Pharmacokinetics and dosage adjustment of cefotiam in renal impaired patients

Rouan, Marie-Claude; Binswanger, U; Bammatter, F.; Theobald, W; Schoeller, JP; Guibert, J.

doi:10.1093/jac/13.6.611

Cited by 7 publications

(10 citation statements)

References 5 publications

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“…The 244 also showed a significant (r = 0.738, P < 0.001) corren 1.c,lation with BSA (Fig. 2, right (16). This dosage may be adjusted without changing the dosing interval for sumo wrestler patients as follows: daily dose = (2 or 4 g) x (BSA/1.7 m2) administered in two divided doses, where the m2 value of 1.7 indicates the average BSA in Japanese male adults (12).…”

Section: Methodsmentioning

confidence: 73%

“…Other likely reasons may include an increased renal blood flow secondary to the changes in blood volume and cardiac output due to the increase in body weight of obese subjects (2,13). Since about 50 to 70% of the cefotiam is excreted unchanged in urine (11,16,17), the larger CL of cefotiam found in the sumo wrestler group is probably attributable to enhanced renal function.…”

Section: Methodsmentioning

confidence: 95%

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Cefotiam disposition in markedly obese athlete patients, Japanese sumo wrestlers

Chiba

Tsuchiya

Katô

et al. 1989

Antimicrob Agents Chemother

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Markedly obese athletes like Japanese sumo wrestlers may frequently suffer various traumas which result in the prophylaxis or treatment of posttraumatic infection with antibiotics. However, appropriate dosage regimens in this group of patients have not been fully known for many antibiotics. Therefore, we studied the kinetic disposition of cefotiam, a parenteral, broad-spectrum cephalosporin with activity against gram-positive and -negative bacteria, after an intravenous dose (2 g) infused over 30 min into 15 sumo wrestler patients with an excess body weight (130 to 220% of ideal body weight) and 10 control patients with a normal weight (90 to 102% of ideal body weight). Mean (± standard deviation) clearance and steady-state volume of distribution were significantly greater in the sumo wrestler than in the control group (38.3 ± 9.4 versus 23.5 ± 6.0 liters/h, P < 0.001, and 30.2 ± 8.0 versus 17.9 ± 6.1 liters, P < 0.001). Mean elimination half-life was slightly but significantly longer in the sumo wrestler than in the control group (0.91 ± 0.14 versus 0.74 ± 0.20 h, P < 0.05). However, mean residence time did not differ between the two groups (0.79 ± 0.10 versus 0.75 ± 0.14 h). The statistical differences in clearance and volume of distribution between the two groups disappeared when these kinetic parameters were corrected for body surface area, but not for total body weight or ideal body weight. The results suggest that the dosage calculation of cefotiam, a hydrophilic antibiotic, should be made on the basis of body surface area in morbidly obese athlete or sumo wrestler patients. However, whether this recommendation should extend to other nonathlete obese subjects remains to be determined.Sumo, a unique form of wrestling with a 2,000-year-old history, is the national sport of Japan (5, 18). There are more than 700 professional sumo wrestlers in the country. The most prominent physical characteristic of sumo wrestlers is obesity (5, 18). Since physical essentials for success in sumo wrestling are heavy weight and low center of gravity, wrestlers desire to gain weight and ingest many calories so that they have a tendency to be markedly obese. The heaviest professional sumo wrestler in the major league weighs 241 kg with a height of 187 cm.

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Section: Methodsmentioning

confidence: 73%

Section: Methodsmentioning

confidence: 95%

Cefotiam disposition in markedly obese athlete patients, Japanese sumo wrestlers

Chiba

Tsuchiya

Katô

et al. 1989

Antimicrob Agents Chemother

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“…The pharmacokinetics of cefotiam have been reported to be dose dependent in normal volunteers after intravenous infusions (15 to 60 min) of doses ranging from 0.5 to 2 g (1). In patients with various degrees of renal impairment, a good correlation has been found between the renal clearance of cefotiam and the creatinine clearance (4). A dosage adjustment was proposed.…”

