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Results for “Cephalexin”

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At least 19 recordsLinked to original sources

PubMed1979

Penetration of antibiotic into interstitial tissue fluid following parenteral administration of lysine cephalexin.

Serum and interstitial fluid levels of antibiotic have been measured at various times following i.m. administration of equivalent doses of lysine cephalexin and sodium ampicillin, in a cross-over design, to dogs fitted with s.c. implanted silastic "tissue cages" and the results subjected to pharmacokinetic analysis. Serum concentrations of cephalexin were consistently higher than those of ampicillin and elimination half-lives were calculated as 1.73 h and 0.87 h, respectively. The rate of appearance of cephalexin in the interstitial fluid (Ka 1.741 h-1 was faster than that for ampicillin (Ka 0.946 h-1) and the maximum concentration obtained also proved to be higher. The half-life of cephalexin in the interstitial fluid (6.79 h) was almost four times longer than that in serum whereas that of ampicillin (2.03 h) was only a little more than twice as long. As a consequence a greater concentration and retention in interstitial fluid was obtained with cephalexin at all times tested. Since the interstitial fluid levels of cephalexin were still relatively high 8-12 h after the administration of a single dose repeated administration of lysine cephalexin 2 or 3 times daily is expected to result in a beneficial accumulation of cephalexin in the interstitial fluid.

Ampicillin↗

PubMed1978

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

S-6437 (Sustained release cephalexin granule for pediatric use) was studied with the following results: 1) Following the single oral administration of 25 mg/kg of S-6437 in 6 children 4 approximately 6 years old, the following blood levels (average) of cephalexin were obtained: 3.1 microgram/ml in one hour after the administration, 8.6 microgram/ml in 2 hours, 8.7 in 4 hours, 7.2 in 6 hours, 4.0 in 8 hours and 1.2 in 12 hours. Effective blood levels of cephalexin by S-6437 were maintained for longer period of time than those by regular cephalexine dry syrup. In 4 of 6 children receiving S-6437, cephalexin was scarcely detected in their blood in 12 hours after the administration. From this, it is not considered that S-6437 is accumulated in body. 2) S-6437 was administered to 38 patients including: 7 with pneumonia, 7 with acute bronchitis, 1 with suppurative lymphadenitis, 4 with acute pharyngitis, 15 with acute tonsillitis and 4 with acute urinary tract infections. Out of the 35 cases, 31 (88.6%) responded to S-6437, and 3 cases could not be evaluated. 3) Transient diarrhea in 2 patients, rash in 1 and elevation of serum GOT, GPT and LDH in 1 were observed. However, these side effects were improved by discontinuation of S-6437.

Age Factors↗

PubMed1976

Cephalexin compared to ampicillin treatment of otitis media.

Cephalexin was compared to ampicillin for the treatment of otitis media in a randomized study. Bacteriologic diagnosis was sought by needle tympanocentesis in 179 children. No overall statistically significant differences were noted between the two groups; however, 20 patients who received cephalexin had a poor response to therapy whereas only five recipients of ampicillin responded poorly. A significant difference (P less than .05) between the two regimens was noted when Hemophilus influenzae was recovered. Fifty per cent of the children with H. influenzae otitis media who were treated with cephalexin responded poorly; no patients receiving ampicillin had a poor response. Our data suggest that the use of cephalexin monohydrate is not warranted for treatment of otitis media due to H. influenzae even when the isolate proves sensitive to this drug in vitro. In selected patients with otitis media caused by Staphylococcus aureus which is resistant to penicillin, cephalexin may provide effective treatment.

Ampicillin↗

PubMed1978

Quantitative determination of cephalexin in cephradine by NMR spectroscopy.

An NMR method to determine quantitatively the presence of cephalexin in cephradine was developed. The method is applicable to the chemical itself as well as to capsules and oral suspension formulations. The determination is based on the NMR signal arising from the five aromatic protons of the cephalexin molecule. Integration of this signal relative to a signal from cephradine provides the data necessary to determine the percentage of cephalexin present. The precision at the 2% cephalexin levels is +/- 0.18%. The time required to carry out a single analysis is about 10 min, and five analyses can be done in about 0.5 hr.

Capsules↗

PubMed1979

[Aqueous-and serum levels of cephalexin and penicillin V after oral application in man (author's transl)].

This clinical study implies orally administered cephalexin and penicillin V as agents with effective aqueous homor penetration in noninfected human eyes. Aqueous humor concentration of cephalexin increases up to 15% of the serum level 2 h after application. Administration of 1 g or 2 g cephalexin revealed no significant difference in aqueous humor concentration. So penetration of blood-aqueous-humor barrier can be regarded as a saturation process. Individual results of 92 cephalexin determinations are variant and not related to body weight or age of the patients.

Aged↗

PubMed1979

[Subinhibitory activity of cefaclor and cephalexin (author's transl)].

The determination of the minimal inhibitory concentration (MIC), which is usually performed after 18 to 24 hours of incubation, results in the case of cefaclor in a false picture of the actual activity. Cefaclor is chemically so unstable that after 24 hours only 2-5% of the substance is microbiologically active. In order to compare the activity of cefaclor and cephalexin, the effect of subinhibitory concentrations of both antibiotics against Escherichia coli and Klebsiella pneumoniae strains was studied by means of turbidimetry. After eight hours the absolute inhibitory concentration of cefaclor was lower than that of cephalexin with both methods. At the same time the effect of subinhibitory concentrations of both antibiotics was equal. Automatic measurement over 20 hours showed at the end of the experiment a higher MIC, and also a higher subinhibitory range, for cefaclor than for cephalexin. In our opinion the absolute inhibitory concentration after eight hours should be the criterion used to evaluate the effectiveness of cefaclor and cephalexin, and not the MIC which is usually used. The eight-hour criterion should also be applied in clinical use.

