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Pharmacokinetics of vindesine bolus and infusion

  • Original Articles
  • Vindesine Pharmacokinetics
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Summary

The pharmacokinetics of vindesine were investigated during treatment of 15 patients with progressive malignancies refractory to conventional treatment. Patients were administered one of three IV dose schedules: 3.0 mg/m2 bolus injection, 1.2 mg/m2/day infusion for 5 days, or 2.0 mg/m2/day infusion for 2 days. Concentrations of the drug in the serum and urine were determined by radioimmunoassay. Serum concentrations were highest (5×10-7 M) in patients receiving a bolus injection, but fell to nondetectable levels by 48 h in four of five patients (terminal t1/2 15.0±9.4 h). Compared with bolus injection, 1.2-to 1.4-fold greater areas under the blood concentration curve were observed during infusions of 2.0 mg/m2 and 1.2 mg/m2. Whereas steady-state concentrations (∼1×10-8 M) were maintained throughout the infusion of 1.2 mg/m2/day progressively increasing serum levels were observed during the infusion of 2.0 mg/m2/day. Serum concentrations fell rapidly following discontinuation of the 2.0-mg/m2 infusion, but were somewhat more sustained in the 1.2-mg/m2 infusion group. The average urinary excretion was similar for each dose-schedule (8%–11% of the total dose). The pharmacokinetics of vindesine are influenced by variations in dose schedule.

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Authors and Affiliations

  1. Oncology Research Center, Bowman Gray School of Medicine of Wake Forest University, 27103, Winston-Salem, NC, USA

    Don V. Jackson Jr., V. Sagar Sethi, Tony R. Long, Hyman B. Muss & Charles L. Spurr

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  1. Don V. Jackson Jr.
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  2. V. Sagar Sethi
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  3. Tony R. Long
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  4. Hyman B. Muss
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  5. Charles L. Spurr
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Jackson, D.V., Sethi, V.S., Long, T.R. et al. Pharmacokinetics of vindesine bolus and infusion. Cancer Chemother. Pharmacol. 13, 114–119 (1984). https://doi.org/10.1007/BF00257126

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  • DOI: https://doi.org/10.1007/BF00257126

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