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PubMed2002

Comparison of several methods used for the determination of cephalosporins. Analysis of cephalexin in pharmaceutical samples.

The precision of UV absorbance of intact and acid degraded cephalosporins, ninhydrin, high performance liquid chromatography and iodometric methods used for analysis of cefoxitin, cefotaxime, cephazolin and cephalexin were compared. To obtain the calibration graphs the analytical signal used were: absorbance, first derivative absorbance, second derivative absorbance and H-point Standard Additions Method by using absorbance values at two selected wavelengths as analytical signal. These methods and calibration graphs were also used for the determination of cephalexin in pharmaceutical samples.

Capsules↗
PubMed2001

Bioaugmentation and treatment of cephalexin drug-based pharmaceutical effluent in an upflow anaerobic fluidized bed system.

Cephalexin is a constituent of the cephalosporin group used for the treatment of bronchitis and other heart diseases due to its enhanced oral activity. The effluent from these industries contains a disintegrated form of the drug contributing high chemical oxygen demand (COD), volatile solids and organic solvent. A laboratory-scale study was conducted to evaluate the efficiency of a fluidized bed reactor operated under anaerobic condition with bioaugmentation to treat the cephalexin containing pharmaceutical factory effluent. The main objective of the study was to show that bioaugmentation could be used to promote biological treatment to applications where conventional operation might be difficult or unfavourable. The effluent, with COD of 12,000-15,000 mg/l, was diluted and studied in single and multiple inoculation experiments with hydraulic retention times of 3-12 h. The removal efficiency after inoculation from an anaerobic sequencing batch reactor was related to influent concentration, mass of inoculum and hydraulic retention time characterized by calculating the initial food to microorganism ratio. Continuous COD removal efficiency attained a maximum value of 88.5% using bioaugmentation through periodic addition of acclimated cells every 2 days with 30-73.2 g of cells from an off-line enricher-reactor.

Anaerobiosis↗
PubMed1983

Ampicillin and cephalexin in renal insufficiency.

We analyzed the relationship between functional damage and transport processes in the kidney in patients with glomerulonephritis and renal failure by a new analytic method. In renal failure patients, there was substantial diminution of maximum transport of secretion in renal tubules. This reduction affected the urinary excretion of ampicillin and cephalexin substantially because both drugs depend on active renal tubular secretion. Our results indicate that dosage adjustment based on creatinine clearance is not appropriate for patients receiving drugs requiring active tubular secretion for urinary excretion. Our data point to a need for a prolongation of the dosage interval of cephalexin to 20 times that in normal subjects, while five times is recommended by the creatinine clearance. In these patients, it is therefore suggested that a dosage adjustment method that involves both factors--glomerular and renal tubular functions--is required.

Acute Kidney Injury↗
PubMed2001

Bullous pemphigoid induced by cephalexin.

Two young men developed severe bullous eruptions with a distinctive clinical picture of severe flexural involvement and extensive mucosal ulceration. Biopsies showed subepidermal bullae and associated inflammation consisted of predominantly neutrophils. Both had IgG and C3 staining of the dermal-epidermal junction on direct immunofluorescence. Bullous pemphigoid was diagnosed on the basis of clinical, histopathological and immunofluorescence findings. Both cases occurred after recent ingestion of cephalexin. We believe they represent the first reported cases of bullous pemphigoid induced by cephalexin.

Adrenal Cortex Hormones↗
PubMedDate not supplied

Excretion of penicillins and cephalexin in bovine milk following intramammary administration.

The elimination into bovine milk of beta-lactam antibiotic residues (procaine penicillin G, cloxacillin, ampicillin, oxacillin, cephalexin) following intramammary administration of 10 preparations marketed in France was studied. The quantitative analysis of residues was carried out by a microbiological agar diffusion method using Bacillus stearothermophilus. Sensitivity ranged from 0.001 I.U./ml for procaine penicillin G and 0.001 micrograms/ml for ampicillin to 0.02 micrograms/ml for cephalexin. The mean periods of elimination on which withholding times are based were between four and seven milkings according to the drugs administered.

Agar↗
PubMed1975

Sensitivities of strains of enteropathogenic Escherichia coli to cephalexin and other antibiotics.

