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Cephalexin monohydrate suspension. Treatment of otitis media.

Cephalexin monohydrate suspension was used in the treatment of 97 children with otitis media. Pretreatment middle-ear exudate specimens in pure or mixed culture yielded Diplococcus pneumoniae in 47 cases, Haemophilus influenzae in 26, Neisseria catarrhalis in 20, group A beta-hemolytic streptococci in 13, and Staphylococcus aureus in one. The usual dosage was 100 mg/kg/day given orally in divided doses for 10 to 12 days. After 48 hours of treatment, follow-up cultures showed that therapy had been successful in 90 children; 81 remained clinically and bacteriologically free of disease for at least three weeks following therapy. Of the seven children for whom therapy failed, H influenzae persisted in five and D pneumoniae in two. Acceptance of the drug was entirely satisfactory with no important side effects encountered.

Adolescent↗

Comparative trials of doxycycline versus amoxicillin, cephalexin and enoxacin in bacterial infections in chronic bronchitis and asthma.

The comparative efficacy of doxycycline versus amoxicillin, cephalexin, cefaclor and enoxacin was examined in four separate cross-over and blinded studies of acute bacterial bronchitis in chronic bronchitis and asthma. The efficacy of doxycycline over the eleven-year period (1975-1986) covered by these studies also was examined. Patients with acute bacterial exacerbations, defined by increased chest symptoms, increased bacteria and sputum neutrophilia, were randomly entered. When a new acute infection occurred, they were re-entered and received the other antibacterial. Response was recorded as successful or not; early rebound infections and the periods free of infection were noted. A total of 136 exacerbations were evaluated in the comparison of doxycycline with the other 4 antibacterials, and 93 exacerbations in the long-term efficacy of doxycycline. The acute success was similar for doxycycline with the other antibacterials and was superior to cefaclor. Early rebound infections occurred less frequently with doxycycline as compared to the cephalosporins and was similar versus amoxicillin and enoxacin. The infection-free period was longer after doxycycline than with the other four antimicrobials. Doxycycline maintained its efficacy to elicit a prompt response and provide a long infection-free period, but an increase of early rebound infections was noted over the eleven-year period.

Adult↗

Sensitive enzyme immunoassay of cephalexin residues in milk, hen tissues, and eggs.

A sensitive enzyme immunoassay for cephalexin (CEX) was developed using the rabbit antiserum to CEX, beta-D-galactosidase-labeled CEX, and a double-antibody separation method. The immunogen of CEX was prepared by coupling the amino group of CEX to thiol groups introduced into bovine serum albumin by the use of N-(m-maleimidobenzoyloxy)succinimide as a cross-linker. Highly titered antiserum to CEX was produced in rabbits immunized with the immunogen. Enzyme labeling of CEX with beta-D-galactosidase was done by using N-(gamma-maleimidobutyryloxy)succinimide as the cross-linker. The limit of detection was 30 ng CEX/mL sample solution. Application of the method to CEX drug residues detected 30 ng/mL in milk, 60 ng/g in egg yolk, and 400 ng/g in hen tissue.

Animals↗

Effect of amoxicillin, cephalexin, and tetracycline-HCl on intestinal L-leucine transport in the rat in vivo.

By utilising an in vivo technique the effects of amoxicillin, cephalexin, and tetracycline-HCl on intestinal L-leucine absorption were studied in the rat. The results showed that amoxicillin caused a time-dependent and reversible inhibition of L-leucine transport while the inhibition induced by the other two antibiotics tested was not reversible. Light microscopic studies revealed that the three antibiotics were without effect on intestinal mucosal morphology.

Amoxicillin↗

Determination of residual cephalexin in chick tissues by Bacillus stearothermophilus paper disc assay.

