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PubMed1984

Three-day therapy with cephalexin for lower urinary tract infections in children.

In a prospective study of children with an acute infection of the lower urinary tract, the effectiveness of a 3-day course of cephalexin, 25-50 mg/kg body weight and day was compared with that of a 10-day course of nitrofurantoin, 3-4 mg/kg/day. 19 children were allotted to treatment with cephalexin and 24 were treated with nitrofurantoin. The immediate cure rates were 90% and 96%, respectively. Two relapses were noted in the cephalexin group and 1 in the nitrofurantoin group. During a mean follow-up period of 7-8 months 2 of the cephalexin treated patients and 4 patients treated with nitrofurantoin had a reinfection. No side effects were noted in either of the treatment groups. The results suggest that treatment with cephalexin for 3 days is a reasonable alternative in children with an acute lower urinary tract infection when commonly used medications for one reason or another are less well tolerated.

Adolescent↗
PubMedDate not supplied

[Pharmacokinetics of cephalexin from two oral formulations in dogs].

Six beagle dogs were treated with cephalexin-monohydrate from 2 oral formulations (Rilexine tablets and Cefaseptin dragees, respectively) in a dosage of 25 mg/kg and plasma concentrations of cephalexin were measured over 8 hours. After solid phase extraction of the samples, cephalexin was determined by high pressure liquid chromatography with UV detection. After administration, Cephalexin was absorbed rapidly and mean maximum plasma concentrations of 30.9 and 27.9 micrograms/ml, respectively, were acquired after approximately 1.6 hours. Minimal inhibitory concentrations of < or = 6.25 micrograms/ml for in vitro sensitive bacteria were maintained for about 5 hours. Cephalexin from the tested preparations reached a mean area under the plasma concentration-time curve of 115.3 and 102.4 micrograms.h/ml, respectively. The plasma concentration decreased rapidly with a mean half life period of 1.4 hours in average. The other calculated pharmacokinetic parameters were also in the area of the data for dogs stated in the literature. There was no clear difference in the pharmacokinetics of both products, especially the bioavailability. Furthermore, both formulations were well tolerated clinically.

Administration, Oral↗
PubMedDate not supplied

[Means of purification of cephalexin with a view to therapeutic use].

Cephalexin (CEX) is the generic word of chemical compound 7-(D-alpha-aminophenylacetamido)-3-methyl-3-cephem-4-carboxylic acid, which is part of first generation oral cephalosporins group. It is use as cephalexin monohydrochloride monohydrate (CEX.HCl.H2O) syrup or tablets for oral administration. For obtaining a compound with great solubility and osmotic pressure, which is ideal for pharmaceutical forms with controlled dosage, it is necessary to achieve the crystalline form of Cephalexin monohydrochloride monohydrate. The therapeutic use Cephalexin has an output over 95 %, so it is necessary to purify CEX depending on it's isoelectric pH (pKa), which is 4.2. A good purification took place at greater or less values of pH, then the isoelectric pH value of CEX. The purification of CEX at greater values of pH then isoelectric point, took place with a greater output (75-76%), and the obtaining Cephalexin is much pure (97-98%).

Administration, Oral↗
PubMed1978

[Clinical experience with sustained release cephalexin (S-6437) in pediatrics (author's transl)].

S-6437 (Sustained release cephalexin granule for pediatric use) was studied with the following results: 1) Following the single oral administration of 25 mg/kg of S-6437 in 6 children 4 approximately 6 years old, the following blood levels (average) of cephalexin were obtained: 3.1 microgram/ml in one hour after the administration, 8.6 microgram/ml in 2 hours, 8.7 in 4 hours, 7.2 in 6 hours, 4.0 in 8 hours and 1.2 in 12 hours. Effective blood levels of cephalexin by S-6437 were maintained for longer period of time than those by regular cephalexine dry syrup. In 4 of 6 children receiving S-6437, cephalexin was scarcely detected in their blood in 12 hours after the administration. From this, it is not considered that S-6437 is accumulated in body. 2) S-6437 was administered to 38 patients including: 7 with pneumonia, 7 with acute bronchitis, 1 with suppurative lymphadenitis, 4 with acute pharyngitis, 15 with acute tonsillitis and 4 with acute urinary tract infections. Out of the 35 cases, 31 (88.6%) responded to S-6437, and 3 cases could not be evaluated. 3) Transient diarrhea in 2 patients, rash in 1 and elevation of serum GOT, GPT and LDH in 1 were observed. However, these side effects were improved by discontinuation of S-6437.

