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PubMed2003

Combination effects of cephalexin and gentamicin on Edwardsiella tarda and Streptococcus iniae.

The objective of this study was to determine the in vitro activity of cephalexin-gentamicin combination by a microbroth chequerboard technique against clinical isolates of Edwardsiella tarda and Streptococcus iniae. Gentamicin was shown more susceptible than cephalexin against both bacteria. The effect of cephalexin-gentamicin combination against both bacteria represented additive interaction. The combination even showed synergic interaction (22%) against E. tarda, with a FIC index of <0.5 as a borderline. No antagonism for cephalexin-gentamicin combination was observed for any bacterial strain.

Animals↗
PubMed2000

Comparison of pivmecillinam and cephalexin in acute uncomplicated urinary tract infection.

The clinical and bacteriological efficacy of a 3-day course of pivmecillinam, 200 mg three times daily, was compared with that of a 7-day course of cephalexin, 250 mg four times daily, in 216 patients with a bacteriologically confirmed, acute, uncomplicated, urinary tract infection. Both treatments were similarly effective. Clinical cure or improvement was obtained in 95.3% of patients given pivmecillinam and in 93.6% of patients given cephalexin. Bacteriological success was achieved in 89.7 and 81.7% patients taking pivmecillinam or cephalexin, respectively. Eradication rates for Escherichia coli were 90.1% for pivmecillinam and 80.6% for cephalexin. Both treatments were well tolerated. This study has confirmed that a 3-day course of pivmecillinam is effective and well tolerated in uncomplicated cystitis.

Acute Disease↗
PubMed1984

Cephalexin for the oral treatment of CAPD peritonitis.

Sixteen episodes of peritonitis in 13 patients undergoing continuous ambulatory peritoneal dialysis (CAPD) were treated with oral cephalexin given at each 6-hourly dialysate exchange. Serial measurements of the antibiotic concentration in serum and dialysate were made in seven cases. Cephalexin levels increased rapidly and by 12 h exceeded 27 mg/l in serum and 20 mg/l in dialysate. Dialysate levels considerably exceeded the minimum bactericidal concentration for organisms considered cephalexin-sensitive and in patients with these the clinical response was usually good. Although dialysate concentrations sometimes reached the minimum inhibitory concentration for organisms considered cephalexin-resistant the clinical response in patients from whom resistant bacteria were cultured was unsatisfactory. Intra-peritoneal antibiotic administration would seem unnecessary in many CAPD patients with peritonitis.

Administration, Oral↗
PubMed1988

In-vitro activity of cefaclor, cephalexin and ampicillin against 2458 clinical isolates of Haemophilus influenzae.

The zone sizes and MICs of ampicillin, cefaclor and cephalexin were determined for 2458 clinical isolates of Haemophilus influenzae collected in 1986 during a national survey of the prevalence of resistance in this species. Cefaclor showed greater in-vitro activity than cephalexin against all isolates, with a modal MIC of 4 mg/l compared with 8 mg/l. MIC50 values for the 2201 ampicillin-sensitive and 157 beta-lactamase-positive resistant strains were similar for both cephalosporins (4 mg/l for cefaclor, and 8 mg/l for cephalexin). A further 100 strains with a reduced zone (less than 20 mm) to a 2 micrograms ampicillin disc showed a definite (MIC greater than or equal to 4 mg/l) or intermediate (MIC 1 or 2 mg/l) degree of intrinsic resistance to ampicillin. Both cephalosporins showed a marked and significant rise in MIC values for this group. Cefaclor is the more active agent against ampicillin-sensitive and beta-lactamase-positive H. influenzae but strains with an intrinsic mechanism of resistance to ampicillin are markedly less sensitive to both cefaclor and cephalexin.

Ampicillin↗
PubMed1985

Cephalexin in the treatment of acute and chronic maxillary sinusitis.

We evaluated the efficacy of cephalexin therapy in 104 patients with infectious maxillary sinusitis. Confirmation of diagnosis was made by x-ray film, antral puncture, and culture. Sixty-nine patients met all criteria for evaluation. The majority of patients received cephalexin, 1 gm/day in four divided doses for ten days, including the 48-hour period after the patient had become asymptomatic. Patients returned for observation one week and two weeks after initiating therapy. Satisfactory clinical results were obtained in 57 (83%). Results showed that cephalexin was effective in treating sinusitis and that adverse reactions were rare. Bacteriology results showed that many of the pathogens usually involved in infectious maxillary sinusitis were resistant to the recommended or frequently prescribed antibiotics. These same pathogens, however, did not show resistance to cephalexin.

