Cefatrizine (SK&amp;F 60771), a New Oral Cephalosporin: Serum Levels and Urinary Recovery in Humans After Oral or Intramuscular Administration – Comparative Study with Cephalexin and Cefazolin

Actor, Paul; Pitkin, Donald; Lucyszyn, George; Weisbach, Jerry A.; Bran, Jose L.

doi:10.1128/aac.9.5.800

“…Cefatrizine shows a good absorption after oral adm inistration and a longer serum half-life than cephalexin [6]. Since the penetration power of cefatrizine into tissue of the female genital tract has been insufficiently investigated, the purpose of the present study was to evaluate the capa bility of this antibiotic to reach effective concentrations in female genital tissues at several time intervals after oral adm inis tration of a fixed dose of 1 g to patients who had to undergo gynaecological sur gery.…”

Section: Introductionmentioning

confidence: 99%

Kinetics of Cefatrizine Penetration into Gynaecological Tissues after Oral Administration

Fraschini

¹

,

Scaglione

²

,

Proto³

et al. 1987

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Twenty-four patients, hospitalized in order to undergo radical gynaecological surgery, were orally administered cefatrizine in a single dose of 1 g at different times before surgery. The tissue levels determined in the organs considered (uterus, ovary, tubae, vagina) proved that cefatrizine possesses good absorption in the genital tract, reaching concentrations near to the MICs of most gram-negative and gram-positive sensitive bacteria lasting even 12 h after administration.

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“…After blood and urine samples were obtained on the morning of the study, two 500-mg capsules of cefadroxil were administered orally with 150 ml of water. Blood samples were obtained from a forearm vein at 0.5, 1,2,4,8,12,18,24, and 48 hr after drug. Urine was collected at 0 to 2, 2 to 4, 4 to 6,6 to 8,8 to 12, 12 to 18, 18 to 24, and 24 to 48 hr after cefadroxil.…”

Section: Methodsmentioning

confidence: 99%

Cefadroxil kinetics in patients with renal insufficiency

Cutler

¹

,

Blair

²

,

Kelly

³

1980

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Kinetic parameters and bioavailability of cefadroxil were studied in 20 subjects with differing renal function as measured by endogenous creatinine clearance (C crY. Two subjects were on hemodialysis. After an overnight fast, each subject ingested two 500-mg capsules of cefadroxil. The peak serum concentration was variable (12 to 57 mg/L) and correlated inversely with the C Cr-All but one patient had maximum absorption within 4 hr of ingestion and in most patients the peak was reached within the 2-hr sample. Urinary recovery within 48 hr was 45% to /06% when C Cr > 8 mllmin. Even in patients with the most severe renal failure (C Cr < 10 mllmin), urine concentrations of cefadroxil were adequate to treat susceptible bacteria. The rate of oral absorption, k a, was not affected by the state of renal function and was 0.76 ::t 0.50 hr-l. The apparent distribution volume (V d ext) was 0.28 ::t 0.09 Llkg. The plasma elimination rate was dependent on C Cr with a small fraction of drug being removed by non renal routes. Except in advanced renal failure, tubular secretion was present since renal clearance of cefadroxil exceeded C Cr. The data suggest that little drug accumulation will occur with the usual 8-to 12-hr dosing schedule except when the C Cr is less than 25 mllmin.

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“…5,1,2,4,8,12,18,24, and 48 hr after drug. The patients fasted overnight before each study and were permitted to eat no food until 4 hr after dosing.…”

Section: Methodsmentioning

confidence: 99%

“…Cefadroxil was assayed by a microbiologic procedure using a cylinder plate and Sarcina lutea (A TCC-934I) as the test organism. 12 The total amount of drug in miIligrams(Mu) excreted in any given time interval in min (tl to t 2 ) was divided by the length of the interval to get the renal excretion rate in mg/min: 1 ) This was divided by the plasma concentration at time (t l + ~)/2. 4 Pharmacokinetic analysis.…”

Section: Methodsmentioning

confidence: 99%

Cefadroxil kinetics in patients with renal insufficiency

Cutler

¹

,

Blair

²

,

Kelly

³

1979

Clin Pharma and Therapeutics

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Kinetic parameters and bioavailability of cefadroxil were studied in 20 subjects with differing renal function as measured by endogenous creatinine clearance (C crY. Two subjects were on hemodialysis. After an overnight fast, each subject ingested two 500-mg capsules of cefadroxil. The peak serum concentration was variable (12 to 57 mg/L) and correlated inversely with the C Cr-All but one patient had maximum absorption within 4 hr of ingestion and in most patients the peak was reached within the 2-hr sample. Urinary recovery within 48 hr was 45% to /06% when C Cr > 8 mllmin. Even in patients with the most severe renal failure (C Cr < 10 mllmin), urine concentrations of cefadroxil were adequate to treat susceptible bacteria. The rate of oral absorption, k a, was not affected by the state of renal function and was 0.76 ::t 0.50 hr-l. The apparent distribution volume (V d ext) was 0.28 ::t 0.09 Llkg. The plasma elimination rate was dependent on C Cr with a small fraction of drug being removed by non renal routes. Except in advanced renal failure, tubular secretion was present since renal clearance of cefadroxil exceeded C Cr. The data suggest that little drug accumulation will occur with the usual 8-to 12-hr dosing schedule except when the C Cr is less than 25 mllmin.

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Cefatrizine (SK&F 60771), a New Oral Cephalosporin: Serum Levels and Urinary Recovery in Humans After Oral or Intramuscular Administration – Comparative Study with Cephalexin and Cefazolin

Cited by 20 publications

References 9 publications

Kinetics of Cefatrizine Penetration into Gynaecological Tissues after Oral Administration

Kinetics of Cefatrizine Penetration into Gynaecological Tissues after Oral Administration

Cefadroxil kinetics in patients with renal insufficiency

Cefadroxil kinetics in patients with renal insufficiency

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