The sensitivity patterns of strains of enteropathogenic Escherichia coli to nine antibiotics were determined. Most strains were sensitive to gentamicin, kanamycin, neomycin, and colistin. Sensitivity to cephalexin was generally greater than sensitivity to ampicillin. Compared with sensitivity patterns of strains isolated in previous years, no significant change in sensitivity patterns of recently isolated strains was detected. All ampicillin-resistant strains destroyed the drug by producing beta-lactamase. The activity of this enzyme against cephalexin was significantly lower than its activity against ampicillin. The role of beta-lactamase, the correlation between its production and resistance to beta-lactamase antibiotics, and the similarity between beta-lactamase produced by EEC and the classified beta-lactamases produced by other enteric bacteria and Escherichia coli, are discussed.

Amidohydrolases↗
PubMed1993

Comparison of azithromycin, roxithromycin, and cephalexin penetration kinetics in early and mature abscesses.

During the process of abscess formation, a myriad of changes are observed histologically that impede the penetration of antimicrobial agents into infection loci. A Staphylococcus aureus foreign body abscess, developed in rats, was employed to evaluate the penetration kinetics of azithromycin, roxithromycin and cephalexin at various stages of abscess development; the progressive patho-histological changes of abscess formation were also characterized in this model. In an early abscess (18 h post-challenge), azithromycin penetration into inflammatory fluid was enhanced (AUC of 351 vs 130 mg.h/kg) and residence prolonged relative to an inflammation control (half-life of 88 vs 27 h). In contrast, roxithromycin and cephalexin penetration into, and residence in, inflammatory fluid were unaltered in the early abscess. However, penetration into, and egress from, a mature abscess (ten days post-challenge) were impeded for all three antimicrobials (P < or = 0.03). The penetration kinetics of azithromycin into inflammatory fluid in an early abscess were independent of the dose regimen, but dependent on the total dose. The persistently high concentrations of azithromycin in inflammatory fluid within abscess were associated with the infiltration of phagocytic cells and encapsulation by fibrous tissue. These data are consistent with a phagocytic delivery mechanism for azithromycin, whereby the presence of high concentrations of azithromycin in inflammatory fluid are a consequence of augmented drug distribution via the release of accumulated intracellular drug from the infiltrating phagocytic cells and fibroblasts associated with abscess formation.

Abscess↗
PubMed1978

Effects of cephalexin, erythromycin and clindamycin on the aerobic Gram-negative faecal flora in man.

The effects of 5-day courses of orally administered cephalexin, clindamycin and erythromycin on the Gram-negative, aerobic faecal flora of healthy adults were examined. The concentration of cephalexin reached in the intestine was high enough to cause the emergence of resistant Gram-negative bacteria; organisms belonging to the genera Enterobacter, Citrobacter and Pseudomonas increased to easily detectable levels. The faecal concentration of erythromycin was high and caused a severe reduction of the coliform flora. Clindamycin administration resulted in a considerable increase in the coliform count; the increase in the proportion of klebsiellae was especially marked.

Administration, Oral↗
PubMed1987

High performance liquid chromatographic analysis of cephalexin in serum and urine.

A rapid, highly sensitive high performance liquid chromatographic method has been developed for the determination of cephalexin in serum and urine. Serum protein was precipitated with 1% zinc sulphate solution containing cephradine as the internal standard. The drugs were eluted from a 5 micron, C-18 reversed-phase column at ambient temperature with a mobile phase consisting of acetonitrile-methanol-acetate buffer of pH 4.2 (10:10:80%), at a flow rate of 1.4 ml/min with ultraviolet detection at 254 nm. Each analysis lasted 9 min. Quantification was achieved by the measurement of the peak-height ratio and the relative and absolute recoveries varied from 98 to 103%. Detection limits for cephalexin were 1 microgram/ml in serum and 5 micrograms/ml in urine. Within-run coefficient of variation ranged from 0.73 to 5.63% at three different concentrations for the serum and urine assay.

Adult↗
PubMedDate not supplied

Cephalexin concentration in the human ejaculate following oral and parenteral administration.