Acute Disease↗
PubMed2005

Comparison of the clinical efficacy of oral terbinafine and ketoconazole combined with cephalexin in the treatment of Malassezia dermatitis in dogs--a pilot study.

The purpose of this randomized, single blinded clinical trial was to evaluate cytologically and clinically the efficacy of oral cephalexin alone and its combination with terbinafine or ketoconazole for the treatment of Malassezia dermatitis in dogs. Twenty-two client-owned dogs with Malassezia dermatitis completed the 3-week study. All received cephalexin (generic, 250 mg or 500 mg) at 22-30 mg kg(-1) twice daily. Eight dogs received terbinafine at 30 mg kg(-1) once daily and seven dogs received ketoconazole (generic, 200 mg) at 5-10 mg kg(-1) twice daily. The remaining seven dogs received cephalexin alone. At week 0 (visit 1) and week 3 (visit 2), mean yeast counts were determined from three affected areas using tape-strip cytology, a clinical index score (CIS) was assigned to the affected areas, and owners evaluated pruritus using a visual analogue scale. All groups showed reduction in mean yeast counts, CIS and pruritus. There was an 86.8%, 80.2% and 28.8% reduction in mean yeast counts from visit 1 to visit 2 for the terbinafine, ketoconazole and cephalexin-only groups, respectively. However, within treatment group comparisons a significant reduction in mean yeast count was only evident for the terbinafine (P < 0.002) and ketoconazole (P < 0.01) groups. Pruritus reduction was only significant for the terbinafine group. These preliminary results suggest that terbinafine should be further assessed for the treatment of canine Malassezia dermatitis.

Administration, Oral↗
PubMed1985

Amino acid substitutions that reduce the affinity of penicillin-binding protein 3 of Escherichia coli for cephalexin.

The location of amino acid substitutions that allow an enzyme to discriminate between the binding of its normal substrate and a substrate analogue may be used to identify regions of the polypeptide that fold to form the substrate binding site. We have isolated a large number of cephalexin-resistant mutants of Escherichia coli in which the resistance is due to the production of altered forms of penicillin-binding protein 3 that have reduced affinity for the antibiotic. Using three mutagens, and a variety of selection procedures, we obtained only five classes of mutants which could be distinguished by their patterns of cross-resistance to other beta-lactam antibiotics. The three classes of mutants that showed the highest levels of resistance to cephalexin were cross-resistant to several other cephalosporins but not to penicillins or to the monobactam, aztreonam. The penicillin-binding protein 3 gene from 46 independent mutants was cloned and sequenced. Each member of the five classes of cephalexin-resistant mutants had the same amino acid substitution in penicillin-binding protein 3. The mutants that showed the highest levels of resistance to cephalexin had alterations of either Thr-308 to Pro, Val-344 to Gly, or Asn-361 to Ser. The Thr-308 to Pro substitution had occurred within the beta-lactam-binding site since the adjacent residue (Ser-307) has been shown to be acylated by benzylpenicillin. The Asn-361 to Ser change occurred in a region that showed substantial similarity to regions in both penicillin-binding protein 1A and 1B and may also define a residue that is located within the beta-lactam-binding site in the three-dimensional structure of the enzyme.

Acyltransferases↗
PubMedDate not supplied

Retapamulin ointment twice daily for 5 days vs oral cephalexin twice daily for 10 days for empiric treatment of secondarily infected traumatic lesions of the skin.

INTRODUCTION: Retapamulin is a novel, topical antibacterial of the pleuromutilin class in development for the treatment of secondarily infected traumatic lesions of the skin. METHODS: The efficacy, safety, and tolerability of topical retapamulin ointment, 1% for 5 days twice daily was evaluated in 2 identical, randomized, double-blind, double-dummy, multicenter studies vs oral cephalexin, 500 mg twice daily for 10 days, in 1904 patients with secondarily infected traumatic lesions. RESULTS: Clinical success rates were 89.5% in protocol-adherent patients receiving retapamulin compared with 91.9% for cephalexin (treatment difference, -2.5% [95% confidence interval, -5.4% to 0.5%]). In patients with Staphylococcus aureus or Streptococcus pyogenes at baseline, clinical success was 89.2% (365/409) for retapamulin and 92.6% (63/68) for cephalexin. Safety and tolerability were similar between treatments. Noncompliance (defined as using or taking <80% of doses) was recorded in 8.0% (51/636) of patients taking cephalexin compared with 0.39% (5/1268) of patients receiving retapamulin. CONCLUSIONS: Retapamulin offers a novel, effective, and convenient topical treatment for secondarily infected traumatic lesions.

