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PubMed1979

[Therapy of bronchitis and bronchopneumonia in adults with cefaclor (author's transl)].

Sixty-two patients with bronchopneumonia or bronchitis were treated with cefaclor. In 42 patients (= 68%), the therapy was clinically successful. Of the patients who did not respond to therapy, cefaclor-resistant bacteria were found in the sputum culture of seven. Of the remaining 13 patients, ten suffered a secondary infection with cefaclor-resistant bacteria, and in three patients the pathogen found before therapy persisted, although sensitive to cefaclor on testing. In seven patients therapy was clinically successful although cefaclor-resistant pathogens were present before the start of therapy. In the entire group of patients investigated no increase of SGOT, SGPT, alkaline phosphatase, bilirubin, urea or creatinine was observed. In two patients alkaline phosphatase and SGOT increased slightly; in three patients SGPT increased slightly. On the other hand, in several patients initially elevated SGOT, SGPT and alkaline phosphatase activity decreased during therapy. Clinical side-effects were seen in two patients. In one patient with known penicillin allergy a pruritic exanthema developed; in the other patient, who had dermatitis herpetiformis, exacerbation of skin efflorescences occurred.

Adult↗

PubMed1978

Treatment of acute otitis media of infancy with cefaclor.

The emergence of ampicillin-resistant Haemophilus as a clinical problem in otitis media necessitates a search for alternative, effective therapy. An orally absorbable cephalosporin derivative, cefaclor, is equally effective in vitro against ampicillin-susceptible and -resistant Haemophilus and against other bacteria that cause acute otitis media. Two dosage schedules of cefaclor (40 and 60 mg/kg/day) were evaluated in 95 infants with acute otitis media. Bacterial origin was determined by a culture of tympanocentesis fluid. Success rates using the smaller dosage were inferior to those using the larger dosage. Results of therapy for pneumococcal and Haemophilus infection with 60 mg/kg/day were comparable to those previously found with amoxicillin trihydrate or with combinations of trisulfapyrimadines with erythromycin or penicillin V. One patient with an ampicillin-resistant Haemophilus infection responded well to cefaclor and did not have a relapse. Cefaclor was well tolerated and caused an acceptably low incidence of minor, adverse effects. Cefaclor deserves further testing as a candidate for preferred status as a single-drug treatment of acute otitis media.

Acute Disease↗

PubMed1979

[Serum and tissue concentrations after a single dose of cefaclor].

Serum and tissue concentrations of cefaclor were determined a total of 155 and 96 times respectively in 16 volunteers after a single dose of 1 g. At this dosage peak concentrations of 13.5, 14.5 and 13.4 mcg/ml were measured after 60, 90 and 120 minutes respectively. Tissues in which concentrations were measured included cortical bone, spongy bone, muscle, fascia, cutis and subcutis. By measuring blood concentrations of the tissue samples, a division could be made for purposes of calculation into intravascular and extravascular active components. Low amounts of extravascular cefaclor could be established merely in the fascia and in the cutis. The cefaclor concentrations found in spongy bone, muscles and subcutis proved to be determined to a large extent by the intravascular antibiotic. No cefaclor could be detected in cortical bone at the given dosage.

Bacteria↗

PubMed1979

[In vitro activity of cefaclor (author's transl)].

A comparative study was conducted on the in vitro activity of cefaclor and other oral cephalosporins against a large number of freshly isolated clinical strains of gram-negative and gram-positive bacteria. The activity of cefaclor against gram-positive pathogens is very similar to that of cephalexin. The action of cefaclor against Streptococcus pneumoniae is superior. Cefaclor is the most active antibiotic against strains of Haemophilus influenzae, and is also more active than cephalexin and cephradine against non-beta-lactamase producing strains of Escherichia coli, Klebsiella species and Proteus mirabilis.

Bacteria↗

PubMed1979

[The antibacterial efficacy of cefaclor against bacteria resistant to ampicillin, tetracycline and co-trimoxazole (author's transl)].

