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PubMed1986

Cefadroxil. A review of its antibacterial, pharmacokinetic and therapeutic properties in comparison with cephalexin and cephradine.

Cefadroxil is an oral cephalosporin which is similar to cephalexin and cephradine in structure and spectrum of antibacterial activity, but has different pharmacokinetic properties. Not only does cefadroxil exhibit a longer serum half-life, and thus a prolonged duration of activity, but it is virtually unaffected by simultaneous food intake. The concentrations of cefadroxil attained in body tissues and fluids are also higher and more sustained than those of cephalexin and cephradine. These characteristics permit the administration of cefadroxil during meals on a once-daily or twice-daily basis, thus encouraging patient compliance which often determines the successful management of out-patient infections. Many studies have established the efficacy of the administration of once- or twice-daily cefadroxil, compared with regimens of cephalexin or cephradine given 4 times daily, in the management of infections in the respiratory tract, urinary tract, skin and soft tissues, and bones and joints.

Cefadroxil↗

PubMed2006

Effects of doxycycline, amoxicillin, cephalexin, and enrofloxacin on hemostasis in healthy dogs.

OBJECTIVE: To determine the effects of enteral administration of doxycycline, amoxicillin, cephalexin, and enrofloxacin at therapeutic dosages for a typical duration on hemostatic variables in healthy dogs. ANIMALS: 14 Beagles. PROCEDURE: Doxycycline (10 mg/kg, PO, q 12 h), amoxicillin (30 mg/kg, PO, q 12 h), cephalexin (30 mg/kg, PO, q 12 h), and enrofloxacin (20 mg/kg, PO, q 24 h) were administered in random order to 10 healthy dogs at standard therapeutic dosages for 7 days, with a 7-day washout period between subsequent antimicrobials. In addition, 4 Beagles served as control dogs. Variables were evaluated before and after antimicrobial administration; they included platelet count, Hct, 1-stage prothrombin time (PT), activated partial thromboplastin time (PTT), fibrinogen concentration, and platelet function. Platelet function was assessed via buccal mucosal bleeding time, aggregation, and a platelet-function analyzer. RESULTS: Administration of all antimicrobials caused a slight prolongation of 1-stage PT and activated PTT and slight decrease in fibrinogen concentration. Cephalexin caused a significant increase in 1-stage PT and activated PTT, amoxicillin caused a significant increase in activated PTT, and enrofloxacin caused a significant decrease in fibrinogen concentration. Platelet count or function did not differ significantly after administration of any antimicrobial. CONCLUSIONS AND CLINICAL RELEVANCE: Oral administration of commonly used antimicrobials in healthy dogs resulted in minor secondary hemostatic abnormalities, with no change in platelet count or function. Although these changes were clinically irrelevant in healthy dogs, additional studies of the effects of antimicrobial administration on hemostasis in animals with underlying disease processes are warranted.

Amoxicillin↗

PubMed1978

High speed liquid chromatographic determination of cephalexin in human plasma and urine.

A rapid and accurate high speed liquid chromatographic method has been developed for the determination of cephalexin in human plasma and urine. The method involves micropore filtration of urine specimens and methanol extraction of plasma samples followed by HSLC separation on a bonded reverse phase column utilizing a mobile phase of methanol-water containing acetic acid. The quantitativity of UV response at 254 nm covered a wide range of cephalexin concentrations down to 0.5 microgram/ml, and no metabolite peaks were detected. The time courses of plasma level and urinary excretion were determined until 6 hours after oral administration of cephalexin capsules to healthy volunteers. The pharmacokinetic parameters were estimated using a two compartment open model.

Cephalexin↗

PubMed2004

[Immunomodulating, antioxidant and hepatoprotective effects of immobilized dosage forms of rifampicin and cephalexin].

