Pharmacokinetics, pharmacodynamics, and safety of clevidipine after prolonged continuous infusion in subjects with mild to moderate essential hypertension.
In: European Journal of Clinical Pharmacology, Jg. 68 (2012-10-01), Heft 10, S. 1385-1394
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Zugriff:
Purpose: Clevidipine is a rapidly-acting intravenous dihydropyridine antihypertensive acting via calcium channel blockade. This was a randomized, single-blind, parallel-design study of a 72-h continuous clevidipine infusion. Method: Doses of 2, 4, 8, or 16.0 mg/h or placebo were evaluated in 61 subjects with mild to moderate essential hypertension. IV clevidipine or placebo was initiated at 2.0 mg/h and force-titrated in doubling increments every 3 min to target dose, then maintained for 72 h. Blood pressure and heart rate were measured during infusion, and for 4, 6 and 8 h after termination of infusion, although oral therapy could be restarted at 4 h. Clevidipine blood levels were obtained during infusion and for 1 hour after termination. Results: Rapid onset of drug effect occurred at all clevidipine dose levels, with consistent pharmacokinetics and rapid offset after 72-h infusion. No evidence of tolerance to the clevidipine drug effect was observed at any dose level over the 72-h infusion. No evidence of rebound hypertension was found for either 4 or 6 h after termination of the clevidipine infusion. At 8 h following cessation of clevidipine, blood pressure was not significantly higher than at baseline. Placebo-treated subjects had blood pressures lower than baseline at 8 h following infusion termination; hence, placebo-adjusted blood pressures tended to be slightly higher than baseline. Conclusion: This study supports the use of up to 72 h of IV clevidipine therapy for the management of blood pressure, with consistent pharmacokinetic/pharmacodynamic characteristics and context insensitive half-life across the dose ranges evaluated. [ABSTRACT FROM AUTHOR]
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Pharmacokinetics, pharmacodynamics, and safety of clevidipine after prolonged continuous infusion in subjects with mild to moderate essential hypertension.
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Autor/in / Beteiligte Person: | Smith, William ; Marbury, Thomas ; Komjathy, Steven ; Sumeray, Mark ; Williams, Gregory ; Hu, Ming-yi ; Mould, Diane |
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Zeitschrift: | European Journal of Clinical Pharmacology, Jg. 68 (2012-10-01), Heft 10, S. 1385-1394 |
Veröffentlichung: | 2012 |
Medientyp: | academicJournal |
ISSN: | 0031-6970 (print) |
DOI: | 10.1007/s00228-012-1260-3 |
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