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confidence: 99%

Pharmacokinetics of cefotiam in humans

Rouan¹,

Lecaillon²,

Guibert³

et al. 1985

Antimicrob Agents Chemother

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After intravenous bolus injections of 0.5, 1, and 2 g of cefotiam to three healthy volunteers, the mean (± standard deviation) total plasma clearances measured for each dose were, respectively, 26.8 ± 2.7, 22.8 ± 0.8, and 17.8 ± 0.9 liters/h; the terminal elimination half-lives were 54.0 ± 0.1, 68 ± 15, and 98 ± 36 min; and the renal clearances were 16.0 ± 2.9, 13.3 ± 1.4, and 11.3 ± 2.6 liters/h. The 24-h urinary recovery was independent of the dose and averaged 53% of the dose. After intramuscular administration of 1 g of cefotiam to three healthy volunteers, a mean (± standard deviation) peak concentration of 16.6 ± 5.1 ,ug/ml was reached at 0.75 to 1 h post dosing. The concurrent intramuscular administration of lidocaine and cefotiam did not modify the kinetics of cefotiam. During a constant-rate infusion, the steady-state plasma clearance decreased slightly when the infusion rate was increased. There was no trend towards accumulation of cefotiam in plasma during chronic treatment with 1 g intravenously every 12 h for 10 days.Cefotiam (Halospor; Ciba-Geigy) is a new injectable cephalosporin with a broad spectrum of activity against grampositive and gram-negative bacteria (5, 6). The pharmacokinetics of cefotiam have been reported to be dose dependent in normal volunteers after intravenous infusions (15 to 60 min) of doses ranging from 0.5 to 2 g (1). In patients with various degrees of renal impairment, a good correlation has been found between the renal clearance of cefotiam and the creatinine clearance (4). A dosage adjustment was proposed.The present study was designed to determine the pharmacokinetic properties of'cefotiam in humans after single bolus administration by the intravenous and intramuscular routes. The effect of the dose was investigated in the range of 0.5 to 2 g after bolus intravenous administration. Since lidocaine may be added to cefotiam when it is given intramuscularly, the effect of its concurrent administration on the pharmacokinetics of cefotiam was examined. To measure eventual variation of the plasma clearance of cefotiam with the concentration of cefotiam in plasma, the steady-state plasma clearance was measured during two successive intravenous infusions at different rates. The pharmacokinetics were also investigated in patients given repeated doses intravenously. The following four treatment regimens were applied. (i) Regimen 1. Three healthy volunteers were given 0.5, 1, and 2 g of cefotiam intravenously in a Latin square design. These doses were dissolved in 3, 6, or 12 ml of sterile water and injected over 1 min. Intervals of 1 week separated administration of the three doses. Blood samples were collected before the injection and at 0, 2, 5, 10, 20, and 30, min and 1, 1.5, 2, 3, 4, 5, 6, and 8 h after injection. Urine was collected before administration and at 0 to 1, 1 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 10, and 10 to 24 h postinjection. MATERIALS AND METHODS(ii) Regimen 2. Three healthy volunteers received 1 g of cefotiam alone intravenously (10 ml) and 1 g of cefotiam intr...

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“…After intravenous administration of cefotiam 0.5, I and 2g, the 12-hour urinary excretion represents 50 to 70% of the administered dose, with 50% during the first 2 hours (Bryskier 1983;Daschner et al 1982;Fillastre et al 1982;FourtilIan et al 1982;Gerardin et al 1982;Rouan et al 1984). The renal clearance ranges from 10.2 to 12.3 L/h (Bryskier 1983;Fillastre et al 1982).…”

Section: Eliminationmentioning

confidence: 99%

“…The renal clearance ranges from 10.2 to 12.3 L/h (Bryskier 1983;Fillastre et al 1982). It is far lower than the body clearance, which is 19.8 to 21 L/h (Bryskier 1983;Rouan et al 1984).…”

Section: Eliminationmentioning

confidence: 99%

Clinical Pharmacokinetics of Cefotiam

Jehl²,

Willemin³

et al. 1989

Clinical Pharmacokinetics

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Cefotiam, a semisynthetic parenteral cephalosporin of the aminothiazole group, exhibits interesting properties: stability against hepatic metabolism and excellent solubility, accounting for an apparent volume of distribution 2 to 3 times higher than that of most other cephalosporins. Its degree of protein binding is about 40%. High concentrations of cefotiam are observed in several tissues (kidney, heart, ear, prostate and genital tract) as well as in fluids and secretions (bile, ascitic fluid). In healthy subjects, the serum elimination half-life is about 1 hour. The pharmacokinetics are linear only for doses lower than 1g. Cefotiam is mostly (and rapidly) eliminated in unchanged form in urine; 50 to 70% of the dose is recovered during the 12 hours following administration, and only severe renal failure, with creatinine clearance less than 5 ml/min, significantly alters the elimination half-life. Although the drug has no proven nephrotoxicity in man, a reduction of the dose is recommended when creatinine clearance is less than 30 ml/min.

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Pharmacokinetics and dosage adjustment of cefotiam in renal impaired patients

Cited by 7 publications

References 5 publications

Cefotiam disposition in markedly obese athlete patients, Japanese sumo wrestlers

Cefotiam disposition in markedly obese athlete patients, Japanese sumo wrestlers

Pharmacokinetics of cefotiam in humans

Clinical Pharmacokinetics of Cefotiam

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