The aim of the study was to lower the immunosuppressory, prooxidant and hepatotoxic effects of rifampicin and cephalexin by their immobilization in erythrocyte vehicles. The experiments were performed on Wistar rats with the use of rifampicin, cephalexin and lysozyme (ZAO Ferane) and hemodes (6% aqueous saline solution of low molecular polyvinylpyrrolidone, mol. wt. 12600+/-2700). Rifampicin- and cephalexin-entrapped erythrocytes were prepared. Spectrophotometric procedures for quantitative assay of the immobilized antibiotics were developed. The impact of the solution concentration and incubation time on the level of the antibiotic entrapping was studied. The erythrocyte vehicles were shown to be able to entrap the antibiotics for 9 days and to preserve their stability for 24 hours. It was observed that the increase of the immunosuppressory, prooxidant and hepatotoxic effects of the antibiotics administered without the vehicles to the laboratory animals infected by staphylococci was dose-dependent. The use of the antibiotics entrapped in the erythrocyte vehicles stimulated the immune reactivity of the animals and normalized the indices of lipid peroxidation, the antioxidant system, cytolysis and cholestasis.

Adjuvants, Immunologic↗

PubMed1997

[Separation of drugs cephalexin, ampicillin, and their biosynthetic precursors L-Phe-L-Cys-D-Val and D-Phe-L-Cys-D-Val by capillary zone electrophoresis].

The separation of drugs cephalexin, ampicillin and their biosynthetic precursors L-Phe-L-Cys-D-Val and D-Phe-L-Cys-D-Val was investigated by using capillary zone electrophoresis in acidic Tris-H3PO4 buffer at pH 2.3. With 50 mmol/L Tris-H3PO4 (pH 2.3) buffer, L-Phe-L-Cys-D-Val and D-Phe-L-Cys-D-Val were only partially separated whereas near baseline separation was achieved between cephalexin and ampicillin. The experiments showed that the addition of beta-type cyclodextrins (beta-CD) to the running buffer can influence the separation selectivity. When beta-CD was used as buffer additives at 12 mmol/L, the separation between L-Phe-L-Cys-D-Val and D-Phe-L-Cys-D-Val was much improved, however, the separation between cephalexin and ampicillin was impaired. When using 50 mmol/L Tris-H3PO4 containing 12 mmol/L DM-beta-CD (pH 2.3) buffer system, all compounds investigated were completely separated. This separation method is simple, fast and easy to operate. It involves only the conventional reagents with a much lower run cost than using HPLC. It is expected to be used in the synthetic process monitoring.

Ampicillin↗

PubMed1990

[Comparison of cefsulodin and cephalexin as selective agents in agar for Bordetella pertussis].

Cefsulodin (12 mg/l) was evaluated as an alternative to cephalexin (40 mg/l) as selective agent in agar for isolation of Bordetella pertussis from clinical specimens. Charcoal horse blood agar with cefsulodin and with cephalexin supported growth of Bordetella pertussis strains (n = 50) equally well. The nasopharyngeal flora of healthy adults (n = 49) was suppressed significantly better by cephalexin, but colony numbers of flora on the agar with cefsulodin in general were low.

Bordetella pertussis↗

PubMed1987

[Biopharmaceutical aspects of the medicinal forms of cephalexin].

The rate of cephalexin release from various dosage forms such as tablets, capsules and suspensions manufactured by several firms was studied. In vivo studies showed that pharmacokinetic indices of the absorption depended on the rate of cephalexin release from the dosage forms. The proposed procedure for in vitro estimation of the cephalexin release rate reflects bioavailability of the antibiotic dosage forms and may be used in quality control of finished dosage forms.

Animals↗

PubMed1978

Kinetics of degradation of cefazolin and cephalexin in aqueous solution.

The kinetics of degradation of cefazolin and cephalexin in aqueous solution were investigated at 60 degrees C and constant ionic strength over the entire pH range. The observed degradation rates were obtained by measuring the residual cephalosporin and were shown to follow pseudo-first-order-kinetics. They were influenced significantly by solvolytic and hydroxide ion catalysis. No primary salt effect was observed in the acid or basic pH region. Of the buffer systems employed in the kinetics studies only the phosphate buffer system showed a catalytic effect. The pH-rate profile for cefazolin showed a degradation minimum between pH 5.5 and 6.5. Cephalexin did not show a pH minimum in that region. The apparent energies of activation were determined for cefazolin and cephalexin at pH 5.5 and were calculated to be 24.3 Kcal/mole and 26.2 Kcal/mole, respectively. The agreement between the calculated theoretical pH-rate profiles and the experimental points for both compounds support the hypothesis presented concerning the reactions involved in their respective degradation pathways.

