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PHARMACOKINETICS

Pharmacokinetics, Safety, and Tolerability of Intramuscular Ziprasidone in Healthy Volunteers

Jeffrey J. Miceli, PhD, Keith D. Wilner, PhD, Suzanne K. Swan, MD and Thomas G. Tensfeldt, MS

From Pfizer Global Research and Development, Groton, Connecticut (Dr Miceli, Mr Tensfeldt); Pfizer Global Research and Development, La Jolla, California (Dr Wilner); and Hennepin County Medical Center and DaVita Clinical Research Unit, Minneapolis, Minnesota (Dr Swan).

Little has been published regarding the pharmacokinetics of the intramuscular (IM) formulation of Ziprasidone. The authors report results from 2 early phase I studies in healthy volunteers: a trial of single 5-, 10-, or 20-mg IM doses of ziprasidone in 24 subjects and an open-label 3-way crossover trial of 5-mg intravenous (IV), 5-mg IM, and 20-mg oral ziprasidone in 12 subjects. Absorption of IM ziprasidone was rapid (Tmax < 1 hour). The IM pharmacokinetic profile was consistent between studies and linear, with dose-related increases in exposure observed. The mean IM elimination t1/2 was short and approximately 2.5 hours. The mean bioavailability for the 5-mg IM ziprasidone dose was approximately 100%. Adverse events were generally mild to moderate, and no subjects were discontinued from the study. No significant effects on renal function or other laboratory values were noted. These results support the use of IM ziprasidone in treating acutely agitated patients with schizophrenia.


Key Words: Acute schizophreniaantipsychoticpharmacokineticssafetytolerabilityziprasidone

Address for reprints: Jeffrey J. Miceli, Pfizer Inc, Pfizer Global Research and Development, 50 Pequot Avenue, MS 6025-B2233, New London, CT 06320.


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