A paper disc method is described for determination of residual cephalexin (CEX) in chick tissues. A trichloroacetic acid extract of plasma and tissues is chromatographed on a macroreticular resin (Diaion HP-20) column to remove endogenous antibacterial substances interfering with the assay. The eluate is evaporated to dryness and the residue, dissolved in methanol-water (1 + 2), is subjected to a paper disc assay using Bacillus stearothermophilus var. calido-lactis C953 NIZO as a test organism. The detection limit was 0.0375 ppm in tissue; the average recovery of CEX ranged from 72.4% in skin to 90.4% in plasma. Water containing 200 or 500 mg/L of CEX was given ad libitum to 2-week-old chicks for 10 days; the highest levels of CEX were found in the kidney, and the lowest were found in muscle at 0 h of withdrawal. CEX disappeared from most tissues at 24 h after withdrawal except from skin of chicks given 500 mg/L. However, the drug was not detected in the skin at 48 h after withdrawal.

Adipose Tissue↗

[The adhesive capacity of representative intestinal microflora in the continuous and split oral administration of cephalexin and erythromycin].

When cephalexin and erythromycin were administered intragastrically with intervals, adhesion of facultative pathogenic bacteria such as Klebsiella, Staphylococcus and E. coli to enterocytes of the small intestine in vitro was more pronounced than with their continuous administration with drinking water. The adhesive capacity of the staphylococcal strains resistant to the antibiotics was higher than that of the sensitive ones.

Administration, Oral↗

[Comparative studies of the efficacy, safety and usefulness of S6472, cefaclor and cephalexin on complicated urinary tract infection by the double-blind method].

To objectively evaluated the usefulness of the standard formulation of cefaclor (CCL) and the long-acting formulation of cefaclor (S6472) in noncatheterized complicated urinary tract infection (UTI), a double-blind comparison study was carried out using cephalexin (CEX) as a control. Patients were orally treated with either 500 mg of CCL 3 times/day, 750 mg of S6472 2 times/day, or 500 mg of CEX 4 times/day for 14 days. Overall clinical effect was evaluated on days 5 and 14 in accordance with the UTI therapeutic evaluation standard, with check for recurrence on day 21. There was no demographic difference between the groups. There was no difference in the effective rate on day 5 among the 3 treatment groups: 58.1% in S6472 group, 66.0% in CCL group and 61.9% in CEX group. Nor on day 14, was there any significant difference in the effective rate among the 3 groups: 70.8% in S6472 group, 63.4% in CCL group and 61.8% in CEX group. Stratification analyses (by UTI group, infection site, in- or out-patient, time of starting treatment, pretreatment severity of pyuria, total number of bacteria before treatment) revealed no significant difference among the 3 groups. Therapeutic effect evaluated by physicians in charge was not significantly different among the 3 groups on day 5 or day 14. In terms of overall therapeutic effect, all 3 products were very effective in patients infected with sensitive bacteria: On day 5, 85.4% in S6472 group, 84.4% in CCL group, and 83.7% in CEX group. There was no significant difference among the 3 groups on either day. The incidence of side effects was not significantly different among the 3 groups: 4 out of 129 patients treated with S6472 (3.1%), 2 of 131 treated with CCL (1.5%) and 2 of 128 with CEX (1.6%). Clinical laboratory tests revealed 4 abnormal findings in 4 patients treated with S6472, 6 findings in 4 treated with CCL, and 4 findings in 2 treated with CEX, showing no significant difference in incidence among the 3 groups. Both side effects and abnormal clinical laboratory findings were mild and reversible. Physicians in charge judged the usefulness of the 3 drugs on days 5 and 14, taking efficacy and safety into consideration. Significant difference was not observed. The presence of recurrence was examined 7 days after drug withdrawal in patients regarded as remarkable responders to 14-day treatment by overall therapeutic effect evaluation.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Oral↗

[Sustained release cephalexin (S-6436) and genitourinary tract infection (author's transl)].

