Pharmacokinetics of teicoplanin upon multiple dose intravenous administration to normal healthy male volunteers

Thompson, Gary A.; Smithers, Jacquelyn A.; Kenny, Michael T.; Dulworth, Jacqueline K.; Kulmala, Henrik K.; Yuh, Lianng; Lewis, Eric; Antony, Kelly K.

doi:10.1002/bdd.2510130307

Cited by 25 publications

(12 citation statements)

References 14 publications

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“…Results from previous studies conducted with normal healthy volunteers indicate that the pharmacokinetics of teicoplanin upon multiple-dose intravenous administration are linear over the range of 3 to 12 mg/kg (11,14,21). In the present study, the pharmacokinetics of teicoplanin upon Results of the present study indicate that teicoplanin total and renal clearances are independent of dose and that total clearance is determined primarily by renal clearance.…”

Section: Discussionsupporting

confidence: 54%

“…As a result of the decreased volume of distribution with no change in clearance, the terminal disposition half-life is decreased (9). As determined with MLTIDOSE (20) Results from multiple-dose studies with similar designs are summarized in Table 4 (11,14,21; also the present study). In the present study, the steady-state volumes of distribution appeared to be lower than those previously' observed.…”

Section: Discussionmentioning

confidence: 81%

“…As a result of the increase in the duration of sample collection, teicoplanin total clearance was found to be slightly less and the volumes of distribution and terminal disposition half-life were found to be greater than previously reported. Results from these more recent studies indicate that the pharmacokinetics of teicoplanin upon multiple-dose intravenous administration are linear over the range of 3 to 12 mg/kg of body weight (11,14,21 predominantly by renal clearance and that dosage adjustments may be necessary for patients with impaired renal function.As a result of a recent increase in the dose being used in clinical investigations, this study was undertaken to evaluate the pharmacokinetics of teicoplanin upon multiple-dose intravenous administration of 3, 12, and 30 mg/kg to healthy volunteers. …”

mentioning

confidence: 99%

“…A review of these studies has recently been published (16). In more recent studies, the duration of sample collection has been extended up to 3 weeks, resulting in a more complete characterization of the serum concentration-time profile (1,11,14,21). As a result of the increase in the duration of sample collection, teicoplanin total clearance was found to be slightly less and the volumes of distribution and terminal disposition half-life were found to be greater than previously reported.…”

mentioning

confidence: 99%

“…As a result of the increase in the duration of sample collection, teicoplanin total clearance was found to be slightly less and the volumes of distribution and terminal disposition half-life were found to be greater than previously reported. Results from these more recent studies indicate that the pharmacokinetics of teicoplanin upon multiple-dose intravenous administration are linear over the range of 3 to 12 mg/kg of body weight (11,14,21). Over this range of doses, teicoplanin pharmacokinetics are characterized by the following median parameters: total clearance of 13.1 ml/h/kg, renal clearance of 10.8 mlIh/kg, steady-state volume of distribution of 1.2 liters/kg, and a terminal disposition half-life of 157 h. These results indicate that total clearance is determined * Corresponding author.…”

mentioning

confidence: 99%

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Pharmacokinetics of teicoplanin upon multiple-dose intravenous administration of 3, 12, and 30 milligrams per kilogram of body weight to healthy male volunteers

Smithers¹,

Kulmala²,

Thompson³

et al. 1992

Antimicrob Agents Chemother

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Teicoplanin pharmacokinetics were evaluated after multiple-dose intravenous administration to healthy male volunteers by using a randomized, double-blind, parallel design. Doses of 3, 12, or 30 mg of teicoplanin per kg of body weight were administered every 24 h for 14 days as 60-min constant-rate intravenous infusions. Blood and urine samples were collected over 21 days and analyzed by a microbiological assay. Twenty-three subjects were included in the pharmacokinetic analysis. The median pharmacokinetic parameters upon multiple-dose intravenous administration of 3, 12, and 30 mg/kg included steady-state volumes of distribution of 0.94, 0.77, and 0.68 liter/kg; total clearances of 11.9, 12.0, and 13.2 ml/h/kg; and terminal disposition half-lives of 143, 166, and 96 h, respectively. Renal clearance accounted for approximately 95% of total clearance. No dose-related differences existed for teicoplanin total or renal clearance. The steady-state volume of distribution decreased significantly with increasing doses. As a result of the decrease in the volume of distribution, the terminal disposition half-life at 30 mg/kg was significantly decreased. However, the decreases in the volume of distribution and terminal disposition half-life are of limited clinical importance, since steady-state trough concentrations in serum increase in proportion to dose. Combined results of all multiple-dose studies with similar durations of sample collection indicate no dose-related differences for any pharmacokinetic parameters from 3 to 12 mg/kg. As observed in the present study, no dose-related differences exist for teicoplanin total and renal clearances from 3 to 30 mg/kg. However, at 30 mg/kg, a significant decrease in the steady-state volume of distribution is observed. As a consequence of the reduction in the volume of distribution at 30 mg/kg with no change in clearance, the terminal disposition half-life is decreased.Teicoplanin is a new glycopeptide antibiotic, chemically related to vancomycin and ristocetin. It is active against aerobic and anaerobic gram-positive bacteria (4,8,12,15). Its effect on susceptible bacteria is bactericidal, and like vancomycin, it interferes with cell wall synthesis (18).In earlier studies, the pharmacokinetics of teicoplanin were determined on the basis of plasma concentration-time profiles obtained over 3 to 4 days (22, 24). A review of these studies has recently been published (16). In more recent studies, the duration of sample collection has been extended up to 3 weeks, resulting in a more complete characterization of the serum concentration-time profile (1,11,14,21). As a result of the increase in the duration of sample collection, teicoplanin total clearance was found to be slightly less and the volumes of distribution and terminal disposition half-life were found to be greater than previously reported. Results from these more recent studies indicate that the pharmacokinetics of teicoplanin upon multiple-dose intravenous administration are linear over the range of 3 to 12 mg/kg of body wei...

