Laboratory Studies with BL-S 578 (Cefadroxil) a New Broad-Spectrum Orally Active Cephalosporin

Ripa, S.; Prenna, M.

doi:10.1159/000237816

Cited by 8 publications

(4 citation statements)

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“…In vitro, it exhibits activity against most strains of Streptococcus pneumoniae, Streptococcus pyogenes, Escherichia coli, Klebsiella sp., and both penicillin-susceptible and resistant Staphylococcus aureus (2,7). The objective of this study was to characterize the pharmacokinetic properties of cefadroxil administered orally in doses -of 250, 500, and 1,000 mg to healthy male volunteers.…”

mentioning

confidence: 99%

Pharmacokinetics of cefadroxil after oral administration in humans

Rosa¹,

Ripa²,

Prenna³

et al. 1982

Antimicrob Agents Chemother

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The human oral pharmacokinetics of cefadroxil were studied in parallel at doses of 250, 500, and 1,000 mg in three groups of 10 healthy young male volunteers. Renal excretion of intact cefadroxil, accounted for 82, 79, and 77% of the above doses. Mean peak serum levels were dose linear: 9, 18, and 35 ,ug/ml at 250, 500, and 1,000 mg, respectively. However, overall pharmacokinetics were linear only in the 250-to 500-mg dose range; apparent serum clearances were 10 liters/h, and true renal clearances were 9 and 8 liters/h at 250 and 500 mg. At 1,000 mg, apparent serum clearance dropped to about 7 liters/h, true renal clearance, dropped to 6 liters/h, and the area under the curve increased disproportionately. At 250 and 500 mg, mean half-life was about 1.2 h; at 1,000 mg, however, it was 1.6 h. The nonlinear decrease in clearance could be related to saturation of active renal tubular secretion of cefadroxil between the 500-and 1,000-mg doses. Previous results indicating that cefadroxil has greater persistence than other oral cephalosporins such as cephalexin, cephradrine, cefaclor were confirmed.acid monohydrate, is a semisynthetic cephalosporin intended for oral administration. In vitro, it exhibits activity against most strains of Streptococcus pneumoniae, Streptococcus pyogenes, Escherichia coli, Klebsiella sp., and both penicillin-susceptible and resistant Staphylococcus aureus (2, 7). The objective of this study was to characterize the pharmacokinetic properties of cefadroxil administered orally in doses -of 250, 500, and 1,000 mg to healthy male volunteers. MATERUILS AND METHODSCefadroxil monohydrate was supplied as formulated 250-mg capsules (Bristol Italiana Sud-Spa). Doses of 250, 500, and 1,000 mg were administered orally to 30 male volunteers, 20 to 29 years of age. None had known sensitivity to 3-lactam antibiotics. All were judged healthy on the basis of clinical examination, urinalysis, and serum chemistry analyses (i.e., hemoglobin, erythrocyte sedimentation rate, leukocyte count, eosinophil count, differential count, bilirubin, serum creatinine, blood urea nitrogen, alkaline phosphatase, lactic acid dehydrogenase, aspartate aminotransferase, alanine aminotransferase, serum iron, total iron-binding capacity, cholesterol, and total protein). Each provided informed consent.Experimental procedure. The 30 volunteers were divided into three groups of 10. In a parallel study, each member of the group received oral cefadroxil doses of 250, 500, or 1,000 mg after overnight fasting.Blood samples were collected at 0.5, 1, 2, 4, 6, and 7 h after dosing. Serum samples were prepared and stored at -20°C until assayed. A total 0 to 7 h urine collection was made.Assay procedure. Cefadroxil concentrations were estimated by bioassay, using a disk plate method (3). Antibiotic assay base agar (210 ml) was seeded with a static culture of Sarcina lutea ATCC 9341 in Trypticase soy broth (4 ml; BBL Microbiology Systems) after overnight incubation of the culture at 37°C. The seeded base agar was placed into 23-cm2 assay plat...