1) Forty (40) patients with comparatively simply urinary tract infections were orally administered 1 g/day of sustained release cephalexin (S-6436) in two divided doses (after breakfast and dinner) for 7 approximately 14 days, and 20 patients complicated with chronic urinary tract infections or epididymitis were orally given 2 g/day of the drug in two divided doses (after breakfast and dinner) for 7 approximately 28 days. Thirty six (90%) patients of the 40 receiving 1 g/day and seventeen (85%) of the 20 with 2 g/day satisfactorily responded to the drug. 2) Disappearance of organisms was observed in 43 patients (75.4%) of the 57 with urinary tract infections on whom bacteriological examination was conducted. Three (7.0%) of the 43, however, recurred within 7 days after the treatment. In six patients (10.5%) of the 57, the organisms were replaced. 3) Side effects such as gastrointestinal disturbance, allergic reactions, abnormality of blood picture, and impairments of renal and hepatic functions were examined and no such side effects were found except uriticaria in whole body was observed in only one patient with 1 g/day, which disappeared after discontinuation of the administration of the drug.

Adolescent↗

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

Oral sustained release cephalexin (S-6437) was administered to 24 pediatric patients. Daily dose used was 18 approximately 60 mg/kg, which was divided into two doses and given after breakfast and dinner. The following are the results of the study. Out of 24 patients, 6 showed very good response, 10 good response, 6 fair, 1 poor and 1 unknown, Ratio of effectiveness was 69.6%. Two patients were reluctant to receive the drug and, therefore, they took other drugs. The other 22 patients, however, were easily given. No remarkable side effects due to S-6437 were found. From the above results, it was recognized that S-6437 has good effectiveness and safety, and it is convenient to give to children because the frequency of the drug administration is only twice a day.

Administration, Oral↗

[Clinical study of sustained release cephalexin (S-6436, S-6437) in dermatology (author's transl)].

S-6436 or S-6437 was orally administered to 30 patients with bacterial infections including some patients with secondary infections. The following results were obtained: 21 patients had excellent effect, good 5, fair 2 and poor 2. The effectiveness was 86.7%. One gram (potency)/day of sustained release cephalexin was given to most of the patients divided into 2 doses after breakfast and dinner. This b.i.d. regimen was popular among outpatients as well. Staph. aureus isolated from 73.3% of the patients disappeared. Overall bacteriological effectiveness was 72.2%. In only 2 patients, side effects were observed. One had a mild pain in stomach and the other had aggravation of itching in complication of eczema. No abnormalities in laboratory studies which were conducted in some patients were found.

Adult↗

[Isolation of a highly pure preparation of cephalexin amidase from bacteria of the genus Xanthomonas].

A procedure for highly purified cephalexin amidase of Xanthomonas was developed. It consists of preparation of a cell-free extract of the culture after cell disintegration, precipitation with ammonium sulfate, dissolution, concentration and elimination of ballast proteins, gel filtration on Sephadex G-25, sorption of ballast proteins on DEAE cellulose and chromatography on KM-cellulose. The enzyme yield is 45-55 per cent. The purity level is 80-90-fold.

Amidohydrolases↗

[Comparative double-blind study of cefroxadine and cephalexin in the treatment of complicated urinary tract infection].

To evaluate the efficacy, safety, and utility of cefroxadine (CXD) for the treatment of complicated urinary tract infections, a double blind study comparing CXD with cephalexin (CEX) was carried out. Patient received either 1,500 mg/day of CXD 3 times a day, or 2,000 mg/day of CEX 4 times a day for 5 days by oral route, and the following results were obtained. Of the 305 patients, clinical efficacies were evaluated in 220 cases (CXD 105 cases, CEX 115 cases) except that excluded or dropped out. Side effect was evaluated in 301 cases (CXD 150 cases, CEX 151 cases). There was no statistically significant difference in the back ground characteristics between the 2 groups. Overall clinical assessment by the committee according to the "Criteria for Evaluation of Clinical Efficacy of Antimicrobial Agents on Urinary Tract Infection" patients evaluated as better than "good" were 64 of 105 (61.0%) for CXD and 75 of 115 (65.2%) for CEX. The difference between the 2 groups was not statistically significant. In effect on pyuria, patients evaluated as better than "decreased" were 58 of 105 (55.2%) for CXD and 69 of 115 (60.0%) for CEX. The difference between the 2 groups was not statistically significant. In effect of bacteriuria, patients evaluated as better than "decreased" were 57 of 105 (54.3%) for CXD and 69 of 115 (60.0%) for CEX. The difference between the 2 groups was not statistically significant. Analyses were stratified according to classification by the type of infection, diagnosis, degree of pyuria before treatment, and bacterial count before treatment. There were no statistically significant differences between the 2 treatment groups as to any item. In evaluation by attending physician, patients evaluated as better than "good" were 81 of 140 (57.9%) for CXD, and 85 of 141 (60.3%) for CEX. Statistically significant difference was not observed between the 2 groups. In drug usefulness by attending physician, patients evaluated as better than "usefulness" were 106 of 140 (75.7%) for CXD, and 109 of 141 (77.3%) for CEX. The difference between the 2 groups was not statistically significant. In evaluation of the infections with sensitive species to both CXD and CEX by the committee according to "Criteria for Evaluation of Clinical Efficacy of Antimicrobial Agents on Urinary Tract Infections, overall clinical efficacies were evaluated in 102 (CXD 48 cases, CEX 54 cases) which were infected with sensitive species. There was no statistically significant difference in the back ground characteristics between the 2 treatment groups.(ABSTRACT TRUNCATED AT 400 WORDS)

