cefroxadine and Bacterial-Infections

The antibacterial spectrum of cefroxadine was as wide as that of CEX, and its antibacterial effect was as strong as that of CEX or even 2-fold stronger against E. coli and Klebsiella. Cefroxadine was also proved to have stronger bactericidal or bacteriolytic effect than CEX and have better affinity with penicillin binding proteins. In clinical trials, an efficacy rate of 82.7% was achieved in a total of 2,009 cases of various infections analyzed. Cefroxadine displayed particularly good clinical and bacteriological effects for the infections of skin, soft tissues, respiratory tract and urinary tract. The rate of bacteria eradication in a total of 1,410 cases was 81.6%, showing good results against the bacteria such as S. aureus (83.9%, 167/199), E. coli (89.0%, 528/593), Klebsiella (78.0%, 78/100) and P. mirabilis (80.0%, 36/45). As for side effects, their incidence was a low of only 2.3%, the main ones being eruption and gastrointestinal symptoms just as recognized in conventional cephalosporins, and none of them was serious. Abnormal laboratory test values were only increases in eosinophil, S-GOT, S-GPT and Al-P values, and their incidence was low. From these findings, we may say that the drug is an effective, safe, and useful antibiotic among all other orally administered cephalosporins.

Topics: Adolescent; Adult; Aged; Animals; Bacteria; Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Clinical Trials as Topic; Drug Resistance, Microbial; Female; Humans; Male; Mice; Middle Aged; Pregnancy; Rabbits; Rats

The antibacterial spectrum of cefroxadine was as wide as that of CEX, and its antibacterial effect was as strong as that of CEX or even 2-fold stronger against E. coli and Klebsiella. Cefroxadine was also proved to have stronger bactericidal or bacteriolytic effect than CEX and have better affinity with penicillin binding proteins. In clinical trials, an efficacy rate of 82.7% was achieved in a total of 2,009 cases of various infections analyzed. Cefroxadine displayed particularly good clinical and bacteriological effects for the infections of skin, soft tissues, respiratory tract and urinary tract. The rate of bacteria eradication in a total of 1,410 cases was 81.6%, showing good results against the bacteria such as S. aureus (83.9%, 167/199), E. coli (89.0%, 528/593), Klebsiella (78.0%, 78/100) and P. mirabilis (80.0%, 36/45). As for side effects, their incidence was a low of only 2.3%, the main ones being eruption and gastrointestinal symptoms just as recognized in conventional cephalosporins, and none of them was serious. Abnormal laboratory test values were only increases in eosinophil, S-GOT, S-GPT and Al-P values, and their incidence was low. From these findings, we may say that the drug is an effective, safe, and useful antibiotic among all other orally administered cephalosporins.

Topics: Adolescent; Adult; Aged; Animals; Bacteria; Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Clinical Trials as Topic; Drug Resistance, Microbial; Female; Humans; Male; Mice; Middle Aged; Pregnancy; Rabbits; Rats

Cefroxadine and cephalexin were compared in a double-blind study in patients with complicated urinary tract infections. Patients were treated orally with 1 g t.i.d. for five days. Bacterial counts in the urine were determined 1, 3 and 8 hours after the first dose and on the second, third and fifth day of treatment. A decrease in the bacterial population below 10(4) organisms/ml of urine was taken as being indicative of chemotherapeutic effect. Urine specimens were inactivated enzymatically before culture to eliminate any residual cephalosporin. A significant reduction in the bacterial count was seen one and three hours after the first dose, and, to a much greater extent, after eight hours. Reduction in the bacterial count was more frequent in the group treated with cefroxadine. The results during the first eight hours indicate that cefroxadine kills more rapidly than cephalexin, which is in agreement with the experimental findings. Whether the transient differences observed in the rates of inhibition are of clinical relevance remains uncertain.

Topics: Adolescent; Adult; Aged; Bacterial Infections; Bacteriuria; Cephalexin; Cephalosporins; Cephradine; Clinical Trials as Topic; Double-Blind Method; Escherichia coli; Female; Humans; Kinetics; Klebsiella; Male; Middle Aged; Proteus mirabilis; Urinary Tract Infections; Urine

Cefroxadine dry syrup was studied clinically and the following results were obtained. The drug was administered to 19 cases of bacterial infections: acute tonsillitis (6), acute bronchitis (6), scarlet fever (2), acute pyelonephritis (4) and acute cystitis (1). The daily dose was about 30 approximately 50 mg/kg except for 1 patient. The drug was given orally, 3 times a day and the duration of administration was from 4 to 11 days. The overall efficacy rate was 100%, i.e., excellent in 17 cases, good in 2 cases. One patient experienced a mild S-GOT elevation and another patient in mild vomiting. From the results obtained in this study, cefroxadine dry syrup seems to be useful in the treatment of infectious diseases of children.

