-exacerbated pemphigus vulgaris: case report and review of the literature.

A 77-year-old patient is described who developed pemphigus vulgaris temporally with the administration of cefadroxil. The disease improved when the drug was discontinued but was exacerbated with the administration of ampicillin. This may be the first case of possible cefadroxil-induced and only the second case of ampicillin-induced pemphigus vulgaris reported. The pathophysiology, diagnosis, and treatment of pemphigus vulgaris is briefly described. Drug-induced pemphigus is reviewed. By far the most incriminated drug has been penicillamine. It is postulated that the sulfhydryl group of penicillamine alters the intercellular cement substance into an antigenic structure with subsequent antibody formation. The chemical similarity between penicillamine, the penicillins, and the cephalosporins is alluded to and the potential for cross-sensitivity between the penicillins and cephalosporins is emphasized. Although the pemphigus vulgaris could have occurred by chance, it seems probable that it was drug-induced.

Aged↗
PubMed1986

Treatment of acute and chronic sinusitis with cefadroxil.

In an open study, 30 patients (mean age 43.7 years) with clinical and radiological evidence of sinusitis were studied by transmaxillary sinus aspirations (19 bilateral and 11 unilateral for a total of 49 aspirates). The sinus aspirations were performed with careful sterile intermeatus needle puncture techniques and the material was cultured for aerobic and anaerobic bacteria. The organisms most frequently recovered from the sinus aspirates were Gram-positive (55%), Gram-negative (33%), and anaerobes (6%). Cefadroxil 1g was given every 12 hours (2g daily) for 10 days. Therapeutic efficacy was then evaluated on the basis of changes in clinical status, radiographic findings and, where possible, bacteriological results. Cefadroxil treatment produced a 90% cure rate assessed clinically and by radiological confirmation; moreover, the drug was well tolerated in the majority of patients.

Acute Disease↗
PubMed1988

Variable in vitro activity of cefaclor, cephalothin and cefadroxil against Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis.

The in vitro activity of cefaclor, cephalothin and cefadroxil to 50 Escherichia coli, 23 Klebsiella pneumoniae and 20 Proteus mirabilis strains was tested with the disc diffusion and microdilution plate techniques. Cefaclor was more active than cefadroxil, while cephalothin was intermediate. The differences seriously affected the classification into the routine SIR system. For susceptibility testing we question the use of cephalothin as a class representative of oral cephalosporins.

Cefaclor↗
PubMed1992

Oral cefadroxil prophylaxis in hip fracture surgery. Serum concentrations studied in 17 patients.

Serum concentration-time curves were determined in seventeen 82 (60-90) year-old patients undergoing trochanteric hip fracture surgery after receiving 1 g of cefadroxil per os. All the patients attained a serum level of antibiotic high enough to inhibit the growth of Staphylococcus aureus and S. epidermidis. When orally administered, cefadroxil should be given within 2 hours before surgery.

Aged↗
PubMed1995

Bone and wound fluid concentrations of cephalosporins. Oral cefadroxil and parenteral cefuroxime compared in 52 patients with a trochanteric fracture.

We performed a prospective and randomized study in 52 patients to compare the concentrations in cancellous bone and wound fluid of antibiotics, given orally (cefadroxil) or intravenously (cefuroxime) as prophylaxis in trochanteric fracture surgery. Oral cefadroxil resulted in adequate antibiotic levels in 22 of 26 patients in wound fluid and cancellous bone, while parenteral cefuroxime resulted in sufficient antibiotic levels in all 26 patients. The concentrations in bone varied greatly between the subjects.

Administration, Oral↗
PubMed1979

Bactericidal activity of cefadroxil, cephalexin, and cephradine in an in vitro pharmacokinetic model.

Cefadroxil (Duricef, Mead Johnson and Company), resembles cephalexin and cephradine in spectrum of antibacterial activity but differs in human pharmacokinetic properties. Whether the latter are likely to affect activity in vivo was assessed by determining bactericidal activity against clinical isolates under conditions simulating the variation of drug concentration in the blood stream after an oral dose of 500 mg to adults. In this kinetic model, cefadroxil was more active than cephalexin or cephradine against Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, Proteus mirabilis, Haemophilus influenzae and one of two strains of Escherichia coli. The other strain of E. coli was virtually unaffected by the cephalosporins. S. pyogenes was equally susceptible to all three cephalosporins. Analysis of the results suggest that the pharmocokinetic properties of an antibiotic affect its activity in the blood stream, provided the susceptibility of the infecting organism is concentration-dependent within the range of drug concentration occurring in serum.

Adult↗
PubMed1989

[Efficacy and tolerability of cefuroxime-axetil in infections of the upper respiratory tract. Comparative study with cefadroxil].

Cefuroxime-axetil is the first oral broad spectrum cephalosporin to be naturally stable in the presence of bêta-lactamases. The aim of this randomized trial was to evaluate the efficacy and safety of cefuroxime-axetil (250 mg twice daily after meal) with cefadroxil (1 g twice daily during meal) for the treatment of upper respiratory tract infection. In this study 150 patients were enrolled. Before treatment, the two groups were comparable. Clinical success was achieved for 94.3% of the patients treated with cefuroxime-axetil versus 90.4% for cefadroxil. Statistical significance was reached (p less than 0.05) concerning the number of days with facial pain for sinusitis (3 days for the cefuroxime-axetil treated group versus 4 days), the rate of normal tympanum at the second examination (58.3% vs 20% respectively) for otitis, and the number of day with painful dysphagia for tonsillitis (2.6 vs 3.8 days respectively). Cefuroxime-axetil was safe (a few advers events occurred, almost all gastro-intestinal). Cefuroxime-axetil is a safe and effective treatment of upper respiratory tract infections.

