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PubMed1992

A rapid first-derivative spectrophotometric analysis of cephalexin and cephradine in human urine.

A rapid, simple, and accurate first-derivative spectrophotometric method has been established for the determination of either cephalexin or cephradine in urine. Quantitative analysis of each antibiotic was achieved by measuring the peak amplitude at 268 nm. The relative and absolute recoveries ranged from 98.90 to 104.00% for cephalexin and from 97.85 to 105.10% for cephradine. The within-day coefficient of variation varied from 3.27 to 6.45%. The applicability of the method for the determination of the cumulative amount of either cephalexin or cephradine excreted unchanged in urine, following an oral dose containing 500 mg of the drug to a human male volunteer, is demonstrated.

Adult↗
PubMed2005

Pharmacokinetics of two once-daily parenteral cephalexin formulations in dogs.

The aims of this study were to describe and compare the pharmacokinetic profiles and T(>MIC90) of two commercially available once-daily recommended cephalexin formulations in healthy adult dogs administered by the intramuscular (i.m.) route. Six beagle dogs received a 10 mg/kg dose of an 18% parenteral suspension of cephalexin of laboratory A (formulation A) and laboratory B (formulation B) 3 weeks apart. Blood samples were collected in predetermined times after drug administration. The main pharmacokinetic parameters were (mean +/- SD): AUC((0-infinity)), 72.44 +/- 15.9 and 60.83 +/- 13.2 microg.h/mL; C(max), 10.11 +/- 1.5 and 8.50 +/- 1.9 microg/mL; terminal half-life, 3.56 +/- 1.5 and 2.57 +/- 0.72 h and MRT((0-infinity)), 5.86 +/- 1.5 and 5.36 +/- 1.2 h for formulations A and B, respectively. T(>MIC90) was 63.1 +/- 14.7 and 62.1 +/- 14.7% of the dosing interval for formulations A and B, respectively. Median (range) for t(max) was 2.0 (2.0-3.0) h and 3.0 (2.0-4.0) for formulations A and B, respectively. Geometric mean ratios of natural log-transformed AUC((0-infinity)) and C(max) and their 90% confidence intervals (CI) were 0.84 (0.72-0.98) and 0.83 (0.64-1.07), respectively. The plasma profiles of cephalexin following the administration of both formulations were similar. No statistical differences between pharmacokinetic parameters or T(>MIC90) were observed, however, bioequivalence between both formulations could not be demonstrated, as lower 90% CI failed to fell within the selected range of 80-125% for bioequivalence.

Animals↗
PubMed1997

Pharmacokinetics of cephalexin in cats after oral administration of the antibiotic in tablet and paste preparations.

OBJECTIVE: To determine the bioequivalence of a paste formulation of cephalexin with that of the tablet form. DESIGN: A two-way cross-over study. ANIMALS: Ten adult cats of mixed breed. PROCEDURE: The cats, randomly allocated to two groups, received either the paste preparation or the tablet orally at 12-hour intervals for 48 h before a 12-hour blood collection period. Two weeks later the treatments were reversed and the blood sampling repeated. The serum concentrations of the antibiotic were determined. The pharmacokinetic factors were analysed using a computer. RESULTS: There were no significant differences between the peak concentration of cephalexin, or the other pharmacokinetic factors obtained from the tablet and paste formulations. The serum profiles of cephalexin following four 12-hourly doses of each formulation were similar with the peak serum values occurring at approximately 2 h after administration. CONCLUSION: The paste formulation and the tablet form are bioequivalent.

Administration, Oral↗
PubMed1977

Comparative pharmacology of cefaclor and cephalexin.

Two cephalosporin antibiotics, cefaclor and cephalexin, were administered orally to healthy, adult male volunteers for comparison of their pharmacological properties. In doses of 250 mg orally, cefaclor produced a peak serum concentration of 6.01 +/- 0.55 (standard deviation [SD]) mug/ml compared with 9.43 +/- 2.36 mug/ml for cephalexin (P < 0.01). The half-lives were 0.58 +/- 0.07 (SD) h and 0.80 +/- 0.12 (SD) h, and elimination constants were 1.22 +/- 0.15 and 0.88 +/- 0.13 h(-1) for cefaclor and cephalexin, respectively (P < 0.001). Neither drug showed accumulation over the dosing period, and both were well tolerated.

Adult↗
PubMed1981

Antibacterial properties of alafosfalin combined with cephalexin.