Adult↗

[Double-blind comparative trial of cefroxadine and cephalexin in the treatment of acute suppurative otitis media and acute exacerbation of chronic suppurative otitis media].

A double-blind controlled trial of cefroxadine (CXD) 250 mg t.i.d. was undertaken to objectively evaluate its safety and effectiveness in the treatment of acute suppurative otitis media and acute exacerbation of chronic suppurative otitis media, using cephalexin (CEX) 250 mg q.i.d. as a control drug, and the following results were obtained. In the treatment of acute suppurative otitis media, the 2 drugs produced almost equal outcomes, showing no significant difference in assessments of both overall effects and usefulness. In the treatment of acute exacerbation of chronic suppurative otitis media, the 2 drugs exhibited no significant difference as well in overall effects by Wilcoxon's two-sample test. However, the CEX group had significantly more nonresponsive patients, i.e. 35.5% as compared with 9.7% of the CXD group (chi 2-test, P less than 0.05). In the assessment of clinical usefulness as well, no significant difference was observed between the 2 groups. In the assessment of overall effects based on the patients whose isolated organisms were sensitive to the drugs, CEX group had more patients not responding to the treatment of acute exacerbation of chronic suppurative otitis media (chi 2-test, P less than 0.05). Bacteriological effects were not significantly different between the 2 drugs in both acute suppurative otitis media and acute exacerbation of chronic suppurative otitis media. Overall safety rating was not significantly different between the 2 drugs. Side effects occurred as the symptoms of digestive organ in 2 patients each in both groups (equally an incidence of 2.6%). As for the improvement of each symptom after treatment (assessed on day 3), CXD was superior in the improvement rate of otorrhea volume as the main symptom of acute exacerbation of chronic suppurative otitis media, while CEX was superior in that of otoobstruction feeling. From the above findings, it is presumed that CXD is a safe drug which can exhibit equal or superior therapeutic effects to CEX in the treatment of acute suppurative otitis media and acute exacerbation of chronic suppurative otitis media, at 3/4 of the CEX dose level.

Adolescent↗

Cephalexin in the treatment of upper respiratory tract infections.

Cephalexin, a semisynthetic cephalosporin antibiotic, has wide clinical application in respiratory infections of children and adults. In pharyngitis and tonsillitis due to beta-haemolytic streptococci, it is comparable to penicillin, cyclocillin, and cephaloglycin, as measured by clinical response, bacteriological cure rate, and incidence of relapse and reinfection. In otitis media, it is effective at dosages of 50-100 mg/kg/day except in those infections caused by Haemophilus influenzae, in which there is failure in 50% of the cases. In other infections of the upper respiratory tract, it appears to be effective except, again, in those caused by H. influenzae. Dosages of 1-2 g/day have been used in adults and 20-100 mg/kg/day in children. Adverse effects, mostly gastrointestinal upsets, rash, and urticaria, have been relatively infrequent and have not required discontinuance of the drug.