Topics: Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Clinical Trials as Topic; Dosage Forms; Drug Evaluation; Female; Humans; Infant; Male

A study was made with the newly developed cefroxadine (CXD) dry syrup by measuring the serum level, urine excretion and recovery rate in 10 children who were orally administered 5, 10 and 20 mg/kg at 1 hour after meals and the following results were gained. Also, its clinical efficacies and side effects were investigated in the following cases who were treated with a mean dose of 33 mg/day divided into 3 to 4 portions for a period of 9 days on the average; viz. a total of 151 cases consisting of 9 cases of pharyngitis, 39 of tonsillitis, 11 of streptococcal infection, i.e. scarlet fever, 7 of bronchitis, 6 of pneumonia, 1 of otitis media, 6 of purulent lymphadenitis, 1 of purulent parotitis, 1 of subcutaneous abscess and 3 of impetigo. 1. The serum level tends to reach its maximum level within 1 hour after administration. The mean concentrations of 5, 10 and 20 mg/kg dose in the foregoing time were 6.35, 9.12 and 21.62 mcg/ml respectively and dose response was observed. CXD showed higher concentration than CEX, CED and CFT. The mean half-life periods of the 3 dose were 72, 84 and 66 minutes respectively and variations were observed, but the drugs maintains a satisfactory serum level. 2. The time which showed highest urine excretion was mainly in the 0 to 2 hours bracket and the average concentrations of 5 , 10 and 20 mg/kg dose in the foregoing time were 381.2, 771.7 and 1,577.7 mcg/ml respectively. The dose response was more evident than in the serum concentrations. The average recovery rates within 6 hours were 93.6, 88.3 and 94.3% respectively and they were similar to those of CEX, CED and CFT. 3. The clinical effects were evaluated were in 148 cases out of the total of 151 and 136 cases, or 91.9% showed good or excellent efficacy response. 4. The daily dose groups of less than 30 mg/kg and 31 to 40 mg/kg formed the majority and there was no difference in the comparison of the clinical effectiveness in these 2 groups. Administration of a daily dose of 20 to 40 mg/kg is sufficient for the treatment of the aforementioned mild diseases except for pneumonia. 5. The clinical effects were compared between the 3 and 4 times a day treatment groups, but there was no difference between these two groups with regard to the foregoing daily dose. The 3 times a day treatment is acceptable, but the 4 times a day treatment is preferable when pharmacokinetics if taken into account. 6. The bacteriological effects in 41 cases, or 97.6% out of the 42 cases were above the e

Topics: Adolescent; Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Clinical Trials as Topic; Female; Humans; Infant; Male

In this multicentre trial, 1072 hospitalized children, 573 boys and 499 girls (847 of whom were aged less than 6 years), affected by respiratory tract (376 patients) or ENT (696 patients) infections were treated for 10 days with cefroxadine per os, at an average dose of 650 mg/day (325 mg every 12 h corresponding to 25 mg/kg b.w.). Most patients (1047; 97.7%) completed the trial, while 25 patients were withdrawn from the study (20 patients for viral diseases and 5 for side-effects). Of the patients affected by respiratory tract infections, 361 completed the trial and 342 of them (94.7%) were cured in 6.0 days on average. Of the patients affected by ENT infections, 686 completed the trial and 649 of them (94.6%) were also cured in an average of 6.0 days. In the two groups the signs and symptoms of the disease significantly (p less than 0.001) decreased by the end of the study. Some patients (80; 7.6%) complained of side-effects, mainly gastric discomfort (4.9%), skin rash (2.2%) and glossitis (0.5%). In conclusion, cefroxadine exerts a satisfactory antibacterial action with only a few days of treatment, and it appears to be very well tolerated.