The phosphonopeptide alafosfalin (L-alanyl-L-1-aminoethylphosphonic acid) exhibited synergy in vitro and in animal studies against a range of bacterial genera when combined with cephalexin. Alafosfalin also showed synergy with mecillinam and, to a much lesser extent, with ampicillin. Synergy with cephalexin was more pronounced when the bacteria were relatively insensitive to the beta-lactam component. The action of this combination involved both an inhibitory and a bacteriolytic mechanism which was abolished by concurrent treatment with the aminopeptidase inhibitor, bestatin. Regrowth of subpopulation resistant to either component was markedly reduced by the combination. The potential of alafosfalin combined with cephalexin for use in therapy is discussed.

Alanine↗
PubMed1986

Single-dose cephalexin therapy for acute bacterial urinary tract infections and acute urethral syndrome with bladder bacteriuria.

The efficacy of single-dose therapy with 3 g of cephalexin was evaluated in 129 women with symptoms of acute uncomplicated lower urinary tract infections. Of 91 patients with significant bacteriuria, 61 (67%) were cured of their original infection; this was similar to the 54 to 79% cure rates reported in unselected populations of women of a wide age range treated for acute uncomplicated urinary tract infections with a single dose of amoxicillin or trimethoprim-sulfamethoxazole (J. Rosenstock, L. P. Smith, M. Gurney, K. Lee, W. G. Weinberg, J. N. Longfield, W. B. Tauber, and W. W. Karney, Antimicrob. Agents Chemother. 27:652-654, 1985; N. E. Tolkoff-Rubin, M. E. Wilson, P. Zuromskis, I. Jacoby, A. R. Martin, and R. H. Rubin, Antimicrob. Agents Chemother. 25:626-629, 1984). The cure rates of (87%) for our younger patients, those less than 25 years of age, was better than that (46%) for our patients over 40 years of age (P less than 0.001). Patients with infections that were negative in an antibody-coated bacteria test were cured at a significantly higher rate than those with infections that were positive in an antibody-coated bacteria test (71 versus 19%; P = 0.003). Those patients with infections caused by cephalexin-susceptible organisms were cured at a rate similar to that for patients with infections caused by cephalexin-resistant organisms (68 versus 50%; P = 0.62). The cure rate for suburban patients was 90%, versus 45% for inner-city patients (P = 0.008). Of the 28 women with acute urethral syndrome due to low-level bacteriuria, 27 were cured.

Acute Disease↗
PubMed1990

Comparative in vitro activities of amoxicillin-clavulanic acid, cefuroxime, cephalexin, and cephalothin against trimethoprim-resistant Escherichia coli isolated from stools of children attending day-care centers.

A high prevalence of fecal colonization with trimethoprim-resistant Escherichia coli was found in diapered children attending day-care centers in Houston, Tex. In the present study, 100 isolates of E. coli resistant to multiple antibiotics, including trimethoprim (100%), sulfisoxazole (100%), streptomycin (94%), and ampicillin (87%), were obtained over a 5-month period from stool samples of diapered children attending four day-care centers and tested for their susceptibilities to amoxicillin-clavulanic acid, cefuroxime, cephalexin, and cephalothin. The MICs for 50 and 90% of strains tested were 16 and 32 micrograms/ml, respectively, for amoxicillin-clavulanic acid, 4 and 16 micrograms/ml, respectively, for cefuroxime, 4 and 64 micrograms/ml, respectively, for cephalexin, and 32 and greater than 64 micrograms/ml, respectively, for cephalothin. Although all three oral beta-lactams tested were generally active at concentrations likely to be achieved in urine, cefuroxime and cephalexin were more potent and are thus more likely to be inhibitory at the concentrations needed for systemic infections.

Amoxicillin↗
PubMed1990

Randomized comparative study of cefixime versus cephalexin in acute bacterial exacerbations of chronic bronchitis.

Patients with purulent exacerbation of chronic bronchitis were randomized to receive either a single 400-mg daily dose of cefixime or 250 mg of cephalexin, orally, four times a day. Patients were males with a mean age of 63 years. Of the 86 patients, 71 (82%) had bronchitis caused by a single organism (29 by Haemophilus influenzae, 27 by Branhamella catarrhalis, 9 by gram-negative enteric organisms, 6 by Streptococcus pneumoniae), while more than one pathogen was implicated in 15 patients (18%). A total of 70.8% of the cefixime group and 50% of the cephalexin group were clinically cured (chi 2 = 3.89, P less than 0.05); however, when the categories of cured and improved were combined, no significant difference was noted between treatment groups (chi 2 = 3.39, P = 0.06). Analysis of side effects included all 130 evaluable and nonevaluable patients: diarrhea was noted in six patients in the cefixime group and none of the patients in the cephalexin group (P = 0.013 by the Fisher exact test). The diarrhea was mild and self-limited in all cases. B. catarrhalis has emerged as a major cause of exacerbation of bronchitis in our experience; there is an increased need to emphasize the examination of sputum samples by Gram staining if cost-effective antibiotic choices are to be made; any empirically chosen antibiotic should have activity against beta-lactamase-producing strains of B. catarrhalis as well as S. pneumoniae and H. influenzae.