Administration, Oral↗
PubMed1978

Microcalorimetric study of the effects of cephalexin and cephaloridin on Escherichia coli and Staphylococcus aureus.

The kinetics of the antibacterial actions of cephalexin and cephaloridin against a strain of Escherichia coli and a strain of Staphylococcus aureus were studied by a flow microcalorimeter. The heat production was related to the number of viable organisms (CFU ml-1), the pH, the optical density of the culture medium (OD540), and the morphology of the antibiotic-exposed bacteria. No heat effects could be registered when the number of CFU was below 10(4) ml-1. The addition of cephalexin, 2.5 microgram ml-1 (5 x MIC), to cultures of S. aureus caused a decrease in the heat production which was only roughly correlated with the number of CFU ml-1. This was also the case when 9.0 microgram ml-1 (2 x MIC) of this drug were added to cultures of E. coli. Two to three hours after the drugs had been added, no heat effects could be registered for the following 6--8 hours, after which an increase in the heat production again occurred. The MIC and MBC of the organisms isolated during this late heat increase were 8--40 times higher than those of the parent test organisms. A direct relation between drug concentration and response, i.e. heat effects produced, was found when increasing concentrations of cephalexin, i.e. 1.0 up to 50 micrograms ml-1 (2--100 x MIC) were added in the logarithmic growth phase to cultures of S. aureus. In ampoule calorimetric experiments, E. coli was cultured in a non-aerated, sealed growth vessel in the presence of cephalexin or cephaloridin in concentrations corresponding to 1/2 x MIC. The thermograms did not differ in shape, although the heat effects occurred somewhat later in the culture containing cephaloridin.

Calorimetry↗
PubMed1977

Comparison of in vitro antibacterial activity of three oral cephalosporins: cefaclor, cephalexin, and cephradine.

Cefaclor, a new oral cephalosporin, was compared in vitro with cephalexin and cephradine against 233 organisms. Evaluations were performed in Mueller-Hinton and nutrient broth and agar using two inoculum sizes. In agar, cefaclor had greater antibacterial activity than either cephalexin or cephradine against isolates of Escherichia coli, Proteus mirabilis, Staphylococcus aureus, Klebsiella pneumoniae, and Salmonella typhi. All three drugs were relatively inactive against isolates of enterococci, Enterobacter species, and indole-positive Proteus. Cefaclor, however, did exhibit the greatest activity of the three antibiotics against these organisms. Although there was wide variability with respect to test parameters, the broth results generally paralleled the agar results. In nutrient broth a clear separation of the results with these three cephalosporins was seen with K. pneumoniae, E. coli, and S. typhi. Cefaclor was the most active, cephalexin had intermediate activity, and cephradine was the least active. From the data obtained in this in vitro study, it can be concluded that cefaclor, which has a substituted chloro group attached to the molecule, had increased antibacterial activity over cephalexin and cephradine. Comparative clinical trials with cefaclor will determine whether the differences outlined above are of clinical significance.

Cephalexin↗
PubMed1978

Pharmacokinetics of cefaclor and cephalexin: dosage nomograms for impaired renal function.

The pharmacokinetics of cefaclor and cephalexin were characterized in patients with creatinine clearances ranging from 0 to 147 ml/min. Each of 24 fasted subjects received a single 500-mg oral dose of cefaclor, and 13 of these subjects later received 500 mg of cephalexin. Serum and urine levels of the antibiotics were measured by bioassay. The serum half-lives were highly correlated with corrected creatinine clearance (cefaclor r = 0.92, cephalexin r = 0.94). Linear regression estimates of the half-life of cefaclor were 2.3 h in the anephric patient and 40 min in the patient with a corrected creatinine clearance of 100 ml/min. For cephalexin, corresponding half-lives were 15.4 h and 58 min. We present a dosage nomogram for calculating the appropriate adjustments to the loading dose based on patient weight and maintenence dose based on corrected creatinine clearance.

Adult↗
PubMed1979

Comparative pharmacokinetics of cephalexin, cefaclor, cefadroxil, and CGP 9000.