Cephalexin levels in the ejaculates of 31 infection-free volunteers have been determined following the administration of 1 g of antibiotic. In 16 subjects the cephalexin was administered by intramuscular injection and in 15 by mouth. In each case the volunteers were divided into groups of five each of which received the drug, 1, 2 or 4 hours before the collection of semen. Antibiotic concentrations were determined microbiologically on agar plates using Sarcina lutea ATCC 9341. For selection purposes healthy subjects were considered to be those showing a normal anamnesis and physical exploration, an absence of leucocytes demonstrable by a cytomorphological evaluation of the semen, semen citric acid and fructose levels within normal limits and a qualitatively and quantitatively similar saprophytic flora to that seen in a culture of urine taken immediately before the collection of semen. Maximum concentrations were obtained 2 hours after the administration of the antibiotic and the concentration following intramuscular injection (6.9 microgram/ml) was significantly greater than that following oral administration (4.7 microgram/ml).

Administration, Oral↗
PubMed2006

Successful treatment of recalcitrant necrotizing eosinophilic folliculitis using indomethacin and cephalexin.

A 56-year-old man presented with a 4-month history of a painful and pruritic eruption consisting of crusted plaques and blisters on his face, scalp and chest. The patient suffered from headaches and malaise but was afebrile. Two skin biopsies revealed an epidermis which was eroded and covered by locules of serum and neutrophils. In the underlying dermis, there was a marked mixed inflammatory reaction including lymphocytes, neutrophils and numerous eosinophils. There was exocytosis of eosinophils into several follicles with areas of follicular mucinosis. A diagnosis of necrotizing eosinophilic folliculitis was made based upon the clinical and histopathological findings. The diagnosis was supported by the rapid response to a combination of indomethacin and cephalexin. The patient has taken continuous indomethacin (with rabeprazole and misoprostol cover) and cephalexin for 2 years. If treatment is withdrawn he experiences a flare of his disease within 2 weeks. This case highlights the potentially chronic nature of this disease.

Administration, Oral↗
PubMed1991

Transport characteristics of ceftibuten, cefixime and cephalexin across human jejunal brush-border membrane.

The transport characteristics of orally active cephalosporins, ceftibuten, cefixime and cephalexin have been examined using brush border membrane vesicles isolated from human jejunum. In the initial uptake of ceftibuten, the stimulation and overshoot phenomena were observed in the presence of an inward H+ gradient. Effects of H+ gradient on the uptake of cefixime and cephalexin were low and no overshoot was observed. These transport characteristics, especially uphill transport phenomena, were in agreement with previous results obtained from rat intestinal brush-border membrane vesicles and suggest that these beta-lactam antibiotics are absorbed by different transport systems, despite their similar molecular structures.

Biological Transport, Active↗
PubMed1991

Transport of cephalexin to the cerebrospinal fluid directly from the nasal cavity.

The aim of the present study has been to confirm the existence of a transport pathway for a drug (cephalexin) to the cerebrospinal fluid (CSF) directly from the nasal cavity, by comparing the drug's concentrations in CSF after intranasal (i.n.), intravenous (i.v.) and intraduodenal (i.d.) administration. Higher levels of the drug were found in CSF following i.n. administration compared with the i.v. and i.d. routes, even though its plasma concentrations were similar. These findings suggest the existence of a direct transport pathway for cephalexin from the nasal cavity to the CSF. The concentration of drug in CSF at 15 min after i.n. administration was higher than that at 30 min. In contrast, its concentrations in CSF at 15 min after i.v. and i.d. administration were not significantly different from those at 30 min. The results confirm the presence of a direct transport pathway to CSF from the nasal cavity. This pathway may represent a new delivery route to CSF and possibly to brain parenchyma.

Administration, Intranasal↗
PubMed1997

Short-period double-dosing for simultaneous evaluation of intestinal absorption and hepatic disposition in a single conscious rat using cephalexin as test drug.