Age Factors↗
PubMed1981

Pharmacokinetics of cephalothin and cephalexin in selected avian species.

Plasma concentrations and the biological half-lives of cephalothin and cephalexin in avian species of a variety of body sizes and metabolic rates were studied. The species chosen were eastern bobwhite quail (Colinus v virginianus), pigeons (Columba livia), hybrid rosybill ducks (Netta sp), greater sandhill cranes (Grus canadensis tabida), and emus (Dromiceius novaehollandiae). In the 1st phase of the study, cephalothin sodium was given IM in a dose of 100 mg/kg of body weight. Plasma concentrations reached peak (av 18 micrograms/ml) at 0.5 hour and were measurable 2.5 to 5.5 hours after drug administration. The biological half-life of cephalothin was 16 to 54 minutes; the half-life varied directly with increased species body weight, with the exception of the ducks studied. In the 2nd phase, cephalexin monohydrate was given orally in doses of 25, 35, and 50 mg/kg of body weight. Plasma concentrations reached peak (av 20 micrograms/ml) at 0.5 to 1 hour and were measurable 2.5 to 5.5 hours after drug administration. The biological half-life of cephalexin was 36 to 126 minutes. In the 3rd phase, differences in plasma concentrations and the half-lives of cephalexin between fed quail and fasted quail were insignificant. Dosage regimens for cephalothin of 100 mg/kg 4 times a day and for cephalexin of 35 to 50 mg/kg 4 times a day would be expected to establish and maintain therapeutic plasma concentrations in large birds (pigeons, cranes, and emus). These same doses, administered every 2 to 3 hours, would be expected to establish and maintain therapeutic plasma concentrations in smaller birds (quail, ducks).

Animals↗
PubMed1976

Cephalexin compared to ampicillin treatment of otitis media.

Cephalexin was compared to ampicillin for the treatment of otitis media in a randomized study. Bacteriologic diagnosis was sought by needle tympanocentesis in 179 children. No overall statistically significant differences were noted between the two groups; however, 20 patients who received cephalexin had a poor response to therapy whereas only five recipients of ampicillin responded poorly. A significant difference (P less than .05) between the two regimens was noted when Hemophilus influenzae was recovered. Fifty per cent of the children with H. influenzae otitis media who were treated with cephalexin responded poorly; no patients receiving ampicillin had a poor response. Our data suggest that the use of cephalexin monohydrate is not warranted for treatment of otitis media due to H. influenzae even when the isolate proves sensitive to this drug in vitro. In selected patients with otitis media caused by Staphylococcus aureus which is resistant to penicillin, cephalexin may provide effective treatment.

Ampicillin↗
PubMed1967

Cephalexin, a new orally absorbed cephalosporin antibiotic.

A new antibiotic, structurally related to cephaloglycin, has been assigned the generic name cephalexin, 7-(D-alpha-amino-alpha-phenylacetamido)-3-methyl-3-cephem-5-carboxylic acid. In vitro antimicrobial activity of cephalexin does not equal that of cephaloglycin. However, excellent oral absorption and lack of serum binding of cephalexin compensates significantly for the lower in vitro activity. Exceptional efficacy against experimental bacterial infections in mice was obtained with cephalexin therapy as compared with cephaloglycin, tetracycline, and chloramphenicol. The data suggest that cephalexin merits clinical trial.

Alcaligenes↗
PubMed1970

Comparison of cephalexin, penicillin V, and ampicillin in streptococcal infections in monkeys.

