Pharmacokinetics of cefuroxime axetil and cefaclor: relationship of concentrations in serum to MICs for common respiratory pathogens

James, N C; Donn, Karl H.; Collins, Jeffrey J.; Davis, Ian M.; Lloyd, Thomas L.; Hart, R. W.; Powell, J. Robert

doi:10.1128/aac.35.9.1860

Cited by 31 publications

(17 citation statements)

References 19 publications

(44 reference statements)

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“…The ANOVA analysis with 90% CI for C max , T max , AUC 0-t , AUC 0-∞ and AUMC, on log transformed data of both the formulations, is mentioned in Table 3. The PK parameters were in agreement to the previously published data [17][18][19][20].…”

Section: Resultssupporting

confidence: 82%

“…The relative bioavailability was 93.89 %. Variation was also observed for the PK data reported among fed state subjects [6,20] and with those given a 500 mg dose [18,21, published data [17][18][19][20]. Although some reports in the literature shows similar studies, but pharmacokinetic studies of 250 mg cefuroxime axetil oral formulation among fasted healthy Pakistani volunteers was not reported.…”

Section: Discussionmentioning

confidence: 73%

“…Pharmacokinetic parameters such as C max , T max , and AUC 0-∞ were found to be slightly different with that of reported one i.e. Sung et al in 1999 observed C max value of 3.69 ± 0.75µg/ml, T max and AUC 0-∞ values of 1.76 ± 0.99hr and 12.20 ± 3.28 mg/L.hr [21], similarly James et al in 1991 reported Cmax, Tmaxand AUC values of 4.19 ± 0.30 µg/ml, 1.39 ± 0.14 hr and 12.66 ± 0.67 mg/L.hr [19]. The relative bioavailability was 93.89 %.…”

Section: Discussionmentioning

confidence: 88%

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Pharmacokinetic and Bioequivalence Studies of Oral Cefuroxime Axetil 250 mg Tablets in Healthy Human Subjects

Muhammad¹,

Shoaib²,

Yousuf³

2014

J Bioequiv Availab

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Section: Resultssupporting

confidence: 82%

Section: Discussionmentioning

confidence: 73%

Section: Discussionmentioning

confidence: 88%

See 1 more Smart Citation

Pharmacokinetic and Bioequivalence Studies of Oral Cefuroxime Axetil 250 mg Tablets in Healthy Human Subjects

Muhammad¹,

Shoaib²,

Yousuf³

2014

J Bioequiv Availab

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“…The MIC so of cefaclor for most of the infections treated by cefaclor is 2 ug/ml (13), hence the calculation of time to reach MIC so and time above MIC so ' 2 ug/ml was used. The individual and mean (SD) of time above MIC so values for all the five treatments are tabulated in Table III.…”

Section: Pharmacokinetic and Pharmacodynamic (Pk-pd) Analysismentioning

confidence: 99%

The effect of four different types of food on the bioavailability of cefaclor

Karim

Ahmed

Monif³

et al. 2003

Eur. J. Drug Metab. Pharmacokinet.

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This randomized, open-label, balanced, five-treatment, five-period, five-sequence, single-dose and crossover pharmacokinetic study assessed the effect of different types of food on the bioavailability of cefaclor in 18 healthy male volunteers. A single dose of cefaclor, 250-mg capsule was administered at five occasions: after overnight fasting, after two vegetarian (high-fat and low-fat) diets and two non-vegetarian (high-fat and low-fat) diets. Serial blood samples were collected upto 8 h post dose. Serum cefaclor concentrations were determined by a validated HPLC method. AUC values were not significantly affected by food intake, but the T(max) was prolonged and C(max) was decreased, depending on the type of meal. The non-vegetarian diets affected the rate of absorption of cefaclor more than the vegetarian diets. The least decrease in C(max) was produced by low-fat vegetarian diet, while the maximum decrease was produced by high-fat non-vegetarian diet. The results of this study indicate that while the rate of absorption of cefaclor is significantly decreased, the extent of absorption and the rate of elimination are not significantly decreased in the presence of food. As compared to high-fat non-vegetarian diet, the time above MIC50 concentration was significantly increased by low-fat vegetarian diet. The implications of these findings for the large vegetarian Indian population are considerable.

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“…[3,4] Cefpirome is extensively used in human beings against infections caused by susceptible organisms for a prolonged period. [5] Although various researchers have worked on the pharmacokinetic aspects of the drug, [6] its effects on biochemical parameters and spermatozoa activity are scarcely available in the literature. [7] Taking all these into considerations, the present study was undertaken to determine the oral kinetic (blood and tissue), tissue half-life, and certain biochemical parameters such as glucose, hemoglobin, protein, ALT, AST, and sperm count in rats with the aim to generate data which could be extrapolated to studies on human beings.…”

mentioning

confidence: 99%

Pharmacokinetic Study of Cefpirome: Fourth Generation Cephalosporin

Mujeeb¹,

Jalikar²

2015

jemds

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Studies on oral kinetics (Blood and tissues) after single therapeutic dose of cefpirome (20mg/kg oral) in rats of either sex and on some biochemical parameters, tissue residue, and spermatozoa motility in male rats after cefpirome administration (20mg/kg oral bid 7days) were undertaken so that generated data could be extrapolated to humans. For kinetic studies, 24 Wister rats of either sex, 3 months of age, (180-210gm) were used (Groups I-IV; n=6). Blood samples collected from each animal of Group I-IV at 0 h to serve as predrug control. All the groups (I-IV) received cefpirome 20mg/kg once orally as a single dose. At the end of 1, 4, 12, and 24 hour post oral administration, Groups I, II, III, and IV were utilized for kinetic studies. Blood samples were collected from each animal and vital organs namely brain, lung, liver, spleen, kidney, and heart, were studied for drug analysis and determination of weight. For biochemical parameters, tissue residue and spermatozoa motility, 12male rats were randomly divided into Groups A and B (n=6). Group B received cefpirome (20mg/kg orally bid 7 days) while Group A served as control. Biochemical parameters [Blood glucose, protein, Aspartate transaminase (AST), Alanine transaminase (ALT), and hemoglobin] were measured at 0 and 7 th day while sperm count (Total, live and dead) and mean organ weight (Study and control group) and tissue residue of drug were evaluated at the end of treatment. Absorption of cefpirome was observed at 2h and reached a maximum at 4h and persisted in blood till 24h. Elimination half-life in lung was highest followed by heart, liver, kidney, and spleen while t½, k in plasma was very low suggesting more affinity of cefpirome for tissues than blood. Blood glucose, protein, AST, and ALT activities were not significantly altered but the hemoglobin level and total and live sperm count decreased significantly in the study group compared to the control group. Residual level of cefpirome was highest in liver followed by kidney and other study organs. Therefore, the drug should be used in human beings judiciously.

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Pharmacokinetics of cefuroxime axetil and cefaclor: relationship of concentrations in serum to MICs for common respiratory pathogens

Cited by 31 publications

References 19 publications

Pharmacokinetic and Bioequivalence Studies of Oral Cefuroxime Axetil 250 mg Tablets in Healthy Human Subjects

Pharmacokinetic and Bioequivalence Studies of Oral Cefuroxime Axetil 250 mg Tablets in Healthy Human Subjects

The effect of four different types of food on the bioavailability of cefaclor

Pharmacokinetic Study of Cefpirome: Fourth Generation Cephalosporin

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