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Ziprasidone: the fifth atypical antipsychotic
Charles F Caley1, Chandra K Cooper
1School of Pharmacy, University of Connecticut, Storrs, CT, USA. ccaley4@netscape.net
The Annals of Pharmacotherapy
|April 30, 2002
Summary
Ziprasidone is an effective atypical antipsychotic for acute schizophrenia management. However, potential cardiac risks suggest second-line use in patients with cardiovascular issues.
Area of Science:
- Pharmacology and Psychiatry
- Neuroscience
Background:
- Schizophrenia requires effective and safe treatment options.
- Atypical antipsychotics offer improved efficacy and tolerability over older agents.
- Ziprasidone is an atypical antipsychotic with a unique pharmacological profile.
Purpose of the Study:
- To review the pharmacology, pharmacokinetics, clinical efficacy, and adverse effects of ziprasidone.
- To evaluate ziprasidone's role in the acute management of schizophrenia.
Main Methods:
- Comprehensive literature search of MEDLINE and other sources (July 2000-October 2001).
- Inclusion of all available published data on ziprasidone's characteristics.
- Evaluation of clinical investigations for design, sample size, and outcomes.
Main Results:
- Ziprasidone exhibits a 5-HT(2A)/D(2) receptor profile, with 5-HT(1A) agonism and weak serotonin/norepinephrine reuptake inhibition.
- Oral bioavailability is ~60% with food; half-life is 6-7 hours; protein binding is >99%.
- Efficacious in acute schizophrenia exacerbations at 120-160 mg/d; common adverse effects include headache, nausea, somnolence; rare QTc prolongation.
Conclusions:
- Ziprasidone is safe and effective for acute schizophrenia management.
- Efficacy and safety support first-line use, but QTc prolongation potential suggests second-line status for patients with cardiovascular risks.