Intravenous inoculation of a group A hemolytic streptococcus caused lethal infections in all of 11 untreated monkeys. Daily intragastric administration of either 25 or 50 mg per kg per day, given in two equal morning and afternoon doses, yielded similar results in monkeys treated with cephalexin, penicillin V, and ampicillin; all eight monkeys in each therapy group survived. At dose levels of 12.5 mg per kg per day, six of eight, four of eight, and one of eight receiving cephalexin, penicillin V, and ampicillin, respectively, died. The differences observed at the lower dose level between cephalexin and ampicillin could be attributed, in part, to differences in the minimal inhibitory concentrations (MIC) of cephalexin (MIC = 0.24 mug/ml) and ampicillin (MIC = 0.01 mug/ml). The differences in results between penicillin V, which had the same MIC as ampicillin, could perhaps be attributed, in part, to shorter duration of antibacterial activity and higher protein binding of penicillin V. These studies support previous observations that cephalexin at 25 to 50 mg/kg doses is effective in severe streptococcal sepsis in monkeys.

Administration, Oral↗
PubMed2001

Modeling of the enzymatic kinetic synthesis of cephalexin--influence of substrate concentration and temperature.

During enzymatic kinetic synthesis of cephalexin, an activated phenylglycine derivative (phenylglycine amide or phenylglycine methyl ester) is coupled to the nucleus 7-aminodeacetoxycephalosporanic acid (7-ADCA). Simultaneously, hydrolysis of phenylglycine amide and hydrolysis of cephalexin take place. This results in a temporary high-product concentration that is subsequently consumed by the enzyme. To optimize productivity, it is necessary to develop models that predict the course of the reaction. Such models are known from literature but these are only applicable for a limited range of experimental conditions. In this article a model is presented that is valid for a wide range of substrate concentrations (0-490 mM for phenylglycine amide and 0-300 mM for 7-ADCA) and temperatures (273-298 K). The model was built in a systematic way with parameters that were, for an important part, calculated from independent experiments. With the constants used in the model not only the synthesis reaction but also phenylglycine amide hydrolysis and cephalexin hydrolysis could be described accurately. In contrast to the models described in literature, only a limited number (five) of constants was required to describe the reaction at a certain temperature. For the temperature dependency of the constants, the Arrhenius equation was applied, with the constants at 293 K as references. Again, independent experiments were used, which resulted in a model with high statistic reliability for the entire temperature range. Low temperatures were found beneficial for the process because more cephalexin and less phenylglycine is formed. The model was used to optimize the reaction conditions using criteria such as the yield on 7-ADCA or on activated phenylglycine. Depending on the weight of the criteria, either a high initial phenylglycine amide concentration (yield on 7-ADCA) or a high initial 7-ADCA concentration (yield on phenylglycine amide) is beneficial.

Cephalexin↗
PubMed1978

Quantitative determination of cephalexin in cephradine by NMR spectroscopy.

An NMR method to determine quantitatively the presence of cephalexin in cephradine was developed. The method is applicable to the chemical itself as well as to capsules and oral suspension formulations. The determination is based on the NMR signal arising from the five aromatic protons of the cephalexin molecule. Integration of this signal relative to a signal from cephradine provides the data necessary to determine the percentage of cephalexin present. The precision at the 2% cephalexin levels is +/- 0.18%. The time required to carry out a single analysis is about 10 min, and five analyses can be done in about 0.5 hr.

Capsules↗
PubMed1979

[Aqueous-and serum levels of cephalexin and penicillin V after oral application in man (author's transl)].

This clinical study implies orally administered cephalexin and penicillin V as agents with effective aqueous homor penetration in noninfected human eyes. Aqueous humor concentration of cephalexin increases up to 15% of the serum level 2 h after application. Administration of 1 g or 2 g cephalexin revealed no significant difference in aqueous humor concentration. So penetration of blood-aqueous-humor barrier can be regarded as a saturation process. Individual results of 92 cephalexin determinations are variant and not related to body weight or age of the patients.