Acute Disease↗
PubMed1973

Double-blind comparison of carbenicillin indanyl sodium, ampicillin, and cephalexin in treatment of urinary tract infection.

Carbenicillin indanyl sodium, ampicillin, or cephalexin was administered orally to 61 patients with urinary tract infections. Assignment of drug was made by a computer-generated, randomized plan in a double-blind fashion. The rates of cure 4 weeks after therapy were 50, 42, and 50% for patients treated with carbenicillin, ampicillin, and cephalexin, respectively. Failure of therapy was correlated with chronicity of infection and sensitivity of the microorganism to the antibiotic used. Thirty-nine percent of the patients developed side effects, but there were no significant differences in side effects among the three antibiotics. This double-blind study demonstrates that carbenicillin indanyl sodium is as effective as ampicillin and cephalexin in treatment of urinary tract infections.

Adolescent↗
PubMed1976

Cefatrizine (SK&F 60771), a new oral cephalosporin: serum levels and urinary recovery in humans after oral or intramuscular administration--comparative study with cephalexin and cefazolin.

Cefatrizine (SK&F 60771), a new broad-spectrum cephalosporin, was administered in a 0.5-g dose either orally or intramuscularly to volunteers in a crossover study. After oral administration, the average peak serum levels were 5.6 and 22.1 mug/ml for cefatrizine and cephalexin, respectively. The serum half-life of cefatrizine appeared to be more extended than that of cephalexin. Urinary recovery of cefatrizine (35%) was approximately half that of cephalexin (68%) after oral administration. After intramuscular injection of 0.5 g, the average peak serum level of cefatrizine (12.0 mug/ml) was approximately one-fourth that of cefazolin (44.0 mug/ml). The serum half-life after intramuscular injection was 86 min for cefatrizine and 118 min for cefazolin. Urinary recovery was 45% of the intramuscularly administered dose, as compared with cefazolin, which was 74%.

Administration, Oral↗
PubMed1983

Cephalexin-supplemented Jones-Kendrick charcoal agar for selective isolation of Bordetella pertussis: comparison with previously described media.

Four agar media, Jones-Kendrick (JK) charcoal agar unsupplemented, JK agar supplemented with 0.5 U of penicillin per ml, JK medium supplemented with 2.5 micrograms of methicillin per ml, and JK medium supplemented with 40 micrograms of cephalexin per ml, were evaluated to determine their ability to support growth of Bordetella pertussis, their ability to selectively inhibit normal pharyngeal flora while maintaining growth of B. pertussis, and their stability during storage. Five stock cultures of B. pertussis were plated on each of the media. Penicillin- and cephalexin-supplemented media were more inhibitory for early growth of B. pertussis than was medium supplemented with methicillin. However, after 5 days of incubation at 35 degrees C, all media supported good growth of this organism. When employed to detect B. pertussis in sham specimens, prepared by mixing normal pharyngeal material with each of the five B. pertussis stock cultures, the medium containing cephalexin was judged superior to all other media tested in its combined ability to suppress the growth of normal pharyngeal flora and to allow early detection of Bordetella colonies. All media tested retained their efficacy after 9 weeks of storage at 2 to 8 degrees C.

Bordetella pertussis↗
PubMed1988

Failure of charcoal-horse-blood broth with cephalexin to significantly increase rate of Bordetella isolation from clinical specimens.

In a field trial conducted in cooperation with pediatricians in private practice, 198 nasopharyngeal swabs from children with suspected whooping cough were placed into charcoal-horse-blood transport medium with cephalexin (40 mg/liter). After preincubation at 36 degrees C for 1 to 2 days, the transport systems were mailed to the laboratory. There, the swabs were plated onto charcoal-horse-blood agar with cephalexin and were subsequently incubated for 48 h in cephalexin-containing charcoal-horse-blood broth which was then subcultured onto the agar. Forty-six Bordetella pertussis strains and seven Bordetella parapertussis strains were isolated (Bordetella isolation rate, 26.8%). Only three (5.7%) of the 53 Bordetella strains were detected exclusively by use of the broth. This low rate of additional isolates is probably explained by the fact that the swabs had been submitted in charcoal-horse-blood transport medium which itself acts as an enrichment medium.

Blood↗
PubMed1972

Double-blind trial to compare ampicillin, cephalexin, co-trimoxazole, and trimethoprim in treatment of urinary infection.

