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Pharmacokinetic Evaluation and Safety Profile of a 15‐Minute Versus 30‐Second Infusion of Palonosetron in Healthy Subjects
Author(s) -
Shah Ajit,
DeGroot Timothy,
Apseloff Glen
Publication year - 2006
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270006291625
Subject(s) - palonosetron , pharmacokinetics , crossover study , medicine , volume of distribution , anesthesia , pharmacology , nausea , vomiting , chemotherapy induced nausea and vomiting , antiemetic , placebo , alternative medicine , pathology
Palonosetron is a potent, selective 5‐HT 3 receptor antagonist effective in the prevention of acute and delayed chemotherapy‐induced nausea and vomiting. In practice, 5‐HT 3 receptor antagonists, including palonosetron, are often coadministered with dexamethasone over approximately 15 minutes, although the approval of palonosetron was based on administration as a 30‐second infusion. This open‐label, randomized, 2‐way crossover trial compared the pharmacokinetics and safety of palonosetron 0.25 mg administered as a 15‐minute 50‐mL intravenous infusion with a 30‐second 5‐mL infusion. Aside from an anticipated 40% decrease in maximum plasma concentration after a 15‐minute infusion, the pharmacokinetics of palonosetron (including area under the plasma concentration‐time curve [AUC], plasma elimination half‐life, total body clearance, and apparent volume of distribution at steady state) were similar for both treatments. Both treatments were well tolerated, with no significant changes in vital signs or electrocardiograms. Palonosetron infused over 15 minutes is well tolerated, with an AUC 0‐∞ equivalent to a 30‐second infusion.