The antibacterial activity of the new oral cephalosporin cefaclor was investigated using 623 freshly isolated bacterial strains. A high degree of efficacy of cefaclor was noticed against Escherichia coli, Proteus mirabilis and Klebsiella. Nearly all strains which were sensitive to ampicillin, tetracycline and co-trimoxazole were also inhibited by cefaclor. Some of the strains resistant to the three above-mentioned antibiotics were also sensitive to cefaclor as follows: all of ten P. mirabilis strains resistant to co-trimoxazole, 54% of the E. coli strains resistant to ampicillin, tetracycline and co-trimoxazole, and 18% of the Klebsiella strains resistant to tetracycline and co-trimoxazole.

Cefaclor↗

PubMed1979

[Bacteriological in vitro investigations with cefaclor. Correlation of inhibition zone diameter and minimal inhibitory concentration (author's transl)].

A comparison of the minimal inhibitory concentrations (MIC) of cefaclor and cephalexin shows that cefaclor is noticeably superior against Citrobacter. Enterobacter and Proteus mirabilis. Only slight differences are seen against other enterobacteria and Staphylococcus aureus. Both cefaclor and cephalexin are completely ineffective against enterococci and Pseudomonas aeruginosa. Regression analysis to correlate the inhibition zone diameter and MIC of cefaclor produced a very good correlation (r = -0.9741). Using 30 mcg discs on DST agar, inhibition zones of more than 20 mm are to be interpreted as "sensitivity" and zones of less than 13 mm as "resistance".

Bacteria↗

PubMed1979

[Pharmacokinetics of cefaclor and initial therapeutical experience (author's transl)].

Twelve normal volunteers in the fasting state were given 1000 mg cefaclor, and the serum and urine concentrations over 8 h and 24 h respectively were measured. The average peak serum concentration was 34.6 +/- 7.8 mg/l, this value being reached after 65.2 +/- 11.1 min; the half-life was 42.5 +/- 8.3 min. In another six volunteers the absorption of 500 mg of 'cefaclor following administration in the fasting state and after a test breakfast was studied. The peak serum concentrations after administration in the fasting state were 16.1 +/- 3.2 mg/l, and after a meal 12.5 +/- 1.9 mg/l; the areas under the curve did not differ. The low recovery rate of cefaclor in urine observed in this series of investigations could be partly explained by the inactivation of the substance in urine. Cefaclor was administered therapeutically to 23 patients, most of whom were suffering from bronchopulmonary infections and chronic pyelonephritis. The results of therapy were good in four patients, satisfactory in 13 patients and unsatisfactory in three patients. Intolerance was rare.

Cefaclor↗

PubMed1979

Cefaclor in the treatment of susceptible infections in infants and children.

Fifjty-two outpatients, aged from six months to 17 years, and suffering from Group A streptococcal pharyngitis, skin and soft tissue infection, urinary tract infection, or otitis media were enrolled in the study. The dosage of cefaclor was 20 to 40 mg/kg/day in three or four divided doses for ten days. In 43 children given either cefaclor suspension or capsules, plasma level estimations were performed. Cefaclor readily produces therapeutic plasma levels in children. Cefaclor appears to be a safe, well tolerated and effective antimicrobial agent in children. It has a distinct advantage over other antibiotics in children with Haemophilus influenzae otitis media and should be considered as a primary drug in treatment of otitis media.

Adolescent↗

PubMedDate not supplied

Successful treatment with cefaclor of gonococcal urethritis in men.