Topics: Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Female; Humans; Infant; Infant, Newborn; Male; Otorhinolaryngologic Diseases; Respiratory Tract Infections

Topics: Adolescent; Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Female; Humans; Infant; Male

Influence of cefroxadine (CXD) dry syrup on intestinal bacterial flora was studied in mice infected with 4 species of bacteria, namely, Escherichia coli, Enterococcus faecalis, Bacteroides fragilis and Bifidobacterium breve, and in pediatric patients having infections in the respiratory tract and cutaneous/soft tissues. The results were summarized as follows: CXD dry syrup was administered for 5 consecutive days to mice infected with the 4 species. No considerable changes were observed in levels of bacteria in the feces and in different parts of digestive tracts. Eleven pediatric patients were orally administered with 30-54 mg/kg of CXD dry syrup a day for 7-15 consecutive days. Symptom of diarrhea was noted in 2 patients. Dominant species of the intestinal flora such as E. coli, Bifidobacterium, and Bacteroides sometimes decreased in patients treated with CXD dry syrup. In general, however, decreases in numbers of these bacteria were insignificant. Changes of intestinal flora in patients treated with CXD dry syrup were apparently smaller than those treated with ampicillin and were similar to those treated with cephalexin or amoxicillin.

Topics: Animals; Bacterial Infections; Bacteroides; Bifidobacterium; Cephalosporins; Cephradine; Child; Child, Preschool; Dosage Forms; Escherichia coli; Female; Humans; Infant; Intestines; Male; Mice

Cefroxadine (CXD), a new cephalosporin, was orally administered to 22 cases in total; 5 with wound infection, 4 with felon, 3 with acute pyelonephritis, 2 with furuncle, 2 with infected atheroma, 2 with phlegmone, 2 with abscess, 1 with acute mastitis, and 1 with lymphadenitis. The daily dose was 500 to 1,000 mg, and maximal total dose and duration was 5 g and 5 days, respectively. Therapeutic results were good in 20 cases (effectiveness rate: 91%), fair in 1 and poor in 1. No side effect was observed in all cases among 22 patients with CXD.

Topics: Administration, Oral; Adolescent; Adult; Aged; Bacterial Infections; Cephalosporins; Cephradine; Child; Drug Evaluation; Female; Humans; Male; Middle Aged; Surgical Wound Infection

Cefroxadine (CXD) is an orally administered synthesized cephalosporin antibiotic developed by Ciba-Geigy Limited (Switzerland) in 1972. We have studied the clinical effectiveness of this drug in a total of 45 cases of various types of infections in the dentistry and the oral surgery. The studies resulted in showing 18 markedly effective cases, 19 effective cases, 5 slightly effective cases, 1 ineffective case, and 2 unknown cases showing an effective rate of 82.2%. Side effects manifested in 2 cases, of which 1 case was considered to be attributable to CXD, and the occurrence frequency of side effects was as low as 2.2%. In bacteriological test, there were many cases of mixed infections by Gram-positive and Gram-negative bacteria, and these infections were those which are observed in high frequency in dentistry and oral surgery infections. As a result of an overall evaluation of CXD clinical effects, the drug considered to be an antibiotic which is highly useful in dentistry and oral surgery.

Topics: Administration, Oral; Adolescent; Adult; Aged; Bacterial Infections; Cephalosporins; Cephradine; Drug Evaluation; Female; Humans; Male; Middle Aged; Parotitis; Periodontal Diseases

Cefroxadine was administered at dose level of 750 mg/day to 21 cases of superficial suppurative diseases and the following results were obtained: The effective rate determined by the treating doctor was 9/21 (42.9%). The effective rate by the evaluation standard was 12/21 (57.1%). The negative-conversion rate was 11/11 (100%) in the 11 cases in which bacteriological effects were clarified. No side effects were observed in all of the 21 cases.

Topics: Administration, Oral; Adult; Aged; Bacterial Infections; Capsules; Cephalosporins; Cephradine; Drug Evaluation; Female; Humans; Male; Middle Aged; Suppuration

Cefroxadine (CXD) was studied in the field of obstetrics and gynecology and the following results were obtained. MIC values of CXD against 55 clinical isolates were investigated, from 6.25 to 12.5 micrograms/ml for 8 strains of E. coli, 6.25 micrograms/ml for 3 strains of K. pneumoniae and from 0.39 to 3.13 micrograms/ml for 9 strains of anaerobes such as Peptostreptococcus and Peptococcus in 10(6) cells/ml. Transfer of CXD into intrapelvic organ such as uterus, uterine tube and ovary after the oral administration of 500 mg was investigated. The concentrations in the tissues of genitalia ranged from 5.84 to 7.44 micrograms/g about 2 hours later after the administration. CXD was orally given to 18 patients with infections of genital organs at daily dose of 1,500 mg (500 mg 3 times a day). The clinical response was good, and efficacy rate was 88.9%. No remarkable side effects were observed.