Cefaclor↗

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↗

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↗

PubMed1977

[Electron microscopic study of the combined action of ampicillin and cephalexin on E. coli].

The data of electron microscopy study of morphological variation of E. coli, strain 423 in the logarithmic phase after exposure to ampicillin (2 gamma/ml) and cephalexin (4 gamma/ml) are presented. Pronounced ultrastructural changes not only in the cell wall but also in the cytoplasm were found. After exposure to ampicillin alone changes of the same type were observed. However, after exposure to the combination of the 2 antibiotics these changes were more pronounced and observed in the predominating part of the cells. Examination of ultrathin slices of the strain treated with cephalexin revealed no ultrastructural changes. The morphological changes in the cells of E. coli, strain 423 after its treatment with ampicillin and cephalexin combination were due mainly to ampicillin effect, while cephalexin increased the level of the changes.

Ampicillin↗

PubMed1979

[Oral cephalexin therapy of osteomyelitis (author's transl)].

40 patients with chronic osteomyelitis were treated per os with the bactericidal beta-lactam-antibiotic cephalexin during 3 to 60 weeks. In 16 patients, who were operated simultaneously, bacterial spreading was prevented by a combination of cephalexin and parenteral cephaloridin during operation and in the postoperative period. In these patients no recurrence occurred during the follow up time (2 to 5 years). In 34 patients general and local signs of inflammation diminished under cephalexin therapy and a complaint-free interval of at least 6 months followed. No serious side effects forcing a stop of therapy were observed. According to the gained experiences oral cephalexin in combination with perenteral cephaloridin is indicated for prevention of bacterial spreading during operations in chronic bone infections and in patients with acute febrile recurrence of chronic osteomyelitis refusing a surgical intervention.

Administration, Oral↗

PubMed1979

[Comparative study of cephalexin and cephradine distribution in the body of rats].

Distribution regularities of cephalexin and cephradine, 2 semisynthetic cephalospor in antibiotics for oral use were studied on rats. It was found that the cephalosporins had a capacity for satisfactory penetration through the histochematological barriers. The drugs were rather rapidly absorbed from the gastrointestinal tract of the rats into the blood. Their maximum blood levels were determined 1 hour after the administration. The highest cephalosporin concentrations were detected in the kidneys and liver. Still, the level of cephradine in the kidneys was lower and that in the liver was higher than the levels of cephalexin. The lowest concentrations were found in the skeletal muscles. The character of cephradine distribution in the lungs, heart and spleen differed from that of cephalexin; the maximum concentrations of cephradine in these organs were achieved 1 hour after its administration, while those of cephalexin were achieved in 30 minutes. The antibiotics were not detected in the brain tissue. No increase in the concentration gradient with time was observed.

Administration, Oral↗

PubMed1978

Pharmacokinetics of oral cephalosporins: cephradine cephalexin.

A crossover experiment was utilized to compare the pharmacokinetics of a 1-g dose of cephalexin tablets, cephalexin capsules, or cephradine capsules in nine normal human volunteers. These antibiotics were administered as three formulations: two 500-mg capsulin every 6 hr for five doses, and one 1000-mg tablet of cephalexin every 6 hr for five doses. Pharmacokinetic parameters in the experimental groups showed no statistical differences (p greater than 0.1), indicating that these drugs are equivalent pharmacokinetically.

Administration, Oral↗

PubMed1978

Clinical comparison of cefadroxil, new oral cephalosporin, and cephalexin in uncomplicated urinary tract infection.

Efficacy and safety of cefadroxil, a new oral cephalosporin, were compared with that of cephalexin in the treatment of 28 women with acute urinary tract infections. According to a randomized double-blind design, each patient received cefadroxil 1,000 mg. twice daily or cephalexin 500 mg. four times a day for ten days. Cures based on urine culture five to nine days post-treatment were obtained for all but 1 patient receiving cefadroxil; reinfection after eradication of the original pathogen was recorded for only 1 patient in each treatment group. No drug-related side effects or significant clinical laboratory abnormalities were observed during the study. Cefadroxil 1,000 mg. given twice daily was as effective and as well tolerated as cephalexin 500 mg. given four times daily. The significance of this dosage schedule advantage is discussed.

Administration, Oral↗

PubMed1977

The comparative efficacy of cephalexin and sulfisoxazole in acute urinary tract infection in children.

A double blind, comparative study of the efficacy of cephalexin versus sulfisoxazole was conducted on 100 children with initial episodes of urinary tract infections. The overall bacteriologic and clinical cure rates were comparable for both antimicrobials. Children treated with cephalexin had a clinical cure rate of 86 per cent and a bacterial cure rate of 84 per cent, while those given sulfisoxazole were found to have rates of 82 and 92 per cent respectively. However, cephalexin was noted to have a rather high rate of failure in the therapy of Proteus micrabilis infections (4/8), casting some doubt on its use in urinary infections caused by the organism. Untoward effects associated with either medication were minimal.

Acute Disease↗

PubMed1979

Concentrations of cephalexin in mandibular alveolar bone, blood, and oral fluids.

Results from this study of 16 patients who underwent extractions and alveoloplasty indicate that cephalexin effectively penetrates alveolar bone. After cephalexin had been administered, 500 mg four times a day for 48 hours, the average concentration in bone exceeded the average minimal inhibitory concentration of six organisms commonly encountered in infections and bacteremias of dental origin. These data and the current knowledge of cephalexin suggest that cephalosporins may have a unique use in dental infections or potentially harmful bacteremias caused by susceptible organisms.

Adult↗

PubMed1978

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

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

Cephalexin↗

PubMed1978

Kinetics of degradation of cefazolin and cephalexin in aqueous solution.

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

Buffers↗