In a randomized crossover study, the pharmacokinetics of three new cephalosporin antibiotics, cefaclor, cefadroxil, and CGP 9000, in comparison to cephalexin, were determined after oral administration, by capsules, of 1,000 mg on an empty stomach in 12 normal subjects. Serum concentrations were measured during a period of 8 h, and urine recovery was measured during 24 h. The significant parameters of bioavailability of an orally administered substance were determined. The maximal serum concentrations (y(max)) for cephalexin, cefaclor, cefadroxil, and CGP 9000 (in milligrams per liter) were: 38.8 +/- 8.1; 34.6 +/- 7.8; 33.0 +/- 5.4; and 23.3 +/- 7.3, respectively. The areas under the curve (in hours x milligrams per liter) were: 93.0 +/- 14.8; 74.5 +/- 9.9; 70.1 +/- 9.0; and 108.5 +/- 18.4, respectively. In a further crossover study with six subjects, 1,000 mg of cephalexin and of cefadroxil were given during a standard breakfast. The y(max) of cephalexin decreased to 23.1 +/- 6.6 mg/liter, in contrast to cefadroxil, with an unchanged y(max) of 32.7 +/- 3.4 mg/liter.

Administration, Oral↗
PubMed1985

Comparative study of amoxicillin-clavulanic acid and cephalexin in the treatment of bacteriuria during pregnancy.

A comparative clinical trial of amoxicillin-clavulanic acid and cephalexin was carried out in 80 women with bacteriuria of pregnancy. Treatment was randomly allocated and consisted of either one tablet of amoxicillin plus clavulanic acid (250 and 125 mg, respectively) three times daily or cephalexin (250 mg) three times daily for 7 days. Overall bacteriological cure rates at 2 weeks were 77% in the amoxicillin-clavulanic acid group and 74% in the cephalexin group. At 6 weeks the respective rates were 76 and 60%. Twenty-five episodes of infection were with ampicillin-resistant strains; cure rates were 82% (2 weeks) and 80% (6 weeks) in the amoxicillin-clavulanic acid group and 85 and 64%, respectively, in the cephalexin group. Differences in cure rates were not statistically significant. No significant difference in the rate of side effects was found. In particular, no toxicity to the fetus was seen which could be ascribed to either drug. Amoxicillin-clavulanic acid would appear to be a safe and effective treatment for bacteriuria of pregnancy.

Amoxicillin↗
PubMed1974

Use of available dosage forms of cephalexin in clinical comparison with phenoxymethyl penicillin and benzathine penicillin in the treatment of streptococcal pharyngitis in children.

The effectiveness of cephalexin, an oral cephalosporin using a dosage equivalent to available capsular dosage forms, was studied in relation to the effectiveness of phenoxymethyl penicillin and benzathine penicillin in the treatment of 128 patients with beta-hemolytic streptococcal pharyngitis, all but six of whom had group A streptococci isolated from throat cultures. Approximately one-half, 66 patients, received cephalexin for 10 days; 34 patients received phenoxymethyl penicillin for 10 days; and 28 patients had a single injection of benzathine penicillin. There were four treatment failures determined bacteriologically post-therapy, two in the cephalexin treatment group and one each in the oral penicillin and intramuscular penicillin groups. Similar cure rates of 96.7, 97.1, and 96.4% were computed for the respective treatment regimens. Whereas intramuscular benzathine penicillin remains the regimen of choice in most instances, cephalexin appeared to be as effective as oral penicillin in the elimination of group A streptococci from the pharynx when oral treatment was desired for streptococcal pharyngitis.

Administration, Oral↗
PubMed1988

Pharmacokinetics of cephalexin in dogs and cats after oral, subcutaneous and intramuscular administration.

A three-way crossover study was carried out in 10 dogs and nine cats to establish the pharmacokinetic parameters of the semi-synthetic cephalosporin antibiotic, cephalexin sodium, when administered orally, subcutaneously or intramuscularly. Ten dogs received a subcutaneous or intramuscular injection of 10 mg/kg bodyweight cephalexin or an oral dose of three 50 mg cephalexin tablets; the peak serum concentrations achieved were 24.9, 31.9 and 18.6 micrograms/ml, respectively, and the times taken to reach these peak levels were 1.2, 0.9 and 1.8 hours. Nine cats received either a subcutaneous or intramuscular dose of 0.25 ml cephalexin suspension (approximately 20 mg/kg bodyweight) or an oral dose of one 50 mg tablet; the peak serum concentrations achieved were 54.0, 61.8 and 18.7 micrograms/ml for the subcutaneous, intramuscular and oral administrations respectively, with times to peak concentrations of 1.1, 0.7 and 2.6 hours.