Topics: Adult; Bacteria; Bacterial Infections; Cephalosporins; Cephradine; Drug Evaluation; Drug Resistance, Microbial; Female; Genital Diseases, Female; Humans; Middle Aged; Uterus

Clinical effect and excretion into wound exudate of a new semisynthetic cephalosporin cefroxadine (CXD), were studied. CXD was given in 25 cases of surgical infections; 6 cases of wound infection, 9 cases of abscess, 9 cases of infected atheroma and 1 case of furuncle. CXD was orally administered in daily dose of 750 to 1,500 mg. Clinical results were excellent in 1 case, good in 18 cases, fair in 3 cases and poor in 3 cases. The overall clinical efficacy rate was 76.0%. Clinical efficacy classified by diagnosis was 66.7% in wound infection, 66.7% in abscess, 88.9% in infected atheroma, and 100% in furuncle. Side effects were not observed in all cases among 25 patients in CXD trials. Studies of excretion into wound exudate of CXD were performed in 1 postoperative case of mamma carcinoma after oral administration of 500 mg of CXD. The concentration of CXD in exudate was 1.12 micrograms/ml in 2 hours, 3.48 micrograms/ml in 3 hours, 4.13 micrograms/ml in 4 hours, 5.56 micrograms/ml in 5 hours and 4.41 micrograms/ml in 6 hours after administration, which was observed that CXD was excreted in wound exudate in high concentration.

Topics: Abscess; Administration, Oral; Adolescent; Adult; Aged; Bacterial Infections; Cephalosporins; Cephradine; Child; Drug Evaluation; Exudates and Transudates; Female; Humans; Male; Middle Aged; Surgical Wound Infection; Wound Infection

Clinical study of cefroxadine (CXD), an orally active cephalosporin, for the treatment of infections in the field of obstetrics and gynecology was carried out and the following results were obtained. Fifteen strains were isolated in present study. These isolates were mainly E. coli and anaerobes (Peptococcus sp., Peptostreptococcus sp.). The distribution of susceptibilities to CXD of E. coli was between 6.25 approximately 12.5 micrograms/ml and that of anaerobes was between 0.39 approximately 1.56 micrograms/ml. These results were similar to those of CEX. CXD was used in the treatment of 11 patients (endometritis 1 case, adnexitis 3 cases, bartholinitis 7 cases). In overall clinical efficacies, patients evaluated as better than "good" were 10 out of 11 (90.9%). Skin eruption was observed in 2 cases. No abnormality in laboratory findings was recognized.

Topics: Adult; Bacteria; Bacterial Infections; Cephalosporins; Cephradine; Drug Evaluation; Drug Resistance, Microbial; Female; Genital Diseases, Female; Humans; Middle Aged

Cefroxadine (CXD), an oral cephalosporin antibiotic was studied in the field of obstetrics and gynecology and the following results were obtained. CXD was orally given to 22 cases at daily dose of 1,500 mg 3 times a day. CXD administration was given to 22 cases in all; 4 with cervicitis, 6 with endometritis, 2 with puerperal fever, 4 with bartholinitis, 5 with adnexitis and 1 with vulvitis, respectively. Overall efficacy rate was 77.3% (17/22) (excellent 4, good 13, fair 5). As for side effects, a slight diarrhea was observed. CXD was considered to be a useful antibiotic in the field of obstetrics and gynecology by above the results.

Topics: Administration, Oral; Adolescent; Adult; Aged; Bacterial Infections; Cephalosporins; Cephradine; Drug Evaluation; Female; Genital Diseases, Female; Humans; Middle Aged; Pregnancy; Puerperal Infection

Clinical studies of cefroxadine (CXD), a new orally active of cephalosporin, in obstetrical and gynecological field were performed, and the results were summarized as follows. CXD was orally administered to 16 cases of obstetrical and gynecological infections in daily dose 750 approximately 1,500 mg. Clinical efficacy was 88.9% in endometritis (9 cases), 100% in cervicitis (2 cases), 75% in adnexitis (4 cases) and 100% in suppurative haematoma vulva (1 case), respectively. Overall efficacy was 87.5% (14/16). Clinical efficacy classified by caused organisms was 83.3% (10/12) overall, and bacteriological effect was 91.7% (11/12). Neither side effects nor abnormalities in laboratory findings caused by this drug were observed. Based on these results, CXD should be considered a very safe and useful drug for treating obstetrical and gynecological infections.