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mentioning

confidence: 99%

Pharmacokinetics of cefadroxil after oral administration in humans

Rosa¹,

Ripa²,

Prenna³

et al. 1982

Antimicrob Agents Chemother

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“…Surveillance is covert if "it is carried out in a manner that is calculated to ensure that persons who are subject to the surveillance are unaware that it is or may be taking place". 189 Under the Regulation of Investigatory Power Act 2000 (RIPA), directed surveillance is one of the recognised forms of covert surveillance. 190 It is undertaken:…”

Section: Appropriate Transparency Overt Use Of Lfr and The Alternativementioning

confidence: 99%

Regulating Use by Law Enforcement Authorities of Live Facial Recognition Technology in Public Spaces: An Incremental Approach

Gikay

2023

C.L.J.

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Amid the growing calls for the complete prohibition of the use by law enforcement authorities of live facial recognition (LFR) technology in public spaces, this article advocates for an incremental approach to regulating the use of the technology. By analysing legislative instruments, judicial decisions, deployment practices of UK law enforcement authorities, various procedural and policy documents, as well as available safeguards, the article suggests incremental adjustments to the existing legal framework instead of sweeping regulatory change. The proposed approach calls for adopting national legal rules governing watch lists and introducing spatial, temporal and contextual limitations on the deployment of technology based on the assessment of proportionality and necessity. To enhance the effectiveness of overt surveillance using LFR, the article recommends adopting a transparency procedure that promotes accountability without undermining the objectives of law enforcement. Alternatively, the overt use of the technology should be limited to deterring the commission of crimes and safeguarding public safety, where transparency does not undermine its effectiveness. Limiting the scope of overt use of LFR technology entails that law enforcement agencies primarily utilise covert surveillance, with prior judicial approval, except in urgent cases, as this would improve effective criminal investigation and public safety. The legal adjustments proposed in this article can be implemented through flexible secondary legislation or local policies, rather than rigid statutory rules.

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“…This semisynthetic and first-generation aminocephalosporin was shown more effective and resistant to β-lactamases than cephalexin against certain bacteria (Ripa and Prenna, 1979). It has been commonly used in the treatment of different kinds of infections including skin, respiratory and urinary tract infections (Tanrisever and Santella, 1986).…”

Section: Introductionmentioning

confidence: 99%

Population pharmacokinetic modeling of cefadroxil renal transport in wild-type andPept2knockout mice

Xie

Shen

et al. 2015

Xenobiotica

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Cefadroxil is a broad-spectrum β-lactam antibiotic that is widely used in the treatment of various infectious diseases. Currently, poor understanding of the drug’s pharmacokinetic profiles and disposition mechanism(s) prevents determining optimal dosage regimens and achieving ideal antibacterial responses in patients. In the present retrospective study, we developed a population pharmacokinetic model of cefadroxil in wildtype and Pept2 knockout mice using the NONMEM approach.Cefadroxil pharmacokinetics were best described by a two-compartment model, with both saturable and nonsaturable elimination processes to/from the central compartment. Through this modeling approach, pharmacokinetic parameters in wildtype and Pept2 knockout mice were well estimated, respectively, as: volume of central compartment V1 (3.43 vs. 4.23 mL), volume of peripheral compartment V2 (5.98 vs. 8.61 mL), inter-compartment clearance Q (0.599 vs. 0.586 mL/min), and linear elimination rate constant K10 (0.111 vs. 0.070 min−1). Moreover, the secretion kinetics (i.e., Vm1 = 17.6 nmoL/min and Km1 = 37.1 μM) and reabsorption kinetics (i.e., Vm2 = 15.0 nmoL/min and Km2 = 27.1 μM) of cefadroxil were quantified in kidney, for the first time, under in vivo conditions.Our model provides a unique tool to quantitatively predict the dose-dependent nonlinear disposition of cefadroxil, as well as the potential for transporter-mediated drug interactions.

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Laboratory Studies with BL-S 578 (Cefadroxil) a New Broad-Spectrum Orally Active Cephalosporin

Cited by 8 publications

References 2 publications

Pharmacokinetics of cefadroxil after oral administration in humans

Pharmacokinetics of cefadroxil after oral administration in humans

Regulating Use by Law Enforcement Authorities of Live Facial Recognition Technology in Public Spaces: An Incremental Approach

Population pharmacokinetic modeling of cefadroxil renal transport in wild-type andPept2knockout mice

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