Cefaclor, a new orally administered cephalosporin, was evaluated by a randomized trial for effectiveness in the treatment of uncomplicated urethritis due to Neisseria gonorrhoeae in men. Regimens included 2,3, and 4 g of cefaclor, with or without 1 g of orally administered probenecid, as single daily doses for three days. The diagnoses were confirmed by isolation of N. gonorrhoeae; cures or therapeutic failures were determined by follow-up cultures on day 7 after completion of therapy. Sixty-six (73%) of 90 treated patients were evaluable for efficacy. The bacteriologic cure rate was 98% (65/66); one patient treated with 2 g of cefaclor plus probenecid had a positive culture for N. gonorrhoeae on follow-up examination. Adverse reactions consisted of mild nausea in five patients (7%) and vomiting in one patient (1%) who received 3- or 4-g doses. No treatment was discontinued, and no abnormality of screening hematologic tests or enzymes was observed. Thus, cefaclor, given in multiple doses, was highly efficacious for treatment of uncomplicated gonococcal urethritis in men.

Cefaclor↗

PubMed1979

Cefaclor in the treatment of uncomplicated gonococcal urethritis.

Cefaclor is a cephalosporin antibiotic whose chemical structure is similar to that of cephalexin. The substitution of a chloro group for the methyl group of cephalexin has produced a compound with markedly improved antibacterial activity, while retaining the property of gastrointestinal absorption. Cefaclor has shown good in vitro activity against Neisseria gonorrhoeae. In a controlled clinical trial, 40 men with uncomplicated gonococcal urethritis received cefaclor given as a one gram loading dose, followed by 500 mg 4 times daily for 3 days, for a total dose of 7 g. All patients were re-evaluated at 3 to 7 days following completion of therapy. Two patients did not complete the entire course of therapy and were eventually treated with another regimen. Of 38 men who took the full course of therapy, 35 were clinically and bacteriologically cured. Two men were clinically infected but had negative pretreatment cultures. Of 19 men with beta-lactamase-positive gonococcal urethritis, 18 were cured, whereas among 17 men with penicillin-sensitive strains, all were cured. There were no adverse reactions to the drug, and all patients expressed a preference for the oral regimen. The success of cefaclor in this pilot study suggests that additional clinical trials should be performed.

Adult↗

PubMed1979

Comparison of cefaclor and ampicillin in the treatment of shigellosis.

Fifty-four children with acute diarrhoea were treated orally with 50 mg/kg/day of either ampicillin in 4 divided doses, or with cefaclor in 3 divided doses for 5 days. Shigella was isolated from the stool of 28 patients, 6 of whom were hospitalized. All isolates, including ampicillin-resistant strains, were susceptible in vitro to cefaclor. For ampicillin-sensitive infections, the clinical response and clearing of Shigella from stools appeared to occur more rapidly in patients treated with ampicillin than in those treated with cefaclor. In areas where ampicillin resistance is a problem, cefaclor appears not to be a drug of choice for the treatment of Shigella.

Ampicillin↗

PubMed1979

Cefaclor in the treatment of susceptible infections in infants and children.

Cefaclor is a new oral cephalosporin with in vitro activity against a wide variety of organisms including S. aureus, S. pneumoniae, S. pyogenes and H. influenzae (including ampicillin-resistant strains). Seventy-nine patients ranging in age from 2 months to 14 years with soft tissue infections (17 cases), otitis media (17), and streptococcal pharyngitis (45) were studied. They received cefaclor orally at a dose of 40 mg/kg per day in three or four divided doses for a minimum of five days. Results were generally good with favourable clinical and bacteriological responses obtained in 90% of cases. Most patients became afebrile within 48 hours after starting cefaclor. Two patients with H. influenzae cellulitis and bacteraemia defervesced within 24 hours and their blood cultures became negative promptly. Hepatic, renal and haematopoietic studies showed no adverse reactions except for an occasional increase in the eosinophil count with no clinical counterpart of hypersensitivity. Pharmacokinetic studies revealed that following a 10 mg/kg oral dose, peak serum levels of 8 micrograms/ml were observed at one hour, followed by a rather rapid tapering off so that at the end of four hours, virtually no cefaclor was detectable in serum.