Topics: Administration, Oral; Adolescent; Adult; Bacteria; Bacterial Infections; Cephalosporins; Cephradine; Drug Evaluation; Drug Resistance, Microbial; Female; Genital Diseases, Female; Humans; Middle Aged

Cefroxadine (CXD) capsules and dry syrup, an oral cephem antibiotic, were administered into 120 cases with ocular infections and the following results were obtained: The daily dose of CXD capsule was ranged from 500 to 1,500 mg and that of CXD dry syrup from 17.9 to 85.7 mg/kg, and the duration of CXD administration was from 2 days to 14 days. Clinical response rates classified by diagnosis The clinical response rates were 77.8% (14/18) in blepharitis, 86.7% (26/30) in hordeolum, 62.5% (5/8) in meibomianitis, 74.6% (44/59) in conjunctivitis, 100% (2/2) in corneal infiltration, 100% (1/1) in cellulitis of the lid, in dacryocystitis and in corneal ulcer, respectively. Clinical response classified by isolated organisms The response rates on S. aureus were 80.0% (20/25), on S. epidermidis 75.8% (47/62) and on S. pneumoniae 66.7% (2/3), respectively. The overall clinical response rate on Gram-positive bacteria was 78.3% (94/120). The response rates on H. influenzae, Acinetobacter spp., P. mirabilis, E. coli and Moraxella spp. were ranged from 42.9 to 100%. The sensitivity distributions of clinically isolated S. aureus and S. epidermidis to CXD were ranged from 1.56 to greater than 100 micrograms/ml and from 0.39 to 12.5 micrograms/ml, respectively. The former showed a peak at 3.13 micrograms/ml and the latter in 1.56 micrograms/ml. Side effects in 3 cases (2.3%) out of 129 were observed. That is; glossitis, thirst feeling and palpitation in each case, respectively.

Topics: Administration, Oral; Adolescent; Adult; Aged; Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Dosage Forms; Drug Evaluation; Eye Diseases; Female; Humans; Infant; Infant, Newborn; Male; Middle Aged

Cefroxadine (CXD), an orally active cephalosporin antibiotic, has a broad spectrum and a bactericidal action. The efficacy of CXD in the surgical field was investigated and the following results were obtained. CXD was administered to 31 cases in all; 13 cases with mastitis, 9 with wound infection, 4 with infected atheroma, 3 with periproctal abscess and 2 with phlegmon, respectively. The daily dose was ranged from 750 mg to 1,500 mg. Clinical effects were good in 27 cases and fair in 4 cases, and the effective rate was 87.1%. As to side effects, a slight diarrhea was observed in 1 case, but the symptom was disappeared after 2 days without a special treatment.

Topics: Administration, Oral; Adolescent; Adult; Aged; Bacteria; Bacterial Infections; Cephalosporins; Cephradine; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Male; Mastitis; Middle Aged; Pregnancy; Surgical Wound Infection; Wound Infection

CGP 9000 (cefroxadine), a new cephalosporine derived from N-acyl-3-alkoxy-7-amino-3-cefem-4-carboxylic acid for exclusively oral use, has been experimented on 67 patients, 41 adults and 20 children. CGP 9000 appeared to possess good therapeutic activity, even in low doses: its rapid absorption and moderate sero-protein bond are a guarantee of an immediate and almost total bioavailability.

Topics: Adolescent; Adult; Bacterial Infections; Biological Availability; Bronchitis; Bronchopneumonia; Cephalosporins; Cephradine; Child; Child, Preschool; Cystitis; Drug Evaluation; Erysipelas; Female; Humans; Infant; Male; Middle Aged; Mouth Diseases; Parotitis; Scarlet Fever