A new method has been developed for simultaneous evaluation of local absorption from the intestine into the portal system and local disposition through the liver, and for assessment of the bioavailability of a drug in a single conscious rat. The method is based on the difference between plasma concentrations in portal and systemic blood (PS method). Because cephalexin is known to be absorbed completely from the intestine and not to be eliminated through the liver, it was used as test drug to confirm the validity of the new method. The portal vein and the femoral artery of a rat were simultaneously cannulated and blood samples were obtained from both sites. Two methods of administration, single-dosing and double-dosing, were investigated and the efficacy of double-dosing (DD) was demonstrated. Rats received an intra-arterial (group A) or oral (group B) dose in single-dosing, whereas rats used for double-dosing received an oral dose 3 h after an intra-arterial dose (group C). After administration of cephalexin, the portal and arterial plasma concentrations were determined by HPLC. Groups A and B were monitored for 4 h and group C for 8 h. The portal-blood flow rate was measured by means of an electromagnetic flow-meter. Global and local moments were calculated by trapezoidal integration with extrapolation to infinite time. On the basis of the PS method, the local absorption ratio (Fa) and the mean local absorption time (t(a)) were estimated to be 0.975 +/- 0.104 and 2.19 +/- 0.51 h, respectively, in group B. By comparing the averaged moments between groups A and B, the extent of bioavailability (F), the mean absorption time (MAT) and the hepatic recovery ratio (FH) were calculated to be 1.01, 1.92 h and 1.04, respectively. The mean hepatic transit time (tH) was negligible. In group C, Fa = 0.936 +/- 0.107, tH = 1.55 +/- 0.32 h, F = 1.08 +/- 0.07, MAT = 1.55 +/- 0.40 h and F(H) = 1.17 +/- 0.14 h, the mean values being close to those from groups A and B. In conclusion, the PS method with short-period double-dosing (PS-DD method) can offer an effective means of evaluating the local absorption kinetics of drugs, because F, MAT and F(H) are obtained from a single conscious rat, and consequently the standard deviations of the quantities can be quickly estimated.

Administration, Oral↗
PubMed1977

Comparison of in vitro activity of cephalexin, cephradine, and cefaclor.

Inhibitory activity of cephalexin, cephradine, and cefaclor was compared by the WHO-ICS agar dilution technique. Cefaclor was substantially more active against staphylococci, streptococci, gonococci, meningococci, Haemophilus, Escherichia coli, Klebsiella pneumoniae, Citrobacter diversus, Proteus mirabilis, salmonellae, and shigellae than was cephalexin, which in turn was more active than cephradine. Cefaclor appeared to be less resistant to staphylococcal penicillinase than did the other two agents. None of these cephalosporins was active against Enterobacter, Serratia, indole-positive Proteeae, Pseudomonas, or Bacteroides fragilis.

Bacteroides↗
PubMed1977

In vitro susceptibility studies with cefaclor and cephalexin.

The in vitro activity of cefaclor and cephalexin against clinical isolates of four bacterial genera was compared. Both agents had a similar range of activity, but cefaclor was significantly more active by weight than cephalexin for most isolates tested.

Bacteria↗
PubMed1980

Pharmacokinetics of alafosfalin, alone and in combination with cephalexin, in humans.

Alafosfalin is a phosphonodipeptide with significant activity as an antibacterial agent and as a potentiator of beta-lactam antibiotics. Studies in humans showed that oral doses of 50 to 2,500 mg were well absorbed, but some metabolic hydrolysis occurred before the drug reached the general circulation. Oral bioavailability was approximately 50% and was largely independent of dose. Alafosfalin has an elimination half-life of about 60 min and does not accumulate during chronic administration. Healthy volunteers excreted intact phosphonodipeptide in the urine. The recovery was dose dependent and increase from 6 +/- 1% after 50-mg doses to 17 +/- 1% after 2,500-mg doses. This change with dose occurred because the human kidney has a small, saturable capacity for reabsorbing the phosphonopeptide. Less alafosfalin was excreted in the urine of subjects with impaired glomerular function. When alafosfalin was coadministered with cephalexin, both compounds wer absorbed, distributed, and eliminated at virtually identical rates. Oral administration of 500 mg of the phosphonodipeptide plus 250 mg of the beta-lactam antibiotic gave approximately equal concentrations of the drugs in plasma, with a fourfold excess of cephalexin in the urine. This 2:1 combination is being tested in the clinic.

Alanine↗
PubMed1980

Pharmacokinetic comparison of cefroxadin (CGP 9000) and cephalexin by simultaneous administration to humans.

The pharmacokinetic parameters of cefroxadin and cephalexin were compared after simultaneous oral administration of the two cephalosporins to 21 subjects. The influence of the dose, the formulation, and food intake on these parameters was investigated. Both drugs were equally well absorbed from all of the tested formulations; identical percentages of the dose were recovered in the urine in all cases. The elimination half-life of cefroxadin and, consequently, the area under the plasma concentration-time curve were about 10% less than those of cephalexin. Plasma concentrations and cumulative excretion curves of the two drugs were almost superimposable. Food intake had the same effect on both drugs; absorption was slowed, but the amounts absorbed were almost the same as those in fasted subjects.

Adult↗