Aged↗
PubMed1979

[Subinhibitory activity of cefaclor and cephalexin (author's transl)].

The determination of the minimal inhibitory concentration (MIC), which is usually performed after 18 to 24 hours of incubation, results in the case of cefaclor in a false picture of the actual activity. Cefaclor is chemically so unstable that after 24 hours only 2-5% of the substance is microbiologically active. In order to compare the activity of cefaclor and cephalexin, the effect of subinhibitory concentrations of both antibiotics against Escherichia coli and Klebsiella pneumoniae strains was studied by means of turbidimetry. After eight hours the absolute inhibitory concentration of cefaclor was lower than that of cephalexin with both methods. At the same time the effect of subinhibitory concentrations of both antibiotics was equal. Automatic measurement over 20 hours showed at the end of the experiment a higher MIC, and also a higher subinhibitory range, for cefaclor than for cephalexin. In our opinion the absolute inhibitory concentration after eight hours should be the criterion used to evaluate the effectiveness of cefaclor and cephalexin, and not the MIC which is usually used. The eight-hour criterion should also be applied in clinical use.

Cefaclor↗
PubMed1984

Carrier-mediated transport of cephalexin via the dipeptide transport system in rat renal brush-border membrane vesicles.

Carrier-mediated transport of aminocephalosporin antibiotics by renal brush-border membrane vesicles has been studied in relation to the transport systems for dipeptides and amino acids. Dipeptides such as L-carnosine (beta-alanyl-L-histidine) and L-phenylalanylglycine competitively inhibited the uptake of cephalexin, but amino acids did not. Cephalexin uptake was stimulated by the countertransport effect of L-carnosine in the normal and papain-treated vesicles, and by the effect of L-phenylalanylglycine only in the papain-treated vesicles. In the papain-treated vesicles, the hydrolysis of dipeptides was markedly decreased, and the specific activity for cephalexin transport was increased approx. 2-fold because of the partial removal of membrane proteins. These results suggest that carrier-mediated transport of cephalexin can be transported by the system for dipeptides in renal brush-border membranes.

Amino Acids↗
PubMed1992

Cefaclor uptake by the proton-dependent dipeptide transport carrier of human intestinal Caco-2 cells and comparison to cephalexin uptake.

The human Caco-2 cell line spontaneously differentiates in culture to epithelial cells possessing intestinal enterocytic-like properties. These cells possess a proton-dependent dipeptide transport carrier that mediates the uptake of the cephalosporin antibiotic cephalexin (Dantzig, A.H. and Bergin, L. (1990) Biochim. Biophys. Acta 1027, 211-217). In the present study, the uptake of cefaclor was examined and found to be sodium-independent, proton-dependent, and energy-dependent. The initial rate of D-[3-phenyl-3H]cefaclor uptake was measured over a wide concentration range; uptake was mediated by a single saturable transport carrier with a Km of 7.6 mM and a Vmax of 7.6 nmol/min per mg protein and by a non-saturable component. Uptake was inhibited by dipeptides but not amino acids. The carrier showed a preference for the L-isomer. The effect of the presence of a 5-fold excess of other beta-lactam antibiotics was examined on the initial rates of 1 mM cefaclor and 1 mM cephalexin uptake. Uptake rates were inhibited by the orally absorbed antibiotics, cefadroxil, cefaclor, loracarbef, and cephradine and less so by the parenteral agents tested. The initial uptake rates of both D-[9-14C]cephalexin and D-[3-phenyl-3H]cefaclor were competitively inhibited by cephalexin, cefaclor, and loracarbef with Ki values of 9.2-13.2, 10.7-6.2, and 7.7-6.4 mM, respectively. Taken together, these data suggest that a single proton-dependent dipeptide transport carrier mediates the uptake of these orally absorbed antibiotics into Caco-2 cells, and provide further support for the use of Caco-2 cells as a cellular model for the study of the intestinal proton-dependent dipeptide transporter.