Buffers↗

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↗

PubMed1986

Effect of cephalexin and tetracycline on galactose absorption in rat small intestine.

The effects of cephalexin and tetracycline HCl on D-galactose absorption in rat small intestine were investigated. Both antibiotics inhibited D-galactose uptake into isolated intestinal mucosa in a dose-dependent fashion. In vivo studies showed that cephalexin and tetracycline HCl reduced D-galactose absorption and that the transport defect was not reversible on cessation of antibiotic perfusion. Both the active and passive components of D-glactose absorption were inhibited by the antibiotics tested. Furthermore, both drugs reduced mucosa O2 consumption and inhibited D-galactose absorption when they were perfused in a contiguous loop. We conclude that the diminished D-galactose transport by rat small intestine after tissue exposure to either cephalexin or tetracycline HCl appears to be in part due to an insufficient energy supply.

Animals↗

PubMed1977

[Cephalexin levels in the bronchial secretion of children (author's transl)].

Cephalexin serum levels and its content in bronchial secretions have been studied in six children with pneumonia or chronic bronchitis following a single oral doses of 30 to 50 mug/kg body weight. The cephalexin content in bronchial secretions reached values between 0,47 and 2,3 mug/ml (on average 0,84 mug/ml). The percentage of the cephalexin content in bronchial secretions varied from 4,3 to 133 percent (on average 22,6%) as compared to the corresponding serum levels.

Administration, Oral↗

PubMed1979

The pharmacokinetics of the oral cephalosporins cefaclor, cephradine and cephalexin.

The pharmacokinetics of the oral cephalosporins cefaclor, cephradine, and cephalexin were examined following single 500 mg oral doses to fasted, healthy volunteers. Absorption of the three compounds was rapid following a brief lag period and peak serum levels were obtained in 1-1.5 hours. Serum levels of cefaclor tended to be lower than those of cephradine and cephalexin during the 2-5 hour postdosing period and cefaclor was eliminated more rapidly than other cephalosporins from serum. No difference was observed in the overall bioavailability of the three antibiotics based on comparable FD/V values. Urine levels of the three cephalosporins greatly exceeded the minimum inhibitory concentrations of susceptible organisms during 0-6 hours postdosing, but were considerably reduced during the 6-12 hour collection period. Total urinary recovery of antibiotic activity accounted for almost 90 percent of dosed cephradine and cephalexin compared to 55 percent of dosed cefaclor. Lower serum levels and reduced urinary recovery of intact cefaclor are probably due primarily to its chemical instability. The reduced levels of cefaclor may be compensated for therapeutically by its greater in vitro antibacterial activity.

Adolescent↗

PubMed1977

[Clinical study of sustained release cephalexin (S-6435 and S-6436) in tonsillitis and pharyngitis (author's transl)].

Clinical study of sustained release cephalexin (S-6435 and S-6436) was conducted with the following results: 1) Pediatric patients with 1.5 approximately 12 years of age having acute tonsillitis and pharyngitis were orally administered 500 approximately 1,000 mg/day of S-6435 or S-6436 divided into 2 doses after breakfast and dinner. Out of 21 patients receiving the preparations, 19 patients satisfactorily responded to them and 2 fairly did. 2) In only one patient of the 21, rash was observed during the treatment. The side effect, however, disappeared 2 days after the initiation of the treatment, and was considered to be due to underlying disease of the patient. No other side effects were observed. Since it has become our concern to conduct injectable therapy in children, oral therapy should first be recommended to them. However, oral drugs, like a regular cephalexin, requiring q.i.d. regimen are inconvenient in giving the drugs to patients because they have to take the drugs once at midnight. S-6435 and S-6436, however, have no such disadvantages and prove to have as much effectiveness and safety as regular cephalexin has.