Fundamental and clinical studies on cefroxadine (CXD) were carried out, and we have obtained the following results. (1) Sensitivity distribution: As for the sensitivity distribution in S. aureus, the peak was within the ranges from 3.13 to 6.25 microgram/ml in the inoculum size of 10(9) CFU/ml, the distribution was less than or equal to 0.1 to 50 microgram/ml in the inoculum size of 10(6) CFU/ml, with the peak at 1.56 to 6.25 microgram/ml. In S. pyogenes, the sensitivity distribution ranged between less than 0.1 and 1.56 microgram/ml, with the peak at 0.1 microgram/ml in the inoculum size of 10(9) CFU/ml. In the inoculum size of 10(6) CFU/ml, however, the all strains were distributed within the ranges of 0.1 to 0.78 microgram/ml, and the growth of 49 out of 54 strains (91%) was inhibited at less than or equal to 0.1 microgram/ml. In E. coli, the sensitivity peak was at 25 to 50 microgram/ml in the inoculum size of 10(8) CFU/ml, and 5 strains (9.3%) were detected with greater than 100 microgram/ml. Of the 5 strains, 1 strain showed cross tolerance with CEX, the remaining 4 strains was at 50 microgram/ml and at 25 microgram/ml in 2 strains each. In the case of inoculum size of 10(6) CFU/ml, the sensitivity distribution was all within the ranges from 0.78 to 12.5 microgram/ml, except for 1 strain at 100 microgram/ml, with the peak being within the ranges from 3.13 to 12.5 microgram/ml. As for the above 100 microgram/ml-strain, it was showing cross tolerance with CEX. (2) Serum concentration: CXD was administered at a dose level of 10 mg/kg and 20 mg/kg between meals to 5 children, and CXD concentration in their serum was measured. In the group of the 10 mg/kg administration: average 30 minutes value; 8.7 microgram/ml, 1 hour value; 9.15 microgram/ml, 2 hours value; 7.4 microgram/ml, 3 hours value; 2.85 microgram/ml, 4 hours value; 1.0 microgram/ml and 6 hours value; 0.32 microgram/ml, with half-life of 0.88 hours. In the group of the 20 mg/kg administration: average 30 minutes value; 11.7 microgram/ml, 1 hour value; 16.8 microgram/ml, 2 hours value; 10.7 microgram/ml, 3 hours value; 8.15 microgram/ml, 4 hours value; 3.33 microgram/ml, 6 hours value; 1.22 microgram/ml, with half-life of 1.03 hours. A significant interrelation in dose response was observed between the 2 groups. (3) CLINICAL RESULTS: Clinical investigation were held in 29 cases (47 boys and 32 girls). Their diseases comprised of 2 acute pharyngitis, 28 acute purulent tonsillitis, 11 scarlet fev

Topics: Adolescent; Age Factors; Bacteria; Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male

The authors have carried out the laboratory and clinical studies of cefroxadine (CXD), and obtained the following results. The antibacterial activities of CXD were measured by plate dilution method on 26 clinical isolates of S. aureus, E. coli and K. pneumoniae. CXD inhibited the growth of all strains of S. aureus at concentrations less than 6.25 microgram/ml, the peak of activity distribution was obtained at 3.13 microgram/ml with an inoculum size of 10(6) cells/ml. And the p eak sensitivity distribution of E. coli was obtained at 6.25 microgram/ml. The growth of all strains of K. pneumoniae was inhibited at concentrations of less than 25 microgram/ml. Phagocytosis was determined by QUIE'S method. In the presence of CXD, phagocytosis of human PMNs was not enhanced to E. coli and K. pneumoniae. For pharmacokinetic study, CXD was given orally at a single dose of 10 mg/kg to 3 children before and after meals. The serum levels of CXD on fasting were 14.2 microgram/ml, 11.0 microgram/ml, 4.0 microgram/ml and 0.57 microgram/ml at 0.5, 1, 2. 4 hours after administration respectively, and the level at 6 hours was not detectable. Half-life was 0.65 hours. The serum levels of CXD after meals were 3.9 microgram/ml, 5.3 microgram/ml, 5.3 microgram/ml, 2.4 microgram/ml and 0.42 microgram/ml at 0.5, 1, 2, 4, 6 hours after administration respectively, but at 8 hours it was not detectable. Half-life was 0.95 hours. The 8-hour urinary excretion rates on fasting and non fasting were 89.4%, 89.0% respectively. CXD was given to 31 cases with tonsillitis, 4 with bronchitis, 1 with impetigo, 3 with cervical lymphadenitis, 7 with U.T.I, totalling 46. A daily dose of CXD 400 approximately 1,500 mg was given for 4 approximately 14 days. Clinical results obtained were good and excellent responses in 43/46 (93.5%) cases. No side effects were observed except for 1 case with elevation of GOT, 2 cases with elevation of GOT and GPT and 1 case with eosinophilia.