Adolescent↗
PubMed1987

Liquid-chromatographic determination of five orally active cephalosporins--cefixime, cefaclor, cefadroxil, cephalexin, and cephradine--in human serum.

We report an isocratic "high-performance" liquid-chromatographic (HPLC) procedure for measurement of five orally administered cephalosporins (cefixime, cefaclor, cefadroxil, cephalexin, and cephradine) in 0.1 mL of human serum. Serum protein is precipitated with acetonitrile, the sample is centrifuged, and the supernate is evaporated under nitrogen. The residue is reconstituted in 0.1 mL of mobile phase, and 50 to 80 microL of this is injected onto a reversed-phase Altex Ultrasphere Octyl (C8) column. The five cephalosporins are resolved by elution with a pH 2.6 mobile phase of methanol/monobasic phosphate buffer (20/80) by vol), flow rate 2 mL/min. The column effluent is monitored at 240 nm. Cefixime serves as the internal standard for the analysis of the four other compounds, cephalexin as the internal standard for cefixime. We used two standard curves for all compounds: a low-range curve for concentrations commonly observed clinically and a higher-range curve for higher concentrations. The former were linear from 1.0 to 10 mg/L for cefaclor, cefadroxil, cephalexin, and cephradine and from 0.1 to 1 mg/L for cefixime. The high-concentration curves were linear from 1 to 10 mg/L for cefixime and from 10 to 100 mg/L for the other compounds. The detection limits were 0.1 mg/L for cefixime, 1 mg/L for the other cephalosporins. Mean within-run and day-to-day CVs were always less than 15% for all compounds studied.

Cefaclor↗
PubMed1984

Comparison of in vitro antibacterial activity of four oral cephems: cephalexin, cefaclor, cefatrizine and cefadroxil.

The in vitro antibacterial activity of four oral cephems: cephalexin, cefaclor, cefatrizine and cefadroxil against clinical isolates of staphylococci, Enterobacteriaceae and Pseudomonas aeruginosa was compared by agar dilution method. All drugs had comparable antistaphylococcal activity. Cefatrizine and cefaclor were more active than cephalexin and cefadroxil against Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis. All four drugs were relatively inactive against isolates of Enterobacter species and indole-positive Proteus. However, cefatrizine demonstrated the greatest activity of the four oral cephems against these organisms. None of these oral cephems was active against Serratia marcescens or Pseudomonas aeruginosa.

Bacteria↗
PubMed1984

Treatment of exacerbations of chronic bronchitis. A comparative double-blind study with cotrimoxazole and cefadroxil.

A double-blind, randomized study was carried out in 40 chronic bronchitic patients, to evaluate the effectiveness of cefadroxil as compared with cotrimoxazole in the treatment of the exacerbation stage. The patients were in hospital while the study lasted and received cotrimoxazole at doses of 160 mg of trimethoprim and 800 mg of sulfamethoxazole twice a day, or cefadroxil 500 mg twice a day, for seven days. To evaluate the response the following parameters were used: clinical improvement, reduction in volume of sputum, reduction in purulence of the sputum and eradication of germs from the sputum. All the parameters improved in both groups of patients without any significant difference between the two types of treatment.

Adult↗
PubMed1983

[Concentration of cefadroxil in kidney tissue and serum after oral administration in patients with normal and impaired renal function].

In 17 patients (7 with normal renal function, 10 with impaired renal function) who underwent renal surgery, renal tissue samples and blood samples were taken 3-4 h following the administration of a single oral dose of 1000 mg cefadroxil. It was demonstrated that the concentrations in renal tissue were within the range from 14.2 to 115 micrograms/g tissue, while the serum levels varied from 11.6 to 63.3 micrograms/ml serum. A statistically significant correlation between serum levels and renal tissue levels can be demonstrated. The correlation of the distribution ratio: serum level/tissue level to serum creatinine level proved to be a linear regression, i.e. the distribution quotient decreased if the serum creatinine level increased. This means that the renal tissue level of cefadroxil in comparison to serum level will be lower in patients with renal impairment. However, even with much impaired renal function the renal tissue level exceeded the minimum inhibitory concentration for the most relevant pathogens.

Administration, Oral↗
PubMed1981

The pharmacokinetics of cefadroxil associated with probenecid.

The effects of probenecid on the pharmacokinetic parameters of cefadroxil administered in a single dose of 500 mg are studied. The serum and urine levels of the antibiotic were determined by a microbiologic plate diffusion method. The antibiotic follows a single-compartment model. The half-life of cefadroxil in serum has an average value of 1.13 h, rising to 1.63 h when the antibiotic is associated with probenecid. The apparent distribution volume remains unmodified with a value close to 23 liters. The lag time is 0.25 h in the absence of probenecid, rising to 1.029 h in the presence of the uricosuric agent.

Adult↗
PubMed1982

Influence of dosage form and administration route on the pharmacokinetic parameters of cefadroxil.

A cross-over study was utilized to compare the pharmacokinetics of 500 mg cefadroxil administered intravenously and orally in solution, suspension, and in capsule form, and to calculate its bioavailability. The antibiotic was administered to four healthy volunteers on whom four experiments were carried out. Cefadroxil was determined in serum and in urine using a microbiologic plate diffusion method. Administered intravenously the antibiotic follows a two-compartment open kinetic model, whereas orally administered, its mode is that of a single-compartment model. There are no statistically significant differences between the parameters defining the elimination of the antibiotic in the four groups studied.

Administration, Oral↗