Adolescent↗

PubMed1976

Metabolism of (14C) cefaclor, a cephalosporin antibiotic, in three species of laboratory animals.

The metabolic fate of the orally effective cephalosporin antibiotic cefaclor (Lilly 99638) has been studied in rats, mice, and dogs. Cefaclor is efficiently absorbed from the gastrointestinal tract as the intact antibiotic. In rats and mice, cefaclor, for the most part, escapes metabolism in the body and is eliminated unchanged as unaltered antibiotic, primarily by renal excretion. In dogs, however, cefaclor is more labile to metabolism and only a portion of the administered antibiotic is eliminated unchanged via the kidney.

Animals↗

PubMed1977

In vitro activity of cefaclor, a new orally administered cephalosporin antibiotic.

The in vitro antibacterial activity of cefaclor, cephalothin, and cephalexin against 261 clinical isolates of Staphylococcus aureus and Enterobacteriaceae was compared. Cefaclor and cephalexin were about equally active against S. aureus. Cefaclor was the most active cephalosporin against Escherichia coli, Proteus mirabilis, and Klebsiella pneumoniae. The effect on the antimicrobial activity using a relatively high and low inoculum was pronounced for cefaclor when compared with that of cephalothin.

Bacteria↗

PubMed1978

Cefaclor: in vitro spectrum of activity and beta-lactamase stability.

The in vitro activity of cefaclor against 556 clinical isolates of gram-positive and gram-negative bacteria was compared with that of other cephalosporins. Cefaclor had activity similar to that of cephalexin against gram-positive bacteria. It showed greater activity against Haemophilus strains than did cephalexin and inhibited beta-lactamase-producing Haemophilus isolates. Cefaclor was more active than cephalexin or cephalothin against Escherichia coli, Salmonella, and Shigella isolates but did not act against Serratia, Acinetobacter, indole-positive Proteus, or Bacteroides isolates. Cefaclor was resistant to type III (TEM) beta-lactamases but was destroyed by type I beta-lactamases and, to a lesser degree, by type IV and type V beta-lactamases.

Amidohydrolases↗

PubMed1978

Susceptibility of Staphylococcus aureus to cefaclor and cephalothin: laboratory and clinical studies.

In vitro susceptibility tests of 201 strains of Staphylococcus aureus by agar dilution revealed 90% to be susceptible to 8 mug or less of cefaclor per ml. Strains from hospitalized children and adults were more often resistant than those from patients with bullous impetigo. Cephalothin was more active than cefaclor against all strains tested. Results with disk tests, including those strains examined from the clinical investigation, revealed some discrepancies in identifying strains more resistant to cefaclor. In clinical studies, cefaclor proved quite effective for the treatment of bullous impetigo. Of 73 patients, 90% were cured and 7% improved after completing 5 or more days of treatment. Prompt improvement was noted among most patients seen 3 to 5 days after treatment was begun. One patient experienced mild diarrhea. There were no other adverse or toxic manifestations attributable to therapy.

Adolescent↗

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

[Treatment of bronchitis with cefaclor (Panoral) (author's transl)].

14 patients from the Allergy Unit of an outpatient clinic suffering from acute exacerbation of chronic bronchitis and 13 outpatients with acute bronchitis were treated with 250 mg cefaclor (Panoral) 3 times daily per os for 5 days. 59% of the organisms isolated from cefaclor-sensitive sputum at the time of prominent clinical symptoms were resistent to tetracycline, 53% of them were resistant to penicillin, and 37% were resistant to ampicillin. 12 out of the 14 patients with acute exacerbation of chronic bronchitis became asymptomatic, and no organisms could be detected in the sputum of 13 out of the same 14 patients two days after cessation of cefaclor treatment. In 12 out of the 13 patients with acute bronchitis, the acute clinical symptoms disappeared and in 11 out of the 13 patients the initial sputum organisms were two days after stopping cefaclor treatment.

Bronchitis↗