Topics: Adolescent; Bacteria; Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male; Phagocytosis

Cefroxadine (CXD) was applied to infectious diseases in children and the following results were obtained. 1. Serum concentration and urinary excretion: CXD was given orally in dose of 10 mg/kg in dry syrup from 30 minutes after meals. The peak serum concentration was at 1 hour after administration in 3 cases and at 2 hours in 1 case, and the average peak serum concentration was 16.41 microgram/ml in these 4 cases. The average urinary excretion rate of the antibiotic during 6 hours after administration was 93.9% in another 4 cases. 2. Antibacterial activity: The MIC of CXD against E. coli was slightly superior to that of CEX, but against S. aureus, S. epidermidis, Str. pyogenes, Str faecalis, Str. pneumoniae, Kleb. pneumoniae, Kleb. oxytoca, Pro. mirabilis, Pro, vulgaris, H. influenzae, H. parainfluenzae, H. parahaemolyticus the MICs of CXD were almost equal to those of CEX. 3. Clinical study: Thirty seven patients with bacterial infections (7 cases of urinary tract infection, 2 of cystitis, 10 of tonsillitis, 9 of scarlet fever, 7 of bronchitis and 2 of bronchopneumonia) were orally treated with CXD dry syrup, 15 approximately 48 mg/kg/day divided into 3 doses. The overall efficacy rate was 91.7%, and side effects inclusive of abnormal laboratory findings were not observed.

Topics: Bacteria; Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Humans; Infant; Male

Cefroxadine (CGP-9000, CXD) is an orally active cephalosporin which has been newly developed by Ciba-Geigy. Its antibacterial activity against clinically isolated organisms, absorption and excretion after oral administration and clinical responses of patients with infections were studied. Its antibacterial activity against S. aureus and K. pneumoniae was comparable to that of CEX. Against E. coli, it showed slightly stronger activity than CEX. The serum concentrations of CXD was measured in 6 patients given orally 10 mg/kg of it after meals. The peak mean serum level attained 1 hour after administration was 11.66 mcg/ml. Forty-three children with various infections (upper respiratory infections, lower respiratory infections, urinary tract infections, etc.) were given 17 approximately 46 mg/kg (averaged 28.7 mg/kg) of CXD daily. The result was excellent in 26 cases, good in 12 cases, fair in 3 cases, fair in 3 cases and poor in 2 cases, showing an effective rate of 88.4%. Side effect of transient leukopenia and elevation of S-GOT were noticed in 2 cases. However, there were no serious adverse reactions in our study. It is concluded that CXD might be effective in rather mild cases of respiratory or urinary tract infections.

Topics: Adolescent; Bacteria; Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male

Basic and clinical evaluations of a new oral cephalosporin cefroxadine (CXD) in pediatric fields were investigated, and the following results were obtained. 1. MICs of CXD against various bacteria were compared with those of cephalexin (CEX). MIC peaks of CXD against clinically isolated S. aureus (22 strains), S. pyogenes (25), S. pneumoniae (8), H. influenzae (23), and E. coli (23) in pediatric fields, were 1.56, 0.2, 1.56, 25 approximately 50 and 6 .25 microgram/ml, respectively in the inoculum size of 10(8) cells/ml, and they were 1.56, less than 0.1, 0.78, 25 and 6.25 microgram/ml respectively in the inoculum size of 10(6) cells/ml. In comparison with CEX, MIC peaks of CXD against S. aureus, S. pyogenes, H. influenzae and E. coli were almost the same with those of the former, it was, however, better by 1 approximately 2 tubes than that of CEX against S. pneumoniae. 2. CXD in the form of dry syrup was administered orally at a dose of either 10 mg/kg or 20 mg/kg to 5 children, and the serum levels and the urinary excretion were evaluated. In the case of 3 children who were administered a dose of 10 mg/kg the mean serum levels were 11.9 microgram/ml after 30 minutes, 13.7 microgram/ml after 1 hour, 4.7 microgram/ml after 2 hours, 0.7 microgram/ml after 4 hours, and 0.3 microgram/ml after 6 hours, while those 2 children who were administered a dose of 20 mg/kg, they were 15.1, 28.5, 12.5, 2.0 and 0.9 microgram/ml respectively. The mean periods of half-life in serum were 0.87 hour in the case of 10 mg/kg and 0.94 hour in the case of 20 mg/kg. The mean excretion rates were 83.8% in the case of 10 mg/kg and 59.8% in the case 20 mg/kg. 3. CXD dry syrup was administered to 31 children with various bacterial infections i.e. acute pharyngitis (15 cases), acute purulent tonsillitis (10 cases), acute bronchitis (4 cases) and 1 case each of acute pyelonephritis and acute purulent cervical lymphadenitis, and the clinical and bacteriological responses and side effect were investigated. The clinical response was either excellent or good in all of the cases. Out of the S. pyogenes (20 strains), S. aureus (1), S. pneumoniae (2), E. coli (1) and H. influenzae (1), bacteriological eradication was observed in all strains with the exception of 1 strain each in S. pyogenes and H. influenzae in which reduction was observed. No side effects and abnormal laboratory findings were observed.