In order to test their value in urinary infection a double-blind trial was carried out using ampicillin, cephalexin, trimethoprim-sulphamethoxazole (co-trimoxazole), and trimethoprim. Eighty-three courses of treatment were given to hospital patients, 149 to pregnant women, and 107 to patients with dysuria and frequency seen in domiciliary practice. Thus infections of varying severity in defined groups of patients caused by organisms with different antibiotic sensitivities were treated.Analysis of the overall results (339 courses) was compared with those from the individual groups and considerable variation in response was found. In domiciliary infections and bacteriuria in pregnancy trimethoprim alone proved to be at least as effective as the other three compounds and caused fewer than half the number of side effects. In the hospital patients co-trimoxazole was superior to trimethoprim.The overall results for ampicillin and cephalexin were similar although cephalexin proved to be inferior in treating symptomatic domiciliary infections.

Ampicillin↗
PubMed1972

Cephalexin levels in human bile in presence of biliary tract disease.

Cephalexin was given to 24 patients before and after operation on the bile ducts and gall bladder. Two patients had obstructive jaundice. Samples of the bile were taken either directly from the gall bladder at operation or via the T-tube. Cephalexin was excreted in the bile, peak levels being obtained after two to three hours. These levels could be raised if probenecid was given concurrently. Higher levels were found in patients with functioning gall-bladders. A trial of cephalexin seems justified for the treatment of typhoid carriers.

Bile↗
PubMed1977

The comparative efficacy of cephalexin and sulfisoxazole in acute urinary tract infection in children.

A double blind, comparative study of the efficacy of cephalexin versus sulfisoxazole was conducted on 100 children with initial episodes of urinary tract infections. The overall bacteriologic and clinical cure rates were comparable for both antimicrobials. Children treated with cephalexin had a clinical cure rate of 86 per cent and a bacterial cure rate of 84 per cent, while those given sulfisoxazole were found to have rates of 82 and 92 per cent respectively. However, cephalexin was noted to have a rather high rate of failure in the therapy of Proteus micrabilis infections (4/8), casting some doubt on its use in urinary infections caused by the organism. Untoward effects associated with either medication were minimal.

Acute Disease↗
PubMed1996

Addition of rifampin to cephalexin therapy for recalcitrant staphylococcal skin infections--an observation.

We report two pediatric patients with recalcitrant staphylococcal infections whose infections resolved when rifampin was added to standard antistaphylococcal therapy. One patient had a post-varicella staphylococcal ulcerative lesion and did not respond to cephalexin alone but did respond when rifampin was added. A second patient had staphylococcal bullous impetigo and did not respond to dicloxacillin or cephalexin but did respond when rifampin was added to the cephalexin. If a patient fails to respond to traditional antistaphylococcal therapy, the addition of rifampin may be beneficial.

Cephalexin↗
PubMed2003

Hydroxypropyl methylcellulose based cephalexin extended release tablets: influence of tablet formulation, hardness and storage on in vitro release kinetics.

The object of this study was to develop hydroxypropyl methylcellulose (HPMC) based cephalexin extended release tablet, which can release the drug for six hours in predetermined rate. Twenty-one batches of cephalexin tablets were prepared by changing various physical and chemical parameters, in order to get required theoretical release profile. The influences of HPMC, microcrystalline cellulose powder (MCCP), granulation technique, wetting agent and tablet hardness on cephalexin release from HPMC based extended release tablets were studied. The formulated tablets were also characterized by physical and chemical parameters. The dissolution results showed that a higher amount of HPMC in tablet composition resulted in reduced drug release. Addition of MCCP resulted in faster drug release. Tablets prepared by dry granulation was released the drug slowly than the same prepared with a wet granulation technique. Addition of wetting agent in the tablets prepared with dry granulation technique showed slower release. An increase in tablet hardness resulted in faster drug release. Tablets prepared with a wet granulation technique and having a composition of 9.3% w/w HPMC with a hardness of 10-12 kg/cm(2) gave predicted release for 6 h. The in vitro release data was well fit in to Higuchi and Korsmeyer-Peppas model. Physical and chemical parameters of all formulated tablets were within acceptable limits. One batch among formulated twenty-one batches was successful and showed required theoretical release. The effect of storage on in vitro release and physicochemical parameters of successful batch was studied and was found to be in acceptable limits.

Cephalexin↗
PubMed1979

Concentrations of cephalexin in mandibular alveolar bone, blood, and oral fluids.

Results from this study of 16 patients who underwent extractions and alveoloplasty indicate that cephalexin effectively penetrates alveolar bone. After cephalexin had been administered, 500 mg four times a day for 48 hours, the average concentration in bone exceeded the average minimal inhibitory concentration of six organisms commonly encountered in infections and bacteremias of dental origin. These data and the current knowledge of cephalexin suggest that cephalosporins may have a unique use in dental infections or potentially harmful bacteremias caused by susceptible organisms.

Adult↗