Acute Disease↗

PubMed1983

Cephalexin for oral treatment of canine urinary tract infection caused by Klebsiella pneumoniae.

Oral treatment with cephalexin resulted in bacteriologic cure in 24 of 25 (96%) dogs with urinary tract infection caused by Klebsiella pneumoniae. All 25 of the isolates of K pneumoniae were susceptible in vitro to cephalexin at a concentration of less than or equal to 64 micrograms/ml, well below the mean concentration of cephalexin attained in the urine of clinically normal dogs given similar doses of this drug.

Administration, Oral↗

PubMed1983

Cephalexin in lower respiratory tract infections.

Cephalexin has had 12 years of extensive clinical usage in the management of respiratory tract and other infections. It is reliably absorbed from the gastrointestinal tract and reaches therapeutic levels in serum and tissues. Toxicity and adverse side effects are minimal. The antimicrobial spectrum includes a majority of the pathogens usually associated with community-acquired lower respiratory tract infections with the significant exception of Haemophilus influenzae. Resistance of H. influenzae strains reduces the uses of cephalexin in the paediatric population and may limit its effectiveness in some patients with acute exacerbations of chronic bronchitis. In contrast, it is inordinately effective in managing most adult patients with lower respiratory tract infections, either as a primary agent, as a substitute for penicillins or other antimicrobial agents in patients unable to receive these, or for continuation of therapy in individuals who no longer require parenteral compounds. As with other cephalosporins, caution should be exercised to exclude meningitis when treating patients with respiratory tract infections since the majority of these compounds, including cephalexin, produce little or no cerebrospinal fluid levels.

Adult↗

PubMed1983

The role of cephalexin in the treatment of skin and soft-tissue infections.

Cephalexin remains an effective and highly useful antibiotic for the treatment of streptococcal and staphylococcal skin infections. Twelve years of experience have not diminished its efficacy, and cure rates of 90% or higher continue to be achieved. Its resistance to degradation by gastric acid and its uniform absorption ensure its bioavailability, and its efficacy in twice-daily dosages enhances medication compliance. The suspension formulation is well accepted by young children, and side effects have generally been mild and infrequent. Cephalexin is comparable to erythromycin, clindamycin, dicloxacillin, cloxacillin, and other cephalosporins in the treatment of streptococcal and staphylococcal infections. Because many of these antibiotics are similar in their efficacy, palatability, and adverse reactions, cost factors may play an important role in choosing one over the other. Penicillin remains the drug of choice for streptococcal skin infections. If the cure rates of the mixed streptococcal-staphylococcal lesions continue to decrease with penicillin, cephalexin and the other alternative antibiotics may assume a more important role in the primary treatment of these infections in the future.

Adolescent↗

PubMed1983

A review of the drug events reported by 12,917 patients treated with cephalexin.

This paper reviews the adverse events reported by 12,917 patients treated with cephalexin in formal clinical trials. Six percent of all patients reported adverse events, and in 3% the association with the drug was thought to be definite or probable. In the remaining 3%, the relationship was uncertain. The gastrointestinal system was most commonly involved, with diarrhoea being reported by 164 patients. Patients in the upper and lower age ranges reported more events than those in the middle range, and most events were reported 6-15 days after treatment started. Patients who received cephalexin 4 times a day reported more events than those who were treated twice daily. Four hundred and sixty-two patients had a known sensitivity to penicillin, and all except 21 of these were treated with cephalexin without developing a sensitivity reaction.

Adolescent↗

PubMed1978

[Bioavailability of new galenic preparations of cephalexin (author's transl)].

After the administration of 12.5 mg/kg Cephalexin as a single oral dose of Ospexin 250 and 375 sirup as well as Ospexin 500 Tbl. maximal plasma levels are reached in approximately 30 min. Within 6 hours the total administered amount of Cephalexin is excreted in biologically active form in the urine. The resorption is not influenced by food. The rapid and complete absorption shows that Cephalexin in this galenic form has an excellent bioavailability.

Administration, Oral↗