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Pharmacokinetics of Nisoldipine

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The pharmacokinetic behaviour of nisoldipine was examined in several studies with intravenous and oral application. Nisoldipine was analyzed from plasma by gas chromatography with ECD and MS detection down to concentrations of 25 pg/ml. Nisoldipine is eliminated from plasma according to a three-compartment model with half-lives of 4 min, 1.7 h and 10.7 h. Vss is ~ 3 liter/kg, the clearance is 544–768 ml/h−1 kg−1; 99.7% of nisoldipine is bound to plasma proteins. After oral dosing nisoldipine is absorbed rapidly from the gastrointestinal tract; Cmax values (after 20 mg tablets) are in the range of 3.5–5.5 ng/ml. It has linear pharmacokinetics measured as doseproportionality from 5 to 20 mg with normalized AUC values of 33–63 (× 10−3 h kg liter−1). Despite its low bioavailability, the intra-individual changes in AUC after repeated drug intake are only 36%. No special recommendations for drug intake related to meals are necessary.


  • Intraindividual Change
  • Height Comparison
  • Isobutyl Methyl
  • Tablet Intake
  • High Clearance Drug

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© 1987 Springer-Verlag Berlin Heidelberg

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Ahr, G., Wingender, W., Kuhlmann, J. (1987). Pharmacokinetics of Nisoldipine. In: Hugenholtz, P.G., Meyer, J. (eds) Nisoldipine 1987. Springer, Berlin, Heidelberg.

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  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-540-18394-5

  • Online ISBN: 978-3-642-73010-8

  • eBook Packages: Springer Book Archive