Adult↗

[A double-blind comparison between cefaclor and cephalexin in the treatment of dental infections].

A comparative clinical study of cefaclor (CCL) with cephalexin (CEX) was carried out by randomized double-blind techniques in order to contemplate the clinical efficacy, side effects and usefulness in treatment of 243 patients with dental infections. In the CEX group, CEX was orally administered 4 times a day at a daily dosage of 1,000 mg for 3 to 5 days. In the CCL group, CCL was orally administered 3 times a day at a daily dosage of 750 mg for 3 to 5 days and 1 capsule of placebo was also given every evening in order to keep the blindness of the administration. Evaluable cases for efficacy of athe drugs were 213 consisting of 108 for CCL and 105 for CEX. There were no significant differences in background of the patients and severity of the disease between 2 treatment groups. Clinical effectiveness on the 3rd day was 89.7% in CCL group and 78.6% in CEX group, showing significant difference between 2 treatment groups. Clinical effectiveness on the final day of administration was 94.4% in CCL group and 92.4% in CEX group, showing no significant difference between 2 treatment groups. Side effects were found in 10.5% of 114 patients receiving CCL and in 4.5% of 112 patients with CEX, and there was no significant difference between 2 treatment groups. The side effects were mostly gastrointestinal origin. According to the judgement by physicians in charge, no significant difference was seen in clinical usefulness between the 2 drugs.

Adult↗

Cephalexin: interpretation of sensitivity disc testing in veterinary practice.

A regression study using 30 micrograms cephalexin sensitivity discs with bacterial strains isolated from veterinary sources is described. Techniques suitable for use in veterinary investigation laboratories were used and critical zone sizes calculated from a linear regression analysis. Zone sizes of less than or equal to 18 mm, 19 to 20 mm and greater than or equal to 21 mm were found to be suitable to categorise strains as resistant, intermediate or sensitive, respectively. Experience in the use of these recommended critical zone sizes in clinical practice will be necessary before firm recommendations can be made.

Animals↗

Effect of storage on the bioavailability of cephalexin from its capsules.

Three brands of locally available cephalexin capsules were stored in paper bags at 40 degrees C/90% relative humidity. Samples were taken at different time intervals and tested for the effect of storage on disintegration, dissolution and drug content for up to 70 days. Bioavailability testing was carried by administering the capsules to four volunteers before storage and after 70 days of storage. Two brands (A and B) showed increase in disintegration time associated with decrease in the rate of dissolution. The third brand (C) showed similar effect but later on irregular disintegration and dissolution were observed. Such behavior was found to be a result of storage effect on the capsule shell. No effect on drug content was observed for brands A and B but significant loss of activity was observed with some samples of brand (C). Bioavailability testing based upon urine analysis for excreted drug indicated that the rate but not the extent of drug absorption for brands A and B decreased by storage. The results with brand C showed serious fluctuations in absorption after storage for more than 25 days. These findings point out to the importance of proper formulation and protection of solid dosage forms handled in places where high temperature and humidity conditions are likely to exist.

Biological Availability↗

Treatment of chronic prostatitis by consecutive per os administration of doxycycline, sulfamethoxazole/trimethoprim, and cephalexin.

Fifty men with cytologically confirmed chronic prostatitis were treated for 3 months by consecutive p.o. administration of doxycycline, sulfamethoxazole/trimethoprim, and cephalexin. The subjective symptoms, palpatory findings, secretory capacity of the accessory genital glands (values of acid phosphatase and fructose in the seminal plasma) were evaluated. The cytologic findings from the expressed prostatic fluid and semen analysis before and after the treatment were also studied. Approximately 60% of the patients were cured of the subjective symptoms. The palpatory findings disappeared in 50% of the cases. The cytologic findings became normal in 70% of the patients (inflammatory cells less than 25/HPF). The secretory function of the prostate and the seminal vesicles was improved in 50% and 25%, respectively, of the patients, and the quantitative and qualitative motility and viability of the spermatozoa after treatment were significantly enhanced.

Administration, Oral↗