A pharmacokinetic and tolerance study of Ro13‐9904, a new cephalosporin antibiotic.

Pickup, M. E.; Bird, H. A.; Lowe, J. R.; Lees, L.; Wright, V.

doi:10.1111/j.1365-2125.1981.tb01188.x

Cited by 21 publications

(6 citation statements)

References 7 publications

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“…Although none of our patients developed diarrhea, two had abdominal cramps. Transient proteinuria, which occurred in two patients, was also reported by Pickup et al (7). It will be important to monitor renal function and hematology when patients are on prolonged treatment with ceftnaxone.…”

Section: Resultsmentioning

confidence: 83%

Kinetic disposition of intravenous ceftriaxone in normal subjects and patients with renal failure on hemodialysis or peritoneal dialysis

Ti¹,

Fortin²,

Kreeft³

et al. 1984

Antimicrob Agents Chemother

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The kinetic disposition of a single intravenous dose of ceftriaxone (250 to 665 mg) was studied in six normal subjects and nine patients with renal insufficiency and normal hepatic function. In normal subjects, ceftriaxone was eliminated with a t1/20 of 5.2 h (range, 4.1 to 5.8). The total body clearance (Qb) was 13.5 ml/kg per h (range, 8.4 to 23.3), and renal clearance was 8.3 ml/kg per h (range, 5.8 to 13.3). In patients with severe renal insufficiency requiring peritoneal or hemodialysis, the mean tl2p was prolonged to 13.4 h (range, 7.7 to 15.8) and the mean Qb was reduced to 6.9 ml/kg per h (range, 3.4 to 12.8). The apparent volumes of distribution (V, and V5,) were not different from those determined in normal subjects. Peritoneal dialysis did not remove ceftriaxone. The dialysate of three patients on continuous peritoneal dialysis did not contain any measurable ceftriaxone, and the kinetic disposition in these patients was similar to the hemodialysis patients between their dialysis treatment. During a 4-h hemodialysis session, the total body clearance of ceftriaxone was reduced, perhaps secondary to a decrease in hepatic blood flow induced by the hemodialysis procedure. After a 12-or 24-h dose regimen, predicted trough concentrations of ceftriaxone in plasma at steady state derived from kinetic data generated from the study and assuming linear pharmacokinetic behavior were well above the minimum inhibitory concentrations of most sensitive bacteria, suggesting the feasibility of a once-a-day dosage regimen especially for patients with severe renal insufficiency.

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Section: Resultsmentioning

confidence: 83%

Kinetic disposition of intravenous ceftriaxone in normal subjects and patients with renal failure on hemodialysis or peritoneal dialysis

Ti¹,

Fortin²,

Kreeft³

et al. 1984

Antimicrob Agents Chemother

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“…At 300 and 600 ,ug/ml, ceftriaxone is 84 and 58% bound to plasma protein, respectively (10,14). The pKa for ceftriaxone is between 2.0 and 4.5 (13,14).…”

Section: Resultsmentioning

confidence: 99%

“…The pKa for ceftriaxone is between 2.0 and 4.5 (13,14). At a physiological plasma pH of 7.4, ceftriaxone exists predominantly in the ionized state.…”

Section: Resultsmentioning

confidence: 99%

“…dose of ceftriaxone is completely absorbed. However, ceftriaxone has been shown to display nonlinear kinetics due to concentration-dependent plasma protein binding (4,13,14). At plasma concentrations above 150 pug/ml, an increase in the unbound fraction of ceftriaxone together with an increase in total plasma clearance has been demonstrated (14).…”

Section: Resultsmentioning

confidence: 99%

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Single-dose pharmacokinetics of ceftriaxone in healthy Chinese adults

Zhou¹,

Chan²,

Arnold³

et al. 1985

Antimicrob Agents Chemother

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The pharmacokinetics of ceftriaxone were investigated in six healthy mainland Chinese adults (four males and two females). A single 1.0-g dose was administered intravenously or intramuscularly in a two-way crossover design. Plasma and saliva samples were collected on 11 occasions between 0 and 36 h after dosing.Ceftriaxone was not detected in any saliva samples. The mean volume of distribution and mean elimination half-life of ceftriaxone in plasma were 8.5 liters and 8.1 h, respectively. The mean total body clearance after intravenous administration was 0.68 liter/h. The mean Tmax and Cmax after intramuscular injection were 1.4 h and 131 ,ug/ml, respectively. The area under the plasma concentration-time curves after intravenous and intramuscular administrations were 1,507 and 1,493 ,Ig h/ml, respectively. The bioavailability for a 1.0-g intramuscular dose of ceftriaxone was calculated to be 100%. These pharmacokinetic parameters for ceftriaxone in healthy Chinese adults were very similar to those previously reported in the literature. Thus, ceftriaxone may be administered to treat Chinese patients without any major modification in the standard dosing regimen.

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“…As noted by others [6], ceftriaxone is particularly well tolerated when adminis tered in a dosage of 1 g daily. An advan tage of this ceftriaxone regimen may prove to be freedom from those side effects such as diarrhea that are commonly observed with many of the broad-spectrum antibiot ics.…”

Section: Discussionmentioning

confidence: 96%

Ceftriaxone Therapy in Otolaryngological and Pulmonary Infections

Fraschini¹,

Braga²,

Falchi³

et al. 1986

Chemotherapy

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The efficacy of ceftriaxone, 1 g given intramuscularly once daily, was evaluated in 38 patients with pneumonia (n = 11), pulmonary empyema (n = 2), bronchitis (n = 4), tonsillitis (n = 9), sinusitis (n = 7), and otitis (n = 5). Causative organisms were Streptococcus pneumoniae (n = 11), viridans type streptococcus (n = 1), Haemophilus influenzae (n = 6), group A streptococcus (n = 10), Staphylococcus aureus (n = 3), Klebsiella pneumoniae (n = 2), Pseudomonas aeruginosa (n = 1), Escherichia coli (n = 2), Proteus mirabilis (n = 1), and Proteus vulgaris (n =1). Sterilization of infected foci was obtained in 89.4% of those treated, with clinical recovery in 86.8%. The ceftriaxone regimen was well tolerated.

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A pharmacokinetic and tolerance study of Ro13‐9904, a new cephalosporin antibiotic.

Cited by 21 publications

References 7 publications

Kinetic disposition of intravenous ceftriaxone in normal subjects and patients with renal failure on hemodialysis or peritoneal dialysis

Kinetic disposition of intravenous ceftriaxone in normal subjects and patients with renal failure on hemodialysis or peritoneal dialysis

Single-dose pharmacokinetics of ceftriaxone in healthy Chinese adults

Ceftriaxone Therapy in Otolaryngological and Pulmonary Infections

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