Administration, Oral↗
PubMed2006

Effects of progesterone and norethisterone on cephalexin transport and peptide transporter PEPT1 expression in human intestinal cell line Caco-2.

We investigated the effects of progesterone and norethisterone on the apical-to-basolateral and basolateral-to-apical transports of cephalexin, a typical peptide transporter PEPT1 substrate, and the PEPT1 mRNA and protein expression levels, using the human intestinal cell line, Caco-2. Caco-2 cell monolayers (passages 50 to 60) were cultured on permeable membrane, plastic culture dish and culture tube. The Caco-2 cell monolayers were pretreated with progesterone and norethisterone (3, 10, 30 microM) for 24 h. After the pretreatment, the apical-to-basolateral and basolateral-to-apical transports of cephalexin were measured, and the densities of PEPT1 mRNA and protein expression levels were analyzed by reverse transcription-polymerase chain reaction (RT-PCR) and Western blot, respectively. The apical-to-basolateral transport of cephalexin was significantly decreased by the progesterone and norethisterone (30 microM each) pretreatments. By contrast, the basolateral-to-apical transport of cephalexin was not altered by the same pretreatments. The densities of PEPT1 mRNA and protein expressions were significantly decreased by progesterone and norethisterone (each at 3 and 10 microM) pretreatments compared with those of the non-treated Caco-2 cells. The results suggest that the transcription of the PEPT1 gene is downregulated by the progesterone and norethisterone pretreatments. Further studies are needed to clarify whether the inhibition of the PEPT1 gene transcription by progesterone pretreatment proceeds via sigma1-receptor or progesterone receptor.

Biological Transport, Active↗
PubMed2005

Purification and characterization of inducible cephalexin synthesizing enzyme in Gluconobacter oxydans.

Cephalexin synthesizing enzyme (CSE) of Gluconobacter oxydans ATCC 9324 was purified up to about 940-fold at a yield of 12%. CSE biosynthesis in G. oxydans was found inducible in the presence of D-phenylglycine but not its substrate phenylglycine methyl ester. The purified enzyme was shown homogeneous on SDS-PAGE and exhibited a specific activity of 440 U per mg protein. The apparent molecular mass of the native enzyme was estimated to be 70 kDa over a Superdex 200 gel filtration column and 68 kDa on SDS-PAGE, indicating that the native enzyme is a monomer. Its isoelectric focusing point is 7.1, indicating a neutral character. The enzyme had maximal activity around pH 6.0 to 6.5, and this activity was thermally stable up to 40 degrees C. Synthesis of cephalexin from D-phenylglycine methyl ester and 7-amino-3-deacetoxycephalosporanic acid (7-ADCA) by the purified CSE was demonstrated. Its L-enantiomer was not accepted by CSE. Apart from cephalexin, ampicillin was also synthesized by the purified CSE from its acyl precursors and 6-aminopenicillanic acid (6-APA). Substrate specificity studies indicated that the enzyme required a free alpha amino group and an activated carboxyl group as a methyl ester of D-form phenylglycine. Interestingly, the purified enzyme did not catalyze hydrolysis of its products, e.g., cephalexin, cephradine, and ampicillin, in contrast to enzymes from other strains of Pseudomonadaceae.

Acyltransferases↗
PubMed1976

3-Deacetoxy-7-(alpha-amino-1-cyclohexenylacetamido) cephalosporanic acid (SCE-100), a new semisynthetic cephalosporin. III. Comparative studies on absorption, distribution and excretion of SCE-100 and cephalexin (CEX) in laboratory animals.

3-Deacetoxy-7-(alpha-amino-1-cyclohexenylacetoamido) cephalosporanic acid (SCE-100) was compared to cephalexin with respect to absorption, tissue distribution, and urinary and biliary excretion in mice, rats, rabbits and dogs. The absorption of SCE-100 after oral administration is generally slower than that of cephalexin, but its disappearance from blood and tissues is delayed. The concentration of SCE-100 in the liver is distinctly higher than that of cephalexin. These properties of SCE-100 are most clearly manifested in rats. There is no significant difference in urinary excretion of the two cephalosporins in rabbits and dogs, while in rabbits, biliary excretion of SCE-100 is more intensive than that of cephalexin.

Administration, Oral↗