Renal tolerance of cefpirome (HR 810), a new cephalosporin antibiotic

Verho, M; Maass, L.; Malerczyk, V.; Grötsch, H.

doi:10.1007/bf01646054

Cited by 10 publications

(9 citation statements)

References 12 publications

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“…The renal tolerance was good, confirm ing the results found earlier with a lower dose of cefpirome [6]. The values for serum f)2-microglobulin levels and creati nine clearance remained unchanged.…”

Section: Discussionsupporting

confidence: 74%

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Safety, Tolerance and Pharmacokinetics of 2.0 g Cefpirome (HR 810) after Single and Multiple Dosing

Badian¹,

Malerczyk

Collins³

et al. 1988

Chemotherapy

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After intravenous injection of a single dose of 2.0 g cefpirome (HR 810) and multiple doses of 2.0 g b.i.d. (11 doses) to 10 healthy male volunteers in an open design, concentrations of unchanged drug were measured at various times in serum and urine over 24 and 96 h, respectively. Cefpirome concentrations were determined using high-pressure liquid chromatography (HPLC). The biological half-life (t_½,β) found by fitting a two-compartment open model to the data was 2 h. No accumulation of the serum levels could be detected during the multiple-dose phase. Urinary concentrations of unchanged cefpirome effective against most clinically relevant bacteria were detected for at least 36 h. The drug was safe and well tolerated. No drug-related changes were observed for blood pressure, heart rate, ECG, haematology, clinical chemistry or urinalysis, including β₂-microglobulin in serum and creatinine clearance.

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Section: Discussionsupporting

confidence: 74%

“…Cefpirome was found to have dose-lin ear kinetics with a half-life of about 2 h and is largely eliminated via the kidneys, almost completely as unchanged drug [3][4][5]. The renal tolerance was good [6],…”

Section: Introductionmentioning

confidence: 99%

Safety, Tolerance and Pharmacokinetics of 2.0 g Cefpirome (HR 810) after Single and Multiple Dosing

Badian¹,

Malerczyk

Collins³

et al. 1988

Chemotherapy

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“…Oxilofrine [1‐(4‐hydroxyphenyl)‐2‐methylaminopropa‐nol] (Fig. ), also known as methylsynephrine or 4‐hydroxyephedrine, is an isomer of etilefrine with similar pharmacological properties . Recently, there have been a few high profile positive findings of oxilofrine in human competitive sports [http://www.espn.co.uk/athletics/sport/story/273773.html.…”

Section: Introductionmentioning

confidence: 99%

“…Both, etilefrine and oxilofrine could be used as stimulants in endurance sports. However, due to their increased polarity, they do not cross the blood–brain barrier readily . The bioavailability is also reduced markedly when administered orally due to first pass effect .…”

Section: Introductionmentioning

confidence: 99%

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Development and validation of a hydrophilic interaction liquid chromatography with tandem mass spectrometry method for the simultaneous detection and quantification of etilefrine and oxilofrine in equine blood plasma and urine

Kong

Rong

Zhao

et al. 2014

J of Separation Science

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A sensitive hydrophilic interaction liquid chromatography coupled with tandem mass spectrometry method was developed and validated for the simultaneous detection and quantification of etilefrine and oxilofrine in equine blood plasma and urine. The method is highly sensitive and specific with good precision and accuracy. In plasma the limit of detection and limit of quantification are 0.03 and 0.1 ng/mL, respectively, for both analytes. In urine the limit of detection and limit of quantification are 0.3 and 1 ng/mL, respectively, for both analytes. The suitability of the method for doping control analysis in equine species is demonstrated by analyzing postadministration samples collected after a single intravenous administration of 50 mg etilefrine to a standardbred mare. Etilefrine was detected up to 120 h in urine and up to 48 h in plasma. Etilefrine is highly conjugated in equine urine whereas it exists in the free form in equine plasma. Therefore, enzyme hydrolysis prior to sample preparation is recommended for the detection and quantification of etilefrine and oxilofrine in equine urine.

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Single‐ and Multiple‐Dose Pharmacokinetics of Intravenous Cefpirome (HR810) to Healthy Volunteers

Nakayama

Akieda²,

Yamaji

et al. 1992

The Journal of Clinical Pharma

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The safety and pharmacokinetics of single and multiple administrations of cefpirome (HR810), a new cephalosporin antibiotic agent with a broad antibacterial spectrum, were studied in healthy male volunteers. The single administration protocols included a 3-minute intravenous injection of 0.5 g or 1 g, and a 1-hour intravenous drip infusion of 0.5 g, 1 g, or 2 g. The multiple administration protocols included nine intravenous injections and 1-hour intravenous drip infusions of 1 g of cefpirome twice a day at intervals of 12 hours. Cefpirome was tolerated, and only a few mild, subjective and hepatic-function side effects were observed. There were no severe abnormalities. The drug concentrations in the plasma and the urine were determined by means of HPLC and bioassay, and the results correlated well (r = 0.99). The pharmacokinetic parameters were calculated using a two-compartment model. The elimination half-life (t1/2 beta) was about 1.7 hours for both intravenous injection and intravenous drip infusion and was not dose-dependent. AUC and Cmax were dose-dependent in this study, although an accumulation due to multiple administrations was not observed, and there were no changes in the pharmacokinetic parameters after the initial and the final administrations. The recovery rate of the unchanged compound in the urine was more than 80% in the 24 hours after a single administration and was the same after multiple administrations. Bioautography did not show any active metabolites in the plasma or the urine. The results, for safety and pharmacokinetics, show that cefpirome can be expected to have excellent clinical efficacy for bacterial infections.

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Renal tolerance of cefpirome (HR 810), a new cephalosporin antibiotic

Cited by 10 publications

References 12 publications

Safety, Tolerance and Pharmacokinetics of 2.0 g Cefpirome (HR 810) after Single and Multiple Dosing

Safety, Tolerance and Pharmacokinetics of 2.0 g Cefpirome (HR 810) after Single and Multiple Dosing

Development and validation of a hydrophilic interaction liquid chromatography with tandem mass spectrometry method for the simultaneous detection and quantification of etilefrine and oxilofrine in equine blood plasma and urine

Single‐ and Multiple‐Dose Pharmacokinetics of Intravenous Cefpirome (HR810) to Healthy Volunteers

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