Topics: Bacteria; Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male

Clinical efficacy of cefroxadine dry syrup, a new oral cephalosporin antibiotic, was evaluated in children, and the following results were obtained. 1. Three children were given a single oral dose of about 10 mg/kg of the drug when fasting, and its blood concentrations were determined. Blood concentrations were maximum at 30 approximately 60 minutes, i.e., 16.9 approximately 18.2 microgram/ml, and markedly low at 4 hours. 2. Thirty-six patients with the following diseases were tested with 23.1 approximately 44.4 mg/kg/day of the drug in 3 to 4 divided doses; 21 patients with lacunar tonsillitis, 2 with tonsillitis, 1 with scarlet fever, 4 with bronchitis and tonsillitis, 2 with cystitis, 4 with pyelonephritis, 1 with impetigo and 1 with probable Mycoplasma pneumonia. An overall efficacy rate in 35 patients excluding the last mentioned case was 91.4%, i.e., excellent in 20, good in 12 and poor in 3, and an eradication rate of the causative organisms was 88.9%. 3. Adverse reactions noted were diarrhea in 1 patient, eruption and diarrhea in 1 transient neutropenia in 1, eosinophilia in 3 and an elevation of GOT and GPT in 1. None were significant. 4. Taste and flavor of the drug was considered to be well palatable to children. 5. Taking into consideration of the results of fundamental evaluation of the drug, cefroxadine dry syrup is considered to be a potent new antibiotic in children, and the recommended dose will be 10 mg/kg 3 to 4 times a day.

Topics: Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Dosage Forms; Drug Evaluation; Female; Humans; Infant; Male

In order to evaluate effectiveness of cefroxadine (CXD) in the treatment of bacterial infections of children, the clinical studies were carried out. CXD was orally administered to 30 patients at daily dose of 27.5 approximately 50.0 mg/kg (average 32.3 mg/kg) in 3 approximately 4 divided dose for 3 approximately 10 days (average 4.9 days). The overall efficacy rate in 30 cases was 93.3%, i.e., excellent 22 (73.3%), good in 6 (20.0%), fair in 1 (3.3%) and poor in 1 case (3.3%). Drug eruption and transient eosinophilia were observed in 1 case each out of 30 cases (6.7%), but any other abnormality was not observed throughout this series. Based on the above results, CXD was thus considered to be a useful antibiotic in treatment of pediatric infections.

Topics: Bacterial Infections; Cephalosporins; Cephradine; Child; Child, Preschool; Drug Evaluation; Female; Humans; Infant; Male

Cefroxadine (GCP-9000; CXD), 7 beta[D-2-amino-2-(1,4-cyclohexadienyl)-acetamido]-3-methoxy-ceph-3-em-carboxylic acid, is a new orally active cephalosporin derivative. The spectrum of antibacterial activity of CXD is identical with that of cephalexin (CEX), but CXD was twofold more effective than CEX against Escherichia coli and Klebsiella pneumoniae, CXD was as stable to penicillinase as CEX, but it was hydrolyzed by cephalosporinase, with a relative rate of hydrolysis similar to that of CEX. The affinities of CXD and CEX to penicillin-binding proteins of E. coli were estimated; the affinity of CXD to penicillin-binding protein 1Bs was higher than that of CEX. Consistent with this, CXD had more intensive lytic activity than CEX. In vivo antibacterial activities of CXD and CEX were compared using systemic infections of mice with E. coli and K. pneumoniae; CXD was consistently more active than CEX.

Topics: Administration, Oral; Animals; Bacteria; Bacterial Infections; beta-Lactamases; Carrier Proteins; Cephalexin; Cephalosporins; Cephradine; Dose-Response Relationship, Drug; Escherichia coli; Hydrolysis; Klebsiella pneumoniae; Male; Mice; Microbial Sensitivity Tests; Penicillins