2,4-Dinitrophenol↗
PubMed1976

Cefazolin and cephalexin levels in prostatic tissue and sera.

A study was carried out on 18 patients given cefazolin intramuscularly and 17 patients given cephalexin by mouth preoperatively prior to transurethral resection of the prostate. Prostatic tissue and serum levels of the two drugs were determined and contrasted with previously reported mean inhibitory concentrations. It was found that cefazolin was present in the sera and prostatic tissues in levels greater than was cephalexin and that cefazolin frequently exceeded the minimum inhibitory concentrations necessary for sensitive organisms to be affected, whereas cephalexin did not. Therefore, it would appear that cefazolin would be preferable to cephalexin in treatment of acute bacterial prostatitis.

Biological Availability↗
PubMed1988

Analysis of cephalexin from canine skin biopsy by liquid chromatography with ultraviolet-visible photodiode-array detection.

A sensitive and selective ion-paired liquid chromatographic method with UV-VIS photodiode-array detection was developed to measure cephalexin in skin biopsy samples. The method involved a sonication of minced canine skin with ethanol-acetonitrile-water (30:20:50, v/v/v) and ultrafiltration of received extract through 10,000 daltons. Separation of cephalexin from other components was by liquid chromatography using a reversed-phase column which was eluted with an ion-paired acetonitrile-water solution. Detection was achieved with a UV-VIS photodiode-array detector scanning from 230 to 320 nm. Cephalexin in the eluate was quantitated at its wavelength maximum of 260 nm. The evaluation of chromatographic peak homogeneity was performed by absorbance ratios, contour maps, first-derivative spectra and a three-dimensional spectrochromatogram. Additionally, the cephalexin peak identity was confirmed by liquid chromatography-mass spectrometry.

Cephalexin↗
PubMed1985

Effect of prophylactic, low dose cephalexin on fecal and vaginal bacteria.

Effective prophylactic antimicrobial therapy for recurrent urinary tract infections depends upon the creation of minimal antimicrobial resistance in the fecal and vaginal flora. Cephalexin is known to be useful for prophylaxis clinically but substantial resistance has been reported in vaginal and rectal Escherichia coli at doses of 2 gm. per day. The effect of 250 mg. cephalexin nightly was studied in 23 women with recurrent bacteriuria who were treated for 6 months. Of the 23 patients 22 remained free of infection for 132 months of observation. Despite heavy carriage of Escherichia coli in the rectal and vaginal reservoirs during therapy, Escherichia coli resistant to 32 micrograms per ml. cephalexin did not occur. These observations explain the prophylactic effectiveness of cephalexin when used in small amounts of single nightly dosages.

Adult↗
PubMed1983

Treatment of staphylococcal skin infections: a comparison of cephalexin and dicloxacillin.

Cephalexin, given twice daily, and dicloxacillin, given four times daily, were compared in a randomly controlled study for the treatment of staphylococcal skin and skin structure infections. Among 70 evaluable patients, 57 had staphylococcal bullous impetigo. The remaining 13 patients had bullous impetigo with streptococcal or mixed streptococcal-staphylococcal cultures (6 patients), abscess (4 patients), or cellulitis with pyoderma (3 patients). Staphylococci were recovered from lesions of 64 of the 70 evaluable patients; all strains were sensitive to both cephalexin and dicloxacillin, but only 2 of the 64 strains were susceptible to penicillin G. Cephalexin and dicloxacillin proved equally effective. Treatment failures were uncommon (1 patient in each group), and recurrences (3 patients in each group) were limited to patients with bullous impetigo. In general, patients with staphylococcal bullous impetigo responded promptly, with clearing of lesions evident within the first week, but delayed healing with persistence of staphylococci in lesions was more common in the group receiving dicloxacillin. Twice-daily dosing with oral antibiotics is obviously convenient and may enhance compliance. Twice-daily therapy with cephalexin for staphylococcal skin and skin structure infections can be recommended with confidence.

Abscess↗