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Section: Discussionsupporting

confidence: 54%

Section: Discussionmentioning

confidence: 81%

mentioning

confidence: 99%

mentioning

confidence: 99%

“…As a result of the increase in the duration of sample collection, teicoplanin total clearance was found to be slightly less and the volumes of distribution and terminal disposition half-life were found to be greater than previously reported. Results from these more recent studies indicate that the pharmacokinetics of teicoplanin upon multiple-dose intravenous administration are linear over the range of 3 to 12 mg/kg of body weight (11,14,21). Over this range of doses, teicoplanin pharmacokinetics are characterized by the following median parameters: total clearance of 13.1 ml/h/kg, renal clearance of 10.8 mlIh/kg, steady-state volume of distribution of 1.2 liters/kg, and a terminal disposition half-life of 157 h. These results indicate that total clearance is determined * Corresponding author.…”

mentioning

confidence: 99%

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Pharmacokinetics of teicoplanin upon multiple-dose intravenous administration of 3, 12, and 30 milligrams per kilogram of body weight to healthy male volunteers

Smithers¹,

Kulmala²,

Thompson³

et al. 1992

Antimicrob Agents Chemother

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Antibiotics: Natural products essential to human health

Demain

2009

Medicinal Research Reviews

164

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For more than 50 years, natural products have served us well in combating infectious bacteria and fungi. Microbial and plant secondary metabolites helped to double our life span during the 20th century, reduced pain and suffering, and revolutionized medicine. Most antibiotics are either (i) natural products of microorganisms, (ii) semi-synthetically produced from natural products, or (iii) chemically synthesized based on the structure of the natural products. Production of antibiotics began with penicillin in the late 1940s and proceeded with great success until the 1970-1980s when it became harder and harder to discover new and useful products. Furthermore, resistance development in pathogens became a major problem, which is still with us today. In addition, new pathogens are continually emerging and there are still bacteria that are not eliminated by any antibiotic, e.g., Pseudomonas aeruginosa. In addition to these problems, many of the major pharmaceutical companies have abandoned the antibiotic field, leaving much of the discovery efforts to small companies, new companies, and the biotechnology industries. Despite these problems, development of new antibiotics has continued, albeit at a much lower pace than in the last century. We have seen the (i) appearance of newly discovered antibiotics (e.g., candins), (ii) development of old but unutilized antibiotics (e.g., daptomycin), (iii) production of new semi-synthetic versions of old antibiotics (e.g., glycylcyclines, streptogrammins), as well as the (iv) very useful application of old but underutilized antibiotics (e.g., teicoplanin).

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Glycopeptides

Gyssens

2013

Fundamentals of Antimicrobial Pharmacokinetics and Pharmacodynamics

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Glycopeptides are a class of antibiotic drugs that is composed of glycosylated cyclic or polycyclic nonribosomal peptides. Older molecules used in clinical practice are vancomycin and teicoplanin. Oritavancin, dalbavancin, and telavancin belong to the subclass of lipoglycopeptides. Glycopeptides inhibit bacterial cell wall peptoglycan synthesis of aerobic and anaerobic Gram-positive bacteria. Glyco (lipo)peptides are not absorbed orally and have to be administered intravenously. In this chapter, the pharmacokinetics (Pk) and the pharmacodynamics (Pd) of the glycopeptides are studied. Pk in serum as well as protein binding and elimination are reviewed. Pharmacodynamic data include MICs of Gram-positive bacteria, PK/Pd effects in in vitro systems, animal models and human studies. Adverse effects of glycopeptides on the host are concentration related nephro-and ototoxicity. In the past, because of fear of toxicity, the older glycopeptides have been underdosed in many settings. The implementation of Pk/Pd knowledge into clinical practice by e.g. administering higher doses of vancomycin and teicoplanin and using continuous infusion of vancomycin is urgently needed. This chapter contains clinical vignettes showing the benefi t of Therapeutic Drug Monitoring of glycopeptides.

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Pharmacokinetics of teicoplanin upon multiple dose intravenous administration to normal healthy male volunteers

Cited by 25 publications

References 14 publications

Pharmacokinetics of teicoplanin upon multiple-dose intravenous administration of 3, 12, and 30 milligrams per kilogram of body weight to healthy male volunteers

Pharmacokinetics of teicoplanin upon multiple-dose intravenous administration of 3, 12, and 30 milligrams per kilogram of body weight to healthy male volunteers

Antibiotics: Natural products essential